224040-86-2Relevant academic research and scientific papers
MAP KINASE MODULATORS AND USES THEREOF
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Paragraph 00247; 00322, (2014/09/29)
The invention provides for novel MAP kinase inhibitors and compositions comprising the same. In some embodiments, the MAP kinase inhibitors are p38a MAP kinase inhibitors. The invention further provides for methods for treatment of diseases comprising adm
Highly selective c-Jun N-terminal kinase (JNK) 3 inhibitors with in vitro CNS-like pharmacokinetic properties II. Central core replacement
Neitz, R. Jeffrey,Konradi, Andrei W.,Sham, Hing L.,Zmolek, Wes,Wong, Karina,Qin, Ann,Lorentzen, Colin,Nakamura, David,Quinn, Kevin P.,Sauer, John-Michael,Powell, Kyle,Ruslim, Lany,Chereau, David,Ren, Zhao,Anderson, John,Bard, Frederique,Yednock, Ted A.,Griswold-Prenner, Irene
scheme or table, p. 3726 - 3729 (2011/08/06)
In this Letter, we describe the evolution of selective JNK3 inhibitors from 1, that routinely exhibit >10-fold selectivity over JNK1 and >1000-fold selectivity over related MAPKs. Strong SAR was found for substitution of the naphthalene ring, as well as f
Pyridinylimidazole inhibitors of Tie2 kinase
Semones, Marcus,Feng, Yanhong,Johnson, Neil,Adams, Jerry L.,Winkler, Jim,Hansbury, Michael
, p. 4756 - 4760 (2008/12/21)
This communication details the evolution of the screening lead SB-203580, a known CSBP/p38 kinase inhibitor, into a potent and selective Tie2 tyrosine kinase inhibitor. The optimized compound 5 showed efficacy in an in vivo model of angiogenesis and a MOP
Design and synthesis of potent pyridazine inhibitors of p38 MAP kinase
Tamayo, Nuria,Liao, Lillian,Goldberg, Martin,Powers, David,Tudor, Yan-Yan,Yu, Violeta,Wong, Lu Min,Henkle, Bradley,Middleton, Scot,Syed, Rashid,Harvey, Timothy,Jang, Graham,Hungate, Randall,Dominguez, Celia
, p. 2409 - 2413 (2007/10/03)
Novel potent trisubstituted pyridazine inhibitors of p38 MAP (mitogen activated protein) kinase are described that have activity in both cell-based assays of cytokine release and animal models of rheumatoid arthritis. They demonstrated potent inhibition o
SUBSTITUTED HETEROCYCLIC COMPOUNDS AND METHODS OF USE
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Page 52, (2008/06/13)
The present invention relates to compounds having the general formula (I) or a pharmaceutically acceptable salt thereof, wherein Rl is a saturated or unsaturated 5-, 6- or 7-membered, ring containing 0, 1, 2 or 3 atoms selected from N, O and S, wherein the ring may be fused with a benzo group, and is substituted by 0, 1 or 2 oxo groups, and wherein R1 is additionally substituted; and R2 is a substituted C1-6balkyl. Also included is a method of prophylaxis or treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis, multiple myeloma, uveititis, acute or chronic myelogenous leukemia, pancreatic β cell destruction, osteoarthritis, rheumatoid spondylitis, gouty arthritis, inflammatory bowel disease, adult respiratory distress syndrome (ARDS), psoriasis, Crohn's disease, allergic rhinitis, ulcerative colitis, anaphylaxis, contact dermatitis, asthma, muscle degeneration, cachexia, Reiter's syndrome, type I diabetes, type II diabetes, bone resorption diseases, graft vs. host reaction, Alzheimer's disease, stroke, myocardial infarction, ischemia reperfusion injury, atherosclerosis, brain trauma, multiple sclerosis, cerebral malaria, sepsis, septic shock, toxic shock syndrome, fever, myalgias due to HIV-1, HIV-2, HIV-3, cytomegalovirus (CMV), influenza, adenovirus, the herpes viruses or herpes zoster infection in a mammal comprising administering an effective amount a compound as described above.
Adenosine A3 receptor antagonists
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, (2008/06/13)
A pharmaceutical composition for antagonizing adenosine at adenosine A3receptors which comprises a 1,3-azole compound substituted on the 4- or 5-position, or both, by a pyridyl which may be substituted is provided and can be used as a prophylactic and therapeutic agent for asthma, allergosis, inflammation, and so on.
