Claims for Patent: 5,753,677

Summary for Patent: 5,753,677

Title:	Benzoheterocyclic compounds
Abstract:	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.
Inventor(s):	Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
Assignee:	Otsuka Pharmaceutical Co Ltd
Application Number:	US08/474,544
Patent Claims:	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 R1 is a hydrogen atom, a halogen atom, a C1 -C6 alkyl, an amino having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkoxy,R2 is a hydrogen atom, a halogen atom, a C1 -C6 alkoxy, a phenyl-(C1 -C6) alkoxy, hydroxy, a C1 -C6 alkyl, an amino having optionally a C1 -C6 alkyl substituent, a carbamoyl-substituted C1 -C6 alkoxy, an amino-substituted C1 -C6 alkoxy having optionally a C1 -C6 alkyl substituent, or a benzoyloxy which has optionally a halogen substituent on the phenyl ring, R3 is a group of the formula: ##STR3331## or a group of the formula: ##STR3332## R4 is a hydrogen atom, a benzoyl which has optionally a halogen substituent on the phenyl ring or a C1 -C6 alkyl, R5 is a group of the formula: ##STR3333## wherein R16 is a halogen atom; a C1 -C6 alkyl which has optionally a substituent selected from a halogen atom and hydroxy; hydroxy; a C1 -C6 alkoxy; a C1 -C6 alkanoyloxy; a C1 -C6 alkylthio; a C1 -C6 alkanoyl; carboxy; a C1 -C6 alkoxycarbonyl; cyano; nitro; an amino which has optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl; phenyl; a C3 -C8 cycloalkyl; a C2 -C6 alkanoyloxy-substituted C1 -C6 alkoxy; a carboxy-substituted C1 -C6 alkoxy; a halogen-substituted C1 -C6 alkoxy; a carbamoyl-substituted C1 -C6 alkoxy; a hydroxy-substituted C1 -C6 alkoxy; a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkoxy; a phthalimido-substituted C1 -C6 alkoxy; an aminocarbonyl-(C1 -C6) alkoxy having a C1 -C6 alkyl substituent; or a group of the formula: ##STR3334## wherein A is a C1 -C6 alkylene, and R6 and R7 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C1 -C6 alkanoyl, or benzoyl, or R6 and R7 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 C1 -C6 alkyl; and m is an integer of 0 to 3, a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3335## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3336## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl, R11 is a hydrogen atom or a C1 -C6 alkyl, R12 is a C3 -C8 cycloalkyl, or a phenyl which has optionally 1 to 3 substituents selected from a C1 -C6 alkoxy, a C1 -C6 alkyl and a halogen atom, W is a group of the formula: --(CH2)p -- wherein p is an integer of 3 to 5, or a group of the formula: --CH═CH--(CH2)q -- wherein q is an integer of 1 to 3, and further said --(CH2)p -- group and said --CH═CH--(CH2)q -- group having optionally 1 to 3 substituents selected from a C1 -C6 alkyl having optionally a hydroxy substituent, a C1 -C6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C1 -C6 alkanoyloxy having optionally a halogen substituent, an amino-(C1 -C6) alkyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkylsulfonyloxy-(C1 -C6) alkyl, an azido-(C1 -C6) alkyl, a group of the formula: ##STR3337## an aminocarbonyloxy having optionally a C1 -C6 alkyl substituent, a C1 -C6 alkoxy, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkoxy, a carboxy-substituted C1 -C6 alkoxy, an aminocarbonyl-(C1 -C6) alkoxy having optionally a C1 -C6 alkyl substituent, an amino-(C1 -C6) alkoxy having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a phthalimido-substituted C1 -C6 alkoxy, hydroxy-imino, a C1 -C6 alkanoyloxy-imino, a C1 -C6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3338## wherein R81 is a hydrogen atom or a C1 -C6 alkyl, hydrazino, pyrrolyl, an amino-(C2 -C6) alkanoyloxy having optionally a C1 -C6 alkyl substituent, a group of the formula: ##STR3339## wherein A is as defined above in this claim, and R82 and R83 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a hydroxy-substituted C1 -C6 alkyl, or a pyridyl-(C1 -C6) alkyl, or R82 and R83 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 C1 -C6 alkyl, a C1 -C6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3340## wherein n is as defined above in this claim, and R14 