Biocatalysis for the synthesis of pharmaceuticals and pharmaceutical intermediates.

On the development of new biocatalytic processes for practical pharmaceutical synthesis.

Biocatalysis in Drug Development—Highlights of the Recent Patent Literature

The chiral feature is a critical factor for the efficacy and safety of many therapeutic agents. At present, about 57% of marketed drugs are chiral drugs and about 99% of purified natural products are chiral compounds. There has been a tremendous potential of functional microorganisms and biocatalysts derived from them for the bioconversion of synthetic chemicals into drugs with high enantio-, chemo-, and regio-selectivities. Biocatalysis is becoming a key subassembly in the medicinal chemist’s toolbox. In fact, the intermediates of many important therapeutic agents such as sitagliptin, pregabalin, ragaglitazar, paclitaxel, epothilone, abacavir, atorvastatin, rosuvastatin, and omapatrilat have been successfully synthesized via biocatalysis. In this review, various biocatalytic systems that enable to synthesize these chiral drug intermediates are updated and discussed regarding their potential application in the pharmaceutical industry. Further development and increased utilization of biocatalysis for production of drugs with emphasis on green chemistry can be expected.

Synthesizing Chiral Drug Intermediates by Biocatalysis

Disclosed are methods for identifying bio-molecules with desired properties (or which are most suitable for a round of directed evolution) from complex bio-molecule libraries or sets of such libraries. Some embodiments of the present disclosure provide methods for virtually screening proteins for beneficial properties. Some embodiments of the present disclosure provide methods for virtually screening enzymes for desired activity and/or selectivity for catalytic reactions involving particular substrates. Some embodiments combine screening and directed evolution to design and develop proteins and enzymes having desired properties. Systems and computer program products implementing the methods are also provided.

Automated screen up of enzyme variants

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.

Biocatalysts and methods for the synthesis of armodafinil

The present disclosure provides engineered transaminase polypeptides useful for the synthesis of chiral amine compounds under industrially relevant conditions. The disclosure also provides polynucleotides encoding the engineered transaminase polypeptides, host cells capable of expressing the engineered transaminases, and methods of using the engineered transaminases for the production of chiral amine compounds.

Engineered transaminase polypeptides for industrial biocatalysis

The present invention provides endoglucanase 1b (EG1b) variants suitable for use in saccharification reactions The present application further provides genetically modified fungal organisms that produce EG1b variants, as well as enzyme mixtures exhibiting enhanced hydrolysis of cellulosic material to fermentable sugars, enzyme mixtures produced by the genetically modified fungal organisms, and methods for producing fermentable sugars from cellulose using such enzyme mixtures

Endoglucanase 1b (eg1b) variants

Cette invention concerne des polypeptides non presents a l'etat naturel utilises pour preparer l'armodafinil, des polynucleotides codant pour lesdits polypeptides et des procedes d'utilisation desdits polypeptides. Les polypeptides de l'invention sont efficaces pour effectuer la conversion biocatalytique (i) du 2-(benzhydrylsulfinyl)acetamide en (-)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), ou (ii) de l'acide benzhydryl-thioacetique en acide (R)-2-(benzhydrylsulfinyl)acetique, intermediaire essentiel dans la synthese de l'armodafinil, en exces enantiomerique.

Biocatalyseurs et procédés de synthèse de l'armodafinil

Biokatalysatoren und verfahren zur synthese von armodafinil

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