KR900701788A - α-아드레날린성 수용체 길항근 - Google Patents
α-아드레날린성 수용체 길항근Info
- Publication number
- KR900701788A KR900701788A KR1019900700204A KR900700204A KR900701788A KR 900701788 A KR900701788 A KR 900701788A KR 1019900700204 A KR1019900700204 A KR 1019900700204A KR 900700204 A KR900700204 A KR 900700204A KR 900701788 A KR900701788 A KR 900701788A
- Authority
- KR
- South Korea
- Prior art keywords
- tetrahydro
- chloro
- benzazin
- methylfuro
- methyl
- Prior art date
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- 239000000674 adrenergic antagonist Substances 0.000 title 1
- 102000004305 alpha Adrenergic Receptors Human genes 0.000 title 1
- 108090000861 alpha Adrenergic Receptors Proteins 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 6
- 241000124008 Mammalia Species 0.000 claims abstract 5
- 125000000217 alkyl group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 22
- OKKJLVBELUTLKV-UHFFFAOYSA-N methanol Substances OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 14
- -1 2-propenyloxy Chemical group 0.000 claims 11
- 125000003342 alkenyl group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 5
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 4
- KFZMGEQAYNKOFK-UHFFFAOYSA-N 2-propanol Substances CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 3
- 125000006201 3-phenylpropyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 3
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 3
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 2
- 229910052698 phosphorus Inorganic materials 0.000 claims 2
- 239000011574 phosphorus Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 claims 1
- 208000018262 Peripheral vascular disease Diseases 0.000 claims 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 claims 1
- 230000003042 antagnostic effect Effects 0.000 claims 1
- 230000036772 blood pressure Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 150000003018 phosphorus compounds Chemical class 0.000 claims 1
- 102000015007 alpha-adrenergic receptor activity proteins Human genes 0.000 abstract 3
- 108040006816 alpha-adrenergic receptor activity proteins Proteins 0.000 abstract 3
- 239000005557 antagonist Substances 0.000 abstract 3
- 230000008485 antagonism Effects 0.000 abstract 2
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/06—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
내용 없음
Description
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음
Claims (18)
- 다음 일반식으로 표시되는 화합물이나 그것의 제약학적 허용염.상기식에서 X는 H, Cl, B F, I, CF3, C1-6알킬, CORl0, CO2R|10, C0NRI6R11, CN, NO2, NR12R13, 0R12,SC1-4알킬, S(CH2)|O-6아릴, SCF3이거나, 세개의 치환체까지의 이들의 어떤 용이한 혼합이며: R은 H, C1-6알킬, 또는 C3-5알케닐이고: R은 W, (CH2)|O-6CWYZ, 또는 C3-5알케닐이며, 여기에서 이중결합이 1-위치에 있는 것은 제외된다.R10은 알킬이거나 (CH2)O-6아릴이고; R11및 R16는 독립적으로 H, C1-6알킬, 또는 (CH2)O-6아릴이며: R12은 H, C1-6알킬, COR14또는 SO2R15이고: R13은 독립적이고 H이거나 C1-6알킬이며; R14과 R15는 각각 독립적으로 C1-6알킬이거나 (CH2)O-6아릴이고: W는 H, N02, C1-6알킬, CH2CH2OH, CN, C(R13)2,(OR2), CH2SR2, COR2, CO2R2, C0NR3R4, S02NR3R4, SC3R2, SO2R5, SOR5, SR5, P(O)+(OR3)(OR4), P(O)R5(OR3), P(O)R5R6, O(O)R5(NR3R4), cl, Br, F, I, CF3또는 (CH2)O-6아릴이고: Y와 Z는 독립적으로 H이거나 C1-6알킬이며: R2, R3및 R4는 독립적으로 H, , C1-6알킬, C3-5알케닐, 또는 (CH2)O-6아릴이고; R5와 R6는 독립적으로 C1-6알킬, C3-5알케닐, 또는 (CH2)O-6아릴이다.