and R15 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C1 -C6 alkanoyl, a C3 -C8 cycloalkyl, an oxiranyl-substituted C1 -C6 alkyl, a C1 -C6 alkyl having 1 to 2 substituents selected from a C1 -C6 alkoxy, hydroxy and an amino having optionally a C1 -C6 alkyl substituent, a phenyl-(C1 -C6) alkyl, a pyridyl-(C1 -C6) alkyl, a C1 -C6 alkylsulfonyl, benzoyl, a C1 -C6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C1 -C6 alkyl substituent, a cyano-substituted C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a carboxy-substituted C1 -C6 alkyl, a tetrahydropyranyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a piperidinyl having optionally a phenyl-(C1 -C6) alkyl substituent on the piperidine ring, a halogen substituted C1 -C6 alkanoyl, an imidazolyl-substituted C2 -C6 alkanoyl, an amino-(C2 -C6) alkanoyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkoxycarbonyl, an aminocarbonyl-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or a phenyl-(C1 -C6) alkoxycarbonyl, or R14 or R15 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 C1 -C6 alkyl, a phenyl-(C1 -C6) alkyl or a C1 -C6 alkanoyl, and a pharmaceutically acceptable salt thereof. 2. The method according to claim 1, wherein R1 is a hydrogen atom. 3. The method according to claim 1, wherein R1 is a halogen atom. 4. The method according to claim 1, wherein R1 is a C1 -C6 alkyl, an amino having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkoxy. 5. The method according to claim 2, wherein R2 is a hydrogen atom. 6. The method according to claim 2, wherein R2 is a halogen atom, a C1 -C6 alkoxy, or a C1 -C6 alkyl. 7. The method according to claim 2, wherein R2 is a phenyl-(C1 -C6) alkoxy, hydroxy, an amino having optionally a C1 -C6 alkyl substituent, a carbamoyl-substituted C1 -C6 alkoxy, an amino-substituted C1 -C6 alkoxy having optionally a C1 -C6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 8. The method according to claim 3, wherein R2 is a hydrogen atom. 9. The method according to claim 3, wherein R2 is a halogen atom, a C1 -C6 alkoxy, or a C1 -C6 alkyl. 10. The method according to claim 3, wherein R2 is a phenyl-(C1 -C6) alkoxy, hydroxy, an amino having optionally a C1 -C6 alkyl substituent, a carbamoyl-substituted C1 -C6 alkoxy, an amino-substituted C1 -C6 alkoxy having optionally a C1 -C6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 11. The method according to claim 4, wherein R2 is a hydrogen atom. 12. The method according to claim 4, wherein R2 is a halogen atom, a C1 -C6 alkoxy, or a C1 -C6 alkyl. 13. The method according to claim 4, wherein R2 is a phenyl-(C1 -C6) alkoxy, hydroxy, an amino having optionally a C1 -C6 alkyl substituent, a carbamoyl-substituted C1 -C6 alkoxy, an amino-substituted C1 -C6 alkoxy having optionally a C1 -C6 alkyl substituent, or a benzoyloxy having optionally a halogen substituent on the phenyl ring. 14. The method according to claim 5, wherein R3 is a group of the formula: ##STR3341## wherein R4 and R5 are as defined in claim 1. 15. The method according to claim 5, wherein R3 is a group of the formula: ##STR3342## wherein R11 and R12 are as defined in claim 1. 16. The method according to claim 6, wherein R3 is a group of the formula: ##STR3343## wherein R4 and R5 are as defined in claim 1. 17. The method according to claim 6, wherein R3 is a group of the formula: ##STR3344## wherein R11 and R12 are as defined in claim 1. 18. The method according to claim 8, wherein R3 is a group of the formula: ##STR3345## wherein R4 and R5 are as defined in claim 1. 19. The method according to claim 8, wherein R3 is a group of the formula: ##STR3346## wherein R11 and R12 are as defined in claim 1. 20. The method according to claim 9, wherein R3 is a group of the formula: ##STR3347## wherein R4 and R5 are as defined in claim 1. 21. The method according to claim 9, wherein R3 is a group of the formula: ##STR3348## wherein R11 and R12 are as defined in claim 1. 22. The method according to claim 14, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3349## and R16 and m are as defined in claim 1. 