专利号:US-2024261416-A1 优先权日:2023-01-31 标题:Synthesis of novel cereblon e3 ligase ligands, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; XIE HAIBO; WU YUNXIANG; LIAO JUNZHUO; LI CHUNRONG; TANDON IRA; TANG HUA 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Provided herein are achiral cereblon (CRBN) ligands based on phenyl dihydrouracil that have optimal binding to CRBN without having chiral carbons. Also provided herein are the proteolysis targeting chimeras (PROTACs) comprising the CRBN ligands and a protein binder, pharmaceutical compositions containing the PROTACs, and methods of treating diseases using the PROTACs.
专利号:US-2009156465-A1 优先权日:2005-12-30 标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors 发明人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND 摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. 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-5321139-A 优先权日:1991-05-03 标题 :Process for the enantioselective synthesis of 2(R)-benzylsuccinic acid monoamide derivatives 发明人:LERCH ULRICH; JENDRALLA HEINER; SEURING BERNHARD; HENNING RAINER 权利人:HOECHST AG 摘要:Two processes are described for the preparation of the optically pure compounds of formula 1: (1) in which R1 and R2 are e.g. alkyl, R3 and R4 are e.g. hydrogen and R5 is e.g. hydrogen. Both processes include, as key steps, the enantioselective hydrogenation of a C=C double bond and the regioselective formation of a dicarboxylic acid monoamide derivative. In one process a phenylitaconic acid derivative is asymmetrically hydrogenated to give an optically active (R)-benzylsuccinic acid which is then converted to a diester, said diester being converted to the monoamide compound of formula 1. In the second process, a phenylitaconic acid derivative is converted to its anhydride, and the anhydride is then converted to a monoamide which is then asymmetrically hydrogenated to give the compound of formula 1.
专利号:US-8399502-B2 优先权日:2008-09-17 标 题 :Analogs of indole-3-carbinol and their use as agents against infection 发明人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN 权利人:JONG LING; JIANG FAMING; LI GAOQUAN; MORTELMANS KRISTIEN; STANFORD RES INST INT 摘要:Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2′-diindolylmethane, 2′,3-diindolylmethane, and 3,3′-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
专利号:WO-2019013789-A1 优先权日:2017-07-12 标 题 :ANTIMICROBIAL COMPOUNDS 发明人:REDDY HARIPRASADA R KANNA; SEBAHAR PAUL R; SERRANO CATHERINE M; LOOPER RYAN E 权利人:CURZA GLOBAL LLC; THE UNIV OF UTAH RESEARCH FOUNDATION 摘要:The invention relates to compounds of formula I or their pharmaceutically acceptable salts. The compounds of formula I are antimicrobial agents which inhibit, for example, Mycobacterium tuberculosis (Mtb) H37Ra. The compounds of formula I also have anti-tuberculous activity, exhibit limited cytotoxicity and inhibit protein synthesis. The invention also relates to methods of making compounds of formula I, as well as methods of using compounds of formula I for the treatment of bacterial infections, particularly tuberculosis.
专利号:US-2004254162-A1 优先权日:2001-07-16 标 题 :Oxazolidinone derivatives as antimicrobials 发明人:MEHTA ANITA; ARORA SUDERSHAN R; DAS BISJAWIT; RAY ABHIJIT; RUDRA SONALI; RATTAN ASHOK 摘要:The present invention relates to certain substituted phenyl oxazolidinones and to processes for the synthesis of the same. This invention also relates to pharma-ceutical compositions containing the compounds of the present invention as anti-microbials. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacterioides spp. and Clostridia spp. species, and acid fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.
[参考文献]: Burrows, Jn, Cumming, Jg, Fillery, Sm, Et Al. Modulators Of The Human Ccr5 Receptor. Part 1: Discovery And Initial Sar Of 1-(3,3-Diphenylpropyl)-Piperidinyl Amides And Ureas Bioorg. Med. Chem. Lett.15(1 )25-28(2005) [参考文献]: Reck, F., Alm, R., Brassil, P., Et Al.Novel N-Linked Aminopiperidine Inhibitors Of Bacterial Topoisomerase Type Ii: Broad-Spectrum Antibacterial Agents With Reduced Herg Activityj. Med . Chem.54(22)7834-7847(2011) [参考文献]: Shinichi Imamura, Et Al. Discovery Of A Piperidine-4-Carboxamide Ccr5 Antagonist (Tak-220) With Highly Potent Anti-Hiv-1 Activity. J Med Chem. 2006 May 4;49(9):2784-93.
合成参考文献
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