9,10-α,α-OH-taxane analogs and methods for production thereof
AssigneeTapestry Pharmaceuticals, Inc.
InventorsJan Zygmunt, James Ferrara, James D. McChesney
Life of this patent
Estimating the term…
Loading patent…
AssigneeTapestry Pharmaceuticals, Inc.
InventorsJan Zygmunt, James Ferrara, James D. McChesney
Estimating the term…
Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: with a second compound of generalized formula R8R9C(OCH3)2 and an acid selected from the group consisting of camphor sulfonic acid (CSA), p-toluene sulfonic acid (PTSA), hydrochloric acid (HCl) and acetic acid (AcOH), wherein R1 and R2 are each selected from H, an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group, or an O-aromatic group; R7 is an alkyl group, an olefinic group, or an aromatic group; P1 is a hydroxyl protecting group; P5 is H or an acid labile protecting group at the 7-O position; R8 is H, alkyl group, olefinic or aromatic group; and R9 is: H, alkyl group, olefinic or aromatic or is as defined in the specification.
A pharmaceutical formulation comprising a taxane compound and a pharmaceutically acceptable carrier, wherein said taxane compound is present in a concentration sufficient to treat cancer in a cancer patient, said cancer selected from the group consisting of Ovarian Carcinoma, Breast Cancer, Neuroblastoma, and Squamous Cell Carcinoma, further wherein the taxane compound has a fused four member ring system wherein there is an acetal bridge between the hydroxyl groups at the 7- and 9-ring positions, of the fused four member ring system, said acetal bridge having a structure of -OC(H)(CH═CH2)O— and having β,α a stereochemistry at the 7- and 9-ring positions, of the fused four member ring system, wherein there is α,α stereochemistry at the 9- and 10-ring positions, of the fused four member ring system, wherein at the 13-ring position there is a group having the structure:
Dependencies are inferred from the claim text.