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US4548820A Expired / Lapsed US ⏱️ 0.0 years remaining

Xanthine compounds

Assignee: Institut Servier de Medecine Translationnelle SARL
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Filing: 1983-07-25
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Granted: 1985-10-22
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Expires: 2003-07-25
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Abstract

Abstract New xanthine compounds of the formula: <IMAGE> in which: R1 is hydrogen or alkyl from C1 to C5 inclusive; R2 is a hydrocarbon radical up to C6 having optionally a double bond, phenyl or benzyl; R3 is hydrogen, alkyl, hydroxyalkyl or dihydroxyalkyl each from C1 to C5 R4 represents: <IMAGE> in which: Y is hydrogen, halogen, alkyl or alkoxy from C1 to C5 or hydroxyl; Z is methylene or a straight or branched hydrocarbon radical from C2 to C5 optionally substituted by hydroxyl; and A is an amino group of the formula: <IMAGE> p being 2 or 3; <IMAGE> in which q is 1 or 2, and X is a single bond, oxygen or <IMAGE> in which R5 is hydrogen, alkyl or alkylene up to C5, or <IMAGE> in which m is an integer from 2 to 6 and R6 is alkyl from C1 to C5. These new compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of all diseases where it is necessary to inhibit the antigenic antibody reactions.

Inventors

  • 👤 Gilbert Regnier
  • 👤 Claude Guillonneau
  • 👤 Jacques Duhault
  • 👤 Michelle Boulanger

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-26 18:11
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; A61P37/00; A61P37/08; A61P43/00; C07D473/00; C07D473/02; C07D473/04; C07D473/06; C07D473/08; C07D473/10; C07D473/12

Claims Analysis

Total Claims: 14
Claim 1
Independent Claim 282 words
A compound selected from the group consisting of: xanthine compounds of the formula I: ##STR36## in which: R 1 is selected from the group consisting of: hydrogen, and straight and branched alkyl having from 1 to 5 carbon atoms inclusive; R 2 is selected from the group consisting of straight and branched hydrocarbon radicals having up to 6 carbon atoms inclusive, and these radicals having a double bond, phenyl, and benzyl; R 3 is selected from the group consisting of hydrogen and alkyl, hydroxy alkyl and dihydroxyalkyl each having from 1 to 5 carbon atoms inclusive; R 4 is selected from the group consisting of the group of the formula; ##STR37## in which Y is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy each having from 1 to 5 carbon atoms inclusive, and hydroxyl; Z is selected from the group consisting of methylene and hydrocarbon radicals having from 2 to 5 carbon atoms and these hydrocarbon radicals substituted by hydroxyl, and A is selected from the group consisting of the amino residues of the formula: ##STR38## in which p is selected from the integers 2 and 3, ##STR39## in which q is selected from the integers 1 and 2, and X is selected from the group consisting of a double bond oxygen and ##STR40## in which R 5 is selected from the group consisting of hydrogen and alkyl and alkoxy each having from 1 to 5 carbon atoms inclusive; and ##STR41## in which m is selected from the integers from 2 to 6; and R 6 is selected from the group consisting of alkyls having from 1 to 5 carbon atoms inclusive; and physiologically tolerable acid addition salts thereof.
Claim 2
Dependent Claim 282 words
A compound selected from the group consisting of: xanthine compounds of the formula I: ##STR36## in which: R 1 is selected from the group consisting of: hydrogen, and straight and branched alkyl having from 1 to 5 carbon atoms inclusive; R 2 is selected from the group consisting of straight and branched hydrocarbon radicals having up to 6 carbon atoms inclusive, and these radicals having a double bond, phenyl, and benzyl; R 3 is selected from the group consisting of hydrogen and alkyl, hydroxy alkyl and dihydroxyalkyl each having from 1 to 5 carbon atoms inclusive; R 4 is selected from the group consisting of the group of the formula; ##STR37## in which Y is selected from the group consisting of hydrogen, halogen, alkyl and alkoxy each having from 1 to 5 carbon atoms inclusive, and hydroxyl; Z is selected from the group consisting of methylene and hydrocarbon radicals having from 2 to 5 carbon atoms and these hydrocarbon radicals substituted by hydroxyl, and A is selected from the group consisting of the amino residues of the formula: ##STR38## in which p is selected from the integers 2 and 3, ##STR39## in which q is selected from the integers 1 and 2, and X is selected from the group consisting of a double bond oxygen and ##STR40## in which R 5 is selected from the group consisting of hydrogen and alkyl and alkoxy each having from 1 to 5 carbon atoms inclusive; and ##STR41## in which m is selected from the integers from 2 to 6; and R 6 is selected from the group consisting of alkyls having from 1 to 5 carbon atoms inclusive; and physiologically tolerable acid addition salts thereof.
Claim 3
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-8[2-(4-diphenylmethylpiperazinyl)ethyl]xanthine.
Claim 4
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-8-[3-(4-diphenylmethylpiperazinyl)propyl]xanthine.
Claim 5
Dependent Claim 8 words
A compound of claim 1 which is 1,7-dimethyl-3-isobutyl-8-[3-(4-diphenylmethylpiperazinyl)propyl]xanthine.
Claim 6
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-8-[2-(4-diphenylmethylpiperazinyl)ethyl]xanthine.
Claim 7
Dependent Claim 8 words
A compound of claim 1 which is 1,7-dimethyl-3-isobutyl-8-[3-(4-di[parafluorophenyl]methylpiperazinyl)propyl]xanthine.
Claim 8
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-8-[2-(4-diphenylmethylpiperidine)ethyl]xanthine.
Claim 9
Dependent Claim 8 words
A compound of claim 1 which is 1,7-dimethyl-3-isobutyl-8-[3-(4-diphenylmethylpiperidino)propyl]xanthine.
Claim 10
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-8-[2-(4-di[para-fluorophenyl]methylpiperazinyl)ethyl]xanthine.
Claim 11
Dependent Claim 8 words
A compound of claim 1 which is 3-isobutyl-8-[2-(4-diphenylmethylpiperazinyl)ethyl]xanthine.
Claim 12
Dependent Claim 8 words
A compound of claim 1 which is 1-methyl-3-isobutyl-7-(2,3-dihydroxypropyl)-8-[2-(4-diphenylmethylpiperazinyl)ethyl]xanthine.
Claim 13
Dependent Claim 29 words
A pharmaceutical composition suitable for use for its broncho-dilating, anti-allergic and phosphodiesterase inhibiting properties, containing as active ingredient a compound of claim 1, together with a suitable pharmaceutical carrier.
Claim 14
Dependent Claim 49 words
A method for treating a living animal body afflicted with a disease where it is necessary to inhibit the antigenic-antibody reactions comprising the step of administering to the said living animal an amount of a compound of claim 1 which is effective for the alleviation of the said condition.

References Cited (Backward Citations)

US4493837A Cited
US4426383A Cited
US4416878A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1988-10-21 1989-04-22 1989-10-22 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1992-10-21 1993-04-22 1993-10-22 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1996-10-21 1997-04-22 1997-10-22 $7700.00 Window Closed / Lapsed

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