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1. 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）。

2. 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：

3. 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。

4. 发明授权

US06720332B2 Oxindole derivatives 失效
标题翻译：羟吲哚衍生物
公开(公告)号：US06720332B2
公开(公告)日：2004-04-13
申请号：US10362744
申请日：2003-02-27
申请人： Scott Howard Dickerson , David Harold Drewry , James Andrew Linn
发明人： Scott Howard Dickerson , David Harold Drewry , James Andrew Linn
IPC分类号： A61K3144
CPC分类号： C07D471/04
摘要： Oxindole derivatives, specifically pyrrolo[3,2-f]quinoline-2-ones, which are useful as CDK4 inhibitors are described herein. The described invention also includes methods of making such oxindole derivatives as well as methods of using the same in the treatment of hyperproliferative diseases.
摘要翻译：本文描述了可用作CDK4抑制剂的羟吲哚衍生物，特别是吡咯并[3,2-f]喹啉-2-酮。所述的发明还包括制备这种羟吲哚衍生物的方法及其用于治疗过度增殖性疾病的方法。

5. 发明申请

US20080194561A1 Compounds 审中-公开
标题翻译：化合物
公开(公告)号：US20080194561A1
公开(公告)日：2008-08-14
申请号：US11996749
申请日：2006-07-13
申请人： Jerry Leroy Adams , David Harold Drewry , James Andrew Linn
发明人： Jerry Leroy Adams , David Harold Drewry , James Andrew Linn
IPC分类号： A61K31/5377 , C07D409/04 , C07D413/14 , A61P35/00 , C07D409/14 , A61K31/506
CPC分类号： C07D409/04 , C07D409/14 , C07D417/14
摘要： A compound of formula (I): compositions and medicaments containing the same as well as processes for the preparation and use of such compounds, compositions and medicaments, particularly in diseases associated with inappropriate Aurora activity.
摘要翻译：式（I）的化合物：包含其的组合物和药物以及用于制备和使用这些化合物，组合物和药物的方法，特别是在与不适当的Aurora活性相关的疾病中。

6. 发明申请

US20080269298A1 Benzimidazol-1-YL-thiophene compounds for the treatment of cancer 审中-公开
标题翻译：苯并咪唑-1-YL-噻吩化合物用于治疗癌症
公开(公告)号：US20080269298A1
公开(公告)日：2008-10-30
申请号：US12113224
申请日：2008-05-01
申请人： Clarence W. Andrews , Mui Cheung , Ronda G. Davis-Ward , David Harold Drewry , Kyle Allen Emmitte , Robert Dale Hubbard , Kevin W. Kuntz , James Andrew Linn , Robert Anthony Mook , Gary Keith Smith , James Marvin Veal
发明人： Clarence W. Andrews , Mui Cheung , Ronda G. Davis-Ward , David Harold Drewry , Kyle Allen Emmitte , Robert Dale Hubbard , Kevin W. Kuntz , James Andrew Linn , Robert Anthony Mook , Gary Keith Smith , James Marvin Veal
IPC分类号： A61K31/4184 , A61P35/00 , A61K31/4439 , C07D409/14 , C07D409/04
CPC分类号： C07D491/04 , C07D409/04 , C07D409/14
摘要： The present invention provides compounds of formula (I): pharmaceutical compositions containing the same, processes for preparing the same and their use as pharmaceutical agents.
摘要翻译：本发明提供式（I）化合物：含有该化合物的药物组合物，其制备方法及其作为药剂的用途。

7. 发明申请

US20080058515A1 Chemical Compounds 审中-公开
标题翻译：化学化合物
公开(公告)号：US20080058515A1
公开(公告)日：2008-03-06
申请号：US10566040
申请日：2004-07-23
申请人： David Harold Drewry , James Andrew Linn , James Marvin Veal
发明人： David Harold Drewry , James Andrew Linn , James Marvin Veal
IPC分类号： C07D211/32 , C07D215/00 , C07D231/56 , C07D261/04 , C07D401/00 , C07D403/00 , C07D413/00 , C07D417/00 , C07D471/10
CPC分类号： C07D417/12 , C04B35/632 , C07D231/56 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/10
摘要： Indazolylacrylamide derivatives, which are useful as SGK-1 inhibitors are described herein. The described invention also includes methods of making such indazolylacrylamide derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate SGK-1 activity.
摘要翻译：本文描述了可用作SGK-1抑制剂的吲唑基丙烯酰胺衍生物。所述的发明还包括制备这种吲唑基丙烯酰胺衍生物的方法以及使用该吲唑基丙烯酰胺衍生物的方法来治疗由不适当的SGK-1活性介导的疾病。

8. 发明申请

US20100105674A1 Chemical Compounds 审中-公开
公开(公告)号：US20100105674A1
公开(公告)日：2010-04-29
申请号：US12531763
申请日：2008-03-12
申请人： Felix Deanda Jr. , David Harold Drewry , James Andrew Linn , Paul Reid
发明人： Felix Deanda Jr. , David Harold Drewry , James Andrew Linn , Paul Reid
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14 , C07D413/12 , C07D403/04 , C07D239/48 , C07D403/12 , A61P35/00 , C07D401/12 , A61K31/505
CPC分类号： C07D239/42 , A61K31/505 , C07D239/48 , C07D401/04 , C07D403/12
摘要： The present invention relates to dianilinopyrimidine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such dianilinopyrimidine derivatives are useful in the treatment of diseases associated with inappropriate Wee1 kinase activity.

9. 发明授权

US07329678B2 Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US07329678B2
公开(公告)日：2008-02-12
申请号：US10543701
申请日：2004-01-27
申请人： David Harold Drewry , Robert Neil Hunter, III
发明人： David Harold Drewry , Robert Neil Hunter, III
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D401/04
摘要： Benzimidazolyl-pyridine derivatives, which are useful as SGK-1 inhibitors are described herein. The described invention also includes methods of making such benzimidazolyl-pyridine derivatives as well as methods of using the same in the treatment of diseases mediated by inappropriate SGK-1 activity.
摘要翻译：本文描述了可用作SGK-1抑制剂的苯并咪唑基 - 吡啶衍生物。所述的发明还包括制备这种苯并咪唑基 - 吡啶衍生物的方法以及使用该方法来治疗由不适当的SGK-1活性介导的疾病。

10. 发明授权

US06172064B2 Formamides as therapeutic agents 失效
标题翻译：甲酰胺作为治疗剂
公开(公告)号：US06172064B2
公开(公告)日：2001-01-09
申请号：US09382333
申请日：1999-08-25
申请人： Robert Carl Andrews , Marc Werner Andersen , David John Cowan , David Norman Deaton , Scott Howard Dickerson , David Harold Drewry , Michael David Gaul , Michael Joseph Luzzio , Brian Edward Marron , Michael Howard Rabinowitz
发明人： Robert Carl Andrews , Marc Werner Andersen , David John Cowan , David Norman Deaton , Scott Howard Dickerson , David Harold Drewry , Michael David Gaul , Michael Joseph Luzzio , Brian Edward Marron , Michael Howard Rabinowitz
IPC分类号： C07D21170
CPC分类号： C07D213/40 , C07C259/06 , C07D295/13 , C07D333/24
摘要： A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof. Also described are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine.
摘要翻译：具有通式结构式W的化合物族是反向异羟肟酸基团，R 1，R 2，R 3，R 4，R 5和R 6如说明书中所述，或其药学上可接受的盐，溶剂化物，生物可水解的酯，可生物水解的酰胺，亲和试剂或其前药。还描述了它们的制备方法，包括这些化合物的药物组合物及其在药物中的用途。

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