- PHOSPHODIESTERASE INHIBITORS
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The present invention relates to purine derivatives, which can be used as selective phosphodiesterase (PDE) type IV inhibitors. Compounds disclosed herein can be useful in the treatment of asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases especially in humans. Also provided are processes for the preparation of disclosed compounds, pharmaceutical composition containing the disclosed compounds and their use as selective phosphodiesterase (PDE) type IV inhibitors.
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Page/Page column 36
(2008/06/13)
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- A Facile Synthesis of Trifluoromethylamines by Oxidative Desulfurization-Fluorination of Dithiocarbamates
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Trifluoromethylamines are easily synthesized from dithiocarbamates by a reagent system consisting of tetrabutylammonium dihydrogentrifluoride and an N-halo imide under mild conditions. When this reaction was applied to dithiocarbamates ArN(R)CS2Me at higher temperatures, the trifluoromethylation was accompanied by halogen substitution at the p-position of the Ar group. The synthesis of trifluoromethyl-substituted adenosine is also described.
- Kanie, Kiyoshi,Mizuno, Katsuya,Kuroboshi, Manabu,Hiyama, Tamejiro
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p. 1973 - 1991
(2007/10/03)
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- Process for preparing N6,9-disubstituted adenine
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A process for preparing N6, 9-disubstituted adenines which comprises reacting a metal salt of N6 -substituted adenine with a benzyl halide compound, preferably in the presence of a phase transfer catalyst. According to the process, the N6,9-disubstuted adenines can be obtained in high yields and good selectivity.
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- 6-(Alkylamino)-9-benzyl-9H-purines. A New Class of Anticonvulsant Agents
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Several 9-alkyl-6-substituted-purines were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats.Most compounds were prepared in three steps from 5-amino-4,6-dichloropyrimidine or in two steps via alkylation of 6-chloropurine.Potent anticonvulsant activity against MES resided in compounds that contain a benzyl substituent at the 9-position of 6-(methylamino)- or 6-(dimethylamino)purine.Among commonly used agents for control of seizures, this type of structure represents a new class of potent anticonvulsant agents.
- Kelley, James L.,Krochmal, Mark P.,Linn, James A.,McLean, Ed W.,Soroko, Francis E.
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p. 606 - 612
(2007/10/02)
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- Purines. XXVI. The Dimroth Rearrangement of 9-Substituted 1-Methyladenines: Accelerating Effect of a β-D-Ribofuranosyl Group at the 9-Position
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The reaction rates in the Dimroth rearrangements of 9-substituted 1-methyladenines (5a-i) were measured in H2O at various pH's and ionic strength 1.0 at 40 deg C.In all cases, attack of hydroxide ion on the protonated species of 5 at the 2-position was fa
- Fujii, Tozo,Saito, Tohru
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p. 3635 - 3644
(2007/10/02)
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