摘要:
The invention relates to the compounds of general formula (I) in which X 1, X 2, X 3 and X 4 are, independently of one another, a nitrogen atom or a C‑R 1 group; W is an oxygen or sulphur atom; n is equal to 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; A is a bicyclic heteroaryl of formula (II) where Z 1 , Z 2 , Z 3 and Z 4 are, independently of one another, a carbon atom, a nitrogen atom or a C‑R 2a group; Z 5, Z 6 and Z 7 are, independently of one another, a nitrogen atom or a C‑R b group; Z 8 is a carbon atom; in the form of a base or of an addition salt with an acid, and also in the form of a hydrate or of a solvate. Process for preparation thereof and therapeutic use.
摘要:
The invention concerns tricyclic Ν-heteroaryl-carboxamide derivatives containing a benzimidazole unit, of general formula (I) wherein: A represents, with the C-N bond of the benzimidazole unit to which it is bound, a 4- to 7-membered monocyclic heterocycle or a monocyclic heteroaryl containing from one to three heteroatoms selected among O, S or N, including the nitrogen atom of the benzimidazole unit; P represents a 8-, 9-, 10-, 11-membered bicyclic heterocycle or a bicyclic heteroaryl, comprising 1 to 6 heteroatoms selected among N, O or S; R1 represents on to four atoms or groups, identical or different; Y represents an oxygen or sulfur atom; R2 represents a hydrogen atom, a halogen atom, a C1C6-alkyl, C3-C7- cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkylene, C1C6-fluoroalkyl or C1C6-alkoxy group; R3 represents from one to three atoms or groups, identical or different; in base or acid addition salt state as well as in hydrate or solvate form. The invention also concerns a method for preparing the compounds and their therapeutic use.
摘要:
The invention relates to compounds of the general formula (I) in which: the pyrrolopyridine node is optionally substituted at the 4, 5, 6 and / or 7 carbonated position by one or more identical or different X substituents selected from a hydrogen or halogen atom or a C1C6-alkyl, C3-C7- cycloalkyl, C3-C7cycloalkyl-C1C6-alkylene, C1C6-fluoroalkyl, C1C6-alkoxyl, C3-C7- cycloalkoxyl, C3-C7-cycloalkyl-C1C6-alkylene-O-, C1C6-fluoroalkoxyl, cyano, C1-C6- thioalkyl, -S(O)-C1C6-alkyl, -S(O)-C2-C6-alkyl, SF5, C(O)NR1R2, SO2NR1R2, nitro, NR1R2, OCONR1R2, NR3COR4, NR3CONR1R2, NR3SO2R5, NR3SO2NR1R2, aryl-C1C6- alkylene, heteroaryl-C1C6-alkylene, aryl or heteroaryl group, the aryl and heteroaryl being optionally substituted; Z1, Z2, Z3, Z4 independently represent a nitrogen atom or a C(R6) group, one of which at least corresponds to a nitrogen atom and one of which at least corresponds to a C(R6) group; Z in a cyclic amine bound by the nitrogen atom or cyclic amine bound by the nitrogen and of the formula NraRb; wherein the compounds can be in the base state or in the state of an addition salt for an acid, or in a hydrate or solvate state. The invention also relates to a method for making the same and to the use thereof in therapy.
摘要:
The invention relates to compounds of general formula (I): in which X1 is a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, cyano, C(O)NR1R2, nitro, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X2 is a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, cyano, C(O)NR1R2, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X3 and X4 are, independently of one another, a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, cyano, C(O)NR1R2, nitro, NR1R2, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, NR3COR4, NR3SO2R5, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; Z1, Z2, Z3 and Z4 are, independently of one another, a nitrogen atom or a C(R6) group; n is equal to 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; Ra and Rb are, independently of one another, a hydrogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, hydroxyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, aryl or heteroaryl group, wherein Ra and Rb may be optionally substituted; in the form of a base or an addition salt with an acid, and also in the form of a hydrate or of a solvate. Process for the preparation thereof and therapeutic use.
摘要:
The invention concerns tricyclic Ν-heteroaryl-carboxamide derivatives containing a benzimidazole unit, of general formula (I) wherein: A represents, with the C-N bond of the benzimidazole unit to which it is bound, a 4- to 7-membered monocyclic heterocycle or a monocyclic heteroaryl containing from one to three heteroatoms selected among O, S or N, including the nitrogen atom of the benzimidazole unit; P represents a 8-, 9-, 10-, 11-membered bicyclic heterocycle or a bicyclic heteroaryl, comprising 1 to 6 heteroatoms selected among N, O or S; R1 represents on to four atoms or groups, identical or different; Y represents an oxygen or sulfur atom; R2 represents a hydrogen atom, a halogen atom, a C1C6-alkyl, C3-C7- cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkylene, C1C6-fluoroalkyl or C1C6-alkoxy group; R3 represents from one to three atoms or groups, identical or different; in base or acid addition salt state as well as in hydrate or solvate form. The invention also concerns a method for preparing the compounds and their therapeutic use.
摘要:
The invention concerns compounds of general formula (I), wherein n is equal to 0, 1, 2 or 3; the pyrrolopyridine ring is a pyrrolo[3,2-b]pyridine group, a pyrrolo[3,2-c]pyridine group, a pyrrolo[2,3-b]pyridin group. The invention also concerns a method for preparing said compounds and their therapeutic use.
摘要:
The invention concerns compounds of general formula (I) wherein: X1, X2, X3, X4 represent, independently of one another, a hydrogen or halogen atom or a C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkylene, C1-C6-fluoroalkyl, C1-C6-alkoxyl, C1-C6-fluoroalkoxyl, cyano, C(O)NR1R2, nitro, NR1R2, C1-C6-thioalkyl, -S(O)-C1-C6-alkyl, -S(O)2-C1-C6-alkyl, SO2NR1R2, NR3COR4, NR3SO2R5 or aryl group, the aryl being optionally substituted; W represents a fused bicyclic group of formula (II) bound to the nitrogen atom by positions 1, 2, 3 or 4; A represents a five- or seven-membered heterocycle comprising from one to three heteroatoms selected among O, S or N; the carbon atom(s) of A being optionally substituted; n is equal to 1, 2 or 3; Y represents an optionally substituted heteroaryl; in base or acid addition salt form, as well as in hydrate or solvate form. The invention also concerns a method for preparing said compounds and their therapeutic use.
摘要:
The invention relates to compounds of the general formula (I) in which: G 1 , G 2 , G 3 et G 4 are independent from one another, a C-X group or a nitrogen atom; one of G 1 , G 2 , G 3 and G 4 and at most one of G 1 , G 2 , G 3 and G 4 is a C-X group In which X is a -Si(X 1 )(X 2 )(X 3 ) group; n is 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; Z1, Z2, Z3, Z4 are independent from one another, a nitrogen atom or a C(R 6 ) group, at least one being a nitrogen atom and at least one being a C(R 6 ) group; Z is cyclic amino or acyclic amino; said compounds can be in the state of a base or an addition salt to an acid, as well as in the hydrate or solvate state. The invention also relates to a method for preparing the same and to the therapeutic use thereof.
摘要:
The invention concerns compounds of general formula (I) : wherein Z1, Z2, Z3, and Z4 represent, independently of one another, a nitrogen atom or a C(R6) group, at least one of which corresponds to a nitrogen atom and at least one of which corresponds to a C(R6) group, n is equal to 0, 1, 2 or 3, Y represents an optionally substituted aryl or heteroaryl, and Z represents a cyclic amine bound by the nitrogen atom of formula , in the base or acid addition salt state, and in the hydrate or solvate state. The invention also concerns a preparation method and a therapeutic application.
摘要:
The invention concerns compounds of general formula (I), wherein: n is equal to 0, 1, 2 or 3; X1, X2, X3, X4, Z1, Z2, Z3, Z4 and Z5 represent a hydrogen atom or certain specific substituents; W represents a fused bicyclic group of formula (a), bound to the nitrogen atom by positions 1, 2, 3 or 4; A represents a 5 to 7-membered optionally substituted heterocycle comprising one to three heteroatoms selected among O, S or N. Said compounds are ligands of the TRPV1 vanilloid receptor useful for treating pain and inflammation.