KR870007920A - 2-치환된 퀴놀린 디오산 - Google Patents

2-치환된 퀴놀린 디오산 Download PDF

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KR870007920A
KR870007920A KR870001190A KR870001190A KR870007920A KR 870007920 A KR870007920 A KR 870007920A KR 870001190 A KR870001190 A KR 870001190A KR 870001190 A KR870001190 A KR 870001190A KR 870007920 A KR870007920 A KR 870007920A
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alkyl
halogen
independently
compound
substd
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엔. 영 로버트
잠보니 로버트
레저 세르지
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잔느씨. 브렐레
머크 프로스트 캐나다, 인코포레이티드
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Publication of KR870007920A publication Critical patent/KR870007920A/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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/18—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/36—Sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

내용 없음

Description

2-치환된 퀴놀린 디오산
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (10)

  1. 하기 일반식(Ⅰ)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서 R¹은 H, 할로겐, C₁- C8알킬, C₂-C8알케닐, C₂-C8알키닐, -CF₃, -CR², -SR², -S(O)R², -S(O)₂R², -NR²R², -CHO, -COOR², -(C=0)R², -C(CH)R²R², -CN, -NO₂, 치환되거나 비치환된 페닐, 치환되거나 비치환된 벤질, 또는 치환되거나 비치환된 펜에틸이고 ; R²는 H, C₁- C8알킬, C₂-C8알케닐, C₂-C8알키닐, -CF₃, 치환되거나 비치환된 페닐, 치환되거나 비치환된 벤질, 또는 치환되거나 비치환된 펜에틸이며, R³는 H, 할로겐 -NC₂, -CN, -OR², -SR², -NR²R² 또는 C₁-C8알킬이고 ; CR³R³는 천연 아미노산의 라디칼일 수 있으며 ; R⁴는 H, 할로겐, -NO₂, -CN, -OR², -SR², NR²R², C₁-C8알킬 또는 -(C=C)R²이고 ; R5는이며 ; R6는 H 또는 C₁-C₄알킬이고 ; R7은 3개 내지 12개의 핵탄소원자 및 1개 또는 2개의 N, S 및 O중에서 선택된 헥헤테로원자를 함유하고 헤테로사이클릭 라디칼의 각 환은 5개 또는 6개의 원자로 형성되는 모노사이클릭 또는 비사이클릭 헤테로사이클릭 라디칼이거나, 라디칼 W-R8이며 ; R8은 21개까지의 탄소원자를 함유하고, 탄화수소 라디칼이거나, 환중에 1개 이하의 헤테로원자를 함유하는 유기 아사이클릭 또는 모노사이클릭 카복실산의 아실라디칼이고 ; R9는 -OR10, -SR10또는 NR10R10이며 ; R10은 H, C₁-C8알킬, -(C=O)R11, 비치환된 페닐, 또는 비치환된 벤질이거나, 동일한 N에 결합된 2개의 R10그룹은 O, S 및 N중에서 선택된 헤테로원자 2개까지를 함유하는 5원 또는 6원환을 형성할 수 있고 ; R11은 H, C₁-C8알킬, C₂-C6알키닐, 또는 -CF₃이거나, 비치환된 페닐, 벤질 도는 펜에틸이며 ; R12는 R² 또는 할로겐이고 ; m 및 m'는 각기 독립적으로 0내지 8이며 ; n및 n'는 각기 독립적으로 0 또는 1이고 ; p및 p'는 각기 독립적으로 0내지 8이며 ; m+n+p는 1내지 10이고 ; m'+n'+p'는 1내지 10이며 ; S는 0내지 3이고 ; Q¹및 Q²는 각기 독립적으로 -COOR², 테트라졸, -COOR5, -CONHS(O)₂R11, -CN, -CONR10R10, -CHO, -CH₂OH, -COCH₂HO 또는 -NHS(O₂)R11이거나, Q¹ 또는 Q²가 COOH이고 R³는 -OH, -SH 또는 -NHR²일 경우에 Q¹ 또는 Q²및 R³와 이들이 부착된 탄소들은 물을 함유하지 않는 헤테로 사이클릭환을 형성할 수 있으며 ; W는 O, S 또는 NH이고 ; X¹은 O, S, -S(O)-,-S(O)₂-,-NR², 또는 -CR²R²-이며 ; X²및 X³는 각기 독립적으로 O, S, S(O), 또는 S(O)₂이고 ; Y는 -CR²=CR²-, -C≡C-,-CR²R²-X¹-, -X¹-CR²R²-, -CR²R²-X¹-CR²R ²-,C=O,-또는
    NR²이며 Z¹및 Z²는 각기 독립적으로 -CONR²-이다.
  2. 제1항에 있어서, 하기 일반식(Ⅰa)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서 Y는 -CR²=CR²-,-C≡C,-CR₂²O- 또는 -CR₂²S-이고 ; 다른 치환체들은 일반식(Ⅰ)에서 정의한 바와 같다.
  3. 제1항에 있어서, 하기 일반식(Ⅰb)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서 R¹은 H, 할로겐, C₁-C₃ 알킬, -CF₃ 또는 SCF₃이고 ; R²는 H,C₁-C₃ 알킬, C₂-C₃ 알케닐 또는 -CF₃이며 ; X²및 X³는 각기 독립적으로 O 또는 S이고 ; 다른 치환체들은 일반식(Ⅰ)에서 정의한 바와 같다.
  4. 제1항에 있어서, 하기 일반식(Ⅰc)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서 R¹은 H, 할로겐, C₁-C₃ 알킬, -CF₃ 또는 SCF₃이고 ; R²는 H,C₁-C₃ 알킬, C₂-C₃ 알케닐 또는 -CF₃이며 ; X²및 X³는 각기 독립적으로 O 또는 S이고 ; 다른 치환체들은 일반식(Ⅰ)에서 정의한 바와 같다.
  5. 제1항에 있어서, 하기 일반식(Ⅰd)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서 R¹은 H, 할로겐, C₁-C₃ 알킬, CF₃ 또는 SCF₃이고 ; R²는 H,C₁-C₃ 알킬, C₂-C₃ 알케닐 또는 -CF₃이며 ; X²및 X³는 각기 독립적으로 O 또는 S이고 ; Y는 -CR₂²O- 또는 -CR₂²S-이며 ; 다른 치환체들은 일반식(Ⅰ)에서 정의한 바와 같다.
  6. 제1항에 있어서, 하기 일반식(Ⅰe)의 화합물.
  7. 제6항에 있어서, 실시예 4,6,13,16,27 또는 28의 화합물.
  8. 제1항의 화합물 류코트리엔 길항제로서의 유효량 및 약제학적으로 허용되는 담체로 이루어진, 포유동물의 류코트리엔 작용을 길항시키는데 유용한 약제학적 조성물.
  9. 제8항에 있어서, 비스테로이드성 항염증성 약제, 말단 진통제, 사이클로옥시게나제 억제제, 류코트리엔 길항제, 류코트리엔 억제제, H₂-수용체 길항제, 항히스타민제, 프로스글란딘 길항제, 트롬복산 길항제 및 세로토닌 길항제로 이루어진 그룹중에서 선택된 제2의 활성성분 유효량을 추가로 함유하는 약제 조성물.
  10. 포유동물에게 제1항의 화합물 유효량을 투여함을 특징으로하여, 포유동물에게 SRS-A 또는 류코트리엔 D₄의 합성, 작용 또는 방출을 예방하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR870001190A 1986-02-14 1987-02-13 2-치환된 퀴놀린 디오산 KR870007920A (ko)

