355016-52-3Relevant academic research and scientific papers
Development of Novel Phosphino-Oxazoline Ligands and Their Application in Asymmetric Alkynlylation of Benzylic Halides
Guo, Rui,Li, Junxia,Sang, Jiale,Xiao, Haijing,Zhang, Guozhu
supporting information, (2022/03/27)
A new set of stereochemically diverse phosphino-oxazoline ligands derived from simple L-amino acids and 2-(diphenylphosphaneyl)benzoic acid were developed. Those mono anionic tridentated N,N,P-ligands promote the Cu-catalyzed enantioselective radical coupling of terminal alkynes with a broad range of benzylic halides including benzo-fused cyclic α-halides and α-silyl benzyl halides in high yield and excellent enantioselectivity under mild reaction conditions. With multi distinct sites for structural modification, a diverse pool of chiral N,N,P-ligands is readily accessed, allowing for rapid optimization of the ligand structure for a specific substrate. Notably, the enantioselective alkynlylation of benzylic halides bonds in benzo-cyclic molecules has also been realized for the first time.
JAK kinase inhibitor and application
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Paragraph 0096-0097; 0102-0104, (2018/09/08)
The present invention discloses a compound having the following general formula (I). The present invention also discloses a JAK kinase inhibitor comprising the compound and application of the compoundin preparation of a medicament for treating JAK-associated diseases. The JAK kinase inhibitor can inhibit the biological activities of JAK1, JAK2, JAK3 and TYK2 kinases involved in various kinds of signal transduction, can effectively treat various inflammatory diseases and various JAK-mediated signal transduction-driven diseases, and has a very broad application prospect.
FUSED PHENYLALANINE DERIVATIVES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
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Page/Page column 41, (2008/06/13)
The present invention is directed to fused phenylalanine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Amino acid derivatives and use thereof as nep, ace and ece inhibitors
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, (2008/06/13)
Compounds of formula (I): 1 wherein0≦n≦3,0≦m≦6,R3 and R4 together form a phenyl ring,B represents a heteroaryl group,R1 and R2 represent a hydrogen atom or groups as defined in the description.
N-[2-(Indan-1-yl)-3-mercapto-propionyl] amino acids as highly potent inhibitors of the three vasopeptidases (NEP, ACE, ECE): In vitro and In vivo activities
Inguimbert, Nicolas,Poras, Hervé,Teffo, Franck,Beslot, Fran?oise,Selkti, Mohamed,Tomas, Alain,Scalbert, Elizabeth,Bennejean, Caroline,Renard, Pierre,Fournié-Zaluski, Marie-Claude,Roques, Bernard-Pierre
, p. 2001 - 2005 (2007/10/03)
We have previously reported the design of a lead compound 1a for the joint inhibition of neprilysin (NEP, EC 3.4.24.11), angiotensin converting enzyme (ACE, EC 3.4.15.1) and endothelin converting enzyme (ECE-1, EC 3.4.24.71), three metallopeptidases which are implicated in the regulation of fluid homeostasis and vascular tone. We report here the synthesis and biological activities of analogues derived from this lead with inhibitory potencies in the nanomolar range for the three enzymes. Compounds 8b and 15c are the most potent triple inhibitors described to date.
