CAS: 7146-15-8; H-D-Val-Ome.Hcl

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(S)-2-羟基-3-甲基丁酸甲酯置于sodium Azide,水,三乙胺体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 126.17H,反应生成 D-缬氨酸甲酯盐酸盐
参考文献:Tanji,Shigehisa; Kodaka,Yasutaka; Shibata,Takanori,Heterocycles,2000,Vol. 52,# 1,P. 151-158
标题:Tanji,Shigehisa; Kodaka,Yasutaka; Shibata,Takanori,Heterocycles,2000,Vol. 52,# 1,P. 151-158

专利信息

专利号:US-2020181095-A1
优先权日:2017-06-06
标题:Selective matrix metalloproteinase-13 inhibitors
发明人：FIELDS GREGG B; ROUSH WILLIAM R; CHOI JUN YONG; FUERST RITA
权利人:FLORIDA ATLANTIC UNIV BOARD OF TRUSTEES; SCRIPPS RESEARCH INST
摘要:We describe the use of comparative structural analysis and structure-guided molecular design to develop potent and selective inhibitors (10d and (S)-17b) of matrix metalloproteinase 13 (MMP-13). We applied a three-step process, starting with a comparative analysis of the X-ray crystallographic structure of compound 5 in complex with MMP-13 with published structures of known MMP-13 inhibitor complexes followed by molecular design and synthesis of potent, but non-selective zinc-chelating MMP inhibitors (e.g., 10a and 10b). After demonstrating that the pharmacophores of the chelating inhibitors (S)-10a, (R)-10a, and 10b were binding within the MMP-13 active site, the Zn2+ chelating unit was replaced with non-chelating polar residues that bridged over the Zn2+ binding site and reach into a solvent accessible area. After two rounds of structural optimization, these design approaches led to small molecule MMP-13 inhibitors 10d and (S)-17b which bind within the substrate-binding site of MMP-13 and surround the catalytically active Zn2+ ion without chelating to the metal. These compounds exhibit at least 500-fold selectivity versus other MMPs.

专利号:US-9422321-B2
优先权日:2010-09-07
标题 :Pyrimidine nucleoside derivatives, synthesis methods and uses thereof for preparing anti-tumor and anti-virus medicaments
发明人：CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE
权利人:CHANG JUNBIAO; AN HAOYUN; YU XUEJUN; GUO XIAOHE; HIGH & NEW TECH RES CENTER HENAN ACAD OF SCIENCES; ZHENGZHOU GRANLEN PHARMATECH LTD; UNIV ZHENGZHOU
摘要:The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, particularly compounds of the formula shown below: n nAlso disclosed are methods of preparation and uses for these compounds. The compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.

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:CN-108129404-B
优先权日:2018-01-30
标题 :Synthesis method of chiral piperazinone derivative

专利号:CN-102351931-B
优先权日:2010-09-07
标题:Pyrimidine nucleoside derivatives, synthesis method and application in preparation of antitumor and antiviral drugs