KR950702978A - 아미드 유도체(Amide derivatives) - Google Patents

아미드 유도체(Amide derivatives) Download PDF

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KR950702978A
KR950702978A KR1019950700456A KR19950700456A KR950702978A KR 950702978 A KR950702978 A KR 950702978A KR 1019950700456 A KR1019950700456 A KR 1019950700456A KR 19950700456 A KR19950700456 A KR 19950700456A KR 950702978 A KR950702978 A KR 950702978A
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compound
aryl
alkyl
hydrogen
formula
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KR1019950700456A
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앤터니 클리프 이안
채프맨 화이트 앨런
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폴 에이. 리처
존 와이어스 앤드 브라더 리미티드
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Priority claimed from GB929216649A external-priority patent/GB9216649D0/en
Priority claimed from GB939307958A external-priority patent/GB9307958D0/en
Application filed by 폴 에이. 리처, 존 와이어스 앤드 브라더 리미티드 filed Critical 폴 에이. 리처
Publication of KR950702978A publication Critical patent/KR950702978A/ko

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    • 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
    • C07D401/04—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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

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Abstract

일반식(I)의 아미드 유도체 및 약제학적으로 허용되는 이의 염은 5-HT1A결합제이며 예를 들어 불안증 치료제로서 사용될 수 있다.
상기식에서, a 및 b는 각각 0,1,2 또는 3이고, 단 a와 b의 합은 0,1,2 또는 3이며,은 임의의 이중결합이고, A는 임의로 치환된 C1-2-알킬렌 쇄이고, R은 모노 또는 비사이클릭 아릴 또는 헤테로아릴 라디칼이고, R1은 수소 또는 저급 알킬이고, R2는 아릴, 아르알킬, 헤테로아릴 또는 헤테로아릴알킬이고 -CONR3R4는 특정의 아미드 그룹을 나타낸다.

Description

아미드 유도체(Amide derivatives)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 일반식(I)의 화합물 또는 약제학적으로 허용되는 이의 산 부가염.
    상기식에서, a 및 b는 각각 0,1,2 또는 3이고, 단 a와 b의 합은 0,1,2 또는 3이며,은 a가 1이상인 경우, 환에 존재할 수 있는 임의의 이중결합이고, A는 하나 이상의 저급 알킬 그룹에 의해 임의로 치환된 탄소수 1 또는 2의 알킬렌 쇄이고, R은 모노 또는 비사이클릭 아릴 또는 헤테로아릴 라디칼이고, R1은 수소 또는 저급 알킬이고, R2는 아릴, 아릴(저급)알킬, 헤테로아릴 또는 헤테로아릴(저급)알킬 라디칼이고, R3은 수소 또는 저급 알킬이고, R4는 수소, 탄소수 1 내지 10의 알킬 그룹, 탄소수 3 내지 12의 사이클로알킬, 사이클로알킬(저급)알킬, 아릴 또는 아릴(저급)알킬이거나, R3과 R4는, 이들이 결합되어 있는 질소원자와 함께 추가의 헤테로 원자를 함유할 수 있는 포화 헤테로사이클릭 환율을 나타낸다.
  2. 제1항에 있어서, R이 임의로 치환된 페닐 라디칼인 화합물.
  3. 제1항 또는 제2항에 있어서, A가 -CH2또는 -CH2-CH2-인 화합물.
  4. 제1항 내지 제3항 중의 어느 한 항에 있어서, R2가 치환되거나 치환되지 않은 페닐인 화합물.
  5. 제1항 내지 제4항 중의 어느 한 항에 있어서, R3이 수소이고 R4가 3급 알킬 또는 사이클로알킬이거나, R3과 R4가 이들이 결합되어 있는 질소원자와 함께 피페리디노 또는 헥사하이드로아제피노를 나타내는 화합물.
  6. 제1항에 있어서, N - 사이클로헥실-3-(1-(1,2,3,6-테트라하이드로-4-(5-메톡시-1H-인돌-3-일)피리딜))-2-페닐프로판아미톤 또는 2,3,4,5,6,7-헥사하이드로-1-(4-(1-(1,2,3,6-테트라하이드로-4-(2-메톡시페닐)피리딜))-2-페닐부티릴)-1H-아제핀 또는 (+)-2,3,4,5,6,7-헥사하이드로-1-(4(1-(1,2,3,6-테트라하이드로-4-(2-메톡시페닐)피리딜))-2-페닐부티닐)-1H-아제핀 또는 약제학적으로 허용되는 이들의 산 부가염인 화합물.
  7. (a) 일반식(II)의 화합물을 일반식(III)의 그룹을 제공하는 알킬화제로 알킬화시키거나, (b) 일반식(VII)의 아민을 일반시(VIII)의 산 또는 이의 아실화 유도체로 아실화시키거나, (c) 일반식(IX)의 하이드록시 아미드를 탈수시켜 ---이 이중결합을 나타내는 일반식(I)의 화합물을 수득하거나, (d) 제1항에 따른 화합물을 거울상 이성질체로 분할하거나, (e) 제1항에 따른 염기를 약제학적으로 허용되는 염으로 전환시키거나 약제학적으로 허용되는 염을 유리 염기로 전환시킴을 포함하여, 제1항에 따른 화합물을 제조하는 방법.
    상기식에서, a 및 b는 각각 0,1,2 또는 3이고, 단, a와 b의 합은 0,1,2 또는 3이며,은 a가 1이상인 경우, 환에 존재할 수 있는 임의의 이중결합이고, A는 하나 이상의 저급 알킬 그룹에 의해 임의로 치환된 탄소수 1 또는 2의 알킬렌 쇄이고, R은 모노 또는 비사이클릭 아릴 또는 헤테로아틸 라디칼이고, R1은 수소 또는 저급 알킬이고, R2는 아릴, 아릴(저급)알킬, 헤테로아릴 또는 헤테로아릴(저급)알킬 라디칼이고, R3은 수소 또는 저급 알킬이고, R4는 수소, 탄소수 1 내지 10의 알킬 그룹, 탄소수 3 내지 12의 사이클로알킬, 사이클로알킬(저급)알킬, 아릴 또는 아릴(저급)알킬이거나, R3과 R4는, 이들이 결합되어 있는 질소원자와 함께 추가의 헤테로 원자를 함유할 수 있는 포화 헤테로사이클릭 환율을 나타낸다.
  8. 제l항에 따른 화합물을 약제학적으로 허용되는 담체와 배합된 상태로 포함하는 약제학적 조성물.
  9. 제8항에 있어서, 화합물이 제7항의 방법으로 제조되는 약제학적 조성물.
  10. 제1항에 따른 화합물을 약제학적로 허용되는 담체와 배합함을 포함하여, 약제학적 조성물을 제조하는 방법.
  11. 제1항에 있어서, 5-HT1A길항제로서 사용하기 위한 화합물.
  12. 제1항에 있어서, 항우울제, 혈압강하제, 수면/비수면 주기 조절제, 급식 거동 조절제 또는 성기능 조절제 또는 불안치료제 또는 인식 장애 치료제로서 사용하기 위한 화합물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950700456A 1992-08-05 1993-07-22 아미드 유도체(Amide derivatives) KR950702978A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB?9216649.5? 1992-08-05
GB929216649A GB9216649D0 (en) 1992-08-05 1992-08-05 Amide derivatives
GB?9307958.0? 1993-04-17
GB939307958A GB9307958D0 (en) 1993-04-17 1993-04-17 Amide derivateves
PCT/GB1993/001542 WO1994003444A1 (en) 1992-08-05 1993-07-22 Amide derivatives

