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1. 发明授权

US08119624B2 Fused phenyl amido heterocyclic compounds 有权
标题翻译：稠合苯基酰氨基杂环化合物
公开(公告)号：US08119624B2
公开(公告)日：2012-02-21
申请号：US12913059
申请日：2010-10-27
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
IPC分类号： A61K31/44 , A61K31/415 , A61K31/47 , A61K31/42 , A61K31/397 , A61K31/4965 , A61K31/41 , C07D215/00 , C07D401/00 , C07D413/00 , C07D405/00 , C07D403/00 , C07D231/00
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein:Ring A is (4-12)-membered heterocyclyl;Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自环A，环B，环C，R 1，R 1a，R 2，R 3，R 4，L 2，n，t，w和z的稠合苯环如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

2. 发明授权

US07842713B2 Fused phenyl amido heterocyclic compounds 有权
标题翻译：稠合苯基酰氨基杂环化合物
公开(公告)号：US07842713B2
公开(公告)日：2010-11-30
申请号：US11746359
申请日：2007-05-09
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
IPC分类号： A61K31/4155 , C07D231/10
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein:Ring A is (4-12)-membered heterocyclyl;Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自环A，环B，环C，R 1，R 1a，R 2，R 3，R 4，L 2，n，t，w和z的稠合苯环如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

3. 发明授权

US07470715B2 Estrogen modulators 失效
标题翻译：雌激素调节剂
公开(公告)号：US07470715B2
公开(公告)日：2008-12-30
申请号：US11612582
申请日：2006-12-19
申请人： Simon Bailey , Stephen Douglas Barrett , Raj Kumar Raheja , Veerabahu Shanmugasundaram
发明人： Simon Bailey , Stephen Douglas Barrett , Raj Kumar Raheja , Veerabahu Shanmugasundaram
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/08 , C07D261/18 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/08 , C07D471/04
摘要： The present application is directed to a new class of isoxazoles and their use as estrogen modulators.
摘要翻译：本申请涉及一类新的异恶唑及其作为雌激素调节剂的用途。

4. 发明授权

US07141586B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
标题翻译：可用作PDE4抑制剂的烟酰胺衍生物
公开(公告)号：US07141586B2
公开(公告)日：2006-11-28
申请号：US10896315
申请日：2004-07-20
申请人： Simon Bailey , Christopher Gordon Barber , Paul Alan Glossop , Donald Stuart Middleton
发明人： Simon Bailey , Christopher Gordon Barber , Paul Alan Glossop , Donald Stuart Middleton
IPC分类号： C07D213/02 , A61K31/44
CPC分类号： C04B35/632 , C07D213/82 , C07D401/12 , C07D405/12
摘要： This invention relates to nicotinamide derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing, and the uses of such derivatives: wherein each substituent is defined herein.
摘要翻译：本发明涉及式（I）的烟酰胺衍生物以及制备用于制备含有此类衍生物的药物组合物的中间体的方法：其中每个取代基在本文中定义。

5. 发明授权

US06448278B2 Procollagen C-proteinase inhibitors 失效
标题翻译：前胶蛋白C蛋白酶抑制剂
公开(公告)号：US06448278B2
公开(公告)日：2002-09-10
申请号：US09735968
申请日：2000-12-13
申请人： Simon Bailey , Stephane Billotte , Andrew Michael Derrick , Paul Vincent Fish , Kim James , Nicholas Murray Thomson
发明人： Simon Bailey , Stephane Billotte , Andrew Michael Derrick , Paul Vincent Fish , Kim James , Nicholas Murray Thomson
IPC分类号： A61K314245
CPC分类号： C07D271/06 , A61K38/00 , C07C233/48 , C07C259/14 , C07C317/44 , C07C2601/14 , C07D263/32 , C07F9/4006 , C07K5/0222 , C07K5/06139
摘要： Compounds of formula (I): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.
摘要翻译：式（I）化合物及其盐，溶剂合物，前药等，其中取代基具有本文提及的值，为前胶原C-蛋白酶（PCP）抑制剂，并且可用于PCP介导的病症。

