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1.发明申请TRIAZOLE AND IMIDAZOLE DERIVATIVES FOR USE AS TGR5 AGONISTS IN THE TREATMENT OF DIABETES AND OBESITY 有权用作TGR5治疗糖尿病和肥胖的激素的三唑和咪唑衍生物公开(公告)号：US20120040985A1
公开(公告)日：2012-02-16
申请号：US13148811
申请日：2010-02-12
申请人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt , Tie-Lin Wang , Richard Martin , Xiao-Hui Gu
发明人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt , Tie-Lin Wang , Richard Martin , Xiao-Hui Gu
IPC分类号： A61K31/5377 , A61K31/498 , A61K31/473 , A61K31/423 , A61K31/4196 , C07D233/84 , C07D413/06 , C07D403/06 , C07D403/12 , C07D249/12 , A61K31/4164 , C07D405/14 , A61P3/00 , A61P3/04 , A61P9/10 , A61P3/10 , A61P3/06 , C12N5/02
CPC分类号： C07D233/84 , C07D233/64 , C07D233/90 , C07D249/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/14
摘要： The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
摘要翻译： 本发明包括结构式I的TGR5激动剂，其中X，R 1，R 2和R 5在本文中定义，以及它们的N-氧化物及其药学上可接受的盐。 本发明还包括包含化合物，N-氧化物和/或其药学上可接受的盐的组合物。 本发明还包括使用化合物和组合物来治疗其中TGR5是介质或涉及的疾病。 本发明还包括在药物中和用于制备药物中的用途，特别是用于治疗其中TGR5是介质或涉及的疾病。
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2.发明授权Triazole and imidazole derivatives for use as TGR5 agonists in the treatment of diabetes and obesity 有权用作治疗糖尿病和肥胖症的TGR5激动剂的三唑和咪唑衍生物公开(公告)号：US08785488B2
公开(公告)日：2014-07-22
申请号：US13148811
申请日：2010-02-12
申请人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt , Tie-Lin Wang , Richard Martin , Xiao-Hui Gu
发明人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt , Tie-Lin Wang , Richard Martin , Xiao-Hui Gu
IPC分类号： A61K31/4174 , A61K31/4178 , C07D233/56 , C07D233/64
CPC分类号： C07D233/84 , C07D233/64 , C07D233/90 , C07D249/12 , C07D401/04 , C07D401/12 , C07D403/06 , C07D403/14
摘要： The present invention comprises TGR5 agonists of structural formula I, wherein X, R1, R2, and R5 are defined herein, as well as N-oxides of them and pharmaceutically acceptable salts thereof. The invention further comprises composition comprising the compounds, N-oxides, and/or pharmaceutically acceptable salts thereof. The invention also comprises use of the compounds and compositions for treating diseases in which TGR5 is a mediator or is implicated. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases in which TGR5 is a mediator or is implicated.
摘要翻译： 本发明包括结构式I的TGR5激动剂，其中X，R 1，R 2和R 5在本文中定义，以及它们的N-氧化物及其药学上可接受的盐。 本发明还包括包含化合物，N-氧化物和/或其药学上可接受的盐的组合物。 本发明还包括使用化合物和组合物来治疗其中TGR5是介质或涉及的疾病。 本发明还包括在药物中和用于制备药物中的用途，特别是用于治疗其中TGR5是介质或涉及的疾病。
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公开(公告)号：US08846739B2
公开(公告)日：2014-09-30
申请号：US13515132
申请日：2010-08-11
申请人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt
发明人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt
IPC分类号： C07D249/10 , C07D249/08 , C07D233/54 , C07D401/12 , A61K31/454 , A61K31/496 , A61K31/4995 , C07D295/15 , C07D249/12 , A61K31/4164 , A61K31/4178 , A61K31/5377 , A61K31/4196 , C07D403/12 , C07D233/64 , C07D233/84 , A61K31/4439 , C07D487/08
CPC分类号： C07D487/08 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/5377 , C07D233/64 , C07D233/84 , C07D249/12 , C07D295/15 , C07D401/12 , C07D403/12
摘要： TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
摘要翻译： 结构式VIII（Q）的TGR5激动剂，其中X，R 1，R 2和R 5在本说明书中定义，其药学上可接受的盐，其组合物，以及化合物和组合物用于治疗疾病的用途。 本发明还包括在化合物中和用于制备药物中的用途，特别是用于治疗疾病。
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公开(公告)号：US20130303505A1
公开(公告)日：2013-11-14
申请号：US13515132
申请日：2010-08-11
申请人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt
发明人： Venkataiah Bollu , Brant Clayton Boren , Jackaline Dalgard Julien , Brenton T. Flatt , Nadia Haq , Sarah Hudson , Raju Mohan , Michael Morrissey , Benjamin Pratt
IPC分类号： C07D487/08 , A61K31/4995 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/4196 , A61K31/4178 , A61K31/4164 , C07D295/15 , C07D401/12 , C07D249/12 , C07D403/12 , C07D233/84 , C07D233/64 , A61K31/5377
CPC分类号： C07D487/08 , A61K31/4164 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/4995 , A61K31/5377 , C07D233/64 , C07D233/84 , C07D249/12 , C07D295/15 , C07D401/12 , C07D403/12
摘要： TGR5 agonists of structural formula VIII(Q), wherein X, R1, R2, and R5 are defined in the specification, pharmaceutically acceptable salts thereof, compositions thereof, and use of the compounds and compositions for treating diseases. The invention also comprises use of the compounds in and for the manufacture of medicaments, particularly for treating diseases.
