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KR950704253A - 5-HT₁-유사 작용제로서의 카바졸 유도체의 거울상이성질체(Enantiomers of Carbazole Derivatives as 5-HT₁-Like Agonists) - Google Patents

5-HT₁-유사 작용제로서의 카바졸 유도체의 거울상이성질체(Enantiomers of Carbazole Derivatives as 5-HT₁-Like Agonists)

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Publication number
KR950704253A
KR950704253A KR1019950702522A KR19950702522A KR950704253A KR 950704253 A KR950704253 A KR 950704253A KR 1019950702522 A KR1019950702522 A KR 1019950702522A KR 19950702522 A KR19950702522 A KR 19950702522A KR 950704253 A KR950704253 A KR 950704253A
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South Korea
Prior art keywords
carboxamido
tetrahydrocarbazole
hydrate
solvate
methylamino
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KR1019950702522A
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English (en)
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KR100307001B1 (ko
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개리 토마스 보레트
존 키터링검
로데릭 앨런 포터
마크 랄프 쉽톤
미틸리 비말
로드니 크리스토퍼 영
Original Assignee
데이비드 로버츠
스미스클라인 비참 피엘씨
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

본 발명은 R4가 메틸 또는 에틸인 하기 일반식(I)의 화합물의 (＋) 또는 (－) 거울상 이성질체 또는 그의염, 용매화물 또는 수화물, 이들 화합물의 제조 방법 및 이들을 함유하는 계약 조성물에 관한 것이다. 상기 화합물 중 (＋)거울이상이성질체 화합물은 5―HT1―유사 작용작이다.

Description

5―HT1―유사 작용제로서의 카바졸 유도체의 거울상이성질체(Enantiomers of Carbazole Derivatives as 5―HT1―Like Agonists)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 하기 일반식(I)의 화합물의 (＋) 또는 (－) 거울상 이성질체 또는 그의 염, 용매화물 또는 수화물.
    상기 식 중, R4는 메틸 또는 에틸이다.
  2. (＋)―6―카르복스아미도―3―메틸아미노―1,2,3,4―테트라히드로카바졸 또는 그의 염, 용매화물 또는 수화물.
  3. (－)―6―카르복스아미도―3―메틸아미노―1,2,3,4―테트라히드로카바졸 또는 그의 염, 용매화물 또는 수화물.
  4. (＋)―6―카르복스아미도―3―에틸아미노―1,2,3,4―테트라히드로카바졸 또는 그의 염, 용매화물 또는 수화물.
  5. (－)―6―카르복스아미도―3―에틸아미노―1,2,3,4―테트라히드로카바졸 또는 그의 염, 용매화물 또는 수화물.
  6. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 L(＋)―타르타르산염(1 : 1) 또는 그의 용매화물 또는 수화물.
  7. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 D(－)―타르타르산염(1 : 1) 또는 그의 용매화물 또는 수화물.
  8. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 헤미숙신산염(2 : 1) 또는 그의 용매화물 또는 수화물.
  9. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 메탄술폰산염 또는 그의 용매화물 또는 수화물.
  10. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 숙신산염(1 : 1) 또는 그의 용매화물 또는 수화물.
  11. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 염산염 또는 그의 용매화물 또는 수화물.
  12. (＋)―6―카르복스아미도―3―N―메틸아미노―1,2,3,4―테트라히드로카바졸 브롬화수소 산염 또는 그의 용매화물 또는 수화물.
  13. (＋)―6―카르복스아미도―3―N―에틸아미노―1,2,3,4―테트라히드로카바졸 숙신산염(1 : 1) 또는 그의 용매화물 또는 수화물.
  14. (＋)―6―카르복스아미도―3―N―에틸아미노―1,2,3,4―테트라히드로카바졸 염산염 또는 그의 용매화물 또는 수화물.
  15. (a)일반식(I)의 화합물 또는 그의 유도체의 거울상 이성질체 혼합물을 예를들면 키랄성 HPLC 컬럼상에서 크로카토그래피하여 분리하거나, (b)일반식(I)의 화합물의 키랄 유도체의 부분입체이성질체를 예를들면 결정정화 또는 크로마토그래피하여 분리하거나, 또는 (c)3―아미노―6―카르복스아미도―1,2,3,4―테트라히드로카바졸 또는 그의 염의 (＋) 또는 (－) 거울상이성질체를 알킬화하고, 이어서 필요하거나 바람직하다면 임의의 N―보호기를 제거하고, 염을 전환시켜 유리 염기 및(또는) 염을 형성시키는 것으로 이루어지는 일반식(I)의 거울상 이성질체 또는 그의 염, 용매화물 또는 수화물의 제조방법.
  16. 5―HT1―유사 작용체를 필요로 하는 등상의 치료용 약제의 제조에 있어서 제1항 내지 제14항 중 어느한 항에 따른 일반식(I)의 거울상이성질체 또는 그의 생리학적으로 허용가능한 염, 용매화물 또는 수화물의 용도.
  17. 유효량의 일반식(I)의 거울상이성질체 또는 그의 생리적으로 허용가능한 염, 용매화물 또는 수화물을 필요로 하는 환자에게 투여하는 것으로 이루어지는, 5―HT1―유사 작용체를 필요로 하는 증상의 치료 방법.
  18. 제1항 내지 제14항 중 어느 한 항에 따른 일반식(I)의 거울상이성질체 또는 그의 생리적으로 허용가능한 염, 용매화를 또는 수화물, 및 생리적으로 허용가능한 담체로 이루어지는 제약 조성물.
    ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.
KR1019950702522A 1992-12-21 1993-12-16 5-ht1-유사효능제로서의카르바졸유도체의거울상이성질체 KR100307001B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB9226530.5 1992-12-21
GB929226530A GB9226530D0 (en) 1992-12-21 1992-12-21 Compounds
PCT/EP1993/003627 WO1994014772A1 (en) 1992-12-21 1993-12-16 Enantiomers of carbazole derivatives as 5-ht1-like agonists

