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1. 发明授权

US07560467B2 Indazolo-tetrahydropyrimidine-carboxamide derivative kinase inhibitors 失效
标题翻译：吲唑并四氢嘧啶 - 甲酰胺衍生物激酶抑制剂
公开(公告)号：US07560467B2
公开(公告)日：2009-07-14
申请号：US10560502
申请日：2004-06-18
申请人： David Harold Drewry , Brian Evans , Krista B. Goodman , Darren Victor Steven Green , David Kendall Jung , Dennis Lee , Robert A. Stavenger , Sjoerd Nocolaas Wadman
发明人： David Harold Drewry , Brian Evans , Krista B. Goodman , Darren Victor Steven Green , David Kendall Jung , Dennis Lee , Robert A. Stavenger , Sjoerd Nocolaas Wadman
IPC分类号： C07D403/12 , A61K31/416
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D487/04
摘要： The present invention relates to indazolo-tetrahydropyrimidine-carboxamide derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such indazolo-tetrahydropyrimidine-carboxamide derivatives are useful in the treatment of diseases associated with inappropriate ROCK-1 kinase.
摘要翻译：本发明涉及吲哚并四氢嘧啶 - 甲酰胺衍生物，含有它们的组合物和药物，以及制备和使用这些化合物，组合物和药物的方法。这样的吲哚四氢嘧啶 - 甲酰胺衍生物可用于治疗与不适当的ROCK-1激酶相关的疾病。

2. 发明授权

US07348339B2 Imidazopyridine derivatives as kinase inhibitors 失效
标题翻译：咪唑并吡啶衍生物作为激酶抑制剂
公开(公告)号：US07348339B2
公开(公告)日：2008-03-25
申请号：US10508760
申请日：2003-03-21
申请人： Nicholas Bailey , Mark James Bamford , Haifeng Cui , Stephen Garland , Krista B Goodman , Mark A Hilfiker , Dennis Lee , Terence Aaron Panchal , Robert A Stavenger , David Matthew Wilson , Jason Witherington
发明人： Nicholas Bailey , Mark James Bamford , Haifeng Cui , Stephen Garland , Krista B Goodman , Mark A Hilfiker , Dennis Lee , Terence Aaron Panchal , Robert A Stavenger , David Matthew Wilson , Jason Witherington
IPC分类号： A61K31/44 , A01N43/42 , C07D265/30 , C07D295/00 , C07D498/02
CPC分类号： C07D471/04
摘要： A compound of the formula and physiologically acceptable salts and or N-oxides thereof wherein, X1 is N or CR3; X2 is N or CR4; X3 is N or CR5; X4 is N or CR6. with the proviso that at least one but not more than two of X1, X2, X3 and X4 represents N. R1 is a 5-, or 6-membered heterocyclic group selected from group a, b, c or d wherein X5 is a group selected from N or CR7 and X6 is a group selected from O, S or NR8; X7 and X8 which may be the same or different is a group selected from N or CR9; X9 is a group selected from O, S or NR8 and X10 is N or CR10; X11, X12 and X13 may be the same or different and selected from a group N or CR11; processes for their preparation, pharmaceutical compositions containing them and their use in medicine.
摘要翻译：下式的化合物及其生理上可接受的盐和/或其N-氧化物，其中X 1是N或CR 3; X 2是N或CR 4; X 3是N或CR 5; X 4是N或CR 6。条件是X 1，X 2，X 3和X 4中的至少一个但不多于两个， SUB>表示N. R 1是选自a，b，c或d的5-或6-元杂环基，其中X 5是选自 N或CR 7和X 6是选自O，S或NR 8的基团; X 7和X 8可以相同或不同，是选自N或CR 9的基团。 X 9是选自O，S或NR 8和X 10的基团是N或CR 10; X 11，X 12和X 13可以相同或不同，并且选自N或C 11 ; 其制备方法，含有它们的药物组合物及其在医药中的用途。

3. 发明授权

US07547779B2 Preparation of 1,6-disubstituted azabenzimidazoles as kinase inhibitors 有权
标题翻译：制备1,6-二取代的氮杂苯并咪唑作为激酶抑制剂
公开(公告)号：US07547779B2
公开(公告)日：2009-06-16
申请号：US10574676
申请日：2004-10-06
申请人： Dennis Lee , Robert A. Stavenger , Krista B. Goodman , Mark A. Hilfiker , Haifeng Cui , Andrew Q. Viet , Joseph P. Marino
发明人： Dennis Lee , Robert A. Stavenger , Krista B. Goodman , Mark A. Hilfiker , Haifeng Cui , Andrew Q. Viet , Joseph P. Marino
IPC分类号： C07D413/00 , C07D401/00 , C07D471/02 , C07D491/02
CPC分类号： C07D471/04
摘要： Novel inhibitors of Rho-kinases are disclosed.
摘要翻译：公开了Rho激酶的新型抑制剂。

