.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

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

DrugPatentWatch Database Preview

Claims for Patent: 4,503,067

« Back to Dashboard

Claims for Patent: 4,503,067

Title: Carbazolyl-(4)-oxypropanolamine compounds and therapeutic compositions
Abstract:Carbazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkanoyl or aroyl; R.sub.2 is hydrogen, lower alkyl or arylalkyl; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen or lower alkyl, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--; X is a valency bond, --CH.sub.2 --, oxygen or sulfur; Ar is mono- or bicyclic aryl or pyridyl; R.sub.5 and R.sub.6 are individually selected from hydrogen, halogen, hydroxyl, lower alkyl, aminocarbonyl, lower alkoxy, aralkyloxy, lower alkylthio, lower alkylsulphinyl or lower alkylsulphonyl; R.sub.5 and R.sub.6 together can represent methylenedioxy; and the salts thereof with physiologically acceptable acids are outstandingly effective in the treatment and prophylaxis of circulatory and cardiac diseases, e.g., hypertension and angina pectoris.
Inventor(s): Wiedemann; Fritz (Weinheim-L/u/ tzelsachsen, DE), Kampe; Wolfgang (Heddesheim, DE), Thiel; Max (Mannheim, DE), Sponer; Gisbert (Hemsbach, DE), Roesch; Egon (Mannheim, DE), Dietmann; Karl (Mannheim-Vogelstang, DE)
Assignee: Boehringer Mannheim GmbH (Mannheim-Waldhof, DE)
Application Number:06/479,921
Patent Claims: 1. Carbazolyl-(4)-oxypropanolamine compound of the formula ##STR9## wherein R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms or aroyl selected from benzoyl and naphthoyl;

R.sub.2 is hydrogen, lower alkyl of up to 6 carbon atoms or arylalkyl selected from benzyl, phenylethyl and phenylpropyl;

R.sub.3 is hydrogen or lower alkyl of up to 6 carbon atoms;

R.sub.4 is hydrogen or lower alkyl of up to 6 carbon atoms, or when X is oxygen, R.sub.4 together with R.sub.5 can represent --CH.sub.2 --O--;

X is a valency bond, --CH.sub.2, oxygen or sulfur;

Ar is selected from phenyl, naphthyl, indanyl and tetrahydronaphthyl;

R.sub.5 and R.sub.6 are individually selected from hydrogen, fluorine, chlorine, bromine, hydroxyl, lower alkyl of up to 6 carbon atoms, a --CONH.sub.2 -- group, lower alkoxy of up to 6 carbon atoms, benzyloxy, lower alkylthio of up to 6 carbon atoms, lower alkylsulphinyl of up to 6 carbon atoms and lower alkylsulphonyl of up to 6 carbon atoms; or

R.sub.5 and R.sub.6 together represent methylenedioxy;

and the salts thereof with physiologically acceptable acids.

2. The compound of claim 1 wherein:

R.sub.1 is hydrogen, lower alkanoyl of up to 6 carbon atoms, or benzoyl;

R.sub.5 and R.sub.6 are individually selected from H, OCH.sub.3, F, CH.sub.3, C(CH.sub.3).sub.3, CONH.sub.2, OH, OC.sub.2 H.sub.5, SCH.sub.3, SOCH.sub.3, OCH.sub.2 C.sub.6 H.sub.5 or

R.sub.5 and R.sub.6 together represent methylenedioxy.

3. The compound of claim 2 wherein

R.sub.1 is H, CHO,COC(CH.sub.3).sub.3, COC.sub.6 H.sub.5, and

R.sub.2 is H or lower alkyl of up to 6 carbons.

4. The compound of claim 2 wherein

R.sub.1 is H; and

X is O.

5. The compound of claim 2 wherein R.sub.5 and R.sub.6 are individually selected from H, OCH.sub.3, OC.sub.2 H.sub.5 and, together with R.sub.4, --CH.sub.2 O--.

6. The compound of claim 5 wherein

R.sub.1 is H;

R.sub.2 is H or CH.sub.3 ;

R.sub.3 is H or CH.sub.3 ;

R.sub.4 is H;

Ar is phenyl;

X is O.

7. The compound of claim 1 wherein:

R.sub.1 is H;

R.sub.2 is H and CH.sub.3 ;

R.sub.3 is H;

R.sub.4 is H;

Ar is phenyl;

X is O

R.sub.5 is H, OCH.sub.3 or OC.sub.2 H.sub.5 ; and

R.sub.6 is H, OCH.sub.3 or OC.sub.2 H.sub.5.

8. The compound as claimed in claim 1 designated 1-[carbazoyl-(4)-oxy]-3-[2-(2-methoxyphenoxy)-ethylamino]-propan-2-ol.

9. The compound as claimed in claim 1 designated 1-[carbazolyl-(4)-oxy]-3-[1,4-benzodioxanyl-(2)-methylamino]-propan-2-ol.

10. The compound as claimed in claim 1 designated 1-[carbazolyl-(4)-oxy]-3-[2-(2-ethoxyphenoxy)-ethylamino]-propan-2-ol.

11. The compound as claimed in claim 1 designated 1-[carbazolyl-(4)-oxy]-3-[N-methyl-2-(2-methoxyphenoxy)-ethylamino]-propan -2-ol.

12. A pharmaceutical composition for the treatment and prophylaxis of hypertension and/or angina pectoris comprising a pharmaceutically acceptable carrier and in therapeutically effective amounts, a carbazolyl-(4)-oxypropanolamine compound as claimed in claim 1.

13. A method of treating a subject for hypertension and/or angina pectoris which comprises administering to such subject a therapeutically effective amount of a carbazolyl-(4)-oxypropanolamine compound as claimed in claim 1.

14. The method as claimed in claim 13 wherein such compound is applied in a prophylactic manner.

15. The method as claimed in claim 13 wherein said disease is hypertension.

16. The method as claimed in claim 13 wherein said disease is angina pectoris.

17. The compound of claim 1 wherein R.sub.2 is hydrogen or lower alkyl of up to 6 carbon atoms.

18. The compound of claim 1 wherein Ar is phenyl.
« Back to Dashboard

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

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.

`abc