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    2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1lambd6-THIOMORPHOLIN-4-YL)-4-(2-METHYL OR 4-FLUORO-2-METHYL SUBSTITUTED)PHENYL-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE
    2.
    发明申请
    2-(3,5-BIS-TRIFLUOROMETHYL-PHENYL)-N-[6-(1,1-DIOXO-1lambd6-THIOMORPHOLIN-4-YL)-4-(2-METHYL OR 4-FLUORO-2-METHYL SUBSTITUTED)PHENYL-PYRIDIN-3-YL]-N-METHYL-ISOBUTYRAMIDE 审中-公开
    2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1-氨基-6-吗啉-4-基）-4-（2-甲基或4-氟-2-甲基取代的 ）苯基 - 吡啶-3-基] -N-甲基 - 异丁酰胺

    公开(公告)号：WO03011860A3

    公开(公告)日：2003-09-04

    申请号：PCT/EP0208311

    申请日：2002-07-26

    Applicant: HOFFMANN LA ROCHE

    Inventor： BALLARD THERESA MARIA ,  HOFFMANN TORSTEN ,  POLI SONIA MARIA ,  SCHNIDER PATRICK ,  SLEIGHT ANDREW

    IPC: A61K31/541 ,  A61P1/00 ,  A61P1/08 ,  A61P11/00 ,  A61P11/02 ,  A61P11/06 ,  A61P13/02 ,  A61P13/08 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D213/75

    CPC classification number: C07D213/75

    Abstract: The invention relates to the compounds 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambd6-thiomorpholin-4-yl)-4-o-tolyl-pyridin-3-yl]-N-methyl-isobutyramide and 2-(3,5-bis-trifluoromethyl-phenyl)-N-[6-(1,1-dioxo-1lambd6 -thiomorpholin-4-yl)-4-(4-fluoro-2-methyl-phenyl)-pyridin-3-yl]-N-methyl-isobutyramide, which may be used for the treatment of migraine, rheumatoid arthritis, asthma, bronchial hyperreactivity, inflammatory bowel disease or for the treatment of disorders including Parkinson's disease, anxiety, depression, pain, headache, Alzheimer's disease, multiple sclerosis,oedema, allergic rhinitis, Crohn's disease, ocular injury, ocular inflammatory diseases, psychosis, motion sickness, induced vomiting, emesis, urinary incontinence, psychoimmunologic or psychosomatic disorders, cancer, withdrawel symptoms of addictive drugs from opiates or nicotine, traumatic brain injury or benign prostatic hyperplasia.

    Abstract translation: 本发明涉及化合物2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1,11-硫代吗啉-4-基）-4-邻甲苯基 - 吡啶-3-基 - 基] -N-甲基 - 异丁酰胺和2-（3,5-双 - 三氟甲基 - 苯基）-N- [6-（1,1-二氧代-1-氨基-6-硫代吗啉-4-基）-4-（4- 氟-2-甲基 - 苯基） - 吡啶-3-基] -N-甲基 - 异丁酰胺，其可用于治疗偏头痛，类风湿性关节炎，哮喘，支气管高反应性，炎性肠病或用于治疗疾病，包括 帕金森病，焦虑症，抑郁症，疼痛，头痛，阿尔茨海默氏病，多发性硬化症，水肿，过敏性鼻炎，克罗恩病，眼部损伤，眼部炎症性疾病，精神病，运动病，诱发性呕吐，呕吐，尿失禁，心理免疫或心身疾病， 癌症，从阿片剂或尼古丁，外伤性脑损伤或良性前列腺增生症中消除上瘾药物的症状。

    5.
    发明专利
    未知

    公开(公告)号：DE602004009195D1

    公开(公告)日：2007-11-08

    申请号：DE602004009195

    申请日：2004-07-17

    Applicant: HOFFMANN LA ROCHE

    Inventor： BALLARD THERESA MARIA ,  GATTI MCARTHUR SILVIA ,  GOETSCHI ERWIN ,  WICHMANN JUERGEN ,  WOLTERING THOMAS JOHANNES

    IPC: A61K31/551 ,  A61K31/4535 ,  A61K31/473 ,  A61K31/55 ,  A61K31/662 ,  A61K31/7068 ,  A61K45/06

    Abstract: The present invention relates to a pharmaceutical composition comprising an inhibitor of acetylcholinesterase (AChE inhibitor) and a metabotropic glutamate receptor 2 antagonist (mGluR2 antagonist) and a pharmaceutically acceptable excipient. The invention also relates to a method of treating and/or preventing acute and/or chronic neurological disorders comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said AChE inhibitor and mGluR2 antagonist as well as a kit comprising said AChE inhibitor and mGluR2 antagonist. In particular, the mGluR2 antagonist relates to the compound of formula I wherein, R 1 , R 2 , R 3 , X and Y are described hereinabove. The combination of the AChE inhibitor and mGluR2 antagonist is useful for treating and/or preventing chronic neurological disorders. These disorders include Alzheimer's disease and mild cognitive impairment.

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