A61K31/497

SMALL MOLECULE RPN13 INHIBITORS WITH ANTITUMOR PROPERTIES

Compounds of formula (I), (II), and (III) having the structure shown below are presented: wherein R-R.sub.6 are defined herein. These molecules work as proteasome inhibitors and bind to the RPN13 subunit of the 19S regulatory particle, and can be used in methods of treating a condition or a disease, such as cancer, in a mammal

SMALL MOLECULE RPN13 INHIBITORS WITH ANTITUMOR PROPERTIES

Compounds of formula (I), (II), and (III) having the structure shown below are presented: wherein R-R.sub.6 are defined herein. These molecules work as proteasome inhibitors and bind to the RPN13 subunit of the 19S regulatory particle, and can be used in methods of treating a condition or a disease, such as cancer, in a mammal

MODULATORS OF INTEGRATED STRESS RESPONSE PATHWAY

The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

MODULATORS OF INTEGRATED STRESS RESPONSE PATHWAY

The present disclosure relates generally to therapeutic agents that may be useful as modulators of Integrated Stress Response (ISR) pathway.

SHP2 INHIBITORS AND USES THEREOF
20230010886 · 2023-01-12 ·

Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.

Pyrazine compounds and uses thereof

The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.

Pyrazine compounds and uses thereof

The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.

Pyrazine compounds and uses thereof

The present disclosure novel pyrazine compounds targeting adenosine receptors (especially A1 and A2, particularly A2a). The present disclosure also relates to pharmaceutical compositions comprising one or more of the compounds as an active ingredient, and use of the compounds in the treatment of adenosine receptor (AR) associated diseases, for example cancer such as NSCLC, RCC, prostate cancer, and breast cancer.

SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.

##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of

##STR00002##

Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.

##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

SALTS OF PRODRUGS OF PIPERAZINE AND SUBSTITUTED PIPERIDINE ANTIVIRAL AGENTS

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.

##STR00001## wherein: X is C or N with the proviso that when X is N, R.sup.1 does not exist; W is C or N with the proviso that when W is N, R.sup.2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of

##STR00002##

Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.

##STR00003## wherein: L and M are independently selected from the group consisting of C.sub.1-C.sub.6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.