专利号:US-6432933-B1 优先权日:1997-07-07 标 题 :Glycol and hydroxyphosphonate peptidomimetics as inhibitors of aspartyl proteases 发明人:CARROLL CAROLYN DIIANNI; DOLLE III ROLAND ELLWOOD; SHIMSHOCK YVONNE CLASS; HERPIN TIMOTHEE FELIX 权利人:PHARMACOPEIA INC 摘要:Compounds of Formula I n are disclosed as inhibitors having activity against the aspartyl proteases, plasmepsin and cathepsin D. The compounds are therefore useful for treatment of diseases such as malaria and Alzheimer's disease. In preferred compounds of Formula I, Y is an dialkoxyphosphonate, or α-hydroxyamide group and Z is an acyl or α-ketocarbamate functionality. Intermediates in the solid phase synthesis of compounds of Formula I, in which compounds are attached to a solid support, are also disclosed.
专利号:US-RE42890-E 优先权日:2003-05-23 标题 :Furazanobenzimidazoles 发明人:EBERLE MARTIN; BACHMANN FELIX; STREBEL ALESSANDRO; ROY SUBHO; SRIVASTAVA SUDHIR; SAHA GOUTAM 权利人:BASILEA PHARMACEUTICA AG 摘要:The invention relates to compounds of formula (I) wherein R represents aryl or heteroaryl, X is oxygen, a carbonyl group, an oxime derivative of a carbonyl group or an α,β-unsaturated carbonyl group, and the substituents R 1 to R 6 have the meanings given in the specification, for use as medicaments, to novel compounds of formula (I), to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same
专利号:US-6852711-B2 优先权日:1998-09-11 标题:HIV protease inhibitors 发明人:BOYER JR FREDERICK EARL; DOMAGALA JOHN MICHAEL; ELLSWORTH EDMUND LEE; GAJDA CHRISTOPHER ANDREW; HAGEN SUSAN ELIZABETH; LOVDAHL MICHAEL JAMES; LUNNEY ELIZABETH ANN; MARKOSKI LARRY JAMES; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN 权利人:AGOURON PHARMA 摘要:The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
专利号:US-4073795-A 优先权日:1976-06-22 标 题:Synthesis of tryptophans
专利号:DE-69202005-T2 优先权日:1991-06-24 标 题:Process for the synthesis of symmetrical N, N'-disubstituted aromatic ureas.
专利号:US-5198582-A 优先权日:1989-11-02 标 题 :Process for preparing symmetric N,N'-disubstituted aromatic urea 发明人:OH JAE S; LEE SANG M 权利人:LUCKY LTD 摘要:A process for preparing N,N'-disubstituted urea derivatives of the following formula (I) ##STR1## wherein Ar represents an unsubstituted aromatic radical or an aromatic radical substituted with a halogen atom, an alkyl group, or an alkoxy group, which comprises reacting an aromatic mono-nitro compound, an aromatic primary amine, and synthesis gas in the presence of a catalyst consisting essentially of a divalent palladium compound as a main catalyst component and an ammonium or a phosphonium salt containing halogen atom as a co-catalyst component, and a non-polar solvent.