KR900014387A - 디아제핀 항알레르기제 - Google Patents

디아제핀 항알레르기제 Download PDF

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KR900014387A
KR900014387A KR1019900003870A KR900003870A KR900014387A KR 900014387 A KR900014387 A KR 900014387A KR 1019900003870 A KR1019900003870 A KR 1019900003870A KR 900003870 A KR900003870 A KR 900003870A KR 900014387 A KR900014387 A KR 900014387A
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methyl
alkyl
pyrid
ring
phenyl
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KR920003981B1 (ko
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쿠퍼 켈빈
조나산 프레이 마이클
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데이비드 죤 우드
화이자 인코포레이티드
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    • 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
    • C07D401/10—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 aromatic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
    • C07D403/10—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 aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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Abstract

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Description

디아제핀 항알레르기제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 일반식(Ⅰ),(Ⅱ) 또는 (Ⅲ)의 화합물 및 약제학적으로 허용되는 이의 염.
    상기식에서, A는 융합된 벤젠, 피리딘, 나프탈렌, 퀴놀린, 티오펜, 벤조티오펜, 피라졸 또는 이소티아졸 환으로서, 환(들)은 C1-C4알킬, C4-C7사이클로알킬, 할로, 퍼플루오로-(C1-C4알킬), 시아노 (C1-C4알콕시)-카보닐, 니트로, 아미노 (C1-C4알킬)설포닐에 의해 치환된 아미노, (C1-C4알킬) 옥살릴에 의해 치환된 아미노, C1-C4알콕시-(C1-C4알킬)아미노, 하이드록시(C1-C4알킬), (C1-C4알콕시)-C1-C4알킬, (C1-C4알콕시)-(C2-C4알콕시)-C1-C4알킬, -CONR5R6(여기서, R5및 R6는 각각 독립적으로 H 또는 C1-C6알킬이거나, R5는 H 또는 C1-C4알킬이고 R6는 C3-C7사이클로알킬 또는 2-피리딜이거나, R5및 R6는 이들이 결합된 질소원자와 함께 모르폴리노, 피롤리디노 또는 피페리디노그룹을 형성한다), 및 할로겐, 시아노, 트리플루오로 메틸, (C1-C4알콕시)카보닐 또는 카바모일에 의해 임의 치환된 페닐, 티에닐 또는 피리딜중에서 독립적으로 선택된 1 또는 2개의 치환체에 의해 임의 치환되며, X는 O,S 또는 NH이고, Y는 1,4-페닐렌 또는 구조식의 그룹이며, R1은 H또는 페닐, 할로페닐, 피리딜, (C1-C4알콕시) 카보닐 및 디-(C1-C4알킬)아미노 중에서 선택된 치환체에 의해 임의 치환된 C1-C4알킬이거나, 하이드록실 또는 1 또는 2개의 C1-C4알콕시 그룹에 의해 치환된 C2-C4알킬이거나, (CH2)nCONR7R8(여기서 n은 1내지4이고, R7및 R8은 각각 독립적으로 H 또는 C1-C4알킬이다)이고, R2는 H 또는 C1-C4알킬이며, R3는 H 또는 C1-C4알킬이고, B는 1 내지 4개의 질소원자를 함유하는 융합된 5-원헤테로사이클릭 환 또는 2개의 질소원자를 함유하는 융합된 6-원 헤테로사이클릭 환으로서, 상기 5-또는 6-원 환은 C1-C4알킬, C1-C4할로알킬, 할로 및 옥소중에서 독립적으로 선택된 1 또는 2개의 치환체에 의해 임의 치환되며, “Het”는 2 또는 3개의 질소원자를 함유하는 5-원 방향족 헤테로사이클릭 환이거나 피리딘 환으로서, 상기 환은 벤젠 또는 피리딘 환에 또는 추가의 5-원 방향족 헤테로사이클릭 환에 임의로 융합될 수 있고, 하나 이상의 상기 헤테로사이클릭 환은 임의로 황 또는 산소원자를 함유하며, 하나 이상의 상기 환은 C1-C4알킬, C1-C4알콕시, 할로, CF3, CN 및 포르밀 중에서 독립적으로 선택된 1내지 3개의 치환체로 임의치환되고, 점선은 임의의 결합을 나타낸다.
