Patent classifications
C07D209/52
Inhibitors of glycogen synthase 1 (GYS1) and methods of use thereof
Provided herein are compounds of formula (I′): ##STR00001##
or a stereoisomer or tautomer thereof, or a pharmaceutically acceptable salt of any of the foregoing, wherein Y.sup.2, Y.sup.3, L.sup.1, L.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, Q.sup.1, R.sup.1, R.sup.2, R.sup.k, R.sup.m, and R.sup.n are as defined elsewhere herein. Also provided herein are methods of preparing compounds of formula (I′). Also provided herein are methods of inhibiting GYS1 and methods of treating a GYS1-mediated disease, disorder, or condition in an individual in need thereof.
Bicyclic-Fused Heteroaryl or Aryl Compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
##STR00001##
as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.
Bicyclic-Fused Heteroaryl or Aryl Compounds
- John David Trzupek ,
- Katherine Lin Lee ,
- Mark Edward Bunnage ,
- Seungil Han ,
- David Hepworth ,
- Frank Eldridge Lovering ,
- John Paul Mathias ,
- Nikolaos Papaioannou ,
- Betsy Susan Pierce ,
- Joseph Walter Strohbach ,
- Stephen Wayne Wright ,
- Christoph Wolfgang Zapf ,
- Lori Krim Gavrin ,
- Arthur Lee ,
- David Randolph Anderson ,
- Kevin Joseph Curran ,
- Christoph Martin Dehnhardt ,
- Eddine Saiah ,
- Joel Adam Goldberg ,
- Xiaolun Wang ,
- Horng-Chih Huang ,
- Richard Vargas ,
- Michael Dennis Lowe ,
- Akshay Patny
Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia,
##STR00001##
as defined in the specification. In an embodiment, a pharmaceutical composition can be in a liquid dosage form and can comprise a therapeutically effective amount of the compound or a pharmaceutically acceptable salt thereof as an adjuvant and a therapeutic agent. In another embodiment, a method of adjuvant treating a disorder or condition can comprising administering the pharmaceutical composition to a patient.
Antagonists of the muscarinic acetylcholine receptor M.SUB.4
Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M.sub.4 (mAChR M.sub.4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
Antagonists of the muscarinic acetylcholine receptor M.SUB.4
Disclosed herein are substituted hexahydro-1H-cyclopenta[c]pyrrole compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M.sub.4 (mAChR M.sub.4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.
N-ALKYLARYL-5-OXYARYL-OCTAHYDRO-CYCLOPENTA[C]PYRROLE NEGATIVE ALLOSTERIC MODULATORS OF NR2B
The present disclosure relates to N-alkylaryl-5-oxyaryl-octadihydrocyclopent[c]pyrrole negative allosteric modulators of NR2B receptors useful in the treatment of neurological diseases having the Formula I:
##STR00001##
where R.sub.1, R.sub.2, L.sub.1, L.sub.2, X, Y, and Y′ are described therein.
N-ALKYLARYL-5-OXYARYL-OCTAHYDRO-CYCLOPENTA[C]PYRROLE NEGATIVE ALLOSTERIC MODULATORS OF NR2B
The present disclosure relates to N-alkylaryl-5-oxyaryl-octadihydrocyclopent[c]pyrrole negative allosteric modulators of NR2B receptors useful in the treatment of neurological diseases having the Formula I:
##STR00001##
where R.sub.1, R.sub.2, L.sub.1, L.sub.2, X, Y, and Y′ are described therein.
Thalidomide analogs and methods of use
Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.
Thalidomide analogs and methods of use
Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.
BISAMIDE SARCOMERE ACTIVATING COMPOUNDS AND USES THEREOF
- Luke Ashcraft ,
- Alessandro Boezio ,
- John Butler ,
- Aroop CHANDRA ,
- Chihyuan Chuang ,
- Scott E. Collibee ,
- Mikkel Debenedetto ,
- Vincent Dimassa ,
- Russell Graceffa ,
- Justin Malinowski ,
- David Moebius ,
- Bradley P. Morgan ,
- Joshua Payette ,
- Antonio ROMERO ,
- David St. Jean, Jr. ,
- Richard Vargas ,
- John Yeoman ,
- Hanmo Zhang ,
- Alan Cheng ,
- Felix Gonzalez Lopez De Turiso ,
- Michael Garrett Johnson
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
##STR00001##