7-Oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
申请人:E.R. SQUIBB & SONS, INC.
公开号:EP0374952A2
公开(公告)日:1990-06-27
7-Oxabicycloheptane substituted prostaglandin analogs which are thromboxane A2 (TxA2) receptor antagonists or combined thromboxane A2 receptor antagonists/thromboxane synthase inhibitors useful, for example, in treating thrombotic and vasospastic disease have the structural formula
wherein m is 1, 2 or 3; n is 0, 1, 2, 3 or 4; Z is -(CH2)2- or -CH=CH-, with the proviso when Z is -CH = CH-, n is 1, 2, 3 or 4; R is C02H, CO2lower alkyl, CH2OH, CO2alkali metal, CONHSOR3, CONHR3a or -CH2-5-tetrazolyl, X is 0, S or NH; and where R1, R2, R3 and R3a are as defined herein.
7-氧杂双环庚烷取代的前列腺素类似物是血栓素 A2(TxA2)受体拮抗剂或血栓素 A2 受体拮抗剂/血栓素合成酶联合抑制剂,可用于治疗血栓性疾病和血管痉挛性疾病等,其结构式为
其中 m 是 1、2 或 3;n 是 0、1、2、3 或 4;Z 是-(CH2)2- 或-CH=CH-,但当 Z 是-CH=CH-时,n 是 1、2、3 或 4;R 是 C02H、CO2lower 烷基、CH2OH、CO2 碱金属、CONHSOR3、CONHR3a 或-CH2-5-四唑基,X 是 0、S 或 NH;其中 R1、R2、R3 和 R3a 如本文所定义。