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118 条记录 (耗时 0.051 秒)

    DIARYL MORPHOLINES AS CB1 MODULATORS
    56.
    发明申请
    DIARYL MORPHOLINES AS CB1 MODULATORS 审中-公开
    二元醇作为CB1调节剂

    公开(公告)号：US20100197564A1

    公开(公告)日：2010-08-05

    申请号：US12593777

    申请日：2008-04-17

    申请人： Jack D. Scott ,  Andrew Stamford

    发明人： Jack D. Scott ,  Andrew Stamford

    IPC分类号： A61K31/5355 ,  C07D265/30 ,  A61K31/5375 ,  C07D413/12 ,  A61K38/28 ,  A61K31/397 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P25/00 ,  A61P29/00 ,  A61P1/00 ,  A61P9/00

    CPC分类号： C07D265/30 ,  C07D265/32 ,  C07D413/12

    摘要： The present invention provides compounds having the general structure of Formula (I) or a pharmaceutically acceptable salt, solvate, ester or prodrug thereof, which are useful as CB1 receptor antagonists. The compounds of the invention may be useful in treating diseases, disorders, or conditions responsive to CB1 receptor antagonists, including, but not limited to, metabolic syndrome, obesity, waist circumference, dyslipidemia, insulin sensitivity, neuroinflammatory disorders, cognitive disorders, psychosis, addictive behavior, gastrointestinal disorders, and cardiovascular conditions.

    摘要翻译： 本发明提供具有式（I）的通式结构的化合物或其药学上可接受的盐，溶剂合物，酯或前药，其可用作CB1受体拮抗剂。 本发明的化合物可用于治疗对CB1受体拮抗剂反应的疾病，病症或病症，包括但不限于代谢综合征，肥胖症，腰围，血脂异常，胰岛素敏感性，神经炎症性疾病，认知障碍，精神病， 成瘾行为，胃肠道疾病和心血管疾病。

    CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT
    58.
    发明申请
    CYCLIC AMINE BACE-1 INHIBITORS HAVING A HETEROCYCLIC SUBSTITUENT 有权
    具有杂环取代基的循环胺BACE-1抑制剂

    公开(公告)号：US20090312341A1

    公开(公告)日：2009-12-17

    申请号：US12490884

    申请日：2009-06-24

    申请人： Jared N. Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X. H. Le ,  Jeffrey F. Lowrie

    发明人： Jared N. Cumming ,  Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Yusheng Wu ,  Jianping Pan ,  Tao Guo ,  Douglas W. Hobbs ,  Thuy X. H. Le ,  Jeffrey F. Lowrie

    IPC分类号： A61K31/496 ,  C12N9/99 ,  A61P25/28

    CPC分类号： C04B35/632 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24) (R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

    摘要翻译： 公开了下式的新化合物或其药学上可接受的盐或溶剂合物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24）（R 25）或-SR 35; R41是烷基，环烷基，-SO2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH3; 其余变量如本说明书中所定义。 还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂 疾病

    Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction
    59.
    发明授权
    Metabolite of xanthine Phosphodiesterase 5 inhibitor and derivatives thereof useful for treatment of erectile dysfunction 失效
    黄嘌呤的代谢物磷酸二酯酶5抑制剂及其衍生物可用于治疗勃起功能障碍

    公开(公告)号：US07312223B2

    公开(公告)日：2007-12-25

    申请号：US10901574

    申请日：2004-07-29

    申请人： Anima Ghosal ,  Wei Tong ,  Swapan K. Chowdhury ,  Shmuel Zbaida ,  Mark A. Wirth ,  Kevin B. Alton ,  James E. Patrick ,  Craig D. Boyle ,  Andrew Stamford

    发明人： Anima Ghosal ,  Wei Tong ,  Swapan K. Chowdhury ,  Shmuel Zbaida ,  Mark A. Wirth ,  Kevin B. Alton ,  James E. Patrick ,  Craig D. Boyle ,  Andrew Stamford

    IPC分类号： C07D473/06 ,  A61K31/522 ,  A61P9/10 ,  A61P9/12

    CPC分类号： C07D473/06

    摘要： The present invention is directed to a metabolite of a xanthine Phosphodiesterase type 5 inhibitor having the following structure derivatives, and formulations thereof, and processes for preparing the same. Further disclosed are methods of treating a physiological disorder, symptom or disease in a patient, comprising administering to the patient an effective amount of the above compound, wherein the physiological disorder, symptom or disease is a urogenital, cardiovascular, cerebrovascular or peripheral vascular disorder, angina pectoris, hypertension, restenosis post angioplasty, endarterectomy, stent introduction, cerebral stroke, a respiratory tract disorder such as an allergic condition associated with atopy, pulmonary hypertension, an ischemic heart disorder, impaired glucose tolerance, diabetes and its related complication, insulin resistance syndrome, hyperglycemia, polycystic ovarian syndrome, a glomerular disorder, renal insufficiency, nephritis, a tubular interstitial disorder, an autoimmune disorder, glaucoma, intestinal motility, cachexia or cancer.

    摘要翻译： 本发明涉及具有以下结构衍生物的黄嘌呤磷酸二酯酶5型抑制剂的代谢物及其制剂及其制备方法。 进一步公开的是治疗患者的生理障碍，症状或疾病的方法，包括向患者施用有效量的上述化合物，其中所述生理障碍，症状或疾病是泌尿生殖系统，心血管，脑血管或外周血管疾病， 心绞痛，高血压，血管成形术后再狭窄，内膜切除术，支架引入，脑中风，呼吸道疾病如与过敏相关的过敏性疾病，肺动脉高压，缺血性心脏病，糖耐量异常，糖尿病及其相关并发症，胰岛素抵抗 综合征，高血糖症，多囊卵巢综合征，肾小球疾病，肾功能不全，肾炎，管状间质性疾病，自身免疫性疾病，青光眼，肠蠕动，恶病质或癌症。

    2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
    60.
    发明申请
    2-alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists 有权
    2-炔基 - 和2-烯基 - 吡唑并[4,3-e] -1,2,4-三唑并 - [1,5-c] - 嘧啶腺苷A2a受体拮抗剂

    公开(公告)号：US20050222164A1

    公开(公告)日：2005-10-06

    申请号：US11135261

    申请日：2005-05-23

    申请人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford

    发明人： Bernard Neustadt ,  Jinsong Hao ,  Hong Liu ,  Craig Boyle ,  Samuel Chackalamannil ,  Unmesh Shah ,  Andrew Stamford

    IPC分类号： A61P25/16 ,  C07D487/14 ,  A61K31/519

    CPC分类号： C07D487/14

    摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.

    摘要翻译： 具有结构式I的化合物或其药学上可接受的盐，其中R是R 1，R 2，R 3，R 3， 4和R 5是H，烷基或烷氧基烷基; R 6是H，烷基，羟基烷基或-CH 2 F; R 7，R 8和R 9是H，烷基，烷氧基，烷硫基，烷氧基烷基，卤素或-CF 3， SUB>; 和Z是任选取代的芳基，杂芳基或杂芳基 - 烷基。 还公开了式I化合物在治疗中枢神经系统疾病，特别是帕金森病中单独使用或与用于治疗帕金森病的其它药物组合的用途，以及包含它们的药物组合物的用途。