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1. 发明申请

WO2011087776A1 ISOINDOLINONE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE 审中-公开
标题翻译：羟色胺酮激素抑制剂3-激酶
公开(公告)号：WO2011087776A1
公开(公告)日：2011-07-21
申请号：PCT/US2010/061484
申请日：2010-12-21
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ARONOV, Alex , COME, Jon, H. , DAVIES, Robert, J. , PIERCE, Albert, C. , WANG, Jian , NANTHAKUMAR, Suganthini , CAO, Jingrong , BANDARAGE, Upul, K. , KRUEGER, Elaine , TIRAN, Amaud, Le , LIAO, Yusheng , MESSERSMITH, David , COLLIER, Philip, N. , GREY, Ronald , O'DOWD, Hardwin , HENDERSON, James, A. , GRILLOT, Anne-Laure
发明人： ARONOV, Alex , COME, Jon, H. , DAVIES, Robert, J. , PIERCE, Albert, C. , WANG, Jian , NANTHAKUMAR, Suganthini , CAO, Jingrong , BANDARAGE, Upul, K. , KRUEGER, Elaine , TIRAN, Amaud, Le , LIAO, Yusheng , MESSERSMITH, David , COLLIER, Philip, N. , GREY, Ronald , O'DOWD, Hardwin , HENDERSON, James, A. , GRILLOT, Anne-Laure
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/20 , C07D491/20 , A61K31/352 , A61K31/424 , A61K31/429 , A61P9/00 , A61P29/00 , A61P37/00
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14 , C07D405/14 , C07D417/14 , C07D471/04 , C07D471/20 , C07D491/20
摘要： The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作PI3K抑制剂，特别是PI3Kα的化合物。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

2. 发明申请

WO2006071644A1 SELECTIVE INHIBITORS OF ERK PROTEIN KINASE AND USES THEROF 审中-公开
标题翻译： ERK蛋白激酶的选择性抑制剂及其用途
公开(公告)号：WO2006071644A1
公开(公告)日：2006-07-06
申请号：PCT/US2005/046177
申请日：2005-12-20
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ARONOV, Alex , HALE, Michael, R. , MALTAIS, François , MARTINEZ-BOTELLA, Gabriel , STRAUB, Judith , TANG, Qing
发明人： ARONOV, Alex , HALE, Michael, R. , MALTAIS, François , MARTINEZ-BOTELLA, Gabriel , STRAUB, Judith , TANG, Qing
IPC分类号： C07D403/04 , A61K31/506 , A61P35/00
CPC分类号： C07D403/04
摘要： Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferate disorders such as cancer.
摘要翻译：本文描述的是可用作ERK2抑制剂的化合物。这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

3. 发明申请

WO2005040345A3 4-AZOLE SUBSTITUTED IMIDAZOLE COMPOSITIONS USEFUL AS INHIBITORS OR C-MET RECEPTOR TYROSINE KINASE 审中-公开
标题翻译：作为抑制剂或C-MET受体酪氨酸激酶的4-AZO取代的咪唑组合物
公开(公告)号：WO2005040345A3
公开(公告)日：2005-08-18
申请号：PCT/US2004031401
申请日：2004-09-24
申请人： VERTEX PHARMA , ARONOV ALEX , LAUFFER DAVID J , LI PAN , TOMLINSON RONALD C
发明人： ARONOV ALEX , LAUFFER DAVID J , LI PAN , TOMLINSON RONALD C
IPC分类号： A61K31/4178 , A61K31/4196 , A61K31/42 , C07D233/90 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04 , C07D413/14 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/422 , A61P3/08 , A61P9/00 , A61P29/00 , A61P31/12
CPC分类号： C07D405/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders. Formula (I) where Q is C1-6 alkylidene chain wherein one methylene unit of Q is replaced by -C(O)N(R)-, -C(O)-, -C(O)O-, -N(R)-, -O-, -S-, -SO2-, or -SO2N(R)-; each R is independently hydrogen or an optionally substituted C1-6 aliphatic group, wherein: two R groups on the same nitrogen atom are optionally taken together with said nitrogen atom to form an optionally substituted 3-7 membered saturated, partially unsaturated, of fully unsaturated ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R is H, -N(R)2, or an optionally substituted ring selected from a 3-7 membered saturated or partially unsaturated ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur; a 5-6 membered aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or an 8-10 membered bicyclic partially unsaturated or aryl ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; R is an optionally substituted 6-membered aryl ring having 0-3 nitrogens; R is R, CN, NO2, halogen, N(R)2, OR, or SR; and Ring A is an optionally substituted ring selected from formulas (a), (b), (c), (d), (e), (f), (g), (h), (i), (j), (k), (l), (m), (n), (o) or (p).
摘要翻译：本发明涉及可用于蛋白激酶抑制剂的化合物。本发明还提供了制备本发明化合物的方法，包含本发明化合物的药学上可接受的组合物，以及使用该组合物治疗各种疾病的方法。式（I）其中Q是C 1-6亚烷基链，其中Q的一个亚甲基单元被-C（O）N（R） - ， - C（O） - ， - C（O）（R） - ， - O - ， - S - ， - SO 2 - 或-SO 2 N（R） - ; 每个R独立地为氢或任选取代的C 1-6脂族基团，其中：相同氮原子上的两个R基团任选与所述氮原子一起形成任选取代的3-7元饱和，部分不饱和的完全不饱和的具有1-3个独立地选自氮，氧或硫的杂原子的环; R 1是H，-N（R）2或任选取代的环，其选自具有0-3个独立地选自氮，氧或硫的杂原子的3-7元饱和或部分不饱和的环; 具有0-4个独立地选自氮，氧或硫的杂原子的5-6元芳环; 或具有0-4个独立地选自氮，氧或硫的杂原子的8-10元双环部分不饱和或芳环; R 2是具有0-3个氮的任选取代的6元芳环; R 3是R，CN，NO 2，卤素，N（R）2，OR或SR; 环A是选自式（a），（b），（c），（d），（e），（f），（g），（h），（i），（j），（k），（l），（m），（n），（o）或（p）。