Publications (1)

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KR950702978A true KR950702978A (ko) 1995-08-23

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US (1) US5585374A (ko)
EP (1) EP0664801A1 (ko)
JP (1) JPH08501287A (ko)
KR (1) KR950702978A (ko)
AU (1) AU675964B2 (ko)
CA (1) CA2141810A1 (ko)
FI (1) FI950486A (ko)
HU (2) HUT71899A (ko)
PH (1) PH31209A (ko)
TW (1) TW288017B (ko)
WO (1) WO1994003444A1 (ko)

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GB9314758D0 (en) * 1993-07-16 1993-08-25 Wyeth John & Brother Ltd Heterocyclic derivatives
GB9410512D0 (en) * 1994-05-25 1994-07-13 Smithkline Beecham Plc Novel treatment
US5525600A (en) * 1994-11-28 1996-06-11 American Home Products Corporation (Thiophen-2-yl)-piperidin or tetrahydropyridin carboxamides
US5990114A (en) * 1996-02-28 1999-11-23 Recordati, S.A., Chemical And Pharmaceutical Company Use of 5-HT1A receptor antagonists for the treatment of urinary incontinence
EP1091741A4 (en) 1998-06-30 2002-12-18 Lilly Co Eli AZEPINE DERIVATIVES PLAYING A ROLE IN SEROTONIN ASSOCIATED SYSTEMS
JP2002519321A (ja) * 1998-06-30 2002-07-02 イーライ・リリー・アンド・カンパニー セロトニン関連系に効果を有するピロリジン、及び、ピロリン誘導体
CA2336117A1 (en) * 1998-06-30 2000-01-06 Sidney Xi Liang Piperidine derivatives having effects on serotonin related systems
AU2001281738B2 (en) * 2000-07-21 2006-12-21 H.Lundbeck A/S Indole derivatives useful for the treatment of cns disorders
US6861427B2 (en) * 2001-04-26 2005-03-01 Wyeth Azabicyclylmethyl derivatives of 2,3-dihydro-1,4-dioxino[2,3-f]quinoline as 5-HT1A antagonists
ITMI20021329A1 (it) * 2002-06-14 2003-12-15 Recordati Chem Pharm Nuove ossialchilammine sostituite
US20040058962A1 (en) * 2002-06-14 2004-03-25 Amedeo Leonardi Phenylalkylamines and pyridylalkylamines

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HU9500330D0 (en) 1995-03-28
TW288017B (ko) 1996-10-11
FI950486A0 (fi) 1995-02-03
US5585374A (en) 1996-12-17
JPH08501287A (ja) 1996-02-13
FI950486A (fi) 1995-02-03
CA2141810A1 (en) 1994-02-17
PH31209A (en) 1998-05-05
HU211591A9 (en) 1995-12-28
HUT71899A (en) 1996-02-28
EP0664801A1 (en) 1995-08-02
AU675964B2 (en) 1997-02-27
AU4714593A (en) 1994-03-03
WO1994003444A1 (en) 1994-02-17

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