Patent classifications
C07D233/28
MAX BINDERS AS MYC MODULATORS AND USES THEREOF
The present disclosure provides compounds of Formula (I), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.
##STR00001##
MAX BINDERS AS MYC MODULATORS AND USES THEREOF
The present disclosure provides compounds of Formula (I), Formula (I), Formula (II), Formula (II-A), Formula (III), and Formula (IV). The compounds described herein are MAX binders and/or modulators of Myc, Mad, or Mxi1 (e.g., inhibitors of Myc, Mad, or Mxi1), and may be useful in treating a subject with a disease associated with Myc, such as proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions and kits including the compounds described herein, as well as methods of using and uses of the compounds, compositions, and kits.
##STR00001##
Backfunctionalized imidazolinium salts and NHC carbene-metal complexes
Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: ##STR00001## Wherein R.sup.1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R.sup.2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R.sup.3 and R.sup.4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hnig's base in a solvent.
Backfunctionalized imidazolinium salts and NHC carbene-metal complexes
Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula: ##STR00001## Wherein R.sup.1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R.sup.2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R.sup.3 and R.sup.4 are each an aliphatic group; and X is an anion; the method comprises cyclization of a halogenated acrylate with Hnig's base in a solvent.
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification. ##STR00001##
Substituted pyrazoles as inhibitors of fibroblast growth factor receptor
An indole derivative as expressed by Formula (I), a preparation method thereof, a pharmaceutical salt, and use thereof as a therapeutic agent, especially as a FGFR inhibitor. Each substituent in Formula (I) has identical definition as specified in the specification. ##STR00001##
META-AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS PAN INTEGRIN ANTAGONISTS
The present disclosure provides pharmaceutical agents of the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents for the treatment of a variety of diseases and disorders are also provided.
META-AZACYCLIC AMINO BENZOIC ACID DERIVATIVES AS PAN INTEGRIN ANTAGONISTS
The present disclosure provides pharmaceutical agents of the formula:
##STR00001##
wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents for the treatment of a variety of diseases and disorders are also provided.
BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES
Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula:
##STR00001##
Wherein R.sup.1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R.sup.2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R.sup.3 and R.sup.4 are each selected from the group consisting of a C.sub.1-C.sub.20 alkyl group, C.sub.1-C.sub.20 partially fluorinated alkyl group, an aryl group, an aryl group with para CF.sub.3 functionality, an aryl group having C.sub.1-C.sub.20 partially fluorinated alkyl groups or partially fluorinated alkoxy groups, and a C.sub.1-C.sub.20 partially fluorinated aliphatic group, and a C.sub.1-C.sub.20 aryl group; and X is an anion. The method comprises cyclization of a halogenated acrylate with a formamidine with Hnig's base in a solvent.
BACKFUNCTIONALIZED IMIDAZOLINIUM SALTS AND NHC CARBENE-METAL COMPLEXES
Backfunctionalized imidazolinium salts and methods of synthesizing the same and NHC carbene-metal complexes therefrom. For backfunctionalized imidazolinium salts of the formula:
##STR00001##
Wherein R.sup.1 is selected from the group consisting of an ester group, an amide group, and an aromatic group; R.sup.2 is selected from the group consisting of hydrogen, an ester group, an amide group, and an aromatic group; R.sup.3 and R.sup.4 are each selected from the group consisting of a C.sub.1-C.sub.20 alkyl group, C.sub.1-C.sub.20 partially fluorinated alkyl group, an aryl group, an aryl group with para CF.sub.3 functionality, an aryl group having C.sub.1-C.sub.20 partially fluorinated alkyl groups or partially fluorinated alkoxy groups, and a C.sub.1-C.sub.20 partially fluorinated aliphatic group, and a C.sub.1-C.sub.20 aryl group; and X is an anion. The method comprises cyclization of a halogenated acrylate with a formamidine with Hnig's base in a solvent.