Patent classifications
C07D243/14
COMPOUNDS FOR USE IN ANTI-CANCER IMMUNOTHERAPY
The present disclosure relates to the reversal of T cell exhaustion using aplysiatoxin analogs or PKC theta agonist compounds for anti-cancer immunotherapy. The treatment with aplysiatoxin analogs or PKC theta agonist compounds improve the anti-tumour activity of a T cell, inducing a NFAT-dependent T cell activation, increasing the pool of immune-checkpoint inhibitor responsive T cells, increasing lymphocyte infiltration and increasing the population of activated CD4+ and/or CD8+ cells. The methods of the present disclosure provide treatment of tumors and infections.
3-ARYL-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-ARYL-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.
KRAS G12C INHIBITORS AND METHODS OF USING THE SAME
- John Gordon Allen ,
- Brian Alan Lanman ,
- Jian CHEN ,
- Anthony B. Reed ,
- Victor J. Cee ,
- Longbin Liu ,
- Patricia Lopez ,
- Ryan Paul Wurz ,
- Thomas T. Nguyen ,
- Shon Booker ,
- Jennifer Rebecca ALLEN ,
- Margaret CHU-MOYER ,
- Albert AMEGADZIE ,
- Ning Chen ,
- Clifford GOODMAN ,
- Jonathan D. LOW ,
- Vu Van MA ,
- Ana Elena MINATTI ,
- Nobuko Nishimura ,
- Alexander J. Pickrell ,
- Hui-Ling WANG ,
- Youngsook SHIN ,
- Aaron C. Siegmund ,
- Kevin C. Yang ,
- Nuria A. TAMAYO ,
- Mary WALTON ,
- Qiufen XUE
Provided herein are KRAS G12C inhibitors, such as
##STR00001##
composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.
Compounds for the Treatment of Alzheimer's Disease
The present disclosure provides compounds that are amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.
Compounds for the Treatment of Alzheimer's Disease
The present disclosure provides compounds that are amylin receptor antagonist compounds, compositions that include the subject compounds, methods for preparing and using the amylin receptor antagonists, and compositions containing the amylin receptor antagonists for treating, preventing, or ameliorating Alzheimer's disease. Aspects of the present disclosure include a method of inhibiting activity of an amylin receptor by administering to a subject in need thereof a therapeutically effective amount of an amylin receptor antagonist.
INHIBITORS OF EGFR AND METHODS OF USE THEREOF
The application relates to compounds, or pharmaceutically acceptable salts, hydrates, solvates, or stereoisomers thereof, which modulate the activity of EGFR, a pharmaceutical composition comprising said compounds, and methods of treating or preventing a disease in which EGFR plays a role.
INHIBITORS OF EGFR AND METHODS OF USE THEREOF
The application relates to compounds, or pharmaceutically acceptable salts, hydrates, solvates, or stereoisomers thereof, which modulate the activity of EGFR, a pharmaceutical composition comprising said compounds, and methods of treating or preventing a disease in which EGFR plays a role.
Therapeutic compounds and uses thereof
The present invention relates to compounds of formula (I) and formula (II): ##STR00001##
and to salts thereof, wherein R.sup.1-R.sup.4 of formula (I) and R.sup.5-R.sup.6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Therapeutic compounds and uses thereof
The present invention relates to compounds of formula (I) and formula (II): ##STR00001##
and to salts thereof, wherein R.sup.1-R.sup.4 of formula (I) and R.sup.5-R.sup.6 of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II), or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.