C07D497/22

MACROCYLIC SULFONYL DERIVATIVES MCL-1 INHIBITORS

The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

MACROCYLIC SULFONYL DERIVATIVES MCL-1 INHIBITORS

The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical composition comprising such compounds, and their use as MCL-1 inhibitors, useful for treating diseases such as cancer.

Macrocyclic indoles as Mcl-1 inhibitors

Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R.sup.1a, R.sup.1b, R.sup.1h, L.sup.2, L.sup.3, #, #, # are as defined as set forth in the re) specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer. ##STR00001##

Hexacyclic heteroaromatic compounds for electronic devices

The invention relates to heteroaromatic compounds, particularly for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention and to electronic devices containing same.

MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS

Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R.sup.1a, R.sup.1b, L.sup.1, L.sup.2, L.sup.3, X, A, B and C are as defined as set forth in the specification. Also provided compounds of Formula IA for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

##STR00001##

MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS

Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R.sup.1a, R.sup.1b, L.sup.1, L.sup.2, L.sup.3, X, A, B and C are as defined as set forth in the specification. Also provided compounds of Formula IA for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.

##STR00001##

Mcl-1 inhibitors and methods of use thereof

Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) ##STR00001##
and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.

Mcl-1 inhibitors and methods of use thereof

Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I) ##STR00001##
and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.

METHODS AND COMPOSITIONS FOR SENSITIZING CANCER CELLS TO DRUG-INDUCED APOPTOSIS
20220323376 · 2022-10-13 ·

Disclosed herein are methods of increasing the sensitivity of cancer cells to cell death by an apoptosis-inducing drug. Also disclosed herein are methods of treating cancer in a subject and combination therapeutics.

MCL-1 INHIBITORS AND METHODS OF USE THEREOF

Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid (Formula I)

##STR00001##

and enantiomers and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions of 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1.sup.4,7.0.sup.11,15.0.sup.16,21.0.sup.20,24.0.sup.30,35]octatriaconta-1(37),4(38),6,11,14,16,18,20,23,29,31,33,35-tridecaene-23-carboxylic acid, and enantiomers and pharmaceutically acceptable salts thereof, and methods of treating cancer with such compounds and compositions.