摘要:
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 M3 muscarinic receptor, and selectively, the M2 receptor. 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.
摘要:
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 quaternary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. 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.
摘要:
Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X− is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 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.
摘要:
Compounds of general structure (I), wherein the central benzene ring may be substituted in the meta- or para-position; -A is an optionally substituted hydroxyl, alkoxyl, hydroxylamine, alkoxylamine or amine radical; -W is an N- and C-linked biradical selected from several possibilities; and -Z is a carbon radical selected from several possibilities. These compounds are PPARγ and PPARγ/PPARδ modulators and, therefore, are useful for the prophylactic and/or curative treatment of a condition or a disease mediated by these recetpcors.
摘要:
Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X− is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 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.
摘要:
Compounds of formula (I), wherein X is O, S, NH, OCO, NH—CO, NH—COO, NH—CO—NH, NH—CS or NH—CS—NH; R4 is H, (C1-C3)-alkyl optionally substituted by halogen, or a C-linked heterocyclic radical selected from several possibilities; R1 and R3 are H or F; and R2 is an N-linked or C-linked heterocyclic radical, are useful in the treatment of microbial infections in human or animal body.
摘要:
Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)S—N(R4)—B-J-T; and s, R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPARγ modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.
摘要:
Compounds of general formula I, and the salts and solvates thereof, wherein R1 represents the radical 2-benzoylphenylamino; R2 represents —(CH2)s—N(COR3)-A-J-T or —(CH2)s—N(R4)—B-J-T; and s. R3, R4, A, B, J and T have the meanings disclosed in the description. These compounds are PPARγ modulators and, therefore, are useful for the treatment or prevention of a condition or a disease mediated by these receptors.
摘要:
Compounds of formula (I), and their pharmaceutically acceptable salts and solvates, wherein X represents —O—, —NH—, —S—, —NHC(═O)— or —NHC(═S)—; R1 represents —H or a hydrocarbon chain; R2 represents —H, alkoxy, amino, a hydrocarbon chain or a radical of a cycle; R3 represents —H, a hydrocarbon chain or a radical of a cycle; R4 represents —H or a hydrocarbon chain; alternatively R3 and R4 form together a cycle; R5 and R6 represent —H or halogen, and R7 represents —H, a hydrocarbon chain or heteroaryl, are useful against bacterial infections in animals, including humans.
摘要:
Compounds of general formula (I), wherein from A1 to A5, and from B1 to B5 are H, alkyl, alkoxyl, halogen, carboxylic derivatives or sulfur derivatives, among others; and from P1 to P3 are H, halogen, alkyl or alkoxyl, among others. Said compounds may be used for the chemoprevention and treatment of both precancerous lesions and cancer.