IP Library Granted Patent US 9,447,073
Granted Patent B2
US 9,447,073 · App. 14/893,785 · Granted Sep 20, 2016

Fungicidal compositions

Inventors: William J. Hoekstra (Durham, NC); Michael R. Loso (Carmel, IN); Gary D. Gustafson (Zionsville, IN); Daniel Knueppel (Zionsville, IN); Zachary A. Buchan (Indianapolis, IN); Michael T. Sullenberger (Westfield, IN)
Assignee: Viamet Pharmaceuticals, Inc.
C07D401/06A01N43/713C07D257/04C07D401/14
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Quick Facts
Patent No.
US 9,447,073
App. No.
14/893,785
Granted
Sep 20, 2016
Kind
B2
Abstract

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

Claims (55)

1. A compound of Formula I, or salt, solvate, hydrate or prodrug thereof, wherein:

MBG is

R 1 is H, alkyl, haloalkyl, cycloalkyl, benzyl, or (heteroaryl)alkyl;

R 2 is halo, aryl, heteroaryl, aryloxy, alkoxy, haloalkoxy, heteoaryloxy, alkyl, cycloalkyl, cycloalkoxy, halocycloalkoxy, haloalkyl, (alkoxy)alkyl, (haloalkoxy)alkyl, (aryl)alkyl, (aryl)alkenyl, (aryl)alkynyl, or (heteroaryl)alkyl wherein each of the aryls and heteroaryls can independently be substituted with 1, 2 or 3 groups from R 4 ;

R 3 is aryl, heteroaryl, alkyl or cycloalkyl optionally substituted with 0, 1, 2 or 3 independent R 4 ; and

R 4 is independently halo, alkyl, haloalkyl, thioalkyl, thiohaloalkyl, NO 2 , CN, alkoxy, haloalkoxy, or thioamide ((C═S)NH 2 ).

2. A compound of claim 1 wherein R 1 is H, benzyl or alkyl.

3. A compound of claim 2 wherein R 1 is H.

4. A compound of claim 1 wherein R 2 is aryloxy, heteoaryloxy, alkyl, cycloalkyl, haloalkyl, (alkoxy)alkyl, (haloalkoxy)alkyl, alkoxy, haloalkoxy or halocycloalkoxy wherein each of the aryls and heteroaryls can independently be substituted with 1, 2 or 3 groups from R 4 .

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

6. A compound of claim 5 wherein R 3 is 2,4-difluorophenyl or 2-fluoro-4-chlorophenyl.

7. A compound of claim 1 wherein R 4 is independently F, Cl, Br, CF 3 , OCF 3 , CN or thioamide ((C═S)NH 2 ).

8. A compound of claim 1 wherein:

R 1 is H, benzyl or alkyl;

R 2 is aryloxy, heteoaryloxy, alkyl, cycloalkyl, haloalkyl, (alkoxy)alkyl, (haloalkoxy)alkyl, alkoxy, haloalkoxy or halocycloalkoxy wherein each of the aryls and heteroaryls can independently be substituted with 1, 2 or 3 groups from R 4 ;

R 3 is phenyl optionally substituted with 0, 1, 2 or 3 independent halo; and

R 4 is independently F, Cl, Br, CF 3 , OCF 3 , CN or thioamide ((C═S)NH 2 ).

9. A composition comprising a compound of claim 1 and an agriculturally acceptable carrier.

10. A method of treating or preventing a fungal disease or disorder in or on a plant comprising contacting a compound of claim 1 with the plant or seeds.

11. A method of treating or preventing fungal growth in or on a plant comprising contacting a compound of claim 1 with the plant or seeds.

12. The composition according to claim 9 , further comprising an azole fungicide selected from epoxyconazole, tebuconazole, fluquinconazole, flutriafol, metconazole, myclobutanil, cycproconazole, prothioconazole and propiconazole.

13. The composition according to claim 9 , further comprising a strobilurin fungicide from the group trifloxystrobin, pyraclostrobin, orysastrobin, fluoxastrobin and azoxystrobin.

14. A compound of Formula II wherein:

R 5 is halo, aryl, heteroaryl, aryloxy, alkoxy, haloalkoxy, heteoaryloxy, alkyl, cycloalkyl, cycloalkoxy, halocycloalkoxy, haloalkyl, (alkoxy)alkyl, (haloalkoxy)alkyl, (aryl)alkyl, (aryl)alkenyl, (aryl)alkynyl, or (heteroaryl)alkyl wherein each of the aryls and heteroaryls can independently be substituted with 1, 2 or 3 groups from R 6 ; and

R 6 is independently halo, alkyl, haloalkyl, thioalkyl, thiohaloalkyl, NO 2 , CN, alkoxy, haloalkoxy, or thioamide ((C═S)NH 2 );

with the proviso that R 5 cannot be

15. The compound of claim 1 , that is one of the following compounds:

No.

Structure

F1

F2

F3

F4

F5

F6

F7

F8

F9

F10

F11

F12

F13

F14

or salt, solvate, hydrate or prodrug thereof.

16. The compound of claim 14 , that is one of the following compounds:

Compound No.

R

F15

F16

F17

F18

F19

F20

F21

or salt, solvate, hydrate or prodrug thereof.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 28, 2018
From: VPS-3, INC.
To: DOW AGROSCIENCES LLC
Reel/Frame 047318/0518 →
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 Jan 2, 2018
From: VIAMET PHARMACEUTICALS (NC), INC.
To: VPS-3, INC.
Reel/Frame 044980/0541 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 29, 2016
From: LOSO, MICHAEL; GUSTAFSON, GARY; KNUEPPEL, DANIEL; BUCHAN, ZACHARY A.; SULLENBERGER, MICHAEL T.
To: DOW AGROSCIENCES LLC
Reel/Frame 038122/0293 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 4, 2016
From: DOW AGROSCIENCES LLC
To: VIAMET PHARMACEUTICALS, INC.
Reel/Frame 037893/0336 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 8, 2016
From: HOEKSTRA, WILLIAM J.
To: VIAMET PHARMACEUTICALS, INC.
Reel/Frame 037443/0361 →
Continuity (2)
Provisional Application 61828068 · May 28, 2013
Related Publication 20160102072A1 · Apr 14, 2016