摘要:
New benzothiazine derivatives corresponding to the general formula I: ##STR1## in which: X represents halogen,n represents 0, 1, or 2,B represents the following formula: ##STR2## in which: R.sub.1 & R.sub.2 together with the carbons to which they are attached form a 6-carbon-atom aromatic ring which is optionally substituted by a group X' representing halogen, andY represents the radical --(SO.sub.2).sub.x --Alk--Z, x, Alk, and Z are as defined in the specification;as well as their possible stereoisomers, epimers, N-oxides and pharmaceutically-acceptable acid or base addition salts; and medicinal products containing the same, useful in the treatment of inflammatory disorders requiring an inhibitor of cytokines.
摘要:
Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.
摘要:
Compounds of general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,R.sub.5 denotes a carboxyl, (lower alkyloxy)carbonyl, (lower alkenyloxy)carbonyl or (lower alkynyloxy)-carbonyl,their isomers, stereoisomers and diastereoisomers, and also their addition salts with a pharmaceutically acceptable base.Medicinal products.
摘要翻译:通式(I)的化合物:其中:R1,R2,R3和R4可以相同或不同,表示氢原子,卤原子或低级烷基,低级烯基,低级烷氧基或低级烯氧基 R 5表示羧基,(低级烷氧基)羰基,(低级链烯氧基)羰基或(低级炔氧基) - 羰基,它们的异构体,立体异构体和非对映异构体,以及它们与药学上的加成盐 可接受的基数。 药用产品。
摘要:
A compound selected from those of formula (I): wherein: represents single or double bond, R1 represents hydrogen, alkyl, —R6-aryl, —R6-cycloalkyl, —R6-heterocycle, —CO2R7—, —COR8, or —CONHR8, wherein R6, R7, and R8 are as defined in the description, R2 represents cyano, mono- or di-alkylaminoalkylaminocarbonyl, —CO2R8, —CONHR8, —NR8R9, —NHCO2R7, or —COR8 wherein R7, R8, and R9 are as defined in the description, R3 and R4 together form (C3-C10)cycloalkyl, R5 represents hydrogen, alkyl, or arylalkyl, Ra, Rb, Rc, Rd, which may be identical or different, represent a group as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of CNS disorders.
摘要:
The present invention relates to compounds of formula (I) below in which: —R1 and R3 represent, independently of one another, a methoxy group optionally substituted by one or more fluorine atoms, —R2 and R4 represent, independently of one another, a hydrogen atom or a methoxy group optionally substituted by one or more fluorine atoms, —A represents a ring chosen from the group comprising aryl and heteroaryl groups, said ring possibly being substituted by or fused to a heterocycle, —X represents a nitrogen atom or a CH group, and —Z1 represents a hydrogen atom or a halogen atom, preferably fluorine, and —Z2 represents a hydrogen atom, a halogen atom, preferably fluorine, a C1 to C4 alkyl group, an aryl group or a —CN, —SO2NR12R13, —SO2R9, —COOR15 or —COR15 group, and also to the pharmaceutically acceptable salts thereof, the isomers thereof and the prodrugs thereof.
摘要:
Compounds of formula (I): wherein: R1 represents hydrogen, (C1-C6)alkyl, (C1-C6)aminoalkyl or (C1-C6)hydroxyalkyl, R2 represents hydrogen, or R1 and R2, together with the carbon atoms carrying them, form a carbon-carbon bond, R3 represents hydrogen, R4 represents hydrogen, methyl or (C3-C6)alkyl, (C1-C6)aminoalkyl, (C1-C6)hydroxyalkyl, aryl-(C1-C6)alkyl or heterocycloalkyl-(C1-C6)alkyl, or R3 and R4 together with the carbon atoms carrying them, form a carbon-carbon bond, R5, R6, R7 and R8 represent hydrogen, or a pair of geminal substituents (R5 and R6 and/or R7 and R8) form an oxo, thioxo or imino group, R9 represents hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, R10 and R11 represent hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, n represents an integer between 0 and 4 inclusive, m represents an integer between 0 and 2 inclusive, p represents an integer between 0 and 3 inclusive, X represents a group NR12, R12 represents hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, aryl-(C1-C6)alkyl or (C1-C6)polyhaloalkyl, their enantiomers, diastereoisomers and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.
摘要:
Compounds of formula (I): wherein: A represents a divalent radical: wherein: Z represents an oxygen atom or a sulphur atom, R6 represents a hydrogen atom, an alkyl, alkenyl, arylalkyl or polyhaloalkyl group or a substituted, linear or branched alkyl chain, represents a single bond or a double bond, R1, R2, R3 and R4 represent a hydrogen or halogen atom, an alkyl, alkoxy, hydroxy, cyano, nitro, polyhaloalkyl or optionally substituted amino group, or a linear or branched alkyl chain substituted by one or more groups, R5 represents a hydrogen atom or an alkyl, aminoalkyl or hydroxyalkyl group, X and Y represent a hydrogen atom or an alkyl group, Ra, Rb, Rc and Rd represent a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, cyano, nitro, polyhaloalkyl, optionally substituted amino group, or a substituted, linear or branched alkyl chain, Re represents a hydrogen atom or an alkyl, arylalkyl or alkenyl group or a substituted, linear or branched alkyl chain, their enantiomers, diastereoisomers, and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.