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1. 发明申请

US20120157448A1 COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经损伤性疾病的化合物
公开(公告)号：US20120157448A1
公开(公告)日：2012-06-21
申请号：US13302876
申请日：2011-11-22
申请人： Adam Cook , Indrani W. Gunawardana , Kevin W. Hunt , Nicholas C. Kallan , Andrew T. Metcalf , Brad Newhouse , Tony P. Tang , Allen A. Thomas , Michael Siu , Malcolm Huestis , Matthew Volgraf
发明人： Adam Cook , Indrani W. Gunawardana , Kevin W. Hunt , Nicholas C. Kallan , Andrew T. Metcalf , Brad Newhouse , Tony P. Tang , Allen A. Thomas , Michael Siu , Malcolm Huestis , Matthew Volgraf
IPC分类号： A61K31/4439 , C07D491/20 , A61K31/527 , C07D513/10 , A61K31/444 , A61K31/424 , C07D498/10 , C07D513/20 , A61P25/28 , C07D491/107 , C07D498/20 , A61K31/547
CPC分类号： C07D498/20 , C07D491/107 , C07D491/20 , C07D498/10 , C07D513/10 , C07D513/20
摘要： The invention provides novel tricyclic compounds of Formula I′ that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
摘要翻译：本发明提供抑制APP分解酶切割的新颖的式I'三环化合物，并且可用作治疗神经变性疾病的治疗剂。

2. 发明申请

US20120083501A1 COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
公开(公告)号：US20120083501A1
公开(公告)日：2012-04-05
申请号：US13244034
申请日：2011-09-23
申请人： Kevin W. Hunt , Tony P. Tang , Allen A. Thomas
发明人： Kevin W. Hunt , Tony P. Tang , Allen A. Thomas
IPC分类号： A61K31/4188 , C07D491/20 , A61P25/28 , A61K31/4439 , A61K31/506 , C07D491/107 , A61K31/437
CPC分类号： A61K31/4188 , C07D491/107 , C07D491/20
摘要： The invention provides novel tricyclic compounds of Formula I′ that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.

3. 发明申请

US20120065195A1 COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES 审中-公开
标题翻译：用于治疗神经损伤性疾病的化合物
公开(公告)号：US20120065195A1
公开(公告)日：2012-03-15
申请号：US13077477
申请日：2011-03-31
申请人： Christopher T. Clark , Adam Cook , Indrani W. Gunawardana , Kevin W. Hunt , Nicholas C. Kallan , Michael Siu , Allen A. Thomas , Matthew Volgraf
发明人： Christopher T. Clark , Adam Cook , Indrani W. Gunawardana , Kevin W. Hunt , Nicholas C. Kallan , Michael Siu , Allen A. Thomas , Matthew Volgraf
IPC分类号： A61K31/547 , A61K31/527 , A61K31/4439 , A61K31/423 , A61K31/4184 , C07D279/08 , C07D413/10 , C07D401/14 , C07D263/52 , C07D235/02 , C07D417/10 , A61P25/28 , C07D403/10 , C07D401/10 , C07D491/107 , A61K31/506
CPC分类号： C07D401/14 , C07D263/64 , C07D401/10 , C07D403/10 , C07D413/10 , C07D417/10
摘要： The invention provides novel spirotetrahydronaphthalene compounds of Formula α that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
摘要翻译：本发明提供抑制APP分解酶切割的新颖的式α的四氢四氢化合物，可用作治疗神经变性疾病的治疗剂。

4. 发明授权

US09133187B2 Serine/threonine kinase inhibitors 有权
标题翻译：丝氨酸/苏氨酸激酶抑制剂
公开(公告)号：US09133187B2
公开(公告)日：2015-09-15
申请号：US14002079
申请日：2012-02-28
申请人： James F. Blake , Huifen Chen , Mark Joseph Chicarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwarz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky , Steven Boyd
发明人： James F. Blake , Huifen Chen , Mark Joseph Chicarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwarz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky , Steven Boyd
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00 , C07D471/04 , C07D491/052 , A61K45/06
CPC分类号： C07D471/04 , A61K31/519 , A61K45/06 , C07D491/052
摘要： Compounds having the formula I wherein Z, Z1 Z2 Z3, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译：具有式I的化合物，其中Z，Z 1 Z 2 Z 3，R 3a，R 3b和R b如本文所定义是ERK激酶的抑制剂。还公开了用于治疗过度增殖性疾病的组合物和方法。

