CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

    公开(公告)号:US20080261949A1

    公开(公告)日:2008-10-23

    申请号:US12144843

    申请日:2008-06-24

    摘要: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.

    Sulphonamide derivatives, their preparation and their therapeutic application
    14.
    发明授权
    Sulphonamide derivatives, their preparation and their therapeutic application 失效
    磺酰胺衍生物,其制备及其治疗应用

    公开(公告)号:US07396958B2

    公开(公告)日:2008-07-08

    申请号:US11670586

    申请日:2007-02-02

    IPC分类号: C07C303/00 A01N41/06

    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.

    摘要翻译: 公开了具有本文所定义的通式(I)的化合物,其制备方法及其用于预防或治疗涉及食欲肽2受体相关功能障碍的任何疾病,例如肥胖,食欲或味觉障碍,包括恶病质, 厌食和贪食症,糖尿病,代谢综合征,呕吐和恶心,抑郁和焦虑,瘾,情绪和行为障碍,精神分裂症,睡眠障碍,不宁腿综合征,记忆学习障碍,性和心理性功能障碍,疼痛,内脏或神经性疼痛,痛觉过敏 ,异常性疼痛,消化系统疾病,肠易激综合征,神经元脱色,缺血性或出血性发作,库欣氏病,吉兰巴利综合征,强直性营养不良,尿失禁,甲状腺机能亢进,垂体功能障碍,高血压或低血压。

    2-aminoethyl-benzofuran derivatives, preparation thereof and
therapeutical use thereof
    17.
    发明授权
    2-aminoethyl-benzofuran derivatives, preparation thereof and therapeutical use thereof 失效
    2-氨基乙基 - 苯并呋喃衍生物,其制备及其治疗用途

    公开(公告)号:US6063810A

    公开(公告)日:2000-05-16

    申请号:US125947

    申请日:1998-08-31

    CPC分类号: C07D307/79

    摘要: Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group; each of R.sub.1, R.sub.2 and R.sub.5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl, C.sub.6, C.sub.10 or C.sub.14 aryl, C.sub.1-6 alkoxycarbonyl, C.sub.1-6 hydroxyalkyl, C.sub.1-6 alkoxyalkyl, C.sub.1-6 alkoxy, C.sub.1-8 fluoroalkyl or C.sub.1-8 perfluoroalkyl group, or R.sub.1 and R.sub.2 taken together form a C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkenyl or C.sub.6, C.sub.10 or C.sub.14 aryl ring, except for compounds in which R.sub.1 and R.sub.2 are both hydrogen; each of R.sub.3 and R.sub.4, which are the same or different, is a hydrogen atom or a C.sub.1-8 alkyl, C.sub.1-8 alkenyl, C.sub.3-8 cycloalkyl or C.sub.3-8 cycloalkenyl group, or R.sub.3 and R.sub.4 taken together form a C.sub.2-6 cycloalkyl or C.sub.3-6 cycloalkenyl ring, e.g., piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures;, as well as pharmaceutically acceptable acid addition salts thereof. The compounds may be used in therapy.

    摘要翻译: PCT No.PCT / FR97 / 00383 Sec。 371日期1998年8月31日 102(e)日期1998年8月31日PCT 1997年3月5日PCT公布。 公开号WO97 / 32870 日期:1997年9月12日,式(I)的化合物,其中A为氢原子或羟基; B是氢原子或C 1-8烷基,C 1-8烯基,C 1-8氟烷基或C 1-8全氟烷基; R 1,R 2和R 5各自相同或不同,为氢原子,卤素如氯,溴或氟,C 1-8烷基,C 1-8烯基,C 3-8环烷基,C 3-8环烯基 ,C 6,C 10或C 14芳基,C 1-6烷氧基羰基,C 1-6羟基烷基,C 1-6烷氧基烷基,C 1-6烷氧基,C 1-8氟代烷基或C 1-8全氟烷基,或者R 1和R 2一起形成C 3-8 环烷基,C3-8环烯基或C6,C10或C14芳基环,其中R1和R2均为氢的化合物; R 3和R 4各自相同或不同,为氢原子或C 1-8烷基,C 1-8烯基,C 3-8环烷基或C 3-8环烯基,或者R 3和R 4一起形成C2- 6环烷基或C 3-6环烯基环,例如哌啶基,氮杂环丁烷基或吡咯烷基; 以对映异构体,非对映异构体或其混合物的形式,包括外消旋混合物,以及其药学上可接受的酸加成盐。 该化合物可用于治疗。

    Cyclohexyl(alkyl)propanolamines, preparation method and pharmaceutical compositions containing same

    公开(公告)号:US07622460B2

    公开(公告)日:2009-11-24

    申请号:US12144843

    申请日:2008-06-24

    摘要: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen atom, a (C1-C6)alkyl group, a (C1-C4)alkoxy group, a —COO(C1-C4)alkyl group, a —CO(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl groups, —NO2, —CN, —CONR4R5, —COOH, or a 4,5-dihydro-1,3-oxazol-2-yl or 4,4-dimethyl-4,5-dihydro-1,3-oxazol-2-yl group; R4 and R5 represent, independently, a hydrogen atom, a phenyl, a (C1-C4)alkyl group or a phenyl-(C1-C4)alkyl group or R4 and R5 with the nitrogen atom to which they are attached, may form a ring of 5 to 7 atoms in total; and to the salts or solvates thereof, to the pharmaceutical compositions containing them, to a process for the preparation thereof and to intermediates in this process.