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    COMPOSITIONS AND METHODS FOR THE TREATMENT OF HOMOCYSTINURIA
    1.
    发明申请
    COMPOSITIONS AND METHODS FOR THE TREATMENT OF HOMOCYSTINURIA 审中-公开
    用于治疗嗜酸粒细胞的组合物和方法

    公开(公告)号：WO2015033279A1

    公开(公告)日：2015-03-12

    申请号：PCT/IB2014/064228

    申请日：2014-09-03

    申请人： KANDULA, Mahesh

    发明人： KANDULA, Mahesh

    IPC分类号： A61K31/205 ,  A61K31/202 ,  A61P43/00

    CPC分类号： A61K31/557 ,  C07C229/12 ,  C07D213/66

    摘要： The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of homocystinuria may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of cystathionine beta synthase deficiency or cbs deficiency, is an inherited disorder of the metabolism of the amino acid methionine, often involving cystathionine beta synthase.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，以及其多晶型物，溶剂合物，对映体，立体异构体和水合物。 包含有效量的式I化合物的药物组合物和用于治疗高胱氨酰尿症的方法可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。 这些组合物可用于治疗胱硫醚β合酶缺乏症或cbs缺乏症，是氨基酸甲硫氨酸的代谢遗传性疾病，常涉及胱硫醚β合酶。

    METHOD FOR THE PRODUCTION OF MAGNESIUM PYRIDOXAL-5'-PHOSPHATE GLUTAMATE AND INTERMEDIATE PRODUCTS OBTAINED THEREBY
    5.
    发明申请
    METHOD FOR THE PRODUCTION OF MAGNESIUM PYRIDOXAL-5'-PHOSPHATE GLUTAMATE AND INTERMEDIATE PRODUCTS OBTAINED THEREBY 审中-公开
    生产吡啶羧酸镁 - 谷氨酸镁的方法及其获得的中间产物

    公开(公告)号：WO1997009334A1

    公开(公告)日：1997-03-13

    申请号：PCT/EP1996003749

    申请日：1996-08-26

    申请人： STEIGERWALD ARZNEIMITTELWERK GMBH ,  MAIDONIS, Panagiotis ,  SCHNEIDER, Werner

    发明人： STEIGERWALD ARZNEIMITTELWERK GMBH

    IPC分类号： C07F09/58

    CPC分类号： C07D213/66 ,  C07F9/58

    摘要： The invention relates to a method for the production of magnesium pyridoxal-5'-phosphate glutamate, in which pyridoxine or an acid addition salt thereof is oxidised with manganese (IV) oxide to pyridoxal; pyridoxal is reacted with p-phenetidine under formation of the Schiff's base p-phenetidyl-pyridoxal; p-phenedityl-pyridoxal is selectively phosphorylated on the 5'-hydroxymethyl group under formation of p-phenetidyl-pyridoxal-5'-phosphate; p-phenetidyl-pyridoxal-5'-phosphate is hydrolysed under formation of an alkali metal salt of pyridoxal-5'-phosphate; the alkali metal ions are removed in order to obtain pyridoxal-5'-phosphate; pyridoxal-5'-phosphate is reacted with a reaction product of a magnesium alcoholate and L-glutamic acid; and the formed magnesium pyridoxal-5'-phosphate glutamate is isolated. Furthermore, the invention relates to intermediate products obtained with this method.

    摘要翻译： 本发明涉及一种吡哆醛-5'-磷酸谷氨酸镁的制备方法，其中吡哆醇或其酸加成盐用氧化锰（Ⅳ）氧化成吡哆醛; 吡哆醛与席夫碱碱基对苯乙基 - 吡哆醛的形成反应与对苯乙啶反应; 在对 - 苯乙基 - 吡哆醛-5'-磷酸形成的情况下，在5-羟基甲基上选择性磷酸化p-苯并吡唑并[ 对 - 苯乙基 - 吡哆醛-5'-磷酸酯在吡哆醛-5'-磷酸的碱金属盐的形成下水解; 去除碱金属离子以获得吡哆醛-5'-磷酸; 吡哆醛-5'-磷酸酯与醇镁和L-谷氨酸的反应产物反应; 并分离形成的吡哆酮-5'-磷酸谷氨酸镁。 此外，本发明涉及使用该方法得到的中间产物。

    COMPOSITIONS AND METHODS FOR THE TREATMENT OF MODERATE TO SEVERE PAIN
    6.
    发明申请
    COMPOSITIONS AND METHODS FOR THE TREATMENT OF MODERATE TO SEVERE PAIN 审中-公开
    用于治疗中度疼痛的组合物和方法

