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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

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）。

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

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。 >

5. 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。

6. 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。

7. 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。

8. 发明申请

WO2007002325A1 PYRROLO[2,3-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：吡咯并[2,3-B]吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007002325A1
公开(公告)日：2007-01-04
申请号：PCT/US2006/024361
申请日：2006-06-21
申请人： PLEXXIKON, INC. , IBRAHIM, Prahbha, N. , ARTIS, Dean, R. , BREMER, Ryan , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxiam , ZHU, Hongyao , SHI, Shenghua
发明人： IBRAHIM, Prahbha, N. , ARTIS, Dean, R. , BREMER, Ryan , MAMO, Shumeye , NESPI, Marika , ZHANG, Chao , ZHANG, Jiazhong , ZHU, Yong-Liang , TSAI, James , HIRTH, Klaus-Peter , BOLLAG, Gideon , SPEVAK, Wayne , CHO, Hanna , GILLETTE, Samuel, J. , WU, Guoxiam , 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.
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。

9. 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.

10. 发明申请

WO2009143018A2 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：WO2009143018A2
公开(公告)日：2009-11-26
申请号：PCT/US2009/044151
申请日：2009-05-15
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha, N. , BREMER, Ryan , ZHANG, Jiazhong , NESPI, Marika , CHO, Hanna
发明人： IBRAHIM, Prabha, N. , BREMER, Ryan , ZHANG, Jiazhong , NESPI, Marika , CHO, Hanna
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P29/00 , A61P35/00 , A61P31/12
CPC分类号： C07D487/04 , A61K31/519
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 of Fms protein kinase or Kit protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinases and/or Kit protein kinases, including rheumatoid arthiritis, osteoarthritis, osteoporosis, peri-prosthetic osteolysis, systemic sclerosis, demyelinating disorders, multiple sclerosis, Charcot Marie Tooth syndrome, amyotrophic lateral sclerosis, Alzheimer's disease, Parkinson's disease, ulcerative colitis, Crohn's disease, immune thrombocytopenic purpura, myelopreparation for autologous transplantation, transplant rejection, nephritis, nephropathy, type I diabetes, acute pain, inflammatory pain, neuropathic pain, breast cancer, prostate cancer, pancreatic cancer, lung cancer, ovarian cancer, gliomas, glioblastomas, neurofibromatosis, osteolytic bone metastases, and giant cell tumors.
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Fms蛋白激酶或Kit蛋白激酶中的至少一种上是有活性的。还描述了其用于治疗疾病和病症的方法，包括与Fms蛋白激酶和/或Kit蛋白激酶（包括类风湿性关节炎，骨关节炎，骨质疏松症，骨质疏松症，系统性硬化症，脱髓鞘疾病，多发性硬化症，Charcot玛丽牙综合征，肌萎缩性侧索硬化，阿尔茨海默病，帕金森病，溃疡性结肠炎，克罗恩病，免疫性血小板减少性紫癜，自体移植用骨髓制剂，移植排斥，肾炎，肾病，I型糖尿病，急性疼痛，神经性疼痛，乳腺癌，前列腺癌，胰腺癌，肺癌，卵巢癌，神经胶质瘤，成胶质细胞瘤，神经纤维瘤病，溶骨性骨转移和巨细胞肿瘤。

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