CAS: 83915-83-7; (S)-1-((S)-6-Amino-2-(((S)-1-Carboxy-3-Phenylpropyl)Amino)Hexanoyl)Pyrrolidine-2-Carboxylic Acid Dihydrate

该化合物是一种抗生素,可转化酶,广泛用于治疗高血压和心脏衰竭,其二氢酸盐形式增强了稳定性和溶性,确保了持续的药用动力性能.该化合物表现出高度选择性,有效减少了血压,因为它阻止了将血管1转换为血管2.其特征清晰的晶体结构有助于可靠的配制和生产再生.利西诺普里二氢酸表现出有利的生物利用率和长期的半衰期,允许临床应用中一次性使用.二氢化合物形式还改善了制药加工过程中的处理特性.其功效和安全特征得到了广泛的临床数据的支持,成为心血管治疗的基石.

结构式图片

欧盟法规

ECHA物质C&L通报

合成工艺路线路线简述

    海关参考信息

    专利信息


    专利号:US-10973847-B2
    优先权日:2017-06-30
    标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
    发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R
    权利人:MASSACHUSETTS INST TECHNOLOGY
    摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

    专利号:US-2004033532-A1
    优先权日:2002-08-08
    标题 :Use of three-dimensional crystal structure coordinates to design and synthesize domain-selective inhibitors for angiotensin-converting enzyme (ACE)
    发明人:EHLERS MARIO R W; HOLMQUIST BARTON
    摘要:It has now been discovered that the use of the three-dimensional crystal structure coordinates of angiotensin-converting enzyme (ACE) will enable the design and synthesis, by means of computational chemistry and structure-guided drug design, of inhibitors of ACE that are highly selective and specific for either the N domain or the C domain of the enzyme, for the treatment of diverse diseases. The invention also relates to methods and processes for the structure-guided design and synthesis of dual N- and C-domain ACE inhibitors, and inhibitors that operate by competitive, non-competitive, uncompetitive, and irreversible mechanisms.

    专利号:US-6362009-B1
    优先权日:1997-11-21
    标 题 :Solid phase synthesis of heterocycles
    发明人:MUNOZ BENITO; CHEN CHIXU
    权利人:MERCK & CO INC
    摘要:Methods for solid phase and combinatorial synthesis using a resin activation/capture approach are provided. In particular, methods for the production of dihydropyridones, N-acyidihydropyridones, tetrahydropyridones, pyridines, aminopyridines, N-acyltetrahydropyridines and tetrahydropyridines compounds and libraries containing such compounds are provided. Methods for screening the libraries and compounds and pharmaceutical compositions containing compounds prepared by the methods are provided.

    专利号:US-2008300251-A1
    优先权日:2005-09-05
    标 题 :Derivatives of 3-Azabicyclo[3.1.0] Hexane as Dipeptidyl Peptidase-IV Inhibitors
    发明人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND
    权利人:SATTIGERI JITENDRA A; ANDAPPAN MURUGAIAH M S; KISHORE KAUSHAL; SETHI SACHIN; KANDALKAR SACHIN RAMESH; PAL CHANCHAL KUMAR; MAHAJAN DIPAK C; AHMED SHAHADAT; PARKALE SANTHOSH SADASHIV; SRINIVASAN T; SHARMA LALIMA; BANSAL VINAY S; CHUGH ANITA; DAVIS JOSEPH ALEXANAND
    摘要:The present invention relates to novel 3-azabicyclo[3.1.0]hexane derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the said compounds. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-7612106-B2
    优先权日:2004-12-23
    标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof
    发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU
    权利人:ARENA PHARM INC
    摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
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    主要参考文献


    1: Agarwal R, Sinha AD, Pappas MK, Abraham TN, Tegegne GG. Hypertension in hemodialysis patients treated with atenolol or lisinopril: a randomized controlled trial. Nephrol Dial Transplant. 2014 Mar;29(3):672-81. doi: 10.1093/ndt/gft515. Epub 2014 Jan 6.
    2: Yamal JM, Oparil S, Davis BR, Alderman MH, Calhoun DA, Cushman WC, Fendley HF, Franklin SS, Habib GB, Pressel SL, Probstfield JL, Sastrasinh S; ALLHAT Collaborative Research Group. Stroke outcomes among participants randomized to chlorthalidone, amlodipine or lisinopril in ALLHAT. J Am Soc Hypertens. 2014 Nov;8(11):808-19. doi: 10.1016/j.jash.2014.08.003. Epub 2014 Aug 19.
    3: Georgianos PI, Agarwal R. Effect of lisinopril and atenolol on aortic stiffness in patients on hemodialysis. Clin J Am Soc Nephrol. 2015 Apr 7;10(4):639-45. doi: 10.2215/CJN.09981014. Epub 2015 Mar 17.

    合成参考文献


    参考文献:10.1124/mol.119.115964
    摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
    参考文献:10.1007/s10973-025-14765-w
    摘要:Silva RC, Trevisan MG, Garcia JS. Characterization and study of drug–excipient compatibility of Lisinopril by TGA, FTIR and HPLC. J Therm Anal Calorim. 2025 Sep 23;150(19):15117–27. doi: 10.1007/s10973-025-14765-w.
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