Patent classifications
C07F9/6539
Reducing platelet activation, aggregation and platelet-stimulated thrombosis or blood coagulation by reducing mitochondrial respiration
It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.
Synthesis Process of X-IPM, Stable Crystal Form and Application Thereof
The present application relates to a new method for synthesizing isophosphoramide nitrogen mustard (X-IPM) that is suitable for industrialized production, involves fewer types of solvents, and leads to stable products with high yield. This method is charazterized mainly by the batchwise addition of M (e.g., M is R.sub.3N with R being ethyl; i.e., M is triethylamine) and the specific post-reaction treatment, which make it possible for the reaction to fully proceed, lead to products with less impurities, high yield and relatively stable properties, and can lead to stable crystallized substances with specific crystal structures. The present application also relates to stable crystal forms of the isophosphoramide nitrogen mustard (X-IPM) prepared by the aforementioned method, and use of the same as reactants for the synthesis of aziridine structure-containing compounds.
Synthesis Process of X-IPM, Stable Crystal Form and Application Thereof
The present application relates to a new method for synthesizing isophosphoramide nitrogen mustard (X-IPM) that is suitable for industrialized production, involves fewer types of solvents, and leads to stable products with high yield. This method is charazterized mainly by the batchwise addition of M (e.g., M is R.sub.3N with R being ethyl; i.e., M is triethylamine) and the specific post-reaction treatment, which make it possible for the reaction to fully proceed, lead to products with less impurities, high yield and relatively stable properties, and can lead to stable crystallized substances with specific crystal structures. The present application also relates to stable crystal forms of the isophosphoramide nitrogen mustard (X-IPM) prepared by the aforementioned method, and use of the same as reactants for the synthesis of aziridine structure-containing compounds.
Phosphinyl Amidine Compounds, Metal Complexes, Catalyst Systems, and Their Use to Oligomerize or Polymerize Olefins
N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, N.sup.2-phosphinyl amidinate metal salt complexes are described. Methods for making N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, and N.sup.2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N.sup.2-phosphinyl amidine metal salt complexes and N.sup.2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, and N.sup.2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.
Phosphinyl Amidine Compounds, Metal Complexes, Catalyst Systems, and Their Use to Oligomerize or Polymerize Olefins
N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, N.sup.2-phosphinyl amidinate metal salt complexes are described. Methods for making N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, and N.sup.2-phosphinyl amidinate metal salt complexes are also disclosed. Catalyst systems utilizing the N.sup.2-phosphinyl amidine metal salt complexes and N.sup.2-phosphinyl amidinate metal salt complexes are also disclosed along with the use of the N.sup.2-phosphinyl amidine compounds, N.sup.2-phosphinyl amidinates, N.sup.2-phosphinyl amidine metal salt complexes, and N.sup.2-phosphinyl amidinate metal salt complexes for the oligomerization and/or polymerization of olefins.
Rubber composition including a thiazole derivative
A rubber composition for the manufacture of tires is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more thiazole compounds chosen from compounds having the following formula (I): ##STR00001## Certain specific thiazole derivatives are described.
Rubber composition including a thiazole derivative
A rubber composition for the manufacture of tires is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more thiazole compounds chosen from compounds having the following formula (I): ##STR00001## Certain specific thiazole derivatives are described.
NOVEL KLK4 INHIBITORS
The present invention relates to novel compounds and probes which have a common chemical structure necessary to obtain potent inhibitory activity against KLK4 and/or may be used for the detection of KLK4 peptides and their activity. It further relates to the use of these compounds and methods for inhibiting and/or detecting KLK4 activity in vitro and in vivo by making use of said probes or inhibitors. The compounds of the invention differ from prior art compounds at least in the presence of phenyl guanidine (instead of e.g. benzyl guanidine) and/or the presence of a heteroatom in the tail group, their combined presence unexpectedly leading to potent and selective KLK4 inhibitory activity.
NOVEL ACTIVATORS OF GLUCOKINASE
The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.
NOVEL ACTIVATORS OF GLUCOKINASE
The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinsae activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.