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US4020164A Expired / Lapsed US ⏱️ 0.0 years remaining

Benzomorphan derivatives

Assignee: Bayer Pharma AG
•
Filing: 1975-02-18
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Granted: 1977-04-26
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Expires: 1995-02-18
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Abstract

Abstract Benzomorphans of the formula ##STR1## wherein R 1 is H, CH 3 or C 2 H 5 ; R 2 is CH 3 or C 2 H 5 and R 3 and R 4 , which can be alike or different, each are lower alkyl, and the acid addition salts thereof with physiologically acceptable acids have CNS activity, including analgesic, morphine antagonistic, anti-convulsive, muscle relaxant, sedative and neuroleptic activity.

Inventors

  • 👤 Dieter Rahtz
  • 👤 Eberhard Schroder
  • 👤 Reinhard Horowski
  • 👤 Gert Paschelke
  • 👤 Dieter Palenschat
  • 👤 Helmut Wachtel
  • 👤 Wolfgang Kehr

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 12:59
CPC Classifications
C; C07; C07D; C07D221/00; C07D221/02; C07D221/22; C07D221/26

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 59 words
A benzomorphan of the formula ##STR6## wherein R 1 is H, CH 3 , C 2 H 5 ; R 2 is CH 3 or C 2 H 5 ; and R 3 and R 4 each are alkyl of 1-4 carbon atoms, in free base form or as an acid addition salt thereof with a physiologically acceptable acid.
Claim 2
Dependent Claim 59 words
A benzomorphan of the formula ##STR6## wherein R 1 is H, CH 3 , C 2 H 5 ; R 2 is CH 3 or C 2 H 5 ; and R 3 and R 4 each are alkyl of 1-4 carbon atoms, in free base form or as an acid addition salt thereof with a physiologically acceptable acid.
Claim 3
Dependent Claim 8 words
A hydrochloride acid addition salt of claim 1.
Claim 4
Dependent Claim 9 words
Compounds of claim 1, (±)-2'-hydroxy-2-(2-hydroxy-2-methylpropyl)-5,9-dimethyl-6,7-benzomorphan and the hydrochloride thereof.
Claim 5
Dependent Claim 6 words
The compound of claim 1, (-)-2'-hydroxy-2-(2-hydroxy-2-methylpropyl)-5,9-dimethyl-6,7-benzomorphan.
Claim 6
Dependent Claim 7 words
The compound of claim 1, (±)-5ethyl-2'-hydroxy-2-(2-hydroxy-2-methylpropyl)-9-methyl-6,7-benzomorphan hydrobromide.
Claim 7
Dependent Claim 7 words
The compound of claim 1, (-)-5-ethyl-2'-hydroxy-2-(2-hydroxy-2-methylpropyl)-9-methyl-6,7-benzomorphan hydrobromide.
Claim 8
Dependent Claim 7 words
The compound of claim 1, (±)-9-ethyl-2'-hydroxy-2-(2-hydroxy-2methylpropyl)-5-methyl-6,7-benzomorphan hydrobromide.
Claim 9
Dependent Claim 7 words
The compound of claim 1, (-)-9-ethyl-2'-hydroxy-2(2-hydroxy-2-methylpropyl)-5-methyl-6,7-benzomorphan hydrobromide.
Claim 10
Dependent Claim 7 words
The compound of claim 1, (+)-5-ethyl-2'-hydroxy-2-(2-hydroxypropyl)-9-methyl-6,7-benzomorphan hydrobromide.
Claim 11
Dependent Claim 6 words
The compound of claim 1, (-)-2'-hydroxy-2-(2-hydroxypropyl)-5,9-dimethyl-6,7-benzomorphan.
Claim 12
Dependent Claim 7 words
The compound of claim 1, (±)-2'-hydroxy-2-(2-hydroxybutyl)5,9-dimethyl-6,7-benzomorphan hydrobromide.
Claim 13
Dependent Claim 7 words
The compound of claim 1, (-)-5-ethyl-2'-hydroxy-2-(2-hydroxypropyl)-9-methyl-6,7-benzomorphan hydrobromide.
Claim 14
Dependent Claim 7 words
The compound of claim 1, (+)-5-ethyl-2'-hydroxy-2-(2-hydroxybutyl)-9-methyl-6,7-benzomorphan hydrobromide.
Claim 15
Dependent Claim 7 words
The compound of claim 1, (-)-5-ethyl-2'-hydroxy-2-(2-hydroxybutyl)-9-methyl-6,7-benzomorphane hydrobromide.
Claim 16
Dependent Claim 6 words
The compound of claim 1, (±)-5,9-diethyl-2'-hydroxy-2-(2-hydroxy-2-methylpropyl)-6,7-benzomorphan.
Claim 17
Dependent Claim 6 words
The compound of claim 1, (-)-2'-hydroxy-2-(2-hydroxypropyl)-9-methyl-5-propyl-6,7-benzomorphan.
Claim 18
Dependent Claim 6 words
The compound of claim 1, (-)-2'-hydroxy-2-(2-hydroxypropyl)-5-methyl-9-propyl-6,7-benzomorphan.
Claim 19
Dependent Claim 28 words
A pharmaceutical composition in unit dosage form comprising a non-toxic, analgesic amount per unit dosage of a compound of claim 1 in combination with a pharmaceutically acceptable carrier.

References Cited (Backward Citations)

US3723440A Cited
US3417094A Cited
US3644373A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-04-25 1980-10-25 1981-04-26 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-04-25 1984-10-25 1985-04-26 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-04-25 1988-10-25 1989-04-26 $7700.00 Window Closed / Lapsed

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