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1. 发明授权

US06552036B2 3-(Diarylmethylene)-8-azabicyclo[3.2.1]octane derivatives 有权
标题翻译： 3-（二芳基亚甲基）-8-氮杂双环[3.2.1]辛烷衍生物
公开(公告)号：US06552036B2
公开(公告)日：2003-04-22
申请号：US09791246
申请日：2001-02-22
申请人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
发明人： Robert E. Boyd , John R. Carson , Steven J. Coats , Lou Anne Neilson , Philip M Pitis , Wu-Nan Wu
IPC分类号： C07D45102
CPC分类号： C07D451/02 , A61K31/439
摘要： 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.
摘要翻译：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。

2. 发明申请

US20120302541A1 4-SUBSTITUTED-2-PHENOXY-PHENYLAMINE DELTA OPIOID RECEPTOR MODULATORS 有权
标题翻译： 4-取代-2-苯基 - 苯甲酰三嗪类阿片受体调节剂
公开(公告)号：US20120302541A1
公开(公告)日：2012-11-29
申请号：US13503433
申请日：2010-10-28
申请人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
发明人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
IPC分类号： A61K31/40 , C07D211/26 , A61K31/445 , C07D401/12 , A61K31/4439 , C07D405/12 , A61K31/4025 , C07D409/12 , C07D403/12 , A61K31/506 , C07D295/096 , A61K31/495 , C07D413/12 , A61K31/4245 , C07D451/02 , A61K31/46 , C07C217/84 , A61K31/136 , C07D205/04 , A61K31/397 , C07D453/02 , A61K31/439 , A61P29/00 , A61P19/02 , A61P25/06 , A61P11/02 , A61P13/10 , A61P17/00 , A61P11/12 , A61P25/00 , A61P25/02 , A61P1/00 , A61P35/00 , A61P25/24 , A61P25/16 , A61P25/30 , A61P25/32 , A61P13/00 , A61P15/00 , A61P1/12 , A61P9/00 , A61P11/00 , C07D207/14
CPC分类号： C07D401/12 , C07C211/48 , C07C211/50 , C07C233/08 , C07C233/11 , C07C233/65 , C07C255/50 , C07D205/04 , C07D207/09 , C07D211/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/04 , C07D453/02
摘要： 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, Ra, and Y are defined herein.
摘要翻译：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，Ra和Y如本文所定义。

3. 发明授权

US08846655B2 4-substituted-2-phenoxy-phenylamine delta opioid receptor modulators 有权
标题翻译： 4-取代-2-苯氧基 - 苯胺δ阿片样物质受体调节剂
公开(公告)号：US08846655B2
公开(公告)日：2014-09-30
申请号：US13503433
申请日：2010-10-28
申请人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
发明人： Steven J. Coats , Haiyan Bian , Chaozhong Cai , Bart L. DeCorte , Li Liu , Mark J. Macielag , Scott L. Dax , Philip M. Pitis , Peter J. Connolly , Wei He
IPC分类号： A61K31/40 , A61K31/445 , A61K31/4439 , A61K31/4025 , A61K31/506 , A61K31/495 , C07D211/56 , C07D405/12 , C07D207/09 , C07C255/50 , C07C211/48 , C07D413/12 , C07D401/12 , C07C211/50 , C07D205/04 , C07C233/08 , C07C233/11 , C07C233/65 , C07D451/04 , C07D453/02 , C07D409/12
CPC分类号： C07D401/12 , C07C211/48 , C07C211/50 , C07C233/08 , C07C233/11 , C07C233/65 , C07C255/50 , C07D205/04 , C07D207/09 , C07D211/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/04 , C07D453/02
摘要： 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, Ra, and Y are defined herein.
摘要翻译：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，Ra和Y如本文所定义。

4. 发明授权

US08513271B2 Pyrimidine compounds as delta opioid receptor modulators 有权
标题翻译：嘧啶化合物作为δ阿片受体调节剂
公开(公告)号：US08513271B2
公开(公告)日：2013-08-20
申请号：US12913966
申请日：2010-10-28
申请人： 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
发明人： 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分类号： A01N43/54
CPC分类号： C07D239/47 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： 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.
摘要翻译：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。

5. 发明申请

US20140038968A1 AMINO-HETEROARYL-CONTAINING PROKINETICIN 1 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：含有氨基酸的化合物1受体拮抗剂
公开(公告)号：US20140038968A1
公开(公告)日：2014-02-06
申请号：US13653452
申请日：2012-10-17
申请人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
发明人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
IPC分类号： C07D251/38 , C07D403/12
CPC分类号： C07D251/38 , C07D401/12 , C07D403/12 , C07D405/14
摘要： 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.
摘要翻译：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。

6. 发明授权

US08609627B2 Purine nucleoside monophosphate prodrugs for treatment of cancer and viral infections 有权
公开(公告)号：US08609627B2
公开(公告)日：2013-12-17
申请号：US13144718
申请日：2010-02-09
申请人： Jong Hyun Cho , Steven J. Coats , Raymond F. Schinazi , Hongwang Zhang , Longhu Zhou
发明人： Jong Hyun Cho , Steven J. Coats , Raymond F. Schinazi , Hongwang Zhang , Longhu Zhou
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K31/7076 , A61K31/675 , A61K31/7028 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K31/708 , A61K45/06 , C07D473/16 , C07H19/173 , C07H19/20 , Y02A50/385 , Y02A50/387 , Y02A50/393 , A61K2300/00
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing cancer and viral infections, in particular, HIV, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV in human patients or other animal hosts. The compounds are certain 6-substituted purine monophosphates, and pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof. In particular, the compounds show potent antiviral activity against HIV-1, HIV-2, HCV, Norovirus, Saporovirus, HSV-1, HSV-2, Dengue virus, Yellow fever, and HBV.

