摘要:
The subject of the invention is compounds corresponding to the formula (I): in which: - A represents an unsubstituted or substituted (C 1 -C 6 )alkylene group; - R 1 represents a hydrogen atom or an unsubstituted or substituted (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; - R 3 , R 4 , R 5 , R 6 , R 7 , R 8 each independently represent a hydrogen atom, a halogen atom, a -CN, ‑S(O) n R 14 , or -OS(O) n R 14 group, or an unsubstituted or substituted (C 1 -C 6 )alkyl 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 relates to compounds having the formula (I), wherein R1 represents: a substituted or non-substituted (C1-C12)alkyl; a non aromatic (C3-C12) carbocylic substituted or non substituted radical; a substituted or non substituted phenyl; a substituted or non substituted benzyl; a substituted or non substituted phenethyl; a benzhydryl; a benzhydrylmethyl; a heterocyclic aromatic radical; R2 represents a non substituted or substituted phenyl; R3 represents a substituted or non substituted phenly; R4 represents a hydrogen atom, a (C1-C-4)alkyl, a (C1-C4)alcoxy, a hydroxy; AIk represents a substituted or non substituted (C1-C4)alkyl. The invention also relates to the method for preparing same and to the use thereof in therapeutics as central and/or peripheral cannabinoid CB1 receptor ligands.
摘要:
The invention relates to compounds having formula (I), the preparation method thereof and the use of same in therapeutics, wherein: R1 represents a (C1-C6)alkyl, a (C3-C7)cycloalkyl which is unsubstituted or is mono- or poly-substituted, a (C3-C7)cycloalkylmethyl which is unsubstituted or is mono- or poly-substituted, a phenyl which is unsubstituted or substituted; a benzyl which is unsubstituted or is mono- or disubstituted, a thienyl which is unsubstituted or substituted; R2 represents a hydrogen atom or a (C1-C3)alkyl; R3 represents a hydrogen atom or a (C1-C5)alkyl; R4, R5, R6, R7, R8 and R9 each represent, independently of each other, a hydrogen atom, a halogen atom, a (C1-C7)alkyl, a (C1-C5)alkoxy, a trifluoromethyl radical or a S(O)nAlk group; n represents 0, 1 or 2; and Alk represents a (C1-C4)alkyl. The invention also relates to the preparation method thereof and to the use of same in therapeutics.
摘要:
The invention relates to compounds having formula (I), wherein: X represents a group having formula (II). According to the invention, R1 and R6 represent a hydrogen atom or an alkyl group. R2 represents a radical selected from among: a (C1-C12)alkyl; a non-aromatic carbocyclic radical at (C3-C12); a (C3-C7)cycloalkylmethyl; a phenyl, a benzyl, a benzhydryl, a benzhydrylmethyl, phenethyl, a benzodioxolyl, a dihydrobenzofuranyl, a dihydrobenzodioxinyl; a methyl substituted by a benzodioxolyl, a dihydrobenzofuranyl, a dihydrobenzodioxinyl; a non-substituted 1, 2, 3, 4-tetrahydronaphtalenyl; or a heterocyclic radical, an indolyl, a substituted or non-substituted benzothiazolyl, said radicals being substituted or non-substituted. R3 represents a (C1 -C5)alkyl or a (C3-C7) cycloalkyl. R4 and R5 represent a substituted or non-substituted phenyl. The invention also relates to a method of preparing said derivatives and to the application thereof in therapeutics.
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 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.
摘要:
The invention concerns pyrazolecarboxylic acid tricyclic derivatives of formula (I), wherein R1 represents a C3-C15 carboxycyclic radical or a NR2R3 group. The invention also concerns the method for preparing compounds of formula (I), pharmaceutical compositions containing them. The compounds of formula (I) are active towards CB1 cannabinoid receptors.
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.