The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Mar. 11, 2003
Filed:
Apr. 19, 2001
Kyriacos Costa Nicolaou, La Jolla, CA (US);
Nigel Paul King, Hitchin, GB;
Maruice Raymond Verschoyle Finlay, Macclesfield, GB;
Yun He, Carlsbad, CA (US);
Frank Roschangar, Chapel Hill, NC (US);
Dionisios Vourloumis, San Diego, CA (US);
Hans Vallberg, Huddinge, SE;
Antony Bigot, Paris, FR;
The Scripps Research Institute, La Jolla, CA (US);
Abstract
The invention relates to epothilone analog represented by formula (I) wherein (i) R is absent or oxygen; “a” can be either a single or double bond; “b” can be either absent or a single bond; and “c” can be either absent or a single bond, with the proviso that if R is oxygen then “b” and “c” are both a single bond and “a” is a single bond; if R is absent then “b” and “c” are absent and “a” is a double bond; and if “a” is a double bond, then R , “b” and “c” are absent; R is a radical selected from the group consisting of hydrogen; lower alkyl; —CH═CH ; —C≡CH; —CH F; —CH Cl; —CH —OH; —CH —O—(C -C -alkyl); and —CH —S—(C -C -alkyl); R and R are independently selected from hydrogen, methyl or a protecting group; and R is as defined in the specification, or a salt of a compound of formula (I) where a salt-forming group is present. A further aspect of the invention is related to the synthesis of epothilone E. These compounds have inter alia microtubuli depolymerization inhibiting activity and are e.g. useful against proliferative diseases