KR900018035A - 디아릴스티릴퀴놀린 이산 - Google Patents

디아릴스티릴퀴놀린 이산 Download PDF

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KR900018035A
KR900018035A KR1019900007608A KR900007608A KR900018035A KR 900018035 A KR900018035 A KR 900018035A KR 1019900007608 A KR1019900007608 A KR 1019900007608A KR 900007608 A KR900007608 A KR 900007608A KR 900018035 A KR900018035 A KR 900018035A
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phenyl
chloro
thio
quinolinyl
propyl
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엔. 영 로버트
고티어 자크-이브스
잼보니 로버트
엘. 벨리 마이클
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제임스 에프. 노튼
머크 프로스트 캐나다, 인코포레이티드
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Publication of KR900018035A publication Critical patent/KR900018035A/ko

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    • C07D215/14—Radicals substituted by oxygen atoms
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    • 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
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    • 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
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    • 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
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D409/12—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 chain containing hetero atoms as chain links

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Abstract

내용 없음

Description

디아릴스티릴퀴놀린 이산
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 일반식(I)의 화합물 및 이의 약제학적으로 허용되는 염.
    상기식에서, R1은 H, 할로겐, C1-C8알킬, C2-C8알케닐, C2-C8알키닐, -CF3, -SR2, -S(O)R2, -S(O)2R2, -NR3R3-OR3, -COOR3, -(C=O)R3, -C(OH)R3R3, -CN, -NO2, -N3, 치환되거나 비치환된 페닐, 치환되거나 벤질, 치환되거나 비치환된 2-펜어틸, 또는 치환되거나 비치환된 피리딜이고;R2는 C1-C8알킬, C2-C8알케닐, C2-C8알키닐,-CF3, 치환되거나 비치환된 페닐, 치환되거나 비치환된 벤질, 또는 치환되거나 비치환된 2-펜에틸이며;R3는 H 또는 R2이고;R4는 H, 할로겐, -NO2, -CN, -OR3, -SR3, -NR3R3, 또는 C1-C8알킬이며;CR3R4는 천연적으로 존재하는 아미노산의 라디칼일 수 있고;R5는 H, 할로겐, -NO2, -N3, -CN, -SR2, -NR3R3, -OR3, C1-C8알킬, -(C=O)R3, 또는 -S(O)2R2이며;R6는 -(CH2)s-C(R7R7)-(CH2)s-R5또는 -CH2CONR12R12이고;R7은 H 또는 C1-C4알킬이며;Rs은 A)핵 탄소원자 3 내지 12개 및 N,S 또는 O로 부터 선택된 핵 헤테로원자 1 또는 2개를 함유하며, 헤테로사이클릭 라디칼 중 각각의 환이 5 또는 6개의 원자로 형성되는 일환식 또는 이환식 헤테르사이클릭 라디칼, 또는 B)라디칼 W-R9이고;R9는 탄소수가 21이하이고, (1)탄화수소 라디칼이거나 (2)환 중 헤테로원자 1개 이하를 함유하는 유기 비환식 또는 일환식 카복실산의 아실 라디칼이며;R10은 -SR11, -OR12, 또는 -NR12R12이고;R11은 C1-C6알킬, -(C=O)R14치환되거나 비치환된 페닐, 또는 치환되거나 비치환된 벤질이며;R12는H,R11, 아다만틸, 나프틸, 할로겐-치환된 C1-C6알킬, 또는 C1-C6알킬렌-OR3이거나, 동일한 N에 결합된 R12그룹 2개가 O,S 또는 N으로부터 선택된 헤테로원자 2개 이하를 함유하는 5 또는 6원 환을 형성할 수 있고;R13은C1-C8일킬C2-C8일케닐, C2-C8알키닐, -CF3, 또는 비치환된 페닐, 벤질 또는 2-펜에틸이며;R14는 H 또는 R13이고;R15는 R3또는 할로겐이며;R16은 