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    • 5. 发明申请
    • PYRROLO [2, 3-B] PYRIDINE DERIVATIVES FOR THE INHIBITION OF RAF KINASES
    • PYRROLO [2,3-B]吡啶衍生物用于抑制RAF动物
    • WO2010104945A1
    • 2010-09-16
    • PCT/US2010/026816
    • 2010-03-10
    • PLEXXIKON, INC.IBRAHIM, Prabha N.SPEVAK, WayneCHO, HannaZHU, Hongyao
    • IBRAHIM, Prabha N.SPEVAK, WayneCHO, HannaZHU, Hongyao
    • C07D471/04A61K31/4745A61P13/12A61P35/00
    • C07D471/04A61K31/437
    • 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.
    • 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。
    • 9. 发明申请
    • COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
    • 化合物及其调节方法及其适应症
    • WO2011057022A1
    • 2011-05-12
    • PCT/US2010/055519
    • 2010-11-04
    • PLEXXIKON, INC.ZHANG, JiazhongIBRAHIM, Prabha, N.BREMER, RyanSPEVAK, WayneCHO, Hanna
    • ZHANG, JiazhongIBRAHIM, Prabha, N.BREMER, RyanSPEVAK, WayneCHO, Hanna
    • A01N43/90A61K31/519
    • C07D471/04A61K31/437A61K31/4427A61K31/506C07D401/04C07D401/14
    • 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.
    • 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。