IP Library Granted Patent US 8,716,319
Granted Patent B2
US 8,716,319 · App. 12/702,825 · Granted May 6, 2014

Substituted heterocyclic compounds

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Quick Facts
Patent No.
US 8,716,319
App. No.
12/702,825
Granted
May 6, 2014
Kind
B2
Abstract

The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

Claims (80)

1. A compound selected from the group consisting of:

diethyl 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(thiophen-3-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(thiophen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

5-(3,5-bis(ethoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridin-4-yl)thiophene-2-carboxylic acid,

diethyl 4-(5-ethylthiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzo[b]thiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzo[b]thiophen-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(3-methylbenzo[b]thiophen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(3-methylbenzo[b]thiophen-2-yl)pyridine-3,5-dicarboxylate,

diethyl 4-(5-(4-chlorophenyl)furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(5-(2-(trifluoromethyl)phenyl)furan-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(furan-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-ethylfuran-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzofuran-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 2,6-dimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(5-bromothiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

bis(2-methoxyethyl) 4-(3-bromothiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(5-(4-chlorophenyl)furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(1-(4-fluorophenyl)-5-methyl-1H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(3-(4-fluorophenyl)-1H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

dibenzyl 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

bis(3,4-dimethoxybenzyl) 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-diethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-dipropyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-diisopropyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 1,2,6-trimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2,4-dimethoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-bromophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-cyano-4-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-fluoro-4-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-methoxy-4-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(4-(dimethylamino)-2-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(4-(dimethylamino)-2-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(biphenyl-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and

diethyl 4-(biphenyl-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, or a pharmaceutically acceptable salt thereof.

2. A compound selected from the group consisting of:

diethyl 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(thiophen-3-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(thiophen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

5-(3,5-bis(ethoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridin-4-yl)thiophene-2-carboxylic acid,

diethyl 4-(5-ethylthiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzo[b]thiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzo[b]thiophen-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(3-methylbenzo[b]thiophen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(3-methylbenzo[b]thiophen-2-yl)pyridine-3,5-dicarboxylate,

diethyl 4-(5-(4-chlorophenyl)furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 2,6-dimethyl-4-(5-(2-(trifluoromethyl)phenyl)furan-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(furan-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-ethylfuran-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(benzofuran-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 2,6-dimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(5-bromothiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

bis(2-methoxyethyl) 4-(3-bromothiophen-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(5-(4-chlorophenyl)furan-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(1-(4-fluorophenyl)-5-methyl-1H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diisopropyl 4-(3-(4-fluorophenyl)- 1 H-pyrazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

dibenzyl 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

bis(3,4-dimethoxybenzyl) 2,6-dimethyl-4-(naphthalen-2-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-diethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-dipropyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(5-bromothiophen-2-yl)-2,6-diisopropyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 1,2,6-trimethyl-4-(naphthalen-1-yl)-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2,4-dimethoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-bromophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-cyano-4-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-fluoro-4-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-methoxy-4-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(2-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(4-(dimethylamino)-2-methoxyphenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(4-(dimethylamino)-2-nitrophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate,

diethyl 4-(biphenyl-2-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, and

diethyl 4-(biphenyl-3-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, or a pharmaceutically acceptable salt thereof.

3. A pharmaceutical formulation comprising a compound according to claim 1 or a pharmaceutically acceptable salt or tautomeric form thereof, and at least one pharmaceutically acceptable excipient.

4. A pharmaceutical formulation comprising a compound according to claim 2 or a pharmaceutically acceptable salt or tautomeric form thereof, and at least one pharmaceutically acceptable excipient.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 20, 2014
From: GILEAD PALO ALTO, INC.
To: GILEAD SCIENCES, INC.
Reel/Frame 033151/0406 →
MERGER Recorded Aug 17, 2010
From: APEX MERGER SUB, INC.; CV THERAPEUTICS, INC.
To: GILEAD PALO ALTO, INC.
Reel/Frame 024838/0650 →