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公开(公告)号：US07071212B2
公开(公告)日：2006-07-04
申请号：US10639030
申请日：2003-08-12
申请人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
发明人： Jean Ackermann , Leo Alig , Alexander Chucholowski , Katrin Groebke , Kurt Hilpert , Holger Kuehne , Ulrike Obst , Lutz Weber , Hans Peter Wessel
IPC分类号： A61K31/445 , C07D265/30
CPC分类号： C07D207/27 , C07C257/18 , C07C259/18 , C07C2601/08 , C07C2601/14 , C07D207/12 , C07D209/48 , C07D211/46 , C07D211/58 , C07D211/96 , C07D213/30 , C07D213/55 , C07D213/65 , C07D213/74 , C07D231/12 , C07D233/56 , C07D233/64 , C07D235/18 , C07D249/08 , C07D261/04 , C07D271/06 , C07D277/24 , C07D295/155 , C07D307/12 , C07D307/20 , C07D307/54 , C07D309/12 , C07D309/14 , C07D317/64 , C07D319/18 , C07D321/10 , C07D333/24 , C07D335/04 , C07D403/12
摘要： The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
摘要翻译： 本发明涉及下式的新型N-（4-甲脒基 - 苯基） - 甘氨酸衍生物：其中R 1，E，X 1至X 4 本说明书和权利要求书中所定义的，以及其水合物或溶剂合物及其生理上可用的盐。
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公开(公告)号：US07012077B2
公开(公告)日：2006-03-14
申请号：US10310559
申请日：2002-12-05
IPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61P3/00 , A61P3/06
CPC分类号： C07D213/74 , C07D213/85 , C07D237/20 , C07D237/22 , C07D239/42 , C07D401/04 , C07D409/04
摘要： The present invention relates to compounds of formula (I) wherein A1, A2, A3, A4, A5, A6, U, V, m, n and o are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the 2,3-oxidosqualene-lanosterol cyclase biosynthetic pathway such as hypercholesterolemia and hyperlipemia.
摘要翻译： 本发明涉及式（I）的化合物，其中A 1，A 2，A 3，A 4， 其中，A 5，A 6，U，V，m，n和o如说明书中所定义，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2,3-氧化山梨醇 - 羊毛甾醇环化酶生物合成途径相关的疾病，例如高胆固醇血症和高脂血症。
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公开(公告)号：US20050272774A1
公开(公告)日：2005-12-08
申请号：US11176901
申请日：2005-07-07
申请人： Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Georges Hirth , Hans-Peter Maerki , Olivier Morand
发明人： Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Georges Hirth , Hans-Peter Maerki , Olivier Morand
IPC分类号： C07D295/12 , A61K31/18 , A61K31/223 , A61K31/27 , A61K31/325 , A61K31/397 , A61K31/40 , A61K31/4164 , A61K31/445 , A61K31/4453 , A61K31/505 , A61K31/5375 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P31/10 , A61P33/00 , A61P35/00 , A61P43/00 , C07B61/00 , C07C269/04 , C07C269/06 , C07C271/46 , C07C271/48 , C07C271/52 , C07C291/04 , C07C303/40 , C07C311/17 , C07C311/18 , C07D203/12 , C07D205/04 , C07D207/08 , C07D211/46 , C07D233/52 , C07D233/60 , C07D239/42 , C07D295/084 , C07D295/088 , C07D295/10 , C07D295/135 , C07D521/00 , C07D211/26
CPC分类号： C07D207/08 , C07C271/52 , C07C311/17 , C07C311/18 , C07C2601/14 , C07D205/04 , C07D211/46 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/084 , C07D295/088 , C07D295/135
摘要： The present invention provides compounds of formula (I) wherein A1, A2, A3, A4, A5, A6, A7, A8 , A9, A10, U, V, W, m, n and p-are as indicated in the specification, and pharmaceutically acceptable salts 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 and hyperlipemia.
摘要翻译： 本发明提供式（I）的化合物，其中A 1，A 2，S 3，S 4， ，A 5，A 6，A 7，A 8，A 9， A，U，V，W，m，n和p-如本说明书中所示，及其药学上可接受的盐。 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和高脂血症相关的疾病。
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公开(公告)号：US20050267200A1
公开(公告)日：2005-12-01
申请号：US11178164
申请日：2005-07-08
IPC分类号： A61K31/381 , A61K31/397 , A61K31/428 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P3/00 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P31/10 , A61P33/00 , A61P35/00 , C07D275/04 , C07D275/06 , C07D333/54 , C07D409/12 , C07D417/12 , C07D521/00 , C07D333/72 , C07D409/02
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.
