125218-79-3Relevant academic research and scientific papers
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 102, (2021/02/19)
The present invention covers [1,2,4]triazolo[1,5-c]quinazolin-5-amine compounds of general formula (I) in which R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling, as a sole agent or in combination with other active ingredients.
CONDENSED RING HETEROCYCLIC COMPOUND
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Paragraph 0477, (2015/06/17)
The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. [wherein, R1 represents optionally substituted lower alkyl and the like, R2 represents optionally substituted lower alkyl and the like, R3 represents the formula (II): (wherein, n represents 0 or 1, R3a represents a hydrogen atom and the like, R3b represents a hydrogen atom and the like, and R3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W1 represents a nitrogen atom and the like, W2 represents a nitrogen atom and the like]
Its use as an inhibitor and JAK and SYK deriv. pyrroropyrazine
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Paragraph 0194; 0195; 0197, (2016/11/07)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
MACROCYCLIC BROAD SPECTRUM ANTIBIOTICS
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Page/Page column, (2014/05/25)
Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria.
NITROGEN-CONTAINING HETEROCYCLIC COMPOUND
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Paragraph 0739, (2013/03/26)
The present invention provides a novel compound having a superior activity as an ERR-alpha modulator and useful as an agent for the prophylaxis or treatment of ERR-alpha associated diseases. The present invention relates to a compound represented by the formula (1) wherein each symbol is as defined in the specification, or a salt thereof
3-amido pyrrolopyrazine JAK kinase inhibitors: Development of a JAK3 vs JAK1 selective inhibitor and evaluation in cellular and in vivo models
Soth, Michael,Hermann, Johannes C.,Yee, Calvin,Alam, Muzaffar,Barnett, Jim W.,Berry, Pamela,Browner, Michelle F.,Frank, Karl,Frauchiger, Sandra,Harris, Seth,He, Yang,Hekmat-Nejad, Mohammad,Hendricks, Than,Henningsen, Robert,Hilgenkamp, Ramona,Ho, Hoangdung,Hoffman, Ann,Hsu, Pei-Yuan,Hu, Dong-Qing,Itano, Andrea,Jaime-Figueroa, Saul,Jahangir, Alam,Jin, Sue,Kuglstatter, Andreas,Kutach, Alan K.,Liao, Cheng,Lynch, Stephen,Menke, John,Niu, Linghao,Patel, Vaishali,Railkar, Aruna,Roy, Douglas,Shao, Ada,Shaw, David,Steiner, Sandra,Sun, Yongliang,Tan, Seng-Lai,Wang, Sandra,Vu, Minh Diem
supporting information, p. 345 - 356 (2013/02/23)
The Janus kinases (JAKs) are involved in multiple signaling networks relevant to inflammatory diseases, and inhibition of one or more members of this class may modulate disease activity or progression. We optimized a new inhibitor scaffold, 3-amido-5-cycl
Pyrrolopyrazine Kinase Inhibitors
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, (2011/10/10)
The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q, R2, R3, and Y are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
HETEROCYCLIC COMPOUND HAVING HIV INTEGRASE INHIBITORY ACTIVITY
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Page/Page column 124, (2008/06/13)
A heterocyclic compound of the formula (I): wherein B1 is -C(R2)= or -N=; R1' is H, etc.; one of R1 and R2 is -Z1-Z2-Z3-R5 wherein Z1 and Z3 are independently single bond, optionally substituted alkylene, etc.; Z2 is single bond, optionally substituted alkylene, etc.; R5 is optionally substituted aryl, optionally substituted heteroaryl, etc., and the other of R1 and R2 is H; -A1- is -C(-Y)=C(-RA)-C(-R3)=C(-R4)-, etc. wherein Y is OH, etc.; RA is -COR7 wherein R7 is OH, etc.; one of R3 and R4 is carboxy, etc., and the other of R1 and R2 is H, etc, a prodrug thereof, a pharmaceutically acceptable salt thereof, and a solvate thereof, having an antiviral activity, more particularly, an inhibitory activity against HIV integrase, and a pharmaceutical composition containing the same, especially an anti-HIV drug.
CRYSTAL STRUCTURES OF TWO RETROPEPTIDES RELATED TO THE GLY-GLY AND ALA-ALA SEQUENCES
Masdouri, Larbi El,Aubry, Andre,Gomez, Emmanuel Jose,Vitoux, Bernard,Marraud, Michel
, p. 583 - 588 (2007/10/02)
We have solved the crystal structures of two retropeptides obtained by inversion of the N-terminal amide bond in the peptide Gly-Gly and L-Ala-L-Ala sequences protected on both ends by amide groups.This reversal does not significantly modify the dimensions of the amide groups.Both retropeptide molecules accomodate open conformations linked by intermolecular hydrogen bonds.