H,C1-C4알킬, 또는 OH이고;R17은 C1-C8알킬, C2-C8알케닐, C2-C8알키닐, 또는 치환되거나 비치환된 페닐, 벤질 또는 2-펜에틸이며;R18은 C1-C8알킬, C2-C8알케닐, C2-C8알키닐, -CF3, 또는 치환되거나 비치환된 페닐, 벤질 또는 2-펜에틸이고;R19는 C4-C8알킬,2-C8알케닐, C2-C8알키닐, -CF3, 또는 치환된거나 비치환된 페닐, 벤질 또는 2-펜에틸이며;R20은 H 또는 R17이고;m 및 m'는 독립적으로 0 내지 8이며; n 및 n'는 독립적으로 0 또는 1이나, 둘다 0이지는 않고; p 및 p'는 독립적으로 0내지 8이며; m+n+p는, X2가 O,S,S(O) 또는 S(O)2인 경우, 1내지 10이고; m+n+p는, X2가 CR3R16인 경우, 0내지 10이며; m'+n'+p'는, X3가 O,S,S(O) 또는 S(O)2인 경우, 1내지 10이고; m'+n'+p'는, X2가 CR3R16인 경우, 0내지 10이며; r은, Z1이 HET(-R3, -R5)인 경우, 0 또는 1이고; r은, Z1이 -CONR3이거나 n이 0인 경우, 1이며; r'는 Z2가 HET(-R3, -R5)인 경우, 0 또는 1이고; r'는, Z2가 CONR3이거나 n'가 0일 경우, 1이며; S는 0내지 3이고; Q1및 Q2는 독립적으로 -COOR3, 테트라졸, 메틸테트라졸, -COOR6, -CONHS(O)2R13, -CN, -CONR12R12, -CHO, -CH2OH, -COCH2OH, -NR4S(O)2R13, C(O)R19, -NR20C(O)OR17, -NR12C(O)NR12R12, -NR7C(O)R18, -OC(O)NR12R12, -S(O)2R18, -S(O)R18, -S(O)2NR12R12, -NO2, S-치환된 페닐,이거나, Q1또는 Q2가 COOH이고 R4가 -OH, -SH 또는 -NHR3일 경우, Q1또는 Q2와 R4및 이들이 결합되어 있는 탄소는 물을 상실하며 헤테로사이클릭 환을 형성할 수 있으며; W는 O,S, 또는 NR3이고; X1은 O,S,-S(O)-, -S(O)2-, NR3, 또는 CRR-이며; -CR3R3-이며;X2및 X3는 독립적으로 O,S,S(O),S(O)2또는 CR3R16이고;Y는 -CR3=CR3-, -C=C-, -CR3R3-X1-, -X1-CR3R3-, -CR3R3-X1-CR3R3-,, C=O,O,S 또는 NR3이며;Z1및 Z2는 독립적으로 -CONR3- 또는 -HET(-R3, -R5)-이고, 단 이들 중 적어도 하나는 -HET(-R3, -R5)-이며;HET는이다.
  2. 제1항에 있어서, 치환체가 하기와 같은 화합물.
  3. 제2항에 있어서, 2-(3-(3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)-3-(2-카복시에틸티오)프로필)벤조산, 이나트륨 염;2-(3-(3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)-3-(2-디메틸카바모일)에틸티오)프로필)벤조산, 나트륨 염; 3-(3-(2-(7-클로로퀴놀린-2-일)에틸)페닐)-(2-(디메틸카바모일)에틸티오)메틸)벤조산,나트륨염;5-(3-(3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)(2-(디메틸카바모일)에틸티오)메틸)티오펜-2-카복실산;3-((3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)(2-(디케틸카바모일)에틸티오)메틸)벤조산;4-((3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)(2-(디케틸카바모일)에틸티오)메틸)벤조산;3-((2-(카복시에틸티오)(3-(2-(7-클로로퀴놀린-2-일)에테닐)페닐)메틸)벤조산;6-(3-카복시페닐티오)-6-(3-(2--(7-클로로퀴놀린-2-일)에테닐)페닐)-3-메틸헥사노산;3-((3-((7-클로로퀴놀린-2-일메틸)옥시)페닐(2-(디메틸카바모일)엘틸티오)메틸)벤조산,나트륨염;3-((3-카복시페닐티오) (3-(2-(7-클로로퀴놀린-2-일)에테닐)메틸)벤조산;3-((3-((7-클로로퀴놀린-2-일메틸)옥시)페닐)(2-(3급-부틸카바모일)에틸티오)메틸)벤조산,나트륨염;5-((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)((3-디메틸아미노-3-옥소프로필)티오)메틸)-3-피리딘카복실산, 나트륨염;3-3'-(((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)메틸렌)비스(티오))비스(벤조산), 이나트륨 염;3-((4-카복시페닐)티오)(3-(2-(7-클로로-2-퀴놀리닐)에테닐)페닐)메틸)벤조산, 이나트륨 염;3-((3-(2-(7-클로로-2-퀴놀리닐)에테닐)페닐)((4-(디메틸아미노카보닐)페닐)티오)메틸)벤조산, 나트륨염;3-(2-((2-카복시에틸)티오)2-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)에틸)벤조산;3-(1-(3-(2-(7-클로로-2-퀴놀리닐)에테닐)페닐)-1-((2-카복시-4-피리디닐)티오)메틸)벤조산;3-(1-((2-카복시페닐)티오)-1-(3-(2-(7-클로로-2-퀴놀리닐)에테닐)페닐)메틸)벤조산, 이나트륨 