Patent classifications
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
- Wilfried Braje ,
- George Doherty ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew Judd ,
- Aaron Kunzer ,
- Anthony Mastracchio ,
- Xiaohong Song ,
- Andrew Souers ,
- Gerard Sullivan ,
- Zhi-Fu Tao ,
- Chunqiu Lai ,
- Andreas Kling ,
- Frauke Pohlki ,
- Jesse Teske ,
- Michael Wendt ,
- Patrick Brady ,
- Xilu Wang ,
- Thomas Penning ,
- Yujia Dai ,
- Jane Gong ,
- Roberto Risi ,
- Yiyun Yu ,
- Guidong ZHU ,
- Dominique POTIN ,
- Fabrice Guillier
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
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
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
- Patrick B. Brady ,
- Wilfried Braje ,
- Yujia Dai ,
- George A. Doherty ,
- Jane Gong ,
- Katja Jantos ,
- Cheng Ji ,
- Andrew S. Judd ,
- Aaron R. Kunzer ,
- Chunqiu Lai ,
- Anthony Mastracchio ,
- Roberto M. Risi ,
- Xiaohong Song ,
- Andrew J. Souers ,
- Gerard M. Sullivan ,
- Zhi-Fu Tao ,
- Jesse A. Teske ,
- Xilu Wang ,
- Michael D. Wendt ,
- Yiyun Yu ,
- Guidong ZHU ,
- Thomas D. Penning
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).