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1. 发明授权

US08673928B2 Compounds and methods for kinase modulation, and indications therefor 有权
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：US08673928B2
公开(公告)日：2014-03-18
申请号：US12949741
申请日：2010-11-18
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Chao Zhang , Ying Zhang
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Chao Zhang , Ying Zhang
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P25/16 , A61P35/00 , A61P37/06 , A61P31/18
CPC分类号： C07D487/04 , A61K31/437 , A61K31/519 , A61K31/5377 , C07D401/04 , C07D403/04 , C07D471/04
摘要： and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds of Formula (I) 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：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，所述式（I）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。

2. 发明申请

US20140128373A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20140128373A1
公开(公告)日：2014-05-08
申请号：US13820734
申请日：2012-02-01
申请人： Prabha N. Ibrahim , Chao Zhang , Wayne Spevak , Jiazhong Zhang , Guoxian Wu , Jack Lin , Hanna Cho , Marika Nespi , Songyuan Shi , Todd Ewing , Ying Zhang
发明人： Prabha N. Ibrahim , Chao Zhang , Wayne Spevak , Jiazhong Zhang , Guoxian Wu , Jack Lin , Hanna Cho , Marika Nespi , Songyuan Shi , Todd Ewing , Ying Zhang
IPC分类号： C07D471/04 , A61K31/506 , A61K31/437 , A61K31/5377
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

US20110152258A1 Compounds and Methods for Kinase Modulation, and Indications Therefor 有权
标题翻译：化合物和激酶调节方法及其适应症
公开(公告)号：US20110152258A1
公开(公告)日：2011-06-23
申请号：US12949741
申请日：2010-11-18
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Chao Zhang , Ying Zhang
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Chao Zhang , Ying Zhang
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , C07D413/14 , C07D471/04 , A61K31/437 , A61P9/00 , A61P35/00 , A61P25/28 , A61P1/16 , A61P25/16 , A61P13/12 , A61P29/00 , A61P21/00
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。

4. 发明授权

US08268858B2 Compounds and methods for kinase modulation, and indications therefor 有权
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：US08268858B2
公开(公告)日：2012-09-18
申请号：US11961901
申请日：2007-12-20
申请人： Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
发明人： Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
IPC分类号： A61K31/437 , C07D471/04
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。

5. 发明申请

US20080188514A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
公开(公告)号：US20080188514A1
公开(公告)日：2008-08-07
申请号：US11961901
申请日：2007-12-20
申请人： Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
发明人： Guoxian Wu , Wayne Spevak , Songyuan Shi , Hanna Cho , Prabha N. Ibrahim , Chao Zhang , Shenghua Shi , Yong Zhou , Dean Artis , Jiazhong Zhang
IPC分类号： A61K31/437 , C07D471/04 , A61P9/00 , A61P25/28 , A61P25/16 , A61P25/00 , A61P35/00 , A61P35/02
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.

6. 发明申请

US20120122860A1 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：US20120122860A1
公开(公告)日：2012-05-17
申请号：US13318760
申请日：2010-05-04
申请人： Gary Conard Visor , Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
发明人： Gary Conard Visor , Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
IPC分类号： A61K31/538 , A61K31/437 , A61K31/506 , A61P13/12 , A61K31/496 , C07D495/04 , A61P35/00 , A61P29/00 , C07D471/04 , A61K31/5377
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. 发明授权

US08198273B2 Compounds and methods for kinase modulation, and indications therefor 有权
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：US08198273B2
公开(公告)日：2012-06-12
申请号：US12773798
申请日：2010-05-04
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
IPC分类号： A61K31/5377 , A61K31/437 , A61K31/506 , C07D471/04 , A61P35/00
CPC分类号： 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, 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：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蛋白激酶中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

US20090286783A1 COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR 有权
标题翻译：化合物及其调节方法及其适应症
公开(公告)号：US20090286783A1
公开(公告)日：2009-11-19
申请号：US12467208
申请日：2009-05-15
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi
IPC分类号： A61K31/5377 , C07D487/04 , A61K31/519 , C07D413/02
CPC分类号： C07D487/04
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. 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, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, 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，其衍生物，其衍生物，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，结肠直肠癌，甲状腺癌，卵巢癌，胆管癌，疼痛或多囊肾病）的活动相关的疾病和病症。

9. 发明申请

US20120245174A1 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：US20120245174A1
公开(公告)日：2012-09-27
申请号：US13491480
申请日：2012-06-07
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi , Guoxian Wu
IPC分类号： A61K31/437 , A61P35/00 , A61K31/444 , A61K31/5377 , C07D471/04 , A61K31/506
CPC分类号： 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, 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：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蛋白激酶中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。

10. 发明授权

US08153641B2 Compounds and methods for kinase modulation, and indications therefor 有权
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：US08153641B2
公开(公告)日：2012-04-10
申请号：US12467208
申请日：2009-05-15
申请人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi
发明人： Prabha N. Ibrahim , Wayne Spevak , Hanna Cho , Songyuan Shi
IPC分类号： A01N43/90 , A61K31/519 , C07D487/00
CPC分类号： C07D487/04
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. 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, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, 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，其衍生物，其衍生物，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，结肠直肠癌，甲状腺癌，卵巢癌，胆管癌，疼痛或多囊肾病）的活动相关的疾病和病症。

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