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20 条记录 (耗时 0.04 秒)

    Benzoxazinone dopamine D4 receptor antagonists
    2.
    发明授权
    Benzoxazinone dopamine D4 receptor antagonists 失效
    苯并恶嗪酮多巴胺D4受体拮抗剂

    公开(公告)号：US06177422B1

    公开(公告)日：2001-01-23

    申请号：US09180376

    申请日：1998-11-04

    申请人： Thomas R. Belliotti ,  Lawrence D. Wise ,  David J. Wustrow

    发明人： Thomas R. Belliotti ,  Lawrence D. Wise ,  David J. Wustrow

    IPC分类号： A61K31535

    CPC分类号： C07D265/36

    摘要： This invention relates to compounds that are antagonists of dopamine D4 receptors, to methods of treating psychosis and schizophrenia using a compound that is an antagonist of dopamine D4 receptors, and to pharmaceutically acceptable compositions that contain a dopamine D4 receptor antagonist.

    摘要翻译： 本发明涉及作为多巴胺D4受体的拮抗剂的化合物，使用作为多巴胺D4受体的拮抗剂的化合物治疗精神病和精神分裂症的方法以及含有多巴胺D4受体拮抗剂的药学上可接受的组合物。

    2-substituted amino-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines as antiinflammatory agents
    3.
    发明授权
    2-substituted amino-4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidines as antiinflammatory agents 失效
    2-取代的氨基-4,6-二叔丁基-5-羟基-1,3-嘧啶作为抗炎剂

    公开(公告)号：US5284949A

    公开(公告)日：1994-02-08

    申请号：US29076

    申请日：1993-03-10

    申请人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan

    发明人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan

    IPC分类号： C07D239/46 ,  C07D403/12 ,  C07D417/12 ,  C07D239/02 ,  A61K31/505

    CPC分类号： C07D239/47 ,  C07D403/12 ,  C07D417/12

    摘要： The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.

    摘要翻译： 本发明是2-取代氨基-4,6-二叔丁基-5-羟基-1,3-嘧啶及其药学上可接受的酸加成盐或碱盐，药物组合物及其用途的新化合物。 本发明化合物被描述为具有作为5-脂氧合酶抑制剂和/或环氧合酶的作用的治疗，其提供有利于受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。 因此，本发明还涉及一种药物组合物或制备药物组合物用于治疗使用所提到的条件的方法。

    Thiadiazole or oxadiazole analogs of fenamic acids containing substituted hydroxamate side chains as antiinflammatory agents
    4.
    发明授权
    Thiadiazole or oxadiazole analogs of fenamic acids containing substituted hydroxamate side chains as antiinflammatory agents 失效
    含有取代的异羟肟酸侧链的灭胺酸的噻二唑或恶二唑类似物作为抗炎剂

    公开(公告)号：US5212189A

    公开(公告)日：1993-05-18

    申请号：US809686

    申请日：1991-12-17

    申请人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan

    发明人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan

    IPC分类号： C07D271/10 ,  C07D271/113 ,  C07D285/12 ,  C07D285/125

    CPC分类号： C07D271/113 ,  C07D285/125

    摘要： The present invention is a novel compound which is a thiadiazole or oxadiazole analog of a fenamic acid having a substituted hydroxamate side chain and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use thereof. The invention compounds are now found to have activity as inhibitors of one or both of cyclooxygenase and 5-lipoxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and the like. Thus, the present invention is also a pharmaceutical composition or method of use thereof.

    摘要翻译： 本发明是一种新颖的化合物，它是具有取代的异羟肟酸侧链及其药学上可接受的酸加成盐或碱式盐的茴香唑的噻二唑或恶二唑类似物，药物组合物及其使用方法。 现在发现本发明化合物具有作为环加氧酶和5-脂氧合酶之一或两者的抑制剂的活性，其提供有利地受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。 因此，本发明也是药物组合物或其使用方法。

    Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines
    5.
    发明授权
    Substituted 4,6-di-tertiary-butyl 5-hydroxy-pyrimidines 失效
    取代的4,6-二叔丁基5-羟基嘧啶

