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Last Updated: December 22, 2024

Claims for Patent: 4,258,062


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Summary for Patent: 4,258,062
Title: Phenoxy-amino-propanols
Abstract:New phenoxy-amino-propanols of formula ##STR1## wherein R.sup.1 is alkenyl, alkynyl, alkoxyalkyl or alkenyloxyalkyl with 2-6 C atoms in each case or cycloalkyl with 3-8 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms, aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F and/or Cl or mono-substituted by methylenedioxy, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof, exhibit various pharmacological properties including isoprenaline-antagonism on the heart rate and blood pressure.
Inventor(s): Jonas; Rochus (Darmstadt, DE), Becker; Karl-Heinz (Darmstadt, DE), Enenkel; Hans-Joachim (Darmstadt, DE), Minck; Klaus (Darmstadt, DE), Schliep; Hans-Jochen (Darmstadt, DE)
Assignee: Merck Patent Gesellschaft mit beschrankter Haftung (Darmstadt, DE)
Application Number:06/043,925
Patent Claims: 1. Phenoxy-amino-propanols of the formula ##STR4## wherein R.sup.1 is p-alkoxyalkyl with 2-6 C atoms; and R.sup.2 is alkyl or hydroxyalkyl with 1-6 C atoms in each case, cycloalkyl with 3-8 C atoms or aralkyl or aralkyl wherein the aryl radical is mono- to tri-substituted by alkyl, alkoxy, OH, F, Cl or combinations thereof, with a total of 7-15 C atoms in each case, and the physiologically acceptable acid addition salts thereof.

2. The phenoxy-amino-propanols of claim 1 wherein R.sup.1 is, 2-alkoxyethyl with 3-5 C atoms.

3. The phenoxy-amino-propanols of claim 1 wherein R.sup.2 is alkyl of 1-6 C atoms.

4. The phenoxy-amino-propanols of claim 1 wherein R.sup.2 is tert.-butyl.

5. The phenoxy-amino-propanols of claim 1 wherein R.sup.2 is isopropyl, tert.-butyl, 2-phenylethyl, 1,1-dimethyl-2-phenylethyl or 2-(3,4-dimethoxyphenyl)-ethyl.

6. The phenoxy-amino-propanols of claim 1 wherein R.sup.2 is alkyl with 1-6 C atoms, phenylalkyl with 7-10 C atoms or phenylalkyl wherein phenyl is mono- to tri-substituted by methoxy, with a total of 9-13 C atoms.

7. A pharmaceutical composition which comprises an amount of a compound of claim 1 effective for achieving isoprenaline-antagonism on the heart rate or blood pressure, and a pharmaceutically acceptable adjuvant.

8. A method of achieving isoprenaline antagonism on the heart rate or blood pressure in a mammal, which comprises administering to a mammal an amount of a compound of claim 1 which is effective for achieving isoprenaline-antagonism on the heart rate or blood pressure.

9. 1-(p-2-Isopropoxyethoxymethyl-phenoxy)-3-isopropylamino-propan-2-ol, a compound of claim 1.

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