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1. 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。

2. 发明申请

WO2011079133A2 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 审中-公开
标题翻译：用于激酶调节的化合物和方法及其适应症
公开(公告)号：WO2011079133A2
公开(公告)日：2011-06-30
申请号：PCT/US2010/061601
申请日：2010-12-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha N. , WU, Guoxian , LIN, Jack , SPEVAK, Wayne , CHO, Hanna , EWING, Todd , ZHANG, Chao
发明人： IBRAHIM, Prabha N. , WU, Guoxian , LIN, Jack , SPEVAK, Wayne , CHO, Hanna , EWING, Todd , ZHANG, Chao
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/497 , A61K31/498 , A61K31/506 , A61K31/519 , C07D519/00
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 each of B-Raf, B-Raf V600E and c-Raf-1 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 melanoma, glioma, glioblastoma, pilocytic astrocytoma, liver cancer, biliary tract cancer, cholangiocarcinoma, colorectal cancer, lung cancer, bladder cancer, gallbladder cancer, breast cancer, pancreatic cancer, thyroid cancer, kidney cancer, ovarian cancer, adrenocortical cancer, prostate cancer, gastrointestinal stromal tumors, medullary thyroid cancer, tumor angiogenesis, acute myeloid leukemia, chronic myelomonocytic leukemia, childhood acute lymphoblastic leukemia, plasma cell leukemia, and multiple myeloma.
摘要翻译：描述了化合物及其盐，其制剂，其结合物，其衍生物，其形式及其用途。在某些方面和实施方案中，所述化合物或其盐，其制剂，其缀合物，其衍生物，其形式在B-Raf，B-Raf V600E和c-Raf-1蛋白激酶中均有活性。在某些方面和实施方案中，所述化合物对抑制Ras突变细胞系的增殖具有活性。还描述了用于治疗包括黑素瘤，神经胶质瘤，成胶质细胞瘤，毛细胞性星形细胞瘤，肝癌，胆道癌，胆管癌，结直肠癌，肺癌，膀胱癌，胆囊癌，乳腺癌，胰腺癌，甲状腺癌，肾癌，卵巢癌，肾上腺皮质癌，前列腺癌，胃肠道间质瘤，甲状腺髓样癌，肿瘤血管生成，急性骨髓性白血病，慢性骨髓单核细胞性白血病，儿童急性淋巴细胞白血病，浆细胞白血病和多发性骨髓瘤。 >

3. 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。

4. 发明申请

WO2007002433A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007002433A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024524
申请日：2006-06-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
发明人： IBRAHIM, Prabha, N. , ARTIS, Dean, R. , BREMER, Ryan , HABETS, Gaston , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , ZUCKERMAN, Rebecca , WEST, Brian , SUZUKI, Yoshihisa , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxian , ZHU, Hongyao , SHI, Shenghua
IPC分类号： C07D471/04 , A61K31/435 , C07C49/517 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5377 , C07C37/62 , C07C39/27 , C07C45/00 , C07C45/673 , C07C45/71 , C07C47/565 , C07C47/575 , C07D209/08
摘要： Compounds of formula III which are 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 III).
摘要翻译：描述了对蛋白激酶有活性的式III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III）。

5. 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。

6. 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。

7. 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。

8. 发明申请

WO2007013896A2 COMPOUNDS MODULATING C-KIT AND C-FMS ACTIVITY AND USES THEREFOR 审中-公开
标题翻译：化合物调节C-CIT和C-FMS活性及其用途
公开(公告)号：WO2007013896A2
公开(公告)日：2007-02-01
申请号：PCT/US2006/018726
申请日：2006-05-16
申请人： PLEXXIKON, INC. , ZHANG, Chao , ZHANG, Jiazhong , IBRAHIM, Prabha, N. , HURT, Clarence, R. , ZUCHKERMAN, Rebecca , ARTIS, Dean, R. , BREMER, Ryan , SPEVAK, Wayne , WU, Guoxian , ZHU, Hongyao
发明人： ZHANG, Chao , ZHANG, Jiazhong , IBRAHIM, Prabha, N. , HURT, Clarence, R. , ZUCHKERMAN, Rebecca , ARTIS, Dean, R. , BREMER, Ryan , SPEVAK, Wayne , WU, Guoxian , ZHU, Hongyao
CPC分类号： C07D471/04
摘要： Compounds active on the receptor protein tyrosine kinases c-kit and c-fms are provided herewith. Also provided herewith are compositions useful for treatment of c-kit mediated diseases or condition and c-fms-mediated diseases or condition, and methods for the use thereof.
摘要翻译：本文提供了对受体蛋白酪氨酸激酶c-kit和c-fms有活性的化合物。本文还提供了可用于治疗c-kit介导的疾病或病症和c-fms介导的疾病或病症的组合物及其使用方法。

9. 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。

10. 发明申请

WO2008080001A2 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：WO2008080001A2
公开(公告)日：2008-07-03
申请号：PCT/US2007/088412
申请日：2007-12-20
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha N. , BREMER, Ryan , ZHANG, Chao , ZHANG, Jiazhong , HIRTH, Klaus-Peter , WU, Guoxian , ZHU, Hongyao
发明人： IBRAHIM, Prabha N. , BREMER, Ryan , ZHANG, Chao , ZHANG, Jiazhong , HIRTH, Klaus-Peter , WU, Guoxian , ZHU, Hongyao
IPC分类号： C07D471/04 , A61K31/437 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D471/04
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。

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