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1. 发明授权

US07132419B2 Pharmaceutical compounds 失效
公开(公告)号：US07132419B2
公开(公告)日：2006-11-07
申请号：US11024759
申请日：2004-12-30
申请人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Alexander Denny
发明人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Alexander Denny
IPC分类号： C07D241/46 , A61K31/498
CPC分类号： C07D403/12 , C07D241/46
摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1–C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1–C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R12)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1–C6 alkoxy, C1–C6 alkyl, SR10 and N(R12)2; Q is C1–C6 alkylene which is unsubstituted or substituted by (i) C1–C6 alkyl which is unsubstituted or substituted, (ii) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1–C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; R11 is C1–C6 alkyl, C3–C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1–C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

2. 发明申请

US20050143383A1 Pharmaceutical compounds 失效
公开(公告)号：US20050143383A1
公开(公告)日：2005-06-30
申请号：US11024759
申请日：2004-12-30
申请人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Denny
发明人： John Milton , Nigel Vicker , Adrian Folkes , Shouming Wang , William Denny
IPC分类号： C07D241/46 , C07D403/12 , A61K31/498 , C07D241/36
CPC分类号： C07D403/12 , C07D241/46
摘要： A compound which is a benzo[a]phenazine-11-carboxamide derivative of formula (I) wherein each of R1 to R4, which are the same or different, is selected from hydrogen, halogen, hydroxyl, C1-C6 alkoxy which is unsubstituted or substituted, heteroaryloxy, C1-C6 alkyl which is unsubstituted or substituted, nitro, cyano, azido, amidoxime, CO2R10, CON(R12)2, OCON(R12), SR10, SOR11, SO2R11, SO2N(R12)2, N(R2)2, NR10SO2R11, N(SO2R11)2 NR10(CH2)nCN, NR10COR11, OCOR11 or COR10; each of R5 to R7, which are the same or different, is selected from hydrogen, halogen, hydroxy, C1-C6 alkoxy, C1-C6 alkyl, SR10 and N(R12)2; Q is C1-C6 alkylene which is unsubstituted or substituted by (i) C1-C6 alkyl which is unsubstituted or substituted, (II) hydroxy, provided that the hydroxy group is not α to either of the N atoms adjacent to Q in formula (I), (iii) CO2R10, or (iv) CON(R12); R8 and R9, which are the same or different, are each hydrogen or C1-C6 alkyl, or R8 and R9 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered N-containing heterocyclic ring which may include one additional heteroatom selected from O, N and S, or one of R8 and R9 is an alkylene chain optionally interrupted by O, N or S, which is attached to a carbon atom on the alkylene chain represented by Q to complete a saturated 5- or 6-membered N-containing heterocyclic ring as defined above; R10 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; R11 is C1-C6 alkyl, C3-C6 cycloalkyl, benzyl or phenyl; each R12, which are the same or different, is hydrogen, C1-C6 alkyl cycloalkyl, benzyl or phenyl, or the two R12 groups form, together with the nitrogen atom to which they are attached a 5- or 6-membered saturated N-containing heterocyclic ring which may include 1 or 2 additional heteroatoms selected from O, N and S; and n is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; with the proviso that at least one of R1 to R4 is other than hydrogen. These compounds are inhibitors of topoisomerase I and/or topoisomerase II and can be used to treat tumours, including tumours which express MDR.

3. 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。

4. 发明授权

US08343955B2 Benzoxazepin PI3K inhibitor compounds and methods of use 有权
公开(公告)号：US08343955B2
公开(公告)日：2013-01-01
申请号：US13477587
申请日：2012-05-22
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, 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 B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, 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.

