KR950703558A - 세로토닌 수용체 작용제(Serotonin Receptor Agents) - Google Patents

세로토닌 수용체 작용제(Serotonin Receptor Agents) Download PDF

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KR950703558A
KR950703558A KR1019950701026A KR19950701026A KR950703558A KR 950703558 A KR950703558 A KR 950703558A KR 1019950701026 A KR1019950701026 A KR 1019950701026A KR 19950701026 A KR19950701026 A KR 19950701026A KR 950703558 A KR950703558 A KR 950703558A
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hydrogen
compound according
alkyl
administering
patient
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KR1019950701026A
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KR100195809B1 (ko
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로날드 씨. 베르노타즈
제프리 에스. 스프로우즈
시엔 씨. 쳉
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스티븐 엘. 네스비트
메렐 다우 파마슈티칼스 인크.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • 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
    • A61P25/04—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
    • 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
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/58—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 hetero ring
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2

Abstract

본 발명은 세로토닌 5HT1A및 5HT1D수용체 작용제인 신규한 부류의 2-임의 치환된 -4-피페라진-벤조티오펜 유도체에 관한 것이다.

Description

세로토닌 수용체 작용제(Serotonin Receptor Agents)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (15)

  1. 하기 일반식(I)의 화합물 및 이의 제약상 허용되는 부가염.
    상기식에서 Y는 수소 또는 C1-3알킬이고; R은 수소, C1-4알킬, C1-4알콕시, 할로겐, -CF3, -OCF3및 -OH로 이루어진 군으로부터 선택된 치환체이며;R1은 수소, 시클로알킬, C1-6알킬, 임의 치환된 페닐, 페닐알킬 또는 페닐아미도알킬이고;X는 수소, -(CH2)nX1, -CH=CHX1또는 -CHX2-(CH2)q-CH3이며; n은 정수 0내지 2이고;q는 정수 0또는 1이며;X1은 -OH, -OR2, -NR2R3, -CO2R2, -CONR2R3, -CN 또는 -CHR2이고;R2및 R3는 서로 독립적으로 수소, C1-4알킬, 임의 치환된 페닐, 페닐알킬이거나, 또는 R2및 R3가 함께 (CH2)m시클로알킬(여기서, m은 2내지 6임)을 형성하며;X2는 -OR4또는 -NR4R5(여기서, R4및 R5는 서로 독립적으로 수소 또는 C1-4알킬임)이고; 단, n이 0이거나 X가 -CH-CHX1일 때, X1은 OH, OR2또는 NR2R3가 아니다.
  2. 제1항에 있어서, R1이 페닐알킬인 화합물.
  3. 제2항에 있어서, Y가 H인 화합물.
  4. 제3항에 있어서, X가 CH2OH인 화합물.
  5. 제2항에 있어서, X가 CONR2R3(여기서, R2및 R3는 각각 독립적으로 H 또는 C1-4알킬임)인 화합물.
  6. 제1항에 따른 화합물을 항우울 유효량 투여하는 것으로 이루어지는 우울증의 치료 방법.
  7. 제1항에 따른 화합물을 불안해소 유효량 투여하는 것으로 이루어지는 불안증의 치료 방법.
  8. 제1항에 따른 화합물을 처리가 필요한 환자에게 투여하는 것으로 이루어지는 5HT1A또는 5HT1D수용체에서 효능제 효과를 일으키는 방법.
  9. 유효량의 제1항에 따른 화합물을 고혈압 환자에게 투여하는 것으로 이루어지는 고혈압의 치료 방법.
  10. 유효량의 제1항에 따른 화합물을 편두통 환자에게 투여하는 것으로 이루어지는 편두통의 치료 방법.
  11. 제1항에 따른 화합물을 투여하는 것으로 이루어지는, 진통이 필요한 환자에게 진통 효과를 일으키는 방법.
  12. 제1항에 따른 화합물을 발작 환자에게 투여하는 것으로 이루어지는 발작의 치료 방법.
  13. 제1항에 따른 화합물을 아기나 환자에게 투여하는 것으로 이루어지는 앙기나의 치료 방법.
  14. 제1항에 따른 화합물과 불활성 담체와의 혼합물로 이루어진 조성물.
  15. 제10항에 있어서, 제약 조성물인 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950701026A 1992-09-17 1993-09-17 세로토닌 수용체 작용제 KR100195809B1 (ko)

Applications Claiming Priority (10)

Application Number Priority Date Filing Date Title
US94700792A 1992-09-17 1992-09-17
US07/947007 1992-09-17
US7/947007 1992-09-17
US7969293A 1993-06-17 1993-06-17
US8/079692 1993-06-17
US08/079692 1993-06-17
US8/119791 1993-09-15
US08/119,791 US5436246A (en) 1992-09-17 1993-09-15 Serotonin receptor agents
US08/119291 1993-09-15
PCT/US1993/008865 WO1994006789A1 (en) 1992-09-17 1993-09-17 Serotonin receptor agents

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KR950703558A true KR950703558A (ko) 1995-09-20
KR100195809B1 KR100195809B1 (ko) 1999-06-15

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US (1) US5436246A (ko)
EP (1) EP0660832B1 (ko)
JP (1) JP3298107B2 (ko)
KR (1) KR100195809B1 (ko)
AT (1) ATE162190T1 (ko)
AU (1) AU671494B2 (ko)
CA (1) CA2144947C (ko)
DE (1) DE69316377T2 (ko)
ES (1) ES2112434T3 (ko)
FI (1) FI951249A (ko)
GR (1) GR3026297T3 (ko)
HU (1) HU222725B1 (ko)
NO (1) NO310461B1 (ko)
NZ (1) NZ256561A (ko)
WO (1) WO1994006789A1 (ko)

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JP3298107B2 (ja) 2002-07-02
HU9500796D0 (en) 1995-05-29
CA2144947A1 (en) 1994-03-31
KR100195809B1 (ko) 1999-06-15
AU671494B2 (en) 1996-08-29
NZ256561A (en) 1996-06-25
ES2112434T3 (es) 1998-04-01
CA2144947C (en) 2000-02-01
JPH08501559A (ja) 1996-02-20
FI951249A0 (fi) 1995-03-16
GR3026297T3 (en) 1998-06-30
DE69316377T2 (de) 1998-08-27
NO951015L (no) 1995-05-15
US5436246A (en) 1995-07-25
EP0660832B1 (en) 1998-01-14
NO951015D0 (no) 1995-03-16
EP0660832A1 (en) 1995-07-05
HU222725B1 (hu) 2003-09-29
DE69316377D1 (de) 1998-02-19
FI951249A (fi) 1995-03-16
HUT72662A (en) 1996-05-28
ATE162190T1 (de) 1998-01-15
WO1994006789A1 (en) 1994-03-31
AU5132193A (en) 1994-04-12
NO310461B1 (no) 2001-07-09

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