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    Aryl-substituted indirubin derivatives, their production and use
    52.
    发明申请
    Aryl-substituted indirubin derivatives, their production and use 审中-公开
    芳基取代的靛玉红衍生物，其生产和使用

    公开(公告)号：US20020132792A1

    公开(公告)日：2002-09-19

    申请号：US09995862

    申请日：2001-11-29

    申请人： Schering AG

    发明人： Olaf Prien ,  Andreas Steinmeyer ,  Gerhard Siemeister ,  Rolf Jautelat

    IPC分类号： A61K031/695 ,  C07D43/02 ,  A61K031/404

    CPC分类号： C07D209/40 ,  C07D209/36

    摘要： Aryl-substituted indirubin derivatives, their production and their intermediate products for production, as well as their use as medications for treating cancer, such as solid tumors and leukemia; auto-immune diseases, such as psoriasis, alopecia and multiple sclerosis, chemotherapy agent-induced alopecia and mucositis; cardiovascular diseases, such as stenoses, arterioscleroses and restenoses; infectious diseases, such as, e.g., those caused by unicellular parasites, such as trypanosoma, toxoplasma or plasmodium, or those caused by fungi; nephrological diseases, such as, e.g., glomerulonephritis; chronic neurodegenerative diseases, such as Huntington's disease, amyotrophic lateral sclerosis, Parkinson's disease, AIDS dementia and Alzheimer's disease; acute neurodegenerative diseases, such as ischemias of the brain and neurotraumas; viral infections, such as, e.g., cytomegalic infections, herpes, hepatitis B and C, and HIV diseases, are described.

    摘要翻译： 芳基取代的靛玉红衍生物，其生产及其中间产物用于生产，以及它们用作治疗癌症的药物，例如实体瘤和白血病; 自身免疫性疾病，如牛皮癣，脱发和多发性硬化，化疗药物引起的脱发和粘膜炎; 心血管疾病，如狭窄，动脉硬化和再狭窄; 感染性疾病，例如由单细胞寄生虫如锥虫病，弓形虫或疟原虫引起的传染病或由真菌引起的传染病; 肾脏疾病，例如肾小球性肾炎; 慢性神经变性疾病，如亨廷顿舞蹈病，肌萎缩性侧索硬化，帕金森病，艾滋病痴呆和阿尔茨海默病; 急性神经变性疾病，如脑缺血和神经痛; 描述了病毒感染，例如巨细胞病毒感染，疱疹，乙型和丙型肝炎，以及HIV疾病。

    Process for the synthesis of a-nor-seco compounds with sterane skeleton
    53.
    发明授权
    Process for the synthesis of a-nor-seco compounds with sterane skeleton 失效
    用甾烷骨架合成α-间歇化合物的方法

    公开(公告)号：US06448413B1

    公开(公告)日：2002-09-10

    申请号：US10030743

    申请日：2001-11-30

    申请人： Csaba Santa ,  Zoltan Tuba ,  Sandor Maho ,  Janos Szeles ,  Gabor Balogh ,  Janos Brlik ,  Ferenc Trischler ,  Gabriella Szilagyi ,  Erika Bakcsi

    发明人： Csaba Santa ,  Zoltan Tuba ,  Sandor Maho ,  Janos Szeles ,  Gabor Balogh ,  Janos Brlik ,  Ferenc Trischler ,  Gabriella Szilagyi ,  Erika Bakcsi

    IPC分类号： C07D20936

    CPC分类号： C07D209/36 ,  C07C51/285 ,  C07C59/147 ,  C07C62/14

    摘要： The invention relates to a new process for the synthesis of 17&bgr;-hydroxy-17&agr;-methyl-1,3-seco-2-nor-5&agr;-androstane-3-acid derivatives of formula (I) wherein the meaning of Z is carboxyl or formyl group and to the new secoindoxylidene carboxylic acid derivatives of formula (II) wherein R1 and R2 independently are C1-C4 alkyl or alkoxy group, hydrogen or halogen atom—which are intermediates for preparing the compounds of formula (I). The 17&bgr;-hydroxy-17&agr;-methyl-1,3-seco-2-nor-5&agr;-androstane-3-acid derivatives of formula (I) are intermediates in the synthesis of oxandrolon (17&bgr;-hydroxy-17&agr;-methyl-2-oxa-5&agr;-androstane-3-one), which is used as anabolic in therapy.

