발생일자 2015.09.15 

사건번호 1:15-cv-00822 

법원국가 UNITED STATES OF AMERICA 

관할법원명 D.C.Delaware(지방법원) 

침해권리 특허 

원고명 Otsuka Pharmaceutical Co. Ltd. ( 일본 / 외국기업 )  

피고명 Hetero USA, Inc./ Hetero Labs Ltd./ Hetero Labs Ltd. Unit V ( 미국 / 외국기업 )  

소송유형 침해금지 

[Otsuka Pharmaceutical Co. Ltd. v. Hetero USA, Inc. et al] 사건번호 1:15-cv-00822에 따르면 원고 Otsuka Pharmaceutical Co. Ltd.는 피고 Hetero USA, Inc./ Hetero Labs Ltd./ Hetero Labs Ltd. Unit V을(를) 상대로 특허 US5753677을(를) 침해하였다는 이유로 미국 델라웨어 지방법원에 소를 제기하였다. 

분쟁결과 분쟁중 

산업분류 화학∙바이오 > 의약품 

계쟁제품 Generic tolvaptan tablets SAMSCA® 15 and 30 mg dosage forms 

지재권번호/명칭

US5753677   Benzoheterocyclic compounds 

Novel benzoheterocyclic compounds of the formula: ##STR1## which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient. 

1. A method for antagonizing vasopressin which comprises administering to a subject a therapeutically effective amount of a benzoheterocyclic compound of the formula: ##STR3330## wherein R.sup.1 is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.6 alkyl, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkoxy, 

R.sup.2 is a hydrogen atom, a halogen atom, a C.sub.1 -C.sub.6 alkoxy, a phenyl-(C.sub.1 -C.sub.6) alkoxy, hydroxy, a C.sub.1 -C.sub.6 alkyl, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a carbamoyl-substituted C.sub.1 -C.sub.6 alkoxy, an amino-substituted C.sub.1 -C.sub.6 alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a benzoyloxy which has optionally a halogen substituent on the phenyl ring, 

R.sup.3 is a group of the formula: ##STR3331## or a group of the formula: ##STR3332## R.sup.4 is a hydrogen atom, a benzoyl which has optionally a halogen substituent on the phenyl ring or a C.sub.1 -C.sub.6 alkyl, 

R.sup.5 is a group of the formula: ##STR3333## wherein R.sup.16 is a halogen atom; a C.sub.1 -C.sub.6 alkyl which has optionally a substituent selected from a halogen atom and hydroxy; hydroxy; a C.sub.1 -C.sub.6 alkoxy; a C.sub.1 -C.sub.6 alkanoyloxy; a C.sub.1 -C.sub.6 alkylthio; a C.sub.1 -C.sub.6 alkanoyl; carboxy; a C.sub.1 -C.sub.6 alkoxycarbonyl; cyano; nitro; an amino which has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl; phenyl; a C.sub.3 -C.sub.8 cycloalkyl; a C.sub.2 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkoxy; a carboxy-substituted C.sub.1 -C.sub.6 alkoxy; a halogen-substituted C.sub.1 -C.sub.6 alkoxy; a carbamoyl-substituted C.sub.1 -C.sub.6 alkoxy; a hydroxy-substituted C.sub.1 -C.sub.6 alkoxy; a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkoxy; a phthalimido-substituted C.sub.1 -C.sub.6 alkoxy; an aminocarbonyl-(C.sub.1 -C.sub.6) alkoxy having a C.sub.1 -C.sub.6 alkyl substituent; or a group of the formula: ##STR3334## wherein A is a C.sub.1 -C.sub.6 alkylene, and R.sup.6 and R.sup.7 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.1 -C.sub.6 alkanoyl, or benzoyl, or R.sup.6 and R.sup.7 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from piperidinyl and a C.sub.1 -C.sub.6 alkyl; and m is an integer of 0 to 3, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3335## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3336## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl, 

