- IAP ANTAGONISTS AND THEIR THERAPEUTIC APPLICATIONS
-
The present invention relates to Formula I. compounds including their isomers, tautomeric forms and rotamers, salts together with their manufacturing process and their pharmacological use alone or in combination with other active ingredients for the treatment of cell and tissue malignances caused diseases, including uncontrolled cell or tissue growth, proliferation and cancer.
- -
-
Page/Page column 35-36
(2021/11/06)
-
- Small Molecule Inhibitors of Metabolic Enzymes Repurposed as a New Class of Anthelmintics
-
The enormous prevalence of infections caused by parasitic nematodes worldwide, coupled to the rapid emergence of their resistance to commonly used anthelmintic drugs, presents an urgent need for the discovery of new drugs. Herein, we have identified several classes of small molecules with broad spectrum activity against these pathogens. Previously, we reported the identification of carnitine palmitoyltransferases (CPTs) as a representative class of enzymes as potential targets for metabolic chokepoint intervention that was elucidated from a combination of chemogenomic screening and experimental testing in nematodes. Expanding on these previous findings, we have discovered that several chemical classes of known small molecule inhibitors of mammalian CPTs have potent activity as anthelmintics. Cross-clade efficacy against a broad spectrum of adult parasitic nematodes was demonstrated for multiple compounds from different series. Several analogs of these initial hit compounds were designed and synthesized. The compounds we report represent a good starting point for further lead identification and optimization for development of new anthelmintic drugs with broad spectrum activity and a novel mechanism of action.
- Tyagi, Rahul,Maddirala, Amarendar Reddy,Elfawal, Mostafa,Fischer, Chelsea,Bulman, Christina A.,Rosa, Bruce A.,Gao, Xin,Chugani, Ryan,Zhou, Mingzhou,Helander, Jon,Brindley, Paul J.,Tseng, Chih-Chung,Greig, Iain R.,Sakanari, Judy,Wildman, Scott A.,Aroian, Raffi,Janetka, James W.,Mitreva, Makedonka
-
p. 1130 - 1145
(2018/05/15)
-
- PIPERIDINE-AMIDE DERIVATIVES
-
The invention is concerned with novel piperidine-amide derivatives of formula (I) wherein R1, R2, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These comp
- -
-
-