Baccatin derivatives and processes for preparing the same

Details Baccatin derivatives and processes for preparing the same Baccatin derivatives and processes for preparing the same

C - Chemistry, Metallurgy

07

K

C07K 5/06 (2006.01) A61K 31/335 (2006.01) A61K 31/38 (2006.01) A61K 31/40 (2006.01) A61K 38/05 (2006.01) C07D 263/04 (2006.01) C07D 263/06 (2006.01) C07D 305/14 (2006.01) C07D 405/12 (2006.01) C07D 407/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07F 7/10 (2006.01)

Patent

CA 2162759

A compound represented by the formula [I]: Image [I] wherein R3 represents a lower alkanoyl group; R4 represents a substituted or unsubstituted benzoyl group; ring A represents a substituted or unsubstituted cyclopropane ring; X represents a single bond or a group represented by-O-, -S- or - NH-; R represents a substituted or unsubstituted lower alkyl group (wherein saidlower alkyl group may have a cycloalkyl moiety), a substituted or unsubstituted aryl group or a substituted or unsubstituted aromatic heterocyclic group; E represents hydrogen atom or a group represented by -CO(CH2)nZY; Y represents a residue obtained from an amino acid or a dipeptide by removing hydroxyl group in one carboxyl group therefrom (wherein amino group existing in said residue may be protected, and carboxyl group existing in said residue may be esterified or amidated); Z represents a group represented by the formula of -O- or -NH-; and n represents 1, 2, 3, 4, 5 or 6, or a pharmaceutically acceptable salt thereof. Said compounds have excellent antitumor activity so that they are useful in the prophylaxis or treatment of a wide range of tumors such as breast cancer, ovary cancer, lung cancer, malignantmelanoma and the like.

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