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US 10,093,642 B2Granted
Multitarget hedgehog pathway inhibitors and uses thereof
AssigneesUniversita' Degli Studi Di Roma “La Sapienza”, Università Degli Studi Di Siena
InventorsBruno Botta, Alberto Gulino, Maurizio Botta, Mattia Mori, Lucia Di Marcotullio, Paola Infante, Francesca Ghirga, Sara Toscano, Cinzia Ingallina, Romina Alfonsi
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Abstract
The present invention concerns compounds that selectively inhibit the activity of the Hedgehog (Hh) pathway, their preparation and uses thereof. The compounds of the present invention are useful in treating Hh-dependent tumors, such as medulloblastoma (MB).
Claims6
A method for the treatment of a Hedgehog (Hh)-dependent tumor pathology comprising:
- administering to a human subject needing inhibition of the Hedgehog (Hh)-dependent tumor pathology, an effective amount of the compound having general formula I,
- wherein:
- R1 is ORA;
- R2 is ORB;
- wherein each of RA and RB is hydrogen or acyclic branched or straight, saturated or unsaturated aliphatic chain having from 1 to 10 carbon atoms;
- R3 is ORC;
- and
- R4 is ORD;
- wherein each of RC and RD are methyl, ethyl, propyl, isopropyl, prenyl, geranyl, farnesyl or benzyl, wherein the phenyl of the benzyl group can be substituted by halogen, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C6 alkoxy, C1-C6 alkylthio, amino, C1-C6 alkylamino, or C1-C6 dialkylamino, wherein the compound is an antagonist of Gli1 and the effective amount inhibits activation of Gli1 associated with the Hh-pathway.
6 more elements
Dependencies are inferred from the claim text.