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    NOVEL STEROID CARBAMATES AS POTENTIATING AGENTS
    97.
    发明公开
    NOVEL STEROID CARBAMATES AS POTENTIATING AGENTS 失效
    新STEROIDCARBAMATE作为增效

    公开(公告)号：EP0885239A1

    公开(公告)日：1998-12-23

    申请号：EP97901864.0

    申请日：1997-01-17

    申请人： Batra, Satish

    发明人： BATRA, Satish ,  CARLSSON, Jan-Inge ,  FEX, Thomas

    IPC分类号： A61K31 ,  C07J41 ,  C07J43

    CPC分类号： C07J41/005 ,  C07J43/003

    摘要： Novel potentiating steroid carbamates having the general formula (I) ST-OCONR1R2 wherein ST is a steroid or steroid derivative, R1 and R2 are the same or different, or may together form a ring, and R1, R2 is hydrogen or the group (i) wherein A is selected from a bond and an alkyl chain (optionally branched), and B1 and B2 are selected from a bond, a heteroatom such as N, O, S, an alkyl chain (optionally branched), a ring (optionally containing a heteroatom such as N, O, S), and C1, C2, C3 and C4 are selected from hydrogen, an alkyl chain (optionally branched), a carbocyclic/heterocyclic ring system, wherein 1-3 rings may be aromatic (optionally substituted), whereby all of B1 - B2 and C1 - C4 do not need to be present at the same time. Compounds wherein R1 and/or R2 contain an ionizable group can be in the form of addition salts with appropriate pharmaceutically acceptable inorganic or organic counterions. Pharmaceutical compositions comprising steroid carbamates according to formula (I). Methods of treatment comprising administration of steroid carbamates according to formula (I).

    THERAPEUTIC COMPOUND - FATTY ACID CONJUGATES
    100.
    发明公开
    THERAPEUTIC COMPOUND - FATTY ACID CONJUGATES 失效
    治疗复方 - 脂肪酸缀合物

    公开(公告)号：EP0804459A1

    公开(公告)日：1997-11-05

    申请号：EP96900469.0

    申请日：1996-01-15

    申请人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION

    发明人： WHITTAKER, Robert, George ,  BENDER, Veronika, Judith ,  REILLY, Wayne, Gerrard ,  MOGHADDAM, Minoo

    IPC分类号： C07K14 ,  A61K31 ,  A61K38 ,  A61K47 ,  A61P25 ,  A61P29 ,  A61P31 ,  A61P37 ,  C07C237 ,  C07D475 ,  C07D489 ,  C07H19 ,  C07J5 ,  C07J41 ,  C07K5 ,  C07K7

    CPC分类号： C07H19/06 ,  A61K38/00 ,  A61K47/54 ,  A61K47/542 ,  C07C237/22 ,  C07D475/08 ,  C07D489/02 ,  C07H19/04 ,  C07J41/005 ,  C07K5/00 ,  C07K5/06078 ,  C07K7/06

    摘要： The present invention relates to a range of therapeutic compounds conjugated to one to three acyl groups derived from fatty acids. The therapeutic compounds are selected from the following group: 1) the corticosterone family of drugs; 2) opioids and opioid antagonists; 3) antiviral nucleosides, such as AZT; 4) cyclosporins and related cyclopeptides; 5) folate antagonists including methotrexate, folic acid and folic acid analogues; 6) catecholamine precursors, such as DOPA and Dopamine, and catecholamines, such as adrenaline and noradrenaline and derivatives; and 7) alkylating agents containing a carboxylic acid group, such as chlorambucil and melphalan. The therapeutic compound is conjugated to the fatty acid(s) by a link which includes a tromethamine or ethanolamine derivative. In particular the present invention relates to altering the pharmacokinetic profile and mode of delivery of these therapeutic compounds by conjugating them to one, two or three acyl derivatives of fatty acids.

    摘要翻译： 本发明涉及与衍生自脂肪酸的一至三个酰基缀合的一系列治疗化合物。 治疗性化合物选自以下组：1）皮质酮家族的药物; 2）阿片类药物和阿片类拮抗剂; 3）抗病毒核苷，如AZT; 4）环孢菌素和相关的环肽; 5）叶酸拮抗剂，包括甲氨蝶呤，叶酸和叶酸类似物; 6）儿茶酚胺前体，如DOPA和多巴胺，以及儿茶酚胺类，如肾上腺素和去甲肾上腺素及其衍生物; 和7）含有羧酸基团的烷化剂，例如苯丁酸氮芥和美法仑。 治疗化合物通过包含氨丁三醇或乙醇胺衍生物的连接与脂肪酸缀合。 特别地，本发明涉及通过将这些治疗性化合物与一种，两种或三种脂肪酸的酰基衍生物缀合来改变这些治疗性化合物的药代动力学特征和递送模式。