6-amino-2,4-dihydropyrano [2,3-c] pyrazoles and methods of use
AssigneePurdue Research Foundation
InventorsAntonella Pepe, Andrew Mesecar
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Abstract
The present invention generally relates to 6-amino-2,4-dihydropyrano[2,3-c] pyrazoles as a ubiquitin specific protease 7 (USP7) inhibitor useful for the treatment of diseases mediated by malfunction of USP7, such as inflammation, cancer, and immunological disorders. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases mediated by malfunction of USP7, in mammals using compounds disclosed herein.
Claims20
A method for treating a patient having a disease mediated by a USP7 malfunction comprising the step of administering a therapeutically effective amount of one or more compounds having a formula
- or a pharmaceutically acceptable salt thereof, wherein
- R1 is hydrogen, an alkyl or an acyl;
- R2 is a heterocyclyl, cycloalkyl, cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, aryl, heteroaryl, arylalkyl, arylalkenyl, or arylalkynyl, each of which is optionally substituted;
- R3, R4, R6, and R7 represent five substituents each independently selected from the group consisting of hydrogen, halo, azido, cyano, nitro, hydroxy, amino, thio, and derivatives thereof, and an acyl, alkyl, alkenyl, alkynyl, heteroalkyl, heteroalkenyl, oxyalkyl, heteroalkynyl, a heterocyclyl, cycloalkyl, cycloalkenyl, cycloheteroalkyl, cycloheteroalkenyl, aryl, arylalkyl, arylalkenyl, and arylalkynyl, each of which is optionally substituted;
- or any two adjacent substituents that are taken together with the attached carbons to form an optionally substituted heterocycle and each of other substituents is defined as above;
- one or more of R3, R4, R6, and R7 are not hydrogen;
- R5 is —OR, wherein R is an alkyl;
- and
- R8 is cyano or a carboxy ester,
- and one or more carriers, diluents, or excipients, to a patient in need of relief from said disorder.
(You may want to list here some specific examples of the diseases mediated by a USP7 malfunction, prostate cancer, lung cancer, multiple myeloma) . . . .
Dependencies are inferred from the claim text.