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26 条记录 (耗时 0.037 秒)

    Urea derivatives useful as synthetic intermediates
    5.
    发明授权
    Urea derivatives useful as synthetic intermediates 失效
    尿素衍生物可用作合成中间体

    公开(公告)号：US06730784B2

    公开(公告)日：2004-05-04

    申请号：US10147131

    申请日：2002-05-15

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D26530

    CPC分类号： C07D295/185 ,  C07C317/50 ,  C07C323/44 ,  C07C323/59 ,  C07C323/60 ,  C07C327/30 ,  C07C329/06 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2603/74 ,  C07D333/32

    摘要： Objects of the present invention are to create compounds having urea structure as basic structure and having a sulfur atom and an amide bond in side chains and to find pharmacological effects thereof, particularly TNF-&agr; production inhibitory effects. The present invention provides compounds represented by the following formula [I] wherein R1 is H, alkyl, aromatic, RA—CO—, RC—S— or the formula [II]; R2, R3 and R4 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 are H, alkyl, alkenyl, cycloalkyl, cycloalkenyl or aromatic; R5 and R6 can together form a nonaromatic heterocyclic ring; R7 is H, alkyl, cycloalkyl, hydroxy, mercapto, phenyl, RB—O—, RC—S—, RD—COS—, RE—OCO—, RF—N(RG)— or —CONHOH; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是产生具有尿素结构作为碱性结构并在侧链中具有硫原子和酰胺键的化合物，并找到其药理作用，特别是TNF-α产生抑制作用。本发明提供了由 下式[I]其中R 1是H，烷基，芳基，R A -CO-，R c -S-或式[II]; R 2，R 3和R 4是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6是H，烷基，烯基，环烷基，环烯基或芳族; R 5和R 6可以一起形成非芳族杂环; R 7是H，烷基，环烷基，羟基，巯基，苯基，R -O-，R C，-S-，R 6 -COS-，R e -OCO-，R F -N（R G） - 或-CONHOH; A 1和A 2是亚烷基。

    Angiogenesis inhibitors
    7.
    发明授权
    Angiogenesis inhibitors 有权

    公开(公告)号：US06444705B1

    公开(公告)日：2002-09-03

    申请号：US09823360

    申请日：2001-03-30

    申请人： Shiro Mita ,  Hidehito Matsuoka

    发明人： Shiro Mita ,  Hidehito Matsuoka

    IPC分类号： A61K31165

    摘要： A method for inhibiting angiogenesis comprising administering to a patient (mammal, such as a human) in need thereof, a pharmaceutically effective amount of an angiogenesis inhibitor containing a compound of formula (I) or a pharmaceutically acceptable salt thereof, either alone or in combination with a pharmaceutically acceptable carrier. The method of treatment may be used to treat diseases in which the angiogenesis participates, particularly retinal diseases such as diabetic retinopathy, macular degeneration, retinal vein occlusion and retinal artery occlusion, neovascular glaucoma and tumors such as hemangioma.

    Urea derivatives having nitrogen aromatic heterocycle
    8.
    发明授权
    Urea derivatives having nitrogen aromatic heterocycle 失效
    具有氮芳香杂环的脲衍生物

    公开(公告)号：US06420398B2

    公开(公告)日：2002-07-16

    申请号：US09775420

    申请日：2001-02-01

    申请人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    发明人： Shiro Mita ,  Masato Horiuchi ,  Masakazu Ban ,  Hiroshi Suhara

    IPC分类号： C07D21302

    CPC分类号： C07D213/40

    摘要： An object of the present invention is to provide novel urea derivatives which have TNF-&agr; production inhibitory effects and are useful as therapeutic agents for various diseases, particularly as therapeutic agents for autoimmune diseases such as rheumatoid arthritis. The urea derivatives according to the present invention are compounds represented by the formula [I] and salts thereof. In the formula, R1 is H, alkyl, phenyl or a group of the formula [`I]; R2 is H, alkyl, carboxyl or ester thereof or the like; R3 and R4 are each H, alkyl, cycloalkyl or the like; R5 is H, alkyl, hydroxy or the like; R6 is a nitrogen aromatic heterocycle; and A1 and A2 are alkylene.

    摘要翻译： 本发明的目的是提供具有TNF-α产生抑制作用的新型尿素衍生物，可用作各种疾病的治疗剂，特别是作为自身免疫疾病如类风湿性关节炎的治疗剂。 根据本发明的脲衍生物是由式[I]表示的化合物及其盐。 在该式中，R 1是H，烷基，苯基或式[Ⅷ]的基团。 R2是H，烷基，羧基或其酯等; R3和R4各自为H，烷基，环烷基等; R5是H，烷基，羟基等; R6是氮芳香杂环; 并且A1和A2是亚烷基。

    Therapeutic agent for glaucoma
    9.
    发明授权
    Therapeutic agent for glaucoma 失效
    青光眼治疗剂

    公开(公告)号：US06281208B1

    公开(公告)日：2001-08-28

    申请号：US08208497

    申请日：1994-03-10

    申请人： Shiro Mita ,  Eiichi Shirasawa

    发明人： Shiro Mita ,  Eiichi Shirasawa

    IPC分类号： A61K3154

    CPC分类号： A61K31/54 ,  Y10S514/913

    摘要： A therapeutic agent for glaucoma comprises (+)-(R)-3,4-Dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4-methylenedioxy) phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-3-oxo-2H-1,4-benzothiazine or its salt as active ingredient and pharmaceutically acceptable excipients. The therapeutic agent lowers the intraocular pressure upon topical or systemic administration.

    摘要翻译： 青光眼治疗剂包括（+） - （R）-3,4-二氢-2- [5-甲氧基-2- [3- [N-甲基-N- [2 - [（3,4-亚甲二氧基） 苯氧基]乙基]氨基]丙氧基]苯基] -4-甲基-3-氧代-2H-1,4-苯并噻嗪或其盐作为活性成分和药学上可接受的赋形剂。 治疗剂在局部或全身给药时降低眼内压。