Patent classifications
C07D263/24
HETEROBICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS
Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
HETEROBICYCLIC SPHINGOSINE 1-PHOSPHATE ANALOGS
Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
METHODS FOR PRACTICAL SYNTHESIS OF DEUTERATED AMINO ACIDS
Disclosed are a deuterated compound of fomula (I), or a salt thereof, and methods for preparation thereof. The present disclosure may provide a mild, versatile organophotoredox method for the preparation of diverse, enantioenriched α-deuterated α-amino acids. In particular, the present disclosure may address the long-standing challenge of installing sterically demanding side chains into α-amino acids, including late-stage modifications on medicinal agents and natural products.
2-OXO-OXAZOLIDINE-5-CARBOXAMIDES AS NAV1.8 INHIBITORS
- Ashok Arasappan ,
- Ian M. Bell ,
- Christopher James Bungard ,
- Christopher S. Burgey ,
- Jason Michael Cox ,
- Deodial Guy Guiadeen, III ,
- Michael J. Kelly, III ,
- Mark E. Layton ,
- Hong Liu ,
- Jian Liu ,
- James T. Olsen ,
- James J. Perkins ,
- Jeffrey W. Schubert ,
- Akshay A. Shah ,
- Shawn J. Stachel ,
- Michael David VanHeyst ,
- Zhe Wu
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na.sub.v1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na.sub.v1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
##STR00001##
2-OXO-OXAZOLIDINE-5-CARBOXAMIDES AS NAV1.8 INHIBITORS
- Ashok Arasappan ,
- Ian M. Bell ,
- Christopher James Bungard ,
- Christopher S. Burgey ,
- Jason Michael Cox ,
- Deodial Guy Guiadeen, III ,
- Michael J. Kelly, III ,
- Mark E. Layton ,
- Hong Liu ,
- Jian Liu ,
- James T. Olsen ,
- James J. Perkins ,
- Jeffrey W. Schubert ,
- Akshay A. Shah ,
- Shawn J. Stachel ,
- Michael David VanHeyst ,
- Zhe Wu
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Na.sub.v1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Na.sub.v1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
##STR00001##
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. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
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. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS AND METHODS FOR MODULATING RNA FUNCTION
The present invention provides compounds, compositions thereof, and methods of using the same.
INHIBITORS OF INTEGRATED STRESS RESPONSE PATHWAY
The present disclosure relates generally to therapeutic agents that may be useful as inhibitors of Integrated Stress Response (ISR) pathway.