IP Library Granted Patent US 8,299,053
Granted Patent B2
US 8,299,053 · App. 12/397,651 · Granted Oct 30, 2012

Cyclic nitro compounds, pharmaceutical compositions thereof and uses thereof

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Quick Facts
Patent No.
US 8,299,053
App. No.
12/397,651
Granted
Oct 30, 2012
Kind
B2
Abstract

The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.

Claims (51)

1. A pharmaceutical composition comprising a pharmaceutically acceptable vehicle and a compound of structural Formula (I):

or a salt thereof wherein:

R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 4 is nitro;

R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 7 is a substituted acyl selected from the group consisting of substituted —C(O)-cycloalkyl, substituted —C(O)-aryl, substituted —C(O)-arylalkyl, substituted —C(O)-heteroaryl, substituted —C(O)-heteroarylalkyl, and an —C(O)-alkyl substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , —SR 60 , —CF 3 , —OS(O) 2 R 60 , —OP(O)(OR 60 )(OR 61 ), and —OP(O)(OH) 2 ;

R 60 represents independently for each occurrence alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and

R 61 represents independently for each occurrence hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl;

provided that at least two of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are nitro.

2. The pharmaceutical composition of claim 1 , wherein R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl and nitro, and R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl, and nitro.

3. The pharmaceutical composition of claim 1 , wherein R 7 is —C(O)-alkyl, —C(O)-cycloalkyl, —C(O)-aryl, —C(O)-arylalkyl, —C(O)-heteroaryl, or —C(O)-heteroarylalkyl, each of which is substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , —SR 60 , —CF 3 , and —OS(O) 2 R 60 .

4. The pharmaceutical composition of claim 1 , wherein R 7 is —C(O)-alkyl substituted with a halogen, —CF 3 or —OS(O) 2 R 8 , and wherein R 8 is alkyl, substituted alkyl, aryl, or substituted aryl.

5. The pharmaceutical composition of claim 4 , wherein R 3 is nitro; and R 1 , R 2 , R 5 , and R 6 are each independently selected from the group consisting of hydrogen, alkyl, and aryl.

6. The pharmaceutical composition of claim 1 , wherein R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl, and nitro, R 5 and R 6 are each independently selected from the group consisting of hydrogen and alkyl, and R 7 is —C(O)-alkyl, —C(O)-cycloalkyl, —C(O)-aryl, —C(O)-arylalkyl, —C(O)-heteroaryl, or —C(O)-heteroarylalkyl, each of which is substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , and —OS(O) 2 R 60 .

7. The pharmaceutical composition of claim 1 , wherein R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl and nitro; R 5 and R 6 are each independently selected from the group consisting of hydrogen and alkyl; and R 7 is —C(O)-alkyl or —C(O)-arylalkyl, each of which is substituted with a halogen, —CF 3 or —OS(O) 2 R 8 , and wherein R 8 is alkyl, substituted alkyl, aryl, or substituted aryl.

8. The pharmaceutical composition of claim 1 , wherein R 1 and R 2 are each independently selected from the group consisting of hydrogen and alkyl, R 3 is nitro, R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl and nitro, and R 7 is —C(O)-alkyl or —C(O)-arylalkyl, each of which is substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , and —OS(O) 2 R 60 .

9. The pharmaceutical composition of claim 1 , wherein R 1 and R 2 are each independently, hydrogen or alkyl; R 3 is nitro; R 5 and R 6 are each independently, hydrogen, alkyl or nitro; and R 7 is —C(O)-alkyl substituted with a halogen, —CF 3 or —OS(O) 2 R 8 , wherein R 8 is alkyl, substituted alkyl, aryl or substituted aryl.

10. The pharmaceutical composition of claim 1 , wherein R 1 and R 2 are each independently, hydrogen or alkyl; R 3 is nitro; R 5 and R 6 are each, independently, hydrogen, alkyl or nitro; and R 7 is —C(O)-alkyl substituted with a halogen.

