Dupont Pharmaceuticals Company

Bristol-myers Squibb Pharma Company

Bristol-myers Squibb Compnay

The Dupont Merck Pharmaceutical Company

Agrimetis, LLC

Other

E.i. Dupont De Nemours and Company

Acadia Pharmaceuticals Inc.

Pharmasset, Inc.

Cersci Therapeutics, Inc.

Pasquale N Confalone

Hui-Yin Li

Philip Ma

Fuqiang Jin

Jiacheng Zhou

Lynette May Oh

Zhe Wang

Scott L Dax

Brian Michael Green

Thomas E Smyser

Roberta L Dorow

Silvio Campagna

Andrew Calabrese

David R Spring

Jerome Yves Cassayre

David J Meloni

Charles G Clark

Ronald L Magolda

Louis Storace

Scott A Savage

Silvio A Campagna

Nicholas Andrew Magnus

Paul R Johnson

Lucius T Rossano

Robert E Waltermir

Matthew Yates

Chris Teleha

The invention relates to compounds of formula (I), compositions containing the same, and methods for treating and/or diminishing pain in a subject in need thereof. The compounds of formula (I) are effective for treating opioid-induced tachyphylaxis and opioid-induced hyperalgesia.

Compounds for pain treatment, compositions comprising same, and methods of using same

The invention relates to compounds of formula (I), compositions containing the same, and methods for treating and/or diminishing pain in a subject. The compounds of formula (I) are effective for treating opioid-induced tachyphylaxis and opioid-induced hyperalgesia.

Compositions and methods for the production of derivatives of spinosyns are provided. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and/or nematodes and are useful in the agricultural and animal health markets.

Spinosyn derivatives as insecticides

Compositions including derivatives of spinosyns and methods for the production of derivatives of spinosyns are provided. The spinosyn derivatives described herein include spinosyn derivatives functionalized on the C5-C6 double bond of spinosyn A to provide an additional ring system. The method produces spinosyn derivatives that exhibit activity towards insects, arachnids, and/or nematodes and are useful in the agricultural and animal health markets.

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds are useful as factor Xa inhibitors.

Synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

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

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.These compounds are useful as factor Xa inhibitors.

Synthesis of 4,5-dihydro-pyrazolo [3,4-c] pyrid-2-ones

Asymmetric synthesis of amino-pyrrolidinones

The present invention relates to processes for the conversion of nitriles to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.

Efficient method for the conversion of nitriles to amidines

Process for the preparation of macrocyclic metalloprotease inhibitors

The present invention provides of method of preparing phenyl-substituted azoles. This method uses an efficient ligand-accelerated Ullmann coupling reaction of anilines with azoles. The coupling products are useful for preparing factor Xa inhibitors.

Efficient ligand-mediated Ullmann coupling of anilines and azoles

Synthesis of 1,3,5-trisubstituted pyrazoles

The present invention relates to processes for the conversion of nitrites to amidines in the preparation of compounds which are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex. The compounds described herein are potent thrombolytics and useful for the inhibition of platelet aggregation in the treatment of thromboembolic disorders.

A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described.

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

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Wilmington, DE, United States of America

Pasquale N Confalone