23. The method according to claim 14, wherein R4 is a hydrogen atom and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3350## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6)alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3351## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 24. The method according to claim 14, wherein R4 is a C1 -C6 alkyl. 25. The method according to claim 16, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3352## wherein R16 and m are as defined in claim 1. 26. The method according to claim 16, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3353## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3354## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 27. The method according to claim 16, wherein R4 is a C1 -C6 alkyl. 28. The method according to claim 7, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3355## wherein R16 and m are as defined in claim 1. 29. The method according to claim 7, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3356## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3357## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 30. The method according to claim 7, wherein R4 is a C1 -C6 alkyl. 31. The method according to claim 18, wherein R4 is a hydrogen atom, R5 is a group of the formula: ##STR3358## wherein R16 and m are as defined in claim 1. 32. The method according to claim 18, wherein R4 is hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted (C1 -C6) alkanoyl, a group of the formula: ##STR3359## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl), an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3360## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 33. The method according to claim 18, wherein R4 is a C1 -C6 alkyl. 34. The method according to claim 20, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3361## wherein R16 and m are as defined in claim 1. 35. The method according to claim 20, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3362## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C1 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3363## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 C6 alkoxycarbonyl and piperidinyl. 36. The method according to claim 20, wherein R4 is a C1 -C6 alkyl. 37. The method according to claim 10, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3364## wherein R16 and m are as defined in claim 1. 38. The method according to claim 10, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3365## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3366## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 39. The method according to claim 10, wherein R4 is a C1 -C6 alkyl. 40. The method according to claim 11, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3367## wherein R16 and m are as defined in claim 1. 41. The method according to claim 11, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3368## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3369## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C2 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 42. The method according to claim 12, wherein R4 is a C1 -C6 alkyl. 43. The method according to claim 12, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3370## wherein R16 and m are as defined in claim 1. 44. The method according to claim 12, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-carbonyl, tricyclo(3.3.1.1)decanylcarbonyl,naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3371## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3372## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 45. The method according to claim 12, wherein R4 is a C1 -C6 alkyl. 46. The method according to claim 13, wherein R4 is a hydrogen atom, and R5 is a group of the formula: ##STR3373## wherein R16 and m are as defined in claim 1. 