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1. 发明申请

WO2008079903A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES AS KINASE MODULATORS 审中-公开
标题翻译：作为激酶调节剂的吡咯并[2,3-B]吡啶衍生物
公开(公告)号：WO2008079903A1
公开(公告)日：2008-07-03
申请号：PCT/US2007/088231
申请日：2007-12-19
申请人： PLEXXIKON, INC. , SPEVAK, Wayne , CHO, Hanna , IBRAHIM, Prabha, N. , SHI, Shenghua , MAMO, Shumeye , GILLETTE, Sam , ZHU, Hongyao
发明人： SPEVAK, Wayne , CHO, Hanna , IBRAHIM, Prabha, N. , SHI, Shenghua , MAMO, Shumeye , GILLETTE, Sam , ZHU, Hongyao
IPC分类号： C07D471/04 , A61K31/435 , 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：描述了对蛋白激酶具有活性的化合物，以及使用这些化合物治疗与蛋白激酶异常活性有关的疾病和病症的方法。

2. 发明申请

WO2008079906A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES AS KINASE MODULATORS 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶衍生物作为激酶调节剂
公开(公告)号：WO2008079906A1
公开(公告)日：2008-07-03
申请号：PCT/US2007/088237
申请日：2007-12-19
申请人： PLEXXIKON, INC. , SPEVAK, Wayne , CHO, Hanna , IBRAHIM, Prabha N. , SHI, Shenghua , MAMO, Shumeye , GILLETTE, Sam , ZHU, Hongyao
发明人： SPEVAK, Wayne , CHO, Hanna , IBRAHIM, Prabha N. , SHI, Shenghua , MAMO, Shumeye , GILLETTE, Sam , ZHU, Hongyao
IPC分类号： C07D471/04 , A61K31/435 , 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。

3. 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）。

4. 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。

5. 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。

6. 发明申请

WO2010104945A1 PYRROLO [2, 3-B] PYRIDINE DERIVATIVES FOR THE INHIBITION OF RAF KINASES 审中-公开
标题翻译： PYRROLO [2,3-B]吡啶衍生物用于抑制RAF动物
公开(公告)号：WO2010104945A1
公开(公告)日：2010-09-16
申请号：PCT/US2010/026816
申请日：2010-03-10
申请人： PLEXXIKON, INC. , IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , ZHU, Hongyao
发明人： IBRAHIM, Prabha N. , SPEVAK, Wayne , CHO, Hanna , ZHU, Hongyao
IPC分类号： C07D471/04 , A61K31/4745 , A61P13/12 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437
摘要： Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, 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 at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, glioma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer, prostate cancer, and biliary tract cancer.
摘要翻译：丙烷-1-磺酸{2,4-二氟-3- [5-（2-甲氧基 - 嘧啶-5-基）-1H-吡咯并[2,3-b]吡啶-3-羰基] - 苯基} 酰胺，丙烷-1-磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] - 酰胺，丙烷-1-磺酸 [3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2-氟 - 苯基] - 酰胺，N- [3-（5-氰基-1H-吡咯并[ 3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] -2,5-二氟 - 苯磺酰胺，N- [3-（5-氰基-1H-吡咯并[2,3-b] 吡咯-3-羰基）-2,4-二氟 - 苯基] -3-氟 - 苯磺酰胺，吡咯烷-1-磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基） -2,4-二氟 - 苯基] - 酰胺，N，N-二甲基氨基磺酸[3-（5-氰基-1H-吡咯并[2,3-b]吡啶-3-羰基）-2,4-二氟 - 苯基] - 酰胺及其盐，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，所述的化合物或其盐，其制剂，其缀合物，其衍生物及其形式在至少一种Raf蛋白激酶上具有活性。还描述了其用于治疗疾病和病症的方法，包括与Raf蛋白激酶（包括黑素瘤，神经胶质瘤，结肠直肠癌，甲状腺癌，肺癌，卵巢癌，前列腺癌和胆道癌）的活性相关的疾病和病症。

7. 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.

8. 发明申请

WO2011057022A1 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：WO2011057022A1
公开(公告)日：2011-05-12
申请号：PCT/US2010/055519
申请日：2010-11-04
申请人： PLEXXIKON, INC. , ZHANG, Jiazhong , IBRAHIM, Prabha, N. , BREMER, Ryan , SPEVAK, Wayne , CHO, Hanna
发明人： ZHANG, Jiazhong , IBRAHIM, Prabha, N. , BREMER, Ryan , SPEVAK, Wayne , CHO, Hanna
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4427 , A61K31/506 , C07D401/04 , C07D401/14
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, or forms thereof are active on Fms protein kinase, or on Fms and Kit protein kinase, or on Fms and Flt-3 protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Fms protein kinase, Kit protein kinase, or Flt-3 protein kinase including rheumatoid arthiritis, osteoarthritis, multiple sclerosis, Alzheimer's disease, Parkinson's disease, glomerulonephritis, interstitial nephritis, Lupus nephritis, tubular necrosis, diabetic nephropathy, renal hypertrophy, acute myeloid leukemia, melanoma, multiple myeloma, metastatic breast cancer, prostate cancer, pancreatic cancer, neurofibromatosis, brain metastases, and gastrointestinal stromal 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，其衍生物或其形式在Fms蛋白激酶或Fms和Kit蛋白激酶或Fms和Flt-3蛋白激酶上具有活性。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，Kit蛋白激酶或Flt-3蛋白激酶（包括类风湿性关节炎，骨关节炎，多发性硬化症，阿尔茨海默病，帕金森氏病，肾小球性肾炎，间质性肾炎，狼疮性肾炎，肾小管坏死，糖尿病性肾病，肾肥大，急性骨髓性白血病，黑素瘤，多发性骨髓瘤，转移性乳腺癌，前列腺癌，胰腺癌，神经纤维瘤病，脑转移瘤和胃肠道间质瘤。

9. 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。

10. 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。

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