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    Biopterin analogs
    2.
    发明授权
    Biopterin analogs 失效
    生物蝶呤类似物

    公开(公告)号：US4665182A

    公开(公告)日：1987-05-12

    申请号：US799285

    申请日：1985-11-19

    Applicant: Charles A. Nichol ,  John F. Reinhard, Jr. ,  Gary K. Smith ,  Eric C. Bigham

    Inventor： Charles A. Nichol ,  John F. Reinhard, Jr. ,  Gary K. Smith ,  Eric C. Bigham

    IPC: A61K31/505 ,  A61K31/519 ,  A61P25/00 ,  A61P43/00 ,  C07D241/26 ,  C07D475/04 ,  C07D475/08 ,  C07D475/12

    CPC classification number: C07D475/04 ,  C07D241/26 ,  C07D475/08

    Abstract: The compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, lower alkyl of 1-4 carbons, lower alkenyl of 2-4 carbons, --B--X--R.sup.5).sub.n, or --B--Z--B--X--R.sup.5 --.sub.n ; n=0 when X is halogen or n=1 when X is --O--, --NR.sup.6 -- (where R.sup.6 is hydrogen or lower alkyl of 1-4 carbons) or --S(O)q-- (where q=0 to 2); B is lower alkanyl (straight or branched) of 1-5 carbons; R.sup.5 is hydrogen, aralkyl of 7 to 12 carbons or alkyl of 1-10 carbons; Z is --O--, NR.sup.6 --, or --S(O)q--; R.sup.2 is hydrogen or lower alkyl of 1-4 carbons or lower alkenyl of 2-4 carbons or either R.sup.1 and R.sup.2 together with the carbon atom in the pteridine ring structures to which they are attached, form a spirocycloalkyl ring system having 3 to 7 carbon atoms; R.sup.3 and R.sup.4 are hydrogen or methyl; R.sup.2 and R.sup.3, together with the carbon atoms in the pteridine ring structure to which they are attached, form a cycloalkyl ring system having 5 to 7 carbon atoms; provided that at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is hydrogen, and further provided that one of R.sup.1, R.sup.2 and R.sup.3, R.sup.4 represents gem disubstitution; have been found to selectively cofactor the biological conversion of tyrosine to dopamine, and are useful in the treatment of diseases resulting from a deficiency of dopamine in the brain such as Parkinson's disease. A further aspect of this invention comprises novel compounds of formula (I) defined above with the proviso that when both R.sup.3 and R.sup.4 are methyl neither R.sup.1 and R.sup.2 may be methyl, and R.sup.1 and R.sup.2 may not both be hydrogen, or a pharmaceutically acceptable salt thereof.

    Abstract translation: 式（I）化合物其中R1是氢，1-4个碳的低级烷基，2-4个碳的低级链烯基，-B-X-R5）n或-B-Z-B-X-R5-n; 当X为卤素时，n = 0或当X为-O-，-NR 6 - （其中R 6为氢或1-4个碳的低级烷基）或-S（O）q - （其中q = 0至2 ）; B是1-5个碳原子的低级烷基（直链或支链）; R 5是氢，7-12个碳的芳烷基或1-10个碳的烷基; Z是-O-，NR6-或-S（O）q-; R2是氢或1-4个碳原子的低级烷基或2-4个碳原子的低级链烯基，或者R1和R2与它们连接的蝶啶环结构中的碳原子一起形成具有3-7个碳原子的螺环烷基环系统 原子 R3和R4是氢或甲基; R2和R3与它们连接的蝶啶环结构中的碳原子一起形成具有5至7个碳原子的环烷基环系统; 条件是R 1，R 2，R 3和R 4中的至少一个为氢，并且进一步规定，R 1，R 2和R 3，R 4中的一个表示宝石取代; 已被发现选择性地将酪氨酸转化为多巴胺的生物转化，并且可用于治疗由脑中的多巴胺缺乏引起的疾病，例如帕金森病。 本发明的另一方面包括上述定义的新的式（I）化合物，条件是当R 3和R 4都是甲基时，R 1和R 2可以是甲基，并且R 1和R 2不能都是氢，或其药学上可接受的盐 其中。

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