KR920002548A - 피라졸리디논 cck 및 가스트린 길항물질 및 그의 약학 조성물 - Google Patents

피라졸리디논 cck 및 가스트린 길항물질 및 그의 약학 조성물 Download PDF

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KR920002548A
KR920002548A KR1019910012030A KR910012030A KR920002548A KR 920002548 A KR920002548 A KR 920002548A KR 1019910012030 A KR1019910012030 A KR 1019910012030A KR 910012030 A KR910012030 A KR 910012030A KR 920002548 A KR920002548 A KR 920002548A
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phenyl
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alkyl
hydrogen
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프랭크 브라운 레이몬드
제프리 허버트 제임스
린 톱 카렌
앤드류 니일 데이비드
케빈 릴 존
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리로이 휘테커
일라이 릴리 앤드 캄파니
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/06—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D231/08—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with oxygen or sulfur atoms directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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Abstract

내용 없음

Description

피라졸리디논 CCK 및 가스트린 길항물질 및 그의 약학 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (19)

  1. 하기 구조식(Ⅰ) 또는 (Ⅱ)의 화합물 및 그의 약학적으로 허용되는 염.
    상기식에서, R 및 R1은 독립적으로, 수소, C1-C6알킬, 페닐, 벤질, 나프틸, 피리딜, 또는 치환된 페닐(C1-C6알킬, C1-C6알콕시, C1-C6알킬티오, 할로, 트리플루오로메틸, 페닐, 페녹시, 페닐(C1-C4알킬), 페닐(C1-C4알콕시), 페닐아세틸, C1-C6알카노일, 시아노, 카바밀, 니트로, C1-C6알콕시카보닐, 메틸렌디옥시, C3-C6알킬렌, 아미노, -NH(C1-C4알킬 또는 벤질), 및 N(C1-C4알킬)2로 이루어진 그룹중에서 선택된 1,2 또는 3개의 치환체로 치환됨)이고, R2는 수소, C1-C6알킬, 카복시메틸, C1-C4알콕시 카보닐메틸 또는 일반식A)-t-Y(여기에서, t는 1 또는 0이고, A는 -CH2-, -O-, -NH- 또는 -N(C1-C6알킬)-이며, Y는 페닐 또는 상기 정의한 바와 같은 치환된 페닐이다)의 그룹이며, R4는 C1-C6알킬, 카복시메틸, 또는 C1-C4알콕시카보닐메틸이고, R3는 수소 또는 하기 일반식
    (여기에서, B는 O 또는 S이고, X 는 상기 정의한 페닐 치환체중에서 선택되며, m은 0,1 또는 2이고, n은 0또는 1이며, Q는 -NH-, -N(C1-C6알킬)-,-S-또는 -O-이고, R5는 일반식-(CH(R6)q-CH)r-R7의 그룹이며, R6는 수소 또는 C1-C6알킬이고, q는 0 또는 1이며, R은 0,1 또는 2이고, R7은 수소, C1-C8알킬, C3-C8사이클로알킬, 펜타플루오로페닐, 피리딜, 테트라하이드로나프틸, 인돌릴, 퀴놀리닐, 페닐, 나프틸, 또는 페닐에 대해 상기 정의한 바와 같은 1,2 또는 3개의 치환체로 치환된 페닐 또는 나프닐이거나, 또는 그룹 -(Q)nR5는 2-페트라하이드로이소퀴놀리닐이다)의 그룹이나, 단, 그룹 R 또는 R1중 적어도 하나는 수소 또는 C1-C6알킬이외의 다른 것이고, R 또는 R1은 R 및 R1중 다른 하나가 페닐로 치환된 페닐인 경우에만 수소이며, 또한 그룹 R2및 R3중 적어도 하나는 수소 이외의 다른 것이고, R3가 일반식의 그룹인 경우, R2는 일반식의 그룹 이외의 다른 것이다.
  2. 제1항에 있어서, R 및 R1이 트랜스 입체배위로 존재하는 화합물.
  3. 제1항에 있어서, R 및 R1이 시스 입체배위로 존재하는 화합물.
  4. 제1항에 내지 제3항중 어느 한 항에 있어서, 일반식(Ⅱ)을 갖는 화합물,
    상기식에서, R, R1, R3및 R4는 제 1 항에서 정의한 바와 같다.
  5. 제1항 내지 제3항중 어느 한 항에 있어서, 하기 일반식(Ⅰ)을 갖는 화합물.
    상기식에서, R, R1, R2및 R3는 제1항에서 정의한 바와 같다.
  6. 제5항에 있어서, R2가 일반식 -CONHY 그룹인 화합물.
  7. 제1항 내지 제6항중 어느 한 항에 있어서, R3가 수소인 화합물.
  8. 제1항 내지 제6항중 어느 한 항에 있어서, R2가 메틸 또는 카복시메틸인 화합물.
  9. 제1항 내지 제8항중 어느 한 항에 있어서, R 및 R1이 페닐 또는, 치환된 페닐인 화합물.
  10. 제1항 내지 제5항중 어느 한 항에 있어서, R2가 수소인 화합물.
  11. 제10항에 있어서, R3가 하기 일반식의 그룹인 화합물.
    상기식에서, B, X 및 m은 제1항에 정의한 바와 같다.
  12. 제10항 내지 제11항에 있어서, R 및 R1이 페닐인 화합물.
  13. 제10항 내지 제12항중 어느 한 항에 있어서, B가 S인 화합물.
  14. 제10항 내지 제12항중 어느 한 항에 있어서, B가 O인 화합물.
  15. 제10항 및 제12항 내지 제14항중 어느 한 항에 있어서, R3가 그룹 -CB(Q)n-[CH(R6)]q-(CH2)r-R7인 화합물.
  16. 제15항에 있어서, R3가 -CSNH-[CH(R6)]q-(ch2)r-R7인 화합물.
  17. 제15항 또는 제16항에 있어서, q 및 r이 0이고, R7이 페닐 또는 치환된 페닐인 화합물.
  18. 제15항 내지 제17항중 어느 한 항에 있어 R 및 R1이 페닐 또는 치환된 페닐인 화합물.
  19. 활성성분으로서 효과량의 제1항 내지 제18항중 어느 한항에 따르는 화합물 및 그의 약학적으로 허용되는 담체, 부형제 또는 희석재를 포함하는 약학 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910012030A 1990-07-17 1991-07-15 피라졸리디논 cck 및 가스트린 길항물질 및 그의 약학 조성물 KR960005950B1 (ko)

