专利号:RU-2144564-C1 优先权日:1998-10-13 标题:Dna fragment rhtb encoding synthesis of protein rhtb that determines resistance of bacterium escherichia coli to l-homoserine and method of l-amino acid producing
专利号:US-6660832-B1 优先权日:1999-08-20 标题:Macrocyclic compounds and preparation methods thereof 发明人:JEFFERSON ELIZABETH; SWAYZE ERIC EDWARD 权利人:ISIS PHARMACEUTICALS INC 摘要:The present invention is directed to macrocyclic compounds of the formula (I)wherein Q, X, R1 and R5 are as defined herein. Compounds of the invention are useful for therapeutic and prophylactic treatment of bacterial infection in mammals. Solid phase synthetic procedures are provided effecting synthesis of the macrocyclic rings attached to a solid support.
专利号:CN-104284891-A 优先权日:2012-03-17 标 题:Conformational Restricted Total Synthesis of Macrocyclic Compounds
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
[参考文献]: Luckose F, Et Al. Effects Of Amino Acid Derivatives On Physical, Mental, And Physiological Activities. Crit Rev Food Sci Nutr. 2015;55(13):1793-1144.
合成参考文献
参考文献:10.1007/s12668-023-01250-7 摘要:Hariri M, Alivirdiloo V, Ardabili NS, Gholami S, Masoumi S, Mehraban MR, Alem M, Hosseini RS, Mobed A, Ghazi F, Alipourfard I. Biosensor-Based Nanodiagnosis of Carcinoembryonic Antigen (CEA): an Approach to Classification and Precise Detection of Cancer Biomarker. BioNanoSci. 2023 Dec 06;14(1):429–46. doi: 10.1007/s12668-023-01250-7. 参考文献:10.1007/978-981-97-4239-4_1 摘要:Kamat S, Modi SK, Gaur S, Kumari M. Plant–Microbe Interaction: Stress Management for Sustainable Agriculture. 2024. In: Rhizosphere Biology.