IP Library › Granted Patent US 7,405,235
Granted Patent B2
US 7,405,235 · App. 10/700,661 · Granted Jul 29, 2008

Transcription factor modulating compounds and methods of use thereof

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Quick Facts
Patent No.
US 7,405,235
App. No.
10/700,661
Granted
Jul 29, 2008
Kind
B2
Abstract

Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

Claims (199)

1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and an effective amount of a transcription factor modulating compound, wherein said compound is of the formula (Va):

wherein

R 1 is OH;

R 2 is substituted phenyl; and

R 4 , R 5 and R 7 are H;

R 6 is nitro;

or pharmaceutically acceptable salts thereof.

2. The pharmaceutical composition of claim 1 , wherein the composition further comprises an antibiotic.

3. A compound of the formula (Va):

wherein

R 1 is OH;

R 2 is substituted phenyl; and

R 4 , R 5 , R 7 are H;

R 6 is nitro;

and pharmaceutically acceptable salts thereof.

4. The compound of claim 3 , wherein said compound is:

5. The compound of claim 3 , wherein said substituted phenyl is substituted with a substituent selected from the group consisting of substituted or unsubstituted acylamino, aromatic moiety, aminocarbonyl, alkoxy, hydroxyl, halogen, amino, carboxylate, sulfonamido, heterocyclyl, alkylthio, amidino, or a heteroaromatic moiety.

6. The compound of claim 5 , wherein said substituent is acylamino.

7. The compound of claim 6 , wherein said acylamino is alkylaminocarbonyl.

8. The compound of claim 7 , wherein the alkyl of said alkylaminocarbonyl is cycloatkyl.

9. The compound of claim 8 , wherein said cycloalkyl is cyclohexyl.

10. The compound of claim 7 , wherein the alkyl of said alkylaminocarbonyl is methyl or t-butyl.

11. The compound of claim 6 , wherein said acylamino is arylcarbonylamino.

12. The compound of claim 11 , wherein the aryl of said arylcarbonylamino is substituted or unsubstituted pyridinyl, phenyl or furanyl.

13. The compound of claim 12 , wherein said substituted phenyl is substituted with alkoxy, halogen, amino, or a heterocyclyl moiety.

14. The compound of claim 13 , wherein said alkoxy is trifluormethoxy or methoxy.

15. The compound of claim 13 , wherein said halogen is chlorine or fluorine.

16. The compound of claim 13 , wherein said amino is dialkylamino.

17. The compound of claim 16 , wherein the alkyl of said dialkylamino is methyl.

18. The compound of claim 6 , wherein said acylamino is ureido.

19. The compound of claim 5 , wherein said aromatic moiety is phenyl.

20. The compound of claim 5 , wherein said heteroaromatic moiety is pyrrolyl.

21. The compound of claim 5 , wherein said alkoxy is methoxy or trifluoromethoxy.

22. The pharmaceutical composition of claim 1 , wherein said substituted phenyl is substituted with a substituent selected from the group consisting of substituted or unsubstituted acylamino, aromatic moiety, aminocarbonyl, alkoxy, hydroxyl, halogen, amino, carboxylate, sulfonamido, heterocyclyl, alkylthio, amidino, or a heteroaromatic moiety.

23. The pharmaceutical composition of claim 22 , wherein said substituent is acylamino.

24. The pharmaceutical composition of claim 23 , wherein said acylamino is alkylaminocarbonyl.

25. The pharmaceutical composition of claim 24 , wherein the alkyl of said alkylaminocarbonyl is cycloalkyl.

26. The pharmaceutical composition of claim 25 , wherein said cycloalkyl is cyclohexyl.

27. The pharmaceutical composition of claim 24 , wherein the alkyl of said alkylaminocarbonyl is methyl or t-butyl.

28. The pharmaceutical composition of claim 23 , wherein said acylamino is arylcarbonylamino.

29. The pharmaceutical composition of claim 28 , wherein the aryl of said arylcarbonylamino is substituted or unsubstituted pyridinyl, phenyl or furanyl.

30. The pharmaceutical composition of claim 29 , wherein said substituted phenyl is substituted with alkoxy, halogen, amino, or a heterocyclyl moiety.

31. The pharmaceutical composition of claim 30 , wherein said alkoxy is trifluormethoxy or methoxy.

32. The pharmaceutical composition of claim 30 , wherein said halogen is chlorine or fluorine.

33. The pharmaceutical composition of claim 30 , wherein said amino is dialkylamino.

34. The pharmaceutical composition of claim 33 , wherein the alkyl of said dialkylamino is methyl.

35. The pharmaceutical composition of claim 23 , wherein said acylamino is ureido.

36. The pharmaceutical composition of claim 22 , wherein said aromatic moiety is phenyl.

37. The pharmaceutical composition of claim 22 , wherein said heteroaromatic moiety is pyrrolyl.

38. The pharmaceutical composition of claim 22 , wherein said alkoxy is methoxy or trifluoromethoxy.

39. The compound of claim 5 , wherein said substituted phenyl is substituted with more than one substituent.

40. The pharmaceutical composition of claim 22 , wherein said substituted phenyl is substituted with more than one substituent.

41. The compound of claim 3 , wherein said compound is:

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48. A compound of the formula:

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Assignments (7)
TERMINATION OF LIEN ON PATENTS Recorded Dec 23, 2014
From: MCCARTER & ENGLISH, LLP
To: PARATEK PHARMACEUTICALS, INC.
Reel/Frame 034695/0958 →
RELEASE OF SECURITY INTEREST Recorded Oct 31, 2014
From: HBM HEALTHCARE INVESTMENTS (CAYMAN) LTD., AS COLLATERAL AGENT
To: PARATEK PHARMACEUTICALS, INC.
Reel/Frame 034113/0910 →
SECURITY INTEREST Recorded Mar 14, 2014
From: PARATEK PHARMACEUTICALS, INC.
To: HBM HEALTHCARE INVESTMENTS (CAYMAN) LTD., AS COLLATERAL AGENT
Reel/Frame 032448/0001 →
SECURITY INTEREST BY OPERATION OF MASSACHUSETTS LAW Recorded Feb 26, 2014
From: PARATEK PHARMACEUTICALS, INC.
To: MCCARTER & ENGLISH, LLP
Reel/Frame 032335/0935 →
RELEASE OF SECURITY INTEREST Recorded Oct 9, 2009
From: MIDCAP FINANCIAL, LLC
To: PARATEK PHARMACEUTICALS, INC.
Reel/Frame 023348/0621 →
SECURITY AGREEMENT Recorded Jul 6, 2009
From: PARATEK PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL, LLC
Reel/Frame 022917/0112 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 1, 2005
From: LEVY, STUART B.; ALEKSHUN, MICHAEL N.; PODLOGAR, BRENT L.; OHEMENG, KWASI; VERMA, ATUL K.; WARCHOL, TADEUSZ; BHATIA, BEENA; BOWSER, TODD; GRIER, MARK
To: PARATEK PHARMACEUTICALS, INC.
Reel/Frame 015641/0129 →