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|Abstract:||The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.|
|Inventor(s):||Helleday; Thomas (Stockholm, SE), Curtin; Nicola (Tyne and Wear, GB)|
|Assignee:||Cancer Research Technology Limited (London, GB) Pfizer, Inc. (New York, NY)|
|Filing Date:||Jul 23, 2004|
|Claims:||1. A method for treating cancer in a mammal, wherein the cancer is caused by a genetic defect in a gene that mediates homologous recombination, wherein the gene is at least one of BRCA1 and BRCA2, the method comprising: selecting the mammal having the genetic defect; and administering to the mammal a compound selected from the group consisting of a compound of the formula I, formula II and formula III: ##STR00005## or a pharmaceutically acceptable salt thereof, wherein the compound is used as a direct cytotoxic agent. |
2. The method according to claim 1, wherein the compound is the compound of the formula I.
3. The method according to claim 2, wherein the compound of the formula I is in the form of a phosphate salt.
4. The method of claim 1, wherein the cancer is breast cancer.
5. The method of claim 1, wherein the genetic defect is the absence of BRCA1 and/or BRCA2.
6. The method of claim 1, wherein the genetic defect is in the expression of BRCA1 and/or BRCA2.