R.sup.11 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, 

R.sup.12 is a C.sub.3 -C.sub.8 cycloalkyl, or a phenyl which has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkoxy, a C.sub.1 -C.sub.6 alkyl and a halogen atom, 

W is a group of the formula: --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5, or a group of the formula: --CH.dbd.CH--(CH.sub.2).sub.q -- wherein q is an integer of 1 to 3, and further said --(CH.sub.2).sub.p -- group and said --CH.dbd.CH--(CH.sub.2).sub.q -- group having optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.1 -C.sub.6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C.sub.1 -C.sub.6 alkanoyloxy having optionally a halogen substituent, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkylsulfonyloxy-(C.sub.1 -C.sub.6) alkyl, an azido-(C.sub.1 -C.sub.6) alkyl, a group of the formula: ##STR3337## an aminocarbonyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a C.sub.1 -C.sub.6 alkoxy, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkoxy, a carboxy-substituted C.sub.1 -C.sub.6 alkoxy, an aminocarbonyl-(C.sub.1 -C.sub.6) alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, an amino-(C.sub.1 -C.sub.6) alkoxy having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a phthalimido-substituted C.sub.1 -C.sub.6 alkoxy, hydroxy-imino, a C.sub.1 -C.sub.6 alkanoyloxy-imino, a C.sub.1 -C.sub.6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3338## wherein R.sup.81 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, hydrazino, pyrrolyl, an amino-(C.sub.2 -C.sub.6) alkanoyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a group of the formula: ##STR3339## wherein A is as defined above in this claim, and R.sup.82 and R.sup.83 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a hydroxy-substituted C.sub.1 -C.sub.6 alkyl, or a pyridyl-(C.sub.1 -C.sub.6) alkyl, or R.sup.82 and R.sup.83 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen, oxygen or sulfur atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and thiomorpholino, and has optionally a substituent selected from oxo, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3340## wherein n is as defined above in this claim, and R.sup.14 and R.sup.15 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl, an oxiranyl-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkyl having 1 to 2 substituents selected from a C.sub.1 -C.sub.6 alkoxy, hydroxy and an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a phenyl-(C.sub.1 -C.sub.6) alkyl, a pyridyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkylsulfonyl, benzoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, a cyano-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a carboxy-substituted C.sub.1 -C.sub.6 alkyl, a tetrahydropyranyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a piperidinyl having optionally a phenyl-(C.sub.1 -C.sub.6) alkyl substituent on the piperidine ring, a halogen substituted C.sub.1 -C.sub.6 alkanoyl, an imidazolyl-substituted C.sub.2 -C.sub.6 alkanoyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkoxycarbonyl, an aminocarbonyl-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, or R.sup.14 or R.sup.15 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or oxygen atom, wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, and morpholino, and may optionally have a substituent selected from a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl or a C.sub.1 -C.sub.6 alkanoyl, and a pharmaceutically acceptable salt thereof. 

2. The method according to claim 1, wherein R.sup.1 is a hydrogen atom. 

3. The method according to claim 1, wherein R.sup.1 is a halogen atom. 

4. The method according to claim 1, wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkoxy. 

5. The method according to claim 2, wherein R.sup.2 is a hydrogen atom. 

6. The method according to claim 2, wherein R.sup.2 is a halogen atom, a C.sub.1 -C.sub.6 alkoxy, or a C.sub.1 -C.sub.6 alkyl. 

7. The method according to claim 2, wherein R.sup.2 is a phenyl-(C.sub.1 -C.sub.6) alkoxy, hydroxy, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a carbamoyl-substituted C.sub.1 -C.sub.6 alkoxy, an amino-substituted C.sub.1 -C.sub.6 alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 

8. The method according to claim 3, wherein R.sup.2 is a hydrogen atom. 

9. The method according to claim 3, wherein R.sup.2 is a halogen atom, a C.sub.1 -C.sub.6 alkoxy, or a C.sub.1 -C.sub.6 alkyl. 

