883554-96-9Relevant academic research and scientific papers
PYRIDINE COMPOUND SUBSTITUTED WITH AZOLE
-
Paragraph 1052, (2020/07/07)
The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme. (in formula [I] above, the structure represented by formula [II] below: represents any of the structures represented by formula group [III] below: R1, R2, R3, and R4 independently represent a hydrogen atom, a fluorine atom, methyl, or the like, R5 represents any of the structures represented by formula group [IV]:
Structure–Activity Relationship Studies on (R)-PFI-2 Analogues as Inhibitors of Histone Lysine Methyltransferase SETD7
Lenstra, Danny C.,Damen, Eddy,Leenders, Ruben G. G.,Blaauw, Richard H.,Rutjes, Floris P. J. T.,Wegert, Anita,Mecinovi?, Jasmin
, p. 1405 - 1413 (2018/07/29)
SETD7 is a histone H3K4 lysine methyltransferase involved in human gene regulation. Aberrant expression of SETD7 has been associated with various diseases, including cancer. Therefore, SETD7 is considered a good target for the development of new epigenetic drugs. To date, few selective small-molecule inhibitors have been reported that target SETD7, the most potent being (R)-PFI-2. Herein we report structure–activity relationship studies on (R)-PFI-2 and its analogues. A library of 29 structural analogues of (R)-PFI-2 was synthesized and evaluated for inhibition of recombinantly expressed human SETD7. The key interactions were found to be a salt bridge and a hydrogen bond formed between (R)-PFI-2′s NH2+ group and SETD7′s Asp256 and His252 residue, respectively.
AZOLE-SUBSTITUTED PYRIDINE COMPOUND
-
Paragraph 0700; 0701, (2019/01/08)
The present invention provides a compound represented by formula [I'| shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme, wherein the structure represented by formula [III] shown below represents any of the structures represented by formula group [IV] shown below, wherein R1 represents a hydrogen atom, a fluorine atom, methyl, etc.; R2, R3, and R4 each independently represent a hydrogen atom, a fluorine atom, or methyl; W represents a single bond, C1-3alkanediyl, or the formula -O-CH2CH2-; and ring A represents (a) substituted C4-6cycloalkyl, (b) substituted 4- to 6-membered saturated nitrogen-containing heterocyclyl, (c) substituted phenyl, (d) substituted pyridyl, (e) substituted 2,3-dihydrobenzofuran, (f) 4- to 6-membered saturated oxygen-containing heterocyclyl, etc.
PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF DIABETES
-
Paragraph 0249; 0250; 0251, (2016/03/13)
An object is to provide a novel compound which has a glycogen synthase activation ability, but activates a receptor PPAR to a low degree and is highly safe. Provided is a compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: wherein Ar1 represents any one of the following rings (II) and (III): wherein R2 represents an alkyl group, and R3 represents a hydrogen atom or an alkyl group, and R1 represents any one of the following substituents (IV) and (V):
Design and synthesis of novel diamide derivatives of glycine as antihyperglycemic agents
Sharma, Radhika,Soman, Shubhangi S.
supporting information, p. 1307 - 1317 (2016/08/16)
DPP-4 inhibition is one of the most extensively explored approaches for the management of type 2 diabetes (T2D). Most DPP-4 inhibitors in the market contain a proline mimetic active pharmacophore. Herein, we report the design, synthesis, and preliminary e
Amides in one pot from Carboxylic Acids and Amines via Sulfinylamides
Bai, Jianfei,Zambron, Bartosz K.,Vogel, Pierre
supporting information, p. 604 - 607 (2014/04/03)
An efficient method has been developed for the direct amidification of carboxylic acids via sulfinylamides preformed in situ by the reaction of pure amines with prop-2- ene-1-sulfinyl chloride. The method can be applied to aliphatic acids, including pivalic acid, aromatic acids, and primary and secondary amines. It is compatible with acids bearing unprotected alcohol, phenol, and ketone moieties and applicable to the synthesis of peptides. It does not induce their a-epimerization.
NOVEL 3,5-DISUBSTITUED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF PROTEIN KINASES
-
Page/Page column 117, (2011/12/04)
The present invention provides, inter alia, compounds of formula ΙΑ,ΙΙΑ and III as protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
Design, Synthesis, and SAR of Potent and Selective Dipeptide-Derived Inhibitors for Dipeptidyl Peptidases
Senten, Kristel,Van der Veken, Pieter,De Meester, Ingrid,Lambeir, Anne-Marie,Scharpé, Simon,Haemers, Achiel,Augustyns, Koen
, p. 5005 - 5014 (2007/10/03)
In this paper we report the systematic search for new, potent, and selective DPP II inhibitors. A study of the structure-activity relationship was conducted starting from aminoacyl pyrrolidides as lead compounds. Rational exploration of the P1
