Patent classifications
C07D273/02
Asparagine endopeptidase (AEP) inhibitors for managing cancer and compositions related thereto
This disclosure relates to asparagine endopeptidase inhibitors for managing cancer and compositions related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are substituted 3,7-dihydropurine-2,6-dione derivatives useful for treating or preventing metastasis, tumor growth, and/or cancer. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating a cancer comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
Asparagine endopeptidase (AEP) inhibitors for managing cancer and compositions related thereto
This disclosure relates to asparagine endopeptidase inhibitors for managing cancer and compositions related thereto. In certain embodiments, the asparagine endopeptidase inhibitors are substituted 3,7-dihydropurine-2,6-dione derivatives useful for treating or preventing metastasis, tumor growth, and/or cancer. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising an asparagine endopeptidase inhibitor and a pharmaceutically acceptable excipient. In certain embodiments, the disclosure relates to methods of treating a cancer comprising administering an effective amount of pharmaceutical composition a asparagine endopeptidase inhibitor disclosed herein to a subject in need thereof.
BAF Complex Modulating Compounds and Methods of Using the Same
The invention provided here creates a new paradigm for the treatment of a variety of conditions where modulation of a BAF complex is desired. The disclosure that follows outlines a strategy for modulating a BAF complex in a cell, and provides effective compounds, pharmaceutical compositions, development strategies, and treatment protocols, and describes many of the ensuing benefits. A new family of BAF complex modulating compounds has been developed based on a new chemical scaffold including a 12-membered macrolactam core structures. Contacting target cells in vitro or in vivo with the compounds and compositions of this invention can selectively inhibit the activity of BAF complexes in such cells. Some of the BAF complex modulating compounds in this family are particularly effective agents for treating cancer in conjunction with a ATR inhibitor.
BAF Complex Modulating Compounds and Methods of Using the Same
The invention provided here creates a new paradigm for the treatment of a variety of conditions where modulation of a BAF complex is desired. The disclosure that follows outlines a strategy for modulating a BAF complex in a cell, and provides effective compounds, pharmaceutical compositions, development strategies, and treatment protocols, and describes many of the ensuing benefits. A new family of BAF complex modulating compounds has been developed based on a new chemical scaffold including a 12-membered macrolactam core structures. Contacting target cells in vitro or in vivo with the compounds and compositions of this invention can selectively inhibit the activity of BAF complexes in such cells. Some of the BAF complex modulating compounds in this family are particularly effective agents for treating cancer in conjunction with a ATR inhibitor.
COMPOUNDS FOR USE AS IRON(III) MRI CONTRAST AGENTS
Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macro-cyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.
MACROCYCLIC IMMUNOMODULATORS
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II):
##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
CREATINE PRODRUGS, COMPOSITIONS AND METHODS OF USE THEREOF
The present disclosure provides creatine prodrug analogs and their compositions useful for the treatment of creatine deficiencies.
CREATINE PRODRUGS, COMPOSITIONS AND METHODS OF USE THEREOF
The present disclosure provides creatine prodrug analogs and their compositions useful for the treatment of creatine deficiencies.
MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I):
##STR00001##
where the substituents R.sup.1, R.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein and
##STR00002##
where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
Macrocyclic immunomodulators
Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): ##STR00001## including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2a, R.sup.2b, R.sup.2c, R.sup.3, R.sup.4, R.sup.5, R.sup.6a, R.sup.6b, R.sup.6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.