5. 发明申请

US20110076292A1 BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯唑西汀PI3K抑制剂化合物及其使用方法
公开(公告)号：US20110076292A1
公开(公告)日：2011-03-31
申请号：US12890812
申请日：2010-09-27
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , C07D498/04 , C07D491/044 , C07D498/14 , A61K31/4196 , A61K31/496 , A61K31/454 , A61K39/00 , A61P35/00 , A61P35/02 , A61P29/00 , A61P9/00 , A61P1/16 , A61P31/12 , A61P7/00 , A61P3/10
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, 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 B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, 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的苯并氧氮杂化合物，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; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，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。

6. 发明申请

US20110065701A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20110065701A1
公开(公告)日：2011-03-17
申请号：US12840070
申请日：2010-07-20
申请人： Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
发明人： Irina Chuckowree , Adrian Folkes , Tim Hancox , Stephen Shuttleworth
IPC分类号： A61K31/5377 , A61P35/00 , A61P37/00 , A61P29/00 , A61P25/00 , A61P35/02
CPC分类号： A61K31/5355 , C07D495/04
摘要： A thienopyrimidine of formula (I): and the pharmaceutically acceptable salts thereof have activity as inhibitors of PI3K with selectivity for the P110α subtype, and may be used to treat diseases and disorders arising from abnormal cell growth, function or behaviour, particularly those associated with PI3 kinase such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders. Processes for synthesizing the compounds are also described.
摘要翻译：式（I）的噻吩并嘧啶及其药学上可接受的盐具有作为P110α亚型选择性的PI3K抑制剂的活性，并且可用于治疗由异常细胞生长，功能或行为引起的疾病和障碍，特别是与 PI3激酶如癌症，免疫疾病，心血管疾病，病毒感染，炎症，代谢/内分泌障碍和神经障碍。还描述了合成化合物的方法。

7. 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。

8. 发明申请

US20090318411A1 PURINE PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译： PURINE PI3K抑制剂化合物及其使用方法
公开(公告)号：US20090318411A1
公开(公告)日：2009-12-24
申请号：US12474613
申请日：2009-05-29
申请人： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
发明人： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
IPC分类号： A61K31/5377 , C07D473/00
CPC分类号： C07D473/32
摘要： Purine compounds of Formula I, 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 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的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其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，并用于治疗诸如由脂质激酶介导的癌症。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。

9. 发明授权

US08445487B2 Purine PI3K inhibitor compounds and methods of use 有权
标题翻译：嘌呤PI3K抑制剂化合物及其使用方法
公开(公告)号：US08445487B2
公开(公告)日：2013-05-21
申请号：US13369941
申请日：2012-02-09
申请人： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
发明人： Georgette Castanedo , Irina Chuckowree , Adrian Folkes , Daniel P. Sutherlin , Nan Chi Wan
IPC分类号： A61K31/535 , C07D413/00 , C07D473/00
CPC分类号： C07D473/32
摘要： Purine compounds of Formula I, 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 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的嘌呤化合物，并且包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和其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，并用于治疗诸如由脂质激酶介导的癌症。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。

10. 发明申请

US20120244149A1 BENZOXAZEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE 有权
标题翻译：苯唑西汀PI3K抑制剂化合物及其使用方法
公开(公告)号：US20120244149A1
公开(公告)日：2012-09-27
申请号：US13477587
申请日：2012-05-22
申请人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
发明人： Nicole Blaquiere , Steven Do , Danette Dudley , Adrian Folkes , Robert Heald , Timothy Heffron , Mark Jones , Aleksandr Kolesnikov , Chudi Ndubaku , Alan G. Olivero , Stephen Price , Steven Staben , Lan Wang
IPC分类号： A61K31/553 , A61K31/565 , A61P35/00 , A61P29/00 , A61P37/02 , A61P37/04 , A61P9/00 , A61P31/12 , A61P7/00 , A61P3/10 , A61P1/16 , A61K39/395 , A61P25/00
CPC分类号： C07D498/04 , A61K31/553 , A61K45/06 , C07D491/044 , C07D498/14 , C07D519/00
摘要： Benzoxazepin compounds of Formula I, 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 B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, 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的苯并氧氮杂化合物，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; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，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。

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