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    • 10. 发明专利
    • AMINOTRIAZOLOPYRIDINES AND THEIR USE AS KINASE INHIBITORS
    • NZ591551A
    • 2011-10-28
    • NZ59155109
    • 2009-09-08
    • SIGNAL PHARM LLC
    • BAHMANYAR SOGOLEBATES R JBLEASE KATECALABRESE ANDREW ANTONYDANIEL THOMAS ORANDELGADO MERCEDESELSNER JANERDMAN PAULFAHR BRUCEFERGUSON GREGORYLEE BRANDENNADOLNY LISAPACKARD GARRICKPAPA PATRICKPLANTEVIN-KRENITSKY VERONIQUERIGGS JENNIFERROHANE PATRICIASANKAR SABITASAPIENZA JOHNSATOH YOSHITAKASLOAN VICTORSTEVENS RANDALLTEHRANI LIDATIKHE JAYASHREETORRES EDUARDOWALLACE ANDREWWHITEFIELD BRANDON WADEZHAO JINGJING
    • A61P35/00A61K31/437A61P5/00A61P9/00A61P19/00A61P25/00A61P29/00C07D471/04
    • Disclosed is a compound of formula (1) e.g. (R)-3 ,3-dimethyl-6-(5-(methyl(tetrahydrofuran-3-yl)amino )-[1,2,4]triazolo[1 ,5-a ]pyridin-2-ylamino)indolin-2-one or a pharmaceutically acceptable salt, tautomer, stereoisomer, or solvate thereof, wherein: R' is an aryl, or a heterocyclyl; R2 is an alkyl, a cycloalkyl, a heterocyclylalkyl, an aralkyl, -NR3R4, -OR3, -C(=O)R5, -C(=O)NR3R4 -NHC(=O)R3, -(CH2)CR6(OR3)R4, or a heterocyclyl selected from azetidinyl, pyrrolidyl, piperidyl, morpholinyl, piperazin-2-onyl,1,2,3,6-tetrahydropyridyl, isoxazolyl, imidazolyl, indazolyl, benzimidazolyl, 1-H-benzo[d][1 ,2,3]triazolyl, benzisoxazolyl, benzo[ d]oxazolyl, isoindolin-lonyl,1H-imidazo[4,5-b ]pyridyl, isoquinolinyl, or quinolyl; or R2 is pyridyl; R3 and R4 are at each occurrence independently -H, an alkyl, anaryl, a heteroaryl, a cycloalkyl, a substituted or a heterocyclyl, an aralkyl, or a heterocyclylalkyl; R5 is alkyl, an aryl, a heteroaryl, a cycloalkyl, a heterocyclyl, an aralkyl, or a heterocyclylalkyl; and R6 is -H, or an alkyl, or together with R4 and the atoms to which they are attached form a heterocyclyl for the treatment of cancer where the cancer is of the head, neck, eye, mouth, throat, esophagus, bronchus, larynx, pharynx, chest, bone, lung, colon, rectum, stomach, prostate, urinary bladder, uterine, cervix, brea$t, ovaries, testicles or other reproductive organs, skin, thyroid, blood, lymph nodes, kidney, liver, pancreas, brain, central nervous system, solid tumors or blood-borne tumors and Behcet's syndrome, a non-allergy mast cell disease, ankylosing spondylitis, osteoarthritis, rheumatoid arthritis, multiple sclerosis, lupus, inflammatory bowel disease, ulcerative colitis, Crohn's disease, myasthenia gravis, Grave's disease, transplant rejection, humoral transplant rejection, non-humoral transplant rejection, cellular transplant rejection, immune thrombocytopenic purpura, idiopathic thrombocytopenic purpura, diabetes, immunological response to bacterial, parasitic, helminth infestation or viral infection, eczema, dermatitis, graft versus host disease, Goodpasture's disease, hemolytic disease of the newborn, autoimmune hemolytic anemia, anti-phospholipid syndrome, ANCA-associated vasculitis, Churg-Strauss syndrome, Wegeners granulomatosus, pemphigus vulgaris, serum sickness, mixed cryoglobulinemia, peripheralneuropathy associated with IgM antibody, microscopic polyangiitis, Hashimoto's thyroiditis,Sjogrens syndrome, a fibrosing condition or primary biliary cirrhosisnon-ANCA vasculitis, psoriasis, asthma, allergic rhinitis, allergic conjunctivitis, chronic urticaria, hives, anaphylaxis, bronchitis, chronic obstructive pUlmonary disease, cystic fibrosis, inflammatory bowel disease, irritable bowel syndrome, gout, Crohn's disease, mucous colitis, ulcerative colitis, allergy to an intestinal antigen, diabetes or obesity. restenosis, atherosclerosis, stroke, myocardial infarction, ischemic damage Huntington's disease, Alzheimer's disease, or viral or bacterial-associated encephalitis or damage.