.

Deeper Knowledge, Faster

  • Plan your formulary budget
  • Predict branded drug patent expiration
  • Drug patents in 130+ countries

► See Plans & Pricing

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

Serving 500+ biopharmaceutical companies globally:

Merck
Farmers Insurance
Novartis
Teva
Cerilliant
US Department of Justice
Mallinckrodt
McKinsey
Cantor Fitzgerald
Fish and Richardson

Generated: July 24, 2017

DrugPatentWatch Database Preview

Claims for Patent: ► Subscribe

« Back to Dashboard

Claims for Patent: ► Subscribe

Title: Phenol ethers
Abstract:The invention provides phenol ethers of the formula: ##STR1## wherein R is branched C.sub.3-4 alkyl, C.sub.3-4 cycloalkyl, branched cyano(C.sub.3-4 alkyl), phenyl(C.sub.2-3 alkyl), halophenyl(C.sub.2-3 alkyl), (C.sub.1-4 alkoxy)phenyl(C.sub.2-4 alkyl), or (C.sub.1-4 acyl)amino(C.sub.1-4 alkyl), alk is C.sub.1-4 alkyl substituted by a 3 to 6 membered cycloalkyl group, X is --O--, --S-- or --SO.sub.2 --; and R.sub.1 is --C.sub.1-4 alkyl- or --C.sub.1-4 alkoxy-, in their racemic and optically active forms, and their addition salts with pharmaceutically acceptable acids. These compounds are useful in therapy as .beta.-adrenergic blocking agents. Intermediates are also provided.
Inventor(s): Manoury; Philippe M. J. (L'Hay les Roses, FR), Cavero; Icilio A. G. (Paris, FR), Najer; Henry (Paris, FR), Giudicelli; Don P. R. L. (Fontenay sous Bois, FR)
Assignee: Synthelabo (Paris, FR)
Application Number:06/020,463
Patent Claims: 1. A compound of the formula ##STR23## wherein cycloalkyl is cyclopropyl, cyclobutyl, cycloamyl or cyclohexyl;

X is --O--, --S-- or --SO.sub.2 --; and

A is hydrogen or methyl; or a pharmaceutically acceptable salt thereof.

2. A compound of claim 1 wherein said cycloalkyl is cyclopropyl.

3. A compound of claim 1 wherein X is --O--.

4. A compound of claim 1 wherein X is --S--.

5. A compound of claim 1 wherein X is --SO.sub.2 --.

6. A compound of claim 2 wherein X is --O--.

7. The compound of claim 5 which is 1-[4-(2-cyclopropylmethylsulfonylethoxy)-phenoxy]-3-isopropylaminopropan-2 -ol or a pharmaceutically acceptable salt thereof.

8. A compound of claim 6 which is 1-[4-(2-cyclobutylmethoxy-ethoxy)-phenoxy]-3-isopropylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.

9. A compound of claim 4 which is 1-[4-(2-cyclopropylmethylthio-ethoxy)-phenoxy]-3-isopropylamino-propan-2-o l or a pharmaceutically acceptable salt thereof.

10. A compound of claim 6 which is 1-[4-(2-cyclopropylmethoxy-ethoxy)-phenoxy]-3-isopropylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.

11. A compound of claim 6 which is 1-[4-(2-cyclopropylmethoxy-ethoxy)-phenoxy]-3-t-butylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.

12. A compound of the formula ##STR24## wherein cycloalkyl is cyclopropyl, cyclobutyl, cycloamyl or cyclohexyl;

X is --O--, --S-- or --SO.sub.2 --; and

A is hydrogen or methyl

or a pharmaceutically acceptable salt thereof.

13. A compound of claim 12 which is 1-[4-(2-cyclobutylmethylsulfonyl-ethyl)-phenoxy]-3-isopropylamino-propan-2 -ol or a pharmaceutically acceptable salt thereof.

14. A compound of claim 12 which is 1-[4-(2-cyclobutylmethoxy-ethyl)-phenoxy]-3-isopropylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.

15. The compound of claim 12 which is 1-[4-(2-cyclobutylmethylthio-ethyl)-phenoxy]-3-isopropylaminopropan-2-ol or a pharmaceutically acceptable salt thereof.

16. A method for the selective blocking of .beta..sub.1 -adrenergic receptors which comprises introducing into the environment of said receptors an effective amount of 1-[4-(2-cyclopropylmethoxy-ethyl)-phenoxy]-3-isopropylamino-propan-2-ol whereby said .beta..sub.1 -andrenergic receptors are blocked.

17. A method for the selective blocking of .beta..sub.1 -adrenergic receptors which comprises introducing into the environment of said receptors an effective amount of a compound of claim 1, 8, 9, 10, 11, or 7, whereby said .beta..sub.1 -adrenergic receptors are blocked.

18. A method for the selective blocking of .beta..sub.1 -adrenergic receptors which comprises introducing into the environment of said receptors an effective amount of a compound of claim 12, 13, 14, or 15, whereby said .beta..sub.1 -adrenergic receptors are blocked.
« Back to Dashboard

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

Serving 500+ biopharmaceutical companies globally:

Cerilliant
Federal Trade Commission
Harvard Business School
Merck
Farmers Insurance
Cantor Fitzgerald
Daiichi Sankyo
Moodys
Covington
UBS

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 Heap | Mobile and Web Analytics

Follow DrugPatentWatch:



Google
Twitter
Google Plus
botpot