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1. 发明申请

US20060116402A1 N-substituted benzimidazolyl c-Kit inhibitors and combinatorial benzimidazole library 失效
标题翻译： N-取代苯并咪唑c-Kit抑制剂和组合苯并咪唑文库
公开(公告)号：US20060116402A1
公开(公告)日：2006-06-01
申请号：US11290028
申请日：2005-11-30
申请人： Andrew Crew , Matthew Cox , Radoslaw Laufer , Neil Pegg , Colin Sambrook Smith , Yingchuan Sun , Robin Wilkes , Jonathan Williams
发明人： Andrew Crew , Matthew Cox , Radoslaw Laufer , Neil Pegg , Colin Sambrook Smith , Yingchuan Sun , Robin Wilkes , Jonathan Williams
IPC分类号： A61K31/4439 , A61K31/4184 , C07D403/02 , C07D409/02
CPC分类号： C07D235/06 , C07B2200/11 , C07D401/12 , C07D403/10 , C07D403/14 , C07D405/10 , C07D409/10 , C07D409/14 , C07D413/10 , C07D417/14 , C40B40/00
摘要： Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II): are useful in providing compounds to assay for such therapeutically useful compounds.
摘要翻译：由式（I）表示的化合物或其药学上可接受的盐或N-氧化物可用于治疗肿瘤。由式（I）表示的化合物或由式（II）表示的苯并咪唑化合物组成的组合文库可用于提供化合物以测定这些治疗有用的化合物。

2. 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。

3. 发明申请

US20060040988A1 Cox-2 Inhibiting pyridine derivatives 失效
标题翻译： Cox-2抑制吡啶衍生物
公开(公告)号：US20060040988A1
公开(公告)日：2006-02-23
申请号：US10527799
申请日：2003-09-12
申请人： Paul Beswick , Neil Pegg , Martin Swarbrick , John Skidmore , Sandeep Modi
发明人： Paul Beswick , Neil Pegg , Martin Swarbrick , John Skidmore , Sandeep Modi
IPC分类号： A61K31/444 , C07D401/14
CPC分类号： C07D213/74 , C07D213/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发烧和炎症。

4. 发明申请

US20050032821A1 Pyrimidine derivatives useful as selective cox-2 inhibitors 失效
标题翻译：可用作选择性cox-2抑制剂的嘧啶衍生物
公开(公告)号：US20050032821A1
公开(公告)日：2005-02-10
申请号：US10477547
申请日：2002-05-23
申请人： Alan Naylor , Jeremy Payne , Neil Pegg
发明人： Alan Naylor , Jeremy Payne , Neil Pegg
IPC分类号： A61K31/505 , A61K31/513 , A61P29/00 , A61P43/00 , C07D239/34 , C07D401/12 , C07D45/02
CPC分类号： C07D239/34 , A61K31/505 , C07D401/12
摘要： The invention provides the compounds of formula (I) in which: R1 is selected from the group consisting of H, C1-6alkyl, C1-2alkyl substituted by one to five fluorine atoms, C3-6alkenyl, C3-10cycloalkylC0-6alkyl, C4-12bridged cycloalkyl, A(CR4R5)n and b(CR4R5)n; R2 is C1-2alkyl substituted by one to five fluorine atoms; R3 is selected from the group consisting of C1-6alkyl, NH2 and R7CONH; R4 and R5 are independently selected from H or C1-6alkyl; A is an unsubstituted 5- or 6-membered heteroaryl or an unsubstituted 6-membered aryl, or a 5- or 6-membered heteroaryl or a 6-membered aryl substituted by one or more R6; R6 is selected from the group consisting of halogen, C1-6alkyl, C1-6alkyl substituted by one or more fluorine atoms, C1-6alkoxy, C1-6alkoxy substituted by one or more F, NH2SO2 and C1-6alkylSO2; B is selected from the group consisting of Formula (i) and (ii) and where (iv) defines the point of attachment of the ring; R7 is selected from the group consisting of H, C1-6alkyl, C1-6alkoxy, C1-6alkylOC1-6alkyl, phenyl, HO2CC1-6alkyl, C1-6alkylOCOC1-6alkyl, C1-6alkylOCO, H2C1-6alkyl, C1-4alkylOCONHC1-6alkyl and C1-6alkylCONHC1-6alkyl; and n is 0 to 4. Compounds of formula (I) are potent and selective inhibitors of COX-2 and are of use in treatment of the pain, fever and inflammation of variety of conditions and diseases.
摘要翻译：本发明提供式（I）化合物，其中：R 1选自H，C 1-6烷基，被1至5个氟原子取代的C 1-2烷基，C 3-6烯基，C 3-10环烷基C 1-6烷基，C 4-12桥环烷基，A（CR 4 R 5）n和b（CR 4 R 5）n; R 2是被1至5个氟原子取代的C 1-2烷基; R 3选自C 1-6烷基，NH 2和R 7 CONH; R 4和R 5独立地选自H或C 1-6烷基; A是未取代的5-或6-元杂芳基或未取代的6-元芳基，或被一个或多个R 6取代的5-或6-元杂芳基或6-元芳基; R 6选自卤素，C 1-6烷基，被一个或多个氟原子取代的C 1-6烷基，C 1-6烷氧基，被一个或多个F，NH 2 SO 2和C 1-6烷基SO 2取代的C 1-6烷氧基; B选自式（i）和（ii），其中（iv）定义环的连接点; R 7选自H，C 1-6烷基，C 1-6烷氧基，C 1-6烷基C 1-6烷基，苯基，HO 2 C 1-6烷基，C 1-6烷基COOC 1-6烷基，C 1-6烷基COO，H 2 C 1-6烷基，C 1-4烷基OCONHC 1 -6-烷基和C 1-6烷基CONHC 1-6烷基; 并且n为0至4.式（I）化合物是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发热和炎症。