47. The method according to claim 13, wherein R4 is a hydrogen atom, and R5 is a phenyl-(C1 -C6) alkoxycarbonyl, a C1 -C6 alkanoyl, a phenyl(C2 -C6) alkanoyl, a C3 -C8 cycloalkyl-(C2 -C6) alkanoyl, a C3 -C8 cycloalkylcarbonyl, tricyclo(3.3.1.1)decanylcarbonyl, naphthylcarbonyl, pyridylcarbonyl, furoyl, thenoyl, a phenoxy-(C2 -C6) alkanoyl which phenyl ring has optionally 1 to 3 substituents selected from a C1 -C6 alkyl, a C1 -C6 alkoxy and an amino having optionally a C1 -C6 alkanoyl substituent, a phthalimido-substituted C2 -C6 alkanoyl, a C1 -C6 alkoxycarbonyl-(C2 -C6) alkanoyl, a carboxy-(C2 -C6) alkanoyl, a naphthyloxy-(C2 -C6) alkanoyl, a halogen-substituted C1 -C6 alkanoyl, a group of the formula: ##STR3374## wherein R8 is a hydrogen atom, a C1 -C6 alkyl, a phenyl-(C1 -C6) alkoxycarbonyl, a carbamoyl-(C1 -C6) alkyl, an amino-(C2 -C6) alkanoyl having optionally a C1 -C6 alkyl substituent, or a C1 -C6 alkanoyl, an anilinocarbonyl which has optionally a C1 -C6 alkyl substituent on the phenyl ring, phenoxycarbonyl, a phenylsulfonyl which has optionally a substituent selected from a halogen atom and a C1 -C6 alkyl on the phenyl ring, quinolylsulfonyl, or a group of the formula: ##STR3375## wherein B is a C1 -C6 alkylene, n is an integer of 0 or 1, and R9 and R10 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl having optionally a hydroxy substituent, a C3 -C8 cycloalkyl, a phenyl-(C1 -C6) alkyl, a C1 -C6 alkanoyl, a C2 -C6 alkenyl, a phenoxy-(C1 -C6) alkyl, a phenyl which has optionally 1 to 3 substituents selected from an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C1 -C6 alkyl, a C1 -C6 alkoxy and a halogen atom, a phthalimido-substituted C1 -C6 alkyl, an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkanoyl substituent, a C2 -C6 alkynyl, or an amino-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or R9 and R10 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 C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl and piperidinyl. 48. The method according to claim 13, wherein R4 is a C1 -C6 alkyl. 49. The method according to claim 22, wherein R16 is a halogen atom, or a C1 -C6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 50. The method according to claim 25, wherein R16 is a halogen atom, or a C1 -C6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 51. The method according to claim 31, wherein R16 is a halogen atom, or a C1 -C6 alkyl having optionally a substituent selected from a halogen atom and hydroxy. 52. The method according to claim 34, wherein R16 is a halogen atom, or a C1 -C6 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: --(CH2)p -- wherein p is an integer of 3 to 5, and further said --(CH2)p -- group has optionally 1 to 3 substituents selected from a C1 -C6 alkyl having optionally a hydroxy substituent, a C1 -C6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C1 -C6 alkanoyloxy having optionally a halogen substituent, an amino-(C1 -C6) alkyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkylsulfonyloxy-(C1 -C6) alkyl, an azido-(C1 -C6) alkyl, a group of the formula: ##STR3376## an aminocarbonyloxy having optionally a C1 -C6 alkyl substituent, a C1 -C6 alkoxy, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkoxy, a carboxy-substituted C-C6 alkoxy, an amino-carbonyl-(C1 -C6) alkoxy having optionally a C1 -C6 alkyl substituent, an amino-(C1 -C6) alkoxy having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a phthalimido-substituted C1 -C6 alkoxy, hydroxyimino, a C1 -C6 alkanoyloxy-imino, a C1 -C6 alkylidene, a halogen atom, azido, sulfoxy-imino, a group of the formula: ##STR3377## wherein R81 is a hydrogen atom or a C1 -C6 alkyl, hydrazino, pyrrolyl, an amino-(C2 -C6) alkanoyloxy having optionally a C1 -C6 alkyl substituent, a group of the formula: ##STR3378## wherein A is as defined above, and R82 and R83 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a hydroxy-substituted C1 -C6 alkyl, or a pyridyl-(C1 -C6) alkyl, or R82 and R83 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 C1 -C6 alkyl, a C1 -C6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3379## wherein n is as defined above, and R14 and R15 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C1 -C6 alkanoyl, a C3 -C8 cycloalkyl, an oxiranyl-substituted C1 -C6 alkyl, a C1 -C6 alkyl having 1 to 2 substituents selected from a C1 -C6 alkoxy, hydroxy and an amino having optionally a C1 -C6 alkyl substituent, a phenyl-(C1 -C6) alkyl, a pyridyl-(C1 -C6) alkyl, a C1 -C6 alkylsulfonyl, benzoyl, a