CAS: 19335-11-6; 5-Aminoindazole

上下游产品

CAS号5401-94-5 5-硝基吲唑 | CAS号55919-82-9 5-碘-1H-吲唑 | CAS号41330-49-8 ３-氯-１Ｈ-吲哚-５-苯胺 | CAS号21444-01-9 6H-吡唑[3,4-G]苯并噻唑-2-氨 | CAS号74626-47-4 吲唑-5-甲腈 | CAS号1150617-94-9 5-碘-2-甲基-2H-吲唑 | CAS号15579-15-4 1H-吲唑-5-醇 | CAS号166821-66-5 6-[(1H-indazol-... | CAS号78416-41-8 3,6-dihydropyrr... | CAS号78416-43-0 5-氨基-1H-吲唑-4-羧酸甲酯 | CAS号78416-44-1 3,6-dihydropyra...

4-硝基-2-甲苯胺置于palladium 10% On Activated Carbon,氢气,溶剂黄146,Sodium Nitrite体系中,用 甲醇 用作溶剂,25.0~40.0 °C,206.85 Kpa 条件下,反应 72.0H,反应生成5-氨基吲唑
参考文献:具有吲哚美辛-嘧啶类衍生物作为抗癌剂的设计,合成和生物学评估,具有抗血管生成和抗增殖活性†
标题:具有吲哚美辛-嘧啶类衍生物作为抗癌剂的设计,合成和生物学评估,具有抗血管生成和抗增殖活性†
摘要:设计,合成了三种基于吲哚-嘧啶的新型化合物,并将其作为vegfr-2激酶抑制剂进行了生物学评估.针对显示ic 50为1.37μm的huvec细胞系,进一步评估了活性最高的化合物6I(ic 50 = 24.5 Nm).此外,它通过抑制前列腺癌细胞中vegf和tgf-B1的分泌显示出间接的抗血管生成作用.Nci选择了五种化合物以评估其对10μm细胞系完整nci面板的体外抗癌活性.进一步选择化合物6E和6F进行5剂量测试.化合物6E表现出纳摩尔gi 50对几种细胞系的值:Ccrf-Cem(901 Nm),Molt-4(525 Nm)和caki-1(992 Nm),对其余细胞系的数微摩尔活性为1.05μm至2.41μm.化合物6F对整个细胞系范围从1.55μm到7.4μm表现出一位微摩尔活性.使用autodock软件,进行了分子对接研究以研究目标化合物与vegfr-2的预测结合模式.此外,对化合物
Doi:10.1039/c5Md00602C

专利信息

专利号:US-9890126-B2
优先权日:2012-04-24
标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF)
发明人：HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W
权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP
摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.

专利号:US-8188113-B2
优先权日:2006-09-14
标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC
摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:UA-77396-C2
优先权日:2000-05-09
标题 :Anthranilamides as inhibitors of kdr and flt tyrosine kinase, intermediate substances used in synthesis of anthranilamides, pharmaceutical drug and used of anthranilamides for manufacturing pharmaceuticals

专利号:US-10233182-B2
优先权日:2014-04-04
标题 :Substituted spirocyclic inhibitors of autotaxin
发明人：BABISS LEE; CLARK MATTHEW; KEEFE ANTHONY D; MULVIHILL MARK J; NI HAIHONG; RENZETTI LOUIS; RUEBSAM FRANK; WANG CE; XIE ZHIFENG; ZHANG YING
权利人:X RX INC
摘要:The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.