NOVEL ADENINE COMPOUND AND USE THEREOF
    1.
    发明申请
    NOVEL ADENINE COMPOUND AND USE THEREOF 失效
    新颖的化合物及其用途

    公开(公告)号:US20100256118A1

    公开(公告)日:2010-10-07

    申请号:US12793649

    申请日:2010-06-03

    摘要: A drug for topically administration which is effective as an antiallergic agent. The drug for topically administration contains as an active ingredient an adenine compound represented by the general formula (1): [wherein ring A represents a 6 to 10 membered, mono or bicyclic, aromatic hydrocarbon or a 5 to 10 membered, mono or bicyclic, aromatic heterocycle containing one to three heteroatoms selected among 0 to 2 nitrogen atoms, 0 or 1 oxygen atom, and 0 or 1 sulfur atom; n is an integer of 0 to 2; m is an integer of 0 to 2; R represents halogeno, (un)substituted alkyl, etc.; X1 represents oxygen, sulfur, NR1 (R1 represents hydrogen or alkyl), or a single bond; Y1 represents a single bond, alkylene, etc.; Y2 represents a single bond, alkylene, etc.; Z represents alkylene; and at least one of Q1 and Q2 represents —COOR10 (wherein R10 represents (un)substituted alkyl, etc.), etc.] or a pharmaceutically acceptable salt of the compound.

    摘要翻译: 用作局部给药的药物,其作为抗过敏剂有效。 用于局部给药的药物含有作为活性成分的由通式(1)表示的腺嘌呤化合物:[其中环A表示6至10元,单或双环,芳族烃或5至10元,单或双环, 含有1至3个选自0至2个氮原子,0或1个氧原子和0或1个硫原子的杂原子的芳族杂环; n为0〜2的整数, m为0〜2的整数; R代表卤代,(取代)烷基等; X1代表氧,硫,NR1(R1代表氢或烷基)或单键; Y1表示单键,亚烷基等; Y2表示单键,亚烷基等; Z表示亚烷基; 并且Q1和Q2中的至少一个表示-COOR 10(其中R 10表示(un)取代的烷基等)等)或该化合物的药学上可接受的盐。

    8-Oxoadenine Compound
    4.
    发明申请
    8-Oxoadenine Compound 审中-公开
    8-氧基腺嘌呤化合物

    公开(公告)号:US20070225303A1

    公开(公告)日:2007-09-27

    申请号:US10594074

    申请日:2005-03-25

    IPC分类号: A61K31/522 C07D473/34

    摘要: An 8-oxoadenine compound useful as an immuno-modulator having specific activity against Th1/Th2, specifically a prophylactic and therapeutic agent for a topical application for allergic diseases, viral diseases and cancers, which is represented by the following formula (1): wherein A is a group of a formula represented by the formula (2): wherein R2 is a substituted or unsubstituted alkyl group and so on, R3 is hydrogen atom or an alkyl group, R is a halogen atom and so on, n is 0˜2, X1 is oxygen atom, Z is straight or branched chain alkylene, and R1 is an alkyl group which is optionally substituted by hydroxy group, an alkoxy group, alkoxycarbonyl group and so on, or its pharmaceutically acceptable salt.

    摘要翻译: 可用作对Th1 / Th2具有比活性的免疫调节剂的8-氧基腺嘌呤化合物,特别是用于过敏性疾病,病毒性疾病和癌症的局部应用的预防和治疗剂,其由下式(1)表示:其中 A是由式(2)表示的式的基团:其中R 2是取代或未取代的烷基等,R 3是氢原子或 烷基,R为卤素原子等,n为0〜2,X 1为氧原子,Z为直链或支链亚烷基,R 1为 任选被羟基,烷氧基,烷氧基羰基等取代的烷基或其药学上可接受的盐。

