- PYRAZOLO[1,5-A]TRIAZIN-4-AMINE DERIVATIVES USEFUL IN THERAPY
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A compound of formula (I), or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.
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- PYRAZOLO[1,5-A]PYRIMIDINES AS ANTIVIRAL COMPOUNDS
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A compound of formula (I) or a pharmaceutically acceptable salt thereof, useful in therapy, in particular in the treatment of a viral infection.
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- Phenoxide leaving group SNAr strategy for the facile preparation of 7-amino-3-aryl pyrazolo[1,5-a]pyrimidines from a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate
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We have discovered a 3-bromo-7-phenoxypyrazolo[1,5-a]pyrimidine intermediate that allows for the direct sequential funtionalization of the 3-position and 7-position of a pyrazolo[1,5-a]pyrimidine scaffold. The intermediate and general method described herein offer an improvement over prior methods, particularly in cases where multiple unique 3-aryl substituents are to be incorporated in conjunction with multiple unique 7-amino substituents.
- Catalano, John G.,Gaitonde, Vishwanath,Beesu, Mallesh,Leivers, Anna L.,Shotwell, J. Brad
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p. 6077 - 6079
(2015/10/28)
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- ANAPLASTIC LYMPHOMA KINASE MODULATORS AND METHODS OF USE
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The present invention comprises compounds and pharmaceutical compositions comprising the compounds that are inhibitors of ALK. The invention also comprises methods of using the compounds and compositions to treat diseases mediated by ALK, including diseases such as cancer, immunological disorders, cardiovascular diseases, and other degenerative disorders.
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- Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility
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In our efforts to identify potent CRF1 antagonists with proper physicochemical properties, a series of 3-phenylpyrazolo[1,5-a]pyrimidines bearing polar groups, such as amino, hydroxyl, methoxy, sulfoxide, were designed and synthesized. Several positions of the core structure were identified, where a polar group was tolerated with slight reduction in receptor binding. NBI 30545 (18n) was found to have good binding affinity and potent antagonistic activity at the human CRF1 receptor. Moreover, this compound had proper lipophilicity (logD=2.78) and good solubility in water (>10mg/mL), and exhibited good plasma and brain exposure when given orally.
- Chen, Chen,Wilcoxen, Keith M.,Huang, Charles Q.,McCarthy, James R.,Chen, Takung,Grigoriadis, Dimitri E.
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p. 3669 - 3673
(2007/10/03)
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