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US4452788A Expired / Lapsed US ⏱️ 0.0 years remaining

Substituted 8-phenylxanthines

Assignee: Warner Lambert Co LLC
•
Filing: 1982-04-21
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Granted: 1984-06-05
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Expires: 2002-04-21
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Abstract

Abstract Substituted 8-phenylxanthines and their use as bronchodilators is described. Methods for their preparation and use as well as pharmaceutical compositions containing them are also described.

Inventors

  • 👤 James A. Bristol
  • 👤 Edward W. Badger

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 09:47
CPC Classifications
C; C07; C07D; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/46; C07D239/52; C07D239/54; C07D239/545; A; A61; A61P; A61P11/00; A61P11/08; C07D473/00; C07D473/02; C07D473/04; C07D473/06

Claims Analysis

Total Claims: 17
Claim 1
Independent Claim 265 words
A compound having the structural formula ##STR16## wherein R and R 1 may be the same or different and are hydrogen, alkyl of from one to six carbon atoms, hydroxyalkyl of from two to six carbon atoms, (CH 2 ) 2-4 N(R 3 ) 2 wherein R 3 is alkyl of from one to six carbon atoms, Ph(CH 2 ) 1-3 or CF 3 (CH 21-4; the dashed lines mean that the two substituents may only be in the three or four positions; X is hydrogen, halogen, hydroxy, alkyl of from one to six carbon atoms, or NR 4 R 5 wherein R 4 and R 5 are hydrogen or alkyl of from one to six carbon atoms, Y is NR 6 R 7 wherein R 6 is hydrogen, hydroxyalkyl of from two to six carbon atoms or alkyl of from one to six carbon atoms, R 7 is hydrogen, alkyl of from one to six carbon atoms, or (CH 2 ) 2-6 -NR 8 R 9 wherein R 8 and R 9 are hydrogen, alkyl of from one to six carbon atoms or when taken together form ##STR17## wherein m and n may be the same or different and are 1, 2, or 3 provided that the sum of m and n is an integer of from three to six and Z is a direct bond, O, S--(O) k wherein k is 0, 1, or 2 or N-R 10 wherein R 10 is hydrogen or alkyl of from one to six carbon atoms; or R 6 and R 7 when taken together form ##STR18##
Claim 2
Dependent Claim 265 words
A compound having the structural formula ##STR16## wherein R and R 1 may be the same or different and are hydrogen, alkyl of from one to six carbon atoms, hydroxyalkyl of from two to six carbon atoms, (CH 2 ) 2-4 N(R 3 ) 2 wherein R 3 is alkyl of from one to six carbon atoms, Ph(CH 2 ) 1-3 or CF 3 (CH 21-4; the dashed lines mean that the two substituents may only be in the three or four positions; X is hydrogen, halogen, hydroxy, alkyl of from one to six carbon atoms, or NR 4 R 5 wherein R 4 and R 5 are hydrogen or alkyl of from one to six carbon atoms, Y is NR 6 R 7 wherein R 6 is hydrogen, hydroxyalkyl of from two to six carbon atoms or alkyl of from one to six carbon atoms, R 7 is hydrogen, alkyl of from one to six carbon atoms, or (CH 2 ) 2-6 -NR 8 R 9 wherein R 8 and R 9 are hydrogen, alkyl of from one to six carbon atoms or when taken together form ##STR17## wherein m and n may be the same or different and are 1, 2, or 3 provided that the sum of m and n is an integer of from three to six and Z is a direct bond, O, S--(O) k wherein k is 0, 1, or 2 or N-R 10 wherein R 10 is hydrogen or alkyl of from one to six carbon atoms; or R 6 and R 7 when taken together form ##STR18##
Claim 3
Dependent Claim 14 words
wherein m, n, and z are defined above; and the pharmaceutically acceptable salts thereof.
Claim 4
Dependent Claim 14 words
wherein m, n, and z are defined above; and the pharmaceutically acceptable salts thereof.
Claim 5
Dependent Claim 17 words
The compounds defined in claim 1 having the structural formula ##STR19## and the pharmaceutically acceptable salts thereof.
Claim 6
Dependent Claim 17 words
The compounds defined in claim 1 having the structural formula ##STR20## and the pharmaceutically acceptable salts thereof.
Claim 7
Dependent Claim 16 words
The compound defined in claim 1 having the name 3-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)-N-[2-(dimethylamino)ethyl]benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 8
Dependent Claim 16 words
The compound defined in claim 1 having the name (S)-4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)-N-(2-hydroxypropyl)benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 9
Dependent Claim 16 words
The compound defined in claim 1 having the name 4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)-N-[2-(dimethyamino)ethyl]benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 10
Dependent Claim 16 words
The compound defined in claim 1 having the name 4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)-N-[3-(dimethylamino)propyl]benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 11
Dependent Claim 16 words
The compound defined in claim 1 having the name 1-[[4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)phenyl]sulfonyl]-4-methylpiperazine; and the pharmaceutically acceptable salts thereof.
Claim 12
Dependent Claim 16 words
The compound defined in claim 1 having the name 4-[[4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)phenyl]sulfonyl]morpholine; and the pharmaceutically acceptable salts thereof.
Claim 13
Dependent Claim 16 words
The compound defined in claim 1 having the name 4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 14
Dependent Claim 16 words
The compound defined in claim 1 having the name 4-[[4-(1,3-diethyl-2,3,6,7-tetrahydro-2,6-dioxo-1H-purin-8-yl)phenyl]sulfonyl]thiomorpholine; and the pharmaceutically acceptable salts thereof.
Claim 15
Dependent Claim 16 words
The compound defined in claim 1 having the name N-[2-(dimethylamino)ethyl]-4-(2,3,6,7-tetrahydro-2,6-dioxo-1,3-dipropyl-1H-purin-8-yl)benzenesulfonamide; and the pharmaceutically acceptable salts thereof.
Claim 16
Dependent Claim 28 words
A pharmaceutical composition useful for treating bronchoconstriction comprising a compound as defined in claim 1 and the pharmaceutically acceptable salts thereof in combination with a pharmaceutically acceptable carrier.
Claim 17
Dependent Claim 28 words
A method for treating bronchoconstriction in a mammal which comprises administering a sufficient amount of the pharmaceutical composition defined in claim 13 to a mammal in need thereof.

References Cited (Backward Citations)

GB982079A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1987-06-05 1987-12-05 1988-06-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1991-06-05 1991-12-05 1992-06-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1995-06-05 1995-12-05 1996-06-05 $7700.00 Window Closed / Lapsed

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