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Indazolyl-(4)-oxypropanolamine compounds and therapeutic compositions

Assignee: Roche Diagnostics GmbH
•
Filing: 1977-04-25
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Granted: 1979-03-06
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Expires: 1997-04-25
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Abstract

Abstract New indazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R 1 is hydrogen or lower alkyl; and R 2 is straight-chain or branched lower alkyl which can be substituted by lower alkylthio; And the pharmacologically compatible salts thereof; are outstandingly effective adrenergic β-receptor inhibitors and useful in the treatment or prevention of a recurrence of cardiac and circulatory diseases.

Inventors

  • 👤 Fritz Wiedemann
  • 👤 Wolfgang Kampe
  • 👤 Max Thiel
  • 👤 Wolfgang Bartsch
  • 👤 Egon Roesch

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 15:55
CPC Classifications
C; C07; C07D; C07D231/00; C07D231/54; C07D231/56; A; A61; A61P; A61P25/00; A61P25/02; A61P9/00

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 37 words
Indazolyl-(4)-oxy-propanolamine compound of the formula: ##STR7## wherein R 1 is hydrogen or lower alkyl and R 2 is straight-chain or branched one lower alkyl which is optionally substituted by lower alkylthio; and the pharmacologically compatible salts thereof.
Claim 2
Dependent Claim 37 words
Indazolyl-(4)-oxy-propanolamine compound of the formula: ##STR7## wherein R 1 is hydrogen or lower alkyl and R 2 is straight-chain or branched one lower alkyl which is optionally substituted by lower alkylthio; and the pharmacologically compatible salts thereof.
Claim 3
Dependent Claim 12 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1 wherein R 1 is hydrogen.
Claim 4
Dependent Claim 19 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1 wherein R 1 is lower alkyl of up to 4 carbon atoms.
Claim 5
Dependent Claim 19 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1 wherein R 2 is lower alkyl of up to 5 carbon atoms.
Claim 6
Dependent Claim 14 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1 wherein R 2 is isopropyl or tert.-butyl.
Claim 7
Dependent Claim 32 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1 wherein R 2 is alkylthioalkyl with up to 3 carbon atoms in the alkylthio moiety and up to 5 carbon atoms in the alkyl moiety.
Claim 8
Dependent Claim 9 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1, namely 1-[indazolyl-(4)-oxy]-3-tert.-butylaminopropan-2-ol.
Claim 9
Dependent Claim 9 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1, namely 1-[6-methyl-indazolyl-(4)-oxy]-3-isopropylaminopropan-2-ol.
Claim 10
Dependent Claim 9 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1, namely 1-[6-methyl-indazolyl-(4)-oxy]-3-tert.-butylaminopropan-2-ol.
Claim 11
Dependent Claim 9 words
Indazolyl-(4)-oxy-propanolamine compound as claimed in claim 1, namely 1-[6-methyl-indazolyl-(4)-oxy]-3-(methylthio-tert.-butylamino)-propan-2-ol
Claim 12
Dependent Claim 33 words
Therapeutic composition for the treatment or prevention of a recurrence of cardiac and circulatory diseases comprising a pharmaceutically acceptable carrier and in therapeutically effective amounts an indazolyl-(4)-oxypropanolamine compound as claimed in claim 1.
Claim 13
Dependent Claim 64 words
Method of combatting or preventing a recurrence of cardiac and circulatory infirmities which method comprises administering to a subject an effective adrenergic β-receptor blocking amount of an indazolyl-(4)-oxypropanolamine compound of the formula ##STR8## wherein R 1 is hydrogen or lower alkyl; and R 2 is straight-chain or branched lower alkyl which can be substituted by one lower alkylthio; and the pharmacologically compatible salts thereof.
Claim 14
Dependent Claim 64 words
Method of combatting or preventing a recurrence of cardiac and circulatory infirmities which method comprises administering to a subject an effective adrenergic β-receptor blocking amount of an indazolyl-(4)-oxypropanolamine compound of the formula ##STR8## wherein R 1 is hydrogen or lower alkyl; and R 2 is straight-chain or branched lower alkyl which can be substituted by one lower alkylthio; and the pharmacologically compatible salts thereof.
Claim 15
Dependent Claim 15 words
Method as claimed in claim 12 wherein said compound is 1-[indazolyl-(4)-oxy]-3-tert.-butylaminopropan-2-ol; 1-[6-methyl-indazolyl-(4)-oxy]-3-isopropylaminopropan-2-ol; 1-[6-methyl-indazolyl-(4)-oxy]-3-tert.-butylaminopropan-2-ol; or 1-[6-methyl-indazolyl-(4)-oxy]-3-(methylthio-tert.-butylamino)-propan-2-ol.
Claim 16
Dependent Claim 25 words
Method as claimed in claim 12 wherein said compound is administered at a dosage of 1 to 40 mg up to four times a day.
Claim 17
Dependent Claim 19 words
Method as claimed in claim 12 wherein said compound is applied orally in dosages of 20 to 40 mg.
Claim 18
Dependent Claim 23 words
Method as claimed in claim 12 wherein said compound is administered intravenously at a dosage of from 1 to 5 mg per dosage.

References Cited (Backward Citations)

US3843678A Cited
US3920691A Cited
US3966761A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1982-03-05 1982-09-04 1983-03-06 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1986-03-05 1986-09-04 1987-03-06 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1990-03-05 1990-09-04 1991-03-06 $7700.00 Window Closed / Lapsed

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