75250-52-1Relevant academic research and scientific papers
Discovery of a potent G-protein-coupled receptor 119 agonist for the treatment of type 2 diabetes
Pola, Suresh,Shah, Shailesh R.,Pingali, Harikishore,Zaware, Pandurang,Thube, Baban,Makadia, Pankaj,Patel, Hoshang,Bandyopadhyay, Debdutta,Rath, Akshyaya,Giri, Suresh,Patel, Jitendra H.,Ranvir,Sundar,Patel, Harilal,Kumar, Jeevan,Jain, Mukul R.
, (2021/03/30)
The ever-growing prevalence of Type-2 diabetes in the world has an urgent need for multiple orally effective agents that can regulate glucose homeostasis. G-Protein coupled receptor 119 (GPR 119) agonists have demonstrated the glucose-dependent insulin secretion and showed beneficial effects on glycemic control in humans and/or relevant animal models. Herein, we describe our efforts towards identification of a potent and oral GPR 119 agonist 13c (ZY-G19), which showed in vitro potency in the cell-based assay and in vivo efficacy without exerting any significant signs of toxicity in relevant animal models.
SUBSTITUTED CONDENSED THIOPHENES AS MODULATORS OF STING
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Page/Page column 132, (2019/12/04)
A compound of formula (I), wherein: R1 is selected from (i) H, (ii) C3-6cycloalkyl, (iii) C3-7heterocyclyl optionally substituted with a group selected from: methyl and ester, and (iv) linear or branched C1-4alkyl optionally substituted with a group selected from: alkoxy, amino, amido, acylamido, acyloxy, alkyl carboxyl ester, alkyl carbamoyl, alkyl carbamoyl ester, phenyl, phosphonate ester, C3-7heterocyclyl optionally substituted with a group selected from methyl and oxo, and a naturally occurring amino acid, optionally N-substituted with a group selected from methyl, acetyl and boc; A1 is CRA or N; A2 is CRB or N; A3 is CRC or N; A4 is CRD or N; where no more than two of A1, A2, A3, and A4 may be N; one or two of RA, RB, RC, and RD, (if present) are selected from H, F, Cl, Br, Me, CF3, cyclopropyl, cyano, OMe, OEt, CH2OH, CH2OMe and CH2NMe2; the remainder of RA, RB, RC, and RD, (if present) are H; Y is O, NH or CH2; RY is selected from: (RYA) and (RYB).
ANTI-BACTERIAL COMPOUNDS
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Page/Page column 117, (2017/06/28)
A compound of Formula (II): for use in the prevention or treatment of a bacterial infection.
Direct electrochemical α-cyanation of N-protected cyclic amines
Libendi, Samuel Shikuku,Demizu, Yosuke,Onomura, Osamu
experimental part, p. 351 - 356 (2009/03/12)
α-Cyanation of N-protected cyclic amines was achieved using a direct electrochemical method. Unsubstituted N-protected cyclic amines were easily cyanated at the α-position using an undivided cell in high yields; moreover, α-cyanation of α′-substituted pyrrolidine and α′-,β′- or γ-substituted piperidines smoothly proceeded in high yield and with high to excellent diastereoselectivity. α-Substituted N-cyano-pyrrolidines and -piperidines were also cyanated at the more substituted position (the α-position) using a divided cell with high yield and high regioselectivity.
GABA uptake inhibitors. Syntheses and structure-activity studies on GABA analogues containing diarylbutenyl and diarylmethoxyalkyl N-substituents
Falch,Krogsgaard-Larsen
, p. 69 - 77 (2007/10/02)
A number of analogues of GABA or β-alanine containing 4,4-diphenyl-3-butenyl (DPB), benzhydryl ethyl ether (BEE), or benzhydryl propyl ether N-substituents have been synthesized and tested as inhibitors of synaptosomal GABA uptake. Whereas the N-DPB and N
Organic Tellurium and Selenium Chemistry. Reduction of Tellurides, Selenides, and Selenoacetals with Triphenyltin Hydride
Clive, Derrick L. J.,Chittattu, Gim J.,Farina, Vittorio,Kiel, William A.,Menchen, Steven M.,et al.
, p. 4438 - 4447 (2007/10/02)
Preparative and mechanistic details are described for the conversion of selenides into hydrocarbons RH> by heating with triphenyltin hydride at about 120 deg C.The process has been extended to selenoacetals in a form that constitutes a reduction methods for carbonyl compounds RR'C(SePh)2 -> RR'CH2>.Selective reduction of selenoacetals in the presence of thioacetals is possible.Cold-labeled species can be prepared by using triphenyltin deuteride.Tellurides are available easily without problems arising from exposure to air provided that the work is done in a photographic darkroom equipped with a red safety light.These tellurides, as well as the corresponding dichlorides , are reduced under very mild conditions (25-80 deg C) by triphenyltin hydride.The selenium- and tellurium-based chemistry has been used for the unusual process of reducing an epoxide in the presence of a ketone carbonyl.
