KR927003552A - Substituted benzoyl benzene-, biphenyl- and 2-oxazole-alkanoic acid derivatives as PLA2 and lipoxygenase inhibitors - Google Patents

Substituted benzoyl benzene-, biphenyl- and 2-oxazole-alkanoic acid derivatives as PLA2 and lipoxygenase inhibitors Download PDF

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KR927003552A
KR927003552A KR1019920700970A KR920700970A KR927003552A KR 927003552 A KR927003552 A KR 927003552A KR 1019920700970 A KR1019920700970 A KR 1019920700970A KR 920700970 A KR920700970 A KR 920700970A KR 927003552 A KR927003552 A KR 927003552A
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phenyl
lower alkyl
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oxazole
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아크투로 페일리 아메데오
프랭크 크레프트 3세 안토니
헨리 머서 죤
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이건 이. 버그
아메리칸 홈 프로덕츠 코포레이션
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Abstract

내용 없음No content

Description

PLA2및 리폭시게나제 억제제로서의 치환된 벤조일 벤젠-, 비페닐- 및 2-옥사졸-알칸산 유도체Substituted benzoyl benzene-, biphenyl- and 2-oxazole-alkanoic acid derivatives as PLA 2 and lipoxygenase inhibitors

[도면의 간단한 설명][Brief Description of Drawings]

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (11)

하기 일반식의 화합물 및 약리학적으로 허용가능한 이의 염.Compounds of the general formula and pharmacologically acceptable salts thereof. A (CH2)mO-BA (CH 2 ) m OB 상기식에서, A는 페녹시에틸, 페녹시페닐 또는 일반식Wherein A is phenoxyethyl, phenoxyphenyl or a general formula (여기서, X는 -N- 또는이며;Where X is -N- or Is; Z는-S- 또는 -O- 이고;Z is -S- or -O-; R1은 수소, 저급 알킬 또는 페닐이며; R2는 수소 또는 저급 알킬이거나 또는 R1및 R2가 함께 벤젠환을 형성하고; R3는 수소 또는 저급 알킬이다)의 그룹이며; n은 1 내지 2이고; B는R 1 is hydrogen, lower alkyl or phenyl; R 2 is hydrogen or lower alkyl or R 1 and R 2 together form a benzene ring; R 3 is hydrogen or lower alkyl; n is 1 to 2; B is (여기서, R4및 R5는 각각 독립적으로 수소 또는 저급 알킬이며; R6은 할로 또는 니트로이고;Wherein R 4 and R 5 are each independently hydrogen or lower alkyl; R 6 is halo or nitro; R7은또는이며; R8은 저급 알킬이고; m은 0 내지 3이다)이다.R 7 is or Is; R 8 is lower alkyl; m is 0 to 3). 제1항에 있어서, 1-[2-니트로-4'-(2-퀴놀리닐메톡시)-[1, 1'-비페닐]-4-일]에탄온인 화합물.A compound according to claim 1, which is 1- [2-nitro-4 '-(2-quinolinylmethoxy)-[1,1'-biphenyl] -4-yl] ethanone. 제1항에 있어서, 2-플루오로-4'-(2-퀴놀리닐메톡시-[1,1'-비페닐]-4-아세트산인 화합물.The compound of claim 1, which is 2-fluoro-4 '-(2-quinolinylmethoxy- [1,1'-biphenyl] -4-acetic acid. 제1항에 있어서, 3-[4-(2-퀴놀리닐메톡시)벤조일]벤젠 아세트산인 화합물.The compound of claim 1, which is 3- [4- (2-quinolinylmethoxy) benzoyl] benzene acetic acid. 제1항에 있어서, 3-[4-(2-나프탈레닐-메톡시)벤조일]벤젠 아세트산인 화합물.The compound of claim 1, which is 3- [4- (2-naphthalenyl-methoxy) benzoyl] benzene acetic acid. 제1항에 있어서, 5-페닐-4-[4-(2-퀴놀리닐메톡시)-페닐]-2-옥사졸 프로판산인 화합물.The compound of claim 1, which is 5-phenyl-4- [4- (2-quinolinylmethoxy) -phenyl] -2-oxazole propanoic acid. 제1항에 있어서, 4-[4-[2-나프탈레닐-메톡시]페닐]-5-페닐-2-옥사졸 프로판산인 화합물.The compound of claim 1, which is 4- [4- [2-naphthalenyl-methoxy] phenyl] -5-phenyl-2-oxazole propanoic acid. 제1항에 있어서, 4-[4-[2-나프탈레닐-메톡시]페닐]-5-페닐-2-옥사졸 프로판산 메틸에스테르인 화합물.A compound according to claim 1, which is 4- [4- [2-naphthalenyl-methoxy] phenyl] -5-phenyl-2-oxazole propanoic acid methylester. 제1항에 있어서, 4-[4-[(1-메틸-1H-벤즈이미다졸-2-일)메톡시]페닐]-5-페닐-2-옥사졸 프로판산인 화합물.The compound of claim 1, which is 4- [4-[(1-methyl-1H-benzimidazol-2-yl) methoxy] phenyl] -5-phenyl-2-oxazole propanoic acid. a)하기 일반식(I), (II), (III) 또는 (IV)의 화합물을 일반식 A(CH2)n-X(여기서, A 및 n은 제1항에서 정의한 바와 같고, X는 이탈 그룹이다)의 화합물로 에테르화하고 경우에 따라 생성물을 가수분해하여 R5가 수소 또는 저급 알킬인 생성물을 수득하거나; b)-COOR5(여기서, R5는 저급 알콕시이다)잔기를 갖는 일반식(I), (II), (III) 또는 (IV)의 화합물을 가수분해하여 R5가 수소인 화합물 또는 약리학적으로 허용 가능한 이의 염을 수득하거나; c)일반식(I), (II), (III) 또는 (IV)의 화합물을 약리학적으로 허용가능한 이의 염으로 전환시킴을 특징으로 하여, 제1항에 따른 화합물을 제조하는 방법.a) A compound of the general formula (I), (II), (III) or (IV) is represented by the general formula A (CH 2 ) nX wherein A and n are as defined in claim 1 and X is a leaving group Ether) and optionally hydrolyze the product to obtain a product wherein R 5 is hydrogen or lower alkyl; b) a compound or pharmacological agent wherein R 5 is hydrogen by hydrolyzing the compound of formula (I), (II), (III) or (IV) with the residue COCO 5 , wherein R 5 is lower alkoxy To obtain an acceptable salt thereof; c) A process for preparing a compound according to claim 1, characterized in that the compound of formula (I), (II), (III) or (IV) is converted into a pharmacologically acceptable salt thereof. 상기식에서 R4, R6및 m은 제1항에서 정의한 바와 같고;Wherein R 4 , R 6 and m are as defined in claim 1; R7은또는이며; -COOR6는 에스테르 작용기이다.R 7 is or Is; -COOR 6 is an ester functional group. 제10항에 있어서, 실제로 실시예 1C, 2F, 2G, 3G, 3H, 4A, 4B, 5F, 5G, 6A, 6B, 7A 및 7B중 어느한 실시예에서 기술되고 예증된 바와 같은 방법.The method of claim 10, as actually described and illustrated in any one of Examples 1C, 2F, 2G, 3G, 3H, 4A, 4B, 5F, 5G, 6A, 6B, 7A, and 7B. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920700970A 1989-10-27 1990-10-27 Substituted benzoyl benzene-, biphenyl- and 2-oxazole-alkanoic acid derivatives as PLA2 and lipoxygenase inhibitors KR927003552A (en)

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US42767789A 1989-10-27 1989-10-27
US7/427.677 1989-10-27
PCT/US1990/006252 WO1991006538A1 (en) 1989-10-27 1990-10-27 Substituted benzoylbenzene-, biphenyl- and 2-oxazole- alkanoic acid derivatives as inhibitors of pla2 and lipoxygenase

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US5021576A (en) * 1989-10-27 1991-06-04 American Home Products Corporation 2-Anilino phenylacetic acid derivatives
US5229516A (en) * 1989-10-27 1993-07-20 American Home Products Corporation Substituted indole-, indene-, pyranoindole- and tetrahydrocarbazole-alkanoic acid derivatives as inhibitors of PLA2 and lipoxygenase
US5290798A (en) * 1991-09-30 1994-03-01 Merck Frosst Canada, Inc. (hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5190968A (en) * 1991-09-30 1993-03-02 Merck Frosst Canada, Inc. (Polycyclic-arylmethoxy) indoles as inhibitors of leukotriene biosynthesis
US5308850A (en) * 1991-09-30 1994-05-03 Merck Frosst Canada, Inc. (Bicyclic-hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
US5374635A (en) * 1993-03-29 1994-12-20 Merck Frosst Canada, Inc. Furo[3,2-b]pyridines and thieno[3,2-b]pyridines as inhibitors of leukotriene biosynthesis
AU684316B2 (en) * 1993-10-15 1997-12-11 Shionogi & Co., Ltd. Oxazolinone derivative having intracellular phospholipase A2 inhibitor activity
IL141786A0 (en) * 1998-09-17 2002-03-10 Bristol Myers Squibb Co A pharmaceutical composition for treating diabetes containing an ap2 inhibitor
US20070043512A1 (en) * 2003-03-26 2007-02-22 Michael Rolph Therapeutic and prophylactic compositions and uses therefor

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US1710984A (en) * 1923-03-14 1929-04-30 Ingram Harry Closure for tumblers, jars, and other containers
US3578671A (en) * 1967-11-06 1971-05-11 Wyeth John & Brother Ltd Oxazoles
US4659728A (en) * 1985-02-25 1987-04-21 American Home Products Corporation Hydroxy substituted 4,5-diphenyl-2-oxazole propanoic acid
US4681940A (en) * 1985-11-19 1987-07-21 American Home Products Corporation 5-[3-[[2-quinolyl]methoxy]phenyl]-1,3-oxazoles
US4920132A (en) * 1987-11-03 1990-04-24 Rorer Pharmaceutical Corp. Quinoline derivatives and use thereof as antagonists of leukotriene D4
US4920133A (en) * 1987-11-03 1990-04-24 Rorer Pharmaceutical Corp. Quinoline derivatives and use thereof as antagonists of leukotriene D4

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BR9007783A (en) 1992-08-11
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PT95690A (en) 1991-09-13
HUT64750A (en) 1994-02-28
HU9201395D0 (en) 1992-07-28
EP0497888A1 (en) 1992-08-12
WO1991006538A1 (en) 1991-05-16
CA2067138A1 (en) 1991-04-28
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