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1. 发明申请

WO2008079909A1 PYRROLO [2,3-B] PYRIDINES AS KINASE MODULATORS 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶类作为激酶调节剂
公开(公告)号：WO2008079909A1
公开(公告)日：2008-07-03
申请号：PCT/US2007/088243
申请日：2007-12-19
申请人： PLEXXIKON, INC. , WU, Guoxian , SPEVAK, Wayne , SHI, Songyuan , CHO, Hanna , IBRAHIM, Prabha N. , ZHANG, Chao , SHI, Shenghua , ZHOU, Yong , ARTIS, Dean R. , ZHANG, Jiazhong
发明人： WU, Guoxian , SPEVAK, Wayne , SHI, Songyuan , CHO, Hanna , IBRAHIM, Prabha N. , ZHANG, Chao , SHI, Shenghua , ZHOU, Yong , ARTIS, Dean R. , ZHANG, Jiazhong
IPC分类号： A61K31/437 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04 , C07D519/00
摘要： Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

2. 发明申请

WO2012109075A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：WO2012109075A1
公开(公告)日：2012-08-16
申请号：PCT/US2012/023543
申请日：2012-02-01
申请人： PLEXXIKON INC. , IBRAHIM, Prabha N. , ZHANG, Chao , SPEVAK, Wayne , ZHANG, Jiazhong , WU, Guoxian , LIN, Jack , CHO, Hanna , NESPI, Marika , SHI, Songyuan , EWING, Todd , ZHANG, Ying
发明人： IBRAHIM, Prabha N. , ZHANG, Chao , SPEVAK, Wayne , ZHANG, Jiazhong , WU, Guoxian , LIN, Jack , CHO, Hanna , NESPI, Marika , SHI, Songyuan , EWING, Todd , ZHANG, Ying
IPC分类号： A61K31/407
CPC分类号： A61K31/506 , A61K31/437 , A61K31/5377 , C07D471/04
摘要： Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
摘要翻译：描述了对蛋白激酶有活性的化合物，以及制备和使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。

3. 发明申请

WO2010129570A1 SOLID FORMS OF SULFONAMIDES AND AMINO ACIDS 审中-公开
标题翻译：磺酰胺和氨基酸的固体形式
公开(公告)号：WO2010129570A1
公开(公告)日：2010-11-11
申请号：PCT/US2010/033576
申请日：2010-05-04
申请人： PLEXXIKON, INC. , VISOR, Gary Conard , IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
发明人： VISOR, Gary Conard , IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
IPC分类号： C07D213/56 , C07D471/04 , A61K9/16 , A61K47/48 , A61K9/00 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Solid forms of phenyl sulfonamide compounds of formula (I) active on protein kinases, including Raf protein kinases, are described, as well as methods of using such solid forms to treat diseases and conditions associated with activity of protein kinases, e.g. Raf protein kinases, including pain, polycystic kidney disease, melanoma and colorectal cancer.
摘要翻译：描述了对蛋白激酶（包括Raf蛋白激酶）有活性的式（I）的苯基磺酰胺化合物的固体形式，以及使用这些固体形式治疗与蛋白激酶活性相关的疾病和病症的方法，例如， Raf蛋白激酶，包括疼痛，多囊肾病，黑素瘤和结肠直肠癌。

4. 发明申请

WO2010129567A1 PYRROLO [2, 3. B] PYRIDINES WHICH INHIBIT RAF PROTEIN KINASE 审中-公开
标题翻译： PYRROLO [2,3B]抑制RAF蛋白激酶的吡啶
公开(公告)号：WO2010129567A1
公开(公告)日：2010-11-11
申请号：PCT/US2010/033571
申请日：2010-05-04
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
发明人： IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , WU, Guoxian
IPC分类号： C07D471/04 , A61K31/437 , A61P35/02
CPC分类号： C07D471/04
摘要： Compounds (I) and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, and forms thereof are active on each of BRaf and c-Raf -1 protein kinase, and may also be active on either or both of A-Raf and B-Raf V600E protein kinase. Also described are methods of use thereof to treat diseases and conditions, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, and biliary tract cancer.
摘要翻译：描述了化合物（I）及其盐，其制剂，其缀合物，其衍生物，其形式及其用途。在某些方面和实施方案中，所描述的化合物或其盐，其制剂，其缀合物，其衍生物及其形式在BRaf和c-Raf-1蛋白激酶的每一个上都是有活性的，并且还可以在 A-Raf和B-Raf V600E蛋白激酶。还描述了其用于治疗疾病和病症的方法，包括黑素瘤，结肠直肠癌，甲状腺癌，卵巢癌和胆道癌。

