Patent classifications
C07D333/20
Arylcyclohexylamine derivatives and process for preparing same
The present invention relates to the technical field of pharmaceutical synthesis and development of drugs, and to a process for preparing cyclic 2-amino-1-one derivatives and to the reaction products and intermediates obtainable by this process. The present invention further relates to pharmaceutical compositions, in particular drugs or medicaments, comprising the cyclic 2-amino-1-one derivatives and to their use as medicaments, in particular in the prophylactic or therapeutic treatment of diseases of the human or animal body, preferably of neurodegenerative diseases or psychiatric disorders.
Arylcyclohexylamine derivatives and process for preparing same
The present invention relates to the technical field of pharmaceutical synthesis and development of drugs, and to a process for preparing cyclic 2-amino-1-one derivatives and to the reaction products and intermediates obtainable by this process. The present invention further relates to pharmaceutical compositions, in particular drugs or medicaments, comprising the cyclic 2-amino-1-one derivatives and to their use as medicaments, in particular in the prophylactic or therapeutic treatment of diseases of the human or animal body, preferably of neurodegenerative diseases or psychiatric disorders.
Process for the Preparation of N-Monosubstituted beta-Amino Alcohols
A process is disclosed for the preparation of a compound of formula
##STR00001##
and/or an addition salt of a proton acid, wherein R.sup.1 and R.sup.2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
Process for the Preparation of N-Monosubstituted beta-Amino Alcohols
A process is disclosed for the preparation of a compound of formula
##STR00001##
and/or an addition salt of a proton acid, wherein R.sup.1 and R.sup.2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
Azide-based crosslinking agents
The present invention provides compounds of formula ##STR00001##
a process for their preparation, a solution comprising these compounds, a process for the preparation of a device using the solution, devices obtainable by the process and the use of the bis-azide-type compounds as cross-linkers.
Azide-based crosslinking agents
The present invention provides compounds of formula ##STR00001##
a process for their preparation, a solution comprising these compounds, a process for the preparation of a device using the solution, devices obtainable by the process and the use of the bis-azide-type compounds as cross-linkers.
HISTONE DEACETYLASE INHIBITORS
Provided herein are brain penetrant histone deacetylase (HDAC) inhibitors useful for treating diseases or disorders associated with HDAC. An exemplary HDAC inhibitor provided herein exhibits a brain-to-plasma ratio of 20:1. Pharmaceutical compositions comprising HDAC inhibitors and methods for treating diseases associated with HDAC are also provided.
NOVEL INHIBITORS OF HISTONE ACETYLTRANSFERASE P300/CBP FOR CANCER THERAPY
Embodiments of the present disclosure pertain to compositions that include a compound that inhibits the histone acetyl transferase activity of a protein, such as p300 and/or CBP. Further embodiments of the present disclosure pertain to methods of inhibiting the histone acetyl transferase activity of a protein by exposing the protein to a composition that contains one or more of the compounds of the present disclosure. The compositions of the present disclosure may be exposed to a protein in vitro or in vivo. Additional embodiments of the present disclosure pertain to methods of treating a cancer in a subject by administering a composition of the present disclosure to the subject in order to treat the cancer.
NOVEL INHIBITORS OF HISTONE ACETYLTRANSFERASE P300/CBP FOR CANCER THERAPY
Embodiments of the present disclosure pertain to compositions that include a compound that inhibits the histone acetyl transferase activity of a protein, such as p300 and/or CBP. Further embodiments of the present disclosure pertain to methods of inhibiting the histone acetyl transferase activity of a protein by exposing the protein to a composition that contains one or more of the compounds of the present disclosure. The compositions of the present disclosure may be exposed to a protein in vitro or in vivo. Additional embodiments of the present disclosure pertain to methods of treating a cancer in a subject by administering a composition of the present disclosure to the subject in order to treat the cancer.
TRNA synthetase inhibitors
Disclosed herein are secondary amine compounds that inhibit tRNA synthetase. The compounds of the invention are useful in inhibiting tRNA synthetase in Gram-negative bacteria and are useful in killing Gram-negative bacteria. The secondary amine compounds of the invention are also useful in the treatment of tuberculosis.