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    ACETYL MIMIC COMPOUNDS FOR THE INHIBITION OF ISOPRENYL-S-CYSTEINYL METHYLTRANSFERASE
    2.
    发明申请
    ACETYL MIMIC COMPOUNDS FOR THE INHIBITION OF ISOPRENYL-S-CYSTEINYL METHYLTRANSFERASE 审中-公开
    用于抑制异丙肾上腺素甲基衍生物的乙炔化合物

    公开(公告)号：WO2009102997A2

    公开(公告)日：2009-08-20

    申请号：PCT/US2009034120

    申请日：2009-02-13

    Applicant: SIGNUM BIOSCIENCES INC ,  LEE SEUNG-YUB ,  VORONKOV MICHAEL ,  WOLANIN PETER

    Inventor： LEE SEUNG-YUB ,  VORONKOV MICHAEL ,  WOLANIN PETER

    IPC: A61K31/5377

    CPC classification number: C07D233/88 ,  C07C323/57 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07C327/42 ,  C07C335/08 ,  C07D207/22 ,  C07D207/34 ,  C07D213/74 ,  C07D233/70 ,  C07D235/14 ,  C07D239/42 ,  C07D249/04 ,  C07D257/04 ,  C07D263/48 ,  C07D265/30 ,  C07D277/42 ,  C07D295/215 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    Abstract: Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).

    Abstract translation: 除此之外，本发明提供能够有效抑制嗜中性粒细胞，巨噬细胞和血小板中G蛋白或GPCR介导的炎症反应的新型化合物。 特别地，本发明的化合物作为水肿抑制剂，红斑抑制剂和MPO抑制剂（髓过氧化物酶），含有相同化合物的药物组合物及其用于治疗可能受益于水肿，红斑和MPO抑制的疾病的用途 例如炎症（急性或慢性），哮喘，自身免疫疾病和慢性阻塞性肺病（COPD）（例如肺气肿，慢性支气管炎和小气道疾病等），免疫系统的炎症反应，皮肤疾病（例如 对于患有酒渣鼻，特应性皮炎，脂溢性皮炎，牛皮癣的患者，肠易激综合征（例如，Chron氏病和溃疡性结肠炎等）以及中枢神经系统疾病（例如帕金森氏病））减少急性皮肤刺激。

    NITRATE ESTER DERIVATIVES USEFUL FOR PREPARING DRUGS FOR EPILEPSY
    4.
    发明申请
    NITRATE ESTER DERIVATIVES USEFUL FOR PREPARING DRUGS FOR EPILEPSY 审中-公开
    用于制备药物的硝酸酯衍生物有用

    公开(公告)号：WO2003000643A1

    公开(公告)日：2003-01-03

    申请号：PCT/EP2002/006389

    申请日：2002-06-11

    Applicant: NICOX S.A. ,  ONGINI, Ennio ,  DEL SOLDATO, Piero

    Inventor： ONGINI, Ennio ,  DEL SOLDATO, Piero

    IPC: C07C203/04

    CPC classification number: C07D213/30 ,  C07C203/04 ,  C07C229/08 ,  C07C229/28 ,  C07C279/12 ,  C07C279/14 ,  C07C327/34 ,  C07C335/08 ,  C07C2601/14

    Abstract: Nitrooxyderivative compounds or salts thereof having the following general formula (I): A-(B) b0 -(C) co -NO 2 (I) wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A = R-T 1 -, wherein R is the radical of formula (II) as defined in the application; B is such that its precursor is selected from aminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid acid function, C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.

    Abstract translation: 具有以下通式（I）的硝基氧化还原化合物或其盐：A-（B）b0-（C）co-NO2（I）其中：c0为整数，为0或1，b0为整数，为0或 1，A = R-T1-，其中R是如申请中定义的式（II）的基团; B的前体选自氨基酸，羟基酸，多元醇，含有至少一个酸性官能团的化合物，C是含有脂族，杂环或芳族基团的二价基团。

    (2-HYDROXY)ETHYL-THIOUREAS USEFUL AS MODULATORS OF ALPHA2B ADRENERGIC RECEPTORS
    5.
    发明申请
    (2-HYDROXY)ETHYL-THIOUREAS USEFUL AS MODULATORS OF ALPHA2B ADRENERGIC RECEPTORS 审中-公开
    （2-羟基）乙二醇作为ALPHA2B ADRENERGIC受体的调节剂有用

    公开(公告)号：WO2002068384A2

    公开(公告)日：2002-09-06

    申请号：PCT/US2002/005021

    申请日：2002-02-19

    Applicant: ALLERGAN SALES, INC.

    Inventor： CHOW, Ken ,  GIL, Daniel, W. ,  FANG, Wenkui, Ken ,  GARST, Michael, E.

    IPC: C07C335/08

    CPC classification number: C07C335/10 ,  C07C335/08 ,  C07C335/14 ,  C07C2601/08 ,  C07C2601/10 ,  C07C2601/14 ,  C07C2601/16 ,  C07C2601/18

    Abstract: Compounds of formula (i) and of formula (ii), wherein the symbols have the meaning disclosed in the specification, specifically or selectively modulate α 2B and/or α 2C adrenergic receptors in preference over α 2A adrenergic receptors, and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardivascular and/or sedatory activity.

    Abstract translation: 式（ⅰ）和式（ⅱ）的化合物，其中符号具有权利要求中公开的含义，具体地或选择性调节α2A肾上腺素能受体，因此可用于缓解慢性疼痛和异常性疼痛，并且没有或仅有最小的心血管 和/或镇静活性。 本发明还涉及通过施用具有α2B或α2C肾上腺素能受体活性并且没有显着的α2A激动剂活性的化合物来激活哺乳动物中α2B或α2C肾上腺素能受体的方法。

    THIOL-MODIFIED HYALURONAN
    6.
    发明申请
    THIOL-MODIFIED HYALURONAN 审中-公开
    THIOL改性HYALURONONAN

    公开(公告)号：WO2002068383A2

    公开(公告)日：2002-09-06

    申请号：PCT/US2002/005081

    申请日：2002-02-21

    Applicant: ANIKA THERAPEUTICS, INC.

    Inventor： BULPITT, Paul, C., A. ,  SHERWOOD, Charles, H. ,  SADOZAI, Khalid, K.

    IPC: C07C323/25

    CPC classification number: C07C323/25 ,  C07C323/32 ,  C07C323/37 ,  C07C323/44 ,  C07C335/08 ,  C07C335/16 ,  C08B37/0072

    Abstract: 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.

    Abstract translation: 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。 包含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。

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