4. 发明申请

US20080293716A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20080293716A1
公开(公告)日：2008-11-27
申请号：US10597475
申请日：2005-01-28
申请人： David Harold Drewry , Robert Neil Hunter, III , David Kendall Jung , James Andrew Linn , Clark Sehon , Robert A. Stavenger
发明人： David Harold Drewry , Robert Neil Hunter, III , David Kendall Jung , James Andrew Linn , Clark Sehon , Robert A. Stavenger
IPC分类号： A61K31/5377 , C07D409/04 , A61K31/4436 , C07D413/14
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14 , C07D471/10
摘要： There is provided a compound of Formula (I) or a salt, solvate, or physiologically functional derivative thereof:
摘要翻译：提供式（I）化合物或其盐，溶剂合物或生理功能衍生物：

5. 发明授权

US07365085B2 Compounds and methods 有权
标题翻译：化合物和方法
公开(公告)号：US07365085B2
公开(公告)日：2008-04-29
申请号：US10508894
申请日：2003-03-26
申请人： Ajita Bhat , John Jeffrey McAtee , Scott K. Thompson , James S. Frazee , Lara S. Kallander , Chun Ma , Joseph Marino , Michael J. Neeb , Robert A. Stavenger
发明人： Ajita Bhat , John Jeffrey McAtee , Scott K. Thompson , James S. Frazee , Lara S. Kallander , Chun Ma , Joseph Marino , Michael J. Neeb , Robert A. Stavenger
IPC分类号： A01N43/40 , A01N43/64 , A01N43/08 , A61K31/44 , A61K31/41
CPC分类号： C07C311/29 , C07C217/18 , C07C217/20 , C07C217/22 , C07C217/36 , C07C219/22 , C07C229/34 , C07C233/25 , C07C271/28 , C07C275/34 , C07C291/02 , C07C309/73 , C07C311/08 , C07C311/09 , C07C311/21 , C07C323/32 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D211/34 , C07D211/60 , C07D213/38 , C07D213/64 , C07D213/74 , C07D231/14 , C07D233/64 , C07D239/42 , C07D249/08 , C07D257/04 , C07D295/096 , C07D295/125 , C07D295/185 , C07D307/66 , C07D307/68 , C07D317/58 , C07D317/68 , C07D319/18 , C07D333/20
摘要： Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.
摘要翻译：公开了具有下式的化合物：其药学上可接受的盐或溶剂化物和含有该化合物的药物组合物，其中结构变量如本文所定义。本发明的化合物，盐和溶剂化物可用作LXR激动剂。

