IP Library Granted Patent US 8,236,962
Granted Patent B2
US 8,236,962 · App. 13/093,530 · Granted Aug 7, 2012

Metalloenzyme inhibitor compounds

Assignee: Viamet Pharmaceuticals, Inc.
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Quick Facts
Patent No.
US 8,236,962
App. No.
13/093,530
Granted
Aug 7, 2012
Kind
B2
Abstract

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Claims (56)

1. A compound of formula (I), or salt thereof, wherein:

MBG is optionally substituted tetrazolyl, optionally substituted triazolyl, or optionally substituted pyrazolyl;

R 1 is halo;

R 2 is halo;

each R 3 is independently alkyl, cyano, haloalkyl, alkoxy, halo, haloalkoxy,

R 4 is aryl optionally substituted with O, 1, 2 or 3 independent R 3 ;

R 5 is H, or —C(O)alkyl optionally substituted with amino;

n is 0, 1, 2 or 3.

2. The compound of claim 1 , wherein R 1 is fluoro.

3. The compound of claim 1 , wherein R 2 is fluoro.

4. The compound of claim 1 , wherein R 1 and R 2 are fluoro.

5. The compound of claim 1 , wherein R 4 is phenyl optionally substituted with 0, 1, 2 or 3 independent R 3 .

6. The compound of claim 1 , wherein R 4 is phenyl optionally substituted with 0, 1, 2 or 3 independent halo.

7. The compound of claim 1 , wherein R 4 is phenyl optionally substituted with 0, 1, 2 or 3 independent fluoro.

8. The compound of claim 1 , wherein R 4 is 2,4-difluorophenyl.

9. The compound of claim 1 , wherein R 5 is H.

10. The compound of claim 1 , wherein R 5 is amino substituted acyl.

11. The compound of claim 1 , wherein:

R 1 is fluoro;

R 2 is fluoro;

R 4 is 2,4-difluorophenyl; and

R 5 is H.

12. The compound of claim 1 , wherein:

each R 3 is independently cyano, haloalkyl, alkoxy, halo, haloalkoxy, and n is 1 or 2.

13. The compound of claim 11 , wherein:

each R 3 is independently cyano, haloalkyl, alkoxy, halo, haloalkoxy, and n is 1.

14. The compound of claim 1 , which is one of:

4-(6-(2-(2,4-Difluorophenyl)-1,1-difluoro-2-hydroxy-3-(1H-tetrazol-1-yl)propyl)pyridin-3-yl)benzonitrile (1);

2-(2, 4-Difluorophenyl)-1, 1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(trifluoromethyl)phenyl)pyridin-2-yl) propan-2-ol (2);

3-(6-(2-(2,4-Difluorophenyl)-1,1-difluoro-2-hydroxy-3-(1H-tetrazol-1-yl)propyl)pyridin-3-yl)benzonitrile (3);

2-(2,4-Difluorophenyl)-1,1-difluoro-1-(5-(4-isopropoxyphenyl)pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ol (4);

2-(2,4-Difluorophenyl)-1,1-difluoro-1-(5-(4-fluorophenyl)pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ol (5);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(3-(trifluoromethoxy)phenyl)pyridin-2-yl)propan-2-ol (6);

2-(2, 4-Difluorophenyl)-1, 1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl) propan-2-ol (7);

1-(5-(3-Chlorophenyl)pyridin-2-yl)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)propan-2-ol (8);

1-(5-(4-Chlorophenyl)pyridin-2-yl)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)propan-2-ol (9);

2-(2,4-Difluorophenyl)-1-(5-(2,5-difluorophenyl)pyridin-2-yl)-1,1-difluoro-3-(1H-tetrazol-1-yl)propan-2-ol (10);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-ol (11);

2-(2,4-Difluorophenyl)-1,1-difluoro-1-(5-(4-(2,2,3,3,3-pentafluoropropoxy)phenyl)pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ol (12);

