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    METHOTREXATE DERIVATIVES
    2.
    发明公开
    METHOTREXATE DERIVATIVES 审中-公开
    甲基磺酸酯衍生物

    公开(公告)号：EP1135390A1

    公开(公告)日：2001-09-26

    申请号：EP99960710.4

    申请日：1999-12-03

    申请人： COMMONWEALTH SCIENTIFIC AND INDUSTRIAL RESEARCH ORGANISATION

    发明人： WHITTAKER, Robert, George ,  WELLS, Xanthe, E. ,  REILLY, Wayne, Gerrard

    IPC分类号： C07D475/08 ,  A61K31/519 ,  A61P17/06 ,  A61P35/00 ,  A61P19/02 ,  A61P29/00 ,  A61P37/02

    CPC分类号： C07D475/08

    摘要： Methotrexate conjugates of formula (I) are disclosed as well as their use in the treatment of a disease with an autoimmune component and cancers. A particular example of a compound of formula (I) is methotrexate-η-glycine Tris, in which M is methotrexate or an analogue thereof; A=H, CX2-O-R2 or halogen; B=H, CX2-O-R3 or halogen; X is independently H or halogen; n is 0 or greater than or equal to 1; Y is a linker group, and where n is greater than 1, each Y is the same or different; R1, R2, and R3 are the same or different and are either hydrogen, substituted or unsubstituted methyl, ethyl, a saturated or unsaturated fatty acyl group, with the proviso that when n is 0 or 1, and A is CH2-O-R2 and/or B is CH2-O-R3, then R1, R2 and R3 are not selected from a fatty acyl group; with the proviso that when n is greater than or equal to 2, and A is CH2-O-R2 and/or B is CH2-O-R3, and at least one of R1, R2 and R3 is a fatty acyl group, then -[Y]n- is other than -(AA)n- or -Y-(AA)n-1-, where AA is an amino acid.

    摘要翻译： 公开了式（I）甲氨蝶呤缀合物以及它们在治疗具有自身免疫组分和癌症的疾病中的用途。 式（I）化合物的具体实例是甲氨蝶呤-η-甘氨酸Tris，其中M是甲氨蝶呤或其类似物; A = H，CX 2 -O-R 2或卤素; B = H，CX 2 -O-R 3或卤素; X独立地为H或卤素; n是0或大于或等于1; Y是连接基团，当n大于1时，每个Y可以相同或不同; R 1，R 2和R 3相同或不同，并且是氢，取代或未取代的甲基，乙基，饱和或不饱和脂肪酰基，条件是当n是0或1时，A是CH 2 -O-R 2 和/或B是CH2-O-R3，则R1，R2和R3不选自脂肪酰基; 条件是当n大于或等于2并且A是CH 2 -O-R 2和/或B是CH 2 -O-R 3且R 1，R 2和R 3中的至少一个是脂肪酰基时，则 - [Y] n - 不是 - （AA）n - 或-Y-（AA）n-1，其中AA是氨基酸。

    THERAPEUTIC COMPOUND - FATTY ACID CONJUGATES
    3.
    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。