| 摘要 |
Esters (I) of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. - Esters, of formula (I), of fluorene-9-carboxylic acid with a bicyclic nitrogen heterocycle are new. - A = -CH2CH2-, -CH=CH- or oxiranyl; - X- = monovalent anion; - R = hydrogen, hydroxy, Me, Et, trifluoromethyl, difluoromethyl or fluoro; - R1 and R2 = 1-5C alkyl, optionally substituted by 3-6C cycloalkyl, hydroxy or halo, or both together form a 3-5C alkylene bridge; and - R3, R4, R3' and R4' = hydrogen, 1-4C alkyl or alkoxy, trifluoromethyl, difluoromethyl, cyano, nitro or halo. - Independent claims are also included for: - (1) Intermediates of formula (IV) and their acid addition salts; and - (2) Use of intermediates (II), or their acid addition salts, in the preparation of (I). - ACTIVITY - Antiasthmatic; Cardiant; Antiarrhythmic; Uropathic; Gynecological; Spasmolytic. - No biological data available. - MECHANISM OF ACTION - Anticholinergic; - Compounds (I) are antagonists of muscarinic receptors, subtype 3, generally with affinity (Ki) below 10 nM. |
