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1. 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

2. 发明申请

US20050020587A1 Nicotinamide derivatives useful as PDE4 inhibitors 审中-公开
标题翻译：可用作PDE4抑制剂的烟酰胺衍生物
公开(公告)号：US20050020587A1
公开(公告)日：2005-01-27
申请号：US10896355
申请日：2004-07-20
申请人： Simon Bailey , Christopher Barber
发明人： Simon Bailey , Christopher Barber
IPC分类号： C07D401/12 , A61K31/541 , A61K31/4436 , A61K31/496 , A61K31/5377 , C07
CPC分类号： C04B35/632 , C07D401/12
摘要： This invention relates to nicotinamide derivatives of general formula (I): in which X, Y, n, Z, L and R have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
摘要翻译：本发明涉及通式（I）的烟酰胺衍生物：其中X，Y，n，Z，L和R具有本文定义的含义，以及制备用于制备含有和这种衍生物的用途。

3. 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。

4. 发明申请

US20050234066A1 Alpha substituted carboxylic acids 审中-公开
公开(公告)号：US20050234066A1
公开(公告)日：2005-10-20
申请号：US10825923
申请日：2004-04-15
申请人： Simon Bailey , Paul Humphries , Donald Skalitzky , Wei Su , Luke Raymond Zehnder
发明人： Simon Bailey , Paul Humphries , Donald Skalitzky , Wei Su , Luke Raymond Zehnder
IPC分类号： A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506
CPC分类号： C07D263/32
摘要： Alpha substituted carboxylic acids of formula (I): wherein R1 and R2 are as defined in the specification and R3 is wherein Y, Ar1, Ar2, Ar3, R4, R5, R6, R7, R8, R9, R9a, R10, R11, R12, R17, ring A, and p are as defined in the specification; pharmaceutical compositions containing effective amounts of said compounds or their salts are useful for treating PPAR, specifically PPAR α/γ related disorders, such as diabetes, dyslipidemia, obesity and inflammatory disorders.

5. 发明授权

US06897306B2 3-heterocyclylpropanohydroxamic acids 失效
标题翻译： 3-杂环基丙酰氧肟酸
公开(公告)号：US06897306B2
公开(公告)日：2005-05-24
申请号：US10198710
申请日：2002-07-16
申请人： Simon Bailey , Stephane Billotte , Paul Vincent Fish , Kim James , Nicholas Murray Thomson , Andrew Michael Derrick
发明人： Simon Bailey , Stephane Billotte , Paul Vincent Fish , Kim James , Nicholas Murray Thomson , Andrew Michael Derrick
IPC分类号： A61K38/00 , C07C233/48 , C07C259/14 , C07C317/44 , C07D263/32 , C07D271/06 , C07F9/40 , C07K5/02 , C07K5/078 , C07D413/14
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

US20090131397A1 ESTROGEN MODULATORS 审中-公开
标题翻译：雌激素调节剂
公开(公告)号：US20090131397A1
公开(公告)日：2009-05-21
申请号：US12262565
申请日：2008-10-31
申请人： Simon Bailey , Stephen Douglas Barrett , Larry Don Bratton , Stephen Alan Fakhoury , Sandra Marie Jennings , Lorna Helen Mitchell , Raj Kumar Raheja , Veerabahu Shanmugasundaram
发明人： Simon Bailey , Stephen Douglas Barrett , Larry Don Bratton , Stephen Alan Fakhoury , Sandra Marie Jennings , Lorna Helen Mitchell , Raj Kumar Raheja , Veerabahu Shanmugasundaram
IPC分类号： A61K31/397 , C07D261/06 , A61K31/42 , C07D413/02 , A61K31/4439 , A61K31/496 , A61P17/00 , A61K31/5377 , C07D417/02 , A61K31/541 , C07D487/12 , A61K31/506
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。

7. 发明申请

US20060014780A1 Nicotinamide derivatives useful as PDE4 inhibitors 审中-公开
公开(公告)号：US20060014780A1
公开(公告)日：2006-01-19
申请号：US11229395
申请日：2005-09-16
申请人： Simon Bailey , Elisabeth Gautier , Alan Henderson , Thomas Magee , Anthony Marfat , John Mathias , Dale McLeod , Sandra Monaghan , Blanda Stammen
发明人： Simon Bailey , Elisabeth Gautier , Alan Henderson , Thomas Magee , Anthony Marfat , John Mathias , Dale McLeod , Sandra Monaghan , Blanda Stammen
IPC分类号： A61K31/46 , A61K31/4545 , A61K31/4433 , A61K31/4415 , C07D405/02 , C07D401/02 , C07D453/02
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.

