Substituted glycine derivatives for use as medicaments
    43.
    发明申请
    Substituted glycine derivatives for use as medicaments 审中-公开
    用作药物的取代的甘氨酸衍生物

    公开(公告)号:US20040092498A1

    公开(公告)日:2004-05-13

    申请号:US10640520

    申请日:2003-08-13

    摘要: The compounds of formula (I) are substituted glycine derivatives useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included. 1 wherein R1 is hydroxycarbonyl, a carboxylic acid biostere or prodrug thereof; R3, R3a, R2 and R2a are independently selected from H, C1-C6 alkyl, and C1-C6 alkoxy C1-C6 alkyl; Z is; (i) a C-linked, 5 membered heterocycloalky or heteroaryl substituted with C1-C6 alkyl or fused with C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl, or monocyclic heteroaryl, wherein the fused ring is optionally substituted with one or two substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, perfluoro C1-C6 alkyl, perfluoro C1-C6 alkoxy, cyano, C1-C6 alkyl amino, C1-C6 alkyl thio, C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl, and monocyclic heteroaryl; or (ii) the group; 2 wherein R4 and R4a are independently H, C1-C6 alkyl, C1-C6 alkoxy or C1-C6 alkoxy C1-C6 alkyl; R5 is C1-C6 alkyl, C3-C12 cycloalkyl, 4-12 membered heterocycloalkyl, aryl or heteroaryl and R5 is optionally substituted with one or two substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, perfluoro C1-C6 alkyl, perfluoro C1-C6 alkoxy, cyano, C1-C6 alkyl amino, di-C1-C6 alkyl amino, amino C1-C6 alkyl, C1-C6 alkyl amino C1-C6 alkyl, di-C1-C6 alkyl amino C1-C6 alkyl, C1-C6 alkyl thio, C3-C8 cycloalkyl, 4-8 membered heterocycloalkyl, phenyl and monocyclic heteroaryl; nulland either; (i) Y is S, O, NH or CH2 and X is a direct link or C1-C2 alkyl optionally substituted with C1-C6 alkyl or di-C1-C6 alkyl or 1-4 fluorine atoms; or (ii) X is S, O, CH2 or NH and Y is C1-C2 alkyl optionally substituted with C1-C6 alkyl or di-C1-C6 alkyl or 1-4 fluorine atoms.

    摘要翻译: 式(I)化合物是用于治疗癫痫,微弱发作,运动功能减退,颅神经障碍,神经变性疾病,抑郁症,焦虑症,恐慌症,疼痛,关节炎,神经病理学障碍,睡眠障碍,内脏疼痛障碍和胃肠道的取代甘氨酸衍生物 疾病 包括用于制备在该方法中有用的最终产物和中间体的方法。 还包括含有一种或多种化合物的药物组合物。 其中R 1是羟基羰基,羧酸生物降解剂或其前药; R 3,R 3a,R 2和R 2a独立地选自H,C 1 -C 6烷基和C 1 -C 6烷氧基C 1 -C 6烷基; Z是 (i)被C 1 -C 6烷基取代或与C 3 -C 8环烷基,4-8元杂环烷基,苯基或单环杂芳基稠合的C连接的5元杂环烷基或杂芳基,其中稠环任选地被一个或两个 选自卤素,C 1 -C 6烷基,C 1 -C 6烷氧基,全氟C 1 -C 6烷基,全氟C 1 -C 6烷氧基,氰基,C 1 -C 6烷基氨基,C 1 -C 6烷基硫代,C 3 -C 8环烷基, 4-8元杂环烷基,苯基和单环杂芳基; 或(ii)该组; 其中R 4和R 4a独立地是H,C 1 -C 6烷基,C 1 -C 6烷氧基或C 1 -C 6烷氧基C 1 -C 6烷基; R 5是C 1 -C 6烷基,C 3 -C 12环烷基,4-12元杂环烷基,芳基或杂芳基,R 5任选被一个或两个选自以下的取代基取代:卤素,C 1 -C 6烷基, C 1 -C 6烷氧基,全氟C 1 -C 6烷基,全氟C 1 -C 6烷氧基,

    Fluorinated-photoinitiators in dual cure resins
    45.
    发明申请
    Fluorinated-photoinitiators in dual cure resins 审中-公开
    双重固化树脂中的氟化光引发剂

    公开(公告)号:US20040067311A1

    公开(公告)日:2004-04-08

    申请号:US10380572

    申请日:2003-03-13

    IPC分类号: B05D003/10

    摘要: The present invention relates to a process for the preparation of scratch-resistant coatings by dual cure of compositions comprising surface active benzoyl compounds wherein at least one non-polar fluorinated alkyl group is present. The invention also relates to a process for concentrating these surface-active photoinitiators in the surface of coatings, to novel surface active benzoyl compounds wherein at least one non-polar fluorinated alkyl group is present, to compositions wherein the novel surface active fluorinated photoinitiators are present, and to a method for improving the flow of a curable composition on substrates.

    摘要翻译: 本发明涉及一种通过双重固化包含表面活性苯甲酰化合物的组合物制备耐刮擦涂层的方法,其中存在至少一个非极性氟代烷基。 本发明还涉及将这些表面活性光引发剂浓缩到涂层表面的方法,其中存在至少一种非极性氟代烷基的新型表面活性苯甲酰化合物与其中存在新表面活性氟化光引发剂的组合物 以及改善基板上的固化性组合物的流动性的方法。

    Aminoalcohol derivatives
    49.
    发明申请
    Aminoalcohol derivatives 失效
    氨基醇衍生物

    公开(公告)号:US20040006143A1

    公开(公告)日:2004-01-08

    申请号:US10603943

    申请日:2003-06-26

    IPC分类号: A61K031/13

    摘要: The present invention relates to a compound formula nullInull: 1 wherein 2 Y is bond, nullOnull(CH2)nnull (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound nullInull of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.

    摘要翻译: 本发明涉及化合物式[I]:其中Y为键,-O-(CH 2)n - (其中n为1,2,3或4)等,Z为氰基,四唑基等。 R 1是氢,低级烷基等,R 2是氢或氨基保护基,R 3是氢或低级烷基,R 4是氢或低级烷基,R 5是氢, 和R 8各自独立地为氢,卤素,羟基,低级烷基等,R 6为氢,低级烷基等,R 9为氢或低级烷基,i为1或2, 或其盐。 本发明的化合物[I]及其药学上可接受的盐可用于预防和/或治疗呼吸窘迫症或尿失禁。