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    • 8. 发明授权
    • Certain substituted ureas, as modulators of kinase activity
    • 某些取代的脲,作为激酶活性的调节剂
    • US08222421B2
    • 2012-07-17
    • US12840246
    • 2010-07-20
    • Scott A. MitchellMihaela Diana DancaPeter A. BlomgrenDavid R. BrittelliPavel ZhichkinMatthew E. Voss
    • Scott A. MitchellMihaela Diana DancaPeter A. BlomgrenDavid R. BrittelliPavel ZhichkinMatthew E. Voss
    • C07D215/38
    • C07D471/04C07D401/06
    • Certain chemical entities chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, and prodrugs thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicles chosen from carriers, adjuvants, and excipients, are also provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to angiogenic kinase modulation, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer, including breast neoplasia, endometrial cancer, colon cancer, and neck squamous cell carcinoma. Methods of treatment include administering at least one chemical entity as a single active agent or administering such at least one chemical entity in combination with one or more other therapeutic agents. A method for determining the presence or absence of an angiogenic kinase in a sample comprising contacting the sample with at least one chemical entity under conditions that permit detection of activity of the angiogenic kinase, detecting a level of the activity of the angiogenic kinase, and therefrom determining the presence or absence of the angiogenic kinase in the sample.
    • 本文提供了选自式1化合物的某些化学实体及其药学上可接受的盐,溶剂合物,螯合物,非共价复合物及其前体药物。 还提供了包含至少一种化学实体和一种或多种选自载体,佐剂和赋形剂的药学上可接受的载体的药物组合物。 公开了治疗患有对血管生成激酶调节反应的某些疾病和病症的患者的方法,其包括向这些患者施用一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 这些疾病包括癌症,包括乳腺肿瘤,子宫内膜癌,结肠癌和颈部鳞状细胞癌。 治疗方法包括给予至少一种化学实体作为单一活性剂或者与一种或多种其它治疗剂组合施用这样的至少一种化学实体。 一种用于确定样品中存在或不存在血管生成激酶的方法,包括在允许检测血管生成激酶活性,检测血管生成激酶活性水平的条件下将样品与至少一种化学实体接触 确定样品中存在或不存在血管生成激酶。
    • 9. 发明授权
    • Neurotransmitter releasers useful for cognition enhancement
    • 神经递质释放剂可用于认知增强
    • US5414004A
    • 1995-05-09
    • US124523
    • 1993-09-20
    • Wendell W. WilkersonRichard A. EarlMatthew E. Voss
    • Wendell W. WilkersonRichard A. EarlMatthew E. Voss
    • C07D239/26A61K31/44A61K31/4409A61K31/4418A61K31/4427A61K31/443A61K31/495A61P25/28C07D213/24C07D213/44C07D213/50C07D213/55C07D213/57C07D213/61C07D241/12C07D401/06C07D403/06C07D405/06C07D405/12C07D401/14
    • C07D401/06C07D213/50C07D213/55C07D213/57C07D403/06C07D405/06
    • Compounds of the following formula have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man involving learning and cognition, where subnormal levels of this neurochemical are found ##STR1## wherein R.sup.1 is 4-,3-, or 2-pyridyl, 2-fluoro-4-pyridyl or 3-fluoro-4-pyridyl;R.sup.2 is alkyl of 1 to 10 carbons, cycloalkyl of 3 to 8 carbons, 2-,3-, or 4-pyridyl, Phe or Phe-W;Phe is a phenyl group;W is F, Cl, Br, R.sup.4, --OH, --OR.sup.4, --NO.sub.2, --NH.sub.2, --NHR.sup.4, --NR4R.sup.4, --CN, --S(O)m --R.sup.4 ;R.sup.3 is H, F, Cl, Br, --CN, --OH, --NO.sub.2, --NH.sub.2, --CF.sub.3, --NHR.sup.4, --NR.sup.4 R.sup.4, R.sup.4, --OR.sup.4, --S(O).sub.m --R.sup.4R.sup.4 is alkyl of 1 to 4 carbons, CH.sub.2 Phe-- or Phe--;R.sup.5 is --(CH.sub.2).sub.n --Y or --OCOR.sup.4 ;Y is NH.sub.2, --NHR.sup.4, --NR.sup.4 R.sup.4, --NHCOR.sup.4, --NHCO.sub.2 R.sup.4, F, Cl, Br, OR.sup.4, --S(O).sub.m R.sup.4, --CO.sub.2 H, --CO.sub.2 R.sup.4, --CN, --CONR.sup.4 R.sup.4, --CON HR.sup.4, CONHR.sup.4, --CONH.sub.2, --COR.sup.4 ; --CH.dbd.CHCO.sub.2 R.sup.4, OCOR.sup.4, CO.tbd.CCO.sub.2 R.sup.4, --CH.dbd.CHR.sup.4, or --C.tbd.CR.sup.4 ;m is 0, 1 or 2;n is 1 to 7;and physiologically suitable salts thereof.
    • 已经显示下式的化合物增强神经递质乙酰胆碱的释放,因此可用于治疗涉及学习和认知的人的疾病,其中发现该神经化学物质的次正常水平其中R1是4- ,3-或2-吡啶基,2-氟-4-吡啶基或3-氟-4-吡啶基; R2是1至10个碳的烷基,3至8个碳原子的环烷基,2-,3-或4-吡啶基,Phe或Phe-W; Phe是苯基; W是F,Cl,Br,R 4,-OH,-OR 4,-NO 2,-NH 2,-NHR 4,-NR 4 R 4,-CN,-S(O)m -R 4; R3是H,F,Cl,Br,-CN,-OH,-NO2,-NH2,-CF3,-NHR4,-NR4R4,R4,-OR4,-S(O)m -R4 R4是1〜 4个碳,CH2Phe-或Phe-; R5是 - (CH2)n-Y或-OCOR4; Y是NH 2,-NHR 4,-NR 4 R 4,-NHCOR 4,-NHCO 2 R 4,F,Cl,Br,OR 4,-S(O)m R 4,-CO 2 H,-CO 2 R 4,-CN,-CONR 4 R 4,-CON HR 4,CONHR 4, CONH2,-COR4; -CH = CHCO 2 R 4,OCOR 4,CO 3,CCO 2 R 4,-CH = CHR 4或-C 3 CH 3 CR 4; m为0,1或2; n为1〜7; 和其生理适合的盐。