公开(公告)号：US06703508B2

公开(公告)日：2004-03-09

申请号：US10012242

申请日：2001-12-04

申请人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michelle L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

发明人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michelle L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

IPC分类号： C07D21130

CPC分类号： C07D211/22 ,  C07D211/26

摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

摘要翻译： 本发明的一个方面涉及合成取代的哌啶的方法。 本发明的第二方面涉及合成取代的哌啶的立体选择性方法。 本发明的方法将用于合成可用于治疗许多疾病，病症和疾病的哺乳动物，包括但不限于成瘾和疼痛。 本发明的另一方面涉及使用本发明的方法合成取代的哌啶的组合文库。 本发明的另一方面涉及对映体取代的吡咯烷，哌啶和吖庚因。

公开(公告)号：US07005524B2

公开(公告)日：2006-02-28

申请号：US10789414

申请日：2004-02-27

申请人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michelle L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

发明人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michelle L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

IPC分类号： C07D211/26 ,  A61K31/445

CPC分类号： C07D211/22 ,  C07D211/26

摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

公开(公告)号：US07692019B2

公开(公告)日：2010-04-06

申请号：US11364506

申请日：2006-02-28

申请人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michele L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

发明人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Michele L. R. Heffernan ,  Michael Z. Hoemann ,  Donald W. Kessler ,  Liming Shao ,  Xinhe Wu ,  Roger L. Xie

IPC分类号： C07D223/04 ,  C07D211/60 ,  C07D207/46

CPC分类号： C07D211/22 ,  C07D211/26

摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.

摘要翻译： 本发明的一个方面涉及合成取代的哌啶的方法。 本发明的第二方面涉及合成取代的哌啶的立体选择性方法。 本发明的方法将用于合成可用于治疗许多疾病，病症和疾病的哺乳动物，包括但不限于成瘾和疼痛。 本发明的另一方面涉及使用本发明的方法合成取代的哌啶的组合文库。 本发明的另一方面涉及对映体取代的吡咯烷，哌啶和吖庚因。

公开(公告)号：US06645980B1

公开(公告)日：2003-11-11

申请号：US09717174

申请日：2000-11-20

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： A61K31445

CPC分类号： C07D265/30 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D211/26 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D409/06

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：US06635661B2

公开(公告)日：2003-10-21

申请号：US09798803

申请日：2001-03-02

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： A61K31445

CPC分类号： C07D221/04 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D205/06 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D265/30 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D491/10

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：US06703383B2

公开(公告)日：2004-03-09

申请号：US09951137

申请日：2001-09-12

申请人： Xinhe Wu ,  Brian M. Aquila ,  Liming Shao ,  Heike Radeke ,  Gregory D. Cuny ,  James R. Hauske ,  Roger L. Xie

发明人： Xinhe Wu ,  Brian M. Aquila ,  Liming Shao ,  Heike Radeke ,  Gregory D. Cuny ,  James R. Hauske ,  Roger L. Xie

IPC分类号： A61K3133

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/12 ,  C07D409/12

摘要： One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.

摘要翻译： 本发明的一个方面涉及包含磺酰胺部分的杂环化合物。 本发明的第二方面涉及包含磺酰胺部分的杂环化合物在至少部分地由一种或多种GPCR或配体门控离子通道的异常活性引起的疾病，病痛或疾病的用途。 本发明的另一方面涉及包含磺酰胺部分的杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在精神病的动物模型中。

公开(公告)号：US07129228B2

公开(公告)日：2006-10-31

申请号：US10754101

申请日：2004-01-07

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： A61P25/00 ,  A61K31/445 ,  A61K31/675 ,  C07F9/28 ,  C07D211/00

CPC分类号： C07D221/04 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D265/30 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D491/10