摘要翻译： 结构式VIII（Q）的TGR5激动剂，其中X，R 1，R 2和R 5在本说明书中定义，其药学上可接受的盐，其组合物，以及化合物和组合物用于治疗疾病的用途。 本发明还包括在化合物中和用于制备药物中的用途，特别是用于治疗疾病。
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公开(公告)号：US20110301183A1
公开(公告)日：2011-12-08
申请号：US13213894
申请日：2011-08-19
IPC分类号： A61K31/52 , C07D473/40 , C07D417/06 , C07D473/38 , A61K31/428 , A61P35/00 , C07D493/04 , C07D473/30
CPC分类号： C07D493/04 , C07D405/06 , C07D417/06 , C07D519/00
摘要： A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
摘要翻译： 作为包含合成埃坡霉素的药物组合物，公开了一种高活性的合成埃坡霉素化合物，其活性超过了埃博霉素EpoA或EpoB的活性，当被测定为对癌细胞系的细胞毒性剂时。
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公开(公告)号：US20130012894A1
公开(公告)日：2013-01-10
申请号：US13618700
申请日：2012-09-14
申请人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Coullhard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
发明人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Coullhard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
IPC分类号： A61M1/00
CPC分类号： A61M1/0011 , A61M1/0027 , A61M1/0052 , A61M1/0066 , A61M1/0072 , A61M1/0088
摘要： A reduced pressure apparatus includes a first casing portion and a second casing portion slidably coupled to the first casing portion such that the first casing portion is compressible into a plurality of positions relative to the second casing portion. The plurality of positions includes a fully compressed position and a fully uncompressed position. An indicator is disposed on at least one of the first casing portion and the second casing portion, the indicator being exposed when the first casing portion is in the fully uncompressed position.
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公开(公告)号：US20080293747A1
公开(公告)日：2008-11-27
申请号：US12092038
申请日：2006-11-09
IPC分类号： A61K31/52 , C07D417/02 , C07D405/02 , C07D257/04 , A61K31/41 , A61K31/4164 , A61K31/415 , A61K31/4196 , A61K31/426 , C07D277/02 , C07D473/00
CPC分类号： C07D493/04 , C07D405/06 , C07D417/06 , C07D519/00
摘要： A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
摘要翻译： 作为包含合成埃坡霉素的药物组合物，公开了一种高活性的合成埃坡霉素化合物，其活性超过了埃博霉素EpoA或EpoB的活性，当被测定为对癌细胞系的细胞毒性剂时。
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公开(公告)号：US08287507B2
公开(公告)日：2012-10-16
申请号：US12434579
申请日：2009-05-01
申请人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Couthard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
发明人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Couthard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
CPC分类号： A61M1/0011 , A61M1/0027 , A61M1/0052 , A61M1/0066 , A61M1/0072 , A61M1/0088
摘要： A reduced pressure apparatus includes a first casing portion and a second casing portion slidably coupled to the first casing portion such that the first casing portion is compressible into a plurality of positions relative to the second casing portion. The plurality of positions includes a fully compressed position and a fully uncompressed position. An indicator is disposed on at least one of the first casing portion and the second casing portion, the indicator being exposed when the first casing portion is in the fully uncompressed position.
摘要翻译： 减压装置包括第一壳体部分和可滑动地联接到第一壳体部分的第二壳体部分，使得第一壳体部分可压缩成相对于第二壳体部分的多个位置。 多个位置包括完全压缩位置和完全未压缩的位置。 指示器设置在第一壳体部分和第二壳体部分中的至少一个上，当第一壳体部分处于完全未压缩位置时，指示器被暴露。
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公开(公告)号：USD618337S1
公开(公告)日：2010-06-22
申请号：US29317590
申请日：2008-05-02
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公开(公告)号：US20090254066A1
公开(公告)日：2009-10-08
申请号：US12434579
申请日：2009-05-01
申请人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Couthard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
发明人： Keith Patrick Heaton , Ian James Hardman , Richard Daniel John Couthard , Timothy Mark Robinson , Christopher Brian Locke , Aidan Marcus Tout , Benjamin Pratt
IPC分类号： A61M27/00
CPC分类号： A61M1/0011 , A61M1/0027 , A61M1/0052 , A61M1/0066 , A61M1/0072 , A61M1/0088
摘要： A reduced pressure apparatus includes a first casing portion and a second casing portion slidably coupled to the first casing portion such that the first casing portion is compressible into a plurality of positions relative to the second casing portion. The plurality of positions includes a fully compressed position and a fully uncompressed position. An indicator is disposed on at least one of the first casing portion and the second casing portion, the indicator being exposed when the first casing portion is in the fully uncompressed position.
摘要翻译： 减压装置包括第一壳体部分和可滑动地联接到第一壳体部分的第二壳体部分，使得第一壳体部分可压缩成相对于第二壳体部分的多个位置。 多个位置包括完全压缩位置和完全未压缩的位置。 指示器设置在第一壳体部分和第二壳体部分中的至少一个上，当第一壳体部分处于完全未压缩位置时，指示器被暴露。
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