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公开(公告)号：US07449483B2
公开(公告)日：2008-11-11
申请号：US11634573
申请日：2006-12-06
IPC分类号： A61K31/445 , A61K31/38 , A61K31/40 , C07D409/06 , C07D333/58 , C07D333/64 , C07D411/06 , C07D205/02 , C07D205/10
CPC分类号： C07D417/12 , C07D231/12 , C07D233/56 , C07D249/08 , C07D275/04 , C07D275/06 , C07D333/54 , C07D409/12
摘要： The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及异离子OSC抑制剂。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，霉菌病，胆结石，肿瘤和/或过度增殖性疾病相关的疾病，以及治疗和 /或预防糖耐量异常和糖尿病。
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公开(公告)号：US07335687B2
公开(公告)日：2008-02-26
申请号：US11014374
申请日：2004-12-15
申请人： Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
发明人： Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
IPC分类号： A61K31/14 , C07C205/00
CPC分类号： C07D295/088 , C07C233/23 , C07C233/74 , C07C235/54 , C07C235/84 , C07C255/57 , C07C271/52 , C07C271/56 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C291/04 , C07C307/08 , C07C307/10 , C07C311/07 , C07C311/13 , C07C311/20 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/22 , C07C2601/02 , C07C2601/14 , C07D295/135
摘要： The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，胆结石，肿瘤和/或过度增殖性疾病相关的疾病的氨基环己醇衍生物 ，以及治疗和/或预防糖耐量异常和糖尿病。
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公开(公告)号：US07265149B2
公开(公告)日：2007-09-04
申请号：US11074474
申请日：2005-03-08
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： A61K31/4155 , C07D231/10
CPC分类号： C07D403/12
摘要： This invention relates to compounds of the formula I: wherein one of R6, R7 and R8 is and R1 to R15 and n are as defined in the description, and 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 PPAR δ and/or PPARα agonists.
摘要翻译： 本发明涉及式I化合物：其中R 6，R 7和R 8中的一个是R 1和R 2， R 15和R 15如在说明书中所定义，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。
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54.发明授权Thiazolyl-indole derivatives, their manufacture and use as pharmaceutical agents 失效噻唑基 - 吲哚衍生物，其制造和用作药剂公开(公告)号：US07235572B2
公开(公告)日：2007-06-26
申请号：US10878473
申请日：2004-06-28
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： A61K31/427 , C07D417/12
CPC分类号： C07D417/12
摘要： This invention relates to compounds of the formula wherein one of R6, R7 or R8 is and all enantiomers and pharmaceutically acceptable salts and/or esters thereof as well as 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 6，R 7或R 8中的一个是和所有对映异构体和药学上可接受的盐和/ 或其酯，以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。
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公开(公告)号：US20050203160A1
公开(公告)日：2005-09-15
申请号：US11074474
申请日：2005-03-08
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： C07D403/12 , C07D43/02 , A61K31/416
CPC分类号： C07D403/12
摘要： This invention relates to compounds of the formula I: wherein one of R6, R7 and R8 is and R1 to R15 and n are as defined in the description, and 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 PPAR δ and/or PPARα agonists.
摘要翻译： 本发明涉及式I化合物：其中R 6，R 7和R 8中的一个是R 1和R 2， R 15和R 15如在说明书中所定义，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。
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公开(公告)号：US20050176766A1
公开(公告)日：2005-08-11
申请号：US11014374
申请日：2004-12-15
申请人： Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
发明人： Jean Ackermann , Johannes Aebi , Denise Blum , Alexander Chucholowski , Henrietta Dehmlow , Hans-Peter Maerki , Olivier Morand , Rene Trussardi , Elisabeth von der Mark , Sabine Wallbaum , Thomas Weller
IPC分类号： C07D295/08 , A61K31/135 , A61K31/16 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/18 , A61K31/223 , A61K31/255 , A61K31/27 , A61K31/277 , A61K31/341 , A61K31/351 , A61K31/36 , A61K31/381 , A61K31/397 , A61K31/40 , A61K31/404 , A61K31/4164 , A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/5375 , A61K31/54 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/10 , A61P31/10 , A61P33/00 , A61P35/00 , C07C233/23 , C07C233/74 , C07C235/54 , C07C235/84 , C07C255/57 , C07C269/04 , C07C271/24 , C07C271/52 , C07C271/56 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C291/04 , C07C303/38 , C07C307/08 , C07C307/10 , C07C311/07 , C07C311/13 , C07C311/20 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/22 , C07D205/04 , C07D207/12 , C07D209/42 , C07D211/14 , C07D211/22 , C07D211/44 , C07D211/70 , C07D213/81 , C07D215/36 , C07D233/84 , C07D261/10 , C07D295/092 , C07D295/135 , C07D295/14 , C07D307/38 , C07D309/12 , C07D317/58 , C07D333/24 , C07D333/34 , C07D333/40 , C07D211/26
