公开(公告)号：US20140212382A1

公开(公告)日：2014-07-31

申请号：US14117815

申请日：2012-05-16

Applicant: Raymond F. Schinazi ,  Jong Hyun Cho ,  Longhu Zhou ,  Hongwang Zhang ,  Ugo Pradere ,  Steven J. Coats

Inventor： Raymond F. Schinazi ,  Jong Hyun Cho ,  Longhu Zhou ,  Hongwang Zhang ,  Ugo Pradere ,  Steven J. Coats

IPC: C07F9/6558 ,  A61K31/7076 ,  A61K45/06 ,  C07F9/6574

CPC classification number: C07F9/65586 ,  A61K31/7076 ,  A61K45/06 ,  C07D473/16 ,  C07F9/65742 ,  C07H19/20 ,  C07H19/207 ,  C07H19/213

Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing viral infections using nucleoside analog monophosphate prodrugs. More specifically, HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever in human patients or other animal hosts. The compounds are certain 2,6-diamino 2-C-methyl purine nucleoside monophosphate prodrugs and modified prodrug analogs, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HCV, Norovirus, Saporovirus, Dengue virus, Chikungunya virus and Yellow fever. This invention teaches how to modify the metabolic pathway of 2,6-diamino 2′-C-methyl purine and deliver nucleotide triphosphate(s) to polymerases at heretofore unobtainable therapeutically-relevant concentrations.

Abstract translation: 本发明涉及使用核苷类似物单磷酸酯前药治疗或预防病毒感染的化合物，组合物和方法。 更具体地，在人类患者或其他动物宿主中，HCV，诺如病毒，Saporovirus，登革热病毒，基孔肯雅病毒和黄热病。 这些化合物是某些2,6-二氨基2-C-甲基嘌呤核苷单磷酸前体药物和修饰的前药类似物及其药学上可接受的盐，前药和其它衍生物。 特别地，这些化合物显示针对HCV，诺如病毒，Saporovirus，登革热病毒，基孔肯雅病毒和黄热病的有效的抗病毒活性。 本发明教导了如何修饰2,6-二氨基2'-C-甲基嘌呤的代谢途径，并将迄今为止无法获得的治疗相关浓度的核苷酸三磷酸转移至聚合酶。

公开(公告)号：US08415321B2

公开(公告)日：2013-04-09

申请号：US12421362

申请日：2009-04-09

Applicant: Raymond F. Schinazi ,  Richard Anthony Whitaker ,  Tamara Rosario McBrayer ,  Steven J. Coats

Inventor： Raymond F. Schinazi ,  Richard Anthony Whitaker ,  Tamara Rosario McBrayer ,  Steven J. Coats

IPC: A61K31/7068 ,  C07H19/067

CPC classification number: A61K31/7076 ,  A61K38/21 ,  A61K2300/00

Abstract: A method and composition for treating a host infected with a Caliciviridae virus, such as a Norovirus, comprising administering an effective treatment amount of a described modified nucleoside or a pharmaceutically acceptable salt thereof, is provided.

Abstract translation: 提供了用于治疗感染了杯状病毒科（例如诺如病毒）的宿主的方法和组合物，其包括施用有效治疗量的所述修饰的核苷或其药学上可接受的盐。

公开(公告)号：US08394809B2

公开(公告)日：2013-03-12

申请号：US12913948

申请日：2010-10-28

Applicant: Steven J. Coats ,  Yue-Mei Zhang ,  Shu-Chen Lin ,  Li Liu ,  Tamara A. Miskowski ,  Scott L. Dax ,  Henry Breslin ,  Bart L. De Corte ,  Wei He

Inventor： Steven J. Coats ,  Yue-Mei Zhang ,  Shu-Chen Lin ,  Li Liu ,  Tamara A. Miskowski ,  Scott L. Dax ,  Henry Breslin ,  Bart L. De Corte ,  Wei He

IPC: A01N43/54 ,  A61K31/505

CPC classification number: C07D239/52 ,  A61K31/506 ,  C07D239/28 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.

