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1. 发明授权

US08263633B2 Benzoxepin PI3K inhibitor compounds and methods of use 有权
标题翻译：苯并西林PI3K抑制剂化合物及其使用方法
公开(公告)号：US08263633B2
公开(公告)日：2012-09-11
申请号：US12890810
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Richard Goldsmith , Robert Heald , Timothy Heffron , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , BinQing Wei
IPC分类号： A61K31/41 , C07D249/14
CPC分类号： C07D495/04 , A61K31/381 , A61K31/41 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/4365 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K45/06 , C07D249/14 , C07D495/14 , C07D513/04 , C07D513/14
摘要： Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I 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的苯并氧杂环己烯化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。公开了使用式I化合物在体外，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。

2. 发明申请

US20110130363A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯并吡喃和苯唑西林PI3K抑制剂化合物及其使用方法
公开(公告)号：US20110130363A1
公开(公告)日：2011-06-02
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/69 , C07D313/06 , C07D333/00 , C07D491/14 , C07F5/02 , C07D249/10 , C07D405/14 , A61K31/335 , A61K31/381 , A61K31/4196 , A61K31/443 , A61K31/497 , C12N9/99 , A61P35/00 , A61P35/02
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，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，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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。

3. 发明申请

US20090247567A1 BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯并吡喃和苯唑西林PI3K抑制剂化合物及其使用方法
公开(公告)号：US20090247567A1
公开(公告)日：2009-10-01
申请号：US12414403
申请日：2009-03-30
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： A61K31/4353 , A61K31/429 , A61K31/38 , C07D491/044 , C07D513/04 , C07D495/04
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，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，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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。

4. 发明申请

US20070037813A1 Serine Protease Inhibitors 审中-公开
标题翻译：丝氨酸蛋白酶抑制剂
公开(公告)号：US20070037813A1
公开(公告)日：2007-02-15
申请号：US11537482
申请日：2006-09-29
申请人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
发明人： Ignacio Aliagas-Martin , Dean Artis , Michael Dina , John Flygare , Richard Goldsmith , Regina Munroe , Alan Olivero , Richard Pastor , Thomas Rawson , Kirk Robarge , Daniel Sutherlin , Kenneth Weese , Aihe Zhou , Yan Zhu
IPC分类号： A61K31/50 , A61K31/44 , A61K31/165 , C07D237/02
CPC分类号： C07C257/18 , C07C311/05 , C07C311/08 , C07C311/13 , C07C311/18 , C07C311/29 , C07C311/51
摘要： Compounds having the structure shown below are useful to inhibit serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein. These compounds may be used in methods of preventing and/or treating clotting disorders.
摘要翻译：具有如下结构的化合物可用于抑制丝氨酸蛋白酶，例如TF /因子VIIa，因子Xa，凝血酶和激肽释放酶。这些化合物可用于预防和/或治疗凝血障碍的方法。

5. 发明授权

US08399690B2 4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene compounds 有权
标题翻译： 4,5-二氢-6-氧杂-3-硫杂-1-氮杂 - 苯并[e]薁化合物
公开(公告)号：US08399690B2
公开(公告)日：2013-03-19
申请号：US13018068
申请日：2011-01-31
申请人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
发明人： Steven Do , Richard Goldsmith , Tim Heffron , Aleksandr Kolesnikov , Steven Staben , Alan G. Olivero , Michael Siu , Daniel P. Sutherlin , Bing-Yan Zhu , Paul Goldsmith , Tracy Bayliss , Adrian Folkes , Neil Pegg
IPC分类号： C07D313/00 , C07D333/00
CPC分类号： C07F5/02 , A61K31/381 , A61K31/4155 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/4365 , A61K31/4436 , A61K31/496 , A61K31/53 , C07D495/04 , C07D495/14 , C07D513/14
摘要： Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，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，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗疾病如癌症由脂质激酶介导。公开了使用式I和II的化合物在体外，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

US07846929B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
标题翻译：磷酸肌醇3-激酶抑制剂化合物及其使用方法
公开(公告)号：US07846929B2
公开(公告)日：2010-12-07
申请号：US11789427
申请日：2007-04-24
申请人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
发明人： Adrian Folkes , Stephen Shuttleworth , Sally Oxenford , Tim Hancox , Tracy Bayliss , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Kimberly Malesky , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Vickie Tsui , Shumei Wang , Christian Wiesmann , Bing-Yan Zhu , Jennafer Dotson
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia and Ib, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib 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，并且包括立体异构体，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脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。公开了将式Ia和Ib化合物用于体外，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。

