CAS: 58717-02-5; (R)-2-Amino-3-Cyclohexylpropanoic Acid

相似化合物

151899-07-9 27527-05-5 4441-50-3

上下游产品

CAS号127095-92-5 N-B°C-3-环己基-D-丙氨酸

D-苯丙氨酸置于platinum(Iv) Oxide 氢气,三氟乙酸体系中,用 水 作为反应溶剂,60.0 °C,344.74 Kpa 条件下,反应 4.0H,反应生成 (2R)-2-氨基-3-环己基丙酸
参考文献:大环化合物ac-Phe-[orn-Pro-D-Cha-Trp-Arg](一种有效的新型抗炎药)的收敛性溶液相合成.
标题:大环化合物ac-Phe-[orn-Pro-D-Cha-Trp-Arg](一种有效的新型抗炎药)的收敛性溶液相合成.
摘要:在过去的十年中,相对较少的环肽进入了制药市场,大多数是通过发酵而不是合成制备的.通常,这类化合物是通过固相方法以毫克级为研究目的合成的,但是如果要实现大环肽模拟物的潜力,则需要设计和优化低成本的大规模溶液相合成方法,以提供足够的用于临床前,临床和商业用途的数量.在这里,我们描述了人类c5A受体的第一个报道的高效,选择性和口服活性拮抗剂的廉价,中等规模的溶液相合成方法.这种化合物ac-Phe [orn-Pro-D-Cha-Trp-Arg],称为3D53,是人血浆蛋白c5A的大环肽模拟物,在许多人类疾病的动物模型中显示出出色的抗炎活性.在收敛方法中,首先通过使用混合酸酐法的高产率溶液相偶联制备了两个三肽片段ac-Phe-Orn(boc)-Pro-Oh和hd-Cha-Trp(for)-Arg-Oet偶联它们以得到线性六肽,在脱保护后,其可从市售氨基酸中以38%的总产率获得.HPLC纯化后,使用b
DOI:10.1021/jo034228R

专利信息

专利号:US-2023037284-A9
优先权日:2018-11-30
标题:Combination therapy of peptidomimetic macrocycles
发明人：GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-2025084410-A1
优先权日:2015-01-12
标 题:Incorporation of unnatural nucleotides and methods thereof
发明人：PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E
权利人:SYNTHORX INC
摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.

专利号:US-2016319312-A1
优先权日:2013-07-29
标 题 :Synthesis method for l-cyclic alkyl amino acid and pharmaceutical composition having thereof
发明人：HONG HAO; ZHENG CHANGSHENG; GUO LINA
权利人:ASYMCHEM LABORATORIES (TIANJIN) CO LTD; ASYMCHEM LIFE SCIENCE (TIANJIN) CO LTD; TIANJIN ASYMCHEM PHARMACEUTICAL CO LTD; ASYMCHEM LABORATORIES (FUXIN) CO LTD; JILIN ASYMCHEM LABORATORIES CO LTD
摘要:A synthesis method for L-cyclic alkyl amino acid and a pharmaceutical composition having the said amino acid are provide in the present disclosure provides. The synthesis method comprises: step A.) preparing a cyclic alkyl keto acid or a cyclic alkyl keto acid salt having Structural Formula (I) or Structural Formula (II), and step B.) mixing the cyclic alkyl keto acid or the cyclic alkyl keto acid salt with ammonium formate, a leucine dehydrogenase, a formate dehydrogenase and a coenzyme NAD + , and carrying out a reductive amination reaction to generate the L-cyclic alkyl amino acid, wherein the Structural Formula (I) is n n n n n n n n n n where n 1 ≧1, m 1 ≧0 and the M 1 is H or a monovalent cation; the Structural Formula (II) is n n n n n n n n n n where n 2 ≧0, m 2 ≧0, the M 2 is H or a monovalent cation, an amino acid sequence of the leucine dehydrogenase is SEQ ID No.1.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:WO-2021072167-A1
优先权日:2019-10-10
标 题:Compositions and methods for in vivo synthesis of unnatural polypeptides

专利号:US-11091522-B2
优先权日:2018-07-23
标题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.