10. The method according to claim 3, wherein R.sup.2 is a phenyl-(C.sub.1 -C.sub.6) alkoxy, hydroxy, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a carbamoyl-substituted C.sub.1 -C.sub.6 alkoxy, an amino-substituted C.sub.1 -C.sub.6 alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 

11. The method according to claim 4, wherein R.sup.2 is a hydrogen atom. 

12. The method according to claim 4, wherein R.sup.2 is a halogen atom, a C.sub.1 -C.sub.6 alkoxy, or a C.sub.1 -C.sub.6 alkyl. 

13. The method according to claim 4, wherein R.sup.2 is a phenyl-(C.sub.1 -C.sub.6) alkoxy, hydroxy, an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a carbamoyl-substituted C.sub.1 -C.sub.6 alkoxy, an amino-substituted C.sub.1 -C.sub.6 alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 

14. The method according to claim 5, wherein R.sup.3 is a group of the formula: ##STR3341## wherein R.sup.4 and R.sup.5 are as defined in claim 1. 

15. The method according to claim 5, wherein R.sup.3 is a group of the formula: ##STR3342## wherein R.sup.11 and R.sup.12 are as defined in claim 1. 

16. The method according to claim 6, wherein R.sup.3 is a group of the formula: ##STR3343## wherein R.sup.4 and R.sup.5 are as defined in claim 1. 

17. The method according to claim 6, wherein R.sup.3 is a group of the formula: ##STR3344## wherein R.sup.11 and R.sup.12 are as defined in claim 1. 

18. The method according to claim 8, wherein R.sup.3 is a group of the formula: ##STR3345## wherein R.sup.4 and R.sup.5 are as defined in claim 1. 

19. The method according to claim 8, wherein R.sup.3 is a group of the formula: ##STR3346## wherein R.sup.11 and R.sup.12 are as defined in claim 1. 

20. The method according to claim 9, wherein R.sup.3 is a group of the formula: ##STR3347## wherein R.sup.4 and R.sup.5 are as defined in claim 1. 

21. The method according to claim 9, wherein R.sup.3 is a group of the formula: ##STR3348## wherein R.sup.11 and R.sup.12 are as defined in claim 1. 

22. The method according to claim 14, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3349## and R.sup.16 and m are as defined in claim 1. 

23. The method according to claim 14, wherein R.sup.4 is a hydrogen atom and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3350## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6)alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3351## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

24. The method according to claim 14, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

25. The method according to claim 16, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3352## wherein R.sup.16 and m are as defined in claim 1. 

26. The method according to claim 16, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3353## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3354## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

27. The method according to claim 16, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

28. The method according to claim 7, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3355## wherein R.sup.16 and m are as defined in claim 1. 

29. The method according to claim 7, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3356## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3357## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

30. The method according to claim 7, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

31. The method according to claim 18, wherein R.sup.4 is a hydrogen atom, R.sup.5 is a group of the formula: ##STR3358## wherein R.sup.16 and m are as defined in claim 1. 

32. The method according to claim 18, wherein R.sup.4 is hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted (C.sub.1 -C.sub.6) alkanoyl, a group of the formula: ##STR3359## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl), an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3360## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

33. The method according to claim 18, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

34. The method according to claim 20, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3361## wherein R.sup.16 and m are as defined in claim 1. 

35. The method according to claim 20, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3362## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.1 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3363## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 C.sub.6 alkoxycarbonyl and piperidinyl. 

36. The method according to claim 20, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

37. The method according to claim 10, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3364## wherein R.sup.16 and m are as defined in claim 1. 

38. The method according to claim 10, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3365## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3366## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

39. The method according to claim 10, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

40. The method according to claim 11, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3367## wherein R.sup.16 and m are as defined in claim 1. 

41. The method according to claim 11, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3368## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3369## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.2 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

42. The method according to claim 12, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

43. The method according to claim 12, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3370## wherein R.sup.16 and m are as defined in claim 1. 

