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-2024209353-A1 优先权日:2021-04-08 标 题 :Nadk2 inhibition in cancer and fibrotic disorders 发明人:THOMPSON CRAIG B; SCHWOERER SIMON; ZHU JIAJUN 权利人:MEMORIAL SLOAN KETTERING CANCER CENTER; MEMORIAL HOSPITAL FOR CANCER AND ALLIED DISEASES; SLOAN KETTERING INST CANCER RES 摘要:Aspects of the disclosure provide methods for inhibiting cell proliferation and protein synthesis utilizing an antagonist of nicotinamide adenine dinucleotide kinase 2 (NADK2). In some aspects, these methods are used to treat a disease such as cancer or a disorder such as a fibrotic disorder. Further provided herein are compositions comprising a nutrient-deficient cell culture medium and an antagonist of NADK2.
专利号:RU-2166510-C2 优先权日:1993-02-22 标题 :Pseudodipeptides, methods of their synthesis, pharmaceutical compositions, methods of treatment
专利号:EP-2305808-B1 优先权日:2001-06-20 标 题:Templated molecules and methods for using such molecules 发明人:PEDERSEN HENRIK; GOULIAEV ALEX HAAHR; SAMS CHRISTIAN KLARNER; SLØK FRANK ABILGAARD; FRESKGÃ…RD PER-OLA; HOLTMANN ANETTE; OLSEN EVA KAMPMANN; HUSEMOEN GITTE NYSTRUP; FELDING JAKOB; FRANCH THOMAS; THISTED THOMAS; HYLDTOFT LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER 权利人:NUEVOLUTION AS 摘要:The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g . therapeutic activity.
专利号:US-9688980-B2 优先权日:2001-06-20 标 题 :Templated molecules and methods for using such molecules 发明人:PEDERSEN HENRIK; GOULIAEV ALEX HAAHR; FRANCH THOMAS; SAMS CHRISTIAN KLARNER; OLSEN EVA KAMPMANN; SLOK FRANK ABILGAARD; HUSEMOEN GITTE NYSTRUP; FELDING JAKOB; HYLDTOFT LENE; NORREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRODER; THISTED THOMAS; FRESKGARD PER-OLA; HOLTMANN ANETTE 权利人:NUEVOLUTION AS; NUEVOLUTION 摘要:The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The intion allows the generation of libraries which can be screened for e.g. therapeutic activity.
[参考文献]: Han Seul Park, Et Al. Distal γ-C(Sp 3 )-H Olefination Of Ketone Derivatives And Free Carboxylic Acids. Angew Chem Int Ed Engl. 2020 Jul 27;59(31):12853-12859.
合成参考文献
摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 214.