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US4710507A Expired / Lapsed US ⏱️ 0.0 years remaining

Quinolone inotropic agents

Assignee: Pfizer Inc
•
Filing: 1984-12-18
•
Granted: 1987-12-01
•
Expires: 2004-12-18
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Abstract

Abstract A heterocyclic-substituted 2-quinolone compound of the formula: <IMAGE> (I) or a pharmaceutically-acceptable salt thereof, wherein "Het" is an optionally substituted 5-or 6-membered monocyclid aromatic heterocyclic group attached by a carbon atom to the 5-, 6-, 7- or 8- position of the quinolone nucleus; R, which is attached to the 5-, 6-, 7- or 8- position, is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylsulphinyl, C1-C4 alkylsulphonyl, halo, CF3, hydroxy, hydroxymethyl, or cyano; R1 is hydrogen, cyano (C1-C4 alkoxy)carbonyl, C1-C4 alkyl, nitro, halo, -NR3R4 or -CONR3R4 where each of R3 and R4 is hydrogen or C1-C4 alkyl or R3 and R4 together with the nitrogen atom to which they are attached form a saturated 5- or 6-membered heterocyclic group optionally containing a further heteroatom or group selected from O, S and N-R5 where R5 is hydrogen or C 1-C4 alkyl; R2 is hydrogen, C1-C4 alkyl, or 2-hydroxyethyl; Y is hydrogen or C1-C4 alkyl; and the dotted line between the 3- and 4- positions represents an optional bond. The compounds are inotropic agents useful as cardiac stimulants in the treatment of congestive heart failure.

Inventors

  • 👤 Simon F. Campbell
  • 👤 David A. Roberts

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-08 06:52
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/14; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/36; C07D213/40; A; A61; A61P; A61P9/00; A61P9/04; C07D215/00; C07D215/02; C07D215/16; C07D215/18; C07D215/20; C07D215/22; C07D215/227; C07D215/24; C07D215/26; C07D215/28; C07D215/48; C07D215/54; C07D401/02; C07D401/04; C07D407/00; C07D407/02; C07D407/04; C07D409/00; C07D409/02; C07D409/04; C07D413/00; C07D413/02; C07D413/04; C07D417/00; C07D417/02; C07D417/04

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 102 words
A heterocyclic-substituted 2-quinolone compound of the formula: ##STR227## or a pharmaceutically-acceptable salt thereof, wherein "Het" is pyridyl or triazolyl, optionally substituted by 1 or 2 substitutents each selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, cyano, amino and carbamoyl, said "Het" group being attached by a carbon atom to the 6-position of the quinolone nucleus; and R, which is attached to the 8-position, is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulphinyl, C 1 -C 4 alkylsulphonyl, halo, CF 3 , hydroxy, hydroxymethyl, or cyano.
Claim 2
Dependent Claim 102 words
A heterocyclic-substituted 2-quinolone compound of the formula: ##STR227## or a pharmaceutically-acceptable salt thereof, wherein "Het" is pyridyl or triazolyl, optionally substituted by 1 or 2 substitutents each selected from C 1 -C 4 alkyl, C 1 -C 4 alkoxy, cyano, amino and carbamoyl, said "Het" group being attached by a carbon atom to the 6-position of the quinolone nucleus; and R, which is attached to the 8-position, is hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, C 1 -C 4 alkylthio, C 1 -C 4 alkylsulphinyl, C 1 -C 4 alkylsulphonyl, halo, CF 3 , hydroxy, hydroxymethyl, or cyano.
Claim 3
Dependent Claim 13 words
A compound as claimed in claim 1, wherein "Het" is 2,6-dimethylpyrid-3-yl or 1-methyl-(H)-1,2,4-triazol-5-yl.
Claim 4
Dependent Claim 11 words
A compound as claimed in claim 2, wherein R is 8-methyl.
Claim 5
Dependent Claim 21 words
A compound as claimed in claim 3, wherein "Het" is 2,6-dimethylpyrid-3-yl and which is in the form of a sodium salt.
Claim 6
Dependent Claim 27 words
A pharmaceutical cardiac composition stimulant comprising a compound as claimed in claim 1, or a pharmaceutically acceptable salt thereof, together with a pharmaceutically acceptable diluent or carrier.
Claim 7
Dependent Claim 41 words
A method for the treatment of congestive heart failure in a patient which comprises administering to the patient a cardiac stimulating effective amount of a compound of the formula (IA) as claimed in claim 1, or a pharmaceutically acceptable salt thereof.

References Cited (Backward Citations)

US3907808A Cited
US3962445A Cited
US3993656A Cited
JPS5473783A Cited
US4258185A Cited
GB2086896A Cited
EP0052016A1 Cited
WO1982001706A1 Cited
EP0102046A1 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1990-11-30 1991-06-01 1991-12-01 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1994-11-30 1995-06-01 1995-12-01 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1998-11-30 1999-06-01 1999-12-01 $7700.00 Window Closed / Lapsed

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