44. The method according to claim 12, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl,naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3371## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3372## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

45. The method according to claim 12, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

46. The method according to claim 13, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a group of the formula: ##STR3373## wherein R.sup.16 and m are as defined in claim 1. 

47. The method according to claim 13, wherein R.sup.4 is a hydrogen atom, and R.sup.5 is a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a C.sub.1 -C.sub.6 alkanoyl, a phenyl(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl-(C.sub.2 -C.sub.6) alkanoyl, a C.sub.3 -C.sub.8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C.sub.2 -C.sub.6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and an amino having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a phthalimido-substituted C.sub.2 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-(C.sub.2 -C.sub.6) alkanoyl, a carboxy-(C.sub.2 -C.sub.6) alkanoyl, a naphthyloxy-(C.sub.2 -C.sub.6) alkanoyl, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, a group of the formula: ##STR3374## wherein R.sup.8 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, a carbamoyl-(C.sub.1 -C.sub.6) alkyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a C.sub.1 -C.sub.6 alkanoyl, an anilinocarbonyl which has optionally a C.sub.1 -C.sub.6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C.sub.1 -C.sub.6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3375## wherein B is a C.sub.1 -C.sub.6 alkylene, n is an integer of 0 or 1, and R.sup.9 and R.sup.10 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.3 -C.sub.8 cycloalkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.2 -C.sub.6 alkenyl, a phenoxy-(C.sub.1 -C.sub.6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy and a halogen atom, a phthalimido-substituted C.sub.1 -C.sub.6 alkyl, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkanoyl substituent, a C.sub.2 -C.sub.6 alkynyl, or an amino-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or R.sup.9 and R.sup.10 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or an oxygen atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl and morpholino, and has optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl and piperidinyl. 

48. The method according to claim 13, wherein R.sup.4 is a C.sub.1 -C.sub.6 alkyl. 

49. The method according to claim 22, wherein R.sup.16 is a halogen atom, or a C.sub.1 -C.sub.6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 

50. The method according to claim 25, wherein R.sup.16 is a halogen atom, or a C.sub.1 -C.sub.6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 

51. The method according to claim 31, wherein R.sup.16 is a halogen atom, or a C.sub.1 -C.sub.6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 

52. The method according to claim 34, wherein R.sup.16 is a halogen atom, or a C.sub.1 -C.sub.6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 

53. The method according to claim 1, wherein W is a group of the formula: --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5, and further said --(CH.sub.2).sub.p -- group has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.1 -C.sub.6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C.sub.1 -C.sub.6 alkanoyloxy having optionally a halogen substituent, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkylsulfonyloxy-(C.sub.1 -C.sub.6) alkyl, an azido-(C.sub.1 -C.sub.6) alkyl, a group of the formula: ##STR3376## an aminocarbonyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a C.sub.1 -C.sub.6 alkoxy, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkoxy, a carboxy-substituted C-C.sub.6 alkoxy, an amino-carbonyl-(C.sub.1 -C.sub.6) alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, an amino-(C.sub.1 -C.sub.6) alkoxy having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a phthalimido-substituted C.sub.1 -C.sub.6 alkoxy, hydroxyimino, a C.sub.1 -C.sub.6 alkanoyloxy-imino, a C.sub.1 -C.sub.6 alkylidene, a halogen atom, azido, sulfoxy-imino, a group of the formula: ##STR3377## wherein R.sup.81 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, hydrazino, pyrrolyl, an amino-(C.sub.2 -C.sub.6) alkanoyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a group of the formula: ##STR3378## wherein A is as defined above, and R.sup.82 and R.sub.83 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a hydroxy-substituted C.sub.1 -C.sub.6 alkyl, or a pyridyl-(C.sub.1 -C.sub.6) alkyl, or R.sup.82 and R.sup.83 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen, oxygen or sulfur atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and thiomorpholino, and has optionally a substituent selected from oxo, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3379## wherein n is as defined above, and R.sup.14 and R.sup.15 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl, an oxiranyl-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkyl having 1 to 2 substituents selected from a C.sub.1 -C.sub.6 alkoxy, hydroxy and an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a phenyl-(C.sub.1 -C.sub.6) alkyl, a pyridyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkylsulfonyl, benzoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, a cyano-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a carboxy-substituted C.sub.1 -C.sub.6 alkyl, a tetrahydropyranyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a piperidinyl having optionally a phenyl-(C.sub.1 -C.sub.6) alkyl substituent on the piperidine ring, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, an imidazolyl-substituted C.sub.2 -C.sub.6 alkanoyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkoxycarbonyl, an aminocarbonyl-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, or R.sup.14 or R.sup.15 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or oxygen atom, wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, and morpholino, and may optionally have a substituent selected from a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl or a C.sub.1 -C.sub.6 alkanoyl. 

