A preparation method of substituted primary amine is disclosed. The preparation method uses cyanophenyl and a derivative thereof as raw materials, nanoporous palladium as a catalyst, and H.sub.2 as a hydrogen source, and conducts selective hydrogenation to prepare the substituted primary amine. The molar concentration of the cyanophenyl and the derivative thereof in the solvent is 0.01-2 mmol/mL, and the molar ratio of the cyanophenyl to the derivative thereof to the catalyst is 1: 0.01-1: 0.5. The size of a pore framework of the nanoporous palladium is 1 nm-50 nm. The pressure of the H.sub.2 is 0.1-20.0 MPa. The obtained product has high selectivity; the present invention has mild reaction conditions, does not need any additive, and has simple operation and post-processing and good catalyst reproducibility. After repeatedly used, the catalytic activity of the present invention is not significantly reduced, thereby providing the possibility of realizing industrialization.

A preparation method of substituted primary amine is disclosed. The preparation method uses cyanophenyl and a derivative thereof as raw materials, nanoporous palladium as a catalyst, and H.sub.2 as a hydrogen source, and conducts selective hydrogenation to prepare the substituted primary amine. The molar concentration of the cyanophenyl and the derivative thereof in the solvent is 0.01-2 mmol/mL, and the molar ratio of the cyanophenyl to the derivative thereof to the catalyst is 1: 0.01-1: 0.5. The size of a pore framework of the nanoporous palladium is 1 nm-50 nm. The pressure of the H.sub.2 is 0.1-20.0 MPa. The obtained product has high selectivity; the present invention has mild reaction conditions, does not need any additive, and has simple operation and post-processing and good catalyst reproducibility. After repeatedly used, the catalytic activity of the present invention is not significantly reduced, thereby providing the possibility of realizing industrialization.

The present disclosure provides adamantyl compounds having one or more amine groups and one or more nitrate groups. The aminoadamantyl nitrate compounds can be used to treat disorders of the central nervous system, including neurodegenerative and non-neurodegenerative diseases.

The present invention provides an improved process for the manufacture (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to said salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof. ##STR00001##

The present invention provides an improved process for the manufacture (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one, in high purity and high yield, through the use of 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine L-tartrate salt, 1,1-dimethyl-2-(4-methoxyphenyl)ethyl amine maletate salt or the camphorsulfonate salt of intermediate (4). The invention also relates to said salts, to processes for preparing them and to their use for the manufacture of (R)-6-hydroxy-8-[1-hydroxy-2-[2-(4-methoxyphenyl)-1,1-dimethyl-ethylamino-ethyl]-2H-1,4-benzoxazin-3(4H)-one or a pharmaceutically acceptable salt thereof. ##STR00001##

Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof. ##STR00001##

Described are dimethoxyphenyl inhibitors of VMAT2, pharmaceutical compositions thereof, and methods of use thereof. ##STR00001##

The present invention provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of A42 oligomers in a subject. It further provides a method of reducing formation of or disrupting A42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition.

The present invention provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of A42 oligomers in a subject. It further provides a method of reducing formation of or disrupting A42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition.

The present invention provides small molecule drugs and pharmaceutical compositions for the treatment and prevention of diseases related to the formation of A42 oligomers in a subject. It further provides a method of reducing formation of or disrupting A42 oligomers in a subject, the method comprising the step of administering to the subject in need thereof a therapeutically effective amount of a pharmaceutical composition.