公开(公告)号：US20050256117A1

公开(公告)日：2005-11-17

申请号：US10511636

申请日：2003-06-11

申请人： Meng Hsin Chen ,  Luping Liu ,  Peter Meinke ,  Ravi Natarajan ,  William Parsons ,  Dong-Ming Shen ,  Min Shu ,  John Stelmach ,  Harold Wood ,  Fengqi Zhang ,  David Wisnoski ,  James Doherty

发明人： Meng Hsin Chen ,  Luping Liu ,  Peter Meinke ,  Ravi Natarajan ,  William Parsons ,  Dong-Ming Shen ,  Min Shu ,  John Stelmach ,  Harold Wood ,  Fengqi Zhang ,  David Wisnoski ,  James Doherty

IPC分类号： A61K9/08 ,  A61K9/10 ,  A61K31/404 ,  A61K31/41 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/7056 ,  A61K45/00 ,  A61K47/36 ,  A61P3/10 ,  A61P9/06 ,  A61P25/24 ,  A61P25/28 ,  A61P27/02 ,  A61P27/06 ,  A61P27/12 ,  A61P43/00 ,  C07D209/08 ,  C07D209/10 ,  C07D209/12 ,  C07D209/18 ,  C07D401/06 ,  C07D403/10 ,  C07D409/12 ,  C07D413/02 ,  C07D417/02 ,  C07D417/12 ,  C07D417/14 ,  C07H15/26 ,  C07D43/02

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/18 ,  C07D403/10 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07H15/26

摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

公开(公告)号：US20060116366A1

公开(公告)日：2006-06-01

申请号：US10537187

申请日：2003-11-26

申请人： Emma Parmee ,  Fengqi Zhang ,  Dong-Ming Shen ,  John Stelmach

发明人： Emma Parmee ,  Fengqi Zhang ,  Dong-Ming Shen ,  John Stelmach

IPC分类号： A61K31/551 ,  A61K31/519

CPC分类号： C07D403/12 ,  C07D235/02 ,  C07D239/70 ,  C07D471/10

摘要： The present invention relates to spirocyclic ureas, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.

摘要翻译： 本发明涉及螺环脲，含有这些化合物的组合物和治疗方法该化合物是胰高血糖素受体拮抗剂，因此可用于治疗，预防或延缓2型糖尿病的发作。

公开(公告)号：US20090062280A1

公开(公告)日：2009-03-05

申请号：US12225026

申请日：2007-03-09

申请人： James B. Doherty ,  Min Shu ,  Dong-Ming Shen ,  Fengqi Zhang

发明人： James B. Doherty ,  Min Shu ,  Dong-Ming Shen ,  Fengqi Zhang

IPC分类号： A61K31/5377 ,  C07D215/227 ,  C07D413/12 ,  A61K31/498 ,  C07D471/04 ,  A61K31/4375 ,  C07D241/44 ,  A61K31/4704

CPC分类号： C07D215/227 ,  C07D215/20 ,  C07D241/44 ,  C07D401/06 ,  C07D419/12 ,  C07D471/04

摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂用于治疗青光眼和导致患者眼睛眼内压升高的其它病症。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。

公开(公告)号：US20090281154A1

公开(公告)日：2009-11-12

申请号：US12308164

申请日：2007-06-07

申请人： James B. Doherty ,  Swaminathan R. Natarajan ,  Dong-Ming Shen ,  Fengqi Zhang

发明人： James B. Doherty ,  Swaminathan R. Natarajan ,  Dong-Ming Shen ,  Fengqi Zhang

IPC分类号： A61K31/426 ,  C07C233/11 ,  A61K31/165 ,  C07D277/38 ,  A61P27/06 ,  A61P27/02

CPC分类号： C07C235/78 ,  C07C45/54 ,  C07C2601/02 ,  C07C2601/14 ,  C07C49/84

摘要： This invention relates to the use of potent potassium channel blockers or a formulation thereof in the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.

摘要翻译： 本发明涉及有效的钾通道阻滞剂或其制剂在治疗青光眼和导致患者眼睛中眼内压升高的其它病症中的用途。 本发明还涉及这些化合物对哺乳动物物种尤其是人的眼睛的神经保护作用的用途。

公开(公告)号：US20110172256A1

公开(公告)日：2011-07-14

申请号：US13063820

申请日：2009-09-10

申请人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

发明人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

IPC分类号： A61K31/517 ,  C07D215/14 ,  A61K31/47 ,  A61P3/10 ,  C07D215/227 ,  C07D471/04 ,  A61K31/4375 ,  C07D239/74

CPC分类号： C07D215/18 ,  C07D215/227 ,  C07D217/22 ,  C07D217/24 ,  C07D239/70 ,  C07D403/04 ,  C07D413/04

摘要： Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

公开(公告)号：US10329289B2

公开(公告)日：2019-06-25

申请号：US15386009

申请日：2016-12-21

申请人： Jianming Bao ,  Xiaolei Gao ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Debra L. Ondeyka ,  Andrew W. Stamford ,  Fengqi Zhang