5. 发明授权

US07446117B2 Cox-2 inhibiting pyridine derivatives 失效
标题翻译： Cox-2抑制吡啶衍生物
公开(公告)号：US07446117B2
公开(公告)日：2008-11-04
申请号：US10527799
申请日：2003-09-12
申请人： Paul Beswick , Neil Pegg , Martin Swarbrick , John Skidmore , Sandeep Modi
发明人： Paul Beswick , Neil Pegg , Martin Swarbrick , John Skidmore , Sandeep Modi
IPC分类号： A61K31/4418 , C07D213/73 , C07D213/64
CPC分类号： C07D213/74 , C07D213/64 , C07D231/12 , C07D233/56 , C07D249/08 , C07D405/12
摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
摘要翻译：式（I）化合物或其药学上可接受的盐是COX-2的有效和选择性抑制剂，并且可用于治疗各种病症和疾病的疼痛，发热和炎症。

6. 发明申请

US20060047123A1 Mercaptoamides as histone deacetylase inhibitors 审中-公开
标题翻译：巯基乙酰胺作为组蛋白脱乙酰酶抑制剂
公开(公告)号：US20060047123A1
公开(公告)日：2006-03-02
申请号：US11218396
申请日：2005-09-02
申请人： Saleh Ahmed , Celine Combet , Scott Cuthill , Graham Dawson , William Gattrell , Mario Lobell , Neil Pegg , Imaad Saba , Simon Swain , Claire Thomas , Graham Wynne
发明人： Saleh Ahmed , Celine Combet , Scott Cuthill , Graham Dawson , William Gattrell , Mario Lobell , Neil Pegg , Imaad Saba , Simon Swain , Claire Thomas , Graham Wynne
IPC分类号： C07D333/22 , C07D277/18 , C07D263/02
CPC分类号： C07D213/40 , C07C323/32 , C07C323/60 , C07C327/32 , C07C2601/02 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D209/08 , C07D213/74 , C07D213/75 , C07D215/38 , C07D217/06 , C07D233/54 , C07D235/30 , C07D249/08 , C07D263/10 , C07D277/04 , C07D277/46 , C07D277/62 , C07D285/135 , C07D295/088 , C07D295/135 , C07D295/185 , C07D307/52 , C07D307/81 , C07D309/12 , C07D319/18 , C07D333/20 , C07D409/04 , C07D417/04 , C07D513/04
摘要： Mercaptoamide compounds, represented by Formulas (IA), (IB), (IIA), and (IIB): or a pharmaceutically acceptable salt thereof, inhibit histone deacetylase enzyme and are useful for the treatment and/or prevention of various infections, cancerous diseases, and conditions.
摘要翻译：由式（IA），（IB），（IIA）和（IIB）表示的巯丙酰胺化合物或其药学上可接受的盐抑制组蛋白脱乙酰酶，并且可用于治疗和/或预防各种感染，癌性疾病和条件。

7. 发明申请

US20050187235A1 Pyrimidine derivatives useful as selective COX-2 inhibitors 审中-公开
标题翻译：可用作选择性COX-2抑制剂的嘧啶衍生物
公开(公告)号：US20050187235A1
公开(公告)日：2005-08-25
申请号：US11110118
申请日：2005-04-20
申请人： Alan Naylor , Jeremy Payne , Neil Pegg
发明人： Alan Naylor , Jeremy Payne , Neil Pegg
IPC分类号： A61K31/505 , A61K31/513 , A61P29/00 , A61P43/00 , C07D239/34 , C07D401/12 , C07D45/02
CPC分类号： C07D239/34 , A61K31/505 , C07D401/12
摘要： Methods of treating a subject suffering from a condition which is mediated by COX-2.
摘要翻译：治疗患有COX-2介导的病症的受试者的方法。

8. 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。

9. 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。

10. 发明申请

US20050282845A1 Substituted pyrimidines as selective cyclooxygenase-2 inhibitors 审中-公开
标题翻译：取代的嘧啶作为选择性环氧合酶-2抑制剂
公开(公告)号：US20050282845A1
公开(公告)日：2005-12-22
申请号：US11165073
申请日：2005-06-23
申请人： Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
发明人： Malcolm Carter , Alan Naylor , Martin Pass , Jeremy Payne , Neil Pegg
IPC分类号： A61K31/506 , A61P29/00 , A61P43/00 , C07D405/12
CPC分类号： C07D405/12
摘要： Methods for the treatment of pain, fever, inflammation of a variety of conditions and diseases.
摘要翻译：治疗疼痛，发烧，炎症的各种病症和疾病的方法。

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