67751-23-9Relevant articles and documents
A PESTICIDALLY ACTIVE MIXTURE COMPRISING PYRAZOLOPYRIDINE ANTHRANILAMIDE COMPOUND, OXIDES OR SALTS THEREOF
-
Page/Page column 83; 84, (2022/02/09)
The present invention relates to a pesticidal active mixture comprising pyrazolopyridine anthranilamide compound of formula (I), oxides or a salt thereof, Formula (I) wherein, R1, R2, R3, R4, Z and E are as defined in the description, and at least one insecticidally active compound (II) or at least one fungicidally active compound (III).
A Conformational Restriction Strategy for the Identification of a Highly Selective Pyrimido-pyrrolo-oxazine mTOR Inhibitor
Borsari, Chiara,Rageot, Denise,Dall'Asen, Alix,Bohnacker, Thomas,Melone, Anna,Sele, Alexander M.,Jackson, Eileen,Langlois, Jean-Baptiste,Beaufils, Florent,Hebeisen, Paul,Fabbro, Doriano,Hillmann, Petra,Wymann, Matthias P.
, p. 8609 - 8630 (2019/10/16)
The mechanistic target of rapamycin (mTOR) plays a pivotal role in growth and tumor progression and is an attractive target for cancer treatment. ATP-competitive mTOR kinase inhibitors (TORKi) have the potential to overcome limitations of rapamycin derivatives in a wide range of malignancies. Herein, we exploit a conformational restriction approach to explore a novel chemical space for the generation of TORKi. Structure-activity relationship (SAR) studies led to the identification of compound 12b with a ~450-fold selectivity for mTOR over class I PI3K isoforms. Pharmacokinetic studies in male Sprague Dawley rats highlighted a good exposure after oral dosing and a minimum brain penetration. CYP450 reactive phenotyping pointed out the high metabolic stability of 12b. These results identify the tricyclic pyrimido-pyrrolo-oxazine moiety as a novel scaffold for the development of highly selective mTOR inhibitors for cancer treatment.
PYRAZOLOPYRIDINE-DIAMIDES, THEIR USE AS INSECTICIDE AND PROCESSES FOR PREPARING THE SAME.
-
Page/Page column 78, (2019/07/13)
The present invention provides novel pyrazolopyridine-diamides of Formula (I), wherein, the definition of W1, W2, A1, A2, A3, B1, B2, D, Z1, E, R1, R2, R3, R4, m and n is as described in the description. The present invention also relates to the composition, combination, use and method of application of the compounds of Formula (I).