Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H19BrF2N2O3 |
| Molecular Weight | 477.299 |
| Optical Activity | NONE |
| Additional Stereochemistry | Yes |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
| Stereo Comments | AXIAL, S |
SHOW SMILES / InChI
SMILES
CNC(=O)C1=CC=C(C)C(=C1)N2C(C)=CC(OCC3=CC=C(F)C=C3F)=C(Br)C2=O
InChI
InChIKey=KCAJXIDMCNPGHZ-UHFFFAOYSA-N
InChI=1S/C22H19BrF2N2O3/c1-12-4-5-14(21(28)26-3)9-18(12)27-13(2)8-19(20(23)22(27)29)30-11-15-6-7-16(24)10-17(15)25/h4-10H,11H2,1-3H3,(H,26,28)
PH-797804 is a diarylpyridinone inhibitor of p38alpha mitogen-activated protein. The drug was developed by Pfizer for the treatment of inflammatory diseases. PH-797804 is being tested in phase II of clinical trials in patients with COPD, osteoarthritis, rheumatoid arthritis and post-herpetic neuralgia.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL260 |
2.3 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Unknown Approved UseUnknown |
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| Primary | Unknown Approved UseUnknown |
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| Palliative | Unknown Approved UseUnknown |
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| Palliative | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
38.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/26265232/ |
30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered: |
PHA-797804 plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Design and synthesis of inhaled p38 inhibitors for the treatment of chronic obstructive pulmonary disease. | 2011-11-24 |
|
| Discovery of PH-797804, a highly selective and potent inhibitor of p38 MAP kinase. | 2011-07-01 |
|
| Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors. | 2011-07-01 |
Patents
Sample Use Guides
Chronic Obstructive Pulmonary Disease: PH-797804 should be orally administered at maximum dose of 10 mg. Neuralgia: 6 mg dose in oral capsule form, once daily for 28 days. Osteoarthritis: 6 mg once daily for 2 weeks. Rheumatoid Arthritis: the maximum dose is 10 mg taken once daily for 12 weeks.
Route of Administration:
Oral
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SUBSTANCE RECORD