7. 发明申请

US20130210774A1 POTENT AND SELECTIVE INHIBITORS OF HEPATITIS C VIRUS 有权
标题翻译： HEPATITIS C病毒的选择性抑制剂
公开(公告)号：US20130210774A1
公开(公告)日：2013-08-15
申请号：US13817522
申请日：2011-08-26
申请人： Steven J. Coats , Franck Amblard , Hongwang Zhang , Longhu Zhou , Richard Anthony Whitaker , Tamara Rosario McBrayer , Raymond F. Schinazi , Junxing Shi
发明人： Steven J. Coats , Franck Amblard , Hongwang Zhang , Longhu Zhou , Richard Anthony Whitaker , Tamara Rosario McBrayer , Raymond F. Schinazi , Junxing Shi
IPC分类号： A61K31/4178 , C07D403/14 , A61K31/4192 , A61K45/06 , A61K31/5377 , C07D401/14 , A61K31/444 , A61K31/506 , C07D403/04 , A61K31/655
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/4192 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D407/14 , C07D413/14
摘要： The present invention is directed to compounds, compositions and methods for treating or preventing hepatitis C virus (HCV) infection in human subjects or other animal hosts. The compounds are as also pharmaceutically acceptable, salts, prodrugs, and other derivatives thereof as pharmaceutical compositions and methods for treatment or prevention of HCV infection.
摘要翻译：本发明涉及用于治疗或预防人受试者或其他动物宿主中丙型肝炎病毒（HCV）感染的化合物，组合物和方法。作为用于治疗或预防HCV感染的药物组合物和方法，化合物也是其药学上可接受的盐，前药和其它衍生物。

8. 发明授权

US08362247B2 Prokineticin 1 receptor antagonists 有权
标题翻译：原肌动蛋白1受体拮抗剂
公开(公告)号：US08362247B2
公开(公告)日：2013-01-29
申请号：US13113751
申请日：2011-05-23
申请人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
发明人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
IPC分类号： C07D403/06 , C07D403/12 , C07D403/14 , C07D401/06 , C07D401/12 , C07D401/14 , A61K31/506 , A61P1/00 , A61P1/06
CPC分类号： C07D239/545 , C07D251/20 , C07D251/34 , C07D251/38 , C07D251/46 , C07D403/12
摘要： 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.
摘要翻译：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。

9. 发明授权

US07968710B2 Prokineticin 1 receptor antagonists 有权
公开(公告)号：US07968710B2
公开(公告)日：2011-06-28
申请号：US11375407
申请日：2006-03-14
申请人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
发明人： Steven J. Coats , Alexey B. Dyatkin , Wei He , Joseph Lisko , Tamara A. Miskowski , Janet L. Ralbovsky , Mark J. Schulz
IPC分类号： C07D251/30 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D401/12 , C07D403/12 , A61K31/53 , A61P1/12 , A61P1/06 , A61P1/00
CPC分类号： C07D239/545 , C07D251/20 , C07D251/34 , C07D251/38 , C07D251/46 , C07D403/12
摘要： 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.

10. 发明申请

US20100210840A1 STEREOSELECTIVE PROCESS FOR PREPARING PURINE DIOXOLANE NUCLEOSIDE DERIVATIVES 审中-公开
标题翻译：制备嘌呤二氧杂环己烷衍生物的立体选择性方法
公开(公告)号：US20100210840A1
公开(公告)日：2010-08-19
申请号：US12670386
申请日：2008-07-24
申请人： Steven J. Coats
发明人： Steven J. Coats
IPC分类号： C07D473/16
CPC分类号： C07D473/16
摘要： A cost-effective process scale method for preparing purine dioxolane nucleoside derivatives in racemic or optically pure form is disclosed, as are nucleoside derivatives prepared by the method. The method involves reacting a purine or a mono- or polysilylated purine derivative with an activated dioxolane analog to produce the dioxolane nucleoside analog in commercially useful yields. Direct reaction of purine or a mono- or polysilylated purine with dioxolanes takes place with highest reported chemical yields and excellent stereoselectivity when an additive in the form of an alpha cyano carbonyl compound or silylated alpha cyano carbonyl compounds is present in the reaction mixture during the glycosylation reaction.
摘要翻译：公开了一种用于制备外消旋或光学纯的形式的嘌呤二氧戊环核苷衍生物的成本有效的工艺规模方法，以及通过该方法制备的核苷衍生物。该方法包括使嘌呤或单或聚硅酸化嘌呤衍生物与活化的二氧杂环戊烷类似物反应，以商业上有效的收率产生二氧戊环核苷类似物。在糖基化过程中当反应混合物中存在α氰基羰基化合物或甲硅烷基化α氰基羰基化合物形式的添加剂时，嘌呤或单或多聚化嘌呤与二氧戊环的直接反应发生，报道最高的化学产率和优异的立体选择性反应。

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