Patent classifications
C07D233/86
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
Compounds and methods for the targeted degradation of androgen receptor
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
Compounds and methods for the targeted degradation of androgen receptor
The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) Androgen Receptor. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds Androgen Receptor such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of Androgen Receptor.
Modulators of resistant androgen receptor
The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same.
Modulators of resistant androgen receptor
The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same.
Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure: ##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Substituted 3-((3-aminophenyl)amino)piperidine-2,6-dione compounds, compositions thereof, and methods of treatment therewith
- Massimo Ammirante ,
- Sogole Bahmanyar ,
- Matthew D. Correa ,
- Virginia Grant ,
- Joshua Hansen ,
- Evan J. Horn ,
- Timothy S. Kercher ,
- Christopher Mayne ,
- Mark A. Nagy ,
- Rama Krishna Narla ,
- Surendra Nayak ,
- Stephen Norris ,
- Patrick Papa ,
- Veronique Plantevin-Krenitsky ,
- John J. Sapienza ,
- Brandon W. Whitefield ,
- Shuichan Xu
Provided herein are piperidine dione compounds having the following structure: ##STR00001## wherein R.sup.N, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.
Method for synthesis of deuterated amide and deuterated sulfonamide
A novel method for synthesizing deuterated amides and deuterated sulfonamides includes the following steps: (1) adding a compound M, DMAP, R.sup.3—X to a solvent to obtain a compound N after a reaction is complete; and (2) adding the compound N, R.sup.4—NH—R.sup.5, or a salt and base thereof to a solvent, and purifying after a reaction is complete to obtain a compound I. ##STR00001##
Platelet aggregation inhibitor, preparation and uses thereof
This disclosure relates to medicines, and more particularly to a platelet aggregation inhibitor, a pharmaceutical composition containing the same and a preparation and application thereof. The platelet aggregation inhibitor provided herein is a compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer or a pharmaceutically-acceptable solvate thereof. This application also provides an application of the compound of formula (I), or a pharmaceutically-acceptable salt, a tautomer, a pharmaceutically-acceptable solvate or a pharmaceutical composition thereof in the treatment of thrombus.
PROCESS FOR PREPARATION OF ENZALUTAMIDE
The presented invention relates to a process for preparation of Enzalutamide, compound (1) or a salt or a solvate thereof Formula (1). The presented invention also related to 1,4-dioxane solvate of compound (1).
##STR00001##