CAS: 139022-25-6; Imidazo[1,2-A]Pyridine-6-Carboxylic Acid

相似化合物

132213-07-1 158001-04-8 136117-69-6

上下游产品

pyridinecarboxylatemethyl 6-imidazo1,2-apyridinecarboxylate methyl 6-aminonicotinoate 6-aminonicotinic acid 1-bromo-2,2-dimethoxyethanepyridinecarboxylatemethyl 6-imidazo1,2-apyridinecarboxylate N-(4-(5-(dimethylamino)pyrazin-2-ylsulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide N-(4-((3-(trifluoromethoxy)phenyl)sulfonyl)benzyl)imidazo[1,2-a]pyrimidine-6-carboxamide N-(4-(1-isopropyl-1H-pyrazol-4-ylsulfonyl)benzyl)imidazo[1,2-a]pyridine-6-carboxamide

咪唑并[1,2-A]吡啶-6-甲酸甲酯置于lithium Hydroxide体系中,用 四氢呋喃 用作溶剂,化学反应 0.5H,以74%的收率获得咪唑[1,2-A]吡啶-6-甲酸
参考文献:新型微管蛋白聚合抑制剂2-吲哚基恶唑啉的合成及生物学评价.发现作为口服活性抗肿瘤药的a-289099.
标题:新型微管蛋白聚合抑制剂2-吲哚基恶唑啉的合成及生物学评价.发现作为口服活性抗肿瘤药的a-289099.
摘要:由于铅化合物a-105972的结构改性,已发现一系列含吲唑啉的吲哚.该化合物通过在秋水仙碱位点结合抑制微管蛋白聚合而发挥其抗癌活性.A-289099被鉴定为对各种癌细胞系(包括表达mdr表型的癌细胞系)具有活性的口服活性抗有丝分裂剂.描述了a-289099的抗癌活性,药代动力学以及有效和对映选择性的合成.
Doi:10.1016/s0960-894X(01)00759-4

专利信息

专利号:WO-2025076501-A1
优先权日:2023-10-06
标题:High throughput parallel synthesis of small molecule degraders
发明人：SHAUM JAMIE; ERB MICHAEL A; STEEN ERICA
权利人:SCRIPPS RESEARCH INST
摘要:Disclosed herein are high throughput synthetic methods for the deliberate and prospective discovery of molecular glues which can be used to form composite protein-ligand surfaces that facilitate interfacial binding to other proteins over dispersed surfaces. In particular, this application discloses a high throughput approach using sulfur(VI) fluoride exchange (SuFEx) transformations and N-hydroxysuccinimide (NHS)-ester derived amide couplings to prospectively repurpose known ligands for a prolein-of-interest into degraders and compounds capable of inducing proximity to other proteins. Disclosed herein are methods of developing known ligands of a target protein into degraders of the target proteins. Further disclosed are methods of developing novel small molecule chromatin-competitive inhibitors of the eleven nineteen leukemia (ENL) YEATS domain into effective degraders of ENL.

专利号:US-12336981-B2
优先权日:2010-09-03
标题 :Compounds and compositions for the inhibition of NAMPT
发明人：BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; DRAGOVICH Peter; GOSSELIN FRANCIS; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; ROTH BRUCE; SMITH CHASE C; WANG ZHONGGUO; YUEN PO-WAI; ZHENG XIAOZHANG
权利人:VALO HEALTH INC; GENENTECH INC
摘要:The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below: