公开(公告)号：US08394969B2

公开(公告)日：2013-03-12

申请号：US12563782

申请日：2009-09-21

Applicant: Brett C. Bookser ,  Qun Dang ,  Tony S. Gibson ,  Hongjian Jiang ,  De Michael Chung ,  Jianming Bao ,  Jinlong Jiang ,  Andy Kassick ,  Ahmet Kekec ,  Ping Lan ,  Huagang Lu ,  Gergely M. Makara ,  F. Anthony Romero ,  Iyassu Sebhat ,  David Wilson ,  Dariusz Wodka

Inventor： Brett C. Bookser ,  Qun Dang ,  Tony S. Gibson ,  Hongjian Jiang ,  De Michael Chung ,  Jianming Bao ,  Jinlong Jiang ,  Andy Kassick ,  Ahmet Kekec ,  Ping Lan ,  Huagang Lu ,  Gergely M. Makara ,  F. Anthony Romero ,  Iyassu Sebhat ,  David Wilson ,  Dariusz Wodka

IPC: A61K31/4184 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30

CPC classification number: C07D235/26 ,  C07D235/28 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

公开(公告)号：US20130040978A1

公开(公告)日：2013-02-14

申请号：US13641767

申请日：2011-05-13

Applicant: Joseph L. Duffy ,  Jianming Bao ,  Debra L. Ondeyka ,  Sriram Tyagarajan ,  Patrick Shao ,  Feng Ye ,  Revathi Katipally ,  Paul E. Finke ,  Yi Zang ,  Michael A. Plotkin ,  F. Anthony Romero ,  Remond Moningka ,  Zahid Hussain

Inventor： Joseph L. Duffy ,  Jianming Bao ,  Debra L. Ondeyka ,  Sriram Tyagarajan ,  Patrick Shao ,  Feng Ye ,  Revathi Katipally ,  Paul E. Finke ,  Yi Zang ,  Michael A. Plotkin ,  F. Anthony Romero ,  Remond Moningka ,  Zahid Hussain

IPC: C07D498/10 ,  C07D519/00 ,  A61P25/22 ,  A61P3/04 ,  A61P3/00 ,  A61P25/24 ,  A61K31/438 ,  A61P3/10

CPC classification number: C07D498/10 ,  C07D519/00

Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.

Abstract translation: 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。

公开(公告)号：US20100105747A1

公开(公告)日：2010-04-29

申请号：US12593168

申请日：2008-04-07

Applicant: Robert J. DeVita ,  Sander G. Mills ,  Jinlong Jiang ,  Andrew J. Kassick ,  Jianming Bao

Inventor： Robert J. DeVita ,  Sander G. Mills ,  Jinlong Jiang ,  Andrew J. Kassick ,  Jianming Bao

IPC: A61K31/422 ,  C07D209/02 ,  C07D413/04 ,  A61K31/40

CPC classification number: C07D209/44 ,  C07D413/04

Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.

Abstract translation: 本发明涉及某些可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的羟甲基醚异二氢吲哚化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂 以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，LUTS，抑郁和焦虑）中的用途。

公开(公告)号：US20090286777A1

公开(公告)日：2009-11-19

申请号：US12226294

申请日：2007-05-11

Applicant: Jianming Bao ,  Robert J. DeVita ,  Sander G. Mills ,  Gregori J. Morriello

Inventor： Jianming Bao ,  Robert J. DeVita ,  Sander G. Mills ,  Gregori J. Morriello

IPC: A61K31/437 ,  C07D471/04 ,  A61K31/5377 ,  A61K31/506

CPC classification number: C07D471/04

Abstract: The present invention is directed to certain 5,6-fused pyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract translation: 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂的某些5,6-稠合的吡咯烷化合物，以及速激肽抑制剂，特别是物质P。本发明还涉及包含这些化合物的药物制剂 作为活性成分以及化合物及其制剂在治疗某些疾病（包括呕吐，尿失禁，抑郁和焦虑）中的用途。

公开(公告)号：US20090069284A1

公开(公告)日：2009-03-12

申请号：US12288518

申请日：2008-10-21

Applicant: Robert K. Baker ,  Jianming Bao ,  Shouwu Miao ,  Kathleen M. Rupprecht

Inventor： Robert K. Baker ,  Jianming Bao ,  Shouwu Miao ,  Kathleen M. Rupprecht

IPC: A61K31/397 ,  C07D205/04 ,  C07D401/06 ,  A61K31/4427 ,  A61K31/4178 ,  A61K31/4196 ,  C07D205/06 ,  C07D403/06

CPC classification number: C07D205/04 ,  C07D205/06 ,  C07D401/06 ,  C07D403/06 ,  C07D403/10 ,  C07D405/06 ,  C07D409/06

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract translation: 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US20090048248A1