11. The pharmaceutical composition of claim 1 , wherein R 1 and R 2 are hydrogen; R 3 is nitro; R 5 and R 6 are hydrogen; and R 7 is —C(O)—CH 3 substituted with a halogen.

12. A composition, comprising:

a first therapeutic agent comprising a compound of structural Formula (I)

wherein:

R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 4 is nitro;

R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 7 is a substituted acyl selected from the group consisting of substituted —C(O)-cycloalkyl, substituted —C(O)-aryl, substituted —C(O)-arylalkyl, substituted —C(O)-heteroaryl, substituted —C(O)-heteroarylalkyl, and an —C(O)-alkyl substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , —SR 60 , —CF 3 , —OS(O) 2 R 60 , —OP(O)(OR 60 )(OR 61 ), and —OP(O)(OH) 2 ;

R 60 represents independently for each occurrence alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and

R 61 represents independently for each occurrence hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl;

provided that at least two of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are nitro; and

a second therapeutic agent.

13. The pharmaceutical composition of claim 5 , wherein R 7 is —C(O)-alkyl substituted with a halogen or —OS(O) 2 R 8 , wherein R 8 is alkyl or aryl.

14. The pharmaceutical composition of claim 13 , wherein R 1 , R 2 , R 5 , and R 6 are each independently hydrogen or alkyl.

15. The pharmaceutical composition of claim 1 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

16. A compound of structural Formula (I):

or a salt thereof wherein:

R 1 , R 2 , and R 3 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 4 is nitro;

R 5 and R 6 are each independently selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroalkyl, substituted heteroalkyl, heteroarylalkyl, substituted heteroarylalkyl, halo, hydroxy, and nitro;

R 7 is a substituted acyl selected from the group consisting of a, substituted —C(O)-cycloalkyl, substituted —C(O)-aryl, substituted —C(O)-arylalkyl, substituted —C(O)-heteroaryl, substituted —C(O)-heteroarylalkyl, and an —C(O)-alkyl substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , —SR 60 , —CF 3 , —OS(O) 2 R 60 , —OP(O)(OR 60 )(OR 61 ), and —OP(O)(OH) 2 ;

R 60 represents independently for each occurrence alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl; and

R 61 represents independently for each occurrence hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl, or substituted heteroaryl.

17. The compound of claim 16 , wherein at least two of R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are nitro.

18. The compound of claim 17 , wherein R 7 is —C(O)-alkyl, —C(O)-aryl, or —C(O)-arylalkyl, each of which is substituted by one or more substituents independently selected from the group consisting of halogen, —OR 60 , and —OS(O) 2 R 60 .

19. The compound of claim 17 , wherein R 7 is —C(O)-alkyl substituted with one or more halogen, —CF 3 or —OS(O) 2 R 8 , and wherein R 8 is alkyl, substituted alkyl, aryl, or substituted aryl.

20. The compound of claim 19 , wherein R 1 , R 2 , R 3 , R 5 , and R 6 are each independently hydrogen, alkyl, aryl, or nitro.

21. The compound of claim 20 , wherein R 1 and R 2 are each independently hydrogen or alkyl, R 3 is nitro, and R 5 and R 6 are each independently hydrogen or alkyl.

22. The compound of claim 21 , wherein R 7 is —C(O)CH 3 substituted with one or more halogen.

23. The compound of claim 16 , wherein the compound is

or a pharmaceutically acceptable salt thereof.

24. The compound of claim 16 , wherein R 7 is —C(O)-alkyl or —C(O)-arylalkyl, each of which is substituted with one or more halogen, —CF 3 or —OS(O) 2 R 8 , and wherein R 8 is alkyl, substituted alkyl, aryl, or substituted aryl.

