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公开(公告)号：US20100093808A1
公开(公告)日：2010-04-15
申请号：US12637047
申请日：2009-12-14
申请人： André Bubendorf , Olaf Grassmann , Daniel Hunziker , Holger Kuehne , Regina Moog , Urs Schwitter
发明人： André Bubendorf , Olaf Grassmann , Daniel Hunziker , Holger Kuehne , Regina Moog , Urs Schwitter
IPC分类号： A61K31/4439 , C07D401/14 , A61P3/00
CPC分类号： C07D401/14
摘要： The invention is concerned with (2S)-1-{[1,1-Dimethyl-3-(4-pyridin-3-yl-imidazol-1-yl)-propylamino]-acetyl}-pyrrolidine-2-carbonitrile fumarate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.
摘要翻译： 本发明涉及（2S）-1 - {[1,1-二甲基-3-（4-吡啶-3-基 - 咪唑-1-基） - 丙基氨基] - 乙酰基} - 吡咯烷-2-甲腈富马酸盐和 该化合物的结晶多晶型物。 该化合物及其多晶型与先前已知的化合物相比表现出优异的性质，可用作治疗与DPP-IV相关的疾病的药物。
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公开(公告)号：US20070142436A1
公开(公告)日：2007-06-21
申请号：US11638752
申请日：2006-12-14
申请人： Andre Bubendorf , Olaf Grassmann , Daniel Hunziker , Holger Kuehne , Regina Moog , Urs Schwitter
发明人： Andre Bubendorf , Olaf Grassmann , Daniel Hunziker , Holger Kuehne , Regina Moog , Urs Schwitter
IPC分类号： A61K31/4439 , C07D403/14
CPC分类号： C07D401/14
摘要： The invention is concerned with (2S)-1-{[1,1 -Dimethyl-3-(4-pyridin-3-yl-imidazol-1-yl)-propylamino]-acetyl}-pyrrolidine-2-carbonitrile fumarate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.
摘要翻译： 本发明涉及（2S）-1 - {[1,1-二甲基-3-（4-吡啶-3-基 - 咪唑-1-基） - 丙基氨基] - 乙酰基} - 吡咯烷-2-甲腈富马酸盐和 该化合物的结晶多晶型物。 该化合物及其多晶型与先前已知的化合物相比表现出优异的性质，可用作治疗与DPP-IV相关的疾病的药物。
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公开(公告)号：US06861440B2
公开(公告)日：2005-03-01
申请号：US10269519
申请日：2002-10-14
申请人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
发明人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
IPC分类号： A61K20060101 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5355 , A61P1/00 , A61P1/04 , A61P3/04 , A61P3/10 , C07D20060101 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
CPC分类号： C07D277/06 , A61K9/0019 , A61K9/1623 , A61K9/2853 , A61K9/2866 , A61K9/4825 , A61K9/4858 , A61K9/4875 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
摘要翻译： 本发明涉及其中R 1，R 2和X如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：US07803819B2
公开(公告)日：2010-09-28
申请号：US11778796
申请日：2007-07-17
申请人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
发明人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
IPC分类号： A61K31/44 , C07D401/04 , C07D401/14
CPC分类号： C07D277/06 , A61K9/0019 , A61K9/1623 , A61K9/2853 , A61K9/2866 , A61K9/4825 , A61K9/4858 , A61K9/4875 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
摘要翻译： 本发明涉及式（I）化合物，其中R 1，R 2和X如说明书和权利要求中所定义，及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：US07314884B2
公开(公告)日：2008-01-01
申请号：US11010899
申请日：2004-12-13
申请人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
发明人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Michael Loeffler , Ramakanth Sarabu , Hans Peter Wessel
IPC分类号： A61K31/422 , C07D405/12
CPC分类号： C07D277/06 , A61K9/0019 , A61K9/1623 , A61K9/2853 , A61K9/2866 , A61K9/4825 , A61K9/4858 , A61K9/4875 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
摘要翻译： 本发明涉及其中R 1，R 2和X如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：US20070259925A1
公开(公告)日：2007-11-08
申请号：US11778796
申请日：2007-07-17
申请人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Loeffler , Ramakanth Sarabu , Hans Peter Wessel
发明人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Loeffler , Ramakanth Sarabu , Hans Peter Wessel
