Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins
    6.
    发明申请
    Medium and method for enriching, purifying or depleting atp binding proteins from a pool of proteins 审中-公开
    用于从蛋白质池中富集,纯化或消耗atp结合蛋白的培养基和方法

    公开(公告)号:US20060105445A1

    公开(公告)日:2006-05-18

    申请号:US10523577

    申请日:2003-07-29

    IPC分类号: C12N9/12 C07K14/705

    摘要: The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-1H-imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)-phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1H-indole-3-yl)maleinmide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-3-(1H-indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]4-(1-methyl-1H-indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2-a]-indol-10-yl) (1-methyl-1H-indol -3-yl)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-1-yl-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases from a pool of heterogeneous proteins.

    摘要翻译: 本发明涉及一种培养基和一种富含ATP结合蛋白的方法, 蛋白质蛋白酶,来自蛋白质库,如蛋白质组。 本发明的培养基包含特异性抑制剂,例如, 至少一种化合物4- [4-(4-氟 - 苯基)-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺,2- [4-(2-氨基 - 乙氧基) - 苯基氨基] -6-(2,6-二氯 - 苯基)-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮,2- [1-(3-氨基丙基)-1H-吲哚 -3-(3-氨基丙基)-1H-吲哚-3-基] -3-(1H-吲哚-3-基) - 马来酰亚胺,3- [1-(3-氨基丙基) -1H-吲哚-3-基] 4-(1-甲基-1H-吲哚-3-基)马来酰亚胺,3-(8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a] - 吲哚-10-基)(1-甲基-1H-吲哚-3-基) - 马来酰亚胺,[6-(3-氨基 - 丙氧基) - 甲氧基 - 喹唑啉-4-基] - (3-氯 - 苯基) - 胺,6-(3-氨基 - 丙氧基)-7-甲氧基 - 喹唑啉-4-基 - (3-氯-4-氟 - 苯基) - 胺,6-(3Amin-丙氧基)-7-甲氧基 - 喹唑啉 -4-基] - (3-溴 - 苯基) - 胺和4- [4-(4-氨基 - 丁基) - 哌嗪-1-基 - 甲基] -N- [4-甲基-3-(4- 吡啶-3-基 - 嘧啶-2-基氨基) - 苯基] - 苯甲酰胺固定在载体材料上。 根据本发明的方法,上述固定化化合物用于选择性地结合来自异质蛋白库的蛋白激酶。

    Napthyridine Compounds As Rock Inhibitors
    7.
    发明申请
    Napthyridine Compounds As Rock Inhibitors 审中-公开
    萘啶化合物作为岩石抑制剂

    公开(公告)号:US20080207677A1

    公开(公告)日:2008-08-28

    申请号:US11813236

    申请日:2006-01-02

    CPC分类号: C07D471/04

    摘要: The present invention relates to compounds having a naphthyridine scaffold, and stereoisomeric forms, prodrugs, solvates, hydrates and/or pharmaceutically acceptable salts of these compounds as well as pharmaceutical compositions containing at least one of these naphthyridine derivatives together with pharmaceutically acceptable carrier, excipient and/or diluents. Said naphthyridine compounds have been identified as inhibitors of the protein kinase ROCK2, also known as Rho-kinase, and are useful for the treatment of cancers (tumor growth and metastases), erectile dysfunction, cardiovascular diseases, hypertension, angina pectoris, cerebral ischaemia, cerebral vasospasm, myocardial ischaemia, coronary vasospasm, heart failure, myocardial hypertrophy, atherosclerosis, restenosis, spinal cord injuries, neuronal degeneration, thrombotic disorders, asthma, glaucoma, inflammation, anti-viral diseases (e.g. HIV), and osteoporosis.

    摘要翻译: 本发明涉及具有萘啶支架的化合物,以及这些化合物的立体异构形式,前体药物,溶剂合物,水合物和/或药学上可接受的盐,以及含有这些萘啶衍生物中至少一种以及药学上可接受的载体,赋形剂和 /或稀释剂。 所述萘啶化合物已被鉴定为蛋白激酶ROCK2(也称为Rho-激酶)的抑制剂,可用于治疗癌症(肿瘤生长和转移),勃起功能障碍,心血管疾病,高血压,心绞痛,脑缺血, 脑血管痉挛,心肌缺血,冠状动脉血管痉挛,心力衰竭,心肌肥大,动脉粥样硬化,再狭窄,脊髓损伤,神经元变性,血栓形成障碍,哮喘,青光眼,炎症,抗病毒疾病(例如HIV)和骨质疏松症。