IP Library Granted Patent US 8,697,863
Granted Patent B2
US 8,697,863 · App. 13/789,469 · Granted Apr 15, 2014

Fused heterocyclic compounds as ion channel modulators

Inventors: Elfatih Elzein (Fremont, CA); Dmitry Koltun (Foster City, CA); Xiaofen Li (Mountain View, CA); Jeff Zablocki (Los Altos, CA); Chandrasekar Venkataramani (Redwood City, CA)
Assignee: Gilead Sciences, Inc.
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Quick Facts
Patent No.
US 8,697,863
App. No.
13/789,469
Granted
Apr 15, 2014
Kind
B2
Abstract

The present disclosure relates to compounds that are sodium channel inhibitors 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 Z 1 , Z 2 , Z 3 , Z 4 , X, Y, R 2 , R 3 and R 4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Claims (22)

1. A compound selected from the group consisting of:

4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethyl)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one;

4-(pyrimidin-2-ylmethyl)-7-(4-(trifluoromethoxy)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one;

7-(4-chlorophenyl)-4-(pyrimidin-2-ylmethyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one;

7-(4-tert-butylphenyl)-4-(pyrimidin-2-ylmethyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one; and

4-(imidazo[1,2-a]pyridin-2-ylmethyl)-7-(4-(trifluoromethyl)phenyl)-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-one;

or a pharmaceutically acceptable salt thereof.

2. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

3. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

4. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

5. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

6. A compound having the structure:

or a pharmaceutically acceptable salt thereof.

7. A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

8. A method of treating a disease state in a human that is alleviable by treatment with an agent capable of reducing late sodium current, comprising administering to a human in need thereof a therapeutically effective dose of a compound of claim 1 or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein the disease state is selected from the group consisting of atrial arrhythmias, ventricular arrhythmias, heart failure, diastolic heart failure, systolic heart failure, acute heart failure, stable angina, unstable angina, exercise induced angina, congestive heart disease, ischemia, recurrent ischemia, reperfusion injury, myocardial infarction, acute coronary syndrome, peripheral arterial disease, pulmonary hypertension and intermittent claudication.

10. The method of claim 8 , wherein the disease state is diabetes or diabetic peripheral neuropathy.

11. The method of claim 8 , wherein the disease state results in one or more of neuropathic pain, epilepsy, migraine, seizures or paralysis.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 25, 2013
From: CORKEY, BRITTON KENNETH; ELZEIN, ELFATIH; JIANG, ROBERT H.; KALLA, RAO V.; KOLTUN, DMITRY; LI, XIAOFEN; MARTINEZ, RUBEN; PARKHILL, ERIC Q.; PERRY, THAO; ZABLOCKI, JEFF; VENKATARAMANI, CHANDRASEKAR; GRAUPE, MICHAEL; GUERRERO, JUAN
To: GILEAD SCIENCES, INC.
Reel/Frame 031478/0963 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 1, 2013
From: CORKEY, BRITTON KENNETH; ELZEIN, ELFATIH; JIANG, ROBERT H.; KALLA, RAO V.; KOLTUN, DMITRY; LI, XIAOFEN; MARTINEZ, RUBEN; PARKHILL, ERIC Q.; PERRY, THAO; ZABLOCKI, JEFF; VENKATARAMANI, CHANDRASEKAR; GRAUPE, MICHAEL; GUERRERO, JUAN
To: GILEAD SCIENCES, INC.
Reel/Frame 031323/0015 →
Continuity (4)
Continuation 13538847 · Jun 29, 2012
Provisional Application 61503980 · Jul 1, 2011
Provisional Application 61582160 · Dec 30, 2011
Related Publication 20130184255A1 · Jul 18, 2013