5. 发明授权

US08003662B2 Heterobicyclic thiophene compounds and methods of use 有权
标题翻译：异双环噻吩化合物及其使用方法
公开(公告)号：US08003662B2
公开(公告)日：2011-08-23
申请号：US11699830
申请日：2007-01-30
申请人： James F. Blake , Steven Boyd , Jason De Meese , John J. Gaudino , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian
发明人： James F. Blake , Steven Boyd , Jason De Meese , John J. Gaudino , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian
IPC分类号： A61K31/4365
CPC分类号： C07D495/04 , C07D519/00
摘要： Compounds of Formula I and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula I and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式I化合物及其药学上可接受的盐可用于抑制受体酪氨酸激酶和用于治疗由此介导的病症。公开了使用式I化合物及其药学上可接受的盐在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

6. 发明授权

US06521431B1 Biodegradable cross-linkers having a polyacid connected to reactive groups for cross-linking polymer filaments 失效
标题翻译：具有连接到用于交联聚合物长丝的反应性基团的多元酸的可生物降解的交联剂
公开(公告)号：US06521431B1
公开(公告)日：2003-02-18
申请号：US09338404
申请日：1999-06-22
申请人： Patrick F. Kiser , Allen A. Thomas
发明人： Patrick F. Kiser , Allen A. Thomas
IPC分类号： C12N1102
CPC分类号： A61K9/5138 , A61K9/1635 , A61K9/2027 , A61K9/5146 , A61L24/0042 , A61L27/58 , A61L31/148 , C07C69/675 , C07C233/20 , C07C243/28 , C07D207/46 , C08F8/00 , C08F2800/10 , C08F2810/20 , C08G63/00 , Y10S530/812 , Y10S530/813 , Y10S530/815 , Y10S977/906 , Y10T442/184 , C08F220/58
摘要： Biodegradable cross-linkers are provided having a polyacid core with at least two acidic groups covalently connected to reactive groups usable to cross-link polymer filaments. Between at least one reactive group and an acidic group of the polyacid is a biodegradable region which preferably consists of a hydroxyalkyl acid ester sequence having 1, 2, 3, 4, 5 or 6 hydroxyalkyl acid ester groups. The polyacid may be attached to a water soluble region that is attached to the biodegradable region having attached reactive groups. The hydroxyalkyl acid ester group is preferably a lactate or glycolate. Polyacids include diacids, triacids, tetraacids and pentaacids, and the reactive group may contain a carbon-carbon double bond. A network of cross-linked polymer filaments having adefined biodegradation rate can be formed using the cross-linkers. The network may contain biologically active molecules, and can be in the form of a microparticle or nanoparticle, or hydrogel. The polymer filaments may be preformed polymer filaments of polynucleic acids, polypeptides, proteins or carbohydrates. The cross-linkers may be copolymerized with charged monomers such as acrylic monomers containing charged groups. Applications of the cross-linkers and network include controlled release of drugs and cosmetics, tissue engineering, wound healing, hazardous waste remediation, metal chelation, swellable devices for absorbing liquids and prevention of surgical adhesions.
摘要翻译：提供了可生物降解的交联剂，其具有多酸核心，其具有共价连接到可用于交联聚合物长丝的反应性基团的至少两个酸性基团。在多酸的至少一个反应性基团和酸性基团之间是可生物降解的区域，其优选由具有1,2,3,4,5或6个羟烷基酸酯基团的羟烷基酸酯序列组成。多酸可以连接到附着到具有附着的反应性基团的可生物降解区域的水溶性区域。羟烷基酸酯基优选为乳酸盐或乙醇酸盐。多元酸包括二酸，三酸，四酸和五酸，并且反应性基团可以含有碳 - 碳双键。可以使用交联剂形成具有定义的生物降解速率的交联聚合物长丝网。网络可以包含生物活性分子，并且可以是微粒或纳米颗粒或水凝胶的形式。聚合物长丝可以是多核酸，多肽，蛋白质或碳水化合物的预制聚合物长丝。交联剂可以与带电单体共聚，例如含有带电基团的丙烯酸单体。交联剂和网络的应用包括药物和化妆品的控制释放，组织工程，伤口愈合，危险废物修复，金属螯合，用于吸收液体的可膨胀装置和预防手术粘连。