54. The method according to claim 1, wherein W is a group of the formula: --CH.dbd.CH--(CH.sub.2).sub.q -- wherein q is an integer of 1 to 3, and further said --CH.dbd.CH--(CH.sub.2).sub.q -- group has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.1 -C.sub.6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C.sub.1 -C.sub.6 alkanoyloxy having optionally a halogen substituent, an amino-(C.sub.1 -C.sub.6) alkyl having optionally substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkylsulfonyloxy -(C.sub.1 -C.sub.6) alkyl, an azido --(C.sub.1 -C.sub.6) alkyl, a group of the formula: ##STR3380## an aminocarbonyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a C.sub.1 -C.sub.6 alkoxy, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkoxy, a carboxy-substituted C.sub.1 -C.sub.6 alkoxy, an aminocarbonyl-(C.sub.1 -C.sub.6) alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, an amino-(C.sub.1 -C.sub.6) alkoxy having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a phthalimido-substituted C.sub.1 -C.sub.6 alkoxy, hydroxyimino, a C.sub.1 -C.sub.6 alkanoyloxy-imino, a C.sub.1 -C.sub.6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3381## wherein R.sup.18 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, hydrazino, pyrrolyl, an amino-(C.sub.2 -C.sub.6) alkanoyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a group of the formula: ##STR3382## wherein A is as defined above, and R.sup.82 and R.sup.83 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a hydroxy-substituted C.sub.1 -C.sub.6 alkyl, or a pyridyl-(C.sub.1 -C.sub.6) alkyl, or R.sup.82 and R.sup.83 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen, oxygen or sulfur atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and thiomorpholino, and has optionally a substituent selected from oxo, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3383## wherein n is as defined above, and R.sup.14 and R.sup.15 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl, an oxiranyl-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkyl having 1 to 2 substituents selected from a C.sub.1 -C.sub.6 alkoxy, hydroxy and an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a phenyl-(C.sub.1 -C.sub.6) alkyl, a pyridyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkylsulfonyl, benzoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, a cyano-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a carboxy-substituted C.sub.1 -C.sub.6 alkyl, a tetrahydropyranyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a piperidinyl having optionally a phenyl-(C.sub.1 -C.sub.6) alkyl substituent on the piperidine ring, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, an imidazolyl-substituted C.sub.2 -C.sub.6 alkanoyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkoxycarbonyl, an aminocarbonyl-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, or R.sup.14 or R.sup.15 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen atom or an oxygen atom, wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, and morpholino, and may optionally have a substituent selected from a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl or a C.sub.1 -C.sub.6 alkanoyl. 