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：US06677332B1

公开(公告)日：2004-01-13

申请号：US09579398

申请日：2000-05-25

申请人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

发明人： Gregory D. Cuny ,  Liming Shao ,  James R. Hauske ,  Michele L. R. Heffernan ,  Brian M. Aquila ,  Xinhe Wu ,  Fengjiang Wang ,  Thomas D. Bannister

IPC分类号： C07D21126

CPC分类号： C07D221/04 ,  A61K31/397 ,  A61K31/438 ,  A61K31/4523 ,  A61K31/495 ,  A61K31/5375 ,  A61K31/551 ,  A61K31/553 ,  C07D205/04 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/60 ,  C07D211/70 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D243/08 ,  C07D265/30 ,  C07D267/10 ,  C07D333/38 ,  C07D401/06 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D409/12 ,  C07D491/10

摘要： One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.

公开(公告)号：US06872716B2

公开(公告)日：2005-03-29

申请号：US10766300

申请日：2004-01-28

申请人： Xinhe Wu ,  Brian M. Aquila ,  Liming Shao ,  Heike Radeke ,  Gregory D. Cuny ,  James R. Hauske ,  Roger L. Xie

发明人： Xinhe Wu ,  Brian M. Aquila ,  Liming Shao ,  Heike Radeke ,  Gregory D. Cuny ,  James R. Hauske ,  Roger L. Xie

IPC分类号： A61P25/00 ,  C07D211/28 ,  C07D401/04 ,  C07D401/12 ,  C07D409/12 ,  A61K31/44 ,  C07D211/00 ,  C07D401/00

CPC分类号： C07D401/04 ,  C07D211/28 ,  C07D401/12 ,  C07D409/12

摘要： One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.

摘要翻译： 本发明的一个方面涉及包含磺酰胺部分的杂环化合物。 本发明的第二方面涉及包含磺酰胺部分的杂环化合物在至少部分地由一种或多种GPCR或配体门控离子通道的异常活性引起的疾病，病痛或疾病的用途。 本发明的另一方面涉及包含磺酰胺部分的杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在精神病的动物模型中。

公开(公告)号：US07816375B2

公开(公告)日：2010-10-19

申请号：US12403311

申请日：2009-03-12

申请人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

发明人： Brian M. Aquila ,  Thomas D. Bannister ,  Gregory D. Cuny ,  James R. Hauske ,  Joanne M. Holland ,  Paul E. Persons ,  Heike Radeke ,  Fengjiang Wang ,  Liming Shao

IPC分类号： A61P25/00 ,  A61K31/445 ,  C07D211/00

CPC分类号： C40B40/04 ,  C07B2200/11 ,  C07C255/46 ,  C07C2601/04 ,  C07D205/02 ,  C07D207/06 ,  C07D207/08 ,  C07D207/09 ,  C07D211/12 ,  C07D211/16 ,  C07D211/18 ,  C07D211/20 ,  C07D211/26 ,  C07D211/32 ,  C07D211/40 ,  C07D211/42 ,  C07D211/60 ,  C07D233/04 ,  C07D233/10 ,  C07D265/30 ,  C07D267/10 ,  C07D303/08 ,  C07D401/06 ,  C07D401/12 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C40B30/04 ,  C40B50/14

摘要： One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

摘要翻译： 本发明的一个方面涉及杂环化合物。 本发明的第二方面涉及杂环化合物作为各种哺乳动物细胞受体（包括多巴胺，5-羟色胺或去甲肾上腺素转运蛋白）的配体的用途。 本发明的化合物可用于治疗多种疾病，疾病，其包括但不限于成瘾，焦虑，抑郁，性功能障碍，高血压，偏头痛，阿尔茨海默病，肥胖，呕吐，精神病， 精神分裂症，帕金森病，炎症性疼痛，神经性疼痛，Lesche-Nyhane病，Wilson氏病和Tourette综合征。 本发明的另一方面涉及杂环化合物的组合文库的合成，以及用于生物活性的那些文库的筛选，例如在基于多巴胺转运蛋白的测定中。