Patent classifications
C07D295/125
CYCLOALIPHATIC ALDIMINE MIXTURE
A mixture of isomeric aldimines of the formulae (Ia), (Ib) and (Ic) in which the ratio of the trans,trans isomer (Ia) to the sum of the cis,trans isomer (Ib) and the cis,cis isomer (Ic) is in the range of 5/95 to 30/70, and its use as latent hardener for moisture-curing isocyanate-functional polyurethane compositions. The inventive mixture of isomeric aldimines enables polyurethane compositions with very low content of monomeric isophorone diisocyanate and excellent stability under outdoor wheathering conditions and high UV load, which cure quickly to an elastic material of low surface tack and good mechanical properties, particularly in terms of high tensile strength and modulus of elasticity at high elongation. Such compositions are particularly suitable as elastic adhesives and/or sealants or elastic coatings, particularly for outdoor use such as on roofs, floors or ships.
LIPID NANOPARTICLE
The present invention relates to a lipid nanoparticle. The lipid nanoparticle is formed from a compound having the following structure (I) or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof. The present invention also provides use of the lipid nanoparticle for delivering a therapeutic agent component. The present invention also relates to use of the lipid nanoparticle in the manufacture of a medicament.
##STR00001##
VITAMIN D3 DERIVATIVES AND PHARMACEUTICAL USE THEREOF
The present invention relates to vitamin D.sub.3 derivatives of the following formula, wherein each symbol has the same meaning as defined herein, and pharmaceutical or medical use thereof for treating metabolic disease, liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.
##STR00001##
VITAMIN D3 DERIVATIVES AND PHARMACEUTICAL USE THEREOF
The present invention relates to vitamin D.sub.3 derivatives of the following formula, wherein each symbol has the same meaning as defined herein, and pharmaceutical or medical use thereof for treating metabolic disease, liver disease, obesity, diabetes, cardiovascular disease, or cancer in a patient in need thereof.
##STR00001##
Process to prepare propylene amines and propylene amine derivatives
A process is provided to prepare propylene amines of the formula NH.sub.2—(A-NH—).sub.pR, wherein R is a hydrogen atom or an alkyl group, p is at least 1 when R is an alkyl group, and at least 2 when R is a hydrogen atom, or derivatives or precursors thereof wherein one or more units —NH-A-NH— may be present as a cyclic urea unit ##STR00001## or a cyclic unit ##STR00002## or between two units —NH-A-NH— a carbonyl bond is present, each unit -A- can be independently an alkylene unit and at least one unit -A- is a —C.sub.3H.sub.6— unit, wherein each —C.sub.3H.sub.6— unit can be linear or branched. The process includes reacting (i) at least one of a hydroxy-functional compound chosen from the alkanolamine-functional compounds, and dihydroxyalkylene compounds, with (ii) an amine-functional compound, in the presence of (iii) a carbon oxide delivering agent, wherein at least one of the alkanolamine-functional compound, the amine-functional compound and/or the carbon oxide delivering agent contains at least one alkylene unit (A) that is a propylene unit.
Kappa opioid agonists and uses thereof
Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof: ##STR00001## The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
Kappa opioid agonists and uses thereof
Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof: ##STR00001## The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.
VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF
Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof.
PRODRUG COMPOUNDS ACTIVATED BY AKR1C3 AND THEIR USE FOR TREATING HYPERPROLIFERATIVE DISORDERS
AKR1C3-activated prodrugs of Formula (I), pharmaceutical compositions comprising prodrugs of Formula (I), and their use in the treatment of hyperproliferative diseases such as cancer and for cell ablation. The compounds of the invention are able to penetrate neoplasm tissue and be selectively reduced to an active (cytotoxic) form by contact with an AKR1C3 enzyme found in the neoplasm. This active form is therefore able to ablate AKR1C3-expressing target cells of the neoplasm and therefore has particular utility in the treatment of cancer and other hyperproliferative disorders.
##STR00001##
MU OPIOID RECEPTOR MODULATORS
Described herein, inter alia, are compositions and methods for modulating mu opioid receptor activity.