IP Library Granted Patent US 9,206,199
Granted Patent B2
US 9,206,199 · App. 14/364,908 · Granted Dec 8, 2015

Inhibitors of the renal outer medullary potassium channel

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Quick Facts
Patent No.
US 9,206,199
App. No.
14/364,908
Granted
Dec 8, 2015
Kind
B2
Abstract

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.

Claims (276)

1. A compound having structural Formula I:

or a pharmaceutically acceptable salt thereof wherein:

X is O;

R 1 is —C(R 9 )(R 10 )— or —N(R 13 )—;

m is an integer selected from 1 or 2;

X 1 , X 2 and X 3 are each independently selected from C(R 7 ) or N, provided that at least one of X 1 , X 2 and X 3 must be N and at most two of X 1 X 2 and X 3 are N;

Z is

R 2 is —H, —F, —Cl, —C 1-6 alkyl, —C 3-6 cycloalkyl or —OC 1-6 alkyl;

R 3 and R 3a are each independently —H, —F, —Cl, —CN, —C 1-6 alkyl, —C 3-6 cycloalkyl or —OC 1-6 alkyl;

R 4 and R 4a are each independently —F, —Cl, —CN, —C 1-6 alkyl, —C 3-6 cycloalkyl, —OC 1-4 alkyl or N-tetrazolyl;

or R 3 and R 4 are joined together with the carbon atoms in the phenyl ring to which they are attached to form:

wherein R is —H or —C 1-4 alkyl;

R 5 and R 5a are each independently —H, —F, —Cl, —CN, —C 1-4 alkyl, —C 3-6 cycloalkyl or —OC 1-4 alkyl;

provided that when R 3 and R 4 are not joined together, then one and only one of R 3 , R 4 or R 5 is —CN;

and provided that one and only one of R 3a , R 4a or R 5a is —CN;

R 6 is —H or —C 1-4 alkyl;

each R 7 is independently —H, —F, —Cl, —CF 3 , —C 1-4 alkyl or —OC 1-4 alkyl;

R 8 is —H, —F, —Cl, —CF 3 , —C 1-4 alkyl or —OC 1-4 alkyl;

R 9 is —H, —F or —C 1-4 alkyl;

R 10 is —H or —F;

R 11 is —H or —CH 3 ;

R 12 is —H or —CH 3 ; and

R 13 is —H or —C 1-4 alkyl.

2. The compound of claim 1 wherein Z is

and one of R 3 and R 4 is —CN, or a pharmaceutically acceptable salt thereof.

3. The compound of claim 1 wherein Z is

or a pharmaceutically acceptable salt thereof.

4. The compound of claim 1 wherein Z is

or a pharmaceutically acceptable salt thereof.

5. The compound of claim 1 or a pharmaceutically acceptable salt thereof wherein R 1 is —C(R 9 )(R 10 )—.

6. The compound of claim 1 or a pharmaceutically acceptable salt thereof wherein

7. The compound of claim 1 or a pharmaceutically acceptable salt thereof wherein m is 1, R 6 is —H, R 11 is —H and R 12 is —H.

8. The compound of claim 2 having structural Formula IV

or a pharmaceutically acceptable salt thereof wherein:

X is O,

X 1 , X 2 and X 3 are each independently selected from C(R 7 ) or N, provided that at least one of X 1 , X 2 and X 3 must be N and at most two of X 1 X 2 and X 3 are N;

Z is

R is —H or —C 1-3 alkyl; R 2 is —H, —F, —Cl, —C 1-3 alkyl, cyclopropyl or —OC 1-3 alkyl;

R 3 is —H, —F, —Cl, —CN, —C 1-3 alkyl, cyclopropyl or —OC 1-3 alkyl; R 5 is —H, —F, —Cl, —CN, —C 1-3 alkyl, cyclopropyl or —OC 1-3 alkyl; R 7 is —H, —CH 3 , —CH 2 CH 3 , —OCH 3 , —F, —Cl, or —CF 3 ; and

R 8 is —H, —CH 3 or —OCH 3 .

9. The compound of claim 1 which is:

6-((3R,9aS)-8-{[4-(1H-tetrazol-1-yl)phenyl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-3,4-dihydro-1H-isochromen-1-one;

3-((3R,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

3-((3S,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3S)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3R)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one; 6-methoxy-2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-fluoro-2-methoxy-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile; or

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

or a pharmaceutically acceptable salt thereof.

10. The compound of claim 1 which is;

3-((3R,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

3-((3S,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3S)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3R)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

or a pharmaceutically acceptable salt thereof.