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US55348990A 1990-07-17 1990-07-17
US07/553,489 1990-07-17

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KR960005950B1 KR960005950B1 (ko) 1996-05-06

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EP (1) EP0467614A1 (ko)
JP (1) JPH04230367A (ko)
KR (1) KR960005950B1 (ko)
CN (1) CN1032000C (ko)
AU (2) AU644190B2 (ko)
BR (1) BR9103042A (ko)
CA (1) CA2046672A1 (ko)
CS (1) CS219391A3 (ko)
FI (1) FI913431A (ko)
HU (1) HUT58296A (ko)
IE (1) IE912489A1 (ko)
IL (1) IL98785A (ko)
MX (1) MX9100164A (ko)
NO (1) NO912772L (ko)
NZ (1) NZ238912A (ko)
PT (1) PT98323A (ko)
RU (1) RU2076100C1 (ko)
YU (1) YU124391A (ko)
ZA (1) ZA915372B (ko)

Families Citing this family (9)

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Publication number Priority date Publication date Assignee Title
US5191084A (en) * 1991-05-01 1993-03-02 American Home Products Corporation Phenyl pyrazolidinones as bronchodilators and anti-inflammatory agents
US5153191A (en) * 1991-08-20 1992-10-06 Warner-Lambert Company Cholecystokinin antagonists useful for treating depression
US5399708A (en) * 1993-11-12 1995-03-21 Eli Lilly And Company Pyrazolidin-3-one derivatives
GB0011095D0 (en) 2000-05-08 2000-06-28 Black James Foundation astrin and cholecystokinin receptor ligands (III)
PE20020856A1 (es) * 2001-02-13 2002-11-11 Aventis Pharma Gmbh 1,2,3,4-tetrahidronaftil aminas aciladas
UA79804C2 (en) 2002-07-03 2007-07-25 Janssen Pharmaceutica Nv Cck-1 receptor modulators
GB0312368D0 (en) * 2003-05-30 2003-07-02 Univ Aston Novel ureido- and amido-pyrazolone derivatives
US8410135B2 (en) * 2007-06-15 2013-04-02 Solvay Pharmaceuticals B.V. 4,5 dihydro-(1H)-pyrazole derivatives as cannabinoid CB1 receptor modulators
EP3883925A4 (en) * 2018-11-20 2021-12-29 Sironax Ltd Cyclic ureas

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE530886A (ko) * 1953-08-03
FR82186E (fr) * 1959-04-10 1964-01-04 Kodak Pathe Nouveau produit photographique et procédé pour le traitement de ce produit
FR2529786A1 (fr) * 1982-07-12 1984-01-13 Nativelle Sa Ets Compositions pharmaceutiques a base de derives de la pyrazolone-5, nouveaux produits et procede de preparation
DE3407506A1 (de) * 1984-03-01 1985-09-05 A. Nattermann & Cie GmbH, 5000 Köln 3-amino-1-(4,5,6,7-tetrahydro-benzothiazolyl)-2-pyrazoline, verfahren zu ihrer herstellung und deren verwendung
EP0166355A2 (en) * 1984-06-26 1986-01-02 Merck & Co. Inc. Substituted aminophenyl compounds and acylaminophenyl compounds and pharmaceutical compositions containing them
US5089622A (en) * 1988-12-12 1992-02-18 Mitsui Toatsu Chemicals Incorporated (-)-2-pyrazoline compounds and therapeutic agent for cerebrovascular disorders containing the same as effective ingredient
US5191084A (en) * 1991-05-01 1993-03-02 American Home Products Corporation Phenyl pyrazolidinones as bronchodilators and anti-inflammatory agents

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PT98323A (pt) 1992-06-30
HU912376D0 (en) 1991-12-30
AU8040991A (en) 1992-01-23
RU2076100C1 (ru) 1997-03-27
ZA915372B (en) 1993-03-31
YU124391A (sh) 1994-01-20
FI913431A (fi) 1992-01-18
KR960005950B1 (ko) 1996-05-06
NO912772L (no) 1992-01-20
IL98785A0 (en) 1992-07-15
NO912772D0 (no) 1991-07-15
CN1058209A (zh) 1992-01-29
BR9103042A (pt) 1992-04-28
AU5529394A (en) 1994-04-28
CS219391A3 (en) 1992-02-19
JPH04230367A (ja) 1992-08-19
CA2046672A1 (en) 1992-01-18
CN1032000C (zh) 1996-06-12
FI913431A0 (fi) 1991-07-16
IL98785A (en) 1995-11-27
AU644190B2 (en) 1993-12-02
MX9100164A (es) 1992-02-28
NZ238912A (en) 1992-12-23
EP0467614A1 (en) 1992-01-22
HUT58296A (en) 1992-02-28
IE912489A1 (en) 1992-01-29

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