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DERIVES DE 1-ALKYL-1- AZONIABICYCLO (2.2.2) OCTANE CARBAMATE ET LEUR UTILISATION COMME ANTAGONISTES DU RECEPTEUR MUSCARINIQUE
专利权人:
CHIESI FARMACEUTICI S.P.A.
发明人:
申请号:
EP02796673.8
公开号:
EP1461336B1
申请日:
2002.12.18
申请国别(地区):
EP
年份:
2013
代理人:
摘要:
Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO<;SUB>;2<;/SUB>;, SH, CN, F, Cl, Br, I, COOH, CONH<;SUB>;2<;/SUB>;, (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkoxycarbonyl, (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkylsulfanyl, (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkylsulfinyl, (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkylsulfonyl, (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkoxyl optionally substituted with one or several F, and (C<;SUB>;1<;/SUB>;-C<;SUB>;4<;/SUB>;)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C<;SUB>;5<;/SUB>;-C<;SUB>;10<;/SUB>;)-alkyl, a substituted (C<;SUB>;1<;/SUB>;-C<;SUB>;10<;/SUB>;)-alkyl; and X<;SUP>;-<;/SUP>; is a physiologically acceptable anion. Carbamate (I) is selective M<;SUB>;3 <;/SUB>;receptor antagonists versus M<;SUB>;2 <;/SUB>;receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particularly, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.
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