CAS: 129298-91-5; Tnp-470

上下游产品

CAS号4461-30-7 氯乙酰异氰酸酯 | CAS号35903-52-7 Fumagillol

📜氯乙酰异氰酸酯,5-甲氧基-4-[2-甲基-3-(3-甲基丁-2-烯基)环氧乙烷-2-基]-1-氧杂螺[2.5]辛烷-6-醇置于4-二甲氨基吡啶体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,以71%的收率获得4-羟基-Alpha-((乙基氨基)甲基)-苄醇盐酸盐
参考文献:Chemical Modification Of Fumagillin. I. 6-O-Acyl,6-O-Sulfonyl,6-O-Alkyl,And 6-O-(N-Substituted-Carbamoyl)Fumagillols.
标题:Chemical Modification Of Fumagillin. I. 6-O-Acyl,6-O-Sulfonyl,6-O-Alkyl,And 6-O-(N-Substituted-Carbamoyl)Fumagillols.
摘要:烟曲霉素(1)的降解产物烟曲霉醇(3)的羟基被酰化,磺酰化,烷基化或氨基甲酰化,并考察了所得产物的抗血管生成活性.这些化合物抑制了在大鼠角膜微囊中由碱性成纤维细胞生长因子诱导的血管生成以及体外血管内皮细胞的生长.其中,化合物2(agm-1470)被发现对血管内皮细胞生长具有最强的抑制作用,并被选为这一系列的候选药物进一步开发.
Doi:10.1248/cpb.40.96

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-11801232-B2
优先权日:2019-11-27
标 题 :Targeting of ARID1A-deficient cancers by inhibiting de novo pyrimidine synthesis pathway
发明人：HUANG GLORIA
权利人:UNIV YALE
摘要:This application relates to methods and kits for treating ARID1A-mutant tumors, cancers, or aberrantly proliferating cells and subjects harboring the tumors, cancers, or aberrantly proliferating cells. In particular, the methods provided include administering to the subject or cell an effective amount of a pyrimidine synthesis inhibitor and administering to the subject or cell an effective amount of a DNA repair inhibitor. The kits include a) a composition comprising a pyrimidine synthesis inhibitor and b) a composition comprising a DNA repair inhibitor.

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-2015217006-A1
优先权日:2014-02-06
标题:Al-f-18-labeled, al-f-19-labeled and ga-68-labeled gastrin-releasing peptide receptor (grpr)-antagonists for imaging of prostate cancer
发明人：MCBRIDE WILLIAM J; CHATALIC KRISTELL L S; HENDRIKS-DE JONG MARION; BOERMAN OTTO C; GOLDENBERG DAVID M
权利人:IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F-, 19 F- or 68 Ga-labeled molecules of use in PET, SPECT and/or MRI imaging of prostate cancer. Preferably, the 18 F, 19 F or 68 Ga is attached to a chelator moiety on a prostate cancer targeting molecule, more preferably a bombesin analog, more preferably a GRPR antagonist, most preferably JMV5132 or JMV4168. The 18 F or 19 F may form a complex with a group IIIA metal to promote binding to the chelators. The labeled molecules may be used to detect, diagnose and/or image prostate cancer, including metastatic prostate cancer, in vivo.

专利号:WO-9948868-A9
优先权日:1998-03-26
标 题 :Heterocyclic classes of compounds for the modulating tyrosine protein kinase
发明人：FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL
权利人:SUGEN INC; UNIV NEW YORK; MAX PLANCK INST FUR BIOCHEMIE; FONG ANNIE; HANNAH ALISON; HARRIS G DAVIS; HIRTH PETER; HUBBARD STEVEN R; LANGECKER PETER; LIANG CONGXIN; MCMAHON GERALD; MOHAMMADI MOOSA; SCHLESSINGER JOSEPH; SHAWVER LAURA K; SUN LI; TANG PENG C; ULLRICH AXEL
摘要:The invention relates to certain indolinone-based and pyrazolylamide-based compounds, their method of synthesis, and combinatorial libraries consisting of the compounds. The invention also relates to methods of modulating the function of protein kinases using these compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.

专利号:US-12180228-B2
优先权日:2019-06-05
标题:Compounds, conjugates, and compositions of epipolythiodiketopiperazines and polythiodiketopiperazines and uses thereof
发明人：MOVASSAGHI MOHAMMAD; OLSSON CHASE ROBERT; SCOTT TONY Z; CHEAH JAIME; PAYETTE JOSHUA NATHANIEL
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present disclosure provides, e.g., compounds, compositions, kits, methods of synthesis, and methods of use, involving epipolythiodiketopiperazines and polythiodiketopiperazines.