发明人： Jianming Bao ,  Xiaolei Gao ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Debra L. Ondeyka ,  Andrew W. Stamford ,  Fengqi Zhang

IPC分类号： C07D471/04 ,  C07F9/22 ,  C07D519/00 ,  C07D491/048 ,  C07D471/08 ,  C07D491/052 ,  A61K31/437 ,  A61P25/00

摘要： The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US06642237B1

公开(公告)日：2003-11-04

申请号：US09718223

申请日：2000-11-21

申请人： James R. Tata ,  Kevin T. Chapman ,  Joseph Leslie Duffy ,  Nancy J. Kevin ,  Yuan Cheng ,  Thomas A. Rano ,  Fengqi Zhang ,  Tracy Huening ,  Brian Anthony Kirk ,  Zhijian Lu ,  Subharekha Raghavan ,  Fred J. Fleitz ,  Daniel E. Petrillo ,  Joseph D. Armstrong, III ,  Richard J. Varsolona ,  David Askin ,  R. Scott Hoerrner ,  Robert Purick

发明人： James R. Tata ,  Kevin T. Chapman ,  Joseph Leslie Duffy ,  Nancy J. Kevin ,  Yuan Cheng ,  Thomas A. Rano ,  Fengqi Zhang ,  Tracy Huening ,  Brian Anthony Kirk ,  Zhijian Lu ,  Subharekha Raghavan ,  Fred J. Fleitz ,  Daniel E. Petrillo ,  Joseph D. Armstrong, III ,  Richard J. Varsolona ,  David Askin ,  R. Scott Hoerrner ,  Robert Purick

IPC分类号： C07D491048

CPC分类号： C07D401/06 ,  A61K31/00 ,  A61K45/06 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D491/04 ,  C07D495/04 ,  A61K2300/00

摘要： &ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

摘要翻译： γ-羟基-2-（氟烷基氨基羰基）-1-哌嗪戊酰胺化合物是HIV蛋白酶和HIV复制抑制剂的抑制剂。 这些化合物可用于预防或治疗HV的感染和治疗AIDS，无论是化合物，药学上可接受的盐，药物组合物成分，无论是否与其他抗病毒剂，免疫调节剂，抗生素或疫苗结合使用。 还描述了治疗艾滋病的方法和预防或治疗HIV感染的方法。 这些化合物对HIV病毒突变体有效，其对目前用于治疗AIDS和HIV感染的HIV蛋白酶抑制剂具有抗性。

公开(公告)号：US11149036B2

公开(公告)日：2021-10-19

申请号：US16621959

申请日：2018-06-22

申请人： John J. Acton, III ,  Merck Sharp & Dohme Corp. ,  MSD R&D (China) Co., Ltd. ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

发明人： John J. Acton, III ,  Jianming Bao ,  Qiaolin Deng ,  Melissa Egbertson ,  Ronald Ferguson, II ,  Xiaolei Gao ,  Scott Timothy Harrison ,  Sandra L. Knowles ,  Chunsing Li ,  Michael Man-Chu Lo ,  Robert D. Mazzola, Jr. ,  Zhaoyang Meng ,  Meng Na ,  Michael T. Rudd ,  Oleg Selyutin ,  David M. Tellers ,  Ling Tong ,  Fengqi Zhang

IPC分类号： C07D471/04 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D491/048 ,  C07D498/04

摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.

公开(公告)号：US09126976B2

公开(公告)日：2015-09-08

申请号：US14239452

申请日：2012-08-13

申请人： Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

发明人： Rajan Anand ,  Vincent J. Colandrea ,  Maud Reiter ,  Petr Vachal ,  Aaron Zwicker ,  Jonathan E. Wilson ,  Fengqi Zhang ,  Kake Zhao

IPC分类号： A61K31/498 ,  C07D241/42 ,  C07D409/06 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06

CPC分类号： C07D409/06 ,  A61K31/498 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D241/42 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D405/04 ,  C07D405/06

摘要： Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.

摘要翻译： 具有式Ia结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。

公开(公告)号：US08436015B2

公开(公告)日：2013-05-07

申请号：US13063820

申请日：2009-09-10

申请人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward Metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

发明人： Songnian Lin ,  Christian P. Stevenson ,  Emma R. Parmee ,  Libo Xu ,  Xibin Liao ,  Edward Metzger ,  Rui Liang ,  Fengqi Zhang ,  John E. Stelmach

IPC分类号： A01N43/42 ,  A61K31/47 ,  C07D215/00

CPC分类号： C07D215/18 ,  C07D215/227 ,  C07D217/22 ,  C07D217/24 ,  C07D239/70 ,  C07D403/04 ,  C07D413/04

摘要： Glucagon receptor antagonist compounds of formula I are disclosed: The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.

摘要翻译： 公开了式I的胰高血糖素受体拮抗剂化合物：该化合物可用于治疗2型糖尿病和相关病症。 还包括药物组合物和治疗方法。