Patent classifications
C07D213/72
MODULATOR ASSAY
It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. Anew assay for identifying compounds with this mechanism of action is also disclosed.
HETEROARYL INHIBITORS OF PDE4
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
HETEROARYL INHIBITORS OF PDE4
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
COMPOUNDS
- Stephen Collingwood ,
- Clive McCarthy ,
- Jonathan David Hargrave ,
- Duncan Alexander Hay ,
- Thomas Beauregard Schofield ,
- Sarah Ellam ,
- Craig Stephen Buxton ,
- Matthew Habgood ,
- Peter Neville Ingram ,
- Chun Yan Ma ,
- Spencer Charles Robert Napier ,
- Abdul Kadar Shaikh ,
- Matthew Raymond Smith ,
- Christopher Charles Stimson ,
- Edward Richard Walker
Compounds of general formula (I): wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5a, R.sup.5b X.sup.1, X.sup.2, Z and Y are as defined herein are positive modulators of the calcium-activated chloride channel (CaCC), TMEM16A. The compounds are useful for treating diseases and conditions affected by modulation of TMEM16A, particularly respiratory diseases and conditions.
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HETEROARYL INHIBITORS OF PDE4
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
HETEROARYL INHIBITORS OF PDE4
The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.
RAF KINASE INHIBITORS AND METHODS OF USE THEREOF
Described herein are compounds that are RAF inhibitors and their use in the treatment of disorders such as cancers.
Method for identifying a modulator of the TNFα or CD40L interaction with their cognate receptors
It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
Method for identifying a modulator of the TNFα or CD40L interaction with their cognate receptors
It has been demonstrated that certain compounds bind to TNF and stabilise a conformation of trimeric TNF that binds to the TNF receptor. Accordingly, these compounds can be used as modulators of TNF. A new assay for identifying compounds with this mechanism of action is also disclosed.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ANDROGEN RECEPTOR
The present disclosure relates to bifunctional compounds, which find utility to degrade (and inhibit) Androgen Receptor. In particular, the present disclosure is directed to compounds, which contain on one end a cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds Androgen Receptor, such that Androgen Receptor is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of Androgen Receptor. The present disclosure exhibits a broad range of pharmacological activities associated with compounds according to the present disclosure, consistent with the degradation/inhibition of Androgen Receptor.