6. 发明申请

US20080280875A1 FUSED PHENYL AMIDO HETEROCYCLIC COMPOUNDS 有权
标题翻译：熔融的苯胺类杂环化合物
公开(公告)号：US20080280875A1
公开(公告)日：2008-11-13
申请号：US11746359
申请日：2007-05-09
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukul , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukul , Ru Zhou
IPC分类号： A61K31/497 , A61K31/4155 , A61K31/4192 , A61K31/42 , A61K31/4245 , A61K31/426 , A61K31/50 , A61K31/5375 , C07D205/02 , C07D271/06 , C07D261/02 , C07D249/04 , C07D241/02 , C07D239/02 , C07D237/02 , C07D231/02 , C07D221/00 , C07D213/02 , C07D295/00 , C07D285/12 , C07D277/02 , A61P3/00 , A61K31/505 , A61K31/433 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/4965
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自以下的稠合苯环：环A，环B，环C，R 1，R 1a，R 2， R S，R 3，R 4，L 2，n，t，w和z如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

7. 发明申请

US20070149564A1 ESTROGEN MODULATORS 失效
标题翻译：雌激素调节剂
公开(公告)号：US20070149564A1
公开(公告)日：2007-06-28
申请号：US11612582
申请日：2006-12-19
申请人： Simon Bailey , Stephen Barrett , Larry Bratton , Stephen Fakhoury , Sandra Jennings , Lorna Mitchell , Raj Raheja , Veerabahu Shanmugasundaram
发明人： Simon Bailey , Stephen Barrett , Larry Bratton , Stephen Fakhoury , Sandra Jennings , Lorna Mitchell , Raj Raheja , Veerabahu Shanmugasundaram
IPC分类号： A61K31/47
CPC分类号： C07D261/08 , C07D261/18 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/08 , C07D471/04
摘要： The present application is directed to a new class of isoxazoles and their use as estrogen modulators.
摘要翻译：本申请涉及一类新的异恶唑及其作为雌激素调节剂的用途。

8. 发明授权

US07060717B2 Nicotinamide derivatives useful as PDE4 inhibitors 失效
公开(公告)号：US07060717B2
公开(公告)日：2006-06-13
申请号：US10865263
申请日：2004-06-09
申请人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
发明人： Simon Bailey , Elisabeth C. L. Gautier , Alan J. Henderson , Thomas V. Magee , Anthony Marfat , John P. Mathias , Dale G. McLeod , Sandra M. Monaghan , Blanda L. C. Stammen
IPC分类号： A61K31/445 , C07D211/72
CPC分类号： C07D213/82 , A61K31/4433 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , Y02A50/411 , A61K2300/00
摘要： The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic, respiratory diseases, disorders and conditions, as well as wounds.

