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51. 发明授权

US07732452B2 Thiophene derivatives which are HM74A agonists 失效
标题翻译：作为HM74A激动剂的噻吩衍生物
公开(公告)号：US07732452B2
公开(公告)日：2010-06-08
申请号：US11638220
申请日：2006-12-13
申请人： Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Robert Narquizian , Constantinos G. Panousis
发明人： Henrietta Dehmlow , Uwe Grether , Nicole A. Kratochwil , Robert Narquizian , Constantinos G. Panousis
IPC分类号： A61K31/497 , C07D409/02
CPC分类号： C07D409/12 , C07D333/38
摘要： The invention is concerned with novel substituted thiophene derivatives of formula (I) wherein R1 to R8, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型取代噻吩衍生物，其中R 1至R 8，X，m和n如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。这些化合物是HM74A激动剂，可用作药物。

52. 发明申请

US20100093818A1 BENZIMIDAZOLE DERIVATIVES 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US20100093818A1
公开(公告)日：2010-04-15
申请号：US12577765
申请日：2009-10-13
申请人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
发明人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
IPC分类号： A61K31/4184 , C07D235/12 , A61P9/00 , A61P9/10 , A61P35/00 , A61P17/06 , A61P25/00 , A61P25/28 , A61P25/16 , A61P3/10 , A61P3/06
CPC分类号： C07D235/18
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的苯并咪唑衍生物，其中R 1至R 6如在说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物可以用作药物。

53. 发明申请

US20100076026A1 3-AMINO-INDAZOLE OR 3-AMINO-4,5,6,7-TETRAHYDRO-INDAZOLE DERIVATIVES 失效
标题翻译： 3-氨基吲哚或3-氨基-4,5,6,7-四氢吲哚衍生物
公开(公告)号：US20100076026A1
公开(公告)日：2010-03-25
申请号：US12563189
申请日：2009-09-21
申请人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Markus Rudolph , Sven Taylor
发明人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Markus Rudolph , Sven Taylor
IPC分类号： A61K31/4439 , C07D231/56 , A61K31/416 , C07D401/12
CPC分类号： C07D231/56 , C07D401/12 , C07D407/12
摘要： This invention relates to novel indazole derivatives of formula I: wherein R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.
摘要翻译：本发明涉及式I的新型吲唑衍生物：其中R 1至R 7如说明书和权利要求书中所定义，以及其生理上可接受的盐。这些化合物是FXR调节剂，可用作药物。

54. 发明申请

US20100063101A1 NEW BENZIMIDAZOLE DERIVATIVES 有权
标题翻译：新的苯并咪唑衍生物
公开(公告)号：US20100063101A1
公开(公告)日：2010-03-11
申请号：US12554023
申请日：2009-09-04
申请人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
发明人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
IPC分类号： A61K31/4439 , C07D235/12 , C07D401/02 , A61K31/4184 , A61P1/00
CPC分类号： C07D235/18 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D495/04
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein A, n and R1 to R7 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及新的式（I）的苯并咪唑衍生物，其中A，n和R 1至R 7如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物可以用作药物。

55. 发明申请

US20090131482A1 METHYL-BENZIMIDAZOLE DERIVATIVES 有权
标题翻译：甲基苯并咪唑衍生物
公开(公告)号：US20090131482A1
公开(公告)日：2009-05-21
申请号：US12265049
申请日：2008-11-05
申请人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
发明人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
IPC分类号： A61K31/4439 , C07D235/04 , A61K31/4184 , A61P3/00 , A61P25/00 , A61P35/00 , A61P9/00 , C07D401/02
CPC分类号： C07D235/06 , C07D405/12 , C07D409/12
摘要： The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型取代的苯并咪唑衍生物，其中R 1至R 10如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。这些化合物可以用作药物。

56. 发明申请

US20080021027A1 Novel benzimidazole derivatives 失效
标题翻译：新型苯并咪唑衍生物
公开(公告)号：US20080021027A1
公开(公告)日：2008-01-24
申请号：US11821265
申请日：2007-06-22
申请人： Gregory Benson , Konrad Bleicher , Alexander Chucholowski , Henrietta Dehmlow , Uwe Grether , Bernd Kuhn , Rainer Martin , Eric Niesor , Narendra Panday , Hans Richter , Franz Schuler , Xavier Warot , Matthew Wright , Minmin Yang
发明人： Gregory Benson , Konrad Bleicher , Alexander Chucholowski , Henrietta Dehmlow , Uwe Grether , Bernd Kuhn , Rainer Martin , Eric Niesor , Narendra Panday , Hans Richter , Franz Schuler , Xavier Warot , Matthew Wright , Minmin Yang
IPC分类号： A61K31/4184 , A61K31/41 , A61K31/422 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/47 , A61K31/5377 , A61P1/16 , C07D211/12 , C07D215/20 , C07D235/26 , C07D257/04 , C07D261/12 , C07D285/06 , C07D401/04 , C07D413/10 , C07D413/14
CPC分类号： C07D235/18 , C07D235/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/10 , C07D413/04 , C07D417/06
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.
摘要翻译：本发明涉及式（I）的新的苯并咪唑衍生物，其中R 1至R 8如在说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物与法呢型-X受体（FXR）结合，可用于治疗由FXR激动剂如糖尿病和血脂异常调节的疾病。

