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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
    2.
    发明授权
    3-heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use 有权
    3-杂芳基-3,5-二氢-4-氧代-4H-哒嗪并[4,5-B]吲哚-1-甲酰胺衍生物，其制备和治疗用途

    公开(公告)号：US07402682B2

    公开(公告)日：2008-07-22

    申请号：US11427508

    申请日：2006-06-29

    Applicant: Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

    Inventor： Philippe Burnier ,  Jacques Froissant ,  Benoit Marabout ,  Frank Marguet ,  Frederic Puech

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

    CPC classification number: C07D487/04 ,  C07D209/42

    Abstract: 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.

    Abstract translation: 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。

    NOVEL CRYSTALLINE FORM
    3.
    发明申请
    NOVEL CRYSTALLINE FORM 有权
    新型结晶形式

    公开(公告)号：US20080139569A1

    公开(公告)日：2008-06-12

    申请号：US12031243

    申请日：2008-02-14

    Applicant: William L. ROCCO ,  John D. HIGGINS

    Inventor： William L. ROCCO ,  John D. HIGGINS

    IPC: A61K31/503 ,  C07D487/02

    CPC classification number: C07D487/04

    Abstract: Disclosed are a novel crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, processes of preparing said crystalline form of 7-chloro-N,N,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-acetamide, compositions comprising said form in admixture with one or more pharmaceutically acceptable excipients, and uses for the same.

    Abstract translation: 公开了7-氯-N，N，5-三甲基-4-氧代-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺的新型结晶形式，方法 制备所述结晶形式的7-氯-N，N，5-三甲基-4-氧代-3-苯基-3,5-二氢-4H-哒嗪并[4,5-b]吲哚-1-乙酰胺，其组合物包含 所述形式与一种或多种药学上可接受的赋形剂混合，及其用途。

    Bicyclic heterocycles as cannabinoid-1 receptor modulators
    7.
    发明申请
    Bicyclic heterocycles as cannabinoid-1 receptor modulators 有权
    双环杂环作为大麻素-1受体调节剂

    公开(公告)号：US20060287324A1

    公开(公告)日：2006-12-21

    申请号：US11455039

    申请日：2006-06-16

    Applicant: Chongqing Sun ,  Yanting Huang ,  Doree Sitkoff ,  Taekyu Lee ,  William Ewing

    Inventor： Chongqing Sun ,  Yanting Huang ,  Doree Sitkoff ,  Taekyu Lee ,  William Ewing

    IPC: A61K31/503 ,  A61K31/4745 ,  C07D487/04 ,  C07D471/02

    CPC classification number: C07D471/04 ,  C07D487/04

    Abstract: The present application describes compounds according to Formula I, pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formula: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein A, B, R1, R2, R3 and R8 are described herein.

    Abstract translation: 本申请描述了根据式I的化合物，包含至少一种根据式I的化合物和任选的一种或多种另外的治疗剂的药物组合物和使用根据式I的化合物的治疗方法，其单独和与一种或多种另外的 治疗剂。 所述化合物具有以下通式：包括所有前药，溶剂化物，药学上可接受的盐和立体异构体，其中A，B，R 1，R 2，R 3 本文描述了本文和/或 8。

    Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors
    8.
    发明申请
    Heteroaryl 11-beta-hydroxysteroid dehydrogenase type I inhibitors 有权
    杂芳基11-β-羟基类固醇脱氢酶I型抑制剂

    公开(公告)号：US20060281750A1

    公开(公告)日：2006-12-14

    申请号：US11448946

    申请日：2006-06-07

    Applicant: James Li ,  Lawrence Hamann ,  Haixia Wang

    Inventor： James Li ,  Lawrence Hamann ,  Haixia Wang

    IPC: A61K31/503 ,  A61K31/4745 ,  A61K31/4192 ,  C07D471/02

    CPC classification number: C07D471/04

    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: W-L-Z   (I) or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein W, L and Z are defined herein.

    Abstract translation: 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新化合物具有以下结构：<？in-line-formula description =“In-line Formulas”end =“lead”？> WLZ（I）<？in-line-formula description =“In-line Formulas”end = 或其立体异构体或前药或其药学上可接受的盐，其中W，L和Z在本文中定义。

    Novel compounds
    9.
    发明申请
    Novel compounds 审中-公开
    新型化合物

    公开(公告)号：US20060223809A1

    公开(公告)日：2006-10-05

    申请号：US11447343

    申请日：2006-06-06

    Applicant: Martin Cooper ,  Simon Guile ,  Anthony Ingall ,  Rukhsana Rasul

    Inventor： Martin Cooper ,  Simon Guile ,  Anthony Ingall ,  Rukhsana Rasul

    IPC: A61K31/503 ,  C07D498/02

    CPC classification number: C07D495/04

    Abstract: The invention relates to thienopyridazinones of formula (I): wherein: R1 is C1-6 alkyl, C2-6 alkenyl or C3-6 cycloalkyl which is optionally substituted by C1-6 alkyl, each of the above being optionally substituted by one or more halogen atoms; R2 is C1-6 alkyl; R3 is a group CO-G or SO2-G where G is a 5- or 6-membered ring containing a nitrogen atom and a second heteroatom selected from oxygen and sulphur adjacent to the nitrogen, and optionally substituted by up to 3 groups selected from hydroxyl and C1-4 alkyl; Q is CR5R6 where R5 and R6 are as defined in the specification; and R4 is a 5- to 10-membered mono- or bi-cyclic aromatic ring system, containing 0 to 4 heteroatoms independently selected from nitrogen, oxygen and sulphur, the ring system being optionally substituted as described in the specification, and pharmaceutically acceptable salts and solvates thereof. Processes for their preparation, pharmaceutical compositions containing them and their use in therapy, in particular in the modulation of autoimmune disease are also described.

    Abstract translation: 本发明涉及式（I）的噻吩并哒嗪酮：其中：R 1是C 1-6烷基，C 2-6链烯基或C 任选被C 1-6烷基取代的，任选被一个或多个卤素原子取代的C 3-6环烷基; R 2是C 1-6烷基; R 3是基团CO-G或SO 2 -G，其中G是含有氮原子的5-或6-元环，和选自氧和/ 硫邻近氮，并且任选地被多至3个选自羟基和C 1-4烷基的基团取代; Q是CR 5，其中R 5和R 6如说明书中所定义; 并且R 4是含有0至4个独立地选自氮，氧和硫的杂原子的5至10元单环或双环芳族环系统，所述环系统如上所述被任选地取代 在本说明书及其药学上可接受的盐和溶剂化物中。 还描述了其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是在调节自身免疫疾病中。

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