- PHOSPHODIESTERASE 10 INHIBITORS
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The present invention if directed to certain cinnoline compounds that are PDE10 inhibitors, pharmaceutical compositions containing such compounds and processes for preparing such compounds. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 57
(2008/06/13)
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- CINNOLINE AND QUINAZOLINE DERIVATES AS PHOSPHODIESTERASE 10 INHIBITORS
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The present invention is directed to cinnoline and quinazoline compounds of formula (I) that are PDE10 inhibitors, pharmaceutical compounds containing the same and processes for preparing the same. The invention is also directed to methods of treating diseases mediated by PDE10 enzyme such as obesity, non-insulin dependent diabetes, schizophrenia or bipolar disorder, obsessive-compulsive disorder, and the like.
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Page/Page column 53-54
(2010/11/28)
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- COMPOUNDS AND METHODS FOR THE TREATMENT OF VIRUSES AND CANCER
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The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group;; R2 , R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
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Page/Page column 24; 25
(2010/11/26)
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- Optimization of diarylamines as non-nucleoside inhibitors of HIV-1 reverse transcriptase
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Following computational analyses, potential non-nucleoside inhibitors of HIV-1 reverse transcriptase have been pursued through synthesis and assaying for anti-viral activity. The general class Het-NH-Ph-U has been considered, where Het is an aromatic heterocycle and U is an unsaturated, hydrophobic group. Results for compounds with Het = 2-thiazoyl and 2-pyrimidinyl are the focus of this report.
- Ruiz-Caro, Juliana,Basavapathruni, Aravind,Kim, Joseph T.,Bailey, Christopher M.,Wang, Ligong,Anderson, Karen S.,Hamilton, Andrew D.,Jorgensen, William L.
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p. 668 - 671
(2007/10/03)
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