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Serving 500+ biopharmaceutical companies globally:

Colorcon
Cantor Fitzgerald
Cerilliant
US Department of Justice
Boehringer Ingelheim
Dow
Citi
Harvard Business School
Julphar
AstraZeneca

Generated: September 23, 2017

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Title: Tetrahydrofuran antifungals
Abstract: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.
Inventor(s): Saksena; Anil K. (Upper Montclair, NJ), Girijavallabhan; Viyyoor M. (Parsippany, NJ), Lovey; Raymond G. (West Caldwell, NJ), Pike; Russell E. (Stanhope, NJ), Wang; Haiyan (Dayton, NJ), Liu; Yi-Tsung (Morris Township, NJ), Ganguly; Ashit K. (Upper Montclair, NJ), Bennett; Frank (Piscataway, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:08/460,400
Patent Claims: 1. A compound represented by the formula I ##STR109## 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.4 to C.sub.5) alkyl group substituted by a hydroxy group or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 wherein R.sub.1 is a hydroxy-substituted C.sub.4 - or C.sub.5 -alkyl group selected from:

--*CH(C.sub.2 H.sub.5)*CH(R.sub.4)CH.sub.3, --*CH(C.sub.2 H.sub.5)CH.sub.2 CH.sub.2 R.sub.4,

--(CH.sub.2).sub.2 --*CH(R.sub.4)C.sub.2 H.sub.5, --*CH(CH.sub.3)*CH(R.sub.4)CH.sub.3,

--*CH(C.sub.2 H.sub.5)CH.sub.2 R.sub.4 and --*CH(CH.sub.3)CH.sub.2 CH.sub.2 R.sub.4

wherein R.sub.4 is OH and the carbons with the asterisk(*) have the R or S absolute configuration or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 wherein R.sub.1 is a C.sub.4 alkyl group substituted by a hydroxy group.

4. The compound of claim 1 wherein R.sub.1 is a C.sub.5 alkyl group substituted by a hydroxy group.

5. A compound represented by formula III ##STR110## wherein R.sub.5 is ##STR111## wherein R.sub.13 is a hydroxy group, or a pharmaceutically acceptable salt thereof.

6. A compound represented by the formula IV ##STR112## wherein R.sub.9 =--*CH(C.sub.2 H.sub.5)CH(R.sub.6)CH.sub.3 or --*CH(CH.sub.3)CH(R.sub.6)CH.sub.3

wherein R.sub.6 is OH or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition for treating or preventing fungal infection comprising an antifungally effective amount of a compound of claim 1 together with a pharmaceutically acceptable carrier therefor.

8. A method of treating and/or preventing fungal infections in a mammal afflicted with same which comprises administering an antifungally effective amount of a compound of claim 1 sufficient for such treating or preventing.

9. The pharmaceutical composition of claim 1 wherein the mode of administration is oral or parenteral.
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Serving 500+ biopharmaceutical companies globally:

Fish and Richardson
Fuji
Harvard Business School
Novartis
Mallinckrodt
Chubb
Medtronic
Daiichi Sankyo
Merck
Federal Trade Commission

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

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