66183-73-1Relevant academic research and scientific papers
Synthesis of α-Ketoamide-Based Stereoselective Calpain-1 Inhibitors as Neuroprotective Agents
Jastaniah, Ammar,Gaisina, Irina N.,Knopp, Rachel C.,Thatcher, Gregory R. J.
, p. 2280 - 2285 (2020)
Calpain inhibitors have been proposed as drug candidates for neurodegenerative disorders, with ABT-957 entering clinical trials for Alzheimer's disease and mild cognitive impairment. The structure of ABT-957 was very recently disclosed, and trials were te
CARBOXAMIDE COMPOUNDS AND THEIR USE AS CALPAIN INHIBITORS
-
Page/Page column 144-145, (2010/11/18)
The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula (Ia) and (Ib) in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof. Of these compounds those are preferred wherein Y is a moiety CH2-CH2, CH2-CH2-CH2, N(Ry#)-CH2, N(Ry#)-CH2-CH2 or CH=CH-CH=, each optionally having 1 or 2 H-atoms replaced with identical or different radicals Ry, wherein Ry and Ry# have the meanings mentioned in the claims.
Enantiometric iodobenzamides.
-
, (2008/06/13)
Novel iodine-substituted benzamide derivatives of formula I wherein R1 is a hydrogen atom, a lower alkyl group consisting of 1 to 4 carbon atoms, a cycloalkyl group consisting of 3 to 7 carbon atoms, an alkenyl group consisting of 2 to 4 carbon atoms, an alkynyl group consisting of 2 to 4 carbon atoms, a phenyl group, a halogen substituted phenyl group, or an enantiomer or pharmaceutically suitable salt thereof, exhibit high blocking activity and specifity for the dopamine D-2 receptor.