55. The method according to claim 53, wherein W is a group of the formula: --(CH.sub.2).sub.p -- wherein p is an integer of 3 to 5, and said --(CH.sub.2).sub.p -- group has optionally 1 to 3 substituents selected from a C.sub.1 -C.sub.6 alkyl having optionally a hydroxy substituent, a C.sub.1 -C.sub.6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C.sub.1 -C.sub.6 alkanoyloxy having optionally a halogen substituent, an amino-(C.sub.1 -C.sub.6) alkyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkylsulfonyloxy-(C.sub.1 -C.sub.6) alkyl, an azido -(C.sub.1 -C.sub.6) alkyl, a group of the formula: ##STR3384## an aminocarbonyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a C.sub.1 -C.sub.6 alkoxy, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkoxy, a carboxy-substituted C.sub.1 -C.sub.6 alkoxy, an aminocarbonyl-(C.sub.1 -C.sub.6) alkoxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, an amino-(C.sub.1 -C.sub.6) alkoxy having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkanoyl, a phthalimido-substituted C.sub.1 -C.sub.6 alkoxy, hydroxyimino, a C.sub.1 -C.sub.6 alkanoyloxyimino, a C.sub.1 -C.sub.6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3385## wherein R.sup.81 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, hydrazino, pyrrolyl, an amino-(C.sub.2 -C.sub.6) alkanoyloxy having optionally a C.sub.1 -C.sub.6 alkyl substituent, a group of the formula: ##STR3386## wherein A is as defined above, and R.sup.82 and R.sup.83 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a hydroxy-substituted C.sub.1 -C.sub.6 alkyl, or a pyridyl-(C.sub.1 -C.sub.6) alkyl, or R.sup.82 and R.sup.83 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen, oxygen or sulfur atom wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholino, and thiomorpholino, and has optionally a substituent selected from oxo, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3387## wherein n is as defined above, and R.sup.14 and R.sup.15 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.1 -C.sub.6 alkanoyl, a C.sub.3 -C.sub.8 cycloalkyl, an oxiranyl-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkyl having 1 to 2 substituents selected from a C.sub.1 -C.sub.6 alkoxy, hydroxy and an amino having optionally a C.sub.1 -C.sub.6 alkyl substituent, a phenyl-(C.sub.1 -C.sub.6) alkyl, a pyridyl-(C.sub.1 -C.sub.6) alkyl, a C.sub.1 -C.sub.6 alkylsulfonyl, benzoyl, a C.sub.1 -C.sub.6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, a cyano-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxycarbonyl-substituted C.sub.1 -C.sub.6 alkyl, a carbamoyl-substituted C.sub.1 -C.sub.6 alkyl, a carboxy-substituted C.sub.1 -C.sub.6 alkyl, a tetrahydropyranyloxy-substituted C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkanoyloxy-substituted C.sub.1 -C.sub.6 alkyl, a piperidinyl having optionally a phenyl-(C.sub.1 -C.sub.6) alkyl substituent on the piperidine ring, a halogen-substituted C.sub.1 -C.sub.6 alkanoyl, an imidazolyl-substituted C.sub.2 -C.sub.6 alkanoyl, an amino-(C.sub.2 -C.sub.6) alkanoyl having optionally a substituent selected from a C.sub.1 -C.sub.6 alkyl and a C.sub.1 -C.sub.6 alkoxycarbonyl, an aminocarbonyl-(C.sub.1 -C.sub.6) alkyl having optionally a C.sub.1 -C.sub.6 alkyl substituent, or a phenyl-(C.sub.1 -C.sub.6) alkoxycarbonyl, or R.sup.14 or R.sup.15 may bind together with the nitrogen atom to which they are bonded to form a 5- or 6-membered saturated heterocyclic group with or without being intervened with a nitrogen or oxygen atom, wherein the heterocyclic group is one member selected from the group consisting of pyrrolidinyl, piperidinyl, piperazinyl, and morpholino, and may optionally have a substituent selected from a C.sub.1 -C.sub.6 alkyl, a phenyl-(C.sub.1 -C.sub.6) alkyl or a C.sub.1 -C.sub.6 alkanoyl. 

56. The method according to claim 55, wherein p in the group of the formula: --(CH.sub.2).sub.p -- is 3 and the group has no substituent. 

57. The method according to claim 55, wherein p in the group of the formula: --(CH.sub.2).sub.p -- is 3 and the group has a substituent of group of the formula: ##STR3388## 

58. The method according to claim 55, wherein p in the group of the formula: --(CH.sub.2).sub.p -- is 4 and the group has no substituent. 