9. 发明申请

US20050032838A1 Nicotinamide derivatives useful as PDE4 inhibitors 失效
标题翻译：可用作PDE4抑制剂的烟酰胺衍生物
公开(公告)号：US20050032838A1
公开(公告)日：2005-02-10
申请号：US10896315
申请日：2004-07-20
申请人： Simon Bailey , Christopher Barber , Paul Glossop , Donald Middleton
发明人： Simon Bailey , Christopher Barber , Paul Glossop , Donald Middleton
IPC分类号： A61K31/4415 , A61K31/4439 , A61K31/454 , A61P37/00 , C07D213/02 , C07D213/82 , C07D401/12 , C07D405/12 , C07D41/02
CPC分类号： C04B35/632 , C07D213/82 , C07D401/12 , C07D405/12
摘要： This invention relates to nicotinamide derivatives of formula (I) and to processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions containing, and the uses of such derivatives: wherein R1 is selected from the group consisting of hydrogen, methyl or halo; R7 is attached to the 3- or 4-position of the phenyl ring and is S(O)pR8, R8 is (C1-C4)alkyl optionally substituted by (C3-C6)cycloalkyl; p is 0, 1 or 2; R6 is selected from the group consisting of hydrogen, halo, (C1-C3)alkyl and (C1-C3)alkoxy; m is 0 or 1; L is a (C3-C8)carbocyclic non-aromatic ring; R2 is hydrogen, hydroxy, (C1-C3)alkoxy, (C1-C3)alkyl (optionally substituted by hydroxy or by (C1-C3)alkoxy), CO2R9, NR10R11 or CONR10R11; R3 is hydrogen or (C1-C3)alkyl; R9 is hydrogen or (C1-C3)alkyl; R10 and R11 are each independently hydrogen, or, are selected from the group consisting of: (C1-C6)alkyl optionally substituted by phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; (C3-C8)cycloalkyl; CO((C1-C6)alkyl) optionally substituted by hydroxy, halo, (C3-C8)cycloalkyl, (C1-C3)alkoxy, phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; CO(R12), wherein R12 is (C3-C8)cycloalkyl optionally substituted by (C1-C3)alkyl or R12 is phenyl or a 5- or 6-membered heterocyclic ring incorporating 1 to 3 heteroatom(s) independently selected from N, O and S, which phenyl is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl or (C1-C3)alkoxy and which heterocyclic ring is optionally substituted by one or more subsituents selected from hydroxy, halo, (C1-C3)alkyl, (C1-C3)alkoxy or oxo; and CO2(C1-C3)alkyl); or R10 and R11 are taken together with the N atom to which they are attached to form a 5- or 6-membered lactam.
摘要翻译：本发明涉及式（I）的烟酰胺衍生物以及制备用于制备含有此类衍生物的药物组合物的中间体的方法：其中R1选自氢，甲基或光环; R7连接到苯环的3-或4-位，是S（O）p R 8，R 8是任选被（C 3 -C 6）环烷基取代的（C 1 -C 4）烷基; p为0,1或2; R 6选自氢，卤素，（C 1 -C 3）烷基和（C 1 -C 3）烷氧基; m为0或1; L是（C 3 -C 8）碳环非芳香环; R 2是氢，羟基，（C 1 -C 3）烷氧基，（C 1 -C 3）烷基（任选被羟基或被（C 1 -C 3）烷氧基取代），CO 2 R 9，NR 10 R 11或CONR 10 R 11; R3是氢或（C1-C3）烷基; R9是氢或（C1-C3）烷基; R 10和R 11各自独立地为氢，或选自：任选被苯基取代的（C 1 -C 6）烷基或包含1至3个独立地选自N的杂原子的5或6元杂环，O和S，该苯基任选被一个或多个选自羟基，卤素，（C 1 -C 3）烷基或（C 1 -C 3）烷氧基的取代基取代，并且该杂环任选被一个或多个选自羟基，卤代，（C1-C3）烷基，（C1-C3）烷氧基或氧代; （C 3 -C 8）环烷基; 任选被羟基，卤素，（C 3 -C 8）环烷基，（C 1 -C 3）烷氧基，苯基或独立地并入1至3个杂原子的5或6元杂环取代的CO（（C 1 -C 6）烷基）谢尔

10. 发明申请

US20110039821A1 Fused Phenyl Amido Heterocyclic Compounds 有权
标题翻译：熔融苯基酰胺杂环化合物
公开(公告)号：US20110039821A1
公开(公告)日：2011-02-17
申请号：US12913059
申请日：2010-10-27
申请人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
发明人： Hao Bai , Simon Bailey , Dilip Ramakant Bhumralkar , Feng C. Bi , Fengli Guo , Mingying He , Paul Stuart Humphries , Anthony Lai Ling , Jihong Lou , Seiji Nukui , Ru Zhou
IPC分类号： A61K31/397 , C07D405/12 , A61K31/443 , C07D401/14 , A61K31/4155 , C07D403/14 , C07D401/12 , A61K31/4709 , A61K31/4439 , C07D413/12 , A61K31/423 , C07D403/12 , A61K31/497 , A61K31/4192 , A61P3/00
CPC分类号： C07D405/14 , C07D401/12 , C07D405/12
摘要： The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或溶剂化物，其中：环A是（4-12） - 杂环基; 环B是选自环A，环B，环C，R 1，R 1a，R 2，R 3，R 4，L 2，n，t，w和z的稠合苯环如说明书中所定义。本发明还涉及包含式（I）化合物的药物组合物和治疗由葡萄糖激酶调节介导的病症的方法，所述方法包括向哺乳动物施用有效量的式（I）化合物。

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