Dupont Pharmaceuticals Company

Other

Bristol-myers Squibb Compnay

Bristol-myers Squibb Pharma Company

The Dupont Merck Pharmaceutical Company

Pharmasset, Inc.

Fuqiang Jin

Pasquale N Confalone

Zhe Wang

Hui-Yin Li

Christopher A Teleha

David J Meloni

Luigi Anzalone

Jung-Hui Sun

Thomas E Smyser

Roberta L Dorow

Silvio Campagna

Jiacheng Zhou

Lucius T Rossano

Jia C Zhou

An efficient synthetic route to antiviral 2',3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydro-nucleosides, such as 2&#x2032;,3&#x2032;-dideoxy and 2&#x2032;- or 3&#x2032;-deoxyribo-nucleoside analogs, from available precursors is disclosed, with the option of introducing functionality as needed. In one embodiment, a method for the preparation of &#x3b2;-D and &#x3b2;-L-2&#x2032;,3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydro-nucleosides is described that includes: activating a compound of structure (1)wherein B is a pyrimidine or purine base and Y is O, S or CHwith an acyl halide of the formula X&#x2014;C(&#x2550;O)R, X&#x2014;C(&#x2550;O)C(R)OC(&#x2550;O)Ror X&#x2014;C(&#x2550;O)OR(wherein X is a halogen, and each Ris independently hydrogen, lower alkyl, alkyl, aryl or phenyl); reducing the resulting compound with a reducing agent to form a 2&#x2032;,3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydro-nucleoside; and optionally deprotecting the nucleoside. The haloacylation of the first step can form the 2&#x2032;-acyl-3&#x2032;-halonucleoside, the 3&#x2032;-acyl-2&#x2032;-halonucleoside, or a mixture thereof.

Method for the synthesis of 2',3&#x2032;-dideoxy-2&#x2032;,3&#x2032;-didehydronucleosides

Efficient process for the preparation of a factor Xa inhibitor

Process for the preparation of macrocyclic metalloprotease inhibitors

The present invention is directed to a process for the preparation of a compound of formula (X-a):

The present invention relates generally to cyclic carbamates and isoxazolidines or Formula (I)

Cyclic carbamates and isoxazolidines as IIb/IIIa antagonists

This invention relates to 1,3,4-thiadiazoles and 1,3,4-Oxadiazoles of Formula (I) which are useful as antagonists of .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion and the tretment of angioginic disorders, inflammation, bone degradation, tumors, metastases, thrombosis, and other cell aggregation-related conditions.

1,3,4-thiadiazoles and 1,3,4-Oxadiazoles as .alpha..sub.v .beta..sub.3

##STR1## This invention relates generally to cyclic carbamates and hydroxylamines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

##STR1## This invention relates to improved isoxazoline compounds including, but not limited to 1,3,4-thiadiazoles and 1,3,4-oxadiazoles of the formula which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.

1,3,4-thiadiazoles and 1,3,4-oxadiazoles as IIb/IIIa antagonists

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Wilmington, DE, United States of America

Fuqiang Jin