57. 发明授权

US07115611B2 Phenyl derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：苯基衍生物，其制造和用作药剂
公开(公告)号：US07115611B2
公开(公告)日：2006-10-03
申请号：US10978155
申请日：2004-10-29
申请人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Blake Wright
发明人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Blake Wright
IPC分类号： A61K31/4965 , A61K31/44 , A61N43/54 , C07D239/00 , C07D241/04
CPC分类号： C07D213/30 , C07D213/32 , C07D213/38 , C07D213/56 , C07D213/82 , C07D237/08 , C07D239/26 , C07D239/28 , C07D241/12
摘要： This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
摘要翻译：本发明涉及下式的化合物，其中R 5，R 6和R 7中的一个是X 1和X 2 >，X 2，Y 1至Y 4，R 1至R 13中的至少1个 >和m和n在说明书中定义，以及所有对映异构体及其药学上可接受的盐和/或酯。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防由PPARδ和/或PPARα激动剂调节的疾病的用途。

58. 发明授权

US06995263B2 Indolyl and dihydroindolyl derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：吲哚基和二氢吲哚衍生物，其制备和用作药剂
公开(公告)号：US06995263B2
公开(公告)日：2006-02-07
申请号：US10978144
申请日：2004-10-29
申请人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Blake Wright
发明人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Blake Wright
IPC分类号： C07D401/04 , C07D401/14 , C07D403/02
CPC分类号： C04B35/632 , C07D401/12 , C07D403/12
摘要： This invention relates to compounds of the formula wherein one of R6, R7 and R8 is and X, Y1 to Y4, R1 to R14 and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
摘要翻译：本发明涉及下列化合物：化学式id =“CHEM-US-00001”num =“000”

59. 发明申请

US20050096337A1 Phenyl derivatives, their manufacture and use as pharmaceutical agents 失效
标题翻译：苯基衍生物，其制造和用作药剂
公开(公告)号：US20050096337A1
公开(公告)日：2005-05-05
申请号：US10978155
申请日：2004-10-29
申请人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
发明人： Jean Ackermann , Johannes Aebi , Alfred Binggeli , Uwe Grether , Georges Hirth , Bernd Kuhn , Hans-Peter Maerki , Markus Meyer , Peter Mohr , Matthew Wright
IPC分类号： C07D213/30 , C07D213/32 , C07D213/38 , C07D213/56 , C07D213/82 , C07D237/08 , C07D239/26 , C07D239/28 , C07D241/12 , A61K31/44 , A61K31/19 , A61K31/215 , A61K31/277
CPC分类号： C07D213/30 , C07D213/32 , C07D213/38 , C07D213/56 , C07D213/82 , C07D237/08 , C07D239/26 , C07D239/28 , C07D241/12
摘要： This invention relates to compounds of the formula wherein one of R5, R6 and R7 is and X1, X2, Y1 to Y4, R1 to R13 and m and n are defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPARδ and/or PPARα agonists.
摘要翻译：本发明涉及下式的化合物，其中R 5，R 6和R 7中的一个是X 1和X 2 >，X 2，Y 1至Y 4，R 1至R 13中的至少1个 >和m和n在说明书中定义，以及所有对映异构体及其药学上可接受的盐和/或酯。本发明还涉及含有这些化合物的药物组合物，其制备方法及其用于治疗和/或预防由PPARδ和/或PPARα激动剂调节的疾病的用途。

60. 发明授权

US06271345B1 Enzyme cleavable linker bound to solid phase for organic compound synthesis 失效
标题翻译：酶可切割连接子与固相结合，用于有机化合物合成
公开(公告)号：US06271345B1
公开(公告)日：2001-08-07
申请号：US09214100
申请日：1998-12-28
申请人： Herbert Waldmann , Bernd Sauerbrei , Uwe Grether
发明人： Herbert Waldmann , Bernd Sauerbrei , Uwe Grether
IPC分类号： C07K1700
CPC分类号： C40B80/00 , C07B61/00 , C07B2200/11 , C07C271/22 , C12P1/00 , Y10S530/816
摘要： An enzyme cleavable linker is prepared on which organic compounds are synthesized when the linker is bound to a solid phase. The linker contains a functional group on which a synthesized organic compound is bound when synthesis takes place, and a recognition site for a hydrolytic enzyme. Reacting the linker with the enzyme causes the linker to fragment at a site different from the recognition site to liberate the synthesized organic compound. The solid phase may be a crosslinked polyacrylamide containing an amino group for attaching the linker, and the linker is bound to the solid phase via a spacer. The spacer is attached to the solid phase by an ester, ether, amide or amine linkage, or a sulfide or phosphate linkage. In a specific reaction of forming a solid phase containing the linker, 2-acetoxy-5-hydroxymethylbenzoic acid is attached to an amino group-containing polymer via a spacer followed by conversion to a chloroformic ester.
摘要翻译：制备可切割接头的酶切割接头，当接头与固相结合时，合成有机化合物。接头含有合成有机化合物结合的官能团，以及水解酶的识别位点。用酶使接头反应导致接头在不同于识别位点的位点断裂，以释放合成的有机化合物。固相可以是含有用于连接接头的氨基的交联聚丙烯酰胺，并且接头通过间隔物与固相结合。间隔物通过酯，醚，酰胺或胺键或硫化物或磷酸酯键与固相相连。在形成含有连接体的固相的具体反应中，将2-乙酰氧基-5-羟甲基苯甲酸经由间隔物连接到含氨基的聚合物上，然后转化为氯甲酸酯。

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