Astrazeneca Ab

Alphora Research Inc.

Joshua Clayton

Abdelmalik Slassi

Methvin Benjamin Isaac

Fupeng Ma

Ian Egle

James Empfield

Boris Gorin

Dino Alberico

Bradford C Van Wagenen

Rebecca Urbanek

Gary Steelman

Radhakrishnan Ukkiramapandian

Sally Walsh

Jan Oudenes

James Jeffrey Folmer

Babu Joseph

Craig Edward Dixon

Krzysztof Swierczek

Ryan Beharrilall

Varghese Rexon

Gorin Boris

Disclosed is a process for preparing a carbonucleoside of formula (1) and intermediates for use therein. The process involves the step of reacting a compound of formula (2) with a compound of formula (3) under Mitsunobu-type reaction conditions to obtain a compound of formula (4), wherein PG, PG, PGand PGare protecting groups. The compound of formula (4) is deprotected to form the compound of formula (1), as shown below. 

Process for the synthesis of carbonucleoside and intermediates for use therein

Anti-virally active carbanucleosides such as entecavir are prepared by a process which utilizes, throughout the synthesis, an aromatic protectant group for the hydroxyl and the alkyl hydroxy groups of the starting material, removed as the final step of a multi-step synthesis. Such protectant groups yield intermediates which are solid and therefore easily purified at various stages of the process, for an economical and relatively fast process for synthesizing the final product.

Carbanucleoside synthesis and novel intermediate compounds useful therein

Fused cyclopentane-4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required &#x3b1;-side chain and then the required &#x3c9;-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Prostaglandin synthesis and intermediates for use therein

Oxadiazole derivatives and their use as metabotropic glutamate receptor potentiators 842

Compounds of Formula (I) wherein Rand Q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same. 

Oxadiazole derivatives and their use as metabotropic glutamate receptor potentiators&#x2014;842

Fused cyclopentane&#x2014;4-substituted 3,5-dioxalane lactone compounds useful as an intermediate in the synthesis of prostaglandin analogs are provided. The compounds have the formula A: wherein R represents an aryl group such as p-methoxyphenyl. This compound can be reacted with a lower alkyl aluminum compound to open the dioxalane ring and reduce the lactone to lactol, without over-reducing to diol. The resulting compound can be functionalized to insert chemical side groups of target prostaglandins, adding the required &#x3b1;-side chain and then the required &#x3c9;-side chain sequentially and independently of each other. The compounds and process are particularly suitable for preparing lubiprostone.

Compounds of formula I: wherein R, R, R, R, R, R, R, R, Rand n are as defined in the description, processes for the preparing the compounds, new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and uses of the compounds in therapy.

Metabotropic glutamate-receptor-potentiating isoindolones

The present invention is directed to compounds of formula I: wherein R, R, R, R, R, R, R, R, Rand n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Isoindolone compounds and their use as metabotropic glutamate receptor potentiators

Substituted isoindolones and their use as metabotropic glutamate receptor potentiators

The present invention is directed to compounds of Formula I: Wherein R, R, Y, m and n are further defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.

Oxazolidinone compounds and their use as metabotropic glutamate receptor potentiators

Metabotropic glutamate receptor oxadiazole ligands and their use as potentiators 841

Compounds in accord with Formula I: wherein R, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds in therapy and for the treatment of diseases mentioned in the specification.

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Oakville, Canada

Joshua Clayton