Abstract: The present invention provides engineered purine nucleoside phosphorylase (PNP) enzymes, polypeptides having PNP activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. Methods for producing PNP enzymes are also provided. The present invention further provides compositions comprising the PNP enzymes and methods of using the engineered PNP enzymes. The present invention finds particular use in the production of pharmaceutical compounds.

Abstract: The present invention provides engineered purine nucleoside phosphorylase (PNP) enzymes, polypeptides having PNP activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. Methods for producing PNP enzymes are also provided. The present invention further provides compositions comprising the PNP enzymes and methods of using the engineered PNP enzymes. The present invention finds particular use in the production of pharmaceutical compounds.

Abstract: The present invention relates to an enzymatic synthesis of 4?-ethynyl-2?-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.

Abstract: The present invention relates to an enzymatic synthesis of 4?-ethynyl-2?-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.

Abstract: The present invention relates to efficient synthetic processes useful in the preparation of uridine, which is useful in the production of nucleosides and nucleotides that may be active as antiviral agents, as well as compositions and methods thereof.

Abstract: The present invention relates to efficient synthetic processes useful in the preparation of antiviral nucleosides, particularly uridine 4-oxime 5?-(2-methylpropanoate) {(2R,3S,4R,5R)-3,4-dihydroxy-5-[4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl]oxolan-2-yl}methyl 2-methylpropanoate and pharmaceutically acceptable salts, derivatives, tautomers, isomers, and prodrugs of, which may be active as antiviral agents, as well as compositions and methods thereof. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.

Abstract: The present invention provides engineered deoxyribose-phosphate aldolase polypeptides useful under industrial process conditions for the production of pharmaceutical and fine chemical compounds.

Abstract: The present invention provides engineered deoxyribose-phosphate aldolase polypeptides useful under industrial process conditions for the production of pharmaceutical and fine chemical compounds.

Abstract: The present invention relates to an enzymatic synthesis of 4?-ethynyl-2?-deoxy nucleosides and analogs thereof, for example EFdA, that eliminates the use of protecting groups on the intermediates, improves the stereoselectivity of glycosylation and reduces the number of process steps needed to make said compounds. It also relates to the novel intermediates employed in the process.

Abstract: The present invention provides engineered deoxyribose-phosphate aldolase polypeptides useful under industrial process conditions for the production of pharmaceutical and fine chemical compounds.

Abstract: Receiving a plurality of concurrent incoming requests from the plurality of services, with each incoming request and each service subscribing to a topic in a shared message queue. The queue is used for: notifying other subscribers when a request to a back-end service is being made; and/or notifying other subscribers when a response from the back-end service is received.

Abstract: The present invention provides engineered deoxyribose-phosphate aldolase polypeptides useful under industrial process conditions for the production of pharmaceutical and fine chemical compounds.

Abstract: The present invention provides engineered purine nucleoside phosphorylase (PNP) enzymes, polypeptides having PNP activity, and polynucleotides encoding these enzymes, as well as vectors and host cells comprising these polynucleotides and polypeptides. Methods for producing PNP enzymes are also provided. The present invention further provides compositions comprising the PNP enzymes and methods of using the engineered PNP enzymes. The present invention finds particular use in the production of pharmaceutical compounds.

Abstract: Receiving a plurality of concurrent incoming requests from the plurality of services, with each incoming request and each service subscribing to a topic in a shared message queue. The queue is used for: notifying other subscribers when a request to a back-end service is being made; and/or notifying other subscribers when a response from the back-end service is received.

Abstract: Reducing concurrency in a system comprising a plurality of services sending a plurality of concurrent requests to a back-end service through a concurrency reduction service. The concurrency reduction service maps each concurrent incoming request to a key; and determines if the key to which the concurrent incoming request is mapped matches a key mapped from another concurrent incoming request from the plurality of concurrent requests. If the key to which the concurrent incoming request is mapped matches a key mapped from at least one other concurrent incoming request from the plurality of concurrent requests, then the service groups the concurrent incoming request with the at least one other concurrent incoming request to be sent to the back-end service. The concurrency reduction service sends one outgoing request to the back-end service for each of the keys to which the plurality of concurrent incoming requests were mapped.

Abstract: Reducing concurrency in a system comprising a plurality of services sending a plurality of concurrent requests to a back-end service through a concurrency reduction service. The concurrency reduction service maps each concurrent incoming request to a key; and determines if the key to which the concurrent incoming request is mapped matches a key mapped from another concurrent incoming request from the plurality of concurrent requests. If the key to which the concurrent incoming request is mapped matches a key mapped from at least one other concurrent incoming request from the plurality of concurrent requests, then the service groups the concurrent incoming request with the at least one other concurrent incoming request to be sent to the back-end service. The concurrency reduction service sends one outgoing request to the back-end service for each of the keys to which the plurality of concurrent incoming requests were mapped.

Abstract: A process for the preparation of alkyl esters of N-protected oxo-azacycloalkylcarboxylic acids of Formula III: comprises contacting a ketosulfoxonium ylide of Formula II: with an iridium catalyst to obtain Compound III, wherein PG1 is an amine protective group; k is 0, 1, or 2; and RU, R1, R2, and R3 are defined herein. An embodiment of the process further com rises contacting a compound of Formula I: with a sulfoxonium halide of formula (RU)3S(O)Z, wherein Z is halide, in the presence of a strong base to obtain Compound II. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as ?-lactamase inhibitors.

Abstract: Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.

Abstract: The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: Novel crystalline salts of 3-[1-(4-chlorophenyl)-trans-3-fluorocyclobutyl]-4,5-dicyclopropyl-r-4H-1,2,4-triazole are potent inhibitors of 11?-hydroxysteroid dehydrogenase Type 1 and are useful for the treatment of conditions associated with Metabolic Syndrome as well as cognitive impairment. The invention also relates to pharmaceutical compositions containing these novel salts, processes to prepare these salts and their pharmaceutical compositions as well as uses thereof for the treatment of Type 2 diabetes, hyperglycemia, obesity, dyslipidemia, hypertension, and cognitive impairment.