2-PHENYL SUBSTITUTED IMIDAZOTRIAZINONES AS PHOSPHODIESTERASE INHIBITORS

• US 20100016323A1
• Filed: 09/29/2009
• Published: 01/21/2010
• Est. Priority Date: 11/12/1997
• Status: Active Grant

• Current Assignee: Bayer Intellectual Property GmbH (Bayer AG)
• Original Assignee: Bayer Schering Pharma AG (Bayer AG)
• Inventors: Keldenich, Jörg, Perzborn, Elisabeth, Schlemmer, Karl-Heinz, Es-Sayed, Mazen, Serno, Peter, Dembowsky, Klaus, Haning, Helmut, Schenke, Thomas, Niewöhner, Ulrich, Nowakowski, Marc, Niewöhner, Maria, Bischoff, Erwin
• Granted Patent: US 7,696,206 B2
• Time in Patent Office: Days
• US Class Current: 514/243
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: A61P 13/00 Drugs for disorders of the urinary system
• CPC Class Codes: A61P 13/02 of urine or of the urinary tract, e.g. urine acidifiers
• CPC Class Codes: A61P 13/08 of the prostate
• CPC Class Codes: A61P 13/10 of the bladder
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/06 Antiarrhythmics
• CPC Class Codes: A61P 9/08 Vasodilators for multiple indications
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
• CPC Class Codes: A61P 9/12 Antihypertensives
• CPC Class Codes: C07D 487/04 Ortho-condensed systems
• CPC Class Codes: C07F 9/6561 containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Abstract

The application claims a compound of the formula

• • or a salt, a hydrate, or a hydrate of a salt thereof.

The compounds inhibit cGMP-metabolizing phosphodiesterases and are suitable for use as active compounds in pharmaceuticals, for the treatment of erectile dysfunction.

Claims

1. A compound of the formula:

or a salt, a hydrate, or a hydrate of a salt thereof.

2. The compound according to claim 1 having the chemical name 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one hydrochloride.

3. The compound according to claim 1 having the chemical name 2-[2-ethoxy-5-(4-ethyl-piperazine-1-sulphonyl)-phenyl]-5-methyl-7-propyl-3H-imidazo[5,1-f][1,2,4]triazin-4-one hydrochloride trihydrate.

4. A pharmaceutical composition comprising a compound according to claim 1 and a pharmacologically acceptable formulating agent.

5. A method of treating erectile dysfunction comprising administering to a mammal an effective amount of a compound according to claim 1.

6. The method of treating erectile dysfunction according to claim 5 wherein the mammal is a human.