US Patent No. 9,045,498

HEXAHYDROPYRANO[3,4-D][1,3]THIAZIN-2-AMINE COMPOUNDS


Patent No. 9,045,498
Issue Date June 02, 2015
Title Hexahydropyrano[3,4-d][1,3]thiazin-2-amine Compounds
Inventorship Michael Aaron Brodney, Newton, MA (US)
Elizabeth Mary Beck, Cambridge, MA (US)
Christopher Ryan Butler, Canton, MA (US)
Jennifer Elizabeth Davoren, Cambridge, MA (US)
Assignee Pfizer Inc., New York, NY (US)

Claim of US Patent No. 9,045,498

1. A compound of Formula I,
wherein
R1 is hydrogen or methyl, wherein said methyl is optionally substituted with one to three substituents independently selected
from halogen or methoxy;

R2 is C1-6 alkyl, —(C(R5)2)m—(C3-6 cycloalkyl), —C(R5)2)m—(C6-10 aryl), —(C(R5)2)m— (5- to 10-membered heteroaryl) or —(C(R5)2)t—OR6; wherein said alkyl, cycloalkyl, aryl or heteroaryl moieties are optionally substituted with one to three substituents independently
selected from halogen, C1-6 alkyl, —CH2F, —CHF2, —CF3, —CN or —OR7;

R3 is —C(R5)2)m—(CN);

R4 is independently selected from halogen, C1-6 alkyl or C1-6 alkoxy; wherein said alkyl or alkoxy is optionally substituted with one to three fluoro;

R5 at each occurrence is independently selected from hydrogen or C1-3 alkyl, wherein said alkyl is optionally substituted with one to three halogen;

R6 is hydrogen, C1-6 alkyl or —C(R5)2)n—(C6-10 aryl), wherein said alkyl and aryl are optionally substituted with one to three substituents independently selected from halogen,
C1-3 alkyl, —CH2F, —CHF2, —CF3, —CN or —OH;

R7 for each occurrence is hydrogen or C1-6 alkyl, wherein said alkyl is optionally substituted with one to three substituents independently selected from halogen or
C1-6 alkoxy;

m at each occurrence is independently 0, 1 or 2;
n at each occurrence is independently is 1 or 2;
t is 1 or 2; and
x is 0, 1, 2 or 3;
or a tautomer thereof or a pharmaceutically acceptable salt of said compound or tautomer.