86601-75-4Relevant academic research and scientific papers
[1,2,4]TRIAZOLO[1,5-C]QUINAZOLIN-5-AMINES
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Page/Page column 246, (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.
New antimitotic agents with activity in multi-drug-resistant cell lines and in vivo efficacy in murine tumor models
Szczepankiewicz,Chiou,Credo,Alder,Nukkala,Zielinski,Jarvis,Mollison,Frost,Bauch,Hui,Liu,Claiborne,Li,Rosenberg,Jae,Tasker,Gunawardana,Von Geldern,Gwaltney II,Wu-Wong,Gehrke
, p. 4416 - 4430 (2007/10/03)
During a screen for compounds that could inhibit cell proliferation, a series of new tubulin-binding compounds was identified with the discovery of oxadiazoline 1 (A-105972). This compound showed good cytotoxic activity against non-multi-drug-resistant and multi-drug-resistant cancer cell lines, but its utility in vivo was limited by a short half-life. Medicinal chemistry efforts led to the discovery of indolyloxazoline 22g (A-259745), which maintained all of the in vitro activity seen with oxadiazoline 1, but also demonstrated a better pharmacokinetic profile, and dose-dependent in vivo activity. Over a 28 day study, indolyloxazoline 22g increased the life span of tumor-implanted mice by up to a factor of 3 upon oral dosing. This compound, and others of its structural class, may prove to be useful in the development of new chemotherapeutic agents to treat human cancers.
Decomposition of 2-dialkylaminobenzoyl azides to yield isocyanates and 1,1 -dialky lindazol-1-ium-3-olates
Waldron, Norman M.,Raza, Muhammad
, p. 271 - 276 (2007/10/03)
Substituted benzoyl azides normally yield the correspondingly substituted isocyanates but when a dialkylated amino group is in the 2-position, in addition to the isocyanate, the 1,1-dialkylated indazol-1-ium-3-olate is produced. The ratio of the two products is very variable depending upon the substitution in the benzene ring. Largest yields of the zwitterionic products were found when there was a substituent in the 3-position regardless of whether the substituent was electron-donating or -withdrawing.