5. 发明申请

WO2009012283A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：WO2009012283A1
公开(公告)日：2009-01-22
申请号：PCT/US2008/070124
申请日：2008-07-16
申请人： PLEXXIKON INC. , WU, Guoxian , ZHANG, Jiazhong , ZHU, Yong-Liang , ZHANG, Chao , IBRAHIM, Prabha, N. , SHI, Songyuan , SPEVAK, Wayne , ARTIS, Dean, R. , TSAI, James
发明人： WU, Guoxian , ZHANG, Jiazhong , ZHU, Yong-Liang , ZHANG, Chao , IBRAHIM, Prabha, N. , SHI, Songyuan , SPEVAK, Wayne , ARTIS, Dean, R. , TSAI, James
IPC分类号： C07D213/75 , C07D215/38 , C07D231/40 , C07D261/14 , C07D285/16 , C07D401/12 , C07D407/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D285/135 , A61P35/00
CPC分类号： A61K31/44 , A61K31/415 , A61K31/42 , A61K31/433 , A61K31/437 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/549 , A61K45/06 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/82 , C07D215/12 , C07D215/14 , C07D215/20 , C07D215/38 , C07D231/40 , C07D239/48 , C07D239/49 , C07D261/14 , C07D263/48 , C07D285/135 , C07D285/16 , C07D401/12 , C07D405/12 , C07D409/12 , C07D417/04 , C07D417/12 , C07D471/04 , A61K31/4427 , A61K2300/00
摘要： Compounds of formula I active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases. Formula (I) wherein Ar is optionally substituted heteroaryl; R 2 is hydrogen, lower alkyl or halogen; U is selected from the group consisting of -S(O) 2 -, -C(X)-, -C(X)-N(R 10 )-, and -S(O) 2 -N(R 10 )-; R 3 is optionally substituted lower alkyl, optionally substituted C3.6 cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; and wherein R 1 , R 3 , R 4 , m, L 1 , X R 10 are as described herein.
摘要翻译：描述了对蛋白激酶有活性的式I化合物，以及使用这些化合物治疗与蛋白激酶异常活性相关的疾病和病症的方法。式（I）其中Ar是任选取代的杂芳基; R2是氢，低级烷基或卤素; U选自-S（O）2 - ， - C（X） - ， - C（X）-N（R 10） - 和-S（O）2 -N（R 10） - ; R 3是任选取代的低级烷基，任选取代的C 3-6环烷基，任选取代的杂环烷基，任选取代的芳基或任选取代的杂芳基; 并且其中R 1，R 3，R 4，m，L 1，X R 10如本文所述。

6. 发明申请

WO2009143024A3 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
公开(公告)号：WO2009143024A3
公开(公告)日：2009-11-26
申请号：PCT/US2009/044178
申请日：2009-05-15
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan
发明人： IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P29/00 , A61P35/00 , A61P31/12
摘要： Compounds of Formula (I) which are active of Raf protein kinase and useful to treat melanoma, cancer, pain or polycystic kidney disease.

7. 发明申请

WO2011063159A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：WO2011063159A1
公开(公告)日：2011-05-26
申请号：PCT/US2010/057293
申请日：2010-11-18
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , ZHANG, Chao , ZHANG, Ying
发明人： IBRAHIM, Prabha, N. , SPEVAK, Wayne , CHO, Hanna , SHI, Songyuan , ZHANG, Chao , ZHANG, Ying
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： C07D487/04 , A61K31/437 , A61K31/519 , A61K31/5377 , C07D401/04 , C07D403/04 , C07D471/04
摘要： Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on at least one Raf protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of B-Raf V600E mutant protein kinase, including melanoma, glioma, glioblastoma multiforme, pilocytic astrocytoma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, liver cancer, gallbladder cancer, gastrointestinal stromal tumors, biliary tract cancer, and cholangiocarcinoma. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of c-Raf-1 protein kinase, including acute pain, chronic pain or polycystic kidney disease.
摘要翻译：其化合物及其盐，其制剂，其缀合物，其衍生物，其形式及用途。在某些方面和实施方案中，所述的化合物或其盐，其制剂，其缀合物，其衍生物，其形式在至少一种Raf蛋白激酶上具有活性。在某些方面和实施方案中，所述化合物在抑制Ras突变细胞系的增殖中是有活性的。还描述了其用于治疗疾病和病症的方法，包括与B-Raf V600E突变蛋白激酶（包括黑素瘤，神经胶质瘤，多形性成胶质细胞瘤，纤维细胞性星形细胞瘤，结肠直肠癌，甲状腺癌，肺癌，卵巢）的活动相关的疾病和病症癌症，前列腺癌，肝癌，胆囊癌，胃肠道间质瘤，胆道癌和胆管癌。还描述了其用于治疗疾病和病症的方法，包括与c-Raf-1蛋白激酶的活性相关的疾病和病症，包括急性疼痛，慢性疼痛或多囊肾病。