C1 -C6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C1 -C6 alkyl substituent, a cyano-substituted C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a carboxy-substituted C1 -C6 alkyl, a tetrahydropyranyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a piperidinyl having optionally a phenyl-(C1 -C6) alkyl substituent on the piperidine ring, a halogen-substituted C1 -C6 alkanoyl, an imidazolyl-substituted C2 -C6 alkanoyl, an amino-(C2 -C6) alkanoyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkoxycarbonyl, an aminocarbonyl-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or a phenyl-(C1 -C6) alkoxycarbonyl, or R14 or R15 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 C1 -C6 alkyl, a phenyl-(C1 -C6) alkyl or a C1 -C6 alkanoyl. 54. The method according to claim 1, wherein W is a group of the formula: --CH═CH--(CH2)q -- wherein q is an integer of 1 to 3, and further said --CH═CH--(CH2)q -- group has optionally 1 to 3 substituents selected from a C1 -C6 alkyl having optionally a hydroxy substituent, a C1 -C6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C1 -C6 alkanoyloxy having optionally a halogen substituent, an amino-(C1 -C6) alkyl having optionally substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkylsulfonyloxy -(C1 -C6) alkyl, an azido --(C1 -C6) alkyl, a group of the formula: ##STR3380## an aminocarbonyloxy having optionally a C1 -C6 alkyl substituent, a C1 -C6 alkoxy, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkoxy, a carboxy-substituted C1 -C6 alkoxy, an aminocarbonyl-(C1 -C6) alkoxy having optionally a C1 -C6 alkyl substituent, an amino-(C1 -C6) alkoxy having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a phthalimido-substituted C1 -C6 alkoxy, hydroxyimino, a C1 -C6 alkanoyloxy-imino, a C1 -C6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3381## wherein R18 is a hydrogen atom or a C1 -C6 alkyl, hydrazino, pyrrolyl, an amino-(C2 -C6) alkanoyloxy having optionally a C1 -C6 alkyl substituent, a group of the formula: ##STR3382## wherein A is as defined above, and R82 and R83 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a hydroxy-substituted C1 -C6 alkyl, or a pyridyl-(C1 -C6) alkyl, or R82 and R83 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 C1 -C6 alkyl, a C1 -C6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3383## wherein n is as defined above, and R14 and R15 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C1 -C6 alkanoyl, a C3 -C8 cycloalkyl, an oxiranyl-substituted C1 -C6 alkyl, a C1 -C6 alkyl having 1 to 2 substituents selected from a C1 -C6 alkoxy, hydroxy and an amino having optionally a C1 -C6 alkyl substituent, a phenyl-(C1 -C6) alkyl, a pyridyl-(C1 -C6) alkyl, a C1 -C6 alkylsulfonyl, benzoyl, a C1 -C6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C1 -C6 alkyl substituent, a cyano-substituted C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a carboxy-substituted C1 -C6 alkyl, a tetrahydropyranyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a piperidinyl having optionally a phenyl-(C1 -C6) alkyl substituent on the piperidine ring, a halogen-substituted C1 -C6 alkanoyl, an imidazolyl-substituted C2 -C6 alkanoyl, an amino-(C2 -C6) alkanoyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkoxycarbonyl, an aminocarbonyl-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or a phenyl-(C1 -C6) alkoxycarbonyl, or R14 or R15 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 C1 -C6 alkyl, a phenyl-(C1 -C6) alkyl or a C1 -C6 alkanoyl. 55. The method according to claim 53, wherein W is a group of the formula: --(CH2)p -- wherein p is an integer of 3 to 5, and said --(CH2)p -- group has optionally 1 to 3 substituents selected from a C1 -C6 alkyl having optionally a hydroxy substituent, a C1 -C6 alkoxycarbonyl, carboxy, hydroxy, oxo, a C1 -C6 alkanoyloxy having optionally a halogen substituent, an amino-(C1 -C6) alkyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkylsulfonyloxy-(C1 -C6) alkyl, an azido -(C1 -C6) alkyl, a group of the formula: ##STR3384## an aminocarbonyloxy having optionally a C1 -C6 alkyl substituent, a C1 -C6 