Laboratorios Salvat, S.a.

Chiesi Farmaceutici S.p.a.

Carles Farrerons Gallemi

Carmen Lagunas Arnal

Juan Lorenzo Catena Ruiz

Carolina Salcedo Roca

Andrés Fernandez Garcia

Ignacio José Miquel Bono

Dolors Balsa Lopez

Anna Fernandez Serrat

José Ignacio Bonilla Navarro

Carmen Serra Comas

Natividad Toledo Mesa

Andr&eacute;s Fernandez Garcia

Carlos Monserrat Vidal

Ignacio-Jos&eacute; Miquel Bono

Ana Maria Fernandez Serrat

Ferran Gimenez Guasch

Amadeu Llebaria Soldevila

Diego Haro Bautista

Pedro Marrero Gonzalez

Arnau Cordomi Montoya

Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO, SH, CN, F, Cl, Br, I, COOH, CONH, (C-C)-alkoxycarbonyl, (C-C)-alkylsulfanyl, (C-C)-alkylsulfinyl, (C-C)-alkylsulfonyl, (C-C)-alkoxyl optionally substituted with one or several F, and (C-C)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C-C)-alkyl, a substituted (C-C)-alkyl; and Xis a physiologically acceptable anion. Carbamate (I) is selective Mreceptor antagonists versus Mreceptor 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. 

1-alkyl-1-azoniabicyclo' 2.2.2 octane carbamate derivatives and their use as muscarinic receptor antagonists

The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C&#x2013;C)-alkylthio, (C&#x2013;C)-alkoxyl, (C&#x2013;C)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C&#x2013;C)alkyl and (C&#x2013;C)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 quaternary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the Mmuscarinic receptor, and selectively, the Mreceptor. 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.

Carbamates derived from arylalkylamines

The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C-C)-alkylthio, (C-C)-alkoxyl, (C-C)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C-C)-alkyl and (C-C)-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 Mmuscarinic receptor, and selectively, the Mreceptor. 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.

Carbamates derivatived from arylakylamines

The invention refers to new compounds of formula (I), wherein A and B are selected from the group consisting of N and CH, with the condition that when A is N, B is N; R is selected from the group consisting of CH and NH ; R and R are selected from the group consisting of H, CH , Br, Cl, COCH and OCH ; and R , R and R , are selected from the group consisting of H, F, Cl, Br, (C1-C3)-alkyl, trifluoromethyl, (C1-C3)-alkoxy and trifluoromethoxy. Compounds of formula (I) are prepared by reaction of a substituted aminoazine with a substituted 2-bromo-2-(4-R -sulfonylphenyl)-1-phenylethanone in a polar solvent. These new compounds inhibit COX-2 with high selectivity over COX-1. They are useful for the treatment of inflamation and/or cyclooxygenase-mediated diseases, having the additional advantage of a reduced potencial for ulcerogenic effects.

Substituted imidazo 1,2a&rcub;azines as selective inhibitors of cox-2

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Carles Farrerons Gallemi