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    3-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO[4,5-B]INDOLE-1-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE
    3.
    发明申请
    3-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO[4,5-B]INDOLE-1-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE 有权
    3-异丙基-3,5-二氢-4-氧代-4H-吡啶并[4,5-B]吲哚-1-羧酰胺衍生物，其制备和治疗用途

    公开(公告)号：US20060241116A1

    公开(公告)日：2006-10-26

    申请号：US11427508

    申请日：2006-06-29

    申请人： Philippe BURNIER ,  Jacques FROISSANT ,  Benoit MARABOUT ,  Frank MARGUET ,  Frederic PUECH

    发明人： Philippe BURNIER ,  Jacques FROISSANT ,  Benoit MARABOUT ,  Frank MARGUET ,  Frederic PUECH

    IPC分类号： A61K31/503 ,  C07D487/02 ,  C07D209/42

    CPC分类号： C07D487/04 ,  C07D209/42

    摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

    摘要翻译： 本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R 1表示氢原子或（C 1 -C 4 -C 4）烷基; R 2和R 3各自独立地表示氢原子或（C 1 -C 4）烷基， 或者R 2和R 3形式，与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 C 1 -C 4烷基或（C 1 -C 4 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

    3-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO[4,5-B]INDOLE-1-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE
    5.
    发明申请
    3-HETEROARYL-3,5-DIHYDRO-4-OXO-4H-PYRIDAZINO[4,5-B]INDOLE-1-CARBOXAMIDE DERIVATIVES, THEIR PREPARATION AND THERAPEUTIC USE 审中-公开
    3-异丙基-3,5-二氢-4-氧代-4H-吡啶并[4,5-B]吲哚-1-羧酰胺衍生物，其制备和治疗用途

    公开(公告)号：US20090275576A1

    公开(公告)日：2009-11-05

    申请号：US12487902

    申请日：2009-06-19

    申请人： Philippe BURNIER ,  Jacques FROISSANT ,  Benoit MARABOUT ,  Frank MARGUET ,  Frederic PUECH

    发明人： Philippe BURNIER ,  Jacques FROISSANT ,  Benoit MARABOUT ,  Frank MARGUET ,  Frederic PUECH

    IPC分类号： A61K31/5377 ,  A61K31/5025 ,  A61P43/00

    CPC分类号： C07D487/04 ,  C07D209/42

    摘要： A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2 and R3 each represent, independently of one another, a hydrogen atom or a (C1-C4)alkyl group or else R2 and R3 form, with the nitrogen atom which carries them, a pyrrolidinyl, piperidinyl, morpholinyl or 4-alkylpiperazinyl group; and Het represents a heteroaromatic group of pyridinyl, 1-oxidopyridinyl, quinolinyl, isoquinolinyl, pyrimidinyl, pyrazinyl or pyridazinyl type, it being possible for the heteroaromatic group to carry one or more halogen atoms and/or one or more (C1-C4)alkyl or (C1-C4)alkoxy groups; in the form of bases, of addition salts with acids, of solvates or of hydrates, the pharmaceutical compositions comprising them, processes for their preparation and synthetic intermediates.

    摘要翻译： 本发明的主题是通式（I）的化合物，其中X表示氢或卤素原子; R1表示氢原子或（C1-C4）烷基; R2和R3各自独立地表示氢原子或（C1-C4）烷基，或者R2和R3与携带它们的氮原子一起形成吡咯烷基，哌啶基，吗啉基或4-烷基哌嗪基; 并且Het表示吡啶基，1-氧化吡啶基，喹啉基，异喹啉基，嘧啶基，吡嗪基或哒嗪基的杂芳族基团，杂芳基可以携带一个或多个卤素原子和/或一个或多个（C 1 -C 4）烷基 或（C 1 -C 4）烷氧基; 以碱的形式，与酸，溶剂合物或水合物的加成盐，包含它们的药物组合物，其制备方法和合成中间体。

    ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
    7.
    发明申请
    ARYL- AND HETEROARYLPIPERIDINECARBOXYLATE-DERIVATIVES METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
    ARYL-和异二氢吡啶羧酸酯衍生物的制备方法及其作为脂肪酸氨基水解酶酶抑制剂的用途

    公开(公告)号：US20070021405A1

    公开(公告)日：2007-01-25

    申请号：US11465238

    申请日：2006-08-17

    申请人： Ahmed ABOUABDELLAH ,  Antonio ALMARIO GARCIA ,  Christian HOORNAERT ,  Patrick LARDENOIS ,  Frank MARGUET

    发明人： Ahmed ABOUABDELLAH ,  Antonio ALMARIO GARCIA ,  Christian HOORNAERT ,  Patrick LARDENOIS ,  Frank MARGUET

    IPC分类号： C07D417/02 ,  C07D413/02 ,  C07D403/02

    CPC分类号： C07D471/04 ,  C07D207/06 ,  C07D211/16 ,  C07D211/52 ,  C07D401/04 ,  C07D401/06

    摘要： The present invention comprises compounds corresponding to the general formula (I): in which m, n=1 to 3 and m+n=2 to 5; p=1 to 7; A=single bond or X, Y and/or Z; X=optionally substituted methylene; Y=C2-alkenylene, which is optionally substituted, or C2-alkynylene; Z=C3-7-cycloalkyl; R1 represents a group of aryl or heteroaryl type; R2 represents a hydrogen or fluorine atom or a hydroxyl, C1-6-alkoxy or NR8R9 group; R3 represents a hydrogen atom or a C1-6-alkyl group; R4 represents a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-3-alkyl group; in the base form or in the form of an addition salt with an acid, of a hydrate or of a solvate. The compounds are useful in the treatment of a number of diseases and/or pathological conditions such as chronic pain, dizziness, vomiting, nausea, eating disorders, neurological and psychiatric pathologies, acute or chronic neurodegenerative diseases, epilepsy, sleep disorders, cardiovascular diseases, renal ischaemia, cancers, disorders of the immune system, allergic diseases, parasitic, viral or bacterial infectious diseases, inflammatory diseases, osteoporosis, eye conditions, pulmonary conditions, gastrointestinal diseases or urinary incontinence.

    摘要翻译： 本发明包括对应于通式（I）的化合物：其中m，n = 1至3，m + n = 2至5; p = 1〜7; A =单键或X，Y和/或Z; X =任选取代的亚甲基; Y = C 2 - 亚烯基，其任选被取代，或C 2 - 亚炔基; Z = C 3-7 - 环烷基; R 1表示芳基或杂芳基的基团; R 2表示氢或氟原子或羟基，C 1-6 - 烷氧基或NR 8 R 9 >组 R 3表示氢原子或C 1-6 - 烷基; R 4表示氢原子或C 1-6 - 烷基，C 3-7 - 环烷基或C 3-7 环烷基-C 1-3 - 烷基; 以碱的形式或与酸的加成盐，水合物或溶剂化物的形式。 这些化合物可用于治疗许多疾病和/或病理状况，例如慢性疼痛，头晕，呕吐，恶心，进食障碍，神经和精神病理学，急性或慢性神经变性疾病，癫痫症，睡眠障碍，心血管疾病， 肾缺血，癌症，免疫系统疾病，过敏性疾病，寄生虫，病毒或细菌感染性疾病，炎性疾病，骨质疏松症，眼睛条件，肺部疾病，胃肠道疾病或尿失禁。