4. 发明申请

WO2005068468A2 HETEROCYCLIC PROTEIN KINASE INHIBITORS AND USES THEREOF 审中-公开
标题翻译：杂环蛋白激酶抑制剂及其用途
公开(公告)号：WO2005068468A2
公开(公告)日：2005-07-28
申请号：PCT/US2004/040422
申请日：2004-12-02
申请人： VERTEX PHARMACEUTICALS, INC. , STRAUB, Judith , HALE, Michael, R. , MALTAIS, François , MARTINEZ-BOTELLA, Gabriel , ARONOV, Alex , BEMIS, Guy, W.
发明人： STRAUB, Judith , HALE, Michael, R. , MALTAIS, François , MARTINEZ-BOTELLA, Gabriel , ARONOV, Alex , BEMIS, Guy, W.
IPC分类号： C07D487/08
CPC分类号： C07D239/48 , A61K31/506 , A61K45/06 , C07D251/18 , C07D401/04 , C07D403/04 , C07D405/04 , A61K2300/00
摘要： Described herein are compounds that are useful as protein kinase inhibitors of formula (I) or a pharmaceutically acceptable salt thereof, wherein Ring B, Z 1 , Z 2 , U, p, Q, R 1 , R 2 , R 3 , and R 3 are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including stroke, inflammatory disorders, autoimmune diseases such as SLE lupus and psoriasis, proliferative disorders such as cancer, and conditions associated with organ transplantation.
摘要翻译：本文描述的是可用作式（I）的蛋白激酶抑制剂或其药学上可接受的盐的化合物，其中环B，Z 1，Z 2 U，p，Q，R 1，R 2，R 3和R 3分别代表 >如本文所定义。这些化合物及其药学上可接受的组合物可用于治疗或减轻各种疾病的严重程度，包括中风，炎性疾病，自身免疫疾病如SLE红斑狼疮和牛皮癣，增殖性疾病如癌症和与器官移植相关的病症

5. 发明申请

WO2010096389A1 TETRAHYDROTHIAZOLOPYRIDINE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE 审中-公开
标题翻译：磷脂酰肌醇三激酶的四氢吡咯并吡啶抑制剂
公开(公告)号：WO2010096389A1
公开(公告)日：2010-08-26
申请号：PCT/US2010/024323
申请日：2010-02-16
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ARONOV, Alex , BANDARAGE, Upul, Keerthi , COTTRELL, Kevin , DAVIES, Robert , KRUEGER, Elaine , LEDEBOER, Mark , LEDFORD, Brian , LE TIRAN, Arnaud , LIAO, Yusheng , MESSERSMITH, David , WANG, Tiansheng , XU, Jinwang
发明人： ARONOV, Alex , BANDARAGE, Upul, Keerthi , COTTRELL, Kevin , DAVIES, Robert , KRUEGER, Elaine , LEDEBOER, Mark , LEDFORD, Brian , LE TIRAN, Arnaud , LIAO, Yusheng , MESSERSMITH, David , WANG, Tiansheng , XU, Jinwang
IPC分类号： C07D513/04 , A61K31/4365 , A61P25/00
CPC分类号： C07D513/04
摘要： The present invention relates to compounds (I) useful as inhibitors of PBK, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用作PBK抑制剂，特别是PI3Kα的化合物（I）。本发明还提供包含所述化合物的药学上可接受的组合物和使用该组合物治疗各种疾病，病症或病症的方法。