2-(2, 4-difluorophenyl)-1, 1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(2, 2, 2-trifluoroethoxy)phenyl)pyridin-2-yl) propan-2-yl 3-aminopropanoate (13);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-yl 2-aminoacetate hydrochloride (14);

2-(2,4-Difluorophenyl)-1, 1-difluoro-3-(1H-pyrazol-3-yl)-1-(5-(4-(trifluoro methoxy)phenyl)pyridin-2-yl) propan-2-ol (15);

2-(2,4-Difluorophenyl)-1,1-difluoro-1-(5-(4-fluorophenyl)pyridin-2-yl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol (16);

2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-1,2,4-triazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-ol (17);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-1,2,4-triazol-1-yl)-1-(5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl) propan-2-ol (18);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-1,2,3-triazol-1-yl)-1-(5-(4-(trifluoromethoxy)phenyl)pyridin-2-yl) propan-2-ol (19);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(2H-tetrazol-1-yl)-1-(5-(4-(2,2,2-trifluoroethoxy)phenyl)pyridin-2-yl)propan-2-ol (20);

2-(2, 4-Difluorophenyl)-1, 1-difluoro-3-(2H-tetrazol-1-yl)-1-(5-(3-(fluorophenyl)pyridin-2-yl) propan-2-ol (21);

2-(2, 4-Difluorophenyl)-1, 1-difluoro-3-(2H-tetrazol-1-yl)-1-(5-(4-(trifluoromethylphenyl)pyridin-2-yl) propan-2-ol (22);

2-(2, 4-Difluorophenyl)-1, 1-difluoro-3-(1H-1,2,3-triazol-1-yl)-1-(5-(4-(trifluoromethylphenyl)pyridin-2-yl) propan-2-ol (23);

4-(6-(2-(2,4-Difluorophenyl)-1,1-difluoro-2-hydroxy-3-(1H-tetrazol-1-yl)propyl)pyridin-3-yl)phenol (24);

2-(2,4-Difluorophenyl)-1,1-difluoro-1-(5-(3-isopropylphenyl)pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ol (25);

2-(2,4-Difluorophenyl)-1-(5-(3,4-difluorophenyl)pyridin-2-yl)-1,1-difluoro-3-(1H-tetrazol-1-yl)propan-2-ol (26);

1-(5-(3-(Difluoromethoxy)phenyl)pyridin-2-yl)-2-(2,4-difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)propan-2-ol (27);

2-(2,4-Difluorophenyl)-1,1-difluoro-3-(1H-tetrazol-1-yl)-1-(5-(4-((trifluoromethyl) thio)phenyl)pyridin-2-yl)propan-2-ol (28).

15. A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

Assignments (6)
CHANGE OF NAME Recorded Mar 28, 2018
From: VIAMET PHARMACEUTICALS (NC), INC.
To: MYCOVIA PHARMACEUTICALS, INC.
Reel/Frame 045759/0728 →
CHANGE OF NAME Recorded Jan 2, 2018
From: VIAMET PHARMACEUTICALS, INC.
To: VIAMET PHARMACEUTICALS (NC), INC.
Reel/Frame 044978/0893 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2014
From: INNOCRIN PHARMACEUTICALS, INC.
To: VPS-1, INC.
Reel/Frame 034091/0427 →
CHANGE OF NAME Recorded Nov 3, 2014
From: VIAMET PHARMACEUTICALS, INC.
To: INNOCRIN PHARMACEUTICALS, INC.
Reel/Frame 034131/0251 →
CHANGE OF NAME Recorded Nov 3, 2014
From: VPS-1, INC.
To: VIAMET PHARMACEUTICALS, INC.
Reel/Frame 034143/0405 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 23, 2011
From: HOEKSTRA, WILLIAM J.; SCHOTZINGER, ROBERT J.; RAFFERTY, STEPHEN W.
To: VIAMET PHARMACEUTICALS, INC.
Reel/Frame 026487/0929 →
Continuity (3)
Continuation PCTUS2011033597 · Apr 22, 2011
Provisional Application 61327663 · Apr 24, 2010
Related Publication 20110306644A1 · Dec 15, 2011