6. 发明申请

US20080275062A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20080275062A1
公开(公告)日：2008-11-06
申请号：US10597473
申请日：2005-01-28
申请人： David Harold Drewry , David Kendall Jung , James Andrew Linn , Robert Neil Hunter , Dennis Lee , Robert A. Stavenger , Clark Sehon
发明人： David Harold Drewry , David Kendall Jung , James Andrew Linn , Robert Neil Hunter , Dennis Lee , Robert A. Stavenger , Clark Sehon
IPC分类号： A61K31/4409 , C07D213/04 , A61K31/415 , C07D231/10 , C07D239/42 , A61K31/505 , C07D239/24 , C07D231/56 , C07D401/10
CPC分类号： C07D213/56 , C07D231/12 , C07D231/56 , C07D239/26 , C07D239/42 , C07D403/04
摘要： There is provided compounds of Formula (I) and salts, solvates, and physiologically functional derivatives thereof: wherein R1 is hydrogen or C1-6alkyl; n is 1, 2, 3 or 4; R2 is aryl, optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, C1-4alkyl, C1-4alkoxy, C1-4alkanoyl, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy, C1-4alkoxycarbonyl, C1-4alkylsulfonyl and a group R3R4NSO2 (wherein R3 and R4 are independently hydrogen or C1-4alkyl) and a 5- or 6-membered heteroaryl group; or n is 0 and R1 and R2, together with the nitrogen atom to which they are joined, form a 5- or 6-membered monocyclic heterocyclic ring or a 9- or 10-membered bicyclic heterocyclic ring wherein at least the ring which contains the nitrogen atom to which R1 and R2 are joined is non-aromatic, and wherein the 5- or 6-membered monocyclic heterocyclic ring or the 9- or 10-membered bicyclic heterocyclic ring is optionally substituted by one or two groups selected from the group consisting of halogen, hydroxy, cyano, oxo, C1-4alkyl, C1-4alkanoyl, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy, aryl, aryloxy and C1-4alkoxycarbonyl; and X is indazolyl, pyrazolyl or a group: wherein G is CH or N; and Y1 and Y2 are independently hydrogen, halogen and a group NR5R6 (wherein R5 and R6 are independently hydrogen, C1-6alkyl or C2-6alkenyl).
摘要翻译：提供式（I）化合物及其盐，溶剂化物和生理功能衍生物：其中R1是氢或C 1-6烷基; n为1,2,3或4; R2是芳基，任选地被一个或两个选自卤素，羟基，氰基，C 1-4烷基，C 1-4烷氧基，C 1-4烷基，烷基，卤代C 1-4烷基，卤代C 1-4烷氧基，芳基，芳氧基，C 1-4烷基，烷氧基羰基，C 1-4烷基磺酰基和基团R 3 R 4 NSO 2（其中R 3和R 4独立地是氢或C 1-4烷基）和5-或6-元杂芳基; 或n为0，并且R 1和R 2与它们连接的氮原子一起形成5-或6-元单环杂环或9-或10-元双环杂环，其中至少含有 R 1和R 2连接的氮原子是非芳族的，其中5或6元单环杂环或9或10元双环杂环任选被一个或两个选自以下的基团取代：卤素，羟基，氰基，氧代，C 1-4烷基，C 1-4烷酰基，C 1-4烷氧基，卤代C 1-4烷基，烷基，卤代C 1-4烷氧基，芳基，芳氧基和C 1-4烷氧基羰基; 并且X是吲唑基，吡唑基或基团：其中G是CH或N; 和Y 1和Y 2独立地是氢，卤素和基团NR 5 R 6（其中R 5和R 6独立地是氢，C 1-6烷基或C 2-6烯基）。

7. 发明申请

US20080234261A1 Preparation of 1,6-Disubstituted Azabenzimidazoles as Kinase Inhibitors 有权
标题翻译： 1,6-二取代偶氮苯并咪唑作为激酶抑制剂的制备
公开(公告)号：US20080234261A1
公开(公告)日：2008-09-25
申请号：US10574676
申请日：2004-10-06
申请人： Dennis Lee , Robert A. Stavenger , Krista A. Goodman , Mark A. Hilfiker , Haifeng Cui , Andrew Q. Viet , Joseph P. Marino
发明人： Dennis Lee , Robert A. Stavenger , Krista A. Goodman , Mark A. Hilfiker , Haifeng Cui , Andrew Q. Viet , Joseph P. Marino
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , A61P9/00 , A61K31/496
CPC分类号： C07D471/04
摘要： Novel inhibitors of Rho-kinases are disclosed.
摘要翻译：公开了Rho激酶的新型抑制剂。

8. 发明授权

US07186709B2 Dihydropyrancarboxamides and uses thereof 有权
标题翻译：二氢吡喃甲酰胺及其用途
公开(公告)号：US07186709B2
公开(公告)日：2007-03-06
申请号：US10649532
申请日：2003-08-27
申请人： Stuart L. Schreiber , Robert A. Stavenger , Timothy J. Mitchison , Zoltan Maliga
发明人： Stuart L. Schreiber , Robert A. Stavenger , Timothy J. Mitchison , Zoltan Maliga
IPC分类号： A61K31/351 , A61K31/436 , A61K31/4375 , C07D405/06 , C07D405/08
CPC分类号： C07D471/04 , C07D309/30 , C07D405/04 , C07D405/14 , C07D407/04 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/10
摘要： The present invention provides novel dihydropyrancarboxamide compounds of formula (I): and collections of these compounds, and provides methods for the synthesis of these compounds; wherein R1–R6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.
摘要翻译：本发明提供新的式（I）二氢吡喃甲酰胺化合物：这些化合物的收集，并提供这些化合物的合成方法; 其中R 1〜R 6如本文所定义。此外，本发明提供了用于治疗诸如增殖性疾病和癌症等疾病的药物组合物和方法。

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