专利号:US-2006194971-A1 优先权日:2005-02-24 标 题 :Anethole dithiolethione and other dithiolethiones for the treatment of conditions associated with dysfunction of monoamine neruotransmission 发明人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T 权利人:DRUKARCH BENJAMIN; SCHOFFELMEER ANTON N; FEENSTRA ROELOF W; CHRISTEN MARIE-ODILE; BURGOT JEAN-LOUIS; CHOLLET MARYLENE; IWEMA BAKKER WOUTER I; VAN VLIET BERNARD J; TULP MARTINUS T 摘要:The present disclosure relates to dithiolethione derivatives as monoamino oxidase inhibitors, in particular MAO-B inhibitors, to methods for the preparation of these compounds and to novel intermediates useful for the synthesis of said dithiolethiones derivatives. The present disclosure also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. In embodiments of the present disclosure specific compounds disclosed herein are used for the manufacture of a medicament useful in the treatment, amelioration or prevention of conditions associated with dysfunction of monoamine neurotransmission. The compounds have the general formula (1) n nwherein the symbols have the meanings given in the specification.
专利号:US-3962217-A 优先权日:1969-10-24 标 题 :Process for the manufacture of Δ16 -steroid-14β,18,20-triols and -14β,20-diol-18-ols of the pregnane series 发明人:WEHRLI HANSULI; JEGER OSKAR 权利人:CIBA GEIGY CORP 摘要:The invention is for a selective reduction of the 20- oxo group in Δ 16 -steroid-14β,18-diol-20-ones of the pregnane series to form the two epimeric 20-alcohols having the 20 S and 20 R configuration. The process is especially intended for the manufacture of alkaloids of the batrachotoxin type, particularly for batrachotoxinine A, which is a pregnane derivative having a 20 S alcohol grouping, and epimers and derivatives, such as epi-batrachotixinine A or 7,8-dihydrobatrachotoxinine A. The process is characterized by reducing the said Δ 16 -steroid-14β,18-diol-20-ones in form of their 14,18-ketals, for instance the 14,18 acetonides and using appropriate complex light metal hydrides and operating at appropriate temperatures. The separation of the two isomers is easy and can be effected by the usual physical operations, such as crystallization or chromatography. In the 14β,18,20-triols obtained the 18-hydroxy group can be dehydrogenated to the corresponding 18-aldehydes, which are intermediates necessary in the synthesis of the said pharmacological interesting substances, such as batrachotoxin, by treatment with a sulphoxide in the presence of a carboxylic acid anhydride.
专利号:US-7291728-B2 优先权日:2004-05-10 标题:Spirolactams and their synthesis 发明人:MARIN PEDRO NOHEDA; PAJARES MANUEL BERNABE; QUINTANA SERGIO MAROTO; CANTERO NURIA TABARES 权利人:ESTEVE LABOR DR 摘要:The present invention is directed to a compound of formula I: n nwherein R 1 and R 2 are independently selected from H, halogen, protected or unprotected hydroxy, alkylsilyloxy, substituted or unsubstituted alkyl or cycloalkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, nitro, amino, mercapto or alkylthio;n R 3 and R 4 are independently selected from H, substituted alkyl, substituted or unsubstituted alkoxy or aryloxy, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl; Z is —(CRaRb) n — wherein n is a number selected from 1, 2, 3 and Ra and Rb are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy, substituted or unsubstituted amino or halogen; Y is selected from —O—, —S—, —N(Ra)— or —C(O)—, wherein Ra is as previously defined and does not form a cyclic ring; W is a group with sufficient electronic density to stabilize the compound through Ï€ interactions with the benzodienone moiety; or a salt thereof. n The present invention also provides a method for its synthesis and intermediates thereof, as well as a method for absorbing UV comprising exposing a compound of formula I to UV radiation.
专利号:US-2011015382-A1 优先权日:2008-11-29 标 题:Synthesis of N-FMOC protected deoxy nucleosides, ribo nucleosides, modified deoxy and ribo nucleosides, and phosphoramidites, and their use in oligonucleotide synthesis
专利号:US-2011245484-A1 优先权日:2010-03-31 标 题 :Stereoselective synthesis of phosphorus containing actives
专利号:WO-2010094587-A1 优先权日:2009-02-18 标 题:Microbial siderophore synthesis 发明人:WEBER THOMAS; BONGAERTS JOHANNES; EVERS STEFAN; MAURER KARL-HEINZ 权利人:HENKEL AG & CO KGAA; WEBER THOMAS; BONGAERTS JOHANNES; EVERS STEFAN; MAURER KARL-HEINZ 摘要:The product yield for siderophores in a microbial fermentation is improved if the fermented microorganisms have a reduced expression of the fur gene, in particular if the fermentation does not occur under a lack of iron.