염;2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐-3-((2-카복시에틸)티오)프로필)벤조산'2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((3-디메틸아미노-3-옥소프로필)티오)프로필)벤조산, 나트륨 염; 2,2'-(((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)메틸렌)비스(티오)비스 (베노산), 이나트륨 염;2-클로로-5-((3-((7-클로로-2-퀴놀리딜)메톡시)페닐)((3-디메틸아미노-3-옥소프로필)티오)메틸)벤조산, 나트륨 염;2,2'-(((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)메틸렌)비스(티오메틸)비스(벤소산), 이나트륨 염;2-((((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)((3-디메틸아미노-3-옥소프로필)티오)메틸)티오)메틸)벤조산;3-((3-(2-(7-클로로-2-퀴놀리닐)에테닐)페닐)((4-(디메틸아미노)-4-옥소프로필)티오)메틸)벤조산;2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시-페닐)-3-((2-메틸-2-프로필)아미노)-3-옥소프로필)티오)프로필)벤조산, 나트륨염; 2-(3-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-((3-((2-메틸-2-프로필)아미노)-3-옥소프로필)티오)프로필)벤조산; 3-(3-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-((3-디메틸아미노)-3-옥소프로필)티오)프로필)벤조산;2-((3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-((3-디메틸아미노-3-옥소프로필)티오)프로필)벤조산; 2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((3옥소-3-(1-트리사이클로[3,3,1,1,3,7]데실)아미노)프로필)티오)프로필)벤조산, 나트륨염;N,N-디메틸3--((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-2-(1H-테트라졸-5-일)페닐)프로필)티오)프로판아미드, 나트륨염;N,N-디메틸3--((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-2-((1H-테트라졸-5-일)메틸)페닐)프로필)티오)프로판아미드, 나트륨; 2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((3-디메틸아미노-3-옥소프로필)티오)프로필)벤젠아세트산, 나트륨염; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-디메틸아미노카보닐)페닐)프로필)티오)프로파노산, 나트륨염;N,N-디메틸3-((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-1-(3-((1H-테트라졸-5-일)메틸)페닐)메틸)티오)프로판아미드, 나트륨염; 3-(((3-카복시페닐)티오) (3-((7-클로로-2-퀴놀리닐)메톡시)페닐)메틸)벤조산, 이나트륨염; 3-(((3-((7-클로로-2-퀴놀리닐)메톡시)페닐) (3-(2-디메틸아미노-2-옥소에틸)페닐)메틸)티오)프로파노산, 나트륨염; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(4-클로로-2-(디메틸아미노카보닐)페닐)프로필)티오)프로파노산; N,N-디메틸 2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((2-(1H-테트라졸-5-일)에틸)티오)프로필)벤즈아미드, 나트륨염; N,N-디메틸 2-(3-(3-(2-(7-클로로-퀴놀리닐)에틸)페닐)-3-((2-(1H-테트라졸-5-일)프로필)티오)프로필)벤즈아미드, 나트륨염; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-(디메틸아미노카보닐)페닐)프로필)티오)-2-에틸프로파노산, 나트륨염; 3- ((1-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-(2-(1H-테트라졸-5-일)페닐)프로필)티오-2에틸 프로파노산, 이 나트륨염; 3-((1-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-(2-((4-메틸페닐설포닐아미노카보닐)페닐)프로필)티오-2-에틸프로파노산, 일나트륨염; 3-((1-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-(2-(N-메틸-1H-테트라졸-5-일)페닐)프로필)티오-2-에틸 프로파노산, 이나트륨 염; 2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((2-에틸-3-(디메틸아미노)-3-옥소-프로필-티오)프로필)벤조산, 나트륨 염; 2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-((3-아미노-2-에틸-3-옥소프로필)티오)프로필)벤조산, 나트륨 염; 3-((1-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-(2-((에톡시카보닐)아미노)페닐)프로필)티오)-2-에틸프로파노산, 나트륨 염; 3-(((3-((7-클로로-2-퀴놀리닐)메톡시)페닐) (((2-디메틸아미노카보닐)페닐)메틸)티오)메틸)티오)프로파노산, 나트륨 염; 3-((3-(2-(아미노카보닐)페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)티오)-2-메톡시프로파노산, 나트륨 염; 3-((1-(3-(2-(7-클로로-2-퀴놀리닐)에틸)페닐)-3-(2-(시아노페닐)프로필)티오)-2-에틸프로파노산, 나트륨 염; 3-((3-(4-클로로-2-(메틸아미노카보닐)페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)티오)프로파노산; 5-클로로-2-(3-((2-카복시에틸)티오)-3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)벤조산; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-(1-하이드록시아미노)에틸)페닐)프로필)티오)-2-메틸프로파노산, 나트륨 염; (+)-3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(4-클로로-2-디메틸아미노카보닐)페닐)프로필)티오)프로파노산, 나트륨염; (-)-3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시) 페닐)-3-(4-클로로-2-(디메틸아미노카보닐)페닐)프로필)티오)프로파노산, 나트륨 염; 3-((3-(4-클로로-2-((에톡시카보닐)아미노)페닐)-1-(3-((7-클로로-2-퀴놀리메톡시)페닐)프로필)티오) 프로파노산, 나트륨 염; 3-((3-(2-클로로-6-(디메틸아미노카보닐)페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)티오)-프로파노산; 3-((3(4-클로로-2-(디메틸아미노카보닐)페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)설피닐)프로파노산, 나트륨 염; 3-((3-(3-클로로-2-(디메틸아미노카보닐)페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필) 티오)프로파노산, 나트륨 염; 3-((1-(3-(7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-1H-테트라졸-5-일)프로필)티오)-2-메틸-프로파노산, 이나트륨 염; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-아미노카보닐)페닐)프로필)티오)-2-메틸프로파노산, 나트륨 염; (+) 3-((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-디메틸아미노카보닐)페닐)프로필)티오)프로파노산, 나트륨 염; (-) 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)패닐)-3-(2-디메틸아미노카보닐)페닐)프로필)티오)프로파노산, 나트륨 염; 5-브로모-2-(3-((2-카복시에틸)티오)-3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐프로필)벤조산, 이나트륨염; 3-((1-(3-7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(4-클로로-2-(디메틸아미노카보닐)페닐)프로필)티오)부타노산, 나트륨 염; 3-((1-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(5-디메틸아미노카보닐)-2-푸라닐)프로필)티오)프로파노산, 나트륨 염; 3-((3-(아세틸아미노)-4-클로로페닐)-1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)티오)프로파노산; 3-((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐-3-(4-클로로-2-(((메틸설포닐)아미노)카보닐)페닐-프로필)티오)프로파노산, 이나트륨 염; 5-클로로-2-(3-((2-카복시부틸)티오)-3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)벤조산, 이나트륨 염; ****7**** 5-클로로2-(3-((2-카복시프로필)티오)-3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)벤조산, 이나트륨 염; 5-클로로-2-(3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-카복시-2-메톡시에틸)티오)프로필)벤조산, 이나트륨 염; 2-(3-((2-카복시에틸)티오)-3-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)프로필)-5-페닐벤조산; 3-((1-3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-(디메틸아미노카보닐)-3-피리디닐)프로필)티오) 프로파노산, 나트륨 염; 3-((3-(4-클로로-2-(디메틸아미노카보닐)페닐)-1(3-(2-(7-클로로-2-퀴놀리닐)에테닐)프로필)티오)프로파노산; 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(4-클로로-2-(1H-테트라졸-5-일)페닐)프로필)티오)프로파노산, 이나트륨 염; 또는 3-((1-(3-((7-클로로-2-퀴놀리닐)메톡시)페닐)-3-(2-시아노페닐)프로필)티오)-2-메틸프로파노산, 나트륨염인 화합물.
