专利号:US-9938509-B2 优先权日:2010-12-08 标 题 :Biocatalysts and methods for the synthesis of armodafinil 发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN 权利人:CODEXIS INC 摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.
专利号:US-8932838-B2 优先权日:2010-06-17 标 题 :Biocatalysts and methods for the synthesis of (S)-3-(1-aminoethyl)-phenol 发明人:CABIROL FABIEN LOUIS; GOHEL ANUPAM; OH SEONG HO; SMITH DEREK J; WONG BRIAN; LALONDE JAMES J 权利人:CODEXIS INC 摘要:The present disclosure provides engineered transaminase polypeptides having improved properties as compared to naturally occurring transaminases including the ability of converting the substrate, 3′-hydroxyacetophenone to (S)-3-(1-aminoethyl)-phenol in enantiomeric excess and high percentage conversion. Also provided are polynucleotides encoding the engineered transaminases, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases to synthesize (S)-3-(1-aminoethyl)-phenol and related compounds useful in the production of active pharmaceutical ingredients.
专利号:US-8932836-B2 优先权日:2010-08-16 标 题:Biocatalysts and methods for the synthesis of (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine 发明人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK 权利人:LIMANTO JOHN; BEUTNER GREGORY; GRAU BRENDAN; JANEY JACOB; KLAPARS ARTIS; ASHLEY ERIC R; STROTMAN HALLENA R; TRUPPO MATTHEW D; HUGHES GREGORY; CABIROL FABIEN; GOHEL ANUPAM; COLLIER STEVEN J; LIANG JACK; MOCK MARISSA; MUNDORFF EMILY; NOVICK SCOTT; SMITH DEREK; CODEXIS INC 摘要:The disclosure provides transaminase polypeptides capable of converting the substrate, 2-(3,4-dimethoxyphenethoxy)cyclohexanone to the trans diastereomer product (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine in at least a 2:1 diastereomeric ratio relative to the cis diastereomer (1R,2S)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine. The disclosure also provides polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides in processes for preparing (1R,2R)-2-(3,4-dimethoxyphenethoxy)cyclohexanamine and its analogs, which can product compounds can be further used to prepare the aminocyclohexylether compound, (3R)-1-[(1R,2R)-2-[2-(3,4-dimethoxyphenyl)ethoxy]cyclohexyl]pyrrolidin-3-ol, which is an ion channel blocker.
专利号:US-9624478-B2 优先权日:2011-09-08 标题:Biocatalysts and methods for the synthesis of substituted lactams 发明人:CABIROL FABIEN LOUIS; CHEN HAIBIN; GOHEL ANUPAM; SALIM PAULINA ELENA; SMITH DEREK J; JANEY JACOB; KOSJEK BIRGIT; TANG WENG LIN; HSIEH HELEN; PHAM SON Q 权利人:CODEXIS INC 摘要:The present disclosure relates to transaminase polypeptides capable of aminating a dicarbonyl substrate, and polynucleotides, vectors, host cells, and methods of making and using the transaminase polypeptides.
专利号:US-9631181-B2 优先权日:2009-12-08 标 题 :Synthesis of prazole compounds 发明人:BONG YONG KOY; CLAY MICHAEL D; COLLIER STEVEN J; MIJTS BENJAMIN; VOGEL MICHAEL; ZHANG XIYUN; ZHU JUN; NAZOR JOVANA; SMITH DEREK J; SONG SHIWEI 权利人:CODEXIS INC 摘要:The present disclosure relates to non-naturally occurring monooxygenase polypeptides useful for preparing prazole compounds, polynucleotides encoding the polypeptides, and methods of using the polypeptides.
专利号:US-2005214310-A1 优先权日:2004-01-23 标 题 :Melphalan prodrugs 发明人:TOKI BRIAN E; SENTER PETER D 权利人:SEATTLE GENETICS INC 摘要:Shown and described are the synthesis of more potent forms of C-Mel, a prodrug used in Antibody-Directed Enzyme Prodrug Therapy, that releases the clinically used anticancer alkylating agent melphalan extracellularly. Shown and described are the synthesis of a variety of melphalan analogues with the intention to promote facile intracellular drug access. Esters, amides, and peptides of melphalan are shown. Cephalosporin prodrugs of the most interesting melphalan derivatives were synthesized and evaluated for potency, toxicity, therapeutic window, plasma stability, and solubility.
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