.

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Identify first generic entrants
  • Drug patents in 130+ countries

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving leading biopharmaceutical companies globally:

QuintilesIMS
Julphar
Cipla
Federal Trade Commission
Colorcon
Dow
Daiichi Sankyo
Medtronic
Fuji
AstraZeneca

Generated: November 22, 2017

DrugPatentWatch Database Preview

Details for Patent: ► Subscribe

« Back to Dashboard

Details for Patent: ► Subscribe

Title: Cyclic GMP-specific phosphodiesterase inhibitors
Abstract:A compound having the formula (I) ##STR1## and solvates thereof, wherein: R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl; R.sup.1 represents hydrogen or C.sub.1-6 alkyl; R.sup.2 represents the bicyclic ring ##STR2## which may be optionally substituted by one or more groups selected from halogen and C.sub.1-3 alkyl; and R.sup.3 represents hydrogen or C.sub.1-3 alkyl is disclosed. The compounds are potent and selective inhibitors of cGMP-specific PDE, and are useful in a variety of therapeutic areas where such inhibition is beneficial.
Inventor(s): Daugan; Alain Claude-Marie (Les Ulis, FR), Gellibert; Francoise (Les Ulis, FR)
Assignee: ICOS Corporation (Bothell, WA)
Filing Date:May 15, 1998
Application Number:09/000,192
Claims:1. A compound of formula (I) ##STR11## and solvates thereof, in which: R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl;

R.sup.1 represents hydrogen or C.sub.1-6 alkyl;

R.sup.2 represents the bicyclic ring; ##STR12## and R.sup.3 represents hydrogen or C.sub.1-3 alkyl.

2. A compound according to claim 1 wherein R.sup.0 represents hydrogen.

3. A compound according to claim 1 wherein R.sup.1 is selected from hydrogen, methyl, and iso-propyl.

4. A compound according to claim 1 wherein R.sup.3 represents hydrogen or methyl.

5. (6R,1 2aR)-2,3,6,7,12,12a-Hexahydro-6-(5-benzofuranyl)-2-methyl-pyrazino[2',1':6, 1]pyrido[3,4-b]indole-1,4-dione;

(6R,12aR)-2,3,6,7,12,12a-Hexahydro-6-(5-benzofuranyl)-pyrazino[2',1':6,1]py rido[3,4-b]indole-1,4-dione;

(3S,6R,12aR)-2,3,6,7,12,12a-Hexahydro-6-(5-benzofuranyl)-3-methyl-pyrazino[ 2',1':6,1]pyrido[3,4-b]indole-1,4-dione;

(3S,6R,12aR)-2,3,6,7,12,12a-Hexahydro-6-(5-benzofuranyl)-2,3-dimethyl-pyraz ino[2',1':6,1]pyrido[3,4-b]indole-1,4-dione;

(6R,12aR)-2,3,6,7,12,12a-Hexahydro-6-(5-benzofuranyl)-2-isopropyl-pyrazino[ 2',1':6,1]pyrido[3,4-b]indole-1,4-dione;

and physiologically acceptable solvates thereof.

6. (6R,12aR)-2,3,6,7,12,1 2a-Hexahydro-6-(5-benzofuranyl)-2-methyl-pyrazino[2',1':6,1]pyrido[3,4-b]i ndole-1,4-dione.

7. A process for preparing a compound according to claim 1 ##STR13## comprising hydrogenating a compound of formula (III) ##STR14## in which Alk is defined as above and Cbz represents a carbobenzyloxy group, in the presence of a catalyst in a suitable solvent such as an alcohol, at elevated temperature; optionally followed by

i) an interconversion step; and/or

iii) solvate formation.

8. A pharmaceutical composition comprising a compound according to claim 1, together with a pharmaceutically acceptable diluent or carrier therefor.

9. A process of preparing a pharmaceutical composition comprising a compound according to claim 1, which process comprises mixing said compound together with a pharmaceutically acceptable diluent or carrier therefor.

10. A method of treating conditions where inhibition of cGMP specific PDE is of therapeutic benefit, in a human or non-human animal body, which comprises administering to said body a therapeutically effective amount of a compound according to claim 1.

11. The method of claim 10 wherein the condition is erectile dysfunction.

12. The method of claim 11 wherein the animal body is human.

13. The method of claim 11 wherein the compound is administered orally.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

Serving leading biopharmaceutical companies globally:

Teva
Chinese Patent Office
UBS
Farmers Insurance
Cantor Fitzgerald
Colorcon
Boehringer Ingelheim
AstraZeneca
Argus Health
Merck

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

Copyright 2002-2017 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted
Privacy and Cookies
Terms & Conditions

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot