摘要:
The invention relates to compounds of the formula (I) in which: Y is a group selected from N(R7)CO-, -N(R7)CO-N(R7)-, -OCO-, -N(R7)S(O)n-; R1 is a hydrogen atom or a (C1-C4)alkyl group; R6 is a group selected from a (C1-C6)alkyl group, phenyl, benzyl or benzohydryl, a heterocyclic radical, a carbocyclic radical, a C3-C7)cycloalkylmethyl group; said salts being in state of a base or addition salts to an acid. The invention also relates to methods for preparing compounds of the formula (I) and to the use thereof as CB2 receptor antagonists that can cross the intestinal barrier for the treatment for autoimmune disorders, pain, gastrointestinal disorders, cardiovascular disorders and cancer.
摘要:
The present invention relates to compounds corresponding to formula (I): in which: -X represents a group of formula (II), a group of formula (III) or a group -SO2N(R5)- • - R1 represents: an unsubstituted (C2-C12)alkyl or a substituted (C1-C12)alkyl; - R2 represents a hydrogen atom or a (C1-C4)alkyl; - R3 represents an unsubstituted or substituted phenyl; - R4 represents an unsubstituted or substituted phenyl; - R5 represents a hydrogen atom or a (C1-C4)alkyl; preparation process and therapeutic use.
摘要:
The invention relates to compounds having the formula (I), wherein A represents: a substituted or non substituted alkylene (C1-C6) group; a Formula (II) group having m = O, 1 or 2 and p = 0 or 1; R1 represents hydrogen or a (C1 -C2 )alkyl; R2 represents a substituted or non substituted (C3-C10) alkyl group, a substituted or non substituted non aromatic (C3-C12) carbocylic radical, a heterocyclic substituted or non substituted radical, an alkylene (C1-C3) substituted group, a NR10R11 group; R9 represents a functional group or a heterocyclic radical. Preparation method and use in therapy.
摘要:
The invention relates to compounds of formula (I) in which: X represents a group (a); R1 represents an unsubstituted or substituted C1-C12 alkyl; an unsubstituted or substituted non-aromatic C3-C12 carbocyclic radical; an unsubstituted or substituted C3-C7 cycloalkylmethyl; an unsubstituted or substituted phenyl; an unsubstituted or substituted benzyl; an unsubstituted or substituted phenethyl; a benzhydryl; a benzhydryl methyl; an unsubstituted or substituted 1,2,3,4-tetrahydronaphtalenyl; an aromatic heterocyclic radical; R2 represents a hydrogen atom or a C1-C3 alkyl; R3 represents a hydrogen atom or a C1-C5 alkyl; R4 represents an unsubstituted or substituted phenyl; R5 represents an unsubstituted or substituted phenyl; R6 represents a hydrogen atom or a C1-C3 alkyl; n represents 0, 1 or 2; Alk represents an unsubstituted or substituted C1-C4 alkyl; with the condition that R4 and R5 do not simultaneously represent a phenyl substituted by a C1-C4 alkoxy. The invention also relates to a method for preparing the aforementioned compounds and to their therapeutic use.
摘要:
The invention relates to 5,6-diphenylpyridine-3-carboxamide derivatives of general formula (I), where R1 = H, or (C1-C4) alkyl, R2 = a monoazo saturated heterocycle of 5 to 7 atoms, the nitrogen atom being substituted with a (C1 -C4)alkanoyl, NR10R11, a non-aromatic (C3-C10) carbocycle more than tri-substituted with (C1-C4) alkyl, a non-aromatic (C11-C12) carbocycle unsubstituted or mono- or poly-substituted with (C1-C4) alkyl, a monooxygenated saturated heterocycle with 5 to 7 atoms, more than tri-substituted with (C1-C4) alkyl, or R1 and R2, together with the nitrogen atom to which the above are bonded, form a 4-disubstituted piperidin-1-yl group, the salts, solvates and hydrates thereof. The invention further relates to a method for production and therapeutic application thereof.
