C07D515/22

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.

Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication

The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. ##STR00001##

Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication

The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection. ##STR00001##

AZAINDAZOLE MACROCYCLE COMPOUNDS AND USES THEREOF
20240383911 · 2024-11-21 · ·

Provided in the present application are macrocyclic azaindazole compounds of Formula (I), and the use thereof. The compounds have the effect of inhibiting the activity of multiple protein kinases, comprising, for example, HPK1, FLT3 and KDR.

##STR00001##

AZAINDAZOLE MACROCYCLE COMPOUNDS AND USES THEREOF
20240383911 · 2024-11-21 · ·

Provided in the present application are macrocyclic azaindazole compounds of Formula (I), and the use thereof. The compounds have the effect of inhibiting the activity of multiple protein kinases, comprising, for example, HPK1, FLT3 and KDR.

##STR00001##

Modulators of Cystic Fibrosis Transmembrane Conductance Regulator, Pharmaceutical Compositions, Methods of Treatment, and Process for Making the Modulators

Compounds of Formula (I):

##STR00001##

pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

Modulators of Cystic Fibrosis Transmembrane Conductance Regulator, Pharmaceutical Compositions, Methods of Treatment, and Process for Making the Modulators

Compounds of Formula (I):

##STR00001##

pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.

IMPROVED PROCESS FOR THE PREPARATION OF LURBINECTEDIN AND ITS MORPHS THEREOF

The present invention provides unimproved synthetic process for the preparation of Lurbinectedin. The present invention also relates to new intermediates used in the preparation of Lurbinectedin. The present invention further provides new polymorphic form RK-1 of Lurbinectedin and process for producing the same. An improved process for the preparation of amorphous form of Lurbinectedin is also provided.

IMPROVED PROCESS FOR THE PREPARATION OF LURBINECTEDIN AND ITS MORPHS THEREOF

The present invention provides unimproved synthetic process for the preparation of Lurbinectedin. The present invention also relates to new intermediates used in the preparation of Lurbinectedin. The present invention further provides new polymorphic form RK-1 of Lurbinectedin and process for producing the same. An improved process for the preparation of amorphous form of Lurbinectedin is also provided.

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.