19808-30-1Relevant academic research and scientific papers
PYRIMIDINE AND TRIAZINE DERIVATIVES AND THEIR USE AS AXL INHIBITORS
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Page/Page column 88, (2016/07/05)
Compounds of the general formula(I): (I) processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
New P2X3 receptor antagonists. Part 2: Identification and SAR of quinazolinones
Szántó, Gábor,Makó, Attila,Vágó, István,Hergert, Tamás,Bata, Imre,Farkas, Bence,Kolok, Sándor,Vastag, Mónika
, p. 3905 - 3912 (2016/08/01)
Numerous potent P2X3 antagonists have been discovered and the therapeutic potential of P2X3 antagonism already comprises proof-of-concept data obtained in clinical trials with the most advanced compound. We have lately reported the discovery and optimization of thia-triaza-tricycle compounds with potent P2X3 antagonistic properties. This Letter describes the SAR of a back-up series containing a 4-oxo-quinazoline central ring. The discovery of the highly potent compounds 51 is presented.
IMIDAZOPYRROLIDINONE COMPOUNDS
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Page/Page column 125, (2013/08/15)
The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
PYRROLOPYRROLIDINONE COMPOUNDS
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Paragraph 0755; 0756, (2013/12/04)
The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
SUBSTITUTED 5-(PYRAZIN-2-YL)-1H-PYRAZOLO [3,4-B] PYRIDINE AND PYRAZOLO [3,4-B] PYRIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 21, (2012/10/18)
Substituted 5-(pyrazin-2-yl)-1H-pyrazolo [3,4-b] pyridine, 5-(pyrazin-2-yl)-1H-pyrrolo[2,3-b]pyridine and pyrazolo [3,4-b] pyridine derivatives according to formula I, II and VII, and methods for making same, which are inhibitors of constitutively activated Tyrosine Kinase-Like (TKL), CMGC protein kinases family members and can be useful in the treatment of Parkinson?s disease, Alzheimer?s disease, Down?s Syndrome, Huntington?s disease, other neurodegenerative and central nervous system disorders, cancer, metabolic disorders and inflammatory diseases. Also disclosed are pharmaceutical compositions including the compounds and methods of inhibiting wild type and/or mutated protein kinase activities of these families and the treatment of disorders associated there with using compounds and pharmaceutical compositions including the compounds.
Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors
Ameriks, Michael K.,Bembenek, Scott D.,Burdett, Matthew T.,Choong, Ingrid C.,Edwards, James P.,Gebauer, Damara,Gu, Yin,Karlsson, Lars,Purkey, Hans E.,Staker, Bart L.,Sun, Siquan,Thurmond, Robin L.,Zhu, Jian
scheme or table, p. 4060 - 4064 (2010/08/07)
A pyridazin-4-one fragment 4 (hCatS IC50 = 170 μM) discovered through Tethering was modeled into cathepsin S and predicted to overlap in S2 with the tetrahydropyridinepyrazole core of a previously disclosed series of CatS inhibitors. This fragment served as a template to design pyridazin-3-one 12 (hCatS IC50 = 430 nM), which also incorporates P3 and P5 binding elements. A crystal structure of 12 bound to Cys25Ser CatS led to the synthesis of the potent diazinone isomers 22 (hCatS IC50 = 60 nM) and 27 (hCatS IC50 = 40 nM).
Heterobicyclic pyrazole compounds and methods of use
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Page/Page column 75, (2008/06/13)
Compounds of Formulas Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting receptor tyrosine kinases and for treating disorders mediated thereby. Methods of using compounds of Formula Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
Phthalazine, aza- and diaza-phthalazine compounds and methods of use
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Page/Page column 48, (2008/06/13)
The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
Kinase inhibitors
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, (2008/06/13)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
Kinase inhibitors
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Page/Page column 72-73, (2010/01/31)
Compounds having the formula are useful for inhibiting protein kinases. Also disclosed are compositions which inhibit protein kinases and methods of inhibiting protein kinases in a patient.
