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US 2019/0337928 A1Published application
Phthalazine Derivatives as Inhibitors of PARP1, PARP2, and/or Tubulin Useful for the Treatment of Cancer
AssigneeAltasmedx, Inc.
InventorsCsaba J. PETO, David M. JABLONS, Tsze TSANG, Hassan LEMJABBAR-ALAOUI
Life of this patent
Estimating the term…
Abstract
The application relates to phthalazine derivatives of formula (I) which are inhibitors of PARP1, PARP2 and/or tubulin and thus useful for the treatment of cancer. Also disclosed are pharmaceutical formulations containing such compounds, as well as combinations of these compounds with at least one additional therapeutic agent.
Claims30
A compound, or a salt or a hydrate or a solvate thereof, having a structure according to formula (I):
- wherein T has a structure which is
- wherein represents a covalent bond to the methylene group in formula (I) and represents a covalent bond to the U ring in formula (I)
- wherein formula (C)
- wherein represents a covalent bond to the T ring in formula (I) and represents a covalent bond to —NH—Y—Z—R1 in formula (I), has a structure which is
- wherein Y is C(O) or S(O)2;
- Z is —O— or —CH2— or —NH— or —N(CH2R7)— wherein R7 is hydrogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl;
- R1 is unsubstituted C2 or C1 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl or hydrogen or substituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C5 or C9 or C10 alkyl or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 heteroalkyl or substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl or substituted or unsubstituted cycloalkyl or substituted or unsubstituted heterocycloalkyl;
- R2 is hydrogen or halogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl;
- R3 is halogen or hydrogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkoxy;
- R4 is hydrogen or halogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkoxy;
- R5 is hydrogen or halogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl;
- and
- R6 is hydrogen or halogen or substituted or unsubstituted C1 or C2 or C3 or C4 or C5 or C6 or C7 or C8 or C9 or C10 alkyl.
10 more elements
A use of the compound of a preceding claim in the manufacture of a medicament for the treatment of cancer.
Dependencies are inferred from the claim text.