- PYRAZOLO[3,4-B]PYRIDINES AND IMIDAZO[1,5-B]PYRIDAZINES AS PDE1 INHIBITORS
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The present invention provides compounds of formula (I) that are PDEl enzyme inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders. The present invention also provides pharmaceutical compositions comprising compounds of the invention and methods of treating disorders using the compounds of the invention.
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Page/Page column 77
(2019/07/13)
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- OXAZOLE AND THIAZOLE DERIVATIVES AS SELECTIVE PROTEIN KINASE INHIBITORS (C-KIT)
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The present invention relates to compounds of formula I or pharmaceutically acceptable salts thereof: wherein R1, R2, R3, A, Q, W and X are as defined in the description. These compounds selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective native and/or mutant c-kit inhibitors.
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- SUBSTITUTED PYRIDONE COMPOUNDS AND METHODS OF USE
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The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula: (I); wherein A0-3 and R1-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 49
(2008/06/13)
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- ALKYNE-SUBSTITUTED PYRIDONE COMPOUNDS AND METHODS OF USE
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The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I "INSERT STRUCTURE HERE" wherein A1-3, R1 and R3-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
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Page/Page column 32
(2008/06/13)
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- Efficient regioselective preparation of monobromo and bromoiodo hydroxy pyridines from dibromoderivatives via bromine-lithium exchange
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Annular dibromination of hydroxypyridines with NBS in acetonitrile followed by bromine-lithium exchange with RLi and subsequent trapping with H2O or I2 afforded monobromo and bromoiodo derivatives in a completely regioselective way. Iodination of bromo hydroxypyridines with NIS is totally regioselective.
- Meana, ángela,Rodríguez, Justo F.,Sanz-Tejedor, M. Ascensión,García-Ruano, José L.
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p. 1678 - 1682
(2007/10/03)
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