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US3984436A Expired / Lapsed US ⏱️ 0.0 years remaining

Pyrrolyl compounds and processes for their manufacture

Assignee: Novartis Corp
•
Filing: 1974-02-28
•
Granted: 1976-10-05
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Expires: 1994-02-28
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Abstract

Abstract Pyrrolyl compounds of the formula I ##EQU1## wherein Py is optionally lower-alkylated 1-pyrrolyl, Ph is phenylene, R 1 is hydrogen or lower alkyl and R 2 is hydrogen, lower alkyl, aryl-lower alkyl or optionally functionally modified carboxy-lower alkyl or R 1 and R 2 together are lower alkylene, oxa-lower alkylene, thia-lower alkylene or aza-lower alkylene, their antipodes and salts, which are valuable blockers of adrenergic β-receptors.

Inventors

  • 👤 Knut A. Jaeggi
  • 👤 Franz Ostermayer
  • 👤 Herbert Schroter

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 09:31
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/30; C07D207/32; C07D207/325; A; A61; A61P; A61P25/00; A61P25/02; A61P9/00; A61P9/06; A61P9/08; A61P9/10

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 72 words
Pyrrolyl compounds of the formula I ##EQU2## wherein Py is 1-pyrrolyl or mono- or di-lower alkylated 1-pyrrolyl, Ph is phenylene, R 1 is hydrogen or lower alkyl and R 2 is hydrogen, lower alkyl, phenyl-lower alkyl having up to 10 carbon atoms wherein the phenyl ring is unsubstituted or mono-substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R 1 and R 2 together are lower alkylene, their antipodes and salts.
Claim 2
Dependent Claim 72 words
Pyrrolyl compounds of the formula I ##EQU2## wherein Py is 1-pyrrolyl or mono- or di-lower alkylated 1-pyrrolyl, Ph is phenylene, R 1 is hydrogen or lower alkyl and R 2 is hydrogen, lower alkyl, phenyl-lower alkyl having up to 10 carbon atoms wherein the phenyl ring is unsubstituted or mono-substituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl, or R 1 and R 2 together are lower alkylene, their antipodes and salts.
Claim 3
Dependent Claim 34 words
Pyrrolyl compounds of the formula I Py-Ph-O-CH.sub.2 -CHOH-CH.sub.2 -NH-R.sub.2 (I) wherein Py is 1-pyrrolyl or mono- or di-lower alkylated 1-pyrrolyl, Ph is phenylene and R 2 is lower alkyl, their optical antipodes and salts.
Claim 4
Dependent Claim 34 words
Pyrrolyl compounds of the formula I Py-Ph-O-CH.sub.2 -CHOH-CH.sub.2 -NH-R.sub.2 (I) wherein Py is 1-pyrrolyl or mono- or di-lower alkylated 1-pyrrolyl, Ph is phenylene and R 2 is lower alkyl, their optical antipodes and salts.
Claim 5
Dependent Claim 31 words
A compound as claimed in claim 2 having the formula I wherein Py is 1-pyrrolyl or 2,5-dimethyl-1-pyrrolyl, Ph is phenylene and R 2 is lower alkyl, their optical antipodes and salts.
Claim 6
Dependent Claim 33 words
A compound as claimed in claim 2 having the formula I wherein Py is 1-pyrrolyl or 2,5-dimethyl-1-pyrrolyl, Ph is ortho- or para-phenylene and R 2 is lower alkyl, their optical antipodes and salts.
Claim 7
Dependent Claim 36 words
A compound as claimed in claim 2 having the formula I wherein Py is 1-pyrrolyl or 2,5-dimethyl-1-pyrrolyl, Ph is ortho- or para-phenylene and R 2 is methyl, ethyl, isopropyl or tert.-butyl, their optical antipodes and salts.
Claim 8
Dependent Claim 19 words
A compound as claimed in claim 2 having the formula I which is 1-[4-pyrrolyl-(1)-phenoxy]-2-hydroxy-3-isopropylamino-propane, its optical antipodes and salts.
Claim 9
Dependent Claim 9 words
The hydrochloride salt of the compound of claim 6.
Claim 10
Dependent Claim 19 words
A compound as claimed in claim 2 having the formula I which is 1-[2-pyrrolyl-(1)-phenoxy]-2-hydroxy-3-isopropylamino-propane, its optical antipodes and salts.
Claim 11
Dependent Claim 9 words
The hydrochloride salt of the compound of claim 8.
Claim 12
Dependent Claim 19 words
A compound as claimed in claim 2 having the formula I which is 1-tert.-butylamino-3-[o-pyrrol-1-yl)-phenoxy]-2-propanol, its optical antipodes and salts.
Claim 13
Dependent Claim 10 words
The neutral fumarate salt of the compound of claim 10.
Claim 14
Dependent Claim 19 words
A compound as claimed in claim 9 having the formula I which is 1-[o-(2,5-dimethyl-pyrrol-1-yl)-phenoxy]-3-isopropylamino-2-propanol, its optical antipodes and salts.
Claim 15
Dependent Claim 10 words
The neutral fumarate salt of the compound of claim 2.

References Cited (Backward Citations)

US3328417A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1979-10-05 1980-04-05 1980-10-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1983-10-05 1984-04-05 1984-10-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1987-10-05 1988-04-05 1988-10-05 $7700.00 Window Closed / Lapsed

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