Patent classifications
C07D241/12
Use of ruthenium complexes for preparing amides, polypeptides and cyclic dipeptides
A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
Use of ruthenium complexes for preparing amides, polypeptides and cyclic dipeptides
A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
NOVEL COMPOUNDS AS ROR GAMMA MODULATORS
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.a, R.sup.b, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
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NOVEL COMPOUNDS AS ROR GAMMA MODULATORS
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, ring B, L, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.a, R.sup.b, n, m, p and q are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
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AGONISTS OF ROR GAMMAt
The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
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INHIBITORS OF HISTONE DEACETYLASE
The present invention relates to compounds of formula (I):
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or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R.sup.1a, R.sup.2b, R.sup.2c, R.sup.5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
KCNQ2-5 CHANNEL ACTIVATOR
The present invention relates to a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.
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Graphene nanostructure
A graphene nanostructure has a nanographene, a π conjugated functional group bonded to the nanographene via a pyrazine skeleton, and at least one Br group and/or at least one CN group introduced into the π conjugated functional group. A graphene nanostructure preferably has an average size of 1 nm or larger to 100 nm or smaller, a band gap of 0.01 eV or higher to 1.2 eV or lower, and/or a HOMO level of −6.0 eV or higher to −4.0 eV or lower. As the π conjugated functional group into which the Br group(s) and/or the CN group(s) are/is introduced, a 4-bromobenzene group, a 4,5-dibromobenzene group, a 5-bromopyridine group, a 5-bromopyrazine group, a benzonitrile group, a phthalonitrile group, or a 2,3-dicyanopyrazine group is desirable.
Graphene nanostructure
A graphene nanostructure has a nanographene, a π conjugated functional group bonded to the nanographene via a pyrazine skeleton, and at least one Br group and/or at least one CN group introduced into the π conjugated functional group. A graphene nanostructure preferably has an average size of 1 nm or larger to 100 nm or smaller, a band gap of 0.01 eV or higher to 1.2 eV or lower, and/or a HOMO level of −6.0 eV or higher to −4.0 eV or lower. As the π conjugated functional group into which the Br group(s) and/or the CN group(s) are/is introduced, a 4-bromobenzene group, a 4,5-dibromobenzene group, a 5-bromopyridine group, a 5-bromopyrazine group, a benzonitrile group, a phthalonitrile group, or a 2,3-dicyanopyrazine group is desirable.
TOBACCO-DERIVED FLAVORANTS
Methods of forming pyrazines from reactants derived from a plant of the Nicotiana species, including receiving an aqueous reactant solution including at least one tobacco-derived cellulosic sugar and at least one tobacco-derived amino acid, heating the reactant solution to a reactant temperature and holding the reactant solution at the reactant temperature for a reactant time to produce a reactant product including at least one tobacco-derived pyrazine, and isolating the at least one tobacco-derived pyrazine from the reactant product. Tobacco products incorporating the tobacco-derived pyrazines are also provided.