Abbott Laboratories Corporation

Bristol-myers Squibb Compnay

Medivir Ab

Mediver Ab

Steven M Hannick

Thomas J Sowin

Daniel W Norbeck

Richard J Pariza

Lawrence Kolaczkowski

Daniel J Plata

Elizabeth M Doherty

Hing L Sham

Dale J Kempf

Xiaoqi Chen

David A Betebenner

Daniel A Dickman

M Robert Leanna

Jih-Hua Liu

Thomas R Herrin

Ketan M Patel

Michael Rasmussen

Stephen L Condon

Arthur J Cooper

Eric J Stoner

Patricia A Oliver

Gondi N Kumar

Jieh-Heh J Tien

Peter J Stengel

Jianguo Ji

Geoff G Z Zhang

Rodger F Henry

Howard E Morton

Steven J Wittenberger

Jien-Heh J Tien

Kirill A Lukin

Sou-Jen Chang

Timothy A Robbins

Bikshandarkoil A Narayanan

Wenke Li

Gregory S Wayne

Timothy B Towne

Brian J Kotecki

Bhadra Shelat

Zhenping Tian

Weili Wang

Michael J Buckley

Bryan S Macri

Cynthia B Curty

John Bellettini

Tiffany Spitz

Jacob J Plattner

Takahiro Sato

Takayuki Suzuki

Larry L Klein

Terry J Rosen

Geoff G Zhang

David A Riley

Bradley D Gates

Lakshmi Bhagavatula

Pulla Reddy Singam

Weijiang Zhang

Ramesh R Patel

Greg Lannoye

Greg Wayne

Daniel Plata

Cheng-Xi Yang

David L Garmaise

Weili W Wang

Greg S Wayne

A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Retroviral protease inhibiting compounds

The present invention discloses (1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane, salts thereof, and its use to treat pain and other disorders associated with the nicotinic acetylcholine receptor.

(1S,5S)-3-(5,6-dichloro-3-pyridinyl)-3,6-diazabicyclo[3.2.0]heptane

Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.

Synthesis of acyclic nucleoside derivatives

Methods and novel intermediates of the formula:

The present invention relates to a process for the preparation of substituted cyclobutanes and their use as intermediates for the preparation of anti-viral nucleoside analogs.

Process for preparing substituted cyclobutanes

A process is disclosed for the preparation of a substituted diaminodiol.

Process for the preparation of a substituted diaminodiol

A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is as defined above, --CH.sub.2 CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 and R.sub.23 are as defined above, --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2, --CH.sub.2 OPO.sub.3 H.sub.2, --OCH.sub.2 PO.sub.3 H.sub.2 and --CH.sub.2 CO.sub.2 R.sub.3 wherein R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 to C.sub.10 alkyl and R.sub.3 is hydrogen, C.sub.1 to C.sub.10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.

Carbocyclic nucleoside analogs

The present invention relates to a process for the preparation of substantially pure enantiomer of the purines substituted with cyclobutanes.

Process for preparing substituted cyclobutane purines

A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occuring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein R.sub.24 is the side chain of any of the naturally occuring amino acids, --CH.sub.1 SH, --Ch.sub.2 Cl, --Ch.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is as defined above, --CH.sub.2 CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 and R.sub.23 are as defined above, --CH.sub.2 CH.sub.2 PO.sub.3 H.sub.2, --Ch.sub.2 OPO.sub.3 H.sub.2, --OCH.sub.2 PO.sub.3 H.sub.2 and --CH.sub.2 CO.sub.2 R.sub.3 wherein R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1 to C.sub.10 alkyl and R.sub.3 is hydrogen, C.sub.1 to C.sub.10 alkyl, carboxyalkyl or aminoalkyl; or a pharmaceutically acceptable salt thereof.

Process for preparation of intermediates of carbocyclic nucleoside

Semisynthetic antibiotics with improved therapeutic properties made from erythromycin are disclosed. Certain 4'-carbamates of erythromycin, its derivatives, and their salts and esters show superior in vitro antimicrobial activity and reduced gastrointestinal stimulation compared to the parent compounds.

Semisynthetic erythromycin antibiotics

Growing community of inventors

Highland Park, IL, United States of America

Steven M Hannick