Schering Corporation

Dendreon Corporation

Warner-lambert Company

Other

Russell E Pike

Viyyoor Moopil Girijavallabhan

Anil K Saksena

Raymond G Lovey

Ashit K Ganguly

Yi-Tsung Liu

Haiyan Wang

Frank W Bennett

F George Njoroge

Stephane L Bogen

Ashok Arasappan

Odile Esther Levy

Patrick A Pinto

Marguerita S Lim-Wilby

Edwin Jao

Tejal Parekh

Scott Jeffrey Kemp

Zhaoning Zhu

Kevin X Chen

Dinanath F Rane

Tin-Yau Chan

Bama Santhanam

Susan Y Tamura

Srikanth Venkatraman

Henry A Vaccaro

John J Wright

Yuhua Huang

Jinping L McCormick

Wanli Wu

Jinping L Mc Cormick

Siska Hendrata

Charles F Schwender

Jesse K Wong

Terence Kevin Brunck

Latha G Nair

Jagdish A Desai

Henry M Vaccaro

William Brian Morgan

Aleksey Zaks

Srinkanth Venkatraman

Viyyoor M Girijavallabhn

Marguerita Lim-Wilby

Edwin E Jao

Tejal N Parekh

The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

Peptides as NS3-serine protease inhibitors of hepatitis C virus

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.

The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such peptides as well as methods of using them to treat disorders associated with the HCV protease.

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two amino acid ester groups (e.g., an amino acid ester group convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Tetrahydrofuran antifungals

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two groups convertible in vivo into hydroxy moieties, (e.g., a polyether ester, amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two polyetyher ester groups (e.g., a polyether ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether ester (e.g., a polyetherester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester, heterocyclic ester amino acid ester or phosphate ester) thereof and the carbon with the asterisk (*) has the R or S absolute configuration or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Hydroxy-substituted antifungals

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R.sub.1 is a straight or branched chain (C.sub.3 to C.sub.8) alkyl group substituted by one or two hydroxy moieties, an ether or ester thereof (e.g., a polyether ester amino acid ester or phosphate ester) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Disclosed is a process for preparing chiral compounds of the formula (I) ##STR1## wherein: X.sup.1 and X.sup.2 are independently F or Cl; and E is --SO.sub.2 R.sup.2, wherein R.sup.2 is C.sub.1 -C.sub.6 alkyl, --C.sub.6 H.sub.4 CH.sub.3 or --CF.sub.3 ; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula ##STR2## wherein: X.sup.1 and X.sup.2 are independently F or Cl; B represents --C(O)Q* or --CH.sub.2 OR'; Q* represents a chiral auxiliary group; R' represents a hydroxy protecting group selected from --CH.sub.2 C.sub.6 H.sub.5, or --C(O)R.sup.1, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.

Process for preparing intermediates for the synthesis of antifungal

2-Alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-2-(1H-azolyl(C.sub.1 -C.sub.2)alkyl)benzo[b]thiophenes especially 2-alkyl-, 2-alkenyl- and 2-alkynyl-2,3-dihydro-3-hydroxy-2-(1H-1-imidazolylmethyl)-4-,5-,6- and 7-halobenzo[b]thiophenes and related derivatives having antifungal activity are disclosed. Pharmaceutical compositions comprising compounds of the invention and their use in treating fungal infections in susceptible hosts such as humans are also disclosed.

Dihydrobenzo(B)thiophenes and pharmaceutical compositions thereof useful

Growing community of inventors

Stanhope, NJ, United States of America

Russell E Pike