    公开(公告)号：WO2016046674A1

    公开(公告)日：2016-03-31

    申请号：PCT/IB2015/056696

    申请日：2015-09-03

    申请人： MOHAN. M., Alapati

    发明人： MOHAN. M., Alapati

    IPC分类号： A61K31/00

    CPC分类号： A61K31/4415 ,  A61K45/06 ,  C07D207/12 ,  C07D209/14 ,  C07D213/66 ,  C07D213/67 ,  C07D213/82 ,  C07D233/64 ,  C07D339/04 ,  C07D473/04 ,  C07D487/04 ,  C07D495/04 ,  A61K2300/00

    摘要： The compositions and compounds of formula I which includes a salt of pyridoxine or its polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral, syrup, topical, parenteral administration, injection, subdermal, oral solution, rectal administration, nanoparticle, buccal administration or transdermal administration. Such compositions may be used to treatment of musculoskeletal complaints, especially arthritis, rheumatoid arthritis, polymyositis, dermatomyositis, osteoarthritis, dental pain, TMJ pain, peripheral neuropathy, INH, sideroblastic anemia, pyridoxine- dependent epilepsy, mild to moderate peripheral neuropathy, spondylarthritis, ankylosing spondylitis, gout attacks, and pain management.

    摘要翻译： 式I的组合物和化合物，其包含吡哆醇或其多晶型物的盐，对映异构体，立体异构体，溶剂化物和其水合物。 这些盐可以配制成药物组合物。 药物组合物可以配制用于口服，糖浆，局部，肠胃外给药，注射，皮下，口服溶液，直肠给药，纳米颗粒，口腔给药或透皮给药。 此类组合物可用于治疗肌肉骨骼症，特别是关节炎，类风湿性关节炎，多发性肌炎，皮肌炎，骨关节炎，牙痛，TMJ疼痛，周围神经病变，INH，铁粒细胞性贫血，吡哆素依赖性癫痫，轻度至中度周围神经病变，脊椎关节炎， 强直性脊柱炎，痛风发作和疼痛管理。

    TUMOR NECROSIS FACTOR - ALPHA INHIBITORS
    7.
    发明申请
    TUMOR NECROSIS FACTOR - ALPHA INHIBITORS 审中-公开
    肿瘤坏死因子 - 阿尔法抑制剂

    公开(公告)号：WO2008142623A3

    公开(公告)日：2009-12-30

    申请号：PCT/IB2008051932

    申请日：2008-05-16

    申请人： PIRAMAL LIFE SCIENCES LTD ,  BALACHANDRAN SARALA ,  VISHWAKARMA RAM ,  KAKI VENKATRAO ,  YADAV VITTHAL ,  CHAUTHE SIDDHESHWAR ,  SHARMA SOMESH ,  PARIKH SAPNA ,  KHARAS FIRUZA

    发明人： BALACHANDRAN SARALA ,  VISHWAKARMA RAM ,  KAKI VENKATRAO ,  YADAV VITTHAL ,  CHAUTHE SIDDHESHWAR ,  SHARMA SOMESH ,  PARIKH SAPNA ,  KHARAS FIRUZA

    IPC分类号： C07D403/00 ,  C07D413/00

    CPC分类号： C07D213/66 ,  C07D311/22 ,  C07D491/056

    摘要： The present invention relates to small molecules that inhibit Tumor Necrosis Factor- alpha (TNF-a), for example, by interaction with TNF-a protein or its receptor, thereby lowering the overall TNF-a activity, and that are represented by formula (1) or a stereoisomer thereof, tautomer thereof, or mixture thereof in any ratio; a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable polymorph thereof; wherein: A1, A2, X1, X2, n, R1, R2, R3 and R4 are as defined in the specification. The present invention also relates to processes for the preparation of these small molecules and to pharmaceutical compositions containing them. The present invention further relates to a method of treatment of disorders characterized by increased TNF- a activity, such as inflammation.

    摘要翻译： 本发明涉及例如通过与TNF-α蛋白或其受体的相互作用来抑制肿瘤坏死因子-α（TNF-α）的小分子，从而降低总体TNF-α活性，并且由式 1）或其立体异构体，其互变异构体或其混合物; 其药学上可接受的盐，药学上可接受的溶剂合物或其药学上可接受的多晶型物; 其中：A1，A2，X1，X2，n，R1，R2，R3和R4如说明书中所定义。 本发明还涉及制备这些小分子的方法和含有它们的药物组合物。 本发明还涉及以TNF-α活性增加为特征的疾病如炎症的治疗方法。