| 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. [Image] A : -CH 2CH 2-, -CH=CH- or oxiranyl; X ->monovalent anion; R : hydrogen, hydroxy, Me, Et, trifluoromethyl, difluoromethyl or fluoro; R 1> and R 2>1-5C alkyl, optionally substituted by 3-6C cycloalkyl, hydroxy or halo, or both together form a 3-5C alkylene bridge; and R 3>, R 4>, R 3>' and R 4>' : 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). [Image] 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. |