8. 发明申请

WO2014145051A1 HETEROCYCLIC COMPOUNDS AND USES THEREOF 审中-公开
标题翻译：杂环化合物及其用途
公开(公告)号：WO2014145051A1
公开(公告)日：2014-09-18
申请号：PCT/US2014/029701
申请日：2014-03-14
申请人： ZHANG, Jiazhong , BUELL, John , CHAN, Katrina , IBRAHIM, Prabha, N. , LIN, Jack , PHAM, Phuongly , SHI, Songyuan , SPEVAK, Wayne , WU, Guoxian , WU, Jeffrey
发明人： ZHANG, Jiazhong , BUELL, John , CHAN, Katrina , IBRAHIM, Prabha, N. , LIN, Jack , PHAM, Phuongly , SHI, Songyuan , SPEVAK, Wayne , WU, Guoxian , WU, Jeffrey
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07F9/6561 , A61K31/422 , A61K31/437 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/675 , A61K31/695 , C07D413/04 , C07D413/14 , C07D471/04 , C07F7/10 , Y02A50/411
摘要： Heterocyclic compounds of formula (I), methods for their preparation, pharmaceutical compositions containing such a compound and their therapeutic uses.
摘要翻译：式（I）的杂环化合物，其制备方法，含有这种化合物的药物组合物及其治疗用途。

9. 发明申请

WO2005118601A2 SULFONYLETHYL PHOSPHORODIAMIDATES 审中-公开
标题翻译：用于治疗癌症的磺酰氟磷酰胆碱酯酶
公开(公告)号：WO2005118601A2
公开(公告)日：2005-12-15
申请号：PCT/US2005/017880
申请日：2005-05-20
申请人： TELIK, INC. , ALLEN, David, R. , MA, Wenli , PETERSON, Brian, T. , ROBINSON, Louise , SCHOW, Steven, R. , SHI, Songyuan , SIMON, Reyna, J. , WEBER, Kevin, T. , WICK, Michael, M.
发明人： ALLEN, David, R. , MA, Wenli , PETERSON, Brian, T. , ROBINSON, Louise , SCHOW, Steven, R. , SHI, Songyuan , SIMON, Reyna, J. , WEBER, Kevin, T. , WICK, Michael, M.
IPC分类号： C07F9/00
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/5721 , C07F9/581 , C07F9/582 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译：磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。

10. 发明申请

WO2016191296A1 PLX-8394 OR PLX-7904 FOR USE IN THE TREATMENT OF BRAF-V600-RELATED DISEASES 审中-公开
标题翻译： PLX-8394或PLX-7904用于治疗BRAF-V600相关疾病
公开(公告)号：WO2016191296A1
公开(公告)日：2016-12-01
申请号：PCT/US2016/033587
申请日：2016-05-20
申请人： PLEXXIKON INC.
发明人： IBRAHIM, Prabha N. , ZHANG, Chao , SPEVAK, Wayne , ZHANG, Jiazhong , WU, Guoxian , LIN, Jack , CHO, Hanna , NESPI, Marika , SHI, Songyuan , EWING, Todd , ZHANG, Ying , BOLLAG, Gideon
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/506 , A61K31/519 , A61K45/06
摘要： The present disclosure provides methods of treating a subject suffering from or at risk of a BRAF V600 mutation or BRAF fusion mutation related disease or condition, without activating the MAPK pathway or inducing expression of MAPK pathway genes in cells harboring wild-type BRAF.
摘要翻译：本公开提供了治疗患有或处于BRAF V600突变或BRAF融合突变相关疾病或病症风险的受试者的方法，而不激活MAPK途径或诱导携带野生型BRAF的细胞中MAPK途径基因的表达。

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