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    • 2. 发明申请
    • NOVEL CYCLIC UREA DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL USE OF SAME AS KINASE INHIBITORS
    • 新型循环尿素衍生物,其制备方法及其作为激酶抑制剂的药物应用
    • WO2004070050A2
    • 2004-08-19
    • PCT/FR2004000188
    • 2004-01-28
    • AVENTIS PHARMA SA
    • PATEK MARCELNAIR ANILHITTINGER AUGUSTINNEMECEK CONCEPTIONBOND DANIELHARLOW GREGBOUCHARD HERVEMAUGER JACQUESMALLERON JEAN-LUCPALERMO MARKAL-OBEIDI FAHADFAITG THOMASSTROBEL HARTMUTRUF SVENRITTER KURTEL-AHMAD YOUSSEFLESUISSE DOMINIQUEBENARD DIDIER
    • A61P3/00A61P7/02A61P11/06A61P17/06A61P19/02A61P25/00A61P35/00C07D401/06C07D401/14C12Q
    • C07D401/06C07D401/14
    • The invention relates to novel products having formula (I), wherein: p denotes 0 to 2; R and R1 denote O or NH; R2 and R3 denote hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl and heteroaryl, or R2 and R3, together with the carbon atom to which they are bound, form a carbocyclic or heterocyclic radical, all of said radicals being optionally substituted; A1 denotes a single bond, alkyl, allyl and propynyl; Y and Y1 denote H, OCF3, S(O)nCF3, S(O)nAlk, SO2CHF2, SO2CF2CF3, -O-CF2-CHF2, -O-CHF2, -O-CH2-CF3, SF5 and SO2NR5R6, whereby R5 and R6 are selected from among hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, heterocycloalkyl, aryl and heteroaryl, which are optionally substituted, or R5 and R6, together with N to which they are bound, form a heterocyclic radical; A2 denotes Al, CO and SO2; B2 denotes a heterocyclic radical which is optionally substituted with one or more substituents which are selected from the values of Y2; Y2 denotes hydrogen, halogen, hydroxyl, cyano, alkyl, alkoxy, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, -O-alkenyl, -O-alkynyl, O-cycloalkyl, S(O)n-alkyl, -S(O)n-alkenyl, -S(O)n-alkynyl, S(O)n-cycloalkyl, -COOR13,-OCOR13, NR5R6, CONR5R6, S(O)n-NR5R6,-NR10-CO-R13, -NR10-SO2-R13, -NH-SO2-NR5R6, -NR10-CO-NR5R6, -NR10-CS-NR5R6, -NR10-COOR13, all of said radicals being optionally substituted; and n denotes an integer of between 0 and 2. The aforementioned products are in all the isomeric forms and the salts thereof for use as medicaments.
    • 本发明涉及具有式(I)的新产品,其中:p表示0至2; R和R1表示O或NH; R 2和R 3表示氢,烷基,烯基,炔基,环烷基,芳基和杂芳基,或者R 2和R 3与它们所连接的碳原子一起形成碳环或杂环基,所有基团都是任选被取代的; A1表示单键,烷基,烯丙基和丙炔基; Y和Y1表示H,OCF3,S(O)nCF3,S(O)nAlk,SO2CHF2,SO2CF2CF3,-O-CF2-CHF2,-O-CHF2,-O-CH2-CF3,SF5和SO2NR5R6, R 6选自任选取代的氢,烷基,烯基,环烷基,环烯基,杂环烷基,芳基和杂芳基,或R 5和R 6与它们所连接的N一起形成杂环基; A2表示Al,CO和SO2; B2表示任选被一个或多个选自Y2的取代基取代的杂环基; 环烷基,杂环烷基,芳基,杂芳基,-O-烯基,-O-炔基,O-环烷基,S(O)n - 烷基,-S(O)n - 烯基,-S(O)n - 炔基,S(O)n-环烷基,-COOR 13,-OCOR 13,NR 5 R 6,CONR 5 R 6,S(O)n -NR 5 R 6,-NR 10 -CO-R 13,-NR 10 -SO 2 - R13,-NH-SO2-NR5R6,-NR10-CO-NR5R6,-NR10-CS-NR5R6,-NR10-COOR13,所有所述基团任选被取代; 并且n表示0和2之间的整数。上述产物是全部异构形式及其盐,用作药物。