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公开(公告)号：US06965048B2
公开(公告)日：2005-11-15
申请号：US10883431
申请日：2004-07-01
IPC分类号： C07C271/54 , C07C271/56 , C07C311/20 , C07D211/22 , C07D211/46 , C07C271/44 , A61K31/27
CPC分类号： C07D211/46 , C07C271/54 , C07C271/56 , C07C311/20 , C07C2601/14 , C07D211/22
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, X, W, m and n are as defined hereinabove. 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, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， >，X，W，m和n如上所定义。 该化合物可用于治疗和/或预防与2,3-氧化山梨醇 - 羊毛甾醇环化酶相关的疾病，例如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，寄生虫感染，胆结石，肿瘤和/或过度增殖性疾病， 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：US06964974B2
公开(公告)日：2005-11-15
申请号：US09939872
申请日：2001-08-27
申请人： Jean Ackermann , Johannes Aebi , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller
发明人： Jean Ackermann , Johannes Aebi , Alexander Chucholowski , Henrietta Dehmlow , Olivier Morand , Sabine Wallbaum , Thomas Weller
IPC分类号： A61K31/445 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/55 , A61P1/16 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P31/10 , A61P33/00 , A61P35/00 , A61P43/00 , C07D211/18 , C07D211/22 , C07D211/26 , C07D211/44 , C07D211/46 , C07D211/96 , C07D401/12 , C07D405/12 , C07D417/12
CPC分类号： C07D211/46 , C07D211/22 , C07D211/26 , C07D211/96
摘要： The present invention relates to piperidine 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哌啶衍生物 ，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：US06951879B2
公开(公告)日：2005-10-04
申请号：US09999424
申请日：2001-10-31
IPC分类号： A61K31/381 , A61K31/397 , A61K31/428 , A61K31/454 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P3/00 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P13/12 , A61P31/10 , A61P33/00 , A61P35/00 , C07D275/04 , C07D275/06 , C07D333/54 , C07D409/12 , C07D417/12 , C07D521/00
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：US20050065210A1
公开(公告)日：2005-03-24
申请号：US10942154
申请日：2004-09-16
申请人： Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Georges Hirth , Hans-Peter Maerki , Olivier Morand , Narendra Panday
发明人： Jean Ackermann , Johannes Aebi , Henrietta Dehmlow , Georges Hirth , Hans-Peter Maerki , Olivier Morand , Narendra Panday
IPC分类号： A61P9/10 , C07C271/24 , C07C271/56 , C07C311/20 , C07D239/26 , C07D239/30 , C07D239/42 , C07D295/185 , C07D403/12 , A61K31/325 , A61K31/16 , A61K31/18
CPC分类号： C07D239/26 , C07C271/56 , C07C311/20 , C07C2601/14 , C07D239/30 , C07D295/185 , C07D403/12
摘要： The present invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, U, V, W, k and m are as defined in the description and claims, 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, parasit infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及式I化合物，其中R 1，R 2，R 3，R 4，R 5，U，V，W，k和m如说明书中所定义 并且要求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 - 羊毛甾醇环化酶相关的疾病，例如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，寄生虫感染，胆结石，肿瘤和/或过度增殖性疾病， 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：US20050009906A1
公开(公告)日：2005-01-13
申请号：US10883431
申请日：2004-07-01
IPC分类号： C07C271/54 , C07C271/56 , C07C311/20 , C07D211/22 , C07D211/46 , A61K31/325 , A61K31/215 , A61K31/265
CPC分类号： C07D211/46 , C07C271/54 , C07C271/56 , C07C311/20 , C07C2601/14 , C07D211/22
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, X, W, m and n are as defined hereinabove. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualane-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.
摘要翻译： 本发明涉及其中R 1，R 2，R 3，R 4，X，W，m和n如上文所定义的式（I）化合物。 该化合物可用于治疗和/或预防与2,3-二氧代山梨醇 - 羊毛甾醇环化酶相关的疾病，例如高胆固醇血症，高脂血症，动脉硬化，血管疾病，真菌病，寄生虫感染，胆结石，肿瘤和/或过度增殖性疾病， 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：US6140353A
公开(公告)日：2000-10-31
申请号：US204373
申请日：1998-12-02
申请人： Jean Ackermann , Katrin Grobke , Yu-Hua Ji , Sabine Wallbaum , Lutz Weber
发明人： Jean Ackermann , Katrin Grobke , Yu-Hua Ji , Sabine Wallbaum , Lutz Weber
IPC分类号： C07D295/08 , A61K31/00 , A61K31/155 , A61K31/16 , A61K31/395 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4045 , A61K31/415 , A61K31/4164 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/47 , A61K31/472 , A61P35/00 , A61P43/00 , C07C255/59 , C07C257/18 , C07C259/18 , C07C271/64 , C07C311/08 , C07C311/21 , C07C311/46 , C07D207/16 , C07D209/08 , C07D209/14 , C07D209/16 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/69 , C07D215/14 , C07D217/02 , C07D217/04 , C07D217/18 , C07D217/26 , C07D233/24 , C07D233/54 , C07D233/64 , C07D295/092 , C07D317/60 , C07C233/01 , A61K31/165 , C07D213/02
CPC分类号： C07D213/30 , C07C255/59 , C07C257/18 , C07C259/18 , C07C271/64 , C07C311/08 , C07C311/21 , C07C311/46 , C07D207/16 , C07D209/08 , C07D213/40 , C07D213/69 , C07D215/14 , C07D217/02 , C07D217/26 , C07D233/64 , C07D295/088 , C07D317/60 , C07C2101/02 , C07C2101/08 , Y02P20/55
摘要： N-(4-carbamimidophenylamino) phenylglycineamide derivative compounds having the formula: ##STR1## in which E, g.sup.1, g.sup.2, Q, R and X.sup.1 to X.sup.4 are each as defined in the description, and hydrates or solvates and physiologically acceptable salts thereof can be used as inhibitors of the formation of the coagulation factors Xa, IXa and thrombin induced by the factor VIIa and by the tissue factor. These compounds can be used as medicaments for the treatment and/or prevention of thromboses, apoplexy, cardiac infarction, inflammation and arteriosclerosis or as antitumor agents.
摘要翻译： 具有下式的N-（4-氨基甲酰亚氨基苯基氨基）苯基甘氨酰胺衍生物化合物：其中E，g1，g2，Q，R和X1至X4各自如说明书中所定义，其水合物或溶剂合物及其生理学上可接受的盐可用作 由因子VIIa诱导的凝血因子Xa，IXa和凝血酶的形成抑制剂以及组织因子。 这些化合物可以用作治疗和/或预防血栓形成，中风，心肌梗塞，炎症和动脉硬化或作为抗肿瘤剂的药物。
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