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    • 8. 发明申请
    • PROTEIN PHOSPHORYLATION ASSAY
    • 蛋白质磷酸化测定
    • WO2005114198A3
    • 2006-05-26
    • PCT/US2005017711
    • 2005-05-19
    • PHARMACOPEIA INCAULD DOUGLAS S
    • AULD DOUGLAS S
    • C12N9/12C12Q1/42C12Q1/48G01N33/573
    • C12Q1/42C12Q1/485G01N2500/00
    • The present invention provides methods for assaying the activity of protein kinases or phosphatases that involve reacting the enzymes with substrate, at least a portion of which is fluorescently labeled; allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material; and measuring the fluorescence produced by bound, labeled substrate. The invention also provides methods for identifying substances that modulate the activity of protein kinases and phosphatases that comprise reacting the enzymes with a substrate, at least a portion of which is fluorescently labeled, in the presence and absence of test compounds, allowing phosphorylated substrate to bind to a solid support coated with a phosphate-binding material, measuring the fluorescence produced by bound, labeled substrate, and comparing the fluorescence from reactions carried out in the presence and absence of test compounds.
    • 本发明提供了用于测定蛋白激酶或磷酸酶的活性的方法,其涉及使酶与底物反应,其中至少一部分被荧光标记; 允许磷酸化底物结合涂覆有磷酸盐结合材料的固体支持物; 并测量由结合的标记底物产生的荧光。 本发明还提供了用于鉴定调节蛋白激酶和磷酸酶的活性的物质的方法,其包括在存在和不存在测试化合物的情况下使酶与底物反应,其中至少一部分被荧光标记,允许磷酸化底物结合 包被磷酸盐结合材料的固体支持物,测量由结合的标记底物产生的荧光,并比较在存在和不存在测试化合物的情况下进行的反应的荧光。
    • 9. 发明申请
    • IMIDAZOLYL PYRIMIDINE DERIVATIVES USEFUL AS IL-8 RECEPTOR MODULATORS
    • 作为IL-8受体调节剂有用的咪唑啉衍生物衍生物
    • WO2004063192A1
    • 2004-07-29
    • PCT/US2004/000469
    • 2004-01-09
    • PHARMACOPEIA DRUG DISCOVERY, INC.VAN DER LOUW, JaapOHLMEYER, Michael, H., J.BOHNSTEDT, Adolph, C.HO, Koc-KanAULD, Douglas, S.KULTGEN, Steven, G.ROUGHTON, Andrew, Laird
    • VAN DER LOUW, JaapOHLMEYER, Michael, H., J.BOHNSTEDT, Adolph, C.HO, Koc-KanAULD, Douglas, S.KULTGEN, Steven, G.ROUGHTON, Andrew, Laird
    • C07D405/14
    • C07D403/14C07D405/14C07D409/14C07D413/14
    • The invention relates to compounds of the formula I, wherein R1, R2, R3 and R4 are each independently selected from H, (1-4C)alkyl, (1-4C)alkoxy, trifluoromethyl, trifluoromethoxy, halogen, amino, sulfonamide, cyano, OH and nitro; R5 is H or (1-6C)alkyl; R6 is H, (1-6C)alkyl or (1-6C)alkoxy; R7 is H or (1-6C)alkyl; R8 is (1-6C)alkyl, optionally substituted with (1-6C)alkoxy; R9 is -(CH 2 ) n R10, wherein n is 1, 2 or 3 and R10 is selected from (1-4C)alkoxy, (1-4C)alkylthio, trifluoromethyl, (3-8C)cycloalkyl, phenyl optionally substituted with (1-4C)alkoxy, -NR11R12 and -O(CH 2 ) 2 NR11R12, wherein one of R11 and R12 is (1-4C)alkoxy, the other being H or (1-4C)alkyl, or R9 is -CH 2 (2-7C)heterocycloalkyl, provided that when at least one heteroatom in the heterocycloalkyl moiety is nitrogen, the distance between this nitrogen and the nitrogen in "NHR9" is at least three carbon atoms, or R9 is -(CH 2 ) 3 (2-7C)heterocycloalkyl or -(CH 2 ) 2 CHR13R14, wherein R13 and R14 together with the carbon atom to which they are attached, are (2-7C)heterocycloalkyl; and X is O, S or NH; or a pharmaceutically acceptable salt thereof. The compounds of the invention are Il-8 receptor modulators, in particular inhibitors thereof, and can be used for treating or preventing Il-8 receptor mediated disorders, such as atherosclerosis, inflammation, rheumatoid arthritis and related disorders.
    • 本发明涉及式I化合物,其中R 1,R 2,R 3和R 4各自独立地选自H,(1-4C)烷基,(1-4C)烷氧基,三氟甲基,三氟甲氧基,卤素,氨基,磺酰胺,氰基 ,OH和硝基; R5是H或(1-6C)烷基; R6是H,(1-6C)烷基或(1-6C)烷氧基; R 7为H或(1-6C)烷基; R8是(1-6C)烷基,任选被(1-6C)烷氧基取代; R9为 - (CH2)nR10,其中n为1,2或3,R10选自(1-4C)烷氧基,(1-4C)烷硫基,三氟甲基,(3-8C)环烷基,任选被(1 -4C)烷氧基,-NR11R12和-O(CH2)2NR11R12,其中R11和R12之一为(1-4C)烷氧基,另一个为H或(1-4C)烷基,或R9为-CH2(2-7C )杂环烷基,条件是当杂环烷基部分中的至少一个杂原子为氮时,“NHR9”中该氮与氮之间的距离为至少三个碳原子,或者R 9为 - (CH 2)3(2-7C)杂环烷基 或 - (CH 2)2 CHR 13 R 14,其中R 13和R 14与它们所连接的碳原子一起为(2-7C)杂环烷基; X为O,S或NH; 或其药学上可接受的盐。 本发明的化合物是II-8受体调节剂,特别是其抑制剂,并且可用于治疗或预防II-8受体介导的病症,例如动脉粥样硬化,炎症,类风湿性关节炎和相关疾病。