C07D495/18

Heterocyclic compounds and their use in preventing or treating bacterial infections

The present invention relates to compounds of formula (I) and their use for treating or preventing a bacterial infection or as an antibacterial agent and/or as a -lactamase inhibitor.

CRYSTALLINE FORMS OF COMPOUNDS FOR PREVENTING OR TREATING SENSORY HAIR CELL DEATH

Described herein is (4R,7,S)-2-(3-(4-chlorophenyl)ureido)-9-methyl-5,6,7,8-tetrahydro-4H-4,7-epiminocyclohepta[b]thiophene-3-carboxamide mesylate, including crystalline forms and solvates thereof.

CRYSTALLINE FORMS OF COMPOUNDS FOR PREVENTING OR TREATING SENSORY HAIR CELL DEATH

Described herein is (4R,7,S)-2-(3-(4-chlorophenyl)ureido)-9-methyl-5,6,7,8-tetrahydro-4H-4,7-epiminocyclohepta[b]thiophene-3-carboxamide mesylate, including crystalline forms and solvates thereof.

Macrocyclic MCL-1 Inhibitors and Methods of Use

The present disclosure provides for compounds of formula (I)

##STR00001##

wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

Macrocyclic MCL-1 Inhibitors and Methods of Use

The present disclosure provides for compounds of formula (I)

##STR00001##

wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of formula (I).

SYNTHESIS OF CANTHARIDIN

The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

##STR00001##

MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE

The present disclosure provides for compounds of Formula (I)

##STR00001##

wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).

Diindole Compounds Useful In Treatment of Nervous System Disorders
20200095200 · 2020-03-26 ·

The invention provides bridged diindole compounds, related pharmaceutical compositions and methods of use thereof, for the prevention, palliation and/or treatment of nervous system disorders.

Diindole Compounds Useful In Treatment of Nervous System Disorders
20200095200 · 2020-03-26 ·

The invention provides bridged diindole compounds, related pharmaceutical compositions and methods of use thereof, for the prevention, palliation and/or treatment of nervous system disorders.

Macrocyclic MCL-1 Inhibitors and Methods of Use

The present disclosure provides for compounds of Formula (I)

##STR00001##

wherein A.sup.2, A.sup.3, A.sup.4, A.sup.6, A.sup.7, A.sup.8, A.sup.15, R.sup.A, R.sup.5, R.sup.9, R.sup.10A, R.sup.10B, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents for the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).