公开(公告)日：2009-02-19

申请号：US12086810

申请日：2006-12-18

Applicant: Robert J. DeVita ,  Jianming Bao ,  Sander G. Mills

Inventor： Robert J. DeVita ,  Jianming Bao ,  Sander G. Mills

IPC: A61K31/407 ,  C07D491/052 ,  A61K31/5377 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/497 ,  A61K31/427 ,  A61K31/422 ,  A61K31/4196

CPC classification number: C07D491/04

Abstract: The present invention is directed to certain hydropyranopyrrolidine compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract translation: 本发明涉及可用作神经激肽-1（NK-1）受体拮抗剂，速激肽抑制剂，特别是物质P的某些氢吡喃并吡咯烷化合物。本发明还涉及包含这些化合物作为活性成分的药物制剂， 使用化合物及其制剂治疗某些疾病，包括呕吐，尿失禁，抑郁和焦虑。

公开(公告)号：US06809199B2

公开(公告)日：2004-10-26

申请号：US10023231

申请日：2001-12-17

Applicant: James B. Doherty ,  John E. Stelmach ,  Meng-Hsin Chen ,  Luping Liu ,  Julianne A. Hunt ,  Rowena D. Ruzck ,  Joung L. Goulet ,  David D. Wisnoski ,  Swaminathan Ravi Natarajan ,  Kathleen M. Rupprecht ,  Jianming Bao ,  Shouwu Miao ,  Xingfang Hong ,  Peter J. Sinclair ,  Florida Kallashi

Inventor： James B. Doherty ,  John E. Stelmach ,  Meng-Hsin Chen ,  Luping Liu ,  Julianne A. Hunt ,  Rowena D. Ruzck ,  Joung L. Goulet ,  David D. Wisnoski ,  Swaminathan Ravi Natarajan ,  Kathleen M. Rupprecht ,  Jianming Bao ,  Shouwu Miao ,  Xingfang Hong ,  Peter J. Sinclair ,  Florida Kallashi

IPC: C07D23972

CPC classification number: C07D215/227 ,  C07D221/06 ,  C07D231/12 ,  C07D233/56 ,  C07D239/80 ,  C07D249/08 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D409/14 ,  C07D417/12 ,  C07D451/02 ,  C07D471/04 ,  C07D487/08

Abstract: Compounds described by the chemical formula (I) or a pharmaceutically acceptable salt thereof: are inhibitors of p38 useful in the treatment of inflammatory diseases such as arthritis.

Abstract translation: 由化学式（I）表示的化合物或其药学上可接受的盐是可用于治疗炎性疾病如关节炎的p38的抑制剂。

公开(公告)号：US06303637B1

公开(公告)日：2001-10-16

申请号：US09422500

申请日：1999-10-21

Applicant: Jianming Bao ,  Andrew Kotliar ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

Inventor： Jianming Bao ,  Andrew Kotliar ,  Frank Kayser ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

IPC: A61K31445

CPC classification number: C07D211/96 ,  A61K31/445 ,  A61K31/47 ,  A61K31/52 ,  A61K31/535 ,  A61K31/70 ,  A61K38/13 ,  A61K45/06 ,  C07D211/26 ,  A61K31/365 ,  A61K31/16 ,  A61K2300/00

Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.

Abstract translation: 本发明涉及可用作治疗自身免疫性疾病，心律失常等的钾通道抑制剂的一类式I的杂环化合物。

公开(公告)号：US06194458B1

公开(公告)日：2001-02-27

申请号：US09422499

申请日：1999-10-21

Applicant: Robert K. Baker ,  Jianming Bao ,  Frank Kayser ,  Andrew Kotliar ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

Inventor： Robert K. Baker ,  Jianming Bao ,  Frank Kayser ,  Andrew Kotliar ,  William H. Parsons ,  Kathleen M. Rupprecht ,  Christopher F. Claiborne ,  David A. Claremon ,  Nigel Liverton ,  Wayne J. Thompson

IPC: A61K3122

CPC classification number: C07D307/79 ,  A61K45/06 ,  C07C235/60 ,  C07C271/20

Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.

Abstract translation: 本发明涉及一般结构式I的苯甲酰胺钾通道抑制剂。本发明的化合物可用于治疗自身免疫性疾病，预防外来器官移植排斥和相关疾病，疾病和疾病以及心律失常。 也包括本发明范围的药物制剂，其包含式I化合物和药物载体，以及包含式I化合物，一种或多种免疫抑制化合物和药物载体的药物制剂。

公开(公告)号：US5763478A

公开(公告)日：1998-06-09

申请号：US733040

申请日：1996-10-16

Applicant: Robert K. Baker ,  Frank Kayser ,  Jianming Bao ,  William H. Parsons ,  Kathleen M. Rupprecht

Inventor： Robert K. Baker ,  Frank Kayser ,  Jianming Bao ,  William H. Parsons ,  Kathleen M. Rupprecht

IPC: C07D313/06 ,  C07D493/04 ,  A61K31/365 ,  C07D493/02

CPC classification number: C07D493/04 ,  C07D313/06

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.