- 다음 일반식을 갖는 제1항의 화합물 또는 그것의 제약학적 허용염.상기식에서 X는 H, Cl, B F, I, CF3, C1-6알킬, CORl0, CO2R|10, C0NRI6R11, CN, NO2, NR12R13, 0R12,SC1-4알킬, S(CH2)|O-6아릴 또는 SCF3이며; R은 H, C1-6알킬, 또는 C3-5알케닐이고: R은 W, (CH2)O-6CWYZ, 또는 C3-5알케닐이며, 여기에서 이중결합이 1-위치에 있는 것을 제외되며; R10은 알킬이거나 (CH2)O-6아릴이고; R11및 R16는 독립적으로 H, C1-6알킬, 또는 (CH2)O-6아릴이며: RI2은 H, C1-6알킬, COR14또는 SO2R15이고: R13은 독립적이고 H이거나 C1-6알킬이며; R14과 R15는 각각 독립적으로 C1-6알킬이거나 (CH2)O-6아릴이고: W는 H, N02, C1-6알킬, CH2CH|2OH, CN, C(R13)2,(OR2), CH2SR2, COR|2, CO2R2, C0NR3R4, S02NR3R4, SC3R2, SO2R5, SOR5, SR5, P(O)+(OR3)(OR4), P(O)R5(OR3), P(O)R5R6, P(O)(OR2)NR3R4, P(O)(NR3R|4)2, O(O)R5(NR3R4), cl, Br, F, I, CF3또는 (CH2)O-6아릴이고: Y와 Z는 독립적으로 H이거나 C1-6알킬이며: R2, R3및 R4는 독립적으로 H, C1-6알킬, C3-5알케닐, 또는 (CH2)O-6아릴이고; R5와 R6는 독립적으로 C1-6알킬, C3-5알케닐, 또는 (CH2)O-6아릴이다.
- 제1항에 있어서, X가 Cl, Br, F, I, CN, 또는 NR12R13로 구성되는 그룹으로부터 선택되는 한개나 두개의 치환체인 화합물.
- 제3항에 있어서, R이 CH3이거나 H이고 X가 7이나 7, 9위치에 있는 화합물.
- 제4항에 있어서, 7-클로로-3,4,5,6-테트라히드로-2,4-디메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀인 화합물이거나 그것의 제약학적 허용염.
- 제4항에 있어서, 2-브로모-7-클로로-3,4,5,6-테트라히드로-4-메틸푸로 〔4,3,2-에프〕〔3〕-벤즈아제핀인 화합물이거나 그것의 제약학적 허용염.
- 제4항에 있어서, 1. 에틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로- 〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 2. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 3. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스알데히드; 4. 메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 5. 2-프로페닐 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 6. 7-클로로-3,4,5,6-에틸푸로-카보니트릴; 7. 7-클로로-3,4,5,6-메틸푸로; 8. 7-클로로-2-에틸-3,4,5,6-테트라히드로- 4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀: 9. 에틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로피오네이트: 1O. 7-클로로-3,4,5,8-테트라히드로-4-메틸푸로- 〔4,3,2-에프〕〔3〕벤즈아제피-2-프로파놀: 11. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(2-프로페닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 12. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(프로페닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 13. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(3-메틸-2부테닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 14. 7-클로로-3,4,5,6- 테트라히드로-4-메틸-2-〔(2-프로페닐티오)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 15. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-(트리플루오로메틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 16. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드; 17. N-부틸-7-클로로-3,4,5,6-테트라히드로-4-에틸푸로 〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 18. N,N-디메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 19. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 20. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(2-페닐메틸)푸로〔4,3,2-에프〕벤즈아제핀-2-카복스아미드: 21. 7-클로로-3,4,5,6-테트라히드로-N-4-디메틸-N-(2-페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 22. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(3-페닐프로필)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 23. 페닐메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로파노에이트;24. 2,7-디클로로 -3,4,5,6-테트라히드로-4-메틸프로-〔4,3,2-에프〕〔3〕벤즈아제핀: 25. 7-클로로-2-〔(4-클로로페닐)메틸옥시〕-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀: 26. 7-플루오로-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 27. 7-클로로-9-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 28. 7-브로모-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 29. 7-디메틸아미노-3,4,5,6-테드라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 30. 에틸7-시아노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 31. 에틸 7-클로로-9-디에틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3.2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 32. 에틸 7-클로로-9-메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 33. 에틸 7,9-디클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 34. 에틸 7-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 인 화합물이거나 그것들의 제약학적 허용염.
- 제1항의 화합물과 적절한 제약학적 담체로 구성되는 제약학적 조성물.
- 제8항에 있어서, 화합물의 7-클로로-3,4,5,6-테트라히드로-2,4,-디메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀인 제약학적 조성물.
- 제8항에 있어서, 화합물이 2-브로모-7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀 제약학적 조성물.
