CAS: 345627-80-7; N-(5-(((5-(Tert-Butyl)Oxazol-2-yl)Methyl)Thio)Thiazol-2-yl)Piperidine-4-Carboxamide

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CAS号345629-23-4 tert-butyl 4-((... | CAS号76779-98-1 1-azido-3,3-dim... | CAS号5469-26-1 1-溴频哪酮 | CAS号224441-73-0 5-(叔丁基)-2-(氯甲基)噁唑 | CAS号224436-97-9 5-{[(5-叔丁基-1,3-... | CAS号333389-44-9 2-氯-n-(3,3-二甲基-... | CAS号498-94-2 4-哌啶甲酸 | CAS号84358-13-4 1-B°C-4-哌啶甲酸 | CAS号13547-70-1 一氯频哪酮

4-[[5-[[(5-叔丁基恶唑-2-基)甲基]硫基]噻唑-2-基]氨基甲酰]哌啶-1-羧酸叔丁酯置于盐酸体系中,用 1,4-二氧六环,氯仿 作为反应溶剂,化学反应 14.0H,以13.3 G的收率获得产物n-[5-[(5-叔丁基-1,3-恶唑-2-基)甲硫基]-1,3-噻唑-2-基]哌啶-4-甲酰胺
参考文献:细胞周期蛋白依赖性激酶2的n-(环烷基氨基)酰基-2-氨基噻唑抑制剂.n-[5-[[[5-(1,1-二甲基乙基)-2-恶唑基]甲基]硫代]-2-噻唑基]-4-哌啶甲酰胺(bms-387032),一种高效且选择性的抗肿瘤药.
标题:细胞周期蛋白依赖性激酶2的n-(环烷基氨基)酰基-2-氨基噻唑抑制剂.n-[5-[[[5-(1,1-二甲基乙基)-2-恶唑基]甲基]硫代]-2-噻唑基]-4-哌啶甲酰胺(bms-387032),一种高效且选择性的抗肿瘤药.
摘要:发现具有含碱性胺的非芳香族酰基侧链的n-酰基-2-氨基噻唑是有效的,选择性的cdk2 / Cyce抑制剂,在小鼠中表现出抗肿瘤活性.特别是化合物21 [n-[5-[[[5-(1,1-二甲基乙基)-2-恶唑基]甲基]硫代]-2-噻唑基]-4-哌啶基芳酰胺,Bms-387032]被确定为具有atp竞争性和cdk2选择性的抑制剂,已被选作抗肿瘤药物进入1期人类临床试验.在无细胞酶分析中,21显示cdk2 / Cyce Ic(50)= 48 Nm,选择性分别是cdk1 / Cycb和cdk4 / Cycd的10倍和20倍.在一组12种无关的激酶上也具有很高的选择性.在a2780细胞毒性实验中建立了抗增殖活性,其中21个显示ic(50)= 95 Nm.代谢和药代动力学研究表明,21种在三种物种中的血浆半衰期为5-7小时,在小鼠(69%)和人(63%)血清中的蛋白结合率均较低.口服给予小鼠,大鼠
DOI:10.1021/jm0305568

专利信息

专利号:EP-2690438-A1
优先权日:2012-07-24
标题:Synthesis of diverse glycosylphosphatidylinositol glycans and glycolipids from toxoplasma gondii and their application as diagnostic markers and vaccines
发明人：AZZOUZ NAHID; GOETZE SEBASTIAN; SEEBERGER PETER H; SILVA DANIEL VARON; TSAI YU-HSUAN
权利人:MAX PLANCK GESELLSCHAFT
摘要:The present invention relates to the synthesis of compounds derived from glycosylphosphatidylinositol (GPI) glycolipids from Toxoplasma gondii and the resulting products obtained. These synthetic compounds are suitable for diagnosis of toxoplasmosis and for use as a vaccine against diseases caused by infection with T. gondii.

专利号:US-6544952-B1
优先权日:1994-03-15
标 题:Synthesis of glycoconjugates of the globo-H epitope and uses thereof
发明人：DANISHEFSKY SAMUEL J; LIVINGSTON PHILIP O; RAGUPATHI GOVINDASWAMI; KIM IN JONG; SCHER HOWARD; SLOVIN SUSAN
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides a method of synthesizing a compound having the structure:as well as other related glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefore, and in a method for preventing recurrence of epithelial cancer. The present invention also provides a vaccine comprising an amount of the compound described above effective to prevent the recurrence of cancer in a subject.

专利号:US-8729257-B2
优先权日:2009-07-17
标题 :Hybrid lipid compounds based on pentaerythritol, intermediates, preparation methods and use thereof
发明人：DAI ZHIFEI; LIANG XIAOLONG; YUE XIULI
权利人:DAI ZHIFEI; LIANG XIAOLONG; YUE XIULI; HARBIN INST OF TECHNOLOGY
摘要:This invention relates to a novel class of hybrid lipid compound based on pentaerythritol, their intermediates, preparation methods and uses thereof. Different kinds of functional groups such as alkyl chain, siloxane group, azobenzene, porphyrins, cholesterol, benzene ring and carboxyl were introduced into the four hydroxyl groups of pentaerythritol through chemical reaction to obtain the final hybrid lipid compounds based on pentaerythritol. Cerasomes prepared from such lipids have uniform size, silicate network surface, good stability and biocompatibility, and the leakage of drugs is not easy. The present liposome can be used as functional materials such as drugs or drug carriers, or used for optical storage and molecular devices, simulation, design and synthesis of artificial systems, nano-composite membrane materials and the removal of organic pollutants, etc., in addition, the preparation method of the present invention is simple, and it is easy for industrial production.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:US-6645935-B2
优先权日:1994-03-15
标 题:Synthesis of glycoconjugates of the lewis Y epitope and uses thereof
发明人：DANISHEFSKY SAMUEL J; BEHAR VICTOR; LLOYD KENNETH O
权利人:SLOAN KETTERING INST CANCER; UNIV COLUMBIA
摘要:The present invention provides a method of synthesizing an allyl pentasaccharide having the structure: n as well as related oligosaccharide ceramides and other glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefor, and in a method for preventing recurrence of epithelial cancer.

专利号:US-2010184989-A1
优先权日:2007-03-12
标 题 :De Novo Synthesis of Conjugates
发明人：RIGGS-SAUTHIER JENNIFER; DENG BO-LIANG; REN ZHONGXU; ZHANG WEN; GU XUYUAN; DUARTE FRANCO J
权利人:NEKTAR THERAPEUTICS
摘要:The invention provides methods for the preparation of small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a water-soluble oligomer composition. Such drugs are produced through modification of a synthetic pathway to attach the oligomer to an intermediate compound followed by completion of the synthetic path.