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ARYL ALKENSAEUREDERIVATE AS LEUKOTRIA AGENTS

机译:艾丽尔·阿尔肯索瑞德(ALARYSAKENEEURIV)用作白斑病代理商

摘要

Aryl alkenoic acid derivatives, and physiologically acceptable salts thereof, are provided which are potent leukotriene antagonists and may be used for the treatment of circulatory diseases and preferably for respiratory diseases such as asthma. The derivatives have a general formula I CHEM in which X is -S-, -SO-, -SO2- or -O-; W is CH=CH or CH2-CH2; o is 1 to 5; n is 1 to 10; m is 0 to 7; T and Z, same or different, represent oxygen or a direct bond; R2 and R3, same or different, represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro groups; A represents carboxyl, tetrazolyl, CO2R4, CONR5R6 or nitrile group wherein R4 is lower alkyl and R5 and R6 are H, lower alkyl, alkylsulfonyl, arlysulfonyl or R5 and R6 together are an alkylene chain forming a ring; and R is CHEM wherein B represents carboxyl, tetrazolyl, CO2R4, CONR5R6 or nitrile group wherein R4 is lower alkyl and R5 and R6 are H, lower alkyl, alkylsulfonyl, arlysulfonyl or R5 and R6 together are an alkylene chain forming a ring; R7 and R8, same or different, represent H or lower alkyl; R9 represents -OH, -O-alkyl, NH2 or a NHCH2CO2H group; and R10 is H, alkyl, alkoxy, halogen, CF3, CF3O, CN or NO2.
机译:提供了芳族链烯酸衍生物及其生理学上可接受的盐,它们是有效的白三烯拮抗剂,可用于治疗循环系统疾病,优选用于呼吸系统疾病,例如哮喘。衍生物具有通式I ,其中X为-S-,-SO-,-SO2-或-O-; W是CH = CH或CH2-CH2; o是1到5; n为1至10; m为0至7; T和Z相同或不同,表示氧或直接键; R 2和R 3相同或不同,表示氢,烷基,烷氧基,卤素,三氟甲基,三氟甲氧基,氰基或硝基。 A代表羧基,四唑基,CO 2 R 4,CONR 5 R 6或腈基,其中R 4是低级烷基并且R 5和R 6是H,低级烷基,烷基磺酰基,芳磺酰基或R5和R6一起是形成环的亚烷基链; R为,其中B表示羧基,四唑基,CO 2 R 4,CONR 5 R 6或腈基,其中R 4为低级烷基且R 5和R 6为H,低级烷基,烷基磺酰基,芳基磺酰基或R 5和R 6一起为形成环的亚烷基链。 R 7和R 8相同或不同,表示H或低级烷基。 R 9表示-OH,-O-烷基,NH 2或NHCH 2 CO 2 H基团。 R 1 0为H,烷基,烷氧基,卤素,CF 3,CF 3 O,CN或NO 2。

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