11. A pharmaceutical composition comprised of a compound of claim 1 and a pharmaceutically acceptable carrier.

12. A pharmaceutical composition comprised of a compound of claim 10 and a pharmaceutically acceptable carrier.

13. The pharmaceutical composition of claim 11 further comprising an additional active agent selected from losartan, valsartan, candesartan cilexetil, olmesartan medoximil, telmesartan, eprosartan mesylate, irbesartan, azilsartan medoxomil, amlodipine, alacepril, benazepril, captopril, ceronapril, cilazapril, delapril, enalapril, enalaprilat, fosinopril, imidapril, lisinopril, moveltipril, perindopril, quinapril, ramipril, spirapril, temocapril, or trandolapril, amiloride, spironolactone, epleranone or triamterene, or a pharmaceutically acceptable salt thereof, and optionally hydrochlorothiazide.

14. A method for causing diueresis, natriuresis or both, comprising administering a compound of claim 1 in a therapeutically effective amount to a patient in need thereof.

15. A method for the treatment of hypertension comprising administering a compound of claim 1 in a therapeutically effective amount to a patient in need thereof.

16. A method for the treatment of heart failure comprising administering a compound of claim 1 in a therapeutically effective amount to a patient in need thereof.

17. A method for the treatment of one or more disorders selected from hypertension, acute heart failure, chronic heart failure or pulmonary arterial hypertension, comprising administering a compound of claim 1 in a therapeutically effective amount as appropriate, to a patient in need thereof.

18. The compound of claim 1 which is:

6-((3R,9aS)-8-{[4-(1H-tetrazol-1-yl)phenyl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-3,4-dihydro-1H-isochromen-1-one;

3-((3R,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

3-((3S,9aS)-8-(2-(5-(1H-tetrazol-1-yl)pyridin-2-yl)acetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-methyl-5-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

2-methyl-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3r)-3-methyl-6-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3S)-3-methyl-6-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

4-methyl-5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

5-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

5-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-[(3R,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3S)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3S)-3-methyl-6-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3S)-3-methyl-6-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3R)-3-methyl-6-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2-fluoro-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-5-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-methyl-5-[(3S,9aS)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-[(3R,9aS)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2-methoxy-4-[(3R,9aR)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-chloro-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-chloro-5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-bromo-5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-methoxy-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-methoxy-2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2-methoxy-4-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-fluoro-2-methoxy-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-chloro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-chloro-2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-4-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-4-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

3-methyl-4-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]thiophene-2-carbonitrile;

3-methyl-4-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]thiophene-2-carbonitrile;

3-methyl-4-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]thiophene-2-carbonitrile;

3-methyl-4-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]thiophene-2-carbonitrile;

6-methyl-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-methyl-5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]pyridine-3-carbonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{2-[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]propanoyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2,4-difluoro-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,4-difluoro-5-[(3R,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-methyl-5-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[3-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[3-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-3-[(3S,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3S,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3S,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3R,9aS)-8-{[2-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyridin-4-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyridin-4-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3R,9aS)-3-[3-(1H-tetrazol-1-yl)phenyl]-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3R,9aS)-3-[2-methyl-3-(1H-tetrazol-1-yl)phenyl]-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3R)-3-methyl-6-[(3R,9aS)-3-methyl-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

(3S)-3-methyl-6-[(3R,9aS)-3-methyl-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2,6-difluoro-4-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-4-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-4-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-4-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-6-methoxy-4-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-6-methoxy-4-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-6-methoxy-4-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-6-methoxy-4-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2,6-difluoro-4-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-methyl-5-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aR)-8-{[5-(1H-tetrazol-1-yl)pyrazin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-benzofuran-1(3H)-one;

6-fluoro-3-[(3R,9aR)-8-{[3-methoxy-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-methylbenzonitrile;

2-chloro-6-fluoro-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3S,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[6-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[4-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[4-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[6-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-methyl-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[5-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[5-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-methoxy-2-methyl-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-chloro-6-fluoro-3-[(3R,9aR)-8-{[4-methyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methoxy-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-5-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-5-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-methoxy-4-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

6-fluoro-3-[(3R,9aR)-8-{[5-fluoro-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-methylbenzonitrile;

6-fluoro-3-[(3S,9aR)-8-{[5-fluoro-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-methylbenzonitrile;

6-fluoro-3-[(3R,9aS)-8-{[5-fluoro-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-methylbenzonitrile;

6-fluoro-3-[(3S,9aS)-8-{[5-fluoro-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-2-methylbenzonitrile;

3-[(3S,9aS)-8-{[4,6-dimethyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

3-[(3S,9aR)-8-{[4,6-dimethyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

3-[(3R,9aR)-8-{[4,6-dimethyl-2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

3-[(3S,9aS)-8-{[3-chloro-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

3-[(3R,9aR)-8-{[3-chloro-5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridazin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridazin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