- 제9항에 있어서, 화합물이 1. 에틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 2. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 3. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스알데히드; 4. 메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 5. 2-프로페닐 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 6. 7-클로로-3,4,5,6-에틸푸로-카보니트릴; 7. 7-클로로-3,4,5,6-메틸푸로; 8. 7-클로로-2-에틸-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀: 9. 에틸 7-클로로-3,4,5,6-테트라히드로 -4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로피오네이트: 1O. 7-클로로-3,4,5,8-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로파놀: 11. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(2-프로페닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 12. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(프로페닐옥시)에틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 13. 7-클로로-3,4,5,6-테트라히드로 -4-메틸-2-〔(3-메틸-2푸로부테닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 14. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(2-프로페닐티오)메틸〕푸로 〔4,3,2-에프〕〔3〕벤즈아제핀; 15. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-(트리플루오로메틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 16. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드; 17. N-부틸-7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드:18. N,N-디메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 19. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 20. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(2-페닐에틸)푸로〔4,3,2-에프〕벤즈아제핀-2-카복스아미드: 21. 7-클로로-3,4,5,6-테트라히드로-N-4-디메틸-N-(2-페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 22. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(3-페닐프로필)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 23. 페닐메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로파노에이트; 24. 2,7-디클로로-3,4,5,6-테트라히드로-4-메틸프로-〔4,3,2-에프〕〔3〕벤즈아제핀: 25. 7-클로로-2-〔(4-클로로페닐)메틸옥시〕-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀: 26. 7-플루오로-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 27. 7-클로로-9-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 28. 7-브로모-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 29. 7-디메틸아미노-3,4,5,6-테드라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀:30. 에틸 7-시아노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3, 2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 31. 에틸 7-클로로-9-디에틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트;32. 에틸 7-클로로-9-메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 33. 에틸 7,9-디클로로-3,4,5,6-테트라히드로-4-메틸푸 로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 34. 에틸 7-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 인 제약학적 조성물.
- 제1항의 화합물의 유효한 양을 이것을 필요로 하는 대상체에 투여하는 것으로 구성되는 포유동물에 α-아드레날린성 수용체에 길항작용을 일으키는 방법.
- 제12항에 있어서, 화합물의 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로 〔4,3,2-에프〕〔3〕벤즈아제핀인 방법.
- 제8항에 있어서, 화합물이 2-브로모-7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀인 방법.
- 제12항에 있어서, 화합물이 1. 에틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 2. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 3. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스알데히드; 4. 메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 5. 2-프로페닐 7-클로로-3,4,5,6-테트라히드로-4-메틸 푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 6. 7-클로로-3,4,5,6- 에틸푸로-카보니트릴; 7. 7-클로로-3,4,5,6-메틸푸로; 8. 7-클로로-2-에틸-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀: 9. 에틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로피오네이트: 1O. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로-〔4,3,2-에프〕〔3〕벤즈아제피-2-프로파놀: 11. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(2-프로페닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 12. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(프로페닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀: 13. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(3-메틸-2부테닐옥시)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 14. 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-〔(2-프로페닐티오)메틸〕푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 7-클로로-3,4,5,6-테트라히드로-4-메틸-2-(트리플루오로메틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀; 15. 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드; 17. N-부틸-7-클로로-3,4,5,6-테트라히드로-4-에틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 18. N,N-디메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 19. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 20. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(2-페닐메틸)푸로〔4,3,2-에프〕벤즈아제핀-2-카복스아미드: 21. 7-클로로-3,4,5,6-테트라히드로-N-4-디메틸-N-(2-페닐에틸)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 22. 7-클로로-3,4,5,6-테트라히드로-4-메틸-N-(3-페닐프로필)푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복스아미드: 23. 페닐메틸 7-클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-프로파노에이트;24. 2,7-디클로로-3,4,5,6-테트라히드로-4- 메틸프로-〔4,3,2-에프〕〔3〕벤즈아제핀: 25. 7-클로로-2-〔(4-클로로페닐)메틸옥시〕-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀: 26. 7-플루오로-3,4,5,6-테트라히드로-4-메틸프로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 27. 7-클로로-9-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 28. 7-브로모-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 29. 7-디메틸아미노-3,4,5,6-테드라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-메타놀: 30. 에틸7-시아노-3,4,5,6-테트라히드로-4-메틸푸로 〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 31. 에틸 7-클로로-9-디에틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3.2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 32. 에틸 7-클로로-9-메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 33. 에틸 7,9-디클로로-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트; 34. 에틸 7-디메틸아미노-3,4,5,6-테트라히드로-4-메틸푸로〔4,3,2-에프〕〔3〕벤즈아제핀-2-카복실레이트: 인 방법.
- 제1항 화합물의 효과적인 양을 이것을 필요로 하는 대상체에 투여하는 것으로 구성되는 포유동물에서 혈압을 감소시키는 방법.
- 제1항 화합물의 효과적인 양을 이것을 필요로 하는 대상체에 투여하는 것으로 구성되는 포유동물에서 말초혈관의 질병을 치료하는 방법.
