Patent classifications
C07C215/44
SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS
Substituted cyclohexyl chemical entities of Formula (I): wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
##STR00001##
Methods of synthesis of (1R,2R,5R)-5-amino-2-methyl-cyclohexanol hydrochloride and intermediates useful therein
Provided herein are methods and intermediates for making (1R, 2R, 5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.
Methods of synthesis of (1R,2R,5R)-5-amino-2-methyl-cyclohexanol hydrochloride and intermediates useful therein
Provided herein are methods and intermediates for making (1R, 2R, 5R)-5-amino-2-methylcyclohexanol hydrochloride, which are useful for the preparation of compounds useful for the treatment of a disease, disorder, or condition associated with the JNK pathway.
SUBSTITUTED CYCLOHEXYL COMPOUNDS AS NOP INHIBITORS
Substituted cyclohexyl chemical entities of Formula (I):
##STR00001## wherein R.sup.a, G, and R.sup.b have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive therapies; modulating and treating disorders mediated by nociceptin activity or dopamine signaling; treating neurological disorders, neurodegenerative diseases, depression, and schizophrenia; enhancing the efficiency of cognitive and motor training; and treating peripheral disorders, including renal, respiratory, gastrointestinal, liver, genitourinary, metabolic, and inflammatory disorders.
Chiral binuclear metal complexes for stereoselective hydrolysis of saccharides and glycosides
Disclosed herein is a class of chiral binuclear metal complexes for stereoselective hydrolysis of saccharides and glycosides, and more particular chiral binuclear transition metal complex catalysts that discriminate epimeric glycosides and α- and β-glycosidic bonds of saccharides in aqueous solutions at near physiological pHs. The chiral binuclear metal complexes include a Schiff-base-type ligand derived from a chiral diamino building block, and a binuclear transition metal core, each which can be varied for selectivity. The metal core is a Lewis-acidic metal ion, such as copper, zinc, lanthanum, iron and nickel. The Schiff-base may be a reduced or non-reduced Schiff-base derived from aliphatic linear, aliphatic cyclic diamino alcohols or aromatic aldehydes. The ligand can be a penta- or heptadentate ligand derived from pyridinecarbaldehydes, benzaldehydes, linear or cyclic diamines or diamino alcohols.
Chiral binuclear metal complexes for stereoselective hydrolysis of saccharides and glycosides
Disclosed herein is a class of chiral binuclear metal complexes for stereoselective hydrolysis of saccharides and glycosides, and more particular chiral binuclear transition metal complex catalysts that discriminate epimeric glycosides and α- and β-glycosidic bonds of saccharides in aqueous solutions at near physiological pHs. The chiral binuclear metal complexes include a Schiff-base-type ligand derived from a chiral diamino building block, and a binuclear transition metal core, each which can be varied for selectivity. The metal core is a Lewis-acidic metal ion, such as copper, zinc, lanthanum, iron and nickel. The Schiff-base may be a reduced or non-reduced Schiff-base derived from aliphatic linear, aliphatic cyclic diamino alcohols or aromatic aldehydes. The ligand can be a penta- or heptadentate ligand derived from pyridinecarbaldehydes, benzaldehydes, linear or cyclic diamines or diamino alcohols.
EPOXIDE FUNCTIONALIZED POLYAROMATIC FEEDSTOCK AND POLYMERS DERIVED THEREFROM
Epoxide functionalized polyaromatic feedstocks and processes for their preparation are described. The processes involve functionalizing polyaromatic hydrocarbon molecules and/or polyheterocyclic molecules present in petroleum or petrochemical streams with epoxide. The epoxide functionalized poly aromatic feedstock can be further treated so as to effect oligomerization or polymerization. The oligomers or polymers may be thermoplastic or thermoset materials and may find use in, for example, infrastructure applications, composites, fillers, fire retardants and 3-D printing materials.
EPOXIDE FUNCTIONALIZED POLYAROMATIC FEEDSTOCK AND POLYMERS DERIVED THEREFROM
Epoxide functionalized polyaromatic feedstocks and processes for their preparation are described. The processes involve functionalizing polyaromatic hydrocarbon molecules and/or polyheterocyclic molecules present in petroleum or petrochemical streams with epoxide. The epoxide functionalized poly aromatic feedstock can be further treated so as to effect oligomerization or polymerization. The oligomers or polymers may be thermoplastic or thermoset materials and may find use in, for example, infrastructure applications, composites, fillers, fire retardants and 3-D printing materials.
Method of preparation of (1R,3S)-3-amino-1-cyclopentanol and salt thereof
Provided is a method of preparation of (1R, 3S)-3-amino-1-cyclopentanol, the method including: contacting N-acylhydroxyamine and cyclopentadiene for an asymmetric cycloaddition, to yield a first intermediate I; hydrogenating the first intermediate I to yield a second intermediate II; hydrolyzing, ammonolyzing, hydrazinolyzing, or alcoholyzing an amido bond of the second intermediate II to yield a third intermediate III; and hydrogenating the third intermediate III to yield (1R, 3S)-3-amino-1-cyclopentanol.
Method of preparation of (1R,3S)-3-amino-1-cyclopentanol and salt thereof
Provided is a method of preparation of (1R, 3S)-3-amino-1-cyclopentanol, the method including: contacting N-acylhydroxyamine and cyclopentadiene for an asymmetric cycloaddition, to yield a first intermediate I; hydrogenating the first intermediate I to yield a second intermediate II; hydrolyzing, ammonolyzing, hydrazinolyzing, or alcoholyzing an amido bond of the second intermediate II to yield a third intermediate III; and hydrogenating the third intermediate III to yield (1R, 3S)-3-amino-1-cyclopentanol.