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US 8,575,143 B2Granted
3-aryl-substituted quinazolones, and uses thereof
AssigneeProlexys Pharmaceuticals, Inc.
InventorsLongwu Qi, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
Life of this patent
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Abstract
Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.
Claims28
A compound represented by Structural Formula (I):
- or a pharmaceutically acceptable salt thereof, wherein
- Ra is a halogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl-O—, substituted or unsubstituted alkyl-O—, substituted or unsubstituted alkenyl-O— or substituted or unsubstituted alkynyl-O—, wherein alkyl, alkenyl and alkynyl are optionally interrupted by NR, O or S(O)n;
- each R2 is independently selected from the group consisting of substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted non-aromatic heterocyclic, —CN, —COOR′, —CON(R)2, —NRC(O)R, —SO2N(R)2, —N(R)2, —OH and —OR′;
- each R3 is independently selected from the group consisting of halogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted non-aromatic heterocyclic, —CN, —COOR′, —CON(R)2, —NRC(O)R, −SO2N(R)2, —N(R)2, —NO2, —OH and —OR′;
- R4 and R5 are independently selected from the group consisting of —H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted non-aromatic heterocyclic and substituted or unsubstituted aryl, wherein alkyl, alkenyl and alkynyl are optionally interrupted by NR, O or S(O)n;
- or R4 and R5 taken together form a carbocyclic or heterocyclic group;
- V is —NH-L-A-Q or
- Ring C is a substituted or unsubstituted heterocyclic aromatic or non-aromatic ring;
- A is NR or O;
- or A is a covalent bond;
- L is a substituted or unsubstituted hydrocarbyl group optionally interrupted by one or more heteroatoms selected from N, O and S;
- Q is selected from the group consisting of —R, —C(O)R′, —C(O)N(R)2, —C(O)OR′ and —S(O)2R′;
- each R is independently —H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or substituted or unsubstituted non-aromatic heterocyclic;
- each R′ is independently a substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl group, substituted or unsubstituted non-aromatic heterocyclic or substituted or unsubstituted aryl group;
- j is an integer from 1 to 4;
- k is an integer from 0 to 4;
- and
- each n is independently 0, 1 or 2.
15 more elements
A compound represented by Structural Formula (II):
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is a substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or substituted or unsubstituted alkynyl group, each of which is optionally interrupted by NR, O or S(O)n;
- each R2 is independently selected from the group consisting of substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted non-aromatic heterocyclic, —CN, −CON(R)2, −SO2N(R)2, −OH and —OR;
- each R3 is independently selected from the group consisting of halogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted non-aromatic heterocyclic, —CN, —COOR′, —CON(R)2, —SO2N(R)2, —OH and —OR′;
- R4 and R5 are independently selected from the group consisting of —H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted non-aromatic heterocyclic and substituted or unsubstituted aryl, wherein alkyl, alkenyl and alkynyl are optionally interrupted by NR, O or S(O)n;
- or R4 and R5 taken together form a carbocyclic or heterocyclic group;
- V is —NH-L-A-Q or
- Ring C is a substituted or unsubstituted heterocyclic aromatic or non-aromatic ring;
- A is NR or O;
- or A is a covalent bond;
- L is a substituted or unsubstituted hydrocarbyl group optionally interrupted by one or more heteroatoms selected from N, O and S;
- Q is selected from the group consisting of —R, —C(O)R′, —C(O)N(R)2, —C(O)OR′ and —S(O)2R′;
- each R is independently —H, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or substituted or unsubstituted non-aromatic heterocyclic;
- each R′ is independently a substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl group, substituted or unsubstituted non-aromatic heterocyclic or substituted or unsubstituted aryl group;
- j is an integer from 1 to 4;
- k is an integer from 0 to 4;
- and
- each n is independently 0, 1 or 2.
15 more elements
A compound that is
- or pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.