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US4252809A Expired / Lapsed US ⏱️ 0.0 years remaining

Substituted pteridine compounds and pharmaceutical compositions containing the same

Assignee: Roehm Pharma GmbH
•
Filing: 1978-07-11
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Granted: 1981-02-24
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Expires: 1998-07-11
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Abstract

Abstract Pharmaceutical compositions having a diuretic effect and containing as the active ingredient a compound of the formula ##STR1## wherein R is hydrogen, a pharmaceutically acceptable cation, methyl, or a hydrophilic group R', are disclosed, as are novel compounds wherein R is R'. This application is a continuation-in-part of application Ser. No. 860,824 filed Dec. 15, 1977, now abandoned.

Inventors

  • 👤 Heinrich Knauf
  • 👤 Ernst Mutschler
  • 👤 Karl-Dieter Voelger

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 17:26
CPC Classifications
C; C07; C07D; C07D475/00; C07D475/06; C07D475/08

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 38 words
A parenterally administrable pharmaceutical composition for inducing diuresis, said composition comprising a pharmaceutically acceptable carrier for parenteral administration and a diuretically-effective amount of a compound of the formula ##STR12## wherein R is hydrogen or a pharmaceutically acceptable cation.
Claim 2
Dependent Claim 38 words
A parenterally administrable pharmaceutical composition for inducing diuresis, said composition comprising a pharmaceutically acceptable carrier for parenteral administration and a diuretically-effective amount of a compound of the formula ##STR12## wherein R is hydrogen or a pharmaceutically acceptable cation.
Claim 3
Dependent Claim 11 words
A composition as in claim 1 wherein said compound is 2,4,7-triamino-6-(p-hydroxyphenyl)-pteridine.
Claim 4
Independent Claim 34 words
The method of inducing diuresis in a patient which comprises parenterally administering to said patient a diuretically-effective amount of a compound of the formula ##STR13## wherein R is hydrogen, or a pharmaceutically acceptable cation.
Claim 5
Independent Claim 34 words
The method of inducing diuresis in a patient which comprises parenterally administering to said patient a diuretically-effective amount of a compound of the formula ##STR13## wherein R is hydrogen, or a pharmaceutically acceptable cation.
Claim 6
Dependent Claim 271 words
A compound of the formula ##STR14## wherein R' is ##STR15## wherein m is 0, 1, 2, or 3, R 1 is hydrogen, methyl, or ethyl, R 2 is hydrogen, --OH, or alkyl having 1 to 4 carbon atoms, Q is oxygen, sulfur, or --NR 3 , where R 3 ═R 1 , or Q together with R 1 , forms an ammonium ion --N(R 1 ) 3 + Z - , where Z is a pharmaceutically acceptable anion, or Q, together with R 1 , is morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl; or ##STR16## wherein n is 0, 1, 2, 3, or 4 and Y is --OH or a pharmaceutically acceptable salt thereof, or --NR 4 R 5 , wherein R 4 and R 5 are the same or different and are hydrogen or straight-chain or branched alkyl having 1 to 4 carbon atoms, or --(O) r --R 6 , wherein r is 0 or 1 and R 6 is alkyl having 1 to 6 carbon atoms, or --(CH 2 ) q --R 7 wherein q is 0, 1, or 2 and R 7 is morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl bound by a carbon atom thereof or, when q is not 0, R 7 can also be --OH, or ##STR17## wherein v, w, and z are the same or different and are 0, 1, or 2 and R 8 is hydrogen or --OH; or ##STR18## wherein s is 0, 1, 2 or 3; or ##STR19## wherein M is hydrogen, a pharmaceutically acceptable cation, chloro-substituted alkyl having 1 to 3 carbon atoms, or --CH 2 --O--Ar, wherein Ar is phenyl or chloro-substituted phenyl.
Claim 7
Dependent Claim 271 words
A compound of the formula ##STR14## wherein R' is ##STR15## wherein m is 0, 1, 2, or 3, R 1 is hydrogen, methyl, or ethyl, R 2 is hydrogen, --OH, or alkyl having 1 to 4 carbon atoms, Q is oxygen, sulfur, or --NR 3 , where R 3 ═R 1 , or Q together with R 1 , forms an ammonium ion --N(R 1 ) 3 + Z - , where Z is a pharmaceutically acceptable anion, or Q, together with R 1 , is morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl; or ##STR16## wherein n is 0, 1, 2, 3, or 4 and Y is --OH or a pharmaceutically acceptable salt thereof, or --NR 4 R 5 , wherein R 4 and R 5 are the same or different and are hydrogen or straight-chain or branched alkyl having 1 to 4 carbon atoms, or --(O) r --R 6 , wherein r is 0 or 1 and R 6 is alkyl having 1 to 6 carbon atoms, or --(CH 2 ) q --R 7 wherein q is 0, 1, or 2 and R 7 is morpholinyl, pyrrolidinyl, piperidinyl, or piperazinyl bound by a carbon atom thereof or, when q is not 0, R 7 can also be --OH, or ##STR17## wherein v, w, and z are the same or different and are 0, 1, or 2 and R 8 is hydrogen or --OH; or ##STR18## wherein s is 0, 1, 2 or 3; or ##STR19## wherein M is hydrogen, a pharmaceutically acceptable cation, chloro-substituted alkyl having 1 to 3 carbon atoms, or --CH 2 --O--Ar, wherein Ar is phenyl or chloro-substituted phenyl.
Claim 8
Dependent Claim 9 words
A compound as in claim 4 which is 2,4,7-triamino-6-(p-acetoxyphenyl)-pteridine.
Claim 9
Dependent Claim 9 words
A compound as in claim 4 which is 2,4,7-triamino-6-(p-succinoylphenyl)-pteridine.
Claim 10
Dependent Claim 9 words
A compound as in claim 4 which is 2,4,7-triamino-6-(adipinoylphenyl)-pteridine.
Claim 11
Dependent Claim 9 words
A compound as in claim 4 which is 2,4,7-triamino-6-(p-2-hydroxyethoxyphenyl)-pteridine.
Claim 12
Dependent Claim 9 words
A compound as in claim 4 which is 2,4,7-triamino-6-(p-2,3-dihydroxypropoxy-phenyl)-pteridine.
Claim 13
Dependent Claim 19 words
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically-effective amount of a compound as in claim 4.
Claim 14
Dependent Claim 11 words
A composition as in claim 10 wherein said compound is 2,4,7-triamino-6-(p-acetoxyphenyl)-pteridine.
Claim 15
Dependent Claim 27 words
The method of inducing diuresis in a patient which comprises orally or parenterally administering to said patient a diuretically-effective amount of a compound as in claim 4.

References Cited (Backward Citations)

US3081230A Cited
US3256283A Cited
US4077957A Cited
US4118492A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-02-24 1984-08-25 1985-02-24 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-02-24 1988-08-25 1989-02-24 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-02-24 1992-08-25 1993-02-24 $7700.00 Window Closed / Lapsed

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