- PYRIMIDINE DERIVATIVES AS PI3K INHIBITORS FOR USE IN THE TREATMENT OF CANCER
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The present inventions relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2a, R2b, R3, R4, R4a, R5- R23, g, j, m, n, x, y, and z are defined herein. The novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. Additional embodiments relate to pharmaceutical compositions containing the compounds and to methods of using the compounds and compositions in the treatment of abnormal cell growth in mammals.
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Page/Page column 90
(2016/02/28)
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- HETEROARYLOXYCARBOCYCLYL COMPOUNDS AS PDE10 INHIBITORS
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Heteroaryloxycarbocyclyl compounds of formula (I), and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive -compulsive disorder, and the like. Formula (I)
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Page/Page column 44
(2011/12/02)
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- Stereoselective synthesis of cis-1,3-disubstituted cyclobutyl kinase inhibitors
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Matrix presented. Two synthetic routes to a series of structurally novel kinase inhibitors containing a cis-1,3-disubstituted cyclobutane are described. The first route utilized addition of 3-aminocyclobutanol to 1,4-dinitroimidazole 5 as the crucial step in preparing 1, whereas the second route employed a novel 1,4-addition of 4-nitroimidazole 18 to in situ generated cyclobutenone 17 as the key reaction. This allowed for a stereoselective and shorter synthesis that eliminated the use of potentially explosive 1,4-dinitroimidazole 5.
- Helal, Christopher J.,Kang, Zhijun,Lucas, John C.,Bohall, Brooks R.
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p. 1853 - 1856
(2007/10/03)
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