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    Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    4.
    发明授权
    Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权
    氨基四氢吡喃作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病

    公开(公告)号：US07678905B2

    公开(公告)日：2010-03-16

    申请号：US11728673

    申请日：2007-03-27

    申请人： Tesfaye Biftu ,  Ann E. Weber

    发明人： Tesfaye Biftu ,  Ann E. Weber

    IPC分类号： C07D251/00

    CPC分类号： C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

    摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿病 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二肽基肽酶-IV酶的疾病中的用途。

    3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
    5.
    发明授权
    3-Amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes 有权
    3-氨基-4-苯基丁酸衍生物作为二肽基肽酶抑制剂用于治疗或预防糖尿病

    公开(公告)号：US07560455B2

    公开(公告)日：2009-07-14

    申请号：US10556805

    申请日：2004-05-10

    申请人： Tesfaye Biftu ,  Danqing Dennis Feng ,  Gui Bai Liang ,  Xiaoxia Qian

    发明人： Tesfaye Biftu ,  Danqing Dennis Feng ,  Gui Bai Liang ,  Xiaoxia Qian

    IPC分类号： A61P3/10 ,  A61K31/55 ,  C07D491/00

    CPC分类号： C07D487/04

    摘要： The pre-sent invention is directed to 3-amino-4-phenylbutanoic acid derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

    摘要翻译： 预先发明的发明涉及作为二肽基肽酶-IV酶（“DP-IV抑制剂”）的抑制剂的3-氨基-4-苯基丁酸衍生物，其可用于治疗或预防其中二肽基 涉及肽酶-IV酶，如糖尿病，特别是2型糖尿病。 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二肽基肽酶-IV酶的疾病中的用途。

    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders
    8.
    发明授权
    Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders 失效
    用于治疗心血管，炎症和免疫疾病的化合物和方法

    公开(公告)号：US5792776A

    公开(公告)日：1998-08-11

    申请号：US265656

    申请日：1994-06-27

    申请人： Tesfaye Biftu ,  Ralph Scannell ,  Xiong Cai ,  Sajjat Hussoin

    发明人： Tesfaye Biftu ,  Ralph Scannell ,  Xiong Cai ,  Sajjat Hussoin

    IPC分类号： C07D307/14 ,  C07D471/04 ,  A61K31/44 ,  A61K31/40 ,  C07C233/00 ,  C07D307/02

    CPC分类号： C07D471/04 ,  C07D307/14

    摘要： Disubstituted tetrahydrofurans, tetrahydrothiophenes, pyrrolidines and cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. A method to treat disorders mediated by PAF and/or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

    摘要翻译： 公开了二取代的四氢呋喃，四氢噻吩，吡咯烷和环戊烷，其减少趋化性和呼吸道爆发，导致在炎性或免疫反应期间形成多形核白细胞的有害氧自由基。 通过作为PAF受体拮抗剂，通过抑制酶5-脂氧合酶，或通过显示双重活性，化合物表现出这种生物学活性， 即作为PAF受体拮抗剂和5-脂肪氧合酶抑制剂。 还公开了治疗由PAF和/或白三烯介导的病症的方法，其包括任选地在药学上可接受的载体中施用有效量的一种或多种上述化合物或其药学上可接受的盐。