    Macrolide derivatives
    6.
    发明授权
    Macrolide derivatives 失效
    大环内酯衍生物

    公开(公告)号:US08124744B2

    公开(公告)日:2012-02-28

    申请号:US12299229

    申请日:2007-05-01

    IPC分类号: C07H17/08

    摘要: Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

    摘要翻译: 由式(I)和式(IV)表示的化合物具有抑制MMP-9产生的活性,因此作为一种具有比常规MMP酶活性抑制剂更少副作用的药剂可用作致癌剂的预防和治疗药物 血管生成,慢性类风湿关节炎,经皮冠状动脉腔内血管成形术后血管内膜增厚,血管动脉粥样硬化,出血性中风,急性心肌梗塞,慢性心力衰竭,动脉瘤,肺癌转移,成人呼吸窘迫综合征,哮喘,间质性肺纤维化,慢性鼻鼻窦炎, 支气管炎或慢性阻塞性肺疾病(COPD)。

    MACROLIDE DERIVATIVES
    8.
    发明申请
    MACROLIDE DERIVATIVES 失效
    麦角糖衍生物

    公开(公告)号:US20090076253A1

    公开(公告)日:2009-03-19

    申请号:US12299229

    申请日:2007-05-01

    IPC分类号: C07H17/08

    摘要: Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

    摘要翻译: 由式(I)和式(IV)表示的化合物具有抑制MMP-9产生的活性,因此作为一种具有比常规MMP酶活性抑制剂更少副作用的药剂可用作致癌剂的预防和治疗药物 血管生成,慢性类风湿关节炎,经皮冠状动脉腔内血管成形术后血管内膜增厚,血管动脉粥样硬化,出血性中风,急性心肌梗塞,慢性心力衰竭,动脉瘤,肺癌转移,成人呼吸窘迫综合征,哮喘,间质性肺纤维化,慢性鼻鼻窦炎, 支气管炎或慢性阻塞性肺疾病(COPD)。

    Type 2 helper T cell-selective immune response suppressors
    9.
    发明授权
    Type 2 helper T cell-selective immune response suppressors 失效
    2型辅助性T细胞选择性免疫应答抑制剂

    公开(公告)号:US06376501B1

    公开(公告)日:2002-04-23

    申请号:US09582176

    申请日:2000-06-21

    IPC分类号: A61K3152

    摘要: The present invention relates to a type 2 helper T cell-selective immune response inhibitor, an immune response regulator and an anti-allergic agent, individually comprising, as an active ingredient, a purine derivative represented by General Formula (I): wherein R2 is hydrogen or a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; R6 is hydroxyl, amino or amino which is mono- or di-substituted by a hydrocarbon group(s); R8 is hydroxyl, mercapto, acyloxy or hydrocarbon group-substituting oxycarbonyloxy; and R9 is a hydrocarbon group in which —CH2— not directly bound to the purine skeleton may be substituted by CO, SO2, O or S, and C—H not directly bound to the purine skeleton may be substituted by N, C-halogen or C—CN; or its tautomer or a salt of the purine derivative or the tautomer.

    摘要翻译: 本发明涉及一种2型辅助性T细胞选择性免疫应答抑制剂,免疫应答调节剂和抗过敏剂,其各自包含作为活性成分的由通式(I)表示的嘌呤衍生物:其中R 2为氢 或其中不直接结合嘌呤骨架的-CH 2可以被CO,SO 2,O或S取代的烃基,并且不直接键合到嘌呤骨架上的CH可以被N,C-卤素或C-CN R6是羟基,被一个或多个烃基单取代或二取代的氨基或氨基; R8是羟基,巯基,酰氧基或烃基取代的氧羰基氧基; 并且R 9是其中不直接结合嘌呤骨架的-CH 2可以被CO,SO 2,O或S取代的烃基,并且不直接键合到嘌呤骨架上的CH可以被N,C-卤素或C- CN;或其互变异构体或嘌呤衍生物或互变异构体的盐。