Variolin derivatives and their use as antitumor agents

US7772241B2 · kind B2 · utility

Assignee

• PHARMA MAR, S.A. · ES

Inventors

• Modesto Remuinan · Madrid, ES
• Juan Jose Gonzalez · Madrid, ES
• Carlos Del Pozo · Madrid, ES
• Andres Francesh · Madrid, ES
• Carmen Cuevas · Madrid, ES
• Simon Munt · Madrid, ES
• Ignacio Manzanares · Madrid, ES
• Regan James Anderson · Lower Hutt, NZ
• Jonathan Morris · Forbes, AU

Key dates

• Filing date: Jan 7, 2009
• Grant date: Aug 10, 2010
• Expiry date: Jan 7, 2029

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/14
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X2, R1, R2, R3, R6, R7, and R12 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHCOR′, NHSO2R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, carboxyalkyl, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, SH, NO2, NH2, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of R1 and R2, R2 and R3, R3 and R12, R12 and R6, or R6 and R7 may be joined into a carbocyclic or heterocyclic ring system.