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    Immunosuppressive effects of pteridine derivatives
    31.
    发明申请
    Immunosuppressive effects of pteridine derivatives 审中-公开
    蝶啶衍生物的免疫抑制作用

    公开(公告)号：US20060189620A1

    公开(公告)日：2006-08-24

    申请号：US11275601

    申请日：2006-01-18

    Applicant: Mark Jozef Waer ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    Inventor： Mark Jozef Waer ,  Piet Andre Herdewijn ,  Wolfgang Pfleiderer

    IPC: A61K31/525 ,  C07D475/12

    CPC classification number: C07D475/10 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K38/13 ,  C07D471/04 ,  C07D475/04 ,  C07D475/08 ,  A61K2300/00

    Abstract: This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.

    Abstract translation: 本发明涉及一组三取代和四取代的蝶啶衍生物，其药学上可接受的盐，N-氧化物，溶剂化物，二氢和四氢衍生物和对映异构体，具有特别期望的药物性质，特别是高活性免疫抑制剂，因此是 可用于移植排斥和/或治疗某些炎性疾病的治疗。 这些化合物也可用于预防或治疗心血管疾病，过敏性疾病，中枢神经系统疾病和细胞增殖性疾病。

    Biopterin analogs
    32.
    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。

    Protein kinase inhibitors
    39.
    发明授权
    Protein kinase inhibitors 有权
    蛋白激酶抑制剂

    公开(公告)号：US08618106B2

    公开(公告)日：2013-12-31

    申请号：US13593674

    申请日：2012-08-24

    Applicant: Jean-Damien Charrier ,  Steve Durrant

    Inventor： Jean-Damien Charrier ,  Steve Durrant

    IPC: C07D475/12 ,  A61K31/519

    CPC classification number: C07D487/04

    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.

    Abstract translation: 一方面，本发明提供式I化合物或其药学上可接受的盐。 另一方面，本发明提供了治疗由蛋白激酶介导的疾病或病症的方法，其包括施用治疗有效量的本发明化合物。

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