alkoxy, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkoxy, a carboxy-substituted C1 -C6 alkoxy, an aminocarbonyl-(C1 -C6) alkoxy having optionally a C1 -C6 alkyl substituent, an amino-(C1 -C6) alkoxy having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkanoyl, a phthalimido-substituted C1 -C6 alkoxy, hydroxyimino, a C1 -C6 alkanoyloxyimino, a C1 -C6 alkylidene, a halogen atom, azido, sulfoxyimino, a group of the formula: ##STR3385## wherein R81 is a hydrogen atom or a C1 -C6 alkyl, hydrazino, pyrrolyl, an amino-(C2 -C6) alkanoyloxy having optionally a C1 -C6 alkyl substituent, a group of the formula: ##STR3386## wherein A is as defined above, and R82 and R83 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a hydroxy-substituted C1 -C6 alkyl, or a pyridyl-(C1 -C6) alkyl, or R82 and R83 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 C1 -C6 alkyl, a C1 -C6 alkanoyl, and carbamoyl, and a group of the formula: ##STR3387## wherein n is as defined above, and R14 and R15 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, a C2 -C6 alkenyl, a C1 -C6 alkanoyl, a C3 -C8 cycloalkyl, an oxiranyl-substituted C1 -C6 alkyl, a C1 -C6 alkyl having 1 to 2 substituents selected from a C1 -C6 alkoxy, hydroxy and an amino having optionally a C1 -C6 alkyl substituent, a phenyl-(C1 -C6) alkyl, a pyridyl-(C1 -C6) alkyl, a C1 -C6 alkylsulfonyl, benzoyl, a C1 -C6 alkoxycarbonyl, anilinocarbonyl, an aminocarbonyl having optionally a C1 -C6 alkyl substituent, a cyano-substituted C1 -C6 alkyl, a C1 -C6 alkoxycarbonyl-substituted C1 -C6 alkyl, a carbamoyl-substituted C1 -C6 alkyl, a carboxy-substituted C1 -C6 alkyl, a tetrahydropyranyloxy-substituted C1 -C6 alkyl, a C1 -C6 alkanoyloxy-substituted C1 -C6 alkyl, a piperidinyl having optionally a phenyl-(C1 -C6) alkyl substituent on the piperidine ring, a halogen-substituted C1 -C6 alkanoyl, an imidazolyl-substituted C2 -C6 alkanoyl, an amino-(C2 -C6) alkanoyl having optionally a substituent selected from a C1 -C6 alkyl and a C1 -C6 alkoxycarbonyl, an aminocarbonyl-(C1 -C6) alkyl having optionally a C1 -C6 alkyl substituent, or a phenyl-(C1 -C6) alkoxycarbonyl, or R14 or R15 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 C1 -C6 alkyl, a phenyl-(C1 -C6) alkyl or a C1 -C6 alkanoyl. 56. The method according to claim 55, wherein p in the group of the formula: --(CH2)p -- is 3 and the group has no substituent. 57. The method according to claim 55, wherein p in the group of the formula: --(CH2)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: --(CH2)p -- is 4 and the group has no substituent. 59. The method according to claim 55, wherein p in the group of the formula: --(CH2)p -- is 4 and the group has a substituent of a group of the formula: ##STR3389## wherein R14 and R15 and n are as defined in claim 55. 60. The method according to claim 55, wherein p in the group of the formula: --(CH2)p -- is 5. 61. The method according to claim 54, wherein q in the group of the formula: --CH═CH--(CH2)q -- is 1. 62. The method according to claim 54, wherein q in the group of the formula: --CH═CH--(CH2)q -- is 2. 63. The method according to claim 54, wherein q in the group of the formula: --CH═CH--(CH2)q -- is 3. 64. The method according to claim 57 or 59, wherein n in the group of the formula: ##STR3390## is 0, and R14 and R15 are the same or different and are each a hydrogen atom, a C1 -C6 alkyl, or a C3 -C8 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-tetrahydro-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-tetrahydro-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-tetrahydro-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-tetrahydro-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-tetrahydro-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-tetrahydroquinoline. 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-tetrahydro-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-tetrahydro-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-tetrahydro-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-tetrahydro-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)benzoyl!-2,3,4,5-tetrahydro-1H-benzazepine.