Patent classifications
C07F9/65522
Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is OH or OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
ANTIOXIDANT COMPOUND HAVING ANTI ATHEROSCLEROTIC EFFECT AND PREPARATION THEREOF
The present invention relates to an antioxidant compound having anti atherosclerotic effect and preparation thereof. The present invention more particularly relates to the synthesis of TPP+ coupled esculetin (mitochondria-targeted esculetin [Mito-Esc]) followed by the biological evaluation of Mito-Esc for its ability to attenuate Angiotensin-II-induced atherosclerosis in apolipoproteinE knockout (ApoE.sup./ mice along with the endothelial cell age-delaying effects of Mito-Esc.
HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF SUMO ACTIVATING ENZYME
Disclosed are chemical entities which are compounds of formula (I):
##STR00001##
or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
Compound and organic light-emitting device including the same
A compound, an organic light-emitting device including a first electrode; a second electrode facing the first electrode; and an organic layer between the first electrode and the second electrode, and including and emission layer, where the organic layer includes at least one compound represented by Formula 1, and a display apparatus, the compound being represented by Formula 1 below: ##STR00001##
Prodrugs of tetrahydrocannabinol, compositions comprising prodrugs of tetrahydrocannabinol and methods of using the same
Described herein are .sup.9-THC prodrugs, methods of making .sup.9-THC prodrugs, formulations comprising .sup.9-THC prodrugs and methods of using .sup.9-THC. One embodiment described herein relates to the transdermal administration of a .sup.9-THC prodrug for treating and preventing diseases and/or disorders.
Stable hydroformylation catalyst for preparation of high N/Iso ratio aldehyde product
A new stable, catalytically active, tetradentate organophosphorus modified rhodium hydroformylation catalyst has been discovered that is capable of producing aldehyde products with a high linear/branched product ratio from linear olefins. The tetradentate organophosphorus modifier is a tetrasubstituted 2,2,2,5-tetramethyl-1,1:4-1-terphenyl, whereby, each methyl group has one hydrogen substituted by an R, R-diorganophosphine moiety. The R, R may comprise aromatic, alkyl, arylalkyl and alkylaryl groups. The precursor 2,2,2,5-tetramethyl-1,1:4,1-terphenyl hydrocarbon may be prepared from para-xylene and toluene derivatives.
Heteroaryl compounds useful as inhibitors of SUMO activating enzyme
Disclosed are chemical entities which are compounds of formula (I): ##STR00001##
or pharmaceutically acceptable salts thereof; wherein Y, R.sup.a, R.sup.a, R.sup.b, R.sup.c, X.sub.1, X.sub.2, X.sub.3, R.sup.d, Z.sub.1, and Z.sub.2 have the values described herein and stereochemical configurations depicted at asterisked positions indicate absolute stereochemistry. Chemical entities according to the disclosure can be useful as inhibitors of Sumo Activating Enzyme (SAE). Further provided are pharmaceutical compositions comprising a compound of the disclosure and methods of using the compositions in the treatment of proliferative, inflammatory, cardiovascular, and neurodegenerative diseases or disorders.
Substituted chroman-6-yloxy-cycloalkanes and their use as pharmaceuticals
The present invention relates to substituted chroman-6-yloxy-cycloalkanes of the formula (I) in which Ar, R1 to R4, p and q are as defined in the claims. The compounds of the formula (I) are inhibitors of the sodium-calcium exchanger (NCX), especially of the sodium-calcium exchanger of subtype 1 (NCX1), and are suitable for the treatment of diverse disorders in which intracellular calcium homeostasis is disturbed, such as arrhythmias, heart failure and stroke. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use in pharmaceuticals, and pharmaceutical compositions comprising them.
##STR00001##
HETEROCYCLIC SELENAMONOPHOSPHITES PROTECTED ON A HYDROXYL GROUP AND PROCESSES FOR PREPARATION THEREOF
Novel heterocyclic selenamonophosphites protected on the hydroxyl group, processes for preparation thereof and the use thereof as ligand.
HETEROCYCLIC SELENABISPHOSPHITES AND PROCESS FOR PREPARATION THEREOF
Novel heterocyclic selenabisphosphites, process for preparation thereof and use thereof as ligand unit for preparing ligands for use in complexes.