- [1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
-
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.
- -
-
Page/Page column 347-348
(2021/02/19)
-
- Structure-activity relationship studies and biological characterization of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors
-
The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 2 production in A549 lung cancer and LNCaP prostate cancer cells.
- Duveau, Damien Y.,Yasgar, Adam,Wang, Yuhong,Hu, Xin,Kouznetsova, Jennifer,Brimacombe, Kyle R.,Jadhav, Ajit,Simeonov, Anton,Thomas, Craig J.,Maloney, David J.
-
supporting information
p. 630 - 635
(2014/01/23)
-
- Narrow SAR in odorant sensing Orco receptor agonists
-
The systematic exploration of a series of triazole-based agonists of the cation channel insect odorant receptor is reported. The structure-activity relationships of independent sections of the molecules are examined. Very small changes to the compound structure were found to exert a large impact on compound activity. Optimal substitutions were combined using a 'mix-and-match' strategy to produce best-in-class compounds that are capable of potently agonizing odorant receptor activity and may form the basis for the identification of a new mode of insect behavior modification.
- Romaine, Ian M.,Taylor, Robert W.,Saidu, Samsudeen P.,Kim, Kwangho,Sulikowski, Gary A.,Zwiebel, Laurence J.,Waterson, Alex G.
-
p. 2613 - 2616
(2014/06/09)
-
- Pyrimidine Derivatives and Related Compounds. Part 45. Synthesis of 4-Allophanoylpyrazoles via a Pyrimidine-to-pyrazole Ring Transformation
-
Reaction of the 5-formyluracil derivatives (1a-f) with hydrazines in the presence of acetic acid produced a ring contraction to give the corresponding 4-allophanoylpyrazoles (2a-h).Further treatment of these pyrazoles (2a-h) with sodium methoxide afforded methyl pyrazole-4-carboxylate (3a).Conceivable mechanisms for the present pyrimidine-to-pyrazole transformation were discussed.
- Hirota, Kosaku,Kitade, Yukio,Shimada, Kaoru,Senda, Shiego,Maki, Yoshifumi
-
p. 1293 - 1298
(2007/10/02)
-