Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Scynexis, Inc.

Other

Frances A Bouffard

James M Balkovec

James Francis Dropinski

Regina M Black

Robert A Zambias

Weiming Fan

Michael Robert Peel

Ahmed Mamai

Jan S Tkacz

Akinlolu A Adefarati

Mark L Greenlee

Milton L Hammond

Phieng Siliphaivanh

Dongfang Meng

Bruno Tse

Hao Liu

Roland A Bouffard, Legal Representative

Sarah Dimick Gray

Keqaing Li

Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.

Antifungal agents

The present invention relates to novel enfumafungin derivatives of formula I and pharmaceutically acceptable salts thereof, their synthesis, and their use as inhibitors of (1,3)-&#x3b2;-D-glucan synthase. The present compounds and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising the present compounds and pharmaceutically acceptable salts thereof, are useful for treating or preventing antifungal infections and associated diseases and conditions.

Cyclohexapeptidyl amine compounds are disclosed of the formula:

Cyclohexapeptidyl amine compounds

Certain bisamine compounds which have a cyclohexapeptidyl nucleus and which are found to have antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.

Cyclohexapeptidyl bisamine compounds

A compound having the formula ##STR1## in which R.sub.1 is an aminoalkyl group and ##STR2## is an acyl group and salts thereof having high antibiotic activity and being substantially free of lytic activity are described.

1-�4-hydroxy-5-aminoethyloxy-N.sup.2

The present invention is directed to novel carba cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.

Antifungal cyclohexapeptides

A compound of the formula ##STR1## is disclosed which is useful for the treatment of fungal infections and for the treatment of infections caused by Pneumocystis carinii.

Cyclohexapeptidyl bisamine compound, compositions containing said

Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.

Aza cyclohexapeptide compounds

There are disclosed compounds of the general formula ##STR1## wherein all substituents are defined herein. The compounds are useful as antibiotic and antifungal agents.

Cyclohexapeptidyl aminoalkyl ethers

An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.

Process for preparing side chain derivatives of cyclohexapeptidyl

Compounds represented by the formula (Seq ID Nos. 1-6) ##STR1## wherein all substituents are fully defined, are disclosed. These compounds exhibit utilities as antibiotic and antifungal agents and for the treatment and prevention of Pneumocystis infections.

Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof. R.sup.I represents C.sub.9 to C.sub.19 alkyl, C.sub.9 to C.sub.19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C.sub.1 to C.sub.12 alkyl, alkylamino, dialkylamino or alkoxyaryl group. R.sup.1, R.sup.2 and R.sup.4 independently represent H or --OH. R.sup.3 represents H, --OH, --O(CH.sub.2).sub.n NR.sup.V R.sup.VI, where R.sup.V and R.sup.VI independently represent H or C.sub.1-4 alkyl, or --O(CH.sub.2).sub.n NR.sup.V R.sup.VI R.sup.VII+ Y.sup.-, wherein R.sup.V and R.sup.VI are as defined above, R.sup.VII represents H or C.sub.1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion. R.sup.5 represents H, --CH.sub.3 or --OH; R.sup.6 represents H or --CH.sub.3 ; R.sup.7 represents H, --CH.sub.3, --CH.sub.2 C(.dbd.O)NH.sub.2, --(CH.sub.2).sub.2 NR.sup.V R.sup.VI or --(CH.sub.2).sub.2 NR.sup.V R.sup.VI R.sup.VII+ Y.sup.- with n, R.sup.V, R.sup.VI R.sup.VII and Y as defined above; and R.sup.8 represents --Cl, --Br, --I, --NO.sub.2, --N.sub.3, --(CH.sub.2).sub.0-4 NH.sub.2, --(CH.sub.2).sub.0-4 NH(C.sub.1-4 alkyl), --(CH.sub.2).sub.0-4 N(C.sub.1-4 alkyl).sub.2, --(CH.sub.2).sub.0-3 CH(.dbd.NOH), --NHC(.dbd.O)(CH.sub.2).sub.1-6 NH.sub.2 or --NHC(.dbd.O)(CH.sub.2).sub.1-6 NHC(.dbd.NH)(CH.sub.2).sub.0-3 H. Pharmaceutical compositions and methods of use are also disclosed.

Antifungal and anti-pneumocystis compounds, compositions containing such

The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.

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Scotch Plains, NJ, United States of America

Frances A Bouffard