    公开(公告)号：US5356898A

    公开(公告)日：1994-10-18

    申请号：US84188

    申请日：1993-07-01

    申请人： Thomas R. Belliotti ,  Catherine R. Kostlan ,  David T. Connor

    发明人： Thomas R. Belliotti ,  Catherine R. Kostlan ,  David T. Connor

    IPC分类号： A61K31/505 ,  A61K31/506 ,  A61P1/04 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P29/00 ,  A61P43/00 ,  C07D239/34 ,  C07D239/36 ,  C07D401/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D239/02

    CPC分类号： C07D239/36 ,  C07D239/34 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  Y02P20/55

    摘要： The present invention is novel compounds which are 4,6-di-tertiary-butyl-5-hydroxy-1,3-pyrimidine substituted 1,2,4- and 1,3,4-thiadiazoles and oxadiazoles, and 1,2,4-triazoles, and pharmaceutically acceptable additions and base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever, and particularly rheumatoid arthritis, osteoarthritis, other inflammatory conditions, psoriasis, allergic diseases, asthma, inflammatory bowel disease, GI ulcers, cardiovascular conditions, including ischemic heart disease and atherosclerosis, and ischemia-induced cell damage, particularly brain damage caused by stroke. They can also be used topically for treating acne, sunburn, psoriasis, and eczema. Also included are leukotriene mediated pulmonary, gastrointestinal, inflammatory, dermatological, and cardiovascular conditions. The disclosed compounds also have potential utility as antioxidants. The preferred use is in treating inflammatory conditions. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.

    摘要翻译： PCT No.PCT / US92 / 00442 Sec。 371日期：1993年7月1日 102（e）日期1993年7月1日PCT提交1992年1月17日PCT公布。 出版物WO92 / 本发明是4,6-二叔丁基-5-羟基-1,3-嘧啶取代的1,2,4-和1,3,4-噻二唑的新化合物，以及 恶二唑和1,2,4-三唑及其药学上可接受的添加剂和碱盐，药物组合物及其使用方法。 现在发现本发明化合物具有作为5-脂氧合酶和/或环加氧酶的抑制剂的活性，其提供有利地受到包括炎症，关节炎，疼痛，发烧，特别是类风湿性关节炎，骨关节炎，其它炎性病症，牛皮癣， 过敏性疾病，哮喘，炎症性肠病，GI溃疡，心血管疾病，包括缺血性心脏病和动脉粥样硬化，以及缺血诱导的细胞损伤，特别是脑卒中引起的脑损伤。 它们也可以局部用于治疗痤疮，晒伤，牛皮癣和湿疹。 还包括白三烯介导的肺，胃肠道，炎症，皮肤病学和心血管疾病。 所公开的化合物还具有作为抗氧化剂的潜在用途。 优选的用途是治疗炎性病症。 因此，本发明也是制备用于治疗所述病症的药物组合物的药物组合物或方法。

    2-carbonyl substituted-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents
    6.
    发明授权
    2-carbonyl substituted-5-hydroxy-1, 3-pyrimidines as antiinflammatory agents 失效
    2-羰基取代-5-羟基-1,3-嘧啶作为抗炎剂

    公开(公告)号：US5187175A

    公开(公告)日：1993-02-16

    申请号：US847511

    申请日：1992-03-06

    申请人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan ,  Steven R. Miller

    发明人： Thomas R. Belliotti ,  David T. Connor ,  Catherine R. Kostlan ,  Steven R. Miller

    IPC分类号： C07D239/36 ,  C07D403/06 ,  C07D409/06 ,  C07D417/06 ,  C07F7/08

    CPC分类号： C07D239/36 ,  C07D403/06 ,  C07D409/06 ,  C07D417/06 ,  C07F7/0812

    摘要： The present invention is novel compounds which are 2-carbonyl substituted-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are now found to have activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.

    摘要翻译： 本发明是2-羰基取代-5-羟基-1,3-嘧啶及其药学上可接受的酸加成盐或碱盐，药物组合物及其用途的新化合物。 现在发现本发明化合物具有作为5-脂氧合酶抑制剂和/或环加氧酶的活性的作用，其提供有利地受到包括炎症，关节炎，疼痛，发烧等的这种抑制影响的病症的治疗。 因此，本发明也是制备用于治疗所述病症的药物组合物的药物组合物或方法。