Carbamates derivatived from arylakylamines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C546S137000, C546S133000, C546S135000

Reexamination Certificate

active

06916828

ABSTRACT:
The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1-C4)-alkyl and (C1-C4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3muscarinic receptor, and selectively, the M2receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.

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van Zwieten et al. Cardiovascular Durgs and Therapy. 1995, 9(1); 159-67.
Xu et al. Chemical & Pharmaceutical Bulletin, 1998, 46(2); 231-41.

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