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专利信息

专利号:US-5817751-A
优先权日:1994-06-23
标 题 :Method for synthesis of diketopiperazine and diketomorpholine derivatives
发明人：SZARDENINGS ANNA KATRIN; CAMPBELL DAVID
权利人:AFFYMAX TECH NV
摘要:The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.

专利号:US-4427587-A
优先权日:1982-11-10
标 题:Total synthesis of antitumor antibiotics BBM-2040A and BBM-2040B
发明人：KANEKO TAKUSHI; WONG HENRY S L
权利人:BRISTOL MYERS CO
摘要:A new chemical synthesis of the pyrrolobenzodiazepine antibiotics BBM-2040A and B is disclosed. The disclosed total synthesis uses readily available starting materials and provides a useful alternative to the microbiological procedure previously used to prepare these antibiotics.

专利号:US-10787458-B2
优先权日:2014-09-25
标 题:Chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-A]pyrazines
发明人：HOVEYDA HAMID; DUTHEUIL GUILLAUME
权利人:OGEDA SA
摘要:Disclosed is a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I): n nor a solvate thereof. The novel chiral synthesis avoids the use of protection/deprotection steps.

专利号:US-2011130578-A1
优先权日:2009-06-03
标题 :Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
发明人：FANDRICK DANIEL R; KUZMICH DANIEL; REEVES JONATHAN T; SONG JINHUA J; TAN ZHULIN; LEE THOMAS
权利人:BOEHRINGER INGELHEIM INT
摘要:A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) n n n n n n n n n n wherein:n R 1 is an aryl group substituted with one to three substituent groups,n wherein each substituent group of R 1 is independently C 1 -C 5 alkyl, C 2 -C 5 alkenyl, C 2 -C 5 alkynyl, C 1 -C 5 alkoxy, C 1 -C 5 alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, C 1 -C 5 alkoxycarbonylamino, aminosulfonyl, C 1 -C 5 alkylaminosulfonyl, C 1 -C 5 dialkylaminosulfonyl, halogen, hydroxy, carboxy, cyano, trifluoromethyl, trifluoromethoxy, nitro, or C 1 -C 5 alkylthio wherein the sulfur atom is oxidized to sulfoxide or sulfone, and n R 2 and R 3 are each independently hydrogen or C 1 -C 5 alkyl.

专利号:US-7256300-B2
优先权日:2004-03-30
标 题:Stereoselective synthesis of certain trifluoromethyl-substituted alcohols
发明人：LEE THOMAS WAI-HO; PROUDFOOT JOHN ROBERT
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:A process for stereoselective synthesis of a compound of Formula (X) or Formula (X′) n nwherein R 1 , R 2 , and R 3 are as defined herein, the process comprising:n (a) reacting the starting material of formula A with a chiral sulfoxide anion source in a suitable solvent to prepare a compound of formula C or C′; (b) reducing the sulfoxide of formula C or C′ in a suitable solvent to obtain the compound of formula D or D′; and (c) cyclizing the compound of formula D or D′ in a suitable solvent to form the epoxide compound of Formula (X) or Formula (X′),n nor a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

专利号:US-9475814-B2
优先权日:2011-10-03
标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof
发明人：HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC
权利人:EUROSCREEN SA
摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.