59. The method according to claim 55, wherein p in the group of the formula: --(CH.sub.2).sub.p -- is 4 and the group has a substituent of a group of the formula: ##STR3389## wherein R.sup.14 and R.sup.15 and n are as defined in claim 55. 

60. The method according to claim 55, wherein p in the group of the formula: --(CH.sub.2).sub.p -- is 5. 

61. The method according to claim 54, wherein q in the group of the formula: --CH.dbd.CH--(CH.sub.2).sub.q -- is 1. 

62. The method according to claim 54, wherein q in the group of the formula: --CH.dbd.CH--(CH.sub.2).sub.q -- is 2. 

63. The method according to claim 54, wherein q in the group of the formula: --CH.dbd.CH--(CH.sub.2).sub.q -- is 3. 

64. The method according to claim 57 or 59, wherein n in the group of the formula: ##STR3390## is 0, and R.sup.14 and R.sup.15 are the same or different and are each a hydrogen atom, a C.sub.1 -C.sub.6 alkyl, or a C.sub.3 -C.sub.8 cycloalkyl. 

65. The method according to claim 62, wherein the heterocyclic group of the formula: ##STR3391## is 2,3,-dihydro-1 H-benzazepine. 

66. The method according to claim 1, wherein the benzoheterocyclic compound is 5-dimethylamino-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahydro-1H- benzazepine. 

67. The method according to claim 1, wherein the benzoheterocyclic compound is 5-dimethylamino-1-[2-chloro-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetra hydro-1H-benzazepine. 

68. The method according to claim 1, wherein the benzoheterocyclic compound is 5-methylamino-1-[2-chloro-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahy dro-1H-benzazepine. 

69. The method according to claim 1, wherein the benzoheterocyclic compound is 5-cyclopropylamino-1-[2-chloro-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-te trahydro-1H-benzazepine. 

70. The method according to claim 1, wherein the benzoheterocyclic compound is 5-cyclopropylamino-1-[2-chloro-4-(2-chlorobenzoylamino)benzoyl]-2,3,4,5-te trahydro-1H-benzazepine. 

71. The method according to claim 1, wherein the benzoheterocyclic compound is 5-dimethylamino-1-[2-methyl-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetra hydro-1H-benzazepine. 

72. The method according to claim 1, wherein the benzoheterocyclic compound is 4-dimethylamino-1-[3-methoxy-4-(2-methylbenzoylamino)benzoyl]-1,2,3,4-tetr ahydroquinoline. 

73. The method according to claim 1, wherein the benzoheterocyclic compound is 7-chloro-5-methylamino-1-[4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-tetrahy dro-1H-benzazepine. 

74. The method according to claim 1, wherein the benzoheterocyclic compound is 7-chloro-5-methylamino-1-[4-(2-chlorobenzoylamino)benzoyl]-2,3,4,5-tetrahy dro-1H-benzazepine. 

75. The method according to claim 1, wherein the benzoheterocyclic compound is 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)-benzoyl]-2,3,4,5-t etrahydro-1H-benzazepine. 

76. The method according to claim 1, wherein the benzoheterocyclic compound is 7-chloro-5-hydroxy-1-[2-methoxy-4-(2-methylbenzoylamino)-benzoyl]-2,3,4,5- tetrahydro-1H-benzazepine. 

77. The method according to claim 1, wherein the benzoheterocyclic compound is 7-fluoro-5-hydroxy-1-[2-chloro-4-(2-methylbenzoylamino)benzoyl]-2,3,4,5-te trahydro-1H-benzazepine. 

78. The method according to claim 1, wherein the benzoheterocyclic compound is 7-fluoro-5-hydroxymethyl-5-hydroxy-1-[2-chloro-4-(2-methylbenzoylamino)ben zoyl]-2,3,4,5-tetrahydro-1H-benzazepine.