- 제1항 화합물의 효과적인 양을 이것을 필요로 하는 대상체에 투여하는 것으로 구성되는 포유동물에서 양성전립선 비대를 치료하는 방법.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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US20081688A | 1988-06-01 | 1988-06-01 | |
US200,816 | 1988-06-01 | ||
PCT/US1989/002398 WO1989012051A1 (en) | 1988-06-01 | 1989-05-31 | alpha-ADRENERGIC RECEPTOR ANTAGONISTS |
Publications (1)
Publication Number | Publication Date |
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KR900701788A true KR900701788A (ko) | 1990-12-04 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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KR1019900700204A KR900701788A (ko) | 1988-06-01 | 1989-05-31 | α-아드레날린성 수용체 길항근 |
Country Status (13)
Country | Link |
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EP (1) | EP0344982B1 (ko) |
JP (1) | JPH03504606A (ko) |
KR (1) | KR900701788A (ko) |
CN (1) | CN1038099A (ko) |
AT (1) | ATE114310T1 (ko) |
AU (1) | AU630100B2 (ko) |
CA (1) | CA1320485C (ko) |
DE (1) | DE68919438T2 (ko) |
NZ (1) | NZ229296A (ko) |
PT (1) | PT90717B (ko) |
WO (1) | WO1989012051A1 (ko) |
ZA (1) | ZA894096B (ko) |
ZW (1) | ZW6889A1 (ko) |
Families Citing this family (3)
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CA1320486C (en) * | 1988-06-01 | 1993-07-20 | John J. Lafferty | .alpha. -adrenergic receptor antagonists |
CN100391460C (zh) * | 2002-06-20 | 2008-06-04 | 诺瓦乐医药公司 | α-肾上腺素能受体拮抗剂的稳定配方及其用途 |
US9556200B2 (en) | 2012-03-06 | 2017-01-31 | Takeda Pharmaceutical Company Limited | Tricyclic compound |
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BE795451A (fr) * | 1972-02-23 | 1973-08-16 | Pfizer | Agents hypoglycemiants aza indoliques tricycliques |
US3950343A (en) * | 1973-11-06 | 1976-04-13 | Ayerst, Mckenna And Harrison Ltd. | Pyrroloisoquinoline derivatives |
ATE34392T1 (de) * | 1983-10-17 | 1988-06-15 | Synthelabo | Imidazolinderivate, ihre herstellung und therapeutische verwendung. |
DE3525564A1 (de) * | 1985-07-15 | 1987-02-05 | Schering Ag | Tricyclische verbindungen mit indolstruktur, verfahren zu ihrer herstellung und deren verwendung als arzneimittel |
CA1320486C (en) * | 1988-06-01 | 1993-07-20 | John J. Lafferty | .alpha. -adrenergic receptor antagonists |
-
1989
- 1989-05-26 EP EP89305341A patent/EP0344982B1/en not_active Expired - Lifetime
- 1989-05-26 AT AT89305341T patent/ATE114310T1/de not_active IP Right Cessation
- 1989-05-26 NZ NZ229296A patent/NZ229296A/en unknown
- 1989-05-26 CA CA000600796A patent/CA1320485C/en not_active Expired - Fee Related
- 1989-05-26 DE DE68919438T patent/DE68919438T2/de not_active Expired - Fee Related
- 1989-05-29 ZW ZW68/89A patent/ZW6889A1/xx unknown
- 1989-05-30 ZA ZA894096A patent/ZA894096B/xx unknown
- 1989-05-31 KR KR1019900700204A patent/KR900701788A/ko not_active Application Discontinuation
- 1989-05-31 JP JP1506859A patent/JPH03504606A/ja active Pending
- 1989-05-31 WO PCT/US1989/002398 patent/WO1989012051A1/en unknown
- 1989-05-31 AU AU37708/89A patent/AU630100B2/en not_active Ceased
- 1989-06-01 CN CN89103716A patent/CN1038099A/zh active Pending
- 1989-06-01 PT PT90717A patent/PT90717B/pt not_active IP Right Cessation
Also Published As
Publication number | Publication date |
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JPH03504606A (ja) | 1991-10-09 |
PT90717A (pt) | 1989-12-29 |
DE68919438D1 (de) | 1995-01-05 |
CN1038099A (zh) | 1989-12-20 |
PT90717B (pt) | 1994-11-30 |
AU630100B2 (en) | 1992-10-22 |
WO1989012051A1 (en) | 1989-12-14 |
NZ229296A (en) | 1991-05-28 |
DE68919438T2 (de) | 1995-05-04 |
ZW6889A1 (en) | 1989-08-30 |
EP0344982A2 (en) | 1989-12-06 |
ZA894096B (en) | 1990-06-27 |
CA1320485C (en) | 1993-07-20 |
EP0344982A3 (en) | 1991-05-15 |
ATE114310T1 (de) | 1994-12-15 |
EP0344982B1 (en) | 1994-11-23 |
AU3770889A (en) | 1990-01-05 |
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