7. 发明申请

US20080261989A1 Quinoxaline Inhibitors of the Hedgehog Signalling 失效
标题翻译：刺猬信号的喹喔啉抑制剂
公开(公告)号：US20080261989A1
公开(公告)日：2008-10-23
申请号：US11587963
申请日：2005-04-29
申请人： Michael F.T. Koehler , Richard Goldsmith , Daniel P. Sutherlin
发明人： Michael F.T. Koehler , Richard Goldsmith , Daniel P. Sutherlin
IPC分类号： A61K31/498 , C07D241/42 , A61P35/04
CPC分类号： C07D413/12 , C07D241/42 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12
摘要： The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I wherein A is a carbocycle or heterocycle; X is alkylene, NR4C(O), NR4C(S), NR4C(NH), NR4SO, NR4SO2, NR4C(O)NH, NR4C(S)NH, C(O)NR4, C(S)NR4, C(NH)NR4, NR4PO or NR4PO(OH) wherein R4 is H or alkyl; R1 is selected from the group consisting of alkyl, cycloalkyl, aryl or a heterocycle each of which is optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R2 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; R3 is halogen, hydroxyl, alkyl, acyl or alkoxy each optionally substituted with hydroxyl, halogen, amino, nitro, alkyl, acyl, alkylsulfonyl or alkoxy; m is 0-3; n is 0-3; and salts and solvates thereof.
摘要翻译：本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导新型抑制剂，其中化合物具有通式I，其中A是碳环或杂环; X是亚烷基，NR 4 C（O），NR 4 C（S），NR 4 C（NH），NR 4 SO 4，NR 4 SO 2，NR 4 C（O）NH，NR 4， C（S）NH，C（O）NR 4，C（S）NR 4，C（NH）NR 4，其中R 4是H或烷基;其中R 4是氢或烷基;其中R 4是氢或烷基; R 1选自烷基，环烷基，芳基或杂环，其各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R 2是卤素，羟基，烷基，酰基或烷氧基，其各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; R 3是卤素，羟基，烷基，酰基或烷氧基，其各自任选被羟基，卤素，氨基，硝基，烷基，酰基，烷基磺酰基或烷氧基取代; m为0-3; n为0-3; 及其盐和溶剂合物。

8. 发明授权

US08383620B2 Phosphoinositide 3-kinase inhibitor compounds and methods of use 有权
公开(公告)号：US08383620B2
公开(公告)日：2013-02-26
申请号：US12978106
申请日：2010-12-23
申请人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
发明人： Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Sally Oxenford , Nan Chi Wan , Georgette Castanedo , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Steven Staben , Daniel P. Sutherlin , Bing-Yan Zhu
IPC分类号： A61K31/535
CPC分类号： A61K31/5377 , A61K31/519 , C07D413/14 , C07D491/04 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

9. 发明申请

US20100262428A1 PRINT PLATFORM FOR MOBILE MARKETING 审中-公开
标题翻译：打印移动营销平台
公开(公告)号：US20100262428A1
公开(公告)日：2010-10-14
申请号：US12757753
申请日：2010-04-09
申请人： Richard Goldsmith
发明人： Richard Goldsmith
IPC分类号： G06Q30/00 , G06F17/30
CPC分类号： G06Q30/02
摘要： Systems and processes are provided that merge print and/or direct mailing marketing with mobile marketing to assist marketers to identify an interested consumer with the desired product/service in which messages are transmitted between mobile units and at least one market server to identify and provide specific messages identifying users of the mobile units and offers related to a desired product and/or service. The market server identifies such messages through the use of a market database containing unique keywords and consumer information.
摘要翻译：提供了将打印和/或直接邮寄营销与移动营销相结合的系统和流程，以协助营销人员用所需的产品/服务识别感兴趣的消费者，消费在移动单元和至少一个市场服务器之间传送，以识别和提供具体的识别移动单元的用户的消息和与期望的产品和/或服务相关的提供的消息。市场服务器通过使用包含唯一关键字和消费者信息的市场数据库来识别这样的消息。

10. 发明申请

US20080269210A1 PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：磷酸三辛酯抑制剂化合物及其使用方法
公开(公告)号：US20080269210A1
公开(公告)日：2008-10-30
申请号：US11951189
申请日：2007-12-05
申请人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
发明人： Georgette Castanedo , Jennafer Dotson , Richard Goldsmith , Janet Gunzner , Tim Heffron , Simon Mathieu , Alan Olivero , Daniel P. Sutherlin , Shumei Wang , Bing-Yan Zhu , Steven Staben , Vickie Tsui , Tracy Bayliss , Irina Chuckowree , Adrian Folkes , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D495/04 , C07D413/14 , A61P35/00 , A61K31/519
CPC分类号： C07D491/048 , C07D495/04
摘要： Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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-d的化合物，其中X是S或O，mor是吗啉基团，R 3是单环杂芳基，并且包括立体异构体，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其盐可用于调节脂质激酶（包括PI3K）的活性，以及用于治疗由脂质激酶介导的癌症等疾病。公开了使用式Ia-d化合物在体外，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疾病的方法。

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