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    • 6. 发明授权
    • Quinoline and quinoxaline derivatives as inhibitors of kinase enzymatic activity
    • 喹啉和喹喔啉衍生物作为激酶酶活性的抑制剂
    • US08148531B2
    • 2012-04-03
    • US11918898
    • 2006-05-04
    • Alan Hornsby DavidsonStephen John DaviesDavid Festus Charles Moffat
    • Alan Hornsby DavidsonStephen John DaviesDavid Festus Charles Moffat
    • C07D215/00
    • C07D215/42C07D215/233C07D215/36C07D215/44C07D239/90C07D239/94C07D401/12C07D403/12C07D409/12C07D413/12C07D417/12
    • Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, —CH2—, —O—, —S—, —S(═O)2—, or —NR5— where R5 is hydrogen or C1-C4 alkyl; Q is ═N—, ═CH— or ═C(X1)— wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, —(C═O)R3, —(C═O)OR3, or —(C═O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and D is a mono-cyclic heterocyclic ring of 5 or 6 ring atoms.
    • 式(IA)或(IB)的化合物是极光激酶活性的抑制剂:式(IA),(IB)其中-L1Y1- [CH2] z-是连接基,其中Y1,L1和z如 索赔; R6是C1-C4烷氧基,氢或卤素; W表示键,-CH 2 - , - O - , - S - , - S(= O)2 - 或-NR 5 - ,其中R 5是氢或C 1 -C 4烷基; Q为≡N-,═CH-或≡C(X1) - 其中X1为氰基,环丙基或卤素; 连接基团L2如权利要求中所定义; R是式(X)或(Y)的基团:其中R 1是羧酸基团(-COOH)或可被一个或多个细胞内羧酸酯酶水解成羧酸基团的酯基; R4是氢; 或C 1 -C 6烷基,C 3 -C 7环烷基,芳基,芳基(C 1 -C 6烷基) - ,杂芳基,杂芳基(C 1 -C 6烷基) - ,(C = O)R 3, - (C = O)OR 3 ,或 - (C = O)NR 3,其中R3是氢或任选取代的(C1-C6)烷基,C3-C7环烷基,芳基,芳基(C1-C6烷基) - ,杂芳基或杂芳基(C1-C6烷基) ; R 41是氢或任选取代的C 1 -C 6烷基; 且D为5或6个环原子的单环杂环。
    • 10. 发明授权
    • Bicyclic amine derivatives as inhibitors of class 1 receptor tyrosine kinases
    • 双环胺衍生物作为1类受体酪氨酸激酶的抑制剂
    • US07012076B2
    • 2006-03-14
    • US10239941
    • 2001-03-29
    • David Festus Charles MoffatPeter David Davis
    • David Festus Charles MoffatPeter David Davis
    • C07D239/94A61K31/505
    • C07D239/94
    • Fused bicyclic amines of formula (1) are described wherein Ar is an aryl or heteroaryl group; Y is a —S(O2)— or —C(O)— group; R1 is a hydrogen or halogen atom or an alkyl, haloalkyl, alkoxy, haloalkoxy or cyano group; X is a nitrogen atom or a C(R1a) group where R1a is as defined for R1 and may be the same or different; W and Z are each a carbon atom and together with U form an optionally substituted five- or six-membered monocyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the activity of Class 1 receptor tyrosine kinases and are of use in the prophylaxis and treatment of hyperproliferative disorders such as cancer, psoriasis, restenosis, atherosclerosis and fibrosis.
    • 描述了式(1)的稠合双环胺,其中Ar是芳基或杂芳基; Y是-S(O)2 - 或-C(O) - 基; R 1是氢或卤素原子或烷基,卤代烷基,烷氧基,卤代烷氧基或氰基; X是氮原子或C(R 1a)基团,其中R 1a如R 1所定义,并且可以相同或不同 ; W和Z各自为碳原子,与U一起形成任选取代的五元或六元单环芳族或杂芳族基团; 及其盐,溶剂合物,水合物和N-氧化物。 这些化合物能够抑制1类受体酪氨酸激酶的活性,并且可用于预防和治疗过度增殖性疾病如癌症,牛皮癣,再狭窄,动脉粥样硬化和纤维化。