  4. 제1항에 있어서, R1은 H, 할로겐, C1-C8알킬, -CF3, -SR2, -S(O)R2, -S(O)2R2, -OR3, 또는 -CN이고;R2가 C1-C8알킬 또는 -CF3이며;R4가 H, -OR3, SR3, -NR3R3, 또는 C1-C8알킬이고;CR3R4는 천연적으로 존재하는 아미노산의 라디칼일 수 있으며;R5가 H, 할로겐, -CN, -SR2, -OR3, C1-C8알킬, 또는 -(C=O)R3이고;R13이 C1-C8알킬, -CF3, 또는 비치환된 페닐, 벤질 또는 2-펜에틸이며;m 및 m'는 독립적으로 0 내지 4이고;p 및 p'는 독립적으로 0내지 4이며;m+n+p는 X2가 0 또는S인 경우, 1내지 10이고;m'+n'+p'는, X3가 O 또는 S인 경우, 1 내지 10이며;Q1및 Q2는 독립적으로 -COOR3, 테트라졸, -COOR6, -CONNS(O)2R13, -CONR12R12또는 -NHS(O)2R13이거나, Q1또는 Q2가 COOH이고 R4가 -OH, -SH 또는 -NHR3일 경우, Q1또는Q2와 R4및 이들이 결합되어 있는 탄소는 물을 상실하여 헤테로사이클릭환을 형성할 수 있고;W는 O,S, 또는 NH이며;X1은 O,S, -NR3, 또는 -CR3R3-이고;X2및 X3는 독립적으로 O,S, 또는 CR3R16-이고;Y는 -CR3=CR3-, -C=C-, -CR3R3-X1-, 또는 -X1-CR3R3인 화합물 및 이의 약제학적으로 허용되는 염.
  5. 제1항에 있어서, R1은 H, 할로겐, C1-C8알킬, -CF3, -SR2, -S(O)R2, -S(O)2R2, -OR3, 또는 -CN이고;R2가 C1-C8알킬 또는 -CF3이며;R4가 H, -OR3, SR3, -NR3R3, 또는 C1-C8알킬이고;CR3R4는 천연적으로 존재하는 아미노산의 라디칼이 아니며;R5가 H, 할로겐, -CN, -SR2, -OR3, C1-C8알킬, 또는 -(C=O)R3이고;R13이 C1-C8알킬, -CF3, 또는 비치환된 페닐, 벤질 또는 2-펜에틸이며;m 및 m'는 독립적으로 0 내지 4이고;p 및 p'는 독립적으로 0내지 4이며;m+n+p는 X2가 0 또는S인 경우, 1내지 10이고;m'+n'+p'는, X3가 O 또는 S인 경우, 1 내지 10이며;Q1및 Q2는 독립적으로 -COOR3, 테트라졸, 또는 -CONR12R12이고;W는 O,S, 또는 NH이며;X1은 O,S, -NR3, 또는 -CR3R3이고;X2및 X3는 독립적으로 O,S, 또는 CR3R16이며;Y는 -CH=CH-이고;Z1및 Z2는 HET(-R3,-R5)인 화합물 및 이의 약제학적으로 허용되는 염.
  6. 일반식(Ia)의 화합물.
