Provided are pamoate salts of ketamine having a stoichiometry of 2:1 of ketamine to pamoate, including R, S-ketamine pamoate, S-ketamine pamoate, or R-ketamine pamoate, and crystalline or amorphous forms of the pamoate salts, and having excellent safety and properties for pharmaceutical applications. Also provided are pharmaceutical compositions including the pamoate salts of ketamine and their uses in treating a CNS disease or serving as an anesthetic.

Provided are pamoate salts of ketamine having a stoichiometry of 2:1 of ketamine to pamoate, including R, S-ketamine pamoate, S-ketamine pamoate, or R-ketamine pamoate, and crystalline or amorphous forms of the pamoate salts, and having excellent safety and properties for pharmaceutical applications. Also provided are pharmaceutical compositions including the pamoate salts of ketamine and their uses in treating a CNS disease or serving as an anesthetic.

Disclosed is a method for efficiently synthesizing primary amines, which comprises using carbonyl compounds or alcohol compounds as reaction substrate, liquid ammonia or alcohol solutions of ammonia as nitrogen source, and hydrogen as hydrogen source, and reacting in reaction medium catalyzed by a cobalt-based catalyst to obtain the primary amines. Due to high catalytic activity, the method can realize the reductive amination of carbonyl compounds and the hydrogen-borrowing amination of alcohol compounds at low temperatures in a short time to obtain the primary amines with high yield, and is applicable to a wide range of substrates. The obtained primary amines can be used as raw materials with high extra value for producing polymers, medicines, dyes and surfactants. Further, the cobalt-based catalyst has a good industrial application prospect because it is magnetic which can facilitate separation and recycling of the catalyst. Moreover, the inexpensive cobalt-based catalyst can significantly reduce industrialization cost.

Disclosed is a method for efficiently synthesizing primary amines, which comprises using carbonyl compounds or alcohol compounds as reaction substrate, liquid ammonia or alcohol solutions of ammonia as nitrogen source, and hydrogen as hydrogen source, and reacting in reaction medium catalyzed by a cobalt-based catalyst to obtain the primary amines. Due to high catalytic activity, the method can realize the reductive amination of carbonyl compounds and the hydrogen-borrowing amination of alcohol compounds at low temperatures in a short time to obtain the primary amines with high yield, and is applicable to a wide range of substrates. The obtained primary amines can be used as raw materials with high extra value for producing polymers, medicines, dyes and surfactants. Further, the cobalt-based catalyst has a good industrial application prospect because it is magnetic which can facilitate separation and recycling of the catalyst. Moreover, the inexpensive cobalt-based catalyst can significantly reduce industrialization cost.

Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4′-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3′,5′-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1′-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2′-aminopyrimidin-4′-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3′-cycloheptylureido)-N-(5″-methylisoxazol-3″-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.

Cycloalkylamine derivatives may be used for preventing or treating diseases in humans, animals, and have demonstrated efficacy specifically in treating type 2 diabetes. In an embodiment, the cycloalkylamine derivatives can include a compound selected from the group consisting of cycloheptanamine salts, cyclohexanamine salts, cyclopentanamine salts 1-cycloheptyl-[4,4′-bipyridin]-1-ium, N1,N2-dicycloheptyloxalamide, 1-[3′,5′-bis(trifluoromethyl)phenyl]-3-cycloheptylurea, 1,1′-(4-methyl-1,3-phenylene)bis(3-cycloheptylurea), 1-(2′-aminopyrimidin-4′-yl)-3-cycloheptylurea, 4-amino-N-(cycloheptylcarbamoyl)benzenesulfonamide, 4-(3′-cycloheptylureido)-N-(5″-methylisoxazol-3″-yl)benzenesulfonamide, N-(cycloheptylcarbamoyl)-4-methylbenzenesulfonamide, 1-cycloheptylguanidine hydrochloride, (E)-amino[(amino(cycloheptylamino)methylene)amino]methaniminium chloride, or a pharmaceutically acceptable salt thereof.

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##

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.

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.

Ketamine derivatives and pharmaceutical compositions thereof are disclosed. When administered orally the ketamine derivatives provide increased bioavailability of ketamine in the systemic circulation. The ketamine derivatives can be used to treat neurological diseases, psychological diseases and pain.