专利号:US-2017342077-A1 优先权日:2016-05-24 标题 :Diazene directed modular synthesis of compounds with quaternary carbon centers 发明人:MOVASSAGHI MOHAMMAD; LINDOVSKA PETRA 权利人:MOVASSAGHI MOHAMMAD; LINDOVSKA PETRA 摘要:Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): n n n n n n n n n n wherein R 1 -R 5 and q are as defined independently for each occurrence herein. A wide variety of compounds can be accessed in this manner, including oligocyclotryptamines, where the stereochemistry of each subunit is beneficially secured before fragment coupling.
专利号:US-6703213-B2 优先权日:1998-02-02 标 题:Substrate analogs for MurG, methods of making same and assays using same 发明人:KAHNE SUZANNE WALKER; MEN HONGBIN; PARK PETER; GE MIN 权利人:UNIV PRINCETON 摘要:General methods for monitoring the activity of MurG, a GlcNAc transferase involved in bacterial cell wall biosynthesis, is disclosed. More particularly, the synthesis of simplified substrate analogs of Lipid I (the natural substrate for MurG), which function as acceptors for UDP-GlcNAc in an enzymatic reaction catalyzed by MurG, is described. Assays using the substrate analogs of the invention are further disclosed, which are useful for identifying a variety of other substrates, including inhibitors of MurG activity, for facilitating mechanistic and/or structural studies of the enzyme and for other uses. High throughput assays are also described.
专利号:US-2012245199-A1 优先权日:2009-12-23 标题:[4 [4-(aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(1h-pyrrolo-pyridin-yl)-methanones and synthesis thereof 发明人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG 权利人:CHOI-SLEDESKI YONG MI; NIEDUZAK THADDEUS R; POLI GREGORY B; SHUM PATRICK WAI-KWOK; STOKLOSA GREGORY T; ZHAO ZHICHENG; SANOFI SA 摘要:The present invention relates herein to compounds and compositions for the treatment and amelioration of inflammatory disease. Specifically the present invention relates to compounds that having a tryptase inhibition activity and the intermediates thereof, pharmaceutical compositions comprising such compounds, and a method of treating subjects suffering from a condition disease or disorder that can be ameliorated by the administration of an inhibitor of tryptase.
专利号:WO-2017205539-A1 优先权日:2016-05-24 标 题 :Diazene directed modular synthesis of compounds with quaternary carbon centers
专利号:US-2019119286-A1 优先权日:2017-10-13 标题:Diazene directed modular synthesis of compounds with quaternary carbon centers
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.
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合成参考文献
参考文献:10.1186/preaccept-1447819538129143|10.1186/s12934-014-0120-5 摘要:Ruth C, Buchetics M, Vidimce V, Kotz D, Naschberger S, Mattanovich D, Pichler H, Gasser B. Pichia pastoris Aft1 - a novel transcription factor, enhancing recombinant protein secretion. Microbial Cell Factories. 2014;13(1):120. doi: 10.1186/preaccept-1447819538129143.