    상기식에서, R4는 H 또는 C1-C8알킬이고;CR4R4는 천연적으로 존재하는 아미노산의 라디칼이 아니며;m은 1내지 4이고;m'는 0내지 4이며;p'는 0내지 4이고;r'는 0또는 1이며;Q1및 Q2는 독립적으로 -COOR3, 테트라졸, -CONHW(O)2R13, 또는 -CONR12R12이고;X3는 S 또는 CR3R16이며;Y는 -CH=CH- 또는 -CH2O-이고; 나머지 정의는 제4항에서와 같다.
  7. 제1항에 있어서, R1이 할로겐이고, R5가 H, 할로겐, -CN, -SR2, -S(O)2R2, 또는 -OR2이며;R7이 H 또는 C1-C4알킬이고;R21이 R7또는 -O-C1-C4알키이며;r'가 0또는 1이고;m'가 0내지 2이며;p'가 0또는 1이고;Q2가 일반식(I)에 대해 정의한 바와 같고;X3가 S 또는 CH2이며;Y가 -CH2CH2-, -CH=CH- 또는 -CH2O인 일반식(Ib)의 화합물.
  8. 치료학적 유효량의 제1항의 화합물 및 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.
  9. 제8항에 있어서, 비스테로이드성 소염 약제;말초성 진통제;사이클로옥시게나제 억제제;류코트리엔 길항제;류토트리엔 생합성 억제제;H2-수용체 길항제;항히스타민성 제제;프로스타글란딘 길항제;트롬복산 길항제;트롬복산 합성효소 억제제;및 ACE길항제로 이루어진 그룹으로부터 선택된 제2의 활성 성분을 추가로 유효량 함유하는 약제학적 조성물.
  10. 제9항에 있어서, 제2의 활성성분이 비스테로이드성 소염 약제인 약제학적 조성물.
  11. 제10항에 있어서, 제2의 활성성분에 대한 제1항의 화합물의 중량비가 약 1000:1내지1:1000인 약제학적 조성물.
  12. 포유동물에 제1항의 화합물을 유효량 투여함을 특징으로 하여, SRS-A 또는 류코트리엔의 합성, 작용 또는 방출을 예방하는 방법.
  13. 제12항에 있어서, 포유 동물이 인가인 방법.
  14. 세포보호 치료가 필요한 포유동물에 제1항의 화합물을 세포보호량 투여함을 특징으로 하여, 포유동물중에서 세포보호를 유도하는 방법.
  15. 염중 질환 치료가 필요한 포유동물에 제1항의 화합물을 치료학적 유효량 투염함을 특징으로 하여, 포유동물 중 눈의 염중 질환을 치료하는 방법.
  16. 제15항에 있어서, 포유동물이 인간인 방법.
  17. 제1항에 있어서, 치환제가 하기와 같은 화합물.
    ※ 참고사항 : 최초출원내용에 의하여 공개하는 것임.
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JP6038914B2 (ja) * 2011-07-26 2016-12-07 スン プハルマ アドバンセド リサーチ カンパニー リミテド キノリン−、キノキサリン、又はベンゾチアゾールベースのシステイニルロイコトリエンアンタゴニスト（ｌｔｃ４）
AU2014225550C1 (en) 2013-03-08 2017-08-17 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Potent and selective inhibitors of monoamine transporters; method of making; and use thereof
CN105814022B (zh) * 2013-12-09 2018-09-28 Ucb生物制药私人有限公司 作为tnf活性调节剂的稠合的二环杂芳族衍生物
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Publication number Publication date
NZ233752A (en) 1993-05-26
ATE126509T1 (de) 1995-09-15
FI902555A0 (fi) 1990-05-23
DE69021639D1 (de) 1995-09-21
NO902301L (no) 1990-11-26
AU5581190A (en) 1990-12-13
DE69021639T2 (de) 1996-02-15
EP0399818A1 (en) 1990-11-28
IL94484A0 (en) 1991-03-10
JPH0372459A (ja) 1991-03-27
CA2017376C (en) 2000-07-18
NO902301D0 (no) 1990-05-23
ZA903983B (en) 1991-03-27
PT94129A (pt) 1991-02-08
EP0399818B1 (en) 1995-08-16
JPH07103107B2 (ja) 1995-11-08
CA2017376A1 (en) 1990-11-24

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