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31.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。
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32.发明授权公开(公告)号：US08415297B2
公开(公告)日：2013-04-09
申请号：US13398887
申请日：2012-02-17
申请人： Tesfaye Biftu , Ann E. Weber
发明人： Tesfaye Biftu , Ann E. Weber
IPC分类号： A61K31/4162 , A61K38/28 , C07D487/04 , A61P3/10
CPC分类号： C07D309/30 , A61K9/2054 , A61K31/4162 , A61K38/1709 , A61K38/26 , A61K45/06 , C07D487/04
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.
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33.发明授权Hexahydrodiazepinones as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权六氢二氮杂酮作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病公开(公告)号：US07259160B2
公开(公告)日：2007-08-21
申请号：US10566235
申请日：2004-07-27
IPC分类号： C07D243/08 , A61K31/551 , A61P3/10
CPC分类号： C07D243/14 , C07D401/06 , C07D487/04
摘要： The present invention is directed to hexahydrodiazepinone compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-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： 本发明涉及作为二肽基肽酶-IV酶（“DPP-IV抑制剂”）的抑制剂的六氢二氮杂酮化合物，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。
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34.发明授权公开(公告)号：US07101871B2
公开(公告)日：2006-09-05
申请号：US10501059
申请日：2003-10-14
IPC分类号： C07D243/08 , A61K31/551 , A61P3/10
CPC分类号： C07D243/08 , C07D401/06 , C07D403/06 , C07K5/06191
摘要： The present invention is directed to compounds 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.
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35.发明申请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：US20070232676A1
公开(公告)日：2007-10-04
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： A01N43/56
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。
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36.发明申请SUBSTITUTED SEVEN-MEMBERED HETEROCYCLIC COMPOUNDS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 有权作为用于治疗糖尿病的DIPEPTIDYDEPDDIV-IV抑制剂的取代的七分子杂环化合物公开(公告)号：US20130203786A1
公开(公告)日：2013-08-08
申请号：US13643121
申请日：2011-05-16
IPC分类号： C07D487/04 , A61K31/506 , A61K45/06 , A61K31/519 , A61K31/437 , A61K31/4162 , A61K31/4439
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds 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）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，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。
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37.发明申请NOVEL CRYSTALLINE FORMS OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR 有权一种DIPEPTIDYL PEPTIDASE-IV抑制剂的新型结晶形式公开(公告)号：US20140080884A1
公开(公告)日：2014-03-20
申请号：US14118998
申请日：2012-06-25
申请人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
发明人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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38.发明授权Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes 有权取代的七元杂环化合物作为二肽基肽酶-IV抑制剂用于治疗糖尿病公开(公告)号：US08980929B2
公开(公告)日：2015-03-17
申请号：US13643121
申请日：2011-05-16
IPC分类号： A01N43/78 , A61K31/425 , C07D413/00 , C07D498/00 , C07D417/00 , C07D513/00 , C07D271/12 , C07D285/14 , C07D487/04 , C07D471/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K45/06 , C07D471/04
摘要： The present invention is directed to novel amino-substituted seven-membered heterocyclic compounds 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）的新型氨基取代的七元杂环化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防其中二肽基肽酶-IV酶 涉及糖尿病，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。
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公开(公告)号：US08895603B2
公开(公告)日：2014-11-25
申请号：US14118998
申请日：2012-06-25
申请人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
发明人： Itzia Arroyo , Davida Krueger , Ping Chen , Aaron Moment , Tesfaye Biftu , Faye Sheen , Yanfeng Zhang
IPC分类号： A61K31/4162 , C07D231/00 , C07D487/04 , A61K31/4439 , A61K31/4985 , A61K31/513
CPC分类号： C07D487/04 , A61K31/4162 , A61K31/4439 , A61K31/4985 , A61K31/513 , C07B2200/13 , Y02P20/55
摘要： Novel crystalline forms of (2R,3S,5R)-2-(2,5-Difluorophenyl)-5-[2-(methylsulfonyl)-2,6-dihydropyrrolo[3,4-c]pyrazol-5(4H)-yl]tetrahydro-2H-pyran-3-amine are potent inhibitors of dipeptidyl peptidase-IV and are useful for the treatment of non-insulin dependent (Type 2) diabetes mellitus. The invention also relates to pharmaceutical compositions containing these novel forms, processes to prepare these forms and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes.
摘要翻译： （2R，3S，5R）-2-（2,5-二氟苯基）-5- [2-（甲基磺酰基）-2,6-二氢吡咯并[3,4-c]吡唑-5（4H） - 吡啶-3-基]四氢-2H-吡喃-3-胺是二肽基肽酶-IV的有效抑制剂，可用于治疗非胰岛素依赖型（2型）糖尿病。 本发明还涉及含有这些新型形式的药物组合物，制备这些形式的方法及其药物组合物及其用于治疗2型糖尿病的用途。
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40.发明授权(Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds 失效（嘧啶基）（苯基）取代的稠合杂芳基p38抑制和PKG激酶抑制化合物公开(公告)号：US07196095B2
公开(公告)日：2007-03-27
申请号：US10477367
申请日：2002-06-21
申请人： Tesfaye Biftu , Richard Beresis , Richard Berger , Steven L. Colletti , James B. Doherty , Dennis D. Feng , Gui-Bai Liang , Dennis M. Schmatz , Xiaoxia Qian , David A. Claremon , Nigel J. Liverton , Charles J. McIntyre , Ernest W. Kovacs
发明人： Tesfaye Biftu , Richard Beresis , Richard Berger , Steven L. Colletti , James B. Doherty , Dennis D. Feng , Gui-Bai Liang , Dennis M. Schmatz , Xiaoxia Qian , David A. Claremon , Nigel J. Liverton , Charles J. McIntyre , Ernest W. Kovacs
IPC分类号： C07D403/04 , C07D403/14 , C07D417/04 , C07D417/14 , A61K31/506 , A61P19/02
CPC分类号： C07D403/04 , A23K20/10 , A23K20/111 , A61K31/429 , A61K31/4355 , A61K31/506 , A61K31/519 , A61K31/53 , A61K45/06 , C07D453/02 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/14 , C07D513/04 , A61K2300/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are useful in the treatment of cytokine mediated diseases such as arthritis and in the treatment and/or prevention of protozoal diseases such as coccidiosis
摘要翻译： 式（I）化合物及其药学上可接受的盐可用于治疗细胞因子介导的疾病如关节炎和治疗和/或预防原虫感染疾病如球虫病
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