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US4029795A Expired / Lapsed US ⏱️ 0.0 years remaining

4(2' Isoquinolin-1-one)piperidines

Assignee: Novartis Corp
•
Filing: 1975-07-14
•
Granted: 1977-06-14
•
Expires: 1995-07-14
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Abstract

Abstract 1-(3-Aryloxy-2-hydroxypropyl)-4-(1-oxoisoquinolino)-piperidines, e.g. those of the formula ##STR1## R' = H, alkanoylaminoethenyl, carbamoyl, alkanoyl, CN, alkoxycarbonylamino-lower alkyl, halo, OH, alkanoylamino, alkyl, alkoxy, alkenyl, alkenyloxy R" = H, alkyl, alkoxy, alkenyl, alkenyloxy, R'" = alkanoylamino, NH 2 , NO 2 , alkyl, alkoxy, halo CF 3 , OH 2-alkanoic acid esters and acid addition salts thereof are antihypertensive and antiarrhythmic agents.

Inventors

  • 👤 Kurt Eichenberger
  • 👤 Christian Egli
  • 👤 Hans Kuhnis
  • 👤 Oswald Schier

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 12:22
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/72; C07D213/74

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 91 words
A 1-(3-aryloxy-2-hydroxy- or 2-alkanoyloxy-propyl)-4-(1-oxoisoquinolino)-piperidine compound corresponding to formula ##STR26## wherein R' and R" are hydrogen, lower o-alkyl, lower o-alkenyl, lower o-alkoxy, lower o-alkenyloxy or an o-halogen atom and R' and R" together with the phenyl radical form a β-naphthyl radical, R 2 ' denotes hydrogen or lower alkanoyl, R 3 denotes hydrogen, R 4 , R 5 and R 6 denote hydrogen, R'" denotes hydrogen, lower alkyl, lower alkoxy, halogen, or trifluoromethyl, or a therapeutically useful acid addition salt thereof, wherein said open chain groups have up to 4 carbon atoms.
Claim 2
Dependent Claim 91 words
A 1-(3-aryloxy-2-hydroxy- or 2-alkanoyloxy-propyl)-4-(1-oxoisoquinolino)-piperidine compound corresponding to formula ##STR26## wherein R' and R" are hydrogen, lower o-alkyl, lower o-alkenyl, lower o-alkoxy, lower o-alkenyloxy or an o-halogen atom and R' and R" together with the phenyl radical form a β-naphthyl radical, R 2 ' denotes hydrogen or lower alkanoyl, R 3 denotes hydrogen, R 4 , R 5 and R 6 denote hydrogen, R'" denotes hydrogen, lower alkyl, lower alkoxy, halogen, or trifluoromethyl, or a therapeutically useful acid addition salt thereof, wherein said open chain groups have up to 4 carbon atoms.
Claim 3
Dependent Claim 62 words
A compound as claimed in claim 1, corresponding to formula Ia, wherein R' denotes lower o-alkenyl, lower o-alkenyloxy, lower o-alkyl, or lower o-alkoxy, R" represents hydrogen, R 2 ' denotes acetyl, propionyl, pivaloyl, or hydrogen, R 3 denotes a hydrogen, and R 4 , R 5 , R 6 and R'" each denote hydrogen or a therapeutically useful acid addition salt thereof.
Claim 4
Dependent Claim 58 words
A compound as claimed in claim 1, corresponding to formula Ia, wherein R' denotes o-allyl, o-allyloxy, o-methyl or o-methoxy, R" represents hydrogen, R 2 ' denotes the acetyl, propionyl, pivaloyl, or hydrogen, R 3 denotes a hydrogen, and R 4 , R 5 , R 6 and R'" denote hydrogen, or a therapeutically useful acid addition salt thereof.
Claim 5
Dependent Claim 18 words
A compound as claimed in claim 1 and being 2-{1-[3-(o-Allyloxyphenoxy)-2-hydroxypropyl]-4-piperidyl}-3,4-dihydro-1(2H)-isoquinolinone and a therapeutically useful acid addition salt thereof.
Claim 6
Dependent Claim 18 words
A compound as claimed in claim 1 and being 2-{1-[3-(o-chlorophenoxy)-2-hydroxypropyl]-4-piperidyl}-3,4-dihydro-1(2H)-isoquinolinone and a therapeutically useful acid addition salt thereof.
Claim 7
Dependent Claim 18 words
A compound as claimed in claim 1 and being 2-{1-[3-(o-methoxyphenoxy)-2-pivaloyloxy-propyl]-4-piperidyl}-3,4-dihydro-1(2H)-isoquinolinone and a therapeutically useful acid addition salt thereof.
Claim 8
Dependent Claim 18 words
A compound as claimed in claim 1 and being 2-{1-[3-(o-Tolyloxy)-2-hydroxypropyl]-4-piperidyl}-3,4-dihydro-1(2H)-isoquinolinone and a therapeutically useful acid addition salt thereof.
Claim 9
Dependent Claim 18 words
A compound as claimed in claim 1 and being 2-{1-[3-(o-methoxyphenoxy)-2-hydroxypropyl]-4-piperidyl}-3,4-dihydro-1(2H)-isoquinolinone and a therapeutically useful acid addition salt thereof.
Claim 10
Dependent Claim 21 words
An antihypertensive pharmaceutical composition comprising a therapeutically effective amount of a compound claimed in claim 1, together with a pharmaceutical excipient.

References Cited (Backward Citations)

US3600394A Cited
US3594380A Cited
US3753994A Cited
US3879553A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-06-13 1980-12-13 1981-06-14 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-06-13 1984-12-13 1985-06-14 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-06-13 1988-12-13 1989-06-14 $7700.00 Window Closed / Lapsed

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