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    • 3. 发明申请
    • PROTEIN KINASE INHIBITORS
    • 蛋白激酶抑制剂
    • WO2005120513A1
    • 2005-12-22
    • PCT/CH2005/000321
    • 2005-06-09
    • ESBATECH AGBERSET, CatherineAUDETAT, StephanTIETZ, JuliaGUNDE, TeaBARBERIS, AlcideSCHUMACHER, AndreasTRAXLER, Peter
    • BERSET, CatherineAUDETAT, StephanTIETZ, JuliaGUNDE, TeaBARBERIS, AlcideSCHUMACHER, AndreasTRAXLER, Peter
    • A61K31/519
    • A61K31/519A61K31/695
    • The present invention relates to the use of compounds for the treatment of disorders involving a protein kinase, preferably a tyrosine kinase. The compounds e.g. have the general formula (I) wherein R 1 , R 2 and R 4 are independently selected from hydrogen, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, NR 6 R 7 , OR 6 , SR 6 , (CH) m R 6 R 7 , wherein R 6 and R 7 are independently selected from hydrogen, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl, optionally substituted 5- or 6- membered heterocycle, (CH 2 ) n CO(O)R 8 , (CH 2 ) m R' where n = 0, 1, 2, 3, 4 and wherein R 8 is hydrogen, C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl and wherein R' is selected from hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, optionally substituted aryl, halogen, hydroxyl, NO 2 , NH 2 , SO 2 NH 2 , cyano and m is 0, 1, 2, 3, 4; R 3 is hydroxyl, halogen, NH 2 , NO 2 , cyano, SH, optionally substituted C 1 -C 6 alkyl, optionally substituted C 3 -C 8 cycloalkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heterocycle, R 5 is selected from C 1 -C 6 alkyl, hydrogen, alkoxy, NH 2 , halogen, cyano, alkine, COOR'' wherein R'' is selected from hydrogen, C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl.
    • 本发明涉及化合物用于治疗涉及蛋白激酶,优选酪氨酸激酶的病症的用途。 化合物例如 具有通式(I)其中R 1,R 2和R 4独立地选自氢,任选取代的C 1 -C 6烷基,任选取代的C 3 -C 8环烷基,NR 6 R 7,OR 6,SR 6,(CH)m R 6 R 7,其中R 6和R 7独立地 选自氢,任选取代的C 3 -C 8环烷基,任选取代的芳基,任选取代的5-或6-元杂环,(CH 2)n CO(O)R 8,(CH 2)m R',其中n = 0,1,2,3, 4,并且其中R 8是氢,C 1 -C 6烷基,任选取代的C 3 -C 8环烷基,任选取代的芳基,并且其中R'选自氢,C 1 -C 6烷基,C 1 -C 6烷氧基,任选取代的芳基,卤素,羟基,NO 2 ,NH2,SO2NH2,氰基和m是0,1,2,3,4; R3是羟基,卤素,NH2,NO2,氰基,SH,任选取代的C 1 -C 6烷基,任选取代的C 3 -C 8环烷基,任选取代的芳基,任选取代的5-或6-元杂环,R 5选自C 1 -C 6烷基 ,氢,烷氧基,NH 2,卤素,氰基,烷基,COOR“,其中R”选自氢,C 1 -C 6烷基,C 3 -C 8环烷基。
    • 4. 发明申请
    • PHENYL-SUBSTITUTED BICYCLIC HETEROCYCLYL DERIVATIVES AND THEIR USE
    • 苯基取代的双环杂环衍生物及其用途
    • WO1998017662A1
    • 1998-04-30
    • PCT/EP1997005697
    • 1997-10-16
    • NOVARTIS AGTRAXLER, PeterSEQUIN, UrsGREEN, Jennifer, MaryFURET, Pascal
    • NOVARTIS AG
    • C07D311/36
    • C07D215/233A61K31/352C07D311/36
    • The invention relates to the use of a compound of formula (I), wherein R1 and R2, independently of each other, represent hydrogen, hydroxy or lower alkoxy, or R1 and R2 together form lower alkylenedioxy; R3 is halogen, lower alkyl, halogen-substituted lower alkyl, hydroxy, phenyloxy, C3-C7-cycloalkyloxy or lower alkoxy; any R4 is, independently of R3 and independently of any other R4 if present, selected from halogen, lower alkyl, halogen-substituted lower alkyl, hydroxy, phenyloxy, C3-C7-cycloalkyloxy or lower alkoxy; X is oxygen, imino or (halogen-substituted or unsubstituted lower alkanoyl, [lower alkyl or carboxy-, lower alkoxycarbonyl-, aminocarbonyl-, N-mono- or N,N-di-lower alkylamino carbonyl]-lower alkyl; or C6-C12-aryl)-substituted imino; and n is 0, 1, 3 or 4; or a salt thereof if at least one salt-forming group is present, in the treatment of certain diseases and the inhibition of protein kinases, as well as to new compounds of formula (I) and salts thereof.
    • 本发明涉及式(I)化合物的用途,其中R 1和R 2彼此独立地表示氢,羟基或低级烷氧基,或者R 1和R 2一起形成低级亚烷基二氧基; R3是卤素,低级烷基,卤素取代的低级烷基,羟基,苯氧基,C3-C7-环烷氧基或低级烷氧基; 任何R 4独立地为R 3,独立地为任何其它R 4(如果存在),选自卤素,低级烷基,卤素取代的低级烷基,羟基,苯氧基,C 3 -C 7 - 环烷氧基或低级烷氧基; X是氧,亚氨基或(卤素取代或未取代的低级烷酰基,[低级烷基或羧基 - ,低级烷氧基羰基 - ,氨基羰基 - ,N-单 - 或N,N-二 - 低级烷基氨基羰基] - 低级烷基;或C6 -C 12 - 芳基) - 取代的亚氨基; n为0,1,3或4; 如果存在至少一种成盐基团,则可以使用它们的盐,以治疗某些疾病和抑制蛋白激酶,以及新的式(I)化合物及其盐。