3-[(3R,9aR)-8-{[4-ethyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]-6-fluoro-2-methylbenzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[2-(1H-tetrazol-1-yl)-4-(trifluoromethyl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)-4-(trifluoromethyl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aS)-8-{[5-(5-methyl-1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

4-methyl-5-(2-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl)-2-benzofuran-1(3H)-one;

4-methyl-5-(2-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl)-2-benzofuran-1(3H)-one;

4-methyl-5-(2-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl)-2-benzofuran-1(3H)-one;

4-methyl-5-[(3R,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]thiazin-3-yl]-2-benzofuran-1(3H)-one;

4-methyl-5-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]thiazin-3-yl]-2-benzofuran-1(3H)-one;

4-fluoro-2-methoxy-5-[(3R,9aS)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(7S,10aR)-2-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl]benzonitrile;

6-fluoro-2-methyl-3-[(7R,10aS)-2-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl]benzonitrile;

6-fluoro-2-methyl-3-[(7R,10aR)-2-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl]benzonitrile;

6-fluoro-2-methyl-3-[(7S,10aR)-2-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydro-2H-pyrazino[1,2-d][1,4]oxazepin-7-yl]benzonitrile;

2-fluoro-3,6-dimethyl-5-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

2-fluoro-3,6-dimethyl-5-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3R,9aS)-3-(2,1,3-benzoxadiazol-5-yl)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3S,9aS)-3-(4-methyl-2,1,3-benzoxadiazol-5-yl)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3R,9aS)-3-(4-methyl-2,1,3-benzoxadiazol-5-yl)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3R,9aS)-3-(2,1,3-benzoxadiazol-5-yl)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3R,9aS)-3-(2,1,3-benzoxadiazol-5-yl)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

(3S,9aS)-3-(2, 1,3-benzoxadiazol-5-yl)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazine;

2-cyclopropyl-6-fluoro-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

(3R)-3-methyl-6-(9a-methyl-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-3,4-dihydro-1H-isochromen-1-one;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{2-[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]propanoyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{2-[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]propanoyl}octahydropyrazino[2,1-c][1,4]oxazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]thiazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aS)-8-{[5-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]thiazin-3-yl]benzonitrile;

3-[(3S,9aS)-2,2-dioxido-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydropyrazino[2,1-c][1,4]thiazin-3-yl]-6-fluoro-2-methylbenzonitrile;

3-43S,9aS)-8-(2-(2-(1H-tetrazol-1-yl)pyrimidin-5-yl)-2,2-difluoroacetyl)octahydropyrazino[2,1-c][1,4]oxazin-3-yl)-6-fluoro-2-methylbenzonitrile;

3-((3S,9aR)-8-(2-(2-(1H-tetrazol-1-yl)pyrimidin-5-yl)acetyl)octahydro-1H-pyrazino[1,2-a]pyrazin-3-yl)-6-fluoro-2-methylbenzonitrile;

4-methyl-5-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]-2-benzo furan-1 (314)-one;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3S,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

6-fluoro-2-methyl-3-[(3R,9aR)-8-{[5-(1H-tetrazol-1-yl)pyridin-2-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

(3R)-3-methyl-6-[(3R,9aR)-8-{[6-(1H-tetrazol-1-yl)pyridin-3-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]-3,4-dihydro-1H-isochromen-1-one;

2-fluoro-5-[(3R,9aR)-8-{[2-(1H-tetrazol-1-yl)pyrimidin-5-yl]acetyl}octahydro-2H-pyrazino[1,2-a]pyrazin-3-yl]benzonitrile;

(3R,9aS)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3R,9aR)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3R,9aR)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[5-(1H-tetrazol-1-yl)pyridin-2-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3R,9aS)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[5-(1H-tetrazol-1-yl)pyridin-2-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3R,9aR)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3R,9aS)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3S,9aR)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

(3S,9aS)-3-(3-cyano-4-fluoro-2-methylphenyl)-N-[4-methyl-6-(1H-tetrazol-1-yl)pyridin-3-yl]hexahydropyrazino[2,1-c][1,4]oxazine-8(1H)-carboxamide;

or a pharmaceutically acceptable salt thereof.

Assignments (4)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 29, 2014
From: WALSH, SHAWN
To: MERCK SHARP & DOHME CORP
Reel/Frame 033413/0103 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 12, 2014
From: PIO, BARBARA; PASTERNAK, ALEXANDER; SHAHRIPOUR, AURASH
To: MERCK SHARP & DOHME CORP.
Reel/Frame 033091/0493 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 12, 2014
From: TANG, HAIFENG
To: MERCK SHARP & DOHME CORP.
Reel/Frame 033091/0571 →