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    Substituted glycine derivatives for use as medicaments
    71.
    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

    发明人： David Blakemore ,  Justin S. Bryans ,  Wai-Lam Alex Chu ,  Graham N. Maw ,  David J. Rawson ,  Lisa R. Thompson

    IPC分类号： A61K031/397 ,  A61K031/44 ,  A61K031/40

    CPC分类号： C07C323/25 ,  A61K31/198 ,  A61K31/223 ,  A61K31/47 ,  C07C229/12 ,  C07C229/14 ,  C07C323/32 ,  C07D217/02

    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，

    Thiol-modified hyaluronan
    76.
    发明授权
    Thiol-modified hyaluronan 有权
    硫醇改性透明质酸

    公开(公告)号：US06620927B2

    公开(公告)日：2003-09-16

    申请号：US10081019

    申请日：2002-02-21

    申请人： Paul C. A. Bulpitt ,  Charles H. Sherwood ,  Khalid K. Sadozai

    发明人： Paul C. A. Bulpitt ,  Charles H. Sherwood ,  Khalid K. Sadozai

    IPC分类号： C07H702

    CPC分类号： C07C323/25 ,  C07C323/32 ,  C07C323/37 ,  C07C323/44 ,  C07C335/08 ,  C07C335/16 ,  C08B37/0072

    摘要： The present invention relates to biscarbodiimides, thiourea derivatives, urea derivatives, and cross-linked hyaluronan derivatives having at least one intramolecular disulfide bond, and methods of preparation thereof. The invention also includes thiolated hyaluronan derivatives and salts thereof having at least one pendant thiol group or a modified pendant thiol group, and methods of preparation thereof. An example of a modified pendant thiol group is a sulfhydryl group linked to a small molecule such as a bioactive agent, for example a drug or pharmaceutically active moiety. A hyaluronan derivative having a sulfhydryl group linked to a pharmaceutically active moiety is useful as a sustained or controlled release drug delivery vehicle. Compositions containing the hyaluronan derivatives of the invention can reversibly viscosify in vivo or in vitro, in response to mild changes in condition, and are thus useful in ophthalmic surgery and in tissue engineering.

    摘要翻译： 本发明涉及双碳二亚胺，硫脲衍生物，脲衍生物和具有至少一个分子内二硫键的交联透明质酸衍生物及其制备方法。 本发明还包括硫醇化透明质酸衍生物及其盐，其具有至少一个硫醇基侧基或修饰侧链巯基，及其制备方法。 修饰的侧链硫醇基团的实例是与小分子连接的巯基，例如生物活性剂，例如药物或药学活性部分。 具有与药学活性部分连接的巯基的透明质酸衍生物可用作持续或控释药物递送载体。 含有本发明的透明质酸衍生物的组合物可以在体内或体外可逆地粘稠，以响应于条件的轻微变化，因此可用于眼科手术和组织工程。

    Polyamine treatment of neurological disorders
    78.
    发明授权
    Polyamine treatment of neurological disorders 失效
    多胺治疗神经系统疾病

    公开(公告)号：US06576672B1

    公开(公告)日：2003-06-10

    申请号：US09486310

    申请日：2000-02-23

    申请人： Michael A. Murphy

    发明人： Michael A. Murphy

    IPC分类号： A61P2528

    CPC分类号： C07D295/13 ,  A61K31/13 ,  C07C211/13 ,  C07C211/14 ,  C07C211/38 ,  C07C323/25 ,  C07C2603/74 ,  C07F9/5004

    摘要： 2,3,2 Tetramine (3,7-diazanonane-1,9-diamine) is propounded for treatment of Parkingson's Disease and dementias characterized by mitochondrial damage in view of this compound's ability to completely neutralize the dopamine-depriving effect of MPTP in laboratory animals up to 12 hours post MPTP injection, and to retain partial protection at suboptimal tissue levels for up to 36 hours. The effect of injecting combinations of MPTP and/or reducing agents and/or xenobiotics and/or depigmenting agents on Dopamine, Norepinephrine, Serotonin and Epinephrine levels demonstrated that MPTP and MPP+ act as reducing agents that mobilize copper and calcium, and sequester iron, and that the vulnerability of dopamine to these types of neurotoxins and to xenobiotics and metals can be corrected by administration of 2,3,2 tetramine that appears to redistribute metals between diverse storage pools and free metals in cytosol and regulate receptor mediated events, among other antidotal effects analogous to those of some of the endogenous polyamines.

    摘要翻译： 考虑到该化合物完全中和MPTP在实验室中的多巴胺剥夺作用的能力，提出了2,3,2四胺（3,7-二磺酰基-1,9-二胺）用于治疗Parkingson氏病和以线粒体损伤为特征的痴呆症 MPTP注射后长达12小时的动物，并保持部分保护在次最佳组织水平长达36小时。 注射MPTP和/或还原剂和/或异生物和/或脱色素组合对多巴胺，去甲肾上腺素，5-羟色胺和肾上腺素水平的作用表明MPTP和MPP +作为还原剂，其可以动员铜和钙并螯合铁，以及 多巴胺对这些类型的神经毒素和异种生物和金属的脆弱性可以通过施用似乎在细胞溶质中的不同储存池和游离金属之间重新分配金属并调节受体介导的事件的2,3,2四胺来纠正，以及其他解毒剂 效果类似于一些内源多胺的效应。