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US4317832A Expired / Lapsed US ⏱️ 0.0 years remaining

Indolyl and methylindolyl substituted aminoalkyl guanidines

Assignee: Individual
•
Filing: 1979-09-05
•
Granted: 1982-03-02
•
Expires: 1999-09-05
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Abstract

Abstract Compounds corresponding to the formula <IMAGE> I are disclosed, wherein Alk represents a C2-C5-alkylene groups optionally substituted by a hydroxy group and Ar represent an optionally substituted phenyl, naphthyl, tetrahydronaphthyl, indanyl or indenyl radical or a monocyclic or condensed bicyclic or tricyclic heterocyclic radical which is optionally substituted, the heterocyclic radical consisting of individual rings having 5 or 6 members and optionally containing from 1 to 4 hetero atoms, and the acid addition salts thereof. A process for producing these compounds is also disclosed. These substituted aminoalkyl guanidines block the beta -receptors of the adrenergic nerve system, and also reduce blood pressure.

Inventors

  • 👤 Karl-Heinz Klingler
  • 👤 Axel Kleemann
  • 👤 Fritz Stroman
  • 👤 Klaus Thiemer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 10:36
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/04; C07D209/08; A; A61; A61P; A61P25/00; A61P25/02; A61P27/00; A61P27/02; C07C; C07C279/00; C07C279/04; C07C279/12; C07D209/56; C07D209/80; C07D209/82; C07D209/88

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 44 words
A substituted aminoalkyl guanidine corresponding to the following formula: ##STR35## wherein Alk represents a C 2 -C 5 -alkylene group or such a group substituted by a hydroxy group and Ar represents indolyl and methyl indolyl or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim 44 words
A substituted aminoalkyl guanidine corresponding to the following formula: ##STR35## wherein Alk represents a C 2 -C 5 -alkylene group or such a group substituted by a hydroxy group and Ar represents indolyl and methyl indolyl or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim 11 words
A compound according to claim 1 wherein Ar is indolyl-(4)-or 2-methylindolyl-(4)-.
Claim 4
Dependent Claim 11 words
A compound according to claim 2 wherein Ar is 2-methyl indolyl-(4)-.
Claim 5
Dependent Claim 10 words
A compound according to claim 3 which is 3-{-[2-methyl-indolyl-(4)-oxy]-2-hydroxypropylamino}-butyl guanidine.
Claim 6
Dependent Claim 10 words
A compound according to claim 3 which is 3-{3-[2-methyl-indolyl-(4)-oxy]-2-hydroxypropylamino}-propyl guanidine.
Claim 7
Dependent Claim 10 words
A compound according to claim 2 which is 3-{3-[indolyl-(4)-oxy]-2-hydroxypropyl-amine}-propyl guanidine.
Claim 8
Dependent Claim 33 words
A medicament suitable for blocking of β-receptors of the adrenergic nerve system which comprises at least one substituted aminoalkyl guanidine as claimed in claim 1, together with at least one pharmacologically acceptable carrier.
Claim 9
Dependent Claim 37 words
A method of blocking the β-receptors of the adrenergic nerve system in a mammal comprising administering to the mammal an effective amount of a compound of claim 1 to block the β-receptors of the adrenergic nerve system.
Claim 10
Dependent Claim 12 words
A method according to claim 8 wherein the compound is administered orally.
Claim 11
Dependent Claim 12 words
A method according to claim 8 wherein the compound is administered intravenously.
Claim 12
Dependent Claim 11 words
A method according to claim 8 wherein Ar is 2-methyl indolyl-(4).
Claim 13
Dependent Claim 12 words
A method according to claim 11 wherein the compound is 3-{3-[2-methyl-indolyl-(4)-oxy]-2-hydroxypropylamino}-butyl guanidine.
Claim 14
Dependent Claim 12 words
A method according to claim 11 wherein the compound is 3-{3-[2-methyl-indolyl-(4)-oxy]-2-hydroxypropylamino}-propyl guanidine.
Claim 15
Dependent Claim 12 words
A method according to claim 11 wherein the compound is 3-{3-[indolyl-(4)-oxy]-2-hydroxypropylamino}-propyl guanidine.

References Cited (Backward Citations)

FR778027A Cited
US3317570A Cited
US3501497A Cited
US3471515A Cited
US3499003A Cited
US3644353A Cited
US3542873A Cited
US3821301A Cited
GB1398918A Cited
US4144340A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-03-01 1985-08-31 1986-03-02 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-03-01 1989-08-31 1990-03-02 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-03-01 1993-08-31 1994-03-02 $7700.00 Window Closed / Lapsed

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