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US 2006/0079509 A1Published application
Dibenzodiazepinone analogues, processes for their production and their use as pharmaceuticals
AssigneeEcopia BioSciences, Inc.
InventorsJames McAlpine, Arjun Banskota, Mustapha Aouidate
Life of this patent
Estimating the term…
Abstract
The invention relates to biologically active dibenzodiazepinone analogs represented by Formula I, to methods of producing them, to pharmaceutical compositions comprising them and to methods of treating neoplastic conditions.
Claims50
A compound of Formula I:
- wherein,
- W1, W2 and W3 are each independently selected from
- the chain from the tricycle terminates at W3, W2 or W1 with W3, W2 or W1 respectively being either —CH═O, —CH(OC1-6alkyl)2, —CH2OH, —CH2OC1-6alkyl or C(O)OR7;
- R1 is selected from H, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C6-10aryl, C5-10heteroaryl, C3-10cycloalkyl, C3-10heterocycloalkyl, C(O)H, C(O)C1-10alkyl, C(O)C2-10alkenyl, C(O)C2-10alkynyl, C(O)C6-10aryl, C(O)C5-10heteroaryl, C(O)C3-10cycloalkyl;
- C(O)C3-10heterocycloalkyl or a C-coupled amino acid;
- R2, R3, and R4 are each independently selected from H, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C6-10aryl, C5-10heteroaryl, C3-10cycloalkyl, C3-10heterocycloalkyl, C(O)H, C(O)C1-10alkyl, C(O)C2-10alkenyl, C(O)C2-10alkynyl, C(O)C6-10aryl, C(O)C5-10heteroaryl, C(O)C3-10cycloalkyl;
- C(O)C3-10heterocycloalkyl or a C-coupled amino acid;
- R5 and R6 are each independently selected from H, OH, OC1-6alkyl, OC(O)C1-6alkyl, NH2, NHC1-6alkyl, N(C1-6alkyl)2, NHC(O)C1-6alkyl;
- R7 is selected from H, C1-10alkyl, C2-10alkenyl, C2-10alkynyl, C6-10aryl, C5-10heteroaryl, C3-10cycloalkyl and C3-10heterocycloalkyl;
- X1, X2, X3, X4 and X5 are each H;
- or
- one of X1, X2, X3, X4 or X5 is halogen and the remaining ones are H;
- and
- wherein, when any of R1, R2, R3, R4, R5, R6 and R7 comprises an alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group, then the alkyl, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, or heterocycloalkyl group is optionally substituted with substituents selected from acyl, amino, acylamino, acyloxy, carboalkoxy, carboxy, carboxyamido, cyano, halo, hydroxyl, nitro, thio, C1-6alkyl, C2-7alkenyl, C2-7alkynyl, C3-10cycloalkyl, C3-10heterocycloalkyl, C6-10aryl, C5-10heteroaryl, alkoxy, aryloxy, sulfinyl, sulfonyl, oxo, guanidino and formyl;
- with the proviso that when W1, W2 and W3 are all —CH═C(CH3)—, X1, X2, X3, X4 and X5 are all H, and R2, R3 and R4 are all H, then R1 is not H;
- with the proviso that when the chain from the tricycle terminates at W1 or W2 with W2 or W1 respectively being either —CH═O, —CH(OC1-6alkyl)2, —CH2OH, —CH2OC1-6alkyl or C(O)OR7, then R1 is H;
- and an ester, ether, N-alkylated or N-acylated derivative, or a pharmaceutically acceptable salt, solvate or prodrug thereof.
14 more elements
A compound of Formula II:
- wherein,
- R1 is a linear C1-10alkyl;
- or a farnesyl derivative thereof, wherein said farnesyl derivative has one, two or three hydrogenated or hydroalkoxylated double bonds;
- or a pharmaceutically acceptable salt or prodrug thereof.
1 more element
Dependencies are inferred from the claim text.