Patent classifications
C07D413/08
Piperidinyl-propanone derivatives
Compounds of the formula I ##STR00001##
in which X, Q, R.sup.1 and R.sup.2 have the meanings indicated in Claim 1, are inhibitors of pyruvate dehydrogenase kinase (PDHK), and can be employed, inter alia, for the treatment of diseases such as cancer.
3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: ##STR00001##
where R, L, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.
3-alkyl-4-amido-bicyclic [4,5,0] hydroxamic acids as HDAC inhibitors
The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: ##STR00001##
where R, L, X.sup.1, X.sup.2, X.sup.3, X.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, and Y.sup.4 are described herein.
INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, METHOD FOR PREPARATION AND USE THEREOF
The present invention provides a novel indoleamine 2,3-dioxygenase inhibitor, a preparation method thereof, and a pharmaceutical composition, in which the definitions of n, Y, Z, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as stated in the specification. Also provided is a use of the aforementioned compound and pharmaceutically acceptable salts and isomers thereof in the preparation of a drug for indoleamine 2,3-dioxygenase (IDO) related disease, specifically a use in the treatment of major diseases such as cancer, Alzheimer's, depression, cataract, etc. The compound of the invention has improved activity, potential medicinal value, and wide market prospects.
INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, METHOD FOR PREPARATION AND USE THEREOF
The present invention provides a novel indoleamine 2,3-dioxygenase inhibitor, a preparation method thereof, and a pharmaceutical composition, in which the definitions of n, Y, Z, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as stated in the specification. Also provided is a use of the aforementioned compound and pharmaceutically acceptable salts and isomers thereof in the preparation of a drug for indoleamine 2,3-dioxygenase (IDO) related disease, specifically a use in the treatment of major diseases such as cancer, Alzheimer's, depression, cataract, etc. The compound of the invention has improved activity, potential medicinal value, and wide market prospects.
AMYLOID PROTEIN-SELECTIVE BACE INHIBITORS (ASBIs) FOR ALZHEIMER?S DISEASE
The present disclosure provides various compounds, compositions, and methods of BACE inhibition that interact with both BACE and APP to increase selectivity of the inhibitor. Compounds presented herein exhibit desirably low IC.sub.50 values and permeability across the blood-brain barrier.
AMYLOID PROTEIN-SELECTIVE BACE INHIBITORS (ASBIs) FOR ALZHEIMER?S DISEASE
The present disclosure provides various compounds, compositions, and methods of BACE inhibition that interact with both BACE and APP to increase selectivity of the inhibitor. Compounds presented herein exhibit desirably low IC.sub.50 values and permeability across the blood-brain barrier.
PROCESS FOR THE PREPARATION OF (S)-NETARSUDIL,ITS SALTS AND POLYMORPHS
The present invention relates to a process for the preparation of (S)-Netarsudil or its pharmaceutically acceptable salts using novel intermediates. The present invention further provides novel salts, novel intermediates and novel polymorphic forms of the (S)-Netarsudil salts and process for the preparation of the same.
INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE
Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.
INHIBITORS OF RECEPTOR INTERACTING PROTEIN KINASE I FOR THE TREATMENT OF DISEASE
Disclosed herein are compounds which inhibit RIPK1, pharmaceutical compositions, and methods of treatment of RIPK1-mediated diseases, such as neurodegenerative disorders, inflammatory disorders, and cancer.