Methods for preventing and/or treating lysosomal storage disorders
    4.
    发明授权
    Methods for preventing and/or treating lysosomal storage disorders 有权
    用于预防和/或治疗溶酶体储存障碍的方法

    公开(公告)号:US08940766B2

    公开(公告)日:2015-01-27

    申请号:US12757160

    申请日:2010-04-09

    CPC classification number: C12Q1/34 A61K31/445 C07D211/36 G01N2333/924

    Abstract: The present invention provides methods for preventing and/or treating lysosomal storage disorders using 5-(fluoromethyl)piperidine-3,4-diol, 5-(chloromethyl)piperidine-3,4-diol, or a pharmaceutically acceptable salt, solvate, or prodrug thereof, or any combination of two or more thereof. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease.

    Abstract translation: 本发明提供使用5-(氟甲基)哌啶-3,4-二醇,5-(氯甲基)哌啶-3,4-二醇或其药学上可接受的盐,溶剂合物或/或溶剂合物来预防和/或治疗溶酶体贮积病的方法 前药,或其两种或多种的任何组合。 特别地,本发明提供了预防和/或治疗戈谢氏病的方法。

    Novel Cyclic Amino Benzoic Acid Derivative
    9.
    发明申请
    Novel Cyclic Amino Benzoic Acid Derivative 失效
    新型环状氨基苯甲酸衍生物

    公开(公告)号:US20070249580A1

    公开(公告)日:2007-10-25

    申请号:US11659854

    申请日:2005-08-11

    Abstract: The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.

    Abstract translation: 本发明涉及作为人类过氧化物酶体增殖物激活受体(PPAR)激动剂的脂质代谢异常的治疗有效的环状氨基苯甲酸衍生物,特别是作为对人PPARα同种型的激动剂的添加 其盐,以及含有这些化合物的药物组合物。 由通式(1)表示的环状氨基苯甲酸衍生物[其中环Ar表示可具有取代基的芳基等; Y表示C 1 -C 4亚烷基,C 2 -C 4亚烯基,C 2 C 3 -C 4亚炔基等; Z表示氧原子,硫原子或 - (CH 2 CH 2)n - (n表示0,1或2)。 X表示氢原子,卤素原子,可被卤素原子取代的低级烷基等; R代表氢原子或低级烷基,-COOR代替环W的结合位置的邻位或甲基位置]或其药学上可接受的盐。

    Process for preparing 4-substituted 2,2,6,6-tetramethylpiperidin-N-oxy and 2,2,6,6-tetramethylpiperidin-N-hydroxy compounds
    10.
    发明申请
    Process for preparing 4-substituted 2,2,6,6-tetramethylpiperidin-N-oxy and 2,2,6,6-tetramethylpiperidin-N-hydroxy compounds 审中-公开
    制备4-取代的2,2,6,6-四甲基哌啶-N-氧基和2,2,6,6-四甲基哌啶-N-羟基化合物的方法

    公开(公告)号:US20050256312A1

    公开(公告)日:2005-11-17

    申请号:US11125149

    申请日:2005-05-10

    CPC classification number: C07D211/94

    Abstract: A process for preparing 4-substituted 2,2,6,6-tetramethylpiperidin-N-oxy compounds (II) or mixtures of (II) and 4-substituted 2,2,6,6-tetramethylpiperidin-N-hydroxy compounds (III) where X+Y can be O or can represent a cyclic ketal with the radicals or can represent an open-chain ketal in which X═O—R and Y═O—R′, where R and R′ can be identical or different and can each be CH3, CH2—CH3, CH2—CH2—CH3, CH(CH3)—CH3, CH2—CH2—CH2—CH3 and CH2—CH(CH3)—CH3, by oxidizing corresponding 4-substituted 2,2,6,6-tetramethylpiperidines (I) with hydrogen peroxide in the presence of alkali metal hydrogencarbonate and/or ammonium hydrogencarbonate and in the presence or absence of a solvent, in which the reaction is carried out with the addition of Brönsted acids which have an acid strength greater than that of the hydrogencarbonate.

    Abstract translation: 制备4-取代的2,2,6,6-四甲基哌啶-N-氧化合物(II)或(II)和4-取代的2,2,6,6-四甲基哌啶-N-羟基化合物(III)的混合物的方法 )其中X + Y可以是O或可以表示具有自由基的环状缩酮,或者可以表示开链缩酮,其中XOR和YO-R',其中R和R'可以相同或不同, CH 2,CH 2,CH 3,CH 2,-CH 2,-CH 2, CH 3(CH 3 CH 3) - CH 3,CH 2 -CH 2, -CH 2 CH 3和CH 2 -CH(CH 3 CH 3) - CH 3, 通过在碱金属碳酸氢盐和/或碳酸氢铵存在下,在过氧化氢存在下,在有或无溶剂下,用相应的4-取代的2,2,6,6-四甲基哌啶(I)氧化相应的4-取代的2,2,6,6-四甲基哌啶(I) 加入酸强度大于碳酸氢钠的布朗斯台德酸进行反应。

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