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公开(公告)号：US07825131B2
公开(公告)日：2010-11-02
申请号：US10572167
申请日：2004-09-17
IPC分类号： C07D401/02 , A61K31/47
CPC分类号： C07D215/227 , C07D215/38 , C07D215/54 , C07D401/06 , C07D413/06 , C07D413/14
摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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公开(公告)号：US07741322B2
公开(公告)日：2010-06-22
申请号：US10571858
申请日：2004-09-17
申请人： Christopher J. Dinsmore , Jeffrey M. Bergman , Charles J. McIntyre , Richard Isaacs , David A. Claremon
发明人： Christopher J. Dinsmore , Jeffrey M. Bergman , Charles J. McIntyre , Richard Isaacs , David A. Claremon
IPC分类号： A61K31/4725 , C07D401/12
CPC分类号： C07D401/04 , C07D217/24 , C07D401/06
摘要： The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
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公开(公告)号：US20090186871A1
公开(公告)日：2009-07-23
申请号：US12378473
申请日：2009-02-13
IPC分类号： A61K31/404 , C07D413/12 , A61K31/5377 , C07D403/12 , A61P35/00
CPC分类号： C07D487/10 , C07D209/42 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D491/04 , C07D491/10 , C07D513/04 , C07D513/08
摘要： The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
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公开(公告)号：US06562823B1
公开(公告)日：2003-05-13
申请号：US09719878
申请日：2001-06-28
申请人： Christopher J. Dinsmore , Jeffrey M. Bergman , Samuel L. Graham , Diem N. Nguyen , Gerald E. Stokker , Theresa M. Williams , C. Blair Zartman
发明人： Christopher J. Dinsmore , Jeffrey M. Bergman , Samuel L. Graham , Diem N. Nguyen , Gerald E. Stokker , Theresa M. Williams , C. Blair Zartman
IPC分类号： C07D26700
CPC分类号： C07D498/18
摘要： The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
摘要翻译： 本发明涉及抑制异戊烯基 - 蛋白质转移酶和致癌基因蛋白Ras的异戊烯基化的含模拟哌嗪的大环化合物。 本发明还涉及含有本发明化合物的化疗组合物和抑制异戊烯基 - 蛋白质转移酶和癌基因蛋白Ras的异戊烯化的方法。
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公开(公告)号：US5756528A
公开(公告)日：1998-05-26
申请号：US652055
申请日：1996-05-23
申请人： Neville J. Anthony , Jeffrey M. Bergman , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
发明人： Neville J. Anthony , Jeffrey M. Bergman , Chrisopher J. Dinsmore , Robert P. Gomez , Suzanne C. MacTough , Kelly M. Solinsky , Theresa M. Williams
IPC分类号： C07D233/54 , C07D233/61 , C07D401/14 , A61K31/415
CPC分类号： C07D233/64 , C07D401/14
摘要： The present invention comprises low molecular weight peptidyl compounds that inhibit the farnesyl-protein transferase. Furthermore, these compounds differ from the mono- or dipeptidyl analogs previously described as inhibitors of farnesyl-protein transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.
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公开(公告)号：US08399494B2
公开(公告)日：2013-03-19
申请号：US13126620
申请日：2009-10-26
CPC分类号： A61K31/437 , A61K31/4439 , C07D213/56 , C07D213/61 , C07D231/12 , C07D241/12 , C07D401/10 , C07D401/12 , C07D401/14
摘要： The present invention is directed to 2,5-disubstituted phenyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的2,5-二取代的苯基甲酰胺化合物，其可用于治疗或预防其中涉及食欲肽受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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公开(公告)号：US20110301140A1
公开(公告)日：2011-12-08
申请号：US13197800
申请日：2011-08-04
申请人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Swati P. Mercer , Thomas S. Reger , Anthony J. Roecker , Justin T. Steen
发明人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Swati P. Mercer , Thomas S. Reger , Anthony J. Roecker , Justin T. Steen
IPC分类号： A61K31/541 , C07D401/14 , A61K31/4439 , C07D401/04 , A61K31/497 , C07D413/14 , A61P3/04 , A61K31/498 , C07D417/04 , A61P25/20 , A61K31/444 , A61K31/5377
CPC分类号： C07D213/82 , A61K31/4427 , A61K31/4439 , A61K31/444 , C07D401/04 , C07D401/14
摘要： The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的吡啶羧酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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公开(公告)号：US20110195957A1
公开(公告)日：2011-08-11
申请号：US13089677
申请日：2011-04-19
申请人： Jeffrey M. Bergman , Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , Swati P. Mercer , Anthony J. Roecker
发明人： Jeffrey M. Bergman , Michael J. Breslin , Paul J. Coleman , Christopher D. Cox , Swati P. Mercer , Anthony J. Roecker
IPC分类号： A61K31/551 , C07D413/14 , C07D495/04 , C07D403/14 , C07D491/044 , C07D487/04 , A61P25/00 , A61P25/18 , A61P25/16 , A61P25/08 , A61P29/00 , A61P3/04
CPC分类号： C07D413/14 , C07D401/14 , C07D403/14 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D495/04
摘要： The present invention is directed to substituted diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲肽受体的拮抗剂的取代的二氮杂环庚烷化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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公开(公告)号：US20100256121A1
公开(公告)日：2010-10-07
申请号：US12739304
申请日：2008-10-27
IPC分类号： A61K31/551 , A61P25/20 , A61P3/04 , A61P3/10 , A61P25/24 , A61P25/16 , A61P25/02 , A61P25/18 , C07D403/12
CPC分类号： C07D403/14 , C07D403/04 , C07D413/14 , C07D417/14
摘要： The present invention is directed to diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的二氮杂环庚烷化合物，其可用于治疗神经性和精神疾病以及食欲素受体参与的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗其中涉及食欲素受体的疾病中的用途。
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公开(公告)号：US20100197652A1
公开(公告)日：2010-08-05
申请号：US12669909
申请日：2008-08-07
申请人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Swati P. Mercer , Thomas S. Reger , Anthony J. Roecker , Justin T. Steen
发明人： Jeffrey M. Bergman , Paul J. Coleman , Mark E. Fraley , Swati P. Mercer , Thomas S. Reger , Anthony J. Roecker , Justin T. Steen
IPC分类号： A61K31/465 , C07D401/04 , A61K31/4709 , C07D213/82 , C07D401/10 , C07D401/14 , A61K31/501 , A61K31/498 , C07D413/04 , A61K31/5377 , A61K31/4545 , C07D417/04 , A61K31/541 , A61P3/04 , A61P25/00
CPC分类号： C07D213/82 , A61K31/4427 , A61K31/4439 , A61K31/444 , C07D401/04 , C07D401/14
摘要： The present invention is directed to pyridyl carboxamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译： 本发明涉及作为食欲素受体的拮抗剂的吡啶羧酰胺化合物，其可用于治疗或预防涉及食欲素受体的神经和精神病症和疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及食欲肽受体的疾病中的用途。
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