IPC分类号： A61K31/426 , A61K31/40 , A61K31/4439 , A61P3/00 , A61P3/10 , C07D231/10 , C07D277/20 , C07D403/02 , C07D413/02 , C07D401/02 , C07D263/02 , C07D207/04 , A61P3/04 , A61P1/00 , A61K31/421
CPC分类号： C07D277/06 , A61K9/0019 , A61K9/1623 , A61K9/2853 , A61K9/2866 , A61K9/4825 , A61K9/4858 , A61K9/4875 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
摘要翻译： 本发明涉及其中R 1，R 2和X如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：US20050096348A1
公开(公告)日：2005-05-05
申请号：US11010899
申请日：2004-12-13
申请人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Loeffler , Ramakanth Sarabu , Hans Wessel
发明人： Markus Boehringer , Daniel Hunziker , Holger Kuehne , Bernd Loeffler , Ramakanth Sarabu , Hans Wessel
IPC分类号： A61K20060101 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/506 , A61K31/5355 , A61P1/00 , A61P1/04 , A61P3/04 , A61P3/10 , C07D20060101 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07D41/02 , A61K31/426
CPC分类号： C07D277/06 , A61K9/0019 , A61K9/1623 , A61K9/2853 , A61K9/2866 , A61K9/4825 , A61K9/4858 , A61K9/4875 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
摘要翻译： 本发明涉及其中R 1，R 2和X如说明书和权利要求书中所定义的式（I）化合物及其药学上可接受的盐。 所述化合物可用于治疗和/或预防与DPP IV相关的疾病，例如糖尿病，特别是非胰岛素依赖性糖尿病和葡萄糖耐量异常。
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公开(公告)号：US08809384B2
公开(公告)日：2014-08-19
申请号：US13423303
申请日：2012-03-19
申请人： Daniel Hunziker , Werner Neidhart
发明人： Daniel Hunziker , Werner Neidhart
IPC分类号： A61K31/4015 , C07D209/54
CPC分类号： C07D403/06 , A61K31/403 , A61K31/4178 , A61K31/422 , A61K31/4439 , C07D413/06 , C07D417/06
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5 and A are as described herein, compositions including the compounds and methods of using the compounds.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5和A如本文所述，包括该化合物的组合物和使用该化合物的方法。
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9.发明授权Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds 有权六氢环戊吡咯啉酮，六氢吡咯并吡咯啉酮，八氢吡咯并吡喃酮和八氢吡啶酮化合物公开(公告)号：US08501768B2
公开(公告)日：2013-08-06
申请号：US13463863
申请日：2012-05-04
IPC分类号： C07D209/52
CPC分类号： C07D471/04 , C07D209/52 , C07D487/04
摘要： The invention provides novel compounds having the general formula (I) wherein R1, R2, A, E, G and n are as described herein, compositions including the compounds and methods of using the compounds. The compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used for the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R1，R2，A，E，G和n如本文所述，包括该化合物的组合物和使用该化合物的方法。 该化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病或非酒精性脂肪肝 脂肪性肝炎
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公开(公告)号：US08497288B2
公开(公告)日：2013-07-30
申请号：US13461835
申请日：2012-05-02
IPC分类号： A61K31/4188 , A61K31/4439 , C07D401/02
CPC分类号： C07D487/04
摘要： The invention provides novel compounds having the general formula (I), wherein R1, R2, R3 and A are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful as inhibitors of hormone sensitive lipase (HSL) and may be used in the treatment of diabetes, metabolic syndrome, dyslipidemia, atherosclerosis, obesity, cardiovascular diseases, myocardial dysfunction, inflammation, non-alcoholic fatty liver disease and non-alcoholic steatohepatitis.
摘要翻译： 本发明提供具有通式（I）的新化合物，其中R 1，R 2，R 3和A如本文所述，包括该化合物的组合物和使用该化合物的方法。 这些化合物可用作激素敏感性脂肪酶（HSL）的抑制剂，可用于治疗糖尿病，代谢综合征，血脂异常，动脉粥样硬化，肥胖症，心血管疾病，心肌功能障碍，炎症，非酒精性脂肪性肝病和非酒精性脂肪肝 脂肪性肝炎
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