8. 发明授权

US06949573B2 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：US06949573B2
公开(公告)日：2005-09-27
申请号：US10361062
申请日：2003-02-06
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： A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4545 , A61K31/455 , A61K31/46 , A61K31/537 , A61K45/06 , A61P1/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/10 , A61P7/06 , A61P9/12 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/12 , A61P17/02 , A61P17/04 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P25/30 , A61P27/02 , A61P29/00 , A61P31/16 , A61P31/22 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D213/82 , C07D401/12 , C07D405/12 , C07D451/04 , C07D451/10 , C07D213/643
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.
摘要翻译：本发明涉及烟酰胺衍生物以及制备用于制备含有这些衍生物的组合物和用途的中间体的方法。根据本发明的烟酰胺衍生物可用于许多疾病，病症和病症，特别是炎性，过敏性，呼吸道疾病，病症和病症以及伤口。

9. 发明授权

US06837084B2 Interlock mechanisms 失效
标题翻译：联锁机制
公开(公告)号：US06837084B2
公开(公告)日：2005-01-04
申请号：US10203263
申请日：2001-02-06
申请人： Simon Bailey , Timothy Christopher Stubbs , Justin Titus Tun
发明人： Simon Bailey , Timothy Christopher Stubbs , Justin Titus Tun
IPC分类号： E05B35/08 , E05B11/00
CPC分类号： E05B35/086 , F16B2200/30 , Y10T70/7446 , Y10T70/7706 , Y10T70/7768
摘要： An interlock unit (10) for use with at least one other like unit (11) to form an interlock mechanism has a top face (13) and opposed pairs of side walls (12) with at least one runner bar (17, 18) mounted in the unit for lateral sliding movement. An actuator (14, 15, 22) is supported on the top face (13), to effect lateral sliding movement of the runner bar (17, 18). One wall of the unit is provided with one part (27) of a two-part connector with the other part (33) on the opposed wall whereby two similar units may be joined together by relative sliding movement of the two units in the plane of the side walls (12). Joining together of two units (10, 11) in this way also joins together the runner bars (17) or (18) of the two units such that sliding motion of the runner bar (17) of one unit (10) is transferred to the runner bar (17) of the connected unit (11), for at least one direction of sliding movement of the runner bars (17).
摘要翻译：与至少一个其他类似单元（11）一起使用以形成互锁机构的联锁单元（10）具有顶面（13）和相对的一对侧壁（12），其具有至少一个流道杆（17,18）安装在单元中用于横向滑动。致动器（14,15,22）被支撑在顶面（13）上，以实现流道杆（17,18）的横向滑动运动。该单元的一个壁设置有两部分连接器的一部分（27），另一部分（33）在相对的壁上，由此两个相似的单元可以通过两个单元在平面内的相对滑动侧壁（12）。以这种方式将两个单元（10,11）连接在一起也将两个单元的流道杆（17）或（18）连接在一起，使得一个单元（10）的流道杆（17）的滑动运动被转移到所述连接单元（11）的所述流道杆（17）用于所述流道杆（17）的滑动运动的至少一个方向。

10. 发明授权

US06821972B2 3-heterocyclylpropanohydroxamic acid PCP inhibitors 失效
标题翻译： 3-杂环基丙酰氧肟酸PCP抑制剂
公开(公告)号：US06821972B2
公开(公告)日：2004-11-23
申请号：US10112338
申请日：2002-03-29
申请人： Simon Bailey , Paul Vincent Fish , Kim James , Gavin Alistar Whitlock
发明人： Simon Bailey , Paul Vincent Fish , Kim James , Gavin Alistar Whitlock
IPC分类号： C07D27106
CPC分类号： C07D271/06 , C07D263/32 , C07D413/04 , C07D413/14
摘要： Compounds of formula (I): and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a PCP-mediated condition or disease using the same.
摘要翻译：式（I）化合物及其盐，溶剂合物，水合物和前药是有用的PCP抑制剂，其制备方法，包含其的组合物，以及使用其的PCP介导的病症或疾病的治疗方法。

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