Patent classifications
C07D207/26
MODULATORS OF THE INTEGRATED STRESS PATHWAY
Provided herein are compounds of Formula (I) or Formula (II), compositions, and methods there of useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions.
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 the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Compounds and methods for the enhanced degradation of targeted proteins and other polypeptides by an E3 ubiquitin ligase
The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
Levetiracetam Immunoassays
Methods, compositions and kits are disclosed directed at levetiracetam derivatives, immunogens, signal generating moieties, antibodies that bind levetiracetam and immunoassays for detection of levetiracetam.
Levetiracetam Immunoassays
Methods, compositions and kits are disclosed directed at levetiracetam derivatives, immunogens, signal generating moieties, antibodies that bind levetiracetam and immunoassays for detection of levetiracetam.
ANTIVIRAL COMPOUNDS
The present invention relates to novel compounds of general formula (I) wherein R.sup.1 to R.sup.4 and n have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
##STR00001##
ANTIVIRAL COMPOUNDS
The present invention relates to novel compounds of general formula (I) wherein R.sup.1 to R.sup.4 and n have the meanings given in the description and claims, process for preparing these compounds and their use as for treating, preventing or ameliorating viral infections and their use for treating, preventing or ameliorating diseases which are associated with PLA2G16.
##STR00001##
DIFLUOROLACTAM COMPOUNDS AS EP4 RECEPTOR-SELECTIVE AGONISTS FOR USE IN THE TREATMENT OF EP4-MEDIATED DISEASES AND CONDITIONS
Disclosed herein are compounds of formula (I)
##STR00001##
and therapeutic methods of treatment with compounds of formula (I), wherein L.sup.1, L.sup.2, L.sup.4, R.sup.1, R.sup.4, R.sup.5, R.sup.6, and s are as defined in the specification. Compounds of formula (I) are EP4 agonists useful in the treatment of glaucoma, neuropathic pain, and related disorders.