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N-substituted nicotinamide 1-oxide as histamine H2 receptor blockers

Assignee: Sanofi SA
•
Filing: 1983-08-12
•
Granted: 1985-04-30
•
Expires: 2003-08-12
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Abstract

Abstract N-substituted nicotinamide 1-oxide having histamine H2 receptor blocking activity of formula <IMAGE> wherein X is a nitrogen atom or a CH group and Am represents a mono- or disubstituted amino group, a pyrrolidino, morpholino, thiomorpholino, hexamethyleneimino group, or an optionally substituted piperidino or piperazino group; their salts; a process for their preparation; and pharmaceutical compositions containing them as active ingredients.

Inventors

  • 👤 Dino Nisato
  • 👤 Sergio Boveri

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-10 01:07
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/62; C07D213/63; C07D213/64; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/20; C07D211/22; C07D211/36; C07D211/40; C07D211/44; C07D211/46; C07D213/78; C07D213/81; C07D213/82; C07D213/89; C07D295/00; C07D295/04; C07D295/08; C07D295/096; C07D401/00; C07D401/02; C07D401/12

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 208 words
A N-substituted nicotinamide 1-oxide of formula ##STR22## wherein X represents a nitrogen atom or a CH group; Am represents an amino group substituted by lower alkyl, lower alkyl bearing a hydroxy or phenyl group or a cycloalkyl group of from 3 to 6 carbon atoms, or by a radical selected from the group consisting of lower alkenyl, lower alkynyl, phenyl and cycloalkyl of from 3 to 6 carbon atoms; an amino group substituted by two identical or different lower alkenyl or lower alkynyl groups; an amino group substituted by two identical or different (hydroxy)lower alkyl or (lower alkoxy)lower alkyl groups; a lower dialkylamino group; a lower dialkylamino group substituted by a phenyl, cycloalkyl of from 3 to 6 carbon atoms, methoxy or hydroxy group; a pyrrolidino group; a morpholino group; a thiomorpholino group; a hexamethyleneimino group; a piperidino group; a piperidino group substituted by a methyl, hydroxy or hydroxymethyl group or by two methyl groups; a piperazino group substituted in the 4-position by a lower alkyl group or a (hydroxy)lower alkyl group; a piperazino group substituted in the 4-position by a lower alkyl group or a (hydroxy)lower alkyl group and also bearing a methyl group in the 3- and/or 5-position; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim 208 words
A N-substituted nicotinamide 1-oxide of formula ##STR22## wherein X represents a nitrogen atom or a CH group; Am represents an amino group substituted by lower alkyl, lower alkyl bearing a hydroxy or phenyl group or a cycloalkyl group of from 3 to 6 carbon atoms, or by a radical selected from the group consisting of lower alkenyl, lower alkynyl, phenyl and cycloalkyl of from 3 to 6 carbon atoms; an amino group substituted by two identical or different lower alkenyl or lower alkynyl groups; an amino group substituted by two identical or different (hydroxy)lower alkyl or (lower alkoxy)lower alkyl groups; a lower dialkylamino group; a lower dialkylamino group substituted by a phenyl, cycloalkyl of from 3 to 6 carbon atoms, methoxy or hydroxy group; a pyrrolidino group; a morpholino group; a thiomorpholino group; a hexamethyleneimino group; a piperidino group; a piperidino group substituted by a methyl, hydroxy or hydroxymethyl group or by two methyl groups; a piperazino group substituted in the 4-position by a lower alkyl group or a (hydroxy)lower alkyl group; a piperazino group substituted in the 4-position by a lower alkyl group or a (hydroxy)lower alkyl group and also bearing a methyl group in the 3- and/or 5-position; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim 11 words
The N-[3-[3-(3-methylpiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 4
Dependent Claim 11 words
The N-[3-[3-(3-methylpiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 5
Dependent Claim 11 words
The N-[3-[3-(4-methylpiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 6
Dependent Claim 11 words
The N-[3-[3-(4-methylpiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 7
Dependent Claim 11 words
The N-[3-[3-(4-hydroxypiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 8
Dependent Claim 11 words
The N-[3-[3-(4-hydroxypiperidinomethyl)phenoxy]propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 9
Dependent Claim 11 words
The N-[3-(3-hexamethyleneiminomethylphenoxy)propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 10
Dependent Claim 11 words
The N-[3-(3-hexamethyleneiminomethylphenoxy)propyl]-3-pyridinecarboxamide 1-oxide or a pharmaceutically acceptable acid addition salt thereof.
Claim 11
Dependent Claim 37 words
A pharmaceutical composition in dosage unit form having histamine H 2 -blocking action comprising from 10 to 1000 mg of a compound as claimed in one of claims 1 to 5 in admixture with a pharmaceutical carrier.
Claim 12
Dependent Claim 25 words
A composition as claimed in claim 6 comprising from 50 to 500 mg of a compound as claimed in one of claims 1 to 5.

References Cited (Backward Citations)

GB978288A Cited
EP0023578A1 Cited
EP0024510A1 Cited
US4309433A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-04-29 1988-10-29 1989-04-30 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-04-29 1992-10-29 1993-04-30 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-04-29 1996-10-29 1997-04-30 $7700.00 Window Closed / Lapsed

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