7. 发明申请

US20130338140A1 SERINE/THREONINE KINASE INHIBITORS 有权
标题翻译：丝氨酸/螺旋激酶抑制剂
公开(公告)号：US20130338140A1
公开(公告)日：2013-12-19
申请号：US14002079
申请日：2012-02-28
申请人： James F. Blake , Huifen Chen , Mark Joseph Chcarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwartz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky
发明人： James F. Blake , Huifen Chen , Mark Joseph Chcarelli , Jason Demeese , Rustam Garrey , John J. Gaudino , Robert J. Kaus , Gabrielle R. Kolakowski , Allison L. Marlow , Peter J. Mohr , Li Ren , Jacob Schwartz , Christopher S. Siedem , Allen A. Thomas , Eli Wallace , Steven Mark Wenglowsky
IPC分类号： C07D471/04 , A61K45/06 , A61K31/519
CPC分类号： C07D471/04 , A61K31/519 , A61K45/06 , C07D491/052
摘要： Compounds having the formula I wherein Z, Z1 Z2 Z, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
摘要翻译：具有式I的化合物，其中Z，Z 1 Z 2 Z，R 3a，R 3b和R b如本文所定义，是ERK激酶的抑制剂。还公开了用于治疗过度增殖性疾病的组合物和方法。

8. 发明申请

US20100256356A1 HETEROBICYCLIC PYRAZOLE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：异酞菁化合物及其使用方法
公开(公告)号：US20100256356A1
公开(公告)日：2010-10-07
申请号：US12693975
申请日：2010-01-26
申请人： James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
发明人： James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
IPC分类号： C07D471/04 , C07D451/04
CPC分类号： C07D471/04
摘要： Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式Ia和Ib的化合物及其立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制受体酪氨酸激酶和用于治疗由此介导的病症。使用式Ia和Ib化合物及其立体异构体，几何异构体，互变异构体，溶剂化物及其药学上可接受的盐的方法用于体外，原位和体内诊断，预防或治疗哺乳动物细胞中的这种病症或相关病理学条件被公开。

9. 发明授权

US07723330B2 Heterobicyclic pyrazole compounds and methods of use 有权
标题翻译：异双环吡唑化合物及其使用方法
公开(公告)号：US07723330B2
公开(公告)日：2010-05-25
申请号：US11714342
申请日：2007-03-06
申请人： James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
发明人： James F. Blake , Steven Armen Boyd , Jason De Meese , Kin Chiu Fong , John J. Gaudino , Tomas Kaplan , Allison L. Marlow , Jeongbeob Seo , Allen A. Thomas , Hongqi Tian , Frederick Cohen , Wendy B. Young
IPC分类号： A61K31/437 , A61K31/5025 , A61K31/4985 , A61K31/519 , A61K31/55 , A61K31/541 , A61K31/5355 , C07D487/04 , A61K31/551 , A61K31/501 , A61K31/497 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
摘要翻译：式Ia和Ib的化合物及其立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制受体酪氨酸激酶和用于治疗由此介导的病症。使用式Ia和Ib化合物及其立体异构体，几何异构体，互变异构体，溶剂化物及其药学上可接受的盐的方法用于体外，原位和体内诊断，预防或治疗哺乳动物细胞中的这种病症或相关病理学条件被公开。

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