  2. 제 1항에 있어서, A가 융합된 벤젠, 디메틸 벤젠, 디클로로벤젠, 니트로벤젠, 아닐린, 플루오로벤젠, 클로로-벤젠, 피리딘, 퀴놀린, 메틸피리딘, 디메틸피리딘, 에톡시카보닐피리딘, 피리드-2-일 카바모일피리딘, 모르폴리노카보닐피리딘, 디에틸카바모일피리딘, 3급-부틸 카바모일피리딘, 티오펜, 2-메톡시카보닐-5-메틸-티오펜, 1-메틸-3-페닐-피라졸, 1-페닐-3-메틸피라졸, 1,2-디메틸 피라졸, 1,3-디메틸피라졸, 1-피리드-2-일-3-메틸-피라졸, 1-3급-부틸-3-메틸피라졸, 1-(2-하이드록시에틸)-3-메틸피라졸, 1-메틸-3-피리드-3-일피라졸, 1-메틸-3-피리드-4-일피라졸, 1-메틸-3-피리드-2-일피라졸, 1-(2-하이드록시 에틸)-3-페닐-피라졸, 3-(2-메톡시에톡시)메틸-1-메틸피라졸, 1-메틸-3-사이클로헥실-피라졸, 1-메틸-3-하이드록시-메틸피라졸, 3-사이클로헥실피라졸, 1-메틸-3-(3-이소부톡시메틸)피라졸, 1-메틸-3-(4-클로로페닐)피라졸, 1-메틸-3-이소프로필피라졸, 1-피리드-2-일-3-페닐피라졸, 1-메틸-3-(2-클로로페닐)피라졸, 1-메틸-3-(3-트리플루오로메틸)페닐피라졸, 1-메틸-3-티에닐피라졸, 브로모피리딘, 1-에톡시-에틸이미노벤젠, N-에틸설폭시아닐린, 3-메틸이소티아졸 또는 에톡시카보닐카브아미도 벤젠환인 화합물.
  3. 제 1항 또는 2항에 있어서, R1이 H, 메틸, 에틸, 벤질, 4-클로로벤질, -CH2CO2Et, -CH2CH2N(CH3)2, -CH2CON(CH3)2, -CH2CH2CH(OCH3)2또는 4-하이드록시부틸인 화합물.
  4. 제 1항 또는 2항에 있어서, 융합된 환B가 이미다졸, 메틸이미다졸, 트리아졸, 메틸트리아졸, 트리플루오로메틸트리아졸, 트리아졸론, 테트라졸, 피리미돈, 이미다졸린 또는 테트라하이드로 피리미딘 환인 합성물.
  5. 제 1항 내지 4항중 어느 한 항에 있어서, R2및 R3가 독립적으로 수소 또는 메틸인 화합물.
  6. 제 1항 내지 5항중 어느 한 항에 있어서, “Het”가 디메틸피리딜 1또는 2개의 C1-C4알킬 그룹에 의해 임의로 치환된 1,2,4-트리아졸릴, 또는 C1-C4알킬, 할로 및 프로밀 중에서 선택된 3개 이하의 그룹으로 임의 치환되거나 C1-C4알킬 또는 CF3그룹으로 임의 치환되고 벤젠, 티아졸 또는 피리딘 환에 융합된 이미다졸릴인 화합물.
  7. 제 6항에 있어서, Het가 2-메틸-이미다조[4,5-c]피리드-1-일, 2,4,6-트리메틸이미다조[4,5-c]피리드-1-일, 3,5-디메틸-1,2,4-트리아졸-4-일, 1,6-디메틸피리드-3-일, 5-클로로-2-메틸-이미다졸-1-일, 5-클로로-4-포르밀-2-메틸이미다조-1-일 또는 4-메틸이미다조[2,1-b]티아졸-5-일인 화합물.
  8. 8,9-디클로로-5-[4-(2-메틸-1H-이미다조[4,5-c]피리드-1-일)페닐]-4H-이미다조[1,2-a][1,5]벤조디아제핀, 8,9-디클로로-1-메틸-5-[4-(2-메틸-이미다조[4,5-c]피리드-1-일)페닐]-4H-이미다조[1,2-a][1,5]벤조디아제핀, 3,5-디하이드로-2-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-5,7,9-트리메틸-1H-피리도[2,3-b][1,4]디아제핀-4-온, 8-브로모-3,5-디하이드로-1-메틸-2-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-4H-피리도[2,3-b][1,4]디아제핀-4-온, 1,3-디하이드로-1,8-디메틸-6-메톡시카보닐-4-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-2H-티에노[3,4-b]디아제핀-2-온,5-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-1,6,7,8-테트라하이드로-1,3,8-트리메틸-피라졸로[3,4-b][1,4]디아제핀-7-온, 3-사이클로헥실-1,8-디메틸-5-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-1,6,7,8-테트라하이드로피라졸로[3,4-b][1,4]디아제핀-7-온, 8-브로모-S-[4-(2-메틸이미다조[4,5-c]피리드-1-일)페닐]-4H-이미다조-[1,2-a]피리도[2,3-b][1,4]디아제핀, 또는 1,6,7,8-테트라하이드로-1,8-디메틸-5-[4-(2-메틸-1H-이미다조[4,5-c]피리드-1-일)페닐]-7-옥소-3-(3-피리딜)피라졸로[3,4-b][1,4]-디아제핀 및 약제학적으로 허용되는 이들의 염.
  9. 제 1항 내지 8항에 있어서, 약제에 사용하기 위한 화합물.
  10. 혈소판 활성화 인자 길항용 약제 제조를 위한 제 1항 내지 8항중 어느 한 항에 따르는 화합물의 용도.
  11. 제 1항 내지 8항중 어느 한 항에 따르는 화합물 및 약제학적으로 허용되는 희석제 또는 담체를 함유함을 특징으로 하는 약제.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900003870A 1989-03-23 1990-03-22 디아제핀 항알레르기 화합물 KR920003981B1 (ko)