6. 发明申请

WO2006071644A8 SELECTIVE INHIBITORS OF ERK PROTEIN KINASES AND USES THEROF 审中-公开
标题翻译： ERK蛋白激酶的选择性抑制剂及其用途
公开(公告)号：WO2006071644A8
公开(公告)日：2006-08-24
申请号：PCT/US2005046177
申请日：2005-12-20
申请人： VERTEX PHARMA , ARONOV ALEX , HALE MICHAEL R , MALTAIS FRANCOIS , MARTINEZ-BOTELLA GABRIEL , STRAUB JUDITH , TANG QING
发明人： ARONOV ALEX , HALE MICHAEL R , MALTAIS FRANCOIS , MARTINEZ-BOTELLA GABRIEL , STRAUB JUDITH , TANG QING
IPC分类号： C07D403/04 , A61K31/506 , A61P35/00
CPC分类号： C07D403/04
摘要： Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferate disorders such as cancer.
摘要翻译：本文描述的是可用作ERK2抑制剂的化合物。这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

7. 发明申请

WO2006065820A2 INHIBITORS OF ERK PROTEIN KINASE AND USES THEROF 审中-公开
标题翻译： ERK蛋白激酶的抑制剂及其用途
公开(公告)号：WO2006065820A2
公开(公告)日：2006-06-22
申请号：PCT/US2005045079
申请日：2005-12-13
申请人： VERTEX PHARMA , MARTINEZ-BOTELLA GABRIEL , ARONOV ALEX , HALE MICHAEL R , MALTAIS FRANCOIS , STRAUB JUDITH , TANG QING
发明人： MARTINEZ-BOTELLA GABRIEL , ARONOV ALEX , HALE MICHAEL R , MALTAIS FRANCOIS , STRAUB JUDITH , TANG QING
CPC分类号： C07D239/48
摘要： Described herein are compounds that are useful as protein kinase inhibitors of formula (I); or a pharmaceutically acceptable salt thereof, wherein Ring A, Z 1 , Z 2 , U, Q, R 1 , R 2 , and L are as defined herein. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.
摘要翻译：本文描述的是可用作式（I）的蛋白激酶抑制剂的化合物; 或其药学上可接受的盐，其中环A，Z 1，Z 2，U，Q，R 1，R 2，和/或L如本文所定义。这些化合物及其药学上可接受的组合物可用于治疗或减轻各种病症（包括增殖性疾病如癌症）的严重性。

8. 发明申请

WO2005040345A2 IMIDAZOLE COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：咪达唑组合物作为蛋白激酶的抑制剂有用
公开(公告)号：WO2005040345A2
公开(公告)日：2005-05-06
申请号：PCT/US2004/031401
申请日：2004-09-24
申请人： VERTEX PHARMCEUTICALS INCORPORATED , ARONOV, Alex , LAUFFER, David, J. , LI, Pan , TOMLINSON, Ronald, C.
发明人： ARONOV, Alex , LAUFFER, David, J. , LI, Pan , TOMLINSON, Ronald, C.
IPC分类号： C12N
CPC分类号： C07D405/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/04
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides processes for preparing the compounds of this invention, pharmaceutically acceptable compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of various disorders.
摘要翻译：本发明涉及可用于蛋白激酶抑制剂的化合物。本发明还提供了制备本发明化合物的方法，包含本发明化合物的药学上可接受的组合物，以及使用该组合物治疗各种疾病的方法。

9. 发明申请

WO2005028475A2 COMPOSITIONS USEFUL AS INHIBITORS OF PROTEIN KINASES 审中-公开
标题翻译：用作蛋白激酶抑制剂的组合物
公开(公告)号：WO2005028475A2
公开(公告)日：2005-03-31
申请号：PCT/US2004/029094
申请日：2004-09-07
申请人： VERTEX PHARMACEUTICALS INCORPORATED , ARONOV, Alex , LAUFFER, David, J. , LI, Pan , TOMLINSON, Ronald, C.
发明人： ARONOV, Alex , LAUFFER, David, J. , LI, Pan , TOMLINSON, Ronald, C.
IPC分类号： C07D471/00
CPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
摘要翻译：本发明涉及可用于蛋白激酶抑制剂的化合物。本发明还提供了包含所述化合物的药学上可接受的组合物以及使用该组合物治疗各种疾病，病症或障碍的方法。

10. 发明申请

WO2002064586A3 HETEROCYCLIC INHIBITORS OF ERK2 AND USES THEREOF 审中-公开
公开(公告)号：WO2002064586A3
公开(公告)日：2002-08-22
申请号：PCT/US2002/003791
申请日：2002-02-08
申请人： VERTEX PHARMACEUTICALS INCORPORATED , CAO, Jingrong , GREEN, Jeremy , HALE, Michael , MALTAIS, Francois , STRAUB, Judy , TANG, Qing , ARONOV, Alex
发明人： CAO, Jingrong , GREEN, Jeremy , HALE, Michael , MALTAIS, Francois , STRAUB, Judy , TANG, Qing , ARONOV, Alex
IPC分类号： C07D403/04
摘要： Described herein are compounds that are useful as protein kinase inhibitors having the formula (I) wherein Z 1 and Z 2 are each independently nitrogen or CH and Ring A, T m R 1 , QR 2 , U n R 3 , and Sp are as described in the specification. The compounds are especially useful as inhibitors of ERK2 and for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, diabetes, and cardiovascular disease.

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