    摘要翻译： 本发明涉及用于合成式（I）的17β-羟基-17α-甲基-1,3-仲-2-去甲基-α-雄甾烷-3-酸衍生物的新方法，其中Z的含义是羧基或 甲酰基和式​​（II）的新的仲二亚烷基羧酸衍生物，其中R 1和R 2独立地是作为制备式（I）化合物的中间体的C 1 -C 4烷基或烷氧基，氢或卤素原子。17β-羟基 式（I）的-17α-甲基-1,3-仲-2-降-5-醛 - 雄甾烷-3-酸衍生物是合成氧杂螺环酮（17β-羟基-17α-甲基-2-氧杂-5α- 雄甾烷-3-酮），其用于治疗中的合成代谢。

    Indole derivatives
    57.
    发明授权
    Indole derivatives 失效
    吲哚衍生物

    公开(公告)号：US5494928A

    公开(公告)日：1996-02-27

    申请号：US317259

    申请日：1994-10-03

    申请人： Michael Bos

    发明人： Michael Bos

    IPC分类号： A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/4045 ,  A61P1/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/12 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  A61P25/28 ,  A61P43/00 ,  C07D209/04 ,  C07D209/08 ,  C07D209/24 ,  C07D209/30 ,  C07D209/36

    CPC分类号： C07D209/36 ,  C07D209/08

    摘要： The invention releates to indole derivatives of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl or trifluoromethyl, R.sup.5 and R.sup.6 are, independently, hydrogen, halogen, lower-alkyl, cycloalkyl, trifluoromethyl, hydroxy or lower-alkoxy and R.sup.7 is hydrogen or lower-alkyl, andpharmaceutically acceptable acid addition salts thereof.The compounds of formula I bind to serotonin receptors and are therefore useful in the treatment and/or prevention of central nervous system disorders, such as depression.

    摘要翻译： 本发明涉及式I的吲哚衍生物，其中R 1至R 4独立地为氢，卤素，低级烷基，环烷基或三氟甲基，R 5和R 6独立地为氢，卤素，低级烷基，环烷基， 三氟甲基，羟基或低级烷氧基，且R 7为氢或低级烷基，及其药学上可接受的酸加成盐。 式I的化合物结合5-羟色胺受体，因此可用于治疗和/或预防中枢神经系统疾病如抑郁症。

    Chromogenic compounds and methods of using same
    59.
    发明授权
    Chromogenic compounds and methods of using same 失效
    显色化合物及其使用方法

    公开(公告)号：US5364767A

    公开(公告)日：1994-11-15

    申请号：US16511

    申请日：1993-02-11

    申请人： Daniel G. Flowers ,  Marvin Sternfeld

    发明人： Daniel G. Flowers ,  Marvin Sternfeld

    IPC分类号： C07D209/36 ,  C07H17/02 ,  C12Q1/04 ,  C12Q1/34 ,  C12Q1/06 ,  C07H15/00 ,  C12Q1/54

    CPC分类号： C12Q1/04 ,  C07D209/36 ,  C07H17/02 ,  C12Q1/34 ,  C12Q2334/50

    摘要： The present invention relates to chromogenic compounds which are represented by the general Formula (I): ##STR1## wherein R.sub.1 is a sugar group, ester group, hydrocarbyl group, phosphate group, sulfate group or a salt thereof, with the proviso that R.sub.1 is other than .beta.-D-glucuronic acid or .beta.-D-galactopyranoside, R.sub.2 is H or hydrocarbyl group containing 1 to about 5 carbon atoms, X is Cl or H, and Y is Cl or H. The present invention further relates to a method for quantitatively identifying and differentiating a first biological material having enzyme specificity for a first chromogenic compound as represented by Formula (I) above, and a second biological material having enzyme specificity for a second chromogenic compound.

    摘要翻译： 本发明涉及由通式（I）表示的显色化合物：其中R1是糖基，酯基，烃基，磷酸基，硫酸酯基或其盐，条件是 R1不是β-D-葡萄糖醛酸或β-D-吡喃半乳糖苷，R2是H或含有1到约5个碳原子的烃基，X是Cl或H，Y是Cl或H.本发明进一步涉及 涉及一种用于定量鉴定和鉴别具有上述式（I）所示的第一显色化合物的酶特异性的第一生物材料和对第二显色化合物具有酶特异性的第二生物材料的方法。