Patent classifications
C07D277/26
PPARo ACTIVATOR
The present invention provides a PPARδ activator containing a novel PPARδ agonist (peroxisome proliferator-activated receptor δ) as an active ingredient, and an exercise tolerance-improving agent containing the same as an active ingredient. The present invention is a PPARδ activator containing a guanidine derivative or a biguanidine derivative as an active ingredient, wherein the PPARδ activator activates transcriptional activity of PPARδ, and the guanidine derivative and the biguanidine derivative are capable of fitting within a PPARδ ligand binding pocket in a state where a guanidino group or a biguanidino group forms a hydrogen bond with amino acid residues corresponding to each of the 413th histidine, 287th histidine, 253rd threonine and the 437th tyrosine of human PPARδ, among amino acid residues constituting an interior surface of the ligand binding pocket; and is an exercise tolerance-improving agent containing the PPARδ activator as an active ingredient.
Metabotropic Glutamate Receptor Negative Allosteric Modulators (NAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
Metabotropic Glutamate Receptor Negative Allosteric Modulators (NAMS) and Uses Thereof
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
Bisarylsulfonamides useful in the treatment of inflammation and cancer
A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. ##STR00001##
Bisarylsulfonamides useful in the treatment of inflammation and cancer
A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. ##STR00001##
(S)-ENANTIOMERIC FORM OF A HETEROCYCLIC COMPOUND HAVING MOTIVATION IMPROVING AND/OR REFERENCE MEMORY ENHANCING ACTIVITY
The present invention relates to the (S)-enantiomer of the chemical compound having the general formula (I):
##STR00001## wherein R.sub.1 and R.sub.2 are, equal or independently, aryl, heteroaryl, fused aryl, fused heteroaryl, mono or multi-substituted aryl, mono or multi-substituted heteroaryl, mono or multi-substituted fused aryl, mono or multi-substituted fused heteroaryl; and R.sub.TA is a 2-1,3-, or 4-1,3-or 5-1,3-thiazole ring with the general Formula (IIa), which can also be substituted.
The invention also relates to said compound according to formula (I) for use in improving motivation and/or cognitive functions and/or for use in improving the reference memory in human individuals.
(S)-ENANTIOMERIC FORM OF A HETEROCYCLIC COMPOUND HAVING MOTIVATION IMPROVING AND/OR REFERENCE MEMORY ENHANCING ACTIVITY
The present invention relates to the (S)-enantiomer of the chemical compound having the general formula (I):
##STR00001## wherein R.sub.1 and R.sub.2 are, equal or independently, aryl, heteroaryl, fused aryl, fused heteroaryl, mono or multi-substituted aryl, mono or multi-substituted heteroaryl, mono or multi-substituted fused aryl, mono or multi-substituted fused heteroaryl; and R.sub.TA is a 2-1,3-, or 4-1,3-or 5-1,3-thiazole ring with the general Formula (IIa), which can also be substituted.
The invention also relates to said compound according to formula (I) for use in improving motivation and/or cognitive functions and/or for use in improving the reference memory in human individuals.
Compositions and methods for inhibiting group II intron RNA
The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.
Compositions and methods for inhibiting group II intron RNA
The present invention provides compositions and methods for inhibiting group II intron splicing for treating or preventing a disease or disorder associated with an organism harboring an active group II intron. The present invention also provides compositions and methods for inhibiting group II intron splicing for inhibiting, preventing or reducing growth of an organism harboring an active group II intron.
Aromatic sulfonamide derivatives
Substituted aromatic sulfonamides of formula (I) ##STR00001##
pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease.