IP Library Granted Patent US 10,730,848
Granted Patent B2
US 10,730,848 · App. 14/801,247 · Granted Aug 4, 2020

Protective molecules against anthrax toxin

Inventors: Eugene Gillespie (Los Angeles, CA); Robert Damoiseaux (Beverly Hills, CA); Chi-Lee Charlie Ho (Los Angeles, CA); Brian T. Chamberlain (Simi Valley, CA); Michael E. Jung (Los Angeles, CA); Kenneth A. Bradley (Los Angeles, CA)
Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
C07D333/28C07C243/22C07C281/14C07C281/18C07C311/08C07C335/26C07C337/08C07D213/53C07D231/12C07D307/52C07D307/56C07D333/22
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Quick Facts
Patent No.
US 10,730,848
App. No.
14/801,247
Granted
Aug 4, 2020
Kind
B2
Abstract

Disclosed herein inter alia are compositions and methods useful in the treatment of infectious diseases and exposure to toxins.

Claims (46)

1. A method of inhibiting anthrax caused by exposure to Bacillus anthracis in a subject in need thereof, said method comprising administering an effective amount of a compound, or pharmaceutically acceptable salt thereof, to the subject, wherein the compound has the formula:

wherein

R 1 is independently hydrogen, halogen, —CX 3 3 , —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11C R 12C , —OR 13C , —SR 14C , substituted alkyl, substituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 2 is independently hydrogen, halogen, —CX 3 3 , —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NR 11C R 12C , —OR 13C , —SR 14C , substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 3 is independently hydrogen, halogen, —CX 3 3 , —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11C R 12C , —OR 13C , —SR 14C , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

each R 4 is independently hydrogen, halogen, —CX 3 3 , —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11C R 12C , —OR 13C , —SR 14C , substituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 5 is independently hydrogen, —Cl, —Br, —I, —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11C R 12C , —OR 13C , —SR 14C , unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

wherein (i) at least one of R 1 , R 2 , R 3 , R 4 , or R 5 of Formula IV is not hydrogen; and (ii) at least one of R 2 , R 3 , or R 4 of Formula V is not hydrogen;

R 6 is hydrogen or unsubstituted alkyl;

R 7 is O, S, or NH;

each R 8 is independently halogen, —CX 3 , —OCX 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11 R 12 , —OR 13 , —SR 14 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 9 is hydrogen;

each R 11 , R 12 , R 13 , and R 14 is independently a hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 10 is hydrogen, halogen, —C(X 2 ) 3 , —OC(X 2 ) 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NHSO 2 CH 3 , —N 3 , —NR 11B R 12B , —OR 13B , —SR 14B , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 11A , R 12A , R 13A , R 14A , R 11B , R 12B , R 13B , R 14B , R 11C , R 12C , R 13C , and R 14C are independently a hydrogen, substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

L 1 is —S—;

each X is independently a halogen;

X 1 , X 2 and X 3 are independently a halogen; and

wherein the compound is not any of

2. The method of claim 1 , wherein;

R 1 and R 4 are independently hydrogen, halogen, —OR 13C , substituted alkyl, substituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 2 is independently hydrogen, halogen, —CX 3 3 , —CN, —NHSO 2 CH 3 , —N 3 , —OR 13C , substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 3 and R 5 are independently hydrogen, halogen, —CX 3 3 , —OR 13C , unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

each R 8 is independently substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 10 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; and

each R 13C is independently a hydrogen or a substituted or unsubstituted alkyl.

3. The compound, of claim 1 , wherein;

R 1 is independently hydrogen, halogen, or —OR 13C ;

R 2 is independently hydrogen, halogen, —CX 3 3 , —CN, —N 3 , —OR 13C , or unsubstituted alkyl;

R 3 is independently hydrogen, halogen, —CX 3 3 , —OR 13C , or unsubstituted alkyl;

R 4 is independently hydrogen, halogen, —OR 13C , or unsubstituted alkyl;

R 5 is independently hydrogen, halogen, —OR 13C , or unsubstituted alkyl;

R 6 is independently hydrogen or unsubstituted alkyl;

each R 8 is independently an unsubstituted alkyl;

R 9 is independently hydrogen;

R 10 is independently hydrogen or unsubstituted alkyl;

each R 13C is independently an unsubstituted alkyl; and

X 3 is —F.

4. The method of claim 1 , wherein the compound is:

5. The method of claim 1 , wherein the compound is co-administered with an antibiotic.

6. The method of claim 1 , wherein the compound is co-administered with an doxycycline and/or ciprofloxacin.

7. The method of claim 4 , wherein the compound is co-administered with an antibiotic.

8. The method of claim 4 , wherein the compound is co-administered with an doxycycline and/or ciprofloxacin.

9. The method of claim 1 , wherein R 2 is independently halogen, —CX 3 3 , —OCX 3 3 , —CN, —C(O)OH, —CONH 2 , —NO 2 , —SO 2 Cl, —SO 2 NH 2 , —NHNH 2 , —NR 11C R 12C , —OR 13C , —SR 14C , substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

10. The method of claim 1 , wherein R 2 is independently halogen, —CX 3 3 , —CN, —NHSO 2 CH 3 , —N 3 , —OR 13C , substituted or unsubstituted alkyl, unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl.

11. The method of claim 1 , wherein R 2 is independently halogen, —CX 3 3 , —CN, —N 3 , —OR 13C , or unsubstituted alkyl.

Assignments (2)
CONFIRMATORY LICENSE Recorded Jun 10, 2016
From: UNIVERSITY OF CALIFORNIA LOS ANGELES
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 038955/0491 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 8, 2016
From: BRADLEY, KENNETH A.; JUNG, MICHAEL E.; DAMOISEAUX, ROBERT; ZINK, JEFFREY; HO, CHI-LEE CHARLIE; CHAMBERLAIN, BRIAN T.; GILLESPIE, EUGENE; LI, ZONGXI; THOMAS, DIANE
To: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
Reel/Frame 037926/0298 →
Continuity (3)
Continuation PCTUS2014011930 · Jan 16, 2014
Provisional Application 61753355 · Jan 16, 2013
Related Publication 20160016930A1 · Jan 21, 2016