2-thiopyrimidinones

Patent metadata

Field	Value
Publication number	US-9399626-B2
Application number	US-201414299497-A
Country	US
Kind code	B2
Filing date	Jun 9, 2014
Priority date	Nov 11, 2011
Publication date	Jul 26, 2016
Grant date	Jul 26, 2016

Abstract

Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.

First claim

What is claimed:

1. A compound having Formula I

or a pharmaceutically acceptable salt thereof
wherein
R 1 is phenyl and said R 1 is mono-, di-, or tri-substituted independently with hydroxyethoxy, methyl, methoxy, fluoro or chloro; and
R 2 is diaminomethyleneamino(C 2 -C 4 )alkyl, carbamoyl(C 1 -C 4 )alkyl, hydroxy(C 2 -C 4 )alkyl, amino(C 2 -C 4 )alkylcarbamoyl(C 1 -C 4 )alkyl, (C 1 -C 4 )alkylcarbonylamino(C 2 -C 4 )alkyl, amino(C 1 -C 4 ) alkylcarbonylamino(C 2 -C 4 )alkyl, amino(C 3 -C 4 )hydroxyalkyl or amino(C 2 -C 4 )alkyl with the proviso that 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide and N—(2-aminoethyl)-2[6-(2,4-dimethoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin -1(2H)-yl]acetamide or a pharmaceutically acceptable salt of said proviso's compounds are not included.

2. A method of treating cardiovascular conditions comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt of said compound wherein the cardiovascular condition is stroke, primary myocardial infarction, heart failure, congestive heart failure, peripheral arterial disease, pulmonary hypertension, vasculitis or wherein the mammal has unstable angina or has experienced myocardial infarction.

3. A method as recited in claim 2 wherein the cardiovascular condition is heart failure, congestive heart failure, peripheral arterial disease, pulmonary hypertension or vasculitis.

4. A method as recited in claim 2 wherein the mammal has unstable angina or has experienced myocardial infarction.

5. A pharmaceutical composition which comprises a therapeutically effective amount of a compound of claim 1 or a pharmaceutically acceptable salt of said compound and a pharmaceutically acceptable carrier, vehicle or diluent.

6. A pharmaceutical combination composition comprising: a therapeutically effective amount of a composition comprising:
a first compound, said first compound being a compound of claim 1 , or a pharmaceutically acceptable salt of said compound;
a second compound, said second compound being an angiotensin converting enzyme inhibitor, a HMG-CoA reductase inhibitor, a non-steroidal anti-inflammatory agent, a Factor Xa inhibitor or warfarin; and
a pharmaceutical carrier, vehicle or diluents.

Assignees

• Pfizer

Inventors

• Carpino Philip A
• Conn Edward L
• Dow Robert L
• Dowling Matthew S
• Hepworth David
• Kung Daniel Wei-Shung
• Orr Suvi
• Rocke Benjamin N
• Ruggeri Roger B
• Sammons Matthew F
• Warmus Joseph S
• Zhang Yan

Classifications

• A61P9/10

  for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title

• A61P9/12

  Antihypertensives · CPC title

• A61P13/12

  of the kidneys · CPC title