摘要:
Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.
摘要:
The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.
摘要:
The invention relates to a compound corresponding to the general formula (I): wherein, X, R1, R2, R3, R4, R5, R5′ and R6 are as defined herein. More specifically, this invention relates to intermediates to prepare a compound of formula (I) as well as its utility in treating a variety of diseases including Alzheimer's disease and Parkinson's disease.
摘要翻译:本发明涉及对应于通式(I)的化合物:其中X,R 1,R 2,R 3,R R 5,R 5,R 5'和R 6如本文所定义。 更具体地,本发明涉及制备式(I)化合物的中间体以及其在治疗各种疾病(包括阿尔茨海默氏病和帕金森病)中的用途。
摘要:
The present invention relates to compounds of formula: ##STR1## which are agonists of cholecystokinin receptors and pharmaceutical compositions containing them.
摘要:
Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.
摘要:
The invention relates to the compounds of formula (I) ##STR1## in which R.sub.I, R.sub.II, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are as defined in claim 1.
摘要:
Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.
摘要:
The invention relates to thiadiazole derivatives corresponding to the general formula ##STR1## in which Ar represents a nitrogen-containing aromatic heterocycle, in particular indolyl which is substituted or unsubstituted on the nitrogen atom with CO--(C.sub.1 -C.sub.4)alkyl; with (CH.sub.2).sub.n COR in which n represents 1 or 2 and R represents OR.sub.1 or NR.sub.1 R.sub.2 with R.sub.1 and R.sub.2, which may be identical or different, representing H or (C.sub.1 -C.sub.4)alkyl; with (C.sub.1 -C.sub.4) hydroxyalkyl; with (C.sub.2 -C.sub.6) alkoxyalkyl; tetrahydropyranyl; or with a --(CH.sub.2).sub.3 -- chain, the last carbon of which is attached to the phenyl ring of the indole to form a 6-membered ring;Z represents(a) the group ##STR2## where A and B, independently of each other, represent C, CH or N; and X.sub.1, X.sub.2, X.sub.3 and X.sub.4, which may be identical or different, represent H, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, Cl, Br or trifluoromethyl, or alternatively(b) an optionally substituted naphthyl group, as well as their pharmaceutically acceptable salts.
摘要:
The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5′ represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5′ form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate. The invention is applicable in therapy
摘要翻译:本发明涉及通式(I)的化合物,其中:X表示氧或硫原子; R 1表示n = 2或3时彼此独立地表示卤素原子,羟基,C 1 -C 3烷基 C 1 -C 3烷氧基,三氟甲基,三氟甲氧基或亚甲二氧基; R 2表示任选取代的C 1 -C 6烷基,C 3 -C 6烷基, 7个环烷基,哌啶基或苯基,C 3 -C 7环烷基,哌啶基或苯基任选被取代; R 3表示任选取代的氢原子或C 1 -C 6 -C 6烷基; R 4表示氢原子或C 1 -C 4烷基; R 5和R 5'彼此独立地表示氢原子,羟基,卤素原子,C 1〜 C 3烷基或R 5和R 5'一起形成氧代基; R 6表示氢原子,卤素原子,C 1 -C 3烷基,C 1〜 -C 3烷氧基,三氟甲基或三氟甲氧基; 以碱的形式加入酸,水合物或溶剂化物。 本发明适用于治疗
摘要:
The invention relates to the compounds of formula (I) ##STR1## in which R.sub.I, R.sub.II, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are as defined in claim 1.