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US5124326A Expired / Lapsed US ⏱️ 0.0 years remaining

Pharmaceutically efficacious pteridine derivatives

Assignee: Roehm GmbH Darmstadt
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Filing: 1990-04-20
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Granted: 1992-06-23
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Expires: 2010-04-20
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Abstract

Abstract A pharmaceutically efficacious pteridine compound of formula I: ##STR1## wherein A denote a bridging hydrocarbon group containing 1 to 8 carbon atoms and containing a ##STR2## group directly bonded to the phenyl group and one of the methylene radicals of the bridging A group is optionally replaced by --O--; R 1 is hydrogen, a cycloalkyl group with up to 7 carbon ring atoms, or an alkyl group having 1 to 6 carbon atoms, benzyl, or aryl; R 2 is hydrogen or an alkyl group having 1 to 6 carbon atoms, or wherein R 1 and R 2 together form a five- or six-membered heterocyclic group which optionally contains additional hetero atoms selected from the group consisting of nitrogen, oxygen, and sulfur; R 3 is hydrogen or an alkyl group having 1 to 3 carbon atoms; R 3 ' is hydrogen, an optionally substituted alkyl group having 1 to 3 carbon atoms, carboxyl, hydroxyl or R 3 and R 3 ' together with the carbon atom to which they are attached form a cycloalkyl group and the pharmaceutically acceptable acid addition salts thereof.

Inventors

  • 👤 Ernst Mutschler
  • 👤 Angelika Christner
  • 👤 Ingrid Hofmann

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-25 14:12
CPC Classifications
C; C07; C07D; C07D475/00; C07D475/06; C07D475/08; A; A61; A61P; A61P7/00; A61P7/10; A61P9/00; A61P9/06

Claims Analysis

Total Claims: 7
Claim 1
Independent Claim 223 words
A pharmaceutically efficacious pteridine compound of formula I ##STR15## wherein A is cycloalkyl or --CR 3 R' 3 --(CR 3 R 4 ) n --, said --CR 3 R' 3 -- moiety of said group A being directly bonded to the phenyl group of pteridine nucleus; R 1 is hydrogen, a cycloalkyl group of up to 7 carbon ring atoms, an alkyl group of 1 to 6 carbon atoms or benzyl, R 2 is hydrogen or an alkyl group of 1 to 6 carbon atoms, or R 1 and R 2 , together with the nitrogen atom to which they are attached, form ##STR16## wherein Y is >CHR 7 , --O-- or >NR 8 R 6 is hydrogen or alkyl of 1 to 4 carbon atoms, R 7 and R 8 are hydrogen, alkyl of 1 to 6 carbon atoms or benzyl; R 3 is hydrogen or an alkyl group of 1 to 3 carbon atoms; R 3 ' is hydrogen, an alkyl group of 1 to 3 carbon atoms, an alkyl group of 1 to 3 carbon atoms substituted with an OH group or an amino group, a carboxyl group or a hydroxyl group; and R 4 is hydrogen, C 1-4 alkyl, OH or C 1-4 alkoxy; n is 0 or 1 to 7; or a pharmaceutically acceptable acid addition salt thereof.
Claim 2
Dependent Claim 223 words
A pharmaceutically efficacious pteridine compound of formula I ##STR15## wherein A is cycloalkyl or --CR 3 R' 3 --(CR 3 R 4 ) n --, said --CR 3 R' 3 -- moiety of said group A being directly bonded to the phenyl group of pteridine nucleus; R 1 is hydrogen, a cycloalkyl group of up to 7 carbon ring atoms, an alkyl group of 1 to 6 carbon atoms or benzyl, R 2 is hydrogen or an alkyl group of 1 to 6 carbon atoms, or R 1 and R 2 , together with the nitrogen atom to which they are attached, form ##STR16## wherein Y is >CHR 7 , --O-- or >NR 8 R 6 is hydrogen or alkyl of 1 to 4 carbon atoms, R 7 and R 8 are hydrogen, alkyl of 1 to 6 carbon atoms or benzyl; R 3 is hydrogen or an alkyl group of 1 to 3 carbon atoms; R 3 ' is hydrogen, an alkyl group of 1 to 3 carbon atoms, an alkyl group of 1 to 3 carbon atoms substituted with an OH group or an amino group, a carboxyl group or a