Back to results
US 8,372,848 B2Granted
Melanin-concentrating hormone receptor antagonists and methods of use
AssigneesMixture Sciences, Inc., The Regents of the University of California
InventorsRichard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
Life of this patent
Estimating the term…
Abstract
This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).
Claims10
A composition of matter comprising a compound having the following structural formula:
- wherein,
- R1 and R2 are selected from H, a hydrocarbyl having up to 20 carbon atoms, and a hydrocarbyl having up to 20 carbon atoms and substituted with a group selected from hydroxy, alkoxy, amino, substituted amino, thio, alkylthio, guanidino, ureido and heterocyclyl;
- R3 is selected from a hydrocarbyl having up to 20 carbon atoms, and a hydrocarbyl having up to 20 carbon atoms and substituted with a group selected from halo, haloalkyl, hydroxy, alkyl, alkoxy, alkylenedioxy, amino, substituted amino, aminoalkyl, thio, alkylthio, guanidino, ureido, heterocyclyl, heteroaryl, and heteroarylthio;
- R4 is a substituted amino, —NR6R7, wherein R6 and R7 are selected from H and a hydrocarbyl having up to 20 carbon atoms;
- R6 and R7, with inclusion of N, may combine to form a heterocyclic ring such as indolinyl having the formula
- R5 is selected from O, S, NH, N-alkyl, N-alkenyl, N-alkynyl, N-cycloalkyl, N-aryl and N-aralkyl,
- n is 1 to 3;
- and
- wherein the composition is further characterized by at least one additional limitation selected from group consisting of:
- one or more methylene groups of a hydrocarbyl group of R3 being replaced by an oxygen atom;
- R1 being selected from alkyl and aminoalkyl;
- R1 being selected from (S)-Methyl, (R)-Methyl or (S)-Propyl;
- R1 being (S)-Aminopropyl;
- R2 being selected from (R)-Aminomethyl-(imino)-propyl, (S)-Aminomethyl-(imino)-propyl or (S)-Methylthiomethyl;
- R3 being selected from alkyl, aralkyl or substituted aralkyl;
- R3 being 3-bromophenethyl;
- R3 being 3,5 bis-(trifluoromethyl)phenethyl;
- R4 being aralkylamino;
- R4 being benzylamino;
- R6 and R7 with inclusion of n, being heterocyclyl;
- and
- —NR6R7 being isoindolinyl having the formula
19 more elements
Dependencies are inferred from the claim text.