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545 条记录 (耗时 0.051 秒)

    Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates
    72.
    发明申请
    Preparation and use of 2-substituted-5-oxo-3-pyrazolidinecarboxylates 有权

    公开(公告)号：US20070021468A1

    公开(公告)日：2007-01-25

    申请号：US10546165

    申请日：2004-03-25

    申请人： Gary Annis

    发明人： Gary Annis

    IPC分类号： A61K31/4439 ,  A61K31/4152 ,  C07D231/18 ,  C07D403/04

    CPC分类号： C07D231/06 ,  C07D409/04

    摘要： A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II) wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl. Also disclosed is a crystalline composition comprising at least about 90% by weight of the compound of the formula R1OC(O)C(H)(X)C(R2a)(R2b)CO2H (i.e. Formula VI) wherein R2a and R2b are H, X is Br and R1 is methyl.

    Pyrazole modulators of metabotropic glutamate receptors
    75.
    发明申请
    Pyrazole modulators of metabotropic glutamate receptors 审中-公开
    代谢型谷氨酸受体的吡唑调节剂

    公开(公告)号：US20060281803A1

    公开(公告)日：2006-12-14

    申请号：US10572772

    申请日：2004-09-17

    申请人： Craig Lindsley ,  David Wisnoski

    发明人： Craig Lindsley ,  David Wisnoski

    IPC分类号： C07D231/50 ,  A61K31/4152

    CPC分类号： C07D233/88 ,  C07D231/40 ,  C07D233/90 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D495/04

    摘要： The present invention is directed to compounds which are allosteric modulators of metabotropic glutamate receptors, including the mGluR5 receptor, and which are useful in the treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.

    摘要翻译： 本发明涉及作为代谢型谷氨酸受体的变构调节剂（包括mGluR5受体）的化合物，它们可用于治疗与谷氨酸功能障碍相关的神经和精神病学障碍以及参与代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

    Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists
    78.
    发明申请
    Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists 审中-公开
    用作PG12拮抗剂的双（杂）芳基甲酰胺衍生物

    公开(公告)号：US20060247260A1

    公开(公告)日：2006-11-02

    申请号：US10544033

    申请日：2004-01-28

    申请人： Toshiki Murata ,  Takuya Shintani ,  Masaomi Umeda ,  Takashi Iino ,  Toshiya Moriwaki

    发明人： Toshiki Murata ,  Takuya Shintani ,  Masaomi Umeda ,  Takashi Iino ,  Toshiya Moriwaki

    IPC分类号： A61K31/513 ,  A61K31/4412 ,  A61K31/42 ,  A61K31/4152 ,  A61K31/195

    CPC分类号： C07D207/325 ,  C07D211/14 ,  C07D213/64 ,  C07D213/82 ,  C07D231/12 ,  C07D231/14 ,  C07D239/34 ,  C07D261/18 ,  C07D333/38

    摘要： This invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) in which Ar1 and Ar2 independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R6 represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.

    摘要翻译： 本发明涉及式（I）的芳基或杂芳基酰氨基烷烃衍生物，其中Ar 1和Ar 2独立地表示苯基或5或6元杂芳环R 6是代表羧基或四唑基，其余的变量如本文和权利要求中所定义，其可用作药物制剂的活性成分。 本发明的芳基或杂芳基酰氨基烷烃具有PGI 2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。 这些疾病包括泌尿系统疾病或紊乱，如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱反应过度，前列腺肥大 ），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。 本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压;血友病和出血; 和炎症，因为这些疾病也与PGI2有关。