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Application Number Priority Date Filing Date Title
GB8906813.4 1989-03-23
GB89068134 1989-03-23
GB898906813A GB8906813D0 (en) 1989-03-23 1989-03-23 Therapeutic agents
GB898926246A GB8926246D0 (en) 1989-11-21 1989-11-21 Therapeutic agents
GB8926246.3 1989-11-21

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KR900014387A true KR900014387A (ko) 1990-10-23
KR920003981B1 KR920003981B1 (ko) 1992-05-21

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IE901055L (en) 1990-09-23
EP0389189A3 (en) 1991-08-21
FI901441A0 (fi) 1990-03-22
IL93776A (en) 1994-10-21
AU627286B2 (en) 1992-08-20
PH27513A (en) 1993-08-18
ES2052172T3 (es) 1994-07-01
HUT61006A (en) 1992-11-30
JPH0314577A (ja) 1991-01-23
PT93526B (pt) 1996-08-30
CA2012666A1 (en) 1990-09-23
DE69008906D1 (de) 1994-06-23
ATE105839T1 (de) 1994-06-15
NZ233047A (en) 1992-06-25
US5008263A (en) 1991-04-16
DK0389189T3 (da) 1994-06-20
CA2012666C (en) 1997-01-28
CN1045783A (zh) 1990-10-03
NO901329D0 (no) 1990-03-22
FI98463B (fi) 1997-03-14
MY106322A (en) 1995-05-30
NO175151B (no) 1994-05-30
YU47344B (sh) 1995-01-31
HU901794D0 (en) 1990-06-28
JPH0684371B2 (ja) 1994-10-26
FI98463C (fi) 1997-06-25
NO901329L (no) 1990-09-24
EP0389189B1 (en) 1994-05-18
IL93776A0 (en) 1990-12-23
AU5214890A (en) 1990-11-01
NO175151C (no) 1994-09-07
IE62857B1 (en) 1995-03-08
EP0389189A2 (en) 1990-09-26
YU56390A (sh) 1992-12-21
PT93526A (pt) 1990-11-07
KR920003981B1 (ko) 1992-05-21
DE69008906T2 (de) 1994-08-25

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