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    Aryl substituted pyridines, pyrimidines, pyrazines and triazines and the use thereof
    5.
    发明申请
    Aryl substituted pyridines, pyrimidines, pyrazines and triazines and the use thereof 审中-公开
    芳基取代的吡啶，嘧啶，吡嗪和三嗪及其用途

    公开(公告)号：US20040192691A1

    公开(公告)日：2004-09-30

    申请号：US10738989

    申请日：2003-12-19

    Applicant: Euro-Celtique S.A.

    Inventor： Derk J. Hogenkamp ,  Phong Nguyen ,  Bin Shao

    IPC: A61K031/53 ,  A61K031/497 ,  A61K031/505

    CPC classification number: C07D213/81 ,  C07D239/28 ,  C07D239/38 ,  C07D241/24 ,  C07D251/24 ,  C07D403/04

    Abstract: This invention relates aryl substituted pyridines, pyrimidines, pyrazines and triazines of Formula I: 1 or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein A1, A2, A3, R1-R4, X and Y are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

    Abstract translation: 本发明涉及式I的芳基取代的吡啶，嘧啶，吡嗪和三嗪：或其药学上可接受的盐，前药或溶剂化物，其中A1，A2，A3，R1-R4，X和Y置于说明书中。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。

    Treatment of type 1 diabetes with PDE5 inhibitors
    6.
    发明申请
    Treatment of type 1 diabetes with PDE5 inhibitors 审中-公开
    用PDE5抑制剂治疗1型糖尿病

    公开(公告)号：US20040186046A1

    公开(公告)日：2004-09-23

    申请号：US10799191

    申请日：2004-03-12

    Applicant: Pfizer Inc

    Inventor： Gillian Munro Burgess ,  Earl Michael Gibbs ,  Christopher Peter Wayman

    IPC: A61K038/28 ,  A61K031/505 ,  A61K031/401 ,  A61K031/366

    CPC classification number: A61K31/401 ,  A61K31/00 ,  A61K31/366 ,  A61K31/505 ,  A61K31/519 ,  A61K31/53

    Abstract: The use of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof in the preparation of a medicament for the treatment of Type 1 Diabetes. A method of treating Type 1 Diabetes in an individual suffering from Type 1 Diabetes, which method comprises administering to said individual an effective amount of a PDE5 inhibitor without substantial PDE2 inhibiting activity, or a pharmaceutically acceptable salt thereof.

    Abstract translation: 使用没有实质的PDE2抑制活性的PDE5抑制剂或其药学上可接受的盐在制备用于治疗1型糖尿病的药物中的用途。 一种在1型糖尿病个体中治疗1型糖尿病的方法，该方法包括向所述个体施用有效量的不具有实质性PDE2抑制活性的PDE5抑制剂或其药学上可接受的盐。

    Acyclic amide and sulfonamide ligands for the estrogen receptor
    9.
    发明申请
    Acyclic amide and sulfonamide ligands for the estrogen receptor 失效
    用于雌激素受体的非环酰胺和磺酰胺配体

    公开(公告)号：US20040110767A1

    公开(公告)日：2004-06-10

    申请号：US10666811

    申请日：2003-09-17

    Applicant: Pfizer Inc

    Inventor： Kimberly O. Cameron ,  Richard Chesworth

    IPC: A61K031/4965 ,  A61K031/505 ,  C07D213/72

    CPC classification number: C07D249/08 ,  C07C233/60 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/08 ,  C07D207/16 ,  C07D211/14 ,  C07D211/42 ,  C07D211/46 ,  C07D213/38 ,  C07D213/40 ,  C07D215/20 ,  C07D215/36 ,  C07D217/02 ,  C07D231/12 ,  C07D233/56 ,  C07D261/10 ,  C07D295/088 ,  C07D295/135 ,  C07D295/185 ,  C07D307/12 ,  C07D333/34

    Abstract: The present invention provides estrogen receptor (ER) ligands of structural formula (I) 1 the pharmaceutically acceptable salts, stereoisomers, and prodrugs thereof, and the pharmaceutically acceptable salts of the prodrugs, wherein R1, R2, R3, R4, R5, X, and Q are as defined herein. The invention further provides pharmaceutical compositions comprising the compounds of formula (I), and methods for treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER which comprise administering to a mammalian subject in need of treatment therewith, an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug, or a pharmaceutical composition comprising a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, or prodrug thereof, or a pharmaceutically acceptable salt of the prodrug. The invention further provides pharmaceutical compositions comprising combinations of the compounds of formula (I) and one or more of sodium fluoride, estrogen, a bone anabolic agent, a growth hormone or growth hormone secretagogue, a prostaglandin agonist/antagonist, and a parathyroid hormone, and methods of treating or preventing diseases, disorders, conditions, or symptoms mediated by an ER comprising the administration of an effective amount of such combination to a mammalian subject in need of treatment therewith.

    Abstract translation: 本发明提供结构式（I）的药学上可接受的盐，立体异构体和前药的雌激素受体（ER）配体和前药的药学上可接受的盐，其中R 1，R 2，R 3 R 4，R 5，X和Q如本文所定义。 本发明还提供包含式（I）化合物的药物组合物，以及用于治疗或预防由ER介导的疾病，病症，病状或症状的方法，其包括向需要治疗的哺乳动物受试者施用有效量的 式（I）化合物或其药学上可接受的盐，立体异构体或前药，或前药的药学上可接受的盐，或包含式（I）化合物或其药学上可接受的盐，立体异构体， 或前药，或前药的药学上可接受的盐。 本发明进一步提供包含式（I）化合物和一种或多种氟化钠，雌激素，骨合成代谢剂，生长激素或生长激素促分泌素，前列腺素激动剂/拮抗剂和甲状旁腺激素的组合的药物组合物， 以及治疗或预防由ER介导的疾病，病症，病症或症状的方法，包括向需要治疗的哺乳动物受试者施用有效量的这种组合。

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