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CA501932 1986-02-14
CA501932 1986-02-14

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EP (1) EP0233763B1 (ko)
JP (1) JPH0686432B2 (ko)
KR (1) KR870007920A (ko)
AT (1) ATE60584T1 (ko)
AU (1) AU595286B2 (ko)
DE (1) DE3767730D1 (ko)
DK (1) DK168534B1 (ko)
ES (1) ES2031498T3 (ko)
GR (1) GR3001474T3 (ko)
IE (1) IE59889B1 (ko)
IL (1) IL81569A (ko)
NZ (1) NZ219249A (ko)
PT (1) PT84287B (ko)
ZA (1) ZA871064B (ko)

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GB8728051D0 (en) * 1987-12-01 1988-01-06 Leo Pharm Prod Ltd Chemical compounds
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US4883878A (en) * 1988-02-08 1989-11-28 Merck & Co. Inc. Process for unsymmetrical dithioacetals and dithioketals
EP0349062A1 (en) * 1988-06-27 1990-01-03 Merck Frosst Canada Inc. Quinoline ether alkanoic acid
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US4996214A (en) * 1990-06-28 1991-02-26 Smithkline Beecham Corporation Quinolinyl substituted phenyl/thioalkanoic acid substituted propionic acids and leucotriene antagonist use thereof
DE19875039I2 (de) * 1990-10-12 2003-05-22 Merck Frosst Canada Inc Ungesaettigte Hydroxyalkylchinolinsaeuren als Leukotrien-Antagonisten
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DE69113735T2 (de) * 1990-10-12 1996-06-13 Merck Frosst Canada Inc Hydroxyalkylchinolin Äther Säure als Leukotrien-Antagoniste.
US5266568A (en) * 1990-10-12 1993-11-30 Merck Frosst Canada, Inc. Hydroxyalkylquinoline ether acids as leukotriene antagonists
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US5276044A (en) * 1991-08-14 1994-01-04 Allergan, Inc. Leukotriene receptor antagonist and antihistamine complex pharmaceutical compositions
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US20030216571A1 (en) * 1999-12-28 2003-11-20 Yoshiaki Kuroki Tricyclic compounds

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JPS62258363A (ja) 1987-11-10
NZ219249A (en) 1990-07-26
ATE60584T1 (de) 1991-02-15
ES2031498T3 (es) 1992-12-16
PT84287B (pt) 1989-09-14
EP0233763B1 (en) 1991-01-30
IL81569A (en) 1991-11-21
EP0233763A3 (en) 1988-10-19
DK168534B1 (da) 1994-04-18
DK72287D0 (da) 1987-02-13
AU595286B2 (en) 1990-03-29
GR3001474T3 (en) 1992-10-08
ZA871064B (en) 1987-10-28
IE870334L (en) 1987-08-14
PT84287A (en) 1987-03-01
DE3767730D1 (de) 1991-03-07
EP0233763A2 (en) 1987-08-26
AU6871787A (en) 1987-08-20
DK72287A (da) 1987-08-15
IL81569A0 (en) 1987-09-16
IE59889B1 (en) 1994-04-20
JPH0686432B2 (ja) 1994-11-02

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