Assignments (14)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 8, 2021
From: NORTHROP GRUMMAN INNOVATION SYSTEMS LLC
To: NORTHROP GRUMMAN SYSTEMS CORPORATION
Reel/Frame 055256/0892 →
CHANGE OF NAME Recorded Feb 4, 2021
From: NORTHROP GRUMMAN INNOVATION SYSTEMS, INC.
To: NORTHROP GRUMMAN INNOVATION SYSTEMS LLC
Reel/Frame 055223/0425 →
CHANGE OF NAME Recorded Nov 1, 2018
From: ORBITAL ATK, INC.
To: NORTHROP GRUMMAN INNOVATION SYSTEMS, INC.
Reel/Frame 047400/0381 →
TERMINATION AND RELEASE OF SECURITY INTEREST IN PATENTS Recorded Jun 6, 2018
From: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS ADMINISTRATIVE AGENT
To: ORBITAL ATK, INC.
Reel/Frame 046477/0874 →
CHANGE OF NAME Recorded Oct 27, 2015
From: RADIORX, INC.
To: EPICENTRX, INC.
Reel/Frame 036969/0231 →
RELEASE OF SECURITY INTEREST Recorded Oct 8, 2015
From: BANK OF AMERICA, N.A.
To: ALLIANT TECHSYSTEMS INC.; FEDERAL CARTRIDGE CO.; EAGLE INDUSTRIES UNLIMITED, INC.; AMMUNITION ACCESSORIES, INC.; ORBITAL ATK, INC. (F/K/A ALLIANT TECHSYSTEMS INC.)
Reel/Frame 036816/0624 →
RELEASE OF SECURITY INTEREST Recorded Oct 7, 2015
From: BANK OF AMERICA, N.A.
To: ALLIANT TECHSYSTEMS INC.
Reel/Frame 036807/0671 →
SECURITY AGREEMENT Recorded Sep 30, 2015
From: ORBITAL ATK, INC.; ORBITAL SCIENCES CORPORATION
To: WELLS FARGO BANK, NATIONAL ASSOCIATION, AS ADMINISTRATIVE AGENT
Reel/Frame 036732/0170 →
CHANGE OF NAME Recorded May 22, 2015
From: ALLIANT TECHSYSTEMS INC.
To: ORBITAL ATK, INC.
Reel/Frame 035753/0373 →
SECURITY AGREEMENT Recorded Nov 26, 2013
From: ALLIANT TECHSYSTEMS INC.; CALIBER COMPANY; EAGLE INDUSTRIES UNLIMITED, INC.; FEDERAL CARTRIDGE COMPANY; SAVAGE ARMS, INC.; SAVAGE RANGE SYSTEMS, INC.; SAVAGE SPORTS CORPORATION
To: BANK OF AMERICA, N.A.
Reel/Frame 031731/0281 →
SECURITY AGREEMENT Recorded Nov 4, 2010
From: ALLIANT TECHSYSTEMS INC.; AMMUNITION ACCESSORIES INC.; ATK COMMERCIAL AMMUNITION COMPANY INC.; ATK COMMERCIAL AMMUNITION HOLDINGS COMPANY; ATK LAUNCH SYSTEMS INC.; ATK SPACE SYSTEMS INC.; FEDERAL CARTRIDGE COMPANY; EAGLE INDUSTRIES UNLIMITED, INC.; EAGLE MAYAGUEZ, LLC; EAGLE NEW BEDFORD, INC.
To: BANK OF AMERICA, N.A.
Reel/Frame 025321/0291 →
INTELLECTUAL PROPERTY SECURITY AGREEMENT SUPPLEMENT Recorded Sep 24, 2009
From: ALLIANT TECHSYSTEMS INC.
To: BANK OF AMERICA, N.A.
Reel/Frame 023275/0412 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2009
From: CANNIZZO, LOUIS; WARNER, KIRSTIN; WARDLE, ROBERT; VELARDE, STEPHEN
To: ALLIANT TECHSYSTEMS INC.
Reel/Frame 023062/0571 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2009
From: OEHLER, LYNN M.; KNOX, SUSAN; NING, SHOUCHENG
To: RADIORX, INC.
Reel/Frame 023057/0789 →