Abstract translation: 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中R1，Y，R2，R3和Ra在本文中定义。

公开(公告)号：US20120142627A1

公开(公告)日：2012-06-07

申请号：US13306967

申请日：2011-11-29

Applicant: Raymond F. Schinazi ,  Steven J. Coats

Inventor： Raymond F. Schinazi ,  Steven J. Coats

IPC: A61K31/7072 ,  A61P31/20 ,  A61P31/18 ,  C07F9/6561 ,  A61K31/675

CPC classification number: A61K31/7072 ,  A61K31/675 ,  A61K45/06 ,  C07F9/65616 ,  A61K2300/00

Abstract: The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV and HBV, in human patients or other animal hosts. The compounds are certain 6-substituted-2-amino-purine dioxolane monophosphates or phosphonates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof.

Abstract translation: 本发明涉及在人类患者或其他动物宿主中治疗或预防癌症和病毒感染，特别是HIV和HBV的化合物，组合物和方法。 这些化合物是某些6-取代-2-氨基 - 嘌呤二氧戊环单磷酸酯或膦酸酯及其药学上可接受的盐，前药和其它衍生物。

公开(公告)号：US20120129862A1

公开(公告)日：2012-05-24

申请号：US13113751

申请日：2011-05-23

Applicant: Steven J. Coats ,  Alexey B. Dyatkin ,  Wei He ,  Joseph Lisko ,  Tamara A. Miskowski ,  Janet L. Ralbovsky ,  Mark J. Schulz

Inventor： Steven J. Coats ,  Alexey B. Dyatkin ,  Wei He ,  Joseph Lisko ,  Tamara A. Miskowski ,  Janet L. Ralbovsky ,  Mark J. Schulz

IPC: A61K31/53 ,  C07D403/12 ,  C07D251/20 ,  A61P29/00 ,  C07D251/38 ,  A61P1/00 ,  A61P1/12 ,  A61P35/00 ,  C07D251/46 ,  C07D251/30

CPC classification number: C07D239/545 ,  C07D251/20 ,  C07D251/34 ,  C07D251/38 ,  C07D251/46 ,  C07D403/12

Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.

Abstract translation: 本发明涉及某些新的式（I）化合物：以及制备这些化合物，组合物，中间体和衍生物以及用于治疗促动蛋白原1或原激素1受体介导的病症的方法。

公开(公告)号：US20110105520A1

公开(公告)日：2011-05-05

申请号：US12913966

申请日：2010-10-28

Applicant: STEVEN J. COATS ,  HAIYAN BIAN ,  PETER J. CONNOLLY ,  GILLES BIGNAN ,  CHAOZHONG CAI ,  SCOTT L. DAX ,  BART L. DECORTE ,  SHU-CHEN LIN ,  LI LIU ,  MARK J. MACIELAG ,  PHILIP M. PITIS ,  YUE-MEI ZHANG ,  BIN ZHU ,  WEI HE

Inventor： STEVEN J. COATS ,  HAIYAN BIAN ,  PETER J. CONNOLLY ,  GILLES BIGNAN ,  CHAOZHONG CAI ,  SCOTT L. DAX ,  BART L. DECORTE ,  SHU-CHEN LIN ,  LI LIU ,  MARK J. MACIELAG ,  PHILIP M. PITIS ,  YUE-MEI ZHANG ,  BIN ZHU ,  WEI HE

IPC: A61K31/497 ,  C07D239/47 ,  C07D403/14 ,  A61K31/506 ,  A61P25/00 ,  A61P25/28 ,  A61P25/30 ,  A61P25/24 ,  A61P13/00 ,  A61P15/12

CPC classification number: C07D239/47 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, and L, A, and Ra are defined herein.

