Pharma Mar, S.a.

Andres Francesh

Ignacio Manzanares

Carmen Cuevas

Simon Munt

Regan James Anderson

Jonathan Charles Morris

Juan Jose Gonzalez

Carlos Del Pozo

Pilar Gallego

Maria Zarzuelo

Maria Flores

Jose Luis Chicharro

Carolina Fernandez

Modesto Remuiñan

This invention relates to antitumoral ecteinascidin derivatives that contain a fused ecteinascidin five ring system with a 1,4-bridge having the structure of formula (VIa) or (VIb) as described herein and compounds in which the &#x2014;NHor &#x2014;OH of the 1,4-bridge is derivatized, and related pharmaceutical compositions and methods. Such ecteinascidin derivatives include, but are not limited to, those compounds having formula (XVIIb): in which Rand Rtogether form a group of formula (VIa) or (VIb) as described herein, and R, R, R, R, R, R, and Rare as defined herein.

Anititumoral ecteinascidin derivatives

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X, R, R, R, R, R, and Rare each independently selected from the group consisting of H, OH, OR', SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHCOR&#x2032;, NHSOR&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)R&#x2032;, COH, COR&#x2032;, carboxyalkyl, C-Calkyl, C-Calkenyl, C-Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R&#x2032; groups is independently selected from the group consisting of H, OH, SH, NO, NH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups of Rand R, Rand R, Rand R, Rand R, or Rand Rmay be joined into a carbocyclic or heterocyclic ring system.

Variolin derivatives and their use as antitumor agents

Variolin derivatives of formula (5) are provided, wherein the substituent groups defined by X, R, R, R, R, Rand Rare each independently selected from the group consisting of H, OH, OR', SH, SR&#x2032;, SOR&#x2032;, SOR&#x2032;, NO, NH, NHR&#x2032;, N(R&#x2032;), NHCOR&#x2032;, NHSOR&#x2032;, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)R&#x2032;, COH, COR&#x2032;, carboxyalkyl, C-Calkyl, C-Calkenyl, C-Calkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl and substituted or unsubstituted heteroaromatic; wherein each of the R&#x2032; groups is independently selected from the group consisting of H, OH, SH, NO, NH, CN, halogen, &#x2550;O, C(&#x2550;O)H, C(&#x2550;O)CH, COH, COCH, C-Calkyl, C-Calkenyl, C-Calkynyl, aryl, aralkyl and heteroaromatic; wherein the pairs of groups Rand R, Rand R, Rand R, Rand R, or Rand Rmay be joined into a carbocyclic or heterocyclic ring system. 

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Madrid, Spain

Andres Francesh