IP Library Granted Patent US 7,566,732
Granted Patent B2
US 7,566,732 · App. 10/975,761 · Granted Jul 28, 2009

Rhodanine compositions for use as antiviral agents

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Quick Facts
Patent No.
US 7,566,732
App. No.
10/975,761
Granted
Jul 28, 2009
Kind
B2
Abstract

This invention describes compounds and pharmaceutical compositions useful as inhibitors of ubiquitination. The compounds and compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. In particular, the compounds and compositions are useful for treating diseases caused by viruses such as poxviruses and retroviruses. The invention further provides for methods of treating smallpox, Herpes virus and HIV infection in patients using the compounds and compositions of the invention.

Claims (13)

1. A compound of the formula V:

or a pharmaceutically acceptable salt thereof, wherein

R 1 is —NH 2 , C 1 -C 6 alkyl, C 1 -C 2 alkenyl, C 1 -C 6 alkyl-S—C 1 -C 6 alkyl, C 0 -C 6 alky-aryl, C 0 -C 6 alkyl-heteroaryl, C 0 -C 6 alkyl-heterocyclyl, C 0 -C 6 alkyl-carbocyclyl, —NH—SO 2 -aryl, —C 0 -C 6 alkyl-C(S)NR 6 R 7 , C 0 -C 6 alky-heteroaryl-aryl, —NHC(O)-aryl, —SO 2 —R 6 , C(O)—R 6 or —C(O)—OR 6 , wherein each one of the alkyl, aryl, heteroaryl, heterocyclic and carbocyclyl are optionally substituted with one or more R 5 ;

R 2 is independently —H, halogen, C 1 -C 6 alkyl, C 0 -C 6 alky-aryl, —NO 2 , C 0 -C 6 alkyl-C(O)—OR 6 , C 0 -C 6 alkyl-heteroaryl, C 0 -C 6 alkyl-heterocyclyl, C 0 -C 6 alkyl-carbocyclyl, —N(R 6 )—C(O)NR 6 R 7 , —NHSO 2 -aryl, C 0 -C 6 alky-heteroaryl-aryl or —C(O)—R 6 , wherein each one of the aryl, heteroaryl, heterocyclic and carbocyclyl are optionally substituted with one or more R 4 ;

R 4 is halogen, oxo, —C(O)OR 6 , —NO 2 , C 1 -C 6 alkyl optionally substituted with halo, —C 1 -C 6 alkoxy optionally substituted with halo, —CF 3 , —SO 2 NH 2 or —C(O)—OR 6 ;

R 5 is halogen, oxo, C 1 -C 6 alkoxy, C 1 -C 6 alkyl, C 0 -C 6 alkyl-aryl, —NO 2 , di(C 1 -C 6 alkyl)amino, —CF 3 , —OH, —SO 2 NH 2 or —C(O)—OR 6 ;

R 6 and R 7 are independently —H, halogen, C 1 -C 6 alkoxy, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, aryl, di(C 1 -C 6 alkyl)amino, —CF 3 , —OH or —C(O)—OR 6 ;

R 10 is —H, halogen, C 1 -C 6 alkyl, C 0 -C 6 alky-aryl, —NO 2 , C 0 -C 6 alkyl-C(O)—OR 6 , C 0 -C 6 alkyl-heteroaryl, C 0 -C 6 alkyl-heterocyclyl, C 0 -C 6 alkyl-carbocyclyl, —N(R 6 )—C(O)NR 6 R 7 , —NHSO 2 -aryl, C 0 -C 6 alky-heteroaryl-aryl, or —C(O)—R 6 , wherein each one of the aryl, heteroaryl, heterocyclic and carbocyclyl are optionally substituted with one or more R 4 .

2. The compound according to claim 1 wherein

a) R 10 is selected from —H and C 1 -C 6 -alkyl;

b) R 1 is (i) aryl optionally substituted with one or more R 4 wherein in preferred embodiments R 1 is substituted with a single R 4 selected from halo and (C 0 -C 6 -alkyl)(C 0 -C 6 -alkyl)N—, more preferably fluoro, chloro, bromo, or di-ethylamino; or (ii) C 2 -C 6 alkenyl, preferably CH 2 ═CH—; and/or

c) R 2 is —H or C 1 -C 6 alkyl.

3. A composition comprising a compound according to claim 1 together with a pharmaceutically acceptable carrier, excipient, or diluent.

Assignments (3)
SECURITY INTEREST Recorded May 8, 2026
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FUNDING IV TRUST
Reel/Frame 075576/0880 →
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 21, 2005
From: SINGH, RAJINDER; RAMESH, USHA; ISSAKANI, SARKIZ D.; LOOK, GARY CHARLES
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 016378/0352 →