专利号:US-6646125-B1 优先权日:1997-10-14 标 题 :Process for the synthesis of chloropurine intermediates 发明人:JONES MARTIN FRANCIS; WALLIS CHRISTOPHER JOHN 权利人:SMITHKLINE BEECHAM CORP 摘要:The present invention relates to a process for the preparation of a carbocyclic purine nucleoside analogue of formula (I), its salts and pharmaceutically acceptable derivatives thereof which comprises hydrolysing a compound of formula (IV) wherein P is a protecting group, in the presence of an acid, condensing the product of formula (V) formed in situ in the presence of a base with a compound of formula (VI) followed by in situ ring closure of the resulting intermediate.
专利号:US-5874433-A 优先权日:1993-11-29 标题 :Blocking utilization of tetrahydrobiopterin to block induction of nitric oxide synthesis 发明人:GROSS STEVEN S 权利人:CORNELL RES FOUNDATION INC 摘要:Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock). The latter two types are advantageously administered with nitric oxide synthase inhibitors (concurrent therapy) or to potentiate the effect of α 1 -adrenergic agonists in the prophylaxis or treatment of induced hypotension.
专利号:UA-54550-C2 优先权日:1997-10-14 标题 :METHOD OF SYNTHESIS OF CHLORPURINE INTERMEDIATES
专利号:WO-9919327-A1 优先权日:1997-10-14 标题 :Process for the synthesis of chloropurine intermediates
专利号:EP-1023292-B1 优先权日:1997-10-14 标 题:Process for the synthesis of chloropurine intermediates
专利号:EP-1023292-A1 优先权日:1997-10-14 标 题:Process for the synthesis of chloropurine intermediates