IP Library Granted Patent US 9,371,277
Granted Patent B2
US 9,371,277 · App. 14/139,763 · Granted Jun 21, 2016

Benzamide compounds and related methods of use

Inventors: Richard B. Silverman (Winnetka, IL); Hua Wang (Evanston, IL); Mohammad Khanfar (Evanston, IL); Aleksey G. Kazantsev (Boston, MA)
Assignees: Northwestern University; The General Hospital Corporation
C07C311/16C07C235/60C07C255/60C07C257/18C07C311/21C07C311/29C07C311/46C07C311/47C07C317/22C07C317/34C07C317/40C07C317/44C07C317/48C07C323/20C07C323/42C07C323/49C07C323/62C07D207/16C07D213/75C07D213/76C07D213/80C07D213/81C07D213/82C07D213/85C07D217/04C07D223/04C07D237/20C07D239/42C07D261/14C07D271/113C07D277/46C07D295/26C07D305/06C07D311/16C07D403/12C07D413/12C07D417/12C07B2200/07C07C2101/02
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Quick Facts
Patent No.
US 9,371,277
App. No.
14/139,763
Granted
Jun 21, 2016
Kind
B2
Abstract

Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease.

Claims (9)

1. A compound selected from compounds of a formula

wherein each of R 1 and R 2 is independently selected from phenyl, benzyl, heteroaryl, and heteroarylalkyl moieties; each of E 1 and E 2 is independently selected from CH and N, provided at least one of E 1 and E 2 is CH; A is a divalent moiety selected from carbonyl, amino, carboxamido (—C(O)NH—), imidocarbyl (—C(NH)—) and a tautomer thereof (—N ═C(NH 2 )—) with X; X is a divalent moiety selected from methylene, carbonyl, amino, and aza-substituted ethylene (—NHCH 2 —) moieties; Y is a divalent moiety selected from oxy, amino, alkylene, and aza-substituted alkylene moieties; and Z is a divalent moiety selected from sulfonyl, sulfinyl, thio, oxy, amino, and methylene moieties, providing where A is carbonyl, Z is sulfonyl and R 1 and R 2 are selected from phenyl and substituted phenyl, X is not amino or methylamino and Y is not amino, alkylamino, allylamino or benzylamino, and wherein each of R 1 , R 2 , A, X, Y and Z is optionally substituted with 1-10 substituents independently selected from halo, cyano, nitro, hydroxy, amino, alkyl, cycloalkyl, cycloheteroalkyl, aryl, arylalkyl, alkoxy, alkenyl, haloalkyl, aminoalkyl, hydroxyalkyl, alkylene, alkylsulfonyl, haloalkylsulfonyl, haloalkylsulfinyl, alkylamido, alkylsulfonamido, alkylthio, alkylcarbonyl, alkoxycarbonyl and combinations of such substituents; R 3 is selected from said substituents and combinations thereof; and n is an integer from 0-4, and salts of said compounds.

2. The compound of claim 1 where A is carbonyl and E 2 is CH, said compound of a formula

3. The compound of claim 2 wherein X is selected from amino and alkylamino moieties, and Z is methylene, said compound of a formula

4. The compound of claim 3 wherein Y is selected from oxy, alkylene, alkyl-substituted alkylene, amino and substituted amino moieties.

5. The compound of claim 4 wherein R 2 is a substituted benzyl moiety, said substituents selected from 1-3 halo and cyano substituents and combinations thereof.

6. The compound of claim 4 wherein Y is a substituted amino moiety and R 2 is selected from phenyl, substituted phenyl, benzyl, substituted benzyl, heteroaryl, substituted heteroaryl, heteroarylalkyl and substituted heteroarylalkyl moieties.

7. The compound of claim 6 wherein said amino substituent is selected from alkyl and cycloalkyl moieties.

8. The compound of claim 7 wherein said amino substituent is selected from methyl, ethyl, isopropyl and cyclopropyl moieties.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 14, 2014
From: KAZANTSEV, ALEKSEY
To: THE GENERAL HOSPITAL CORPORATION
Reel/Frame 033946/0268 →
CONFIRMATORY LICENSE Recorded Apr 3, 2014
From: NORTHWESTERN UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 032600/0717 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 5, 2014
From: SILVERMAN, RICHARD B.; WANG, HUA; KHANFAR, MOHAMMAD
To: NORTHWESTERN UNIVERSITY
Reel/Frame 032354/0552 →
CONFIRMATORY LICENSE Recorded Feb 24, 2014
From: NORTHWESTERN UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 032329/0955 →
Continuity (2)
Provisional Application 61745056 · Dec 21, 2012
Related Publication 20140234939A1 · Aug 21, 2014