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starch and imidi cyclic with selective receptor antagonist activity adrenergico

机译:具有选择性受体拮抗剂活性的肾上腺素淀粉和亚胺环

摘要

Compounds (I) R and R1 independently = H or C1-C4 alkyl or together = (CH2)2-6, n=0 or 1, u....../u is a single or a double bond, A=CO or CH2, A1 represents a CO or CH2 or CH, each R3 independently = H or C1-C4 alkyl, B is B1 or B2 (B2); Y=N or CH, R2 = halogen, C1-C4 alkyl or CN, R5 = halogen, C1-C4 alkyl, polyfluoroalkyl or NO2, R6 = H or halogen, m is 1 to 3, Z = O, S, NH or NMe) interact selectively with the alpha 1D subtype of the alpha 1 adrenergic receptor. This selectively makes these compounds useful agents in tissues particularly rich in alpha 1D adrenergic receptors, thus useful in reducing contractility of an unstable urinary bladder, in the treatment and prevention of atherosclerosis as they are inhibitors of noradrenaline-mediated cell proliferation in smooth muscles, and in reducing vascular adrenergic tone. The preparation of these compounds, their enantiomers, diastereoisomers, N-oxides and pharmaceutically acceptable salts, and pharmaceutical compositions containing them are also claimed.
机译:化合物(I)R和R1独立= H或C1-C4烷基或一起=(CH2)2-6,n = 0或1, ...... 是一个或一个双键,A = CO或CH 2,A 1表示CO或CH 2或CH,每个R 3独立地= H或C 1 -C 4烷基,B为B 1或B 2(B2); Y = N或CH,R2 =卤素,C1-C4烷基或CN,R5 =卤素,C1-C4烷基,多氟烷基或NO2,R6 = H或卤素,m为1-3,Z = O,S,NH或NMe)与alpha 1肾上腺素受体的alpha 1D亚型选择性相互作用。这选择性地使这些化合物在组织中特别是富含α1D肾上腺素能受体的有用药剂,因此可用于降低不稳定膀胱的收缩力,在治疗和预防动脉粥样硬化中有用,因为它们是去甲肾上腺素介导的平滑肌细胞增殖的抑制剂,并且在减少血管肾上腺素的张力。还要求保护这些化合物,其对映异构体,非对映异构体,N-氧化物和药学上可接受的盐以及含有它们的药物组合物的制备。

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