CPC分类号： C07D295/088 , C07C233/23 , C07C233/74 , C07C235/54 , C07C235/84 , C07C255/57 , C07C271/52 , C07C271/56 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/38 , C07C275/40 , C07C291/04 , C07C307/08 , C07C307/10 , C07C311/07 , C07C311/13 , C07C311/20 , C07C335/14 , C07C335/16 , C07C335/18 , C07C335/22 , C07C2601/02 , C07C2601/14 , C07D295/135
摘要： The present invention relates to aminocyclohexanol derivatives useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，胆结石，肿瘤和/或过度增殖性疾病相关的疾病的氨基环己醇衍生物 ，以及治疗和/或预防糖耐量异常和糖尿病。
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57.发明申请公开(公告)号：US20050096336A1
公开(公告)日：2005-05-05
申请号：US10977651
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 , C07D213/38 , C07D239/26 , A61K31/44 , A61K31/192 , A61K31/277 , A61K31/343 , A61K31/381
CPC分类号： C07D213/30 , C07D213/38 , C07D239/26
摘要： There are presented compounds of the formula wherein R6 and R7 is R4 and R5 or R5 and R6 together with the carbon atoms to which they are attached, form a ring as defined in the description and X1, X2, Y1 to Y4, R1 to R13 and n are as specified 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： 提出下式的化合物其中R 6和R 7是R 4和R 5或R 5， SUP> 5和R 6以及它们所连接的碳原子一起形成如说明书中所定义的环，X 2 ，Y 1至Y 4，R 1至R 13和n分别为 在本说明书中指定，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。
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公开(公告)号：US20050020624A1
公开(公告)日：2005-01-27
申请号：US10648451
申请日：2003-08-26
申请人： Johannes Aebi , Jean Ackermann , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller , Narendra Panday
发明人： Johannes Aebi , Jean Ackermann , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller , Narendra Panday
IPC分类号： A61K31/404 , A61K31/4045 , A61K31/47 , A61K31/4709 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/14 , A61P17/00 , A61P31/10 , A61P35/00 , A61P43/00 , C07D209/08 , C07D215/20 , C07D215/58 , C07D409/06 , C07D209/42 , C07D215/38
CPC分类号： C07D215/20 , C07D209/08
摘要： The present invention relates to novel dihydroindole and tetrahydroquinoline derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及新的二氢吲哚和四氢喹啉衍生物及其药学上可接受的盐和/或其药学上可接受的酯。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，胆结石，肿瘤和/或过度增殖性疾病相关的疾病，以及治疗和 /或预防糖耐量异常和糖尿病。
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公开(公告)号：US5677448A
公开(公告)日：1997-10-14
申请号：US689743
申请日：1996-08-13
申请人： Jean Ackermann , David Banner , Klaus Gubernator , Kurt Hilpert , Gerard Schmid
发明人： Jean Ackermann , David Banner , Klaus Gubernator , Kurt Hilpert , Gerard Schmid
IPC分类号： A61K31/445 , A61K20060101 , A61K31/155 , A61K31/18 , A61K31/33 , A61K31/435 , A61K31/4427 , A61K31/452 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/63 , A61K31/675 , A61K38/00 , A61P7/02 , C07C231/00 , C07C237/16 , C07C277/00 , C07C279/16 , C07C279/18 , C07C279/20 , C07C311/00 , C07C311/19 , C07D20060101 , C07D211/18 , C07D211/26 , C07D211/28 , C07D211/36 , C07D211/56 , C07D265/06 , C07D265/28 , C07D265/30 , C07D295/00 , C07D401/12 , C07D401/14 , C07D413/12 , C07F9/59 , C07K5/06 , C07K5/068 , C07K5/072 , C07K5/078 , C07D211/14
CPC分类号： C07D265/30 , C07D211/26 , C07D401/12 , C07D413/10 , C07D413/12 , C07K5/06026 , C07K5/06086 , C07K5/06104 , C07K5/06113 , C07K5/06139 , A61K38/00
摘要： Sulfonamidocarboxamides of the formula ##STR1## wherein A, M, Q, X and Y have the significance given in the description, as well as hydrates, solvates and salts thereof, which inhibit thrombin-induced blood platelet aggregation and clotting of fibrinogen in plasma, as described. The compounds of formula I can be prepared by amidination of a cyclic amino group standing for grouping X or by C(O)N(Q) amide formation.
摘要翻译： 其中A，M，Q，X和Y具有在说明书中给出的含义的磺酰胺酰胺，其水合物，溶剂化物和盐，其抑制血浆中凝血酶诱导的血小板聚集和纤维蛋白原凝结 ，如上所述。 式I的化合物可以通过用于分组X或通过C（O）N（Q）酰胺形成的环状氨基的酰胺化来制备。
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公开(公告)号：US5583133A
公开(公告)日：1996-12-10
申请号：US511428
申请日：1995-08-04
申请人： Jean Ackermann , David Banner , Klaus Gubernator , Paul Hadvary , Kurt Hilpert , Klaus M uller , Ludvik Labler , G erard Schmid , Thomas B. Tschopp , Hans P. Wessel , Beat Wirz
发明人： Jean Ackermann , David Banner , Klaus Gubernator , Paul Hadvary , Kurt Hilpert , Klaus M uller , Ludvik Labler , G erard Schmid , Thomas B. Tschopp , Hans P. Wessel , Beat Wirz
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61K31/535 , A61K31/5375 , A61K31/55 , A61P7/02 , A61P35/00 , C07D20060101 , C07D211/20 , C07D211/22 , C07D211/26 , C07D211/60 , C07D265/30 , C07D265/32 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/12
CPC分类号： C07D265/30 , C07D211/22 , C07D211/26 , C07D211/60 , C07D265/32 , C07D401/12 , C07D401/14 , C07D409/12 , C07D409/14 , C07D413/10 , C07D413/12 , Y10S514/822
摘要： Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
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