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公开(公告)号:DE2609353A1
公开(公告)日:1977-09-15
申请号:DE2609353
申请日:1976-03-06
Applicant: BASF AG
Inventor: BLIESENER JENS-UWE DIPL CHEM D , FRANKE ALBRECHT DIPL CHEM DR , HIMMELE WALTER DIPL CHEM DR , LENKE DIETER PROF DR , MUELLER CLAUS-DIETER DR MED
IPC: A61K31/135 , C07C87/34 , C07C85/12
Abstract: New diphenylcyclopropylmethylamine derivs. are cpds. of formula (I) including the optically active forms) and their physiologically tolerable acid addn. salts. In formula (I), R1 is lower alkyl; R2 is dialkylamino, or an opt. substd. mono- or poly-nuclear aromatic residue; and A is 1-6C alkylene; in addn., R1 can be H when A is a residue -(CH2)n-CHR3-(CH2)m- in which n is 1,2,3 or 4 and m is 0, 1, 2, 3 or 4, or m and n are both 0, and R3 is H or 1-3C alkyl. (I) are useful as spasmolytics. The spasmolytic activity of (I) was demonstrated on guinea pig ileum segments suspended in oxygenated tyrode and artificially stimulated with BaCl2 (100 mg./l) or acetylcholine (0.1 mg./l.). 1- (2-Phenylpropylamino)methyl -2,2-diphenylcyclopropane in a concn. of 0.820 mg./l. gave 75% control of acetylcholine spasm (9.65 x papaverine) and in a concn. of 1.78 mg./l. gave 75% control of BaCl2 spasms (3.57 x papaverine). Specific cpds. (I) include 1- (2-phenylpropylamino)-methyl -2,2-diphenylcycloproprane.