Abstract translation: 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中R1，R2，R3和L，A和Ra在本文中定义。

公开(公告)号：US20110105455A1

公开(公告)日：2011-05-05

申请号：US12913948

申请日：2010-10-28

Applicant: STEVEN J. COATS ,  Yue-Mei Zhang ,  Shu-Chen Lin ,  Li Liu ,  Tamara A. Miskowski ,  Scott L. Dax ,  Henry Breslin ,  Bart L. De Corte ,  Wei He

Inventor： STEVEN J. COATS ,  Yue-Mei Zhang ,  Shu-Chen Lin ,  Li Liu ,  Tamara A. Miskowski ,  Scott L. Dax ,  Henry Breslin ,  Bart L. De Corte ,  Wei He

IPC: A61K31/506 ,  C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  C07D401/14 ,  A61K31/505 ,  A61K31/5377 ,  A61P29/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/30 ,  A61P25/32 ,  A61P1/12 ,  A61P9/00 ,  A61P15/00 ,  A61P11/00

CPC classification number: C07D239/52 ,  A61K31/506 ,  C07D239/28 ,  C07D239/34 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.

Abstract translation: 公开了用于治疗各种疾病，综合征，病症和障碍（包括疼痛）的化合物，组合物和方法。 这样的化合物由式I表示如下：其中R1，Y，R2，R3和Ra在本文中定义。

公开(公告)号：US20090163505A1

公开(公告)日：2009-06-25

申请号：US12256891

申请日：2008-10-23

Applicant: Steven J. COATS ,  Alexey B. Dyatkin ,  Wei He ,  Joseph Lisko ,  Tamara A. Miskowski ,  Janet L. Ralbovsky ,  Mark J. Schulz

Inventor： Steven J. COATS ,  Alexey B. Dyatkin ,  Wei He ,  Joseph Lisko ,  Tamara A. Miskowski ,  Janet L. Ralbovsky ,  Mark J. Schulz

IPC: A61K31/53 ,  C07D403/12 ,  A61P1/00 ,  A61P35/00

CPC classification number: C07D251/38 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14

Abstract: The present invention relates to certain novel compounds of Formula (I): and methods for preparing these compounds, compositions, intermediates and derivatives thereof and for the treatment of prokineticin 1 or prokinetin 1 receptor mediated disorders.

Abstract translation: 本发明涉及某些新的式（I）化合物：以及制备这些化合物，组合物，中间体及其衍生物以及用于治疗促动蛋白原1或原激素1受体介导的病症的方法。

公开(公告)号：US20090042871A1

公开(公告)日：2009-02-12

申请号：US12248150

申请日：2008-10-09

Applicant: Steven J. Coats ,  Scott L. Dax ,  Bart DeCorte ,  Li Liu ,  Mark McDonnell ,  James J. McNally

Inventor： Steven J. Coats ,  Scott L. Dax ,  Bart DeCorte ,  Li Liu ,  Mark McDonnell ,  James J. McNally

IPC: A61K31/5415 ,  C07D471/08 ,  A61P25/00 ,  A61K31/538

CPC classification number: C07D451/04

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic δ-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract translation: 本发明涉及Δ阿片样物质受体调节剂。 更具体地，本发明涉及三环类阿片样物质调节剂。 还描述了使用本发明的化合物治疗轻度至重度疼痛和各种疾病的药物和兽医组合物和方法。

公开(公告)号：US06552036B2

公开(公告)日：2003-04-22

申请号：US09791246

申请日：2001-02-22

Applicant: Robert E. Boyd ,  John R. Carson ,  Steven J. Coats ,  Lou Anne Neilson ,  Philip M Pitis ,  Wu-Nan Wu

Inventor： Robert E. Boyd ,  John R. Carson ,  Steven J. Coats ,  Lou Anne Neilson ,  Philip M Pitis ,  Wu-Nan Wu

IPC: C07D45102

CPC classification number: C07D451/02 ,  A61K31/439

Abstract: This invention is directed to 3-(diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives useful as &dgr;-opioid or &mgr;-opioid receptor modulators. Depending on their agonist or antagonist effect, the compounds are useful analgesics, immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract translation: 本发明涉及可用作δ-阿片样物质或μ-阿片受体调节剂的3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物。 根据其激动剂或拮抗剂的作用，化合物是有用的止痛剂，免疫抑制剂，抗炎剂，用于治疗神经和精神病症的药剂，用于药物和酒精滥用的药物，用于治疗胃炎和腹泻的药剂，用于治疗的心血管药剂和药剂 的呼吸系统疾病。