摘要:
The subject of the invention is compounds corresponding to the formula (I): in which: - R 1 represents a hydrogen atom or a (C 1 -C 4 )alkyl group; - R 2 represents a homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical, or an amino (C 1 -C 6 )alkyl group; - or R 1 and R 2 , together with the nitrogen atom to which they are attached, constitute a piperazin-1-yl, 1,4-diazepan-1-yl, homopiperidin-1-yl, piperidin-1-yl, pyrrolidin-1-yl or azetidin-1-yl radical; - one of the two substituents R 3 , R 6 represents a Y-A-R 9 group; - Y represents an oxygen atom, or an -S(O) n -, -OSO 2 - or-N(R 18 )- group; ‑ A represents an unsubstituted (C 1 -C 4 )alkylene group; - R 9 represents an -OR 12 , -CN, ‑CO 2 H, NR 12 R 13 , -CONR 12 R 13 , -NR 15 COR 12 ,-CONHNH 2 , -CONHOH, -CONHSO 2 R 14 , ‑S(O) n R 14 , -SO 2 NR 12 R 13 , -NR 18 SO 2 R 14 , or-NR 15 SO 2 NR 12 R 13 group, or an aromatic heterocycle. The present invention also relates to the methods of preparation and the therapeutic applications of the compounds of formula (I).
摘要:
The invention concerns compounds of formula (I) wherein: X represents a -C-, -SO2-, -C-N(R5)-C-N(R5)- group; Y represents an oxygen atom or a sulphur atom; R1 represents a hydrogen atom or a C1-C4 alkyl group; R2 represents a C1-C7 alkyl group, a carbocyclic radical, a methyl substituted by a C3-C12 non aromatic carbocyclic radical, a phenyl, a phenoxymethyl, a benzyl, a benzhydryl, a benzhydrylmethyl group, a 1,2,3,4-tetrahydronaphthalenyl, a pyrrolyl, imidazolyl, pyridyl, pyrazolyl, furyl, thienyl radical; an indolyl; a benzofuryl; R3 represents a substituted or unsubstituted phenyl; R4 represents a substituted or unsubstituted phenyl; R5 represents a hydrogen atom or a C1-C4 alkyl; as well as their salts and solvates. The invention also concerns a method for preparing same and the therapeutic use thereof.
摘要:
The invention concerns compounds of formula (I) wherein: X represents a -C-, -SO2-, -C-N(R5)-C-N(R5)- group; Y represents an oxygen atom or a sulphur atom; R1 represents a hydrogen atom or a C1-C4 alkyl group; R2 represents a C1-C7 alkyl group, a carbocyclic radical, a methyl substituted by a C3-C12 non aromatic carbocyclic radical, a phenyl, a phenoxymethyl, a benzyl, a benzhydryl, a benzhydrylmethyl group, a 1,2,3,4-tetrahydronaphthalenyl, a pyrrolyl, imidazolyl, pyridyl, pyrazolyl, furyl, thienyl radical; an indolyl; a benzofuryl; R3 represents a substituted or unsubstituted phenyl; R4 represents a substituted or unsubstituted phenyl; R5 represents a hydrogen atom or a C1-C4 alkyl; as well as their salts and solvates. The invention also concerns a method for preparing same and the therapeutic use thereof.
摘要:
The invention relates to compounds having formula (I), wherein: R1 represents a heterocylic radical selected from among formula (II), R2 represents a (C1-C5)alkyl or a cyano, R3 represents a substituted or non-substituted phenyl, and R4 represents a substituted or non-substituted phenyl, as well as to the hydrates or solvates thereof.
摘要:
The invention relates to compounds of formula (I) where R1 = H or C1-C4 alkyl, R2 = C4-C10 alkyl, a C3-C12 non-aromatic carbocyclic group, a 1,2,3,4-tetrahydronaphthalenyl, a heterocyclic group, a C1-C3 alkylene group with a carbocyclic group, a phenylalkylene group, a NR9R10 group, or R1 and R2, together with the nitrogen atom to which they are bonded, are either a piperazin-1-yl or 1,4-diazepan-1-yl, or a piperidin-1-yl or pyrrolidin-1-yl, R3, R4, R5, R6, R7, R8 independently = H or halogen, a C1-C6 alkyl, C1-C6 alkoxy, trifluoromethyl or S(O)nAlk group in the form of a base or acid addition salts and in the hydrated or solvated state. The invention further relates to a method for preparation and therapeutic use thereof.