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KR950704253A true KR950704253A (ko) 1995-11-17
KR100307001B1 KR100307001B1 (ko) 2001-12-28

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US (2) US5618947A (ko)
EP (1) EP0674621B1 (ko)
JP (1) JP3364222B2 (ko)
KR (1) KR100307001B1 (ko)
CN (1) CN1039491C (ko)
AT (1) ATE233239T1 (ko)
AU (1) AU688748B2 (ko)
CA (1) CA2152630C (ko)
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GB (1) GB9226530D0 (ko)
HK (1) HK1012368A1 (ko)
MX (1) MX9400035A (ko)
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PT (1) PT674621E (ko)
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NZ259363A (en) 1996-12-20
CN1095712A (zh) 1994-11-30
JPH08504790A (ja) 1996-05-21
ATE233239T1 (de) 2003-03-15
US5650426A (en) 1997-07-22
DE69332718T2 (de) 2003-12-04
AU688748B2 (en) 1998-03-19
WO1994014772A1 (en) 1994-07-07
KR100307001B1 (ko) 2001-12-28
HK1012368A1 (en) 1999-07-30
CA2152630A1 (en) 1994-07-07
ES2193151T3 (es) 2003-11-01
DK0674621T3 (da) 2003-06-10
ZA939457B (en) 1995-06-19
MX9400035A (es) 1994-07-29
EP0674621B1 (en) 2003-02-26
PT674621E (pt) 2003-07-31
JP3364222B2 (ja) 2003-01-08
AU5814594A (en) 1994-07-19
EP0674621A1 (en) 1995-10-04
CN1039491C (zh) 1998-08-12
DE69332718D1 (de) 2003-04-03
GB9226530D0 (en) 1993-02-17
US5618947A (en) 1997-04-08
CA2152630C (en) 2005-07-26

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