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12 条记录 (耗时 0.047 秒)

    Bipyridyl amides as modulators of metabotropic glutamate receptor-5
    4.
    发明申请
    Bipyridyl amides as modulators of metabotropic glutamate receptor-5 审中-公开
    二吡啶基酰胺作为代谢型谷氨酸受体-5的调节剂

    公开(公告)号：US20070149547A1

    公开(公告)日：2007-06-28

    申请号：US10589407

    申请日：2005-02-09

    申请人： Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier

    发明人： Celine Bonnefous ,  Theodore Kamenecka ,  Jean-Michel Vernier

    IPC分类号： A61K31/497 ,  A61K31/444 ,  C07D403/02 ,  C07D401/02

    CPC分类号： C07D401/12 ,  C07D213/81 ,  C07D241/26 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07F7/0812

    摘要： The present invention is directed to novel amides such as those of Formula (I): (I) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel amides and/or compositions containing these compounds.

    摘要翻译： 本发明涉及新型酰胺，例如式（I）：（I）的那些酰胺，其为可用于治疗或预防涉及mGluR5的疾病和病症的mGluR5调节剂，包括但不限于精神和心境障碍 作为精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物 成瘾，药物滥用，戒毒，肥胖等疾病。 本发明还涉及包含这些化合物的药物组合物。 本发明还提供了一种通过施用有效量的这些新型酰胺和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

    Bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5
    5.
    发明申请
    Bipyridyl amines and ethers as modulators of metabotropic glutamate receptor-5 审中-公开
    联吡啶胺和醚作为代谢型谷氨酸受体-5的调节剂

    公开(公告)号：US20070027321A1

    公开(公告)日：2007-02-01

    申请号：US10570068

    申请日：2004-08-27

    申请人： Theodore Kamenecka ,  Jean-Michel Vernier ,  Celine Bonnefous ,  Steven Govek ,  John Hutchinson

    发明人： Theodore Kamenecka ,  Jean-Michel Vernier ,  Celine Bonnefous ,  Steven Govek ,  John Hutchinson

    IPC分类号： A61K31/4743 ,  C07D471/02 ,  C07D401/02 ,  C07D417/14

    CPC分类号： C07D213/74 ,  C04B35/632 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04

    摘要： The present invention is directed to novel bipyridyl amine and ether compounds such as those of Formula (I): (I) (where R?1#191, R?2#191, R?3#191, X and Y are as defined herein) which are mGluR5 modulators useful in the treatment or prevention of diseases and conditions in which mGluR5 is involved, including but not limited to psychiatric and mood disorders such as schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders, such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases. The invention is also directed to pharmaceutical compositions comprising these compounds. This invention further provides a method of treatment of these disorders and conditions by the administration of an effective amount of these novel bipyridyl amine and/or ether compounds and/or compositions containing these compounds.

    摘要翻译： 本发明涉及新型联吡啶胺和醚化合物，例如式（I）的那些：（I）（其中R 1＃191，R 2＃191，R 3＃191，X和Y如上所定义） 这是mGluR5调节剂，其可用于治疗或预防涉及mGluR5的疾病和病症，包括但不限于精神和心境障碍如精神分裂症，焦虑，抑郁，双相情感障碍和恐慌，以及在 治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠障碍，如转移工作诱导的睡眠障碍和时差，药物成瘾，药物滥用，药物戒断，肥胖症等疾病。 本发明还涉及包含这些化合物的药物组合物。 本发明还提供了通过施用有效量的这些新型联吡啶胺和/或醚化合物和/或含有这些化合物的组合物来治疗这些病症和病症的方法。

    Imidazolyl and pyrazolyl ethyne compounds
    7.
    发明申请
    Imidazolyl and pyrazolyl ethyne compounds 审中-公开
    咪唑基和吡唑基乙炔化合物

    公开(公告)号：US20050085523A1

    公开(公告)日：2005-04-21

    申请号：US10874991

    申请日：2004-06-23

    申请人： Nicholas Cosford ,  Theodore Kamenecka ,  Jeffrey Roppe

    发明人： Nicholas Cosford ,  Theodore Kamenecka ,  Jeffrey Roppe

    IPC分类号： C07D213/16 ,  C07D213/30 ,  C07D233/54 ,  C07D233/61 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D285/00 ,  C07D285/01 ,  C07D333/08 ,  A61K31/445 ,  A61K31/416 ,  A61K31/4172 ,  A61K31/4178

    CPC分类号： C07D213/16 ,  C07D213/30 ,  C07D239/26 ,  C07D241/12 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D277/22 ,  C07D277/24 ,  C07D277/40 ,  C07D285/01 ,  C07D333/08

    摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.

    摘要翻译： 根据本发明，提供了一类新的杂环化合物。 本发明的化合物含有包含至少一个氮原子和至少一个碳原子的取代的，不饱和的五，六或七元杂环。 该环另外包括独立地选自碳，氮，硫和氧原子的三个，四个或五个原子。 该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。 该环的强制取代基包括通过碳 - 碳双键，碳 - 碳三键或偶氮基与杂环连接的部分（B）。 强制性取代基位于环氮原子附近。 本发明化合物能够具有多种用途。 例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。 本发明的化合物也可以作为杀虫剂和杀真菌剂。 含有本发明化合物的药物组合物也具有广泛的用途。

    Substituted amidine derivatives as inhibitors of cell adhesion
    10.
    发明授权
    Substituted amidine derivatives as inhibitors of cell adhesion 失效
    取代的脒衍生物作为细胞粘附的抑制剂

    公开(公告)号：US06734311B2

    公开(公告)日：2004-05-11

    申请号：US09862151

    申请日：2001-05-21

    申请人： William K. Hagmann ,  Stephen E. DeLaszlo ,  Theodore Kamenecka ,  Malcolm MacCoss

    发明人： William K. Hagmann ,  Stephen E. DeLaszlo ,  Theodore Kamenecka ,  Malcolm MacCoss

    IPC分类号： C07D20704

    CPC分类号： C07D207/48 ,  C07D205/04

    摘要： Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

    摘要翻译： 式I的化合物是VLA-4和/或α4β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎， 接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症 关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。