Back to results
US 2012/0238488 A1Published application
Compounds and methods for treating neoplasia
OwnerKonstantinos Alevizopoulos, Theodora Calogeropoulou +1inventors
InventorsKonstantinos Alevizopoulos, Theodora Calogeropoulou, Christos Stournaras
Life of this patent
Estimating the term…
Abstract
The invention features compounds, pharmaceutical compositions and methods useful for the treatment of neoplasia. In particular embodiments, the compounds of the invention are useful for the treatment of multidrug resistant neoplasia.
Claims27
A compound of Formula (I)
- wherein:
- represents a single bond or double bond in the ring structure of Formula (I);
- One of R1 and R2 is H, and the other is —OR3;
- alkyl optionally substituted with hydroxyl or alkoxy;
- —C(O)—NH2;
- —C(O)—O-alkyl;
- —NHR8;
- alkynyl;
- or Wand R2 together with the carbon to which they are attached form C═O, C═C(R9)2, or CN—OR10;
- R3 is H;
- —NO2;
- carbonylalkyl;
- carbonylaryl;
- or aminoalkyl optionally substituted with one or more alkyl;
- A is CH(OR4), C═N—OR5, CH—CH═N—OR6, C═CH—CH═N—OR6, CH—CH═CH—R6, CH—SR7, or CH—S(O)R7;
- R4 is alkyl optionally substituted by a 4- to 6-membered heterocyclic ring, a 5 to 14-membered heteroaryl, amino(C1-C4)alkoxyl, (C1-C4)alkoxyl substituted by a 4- or 6-membered heterocyclic ring, or guanidinyl;
- aminoalkyl optionally substituted by one or more alkyl;
- or aminoacyl optionally substituted by alkyl;
- wherein said heterocyclic or heteroaryl ring is further optionally substituted by one or more alkyl
- R5 is aminoalkyl optionally substituted by one or more alkyl or acetyl;
- alkyl optionally substituted by guanidinyl, heteroaryl that is further optionally substituted by one or more alkyl or aminoalkyl optionally substituted by one or more alkyl, or a 4- to 6-membered heterocyclic ring that is further optionally substituted by one or more alkyl;
- or a 4- to 6-membered heterocyclic ring optionally substituted by one or more alkyl;
- R6 and R7, each independently, are aminoalkyl optionally substituted by one or more alkyl;
- R8 is H or formyl;
- R9, for each occurrence, is the same or different and is H or halogen;
- R10 is H or alkyl;
- and
- tautomers, stereoisomers, Z and E isomers, optical isomers, N-oxides, hydrates, polymorphs, pharmaceutically acceptable esters, salts, prodrugs and/or isotopic derivatives thereof.
25 more elements
4-9. (canceled)
11-35. (canceled)
45-165. (canceled)
167-191. (canceled)
194-205. (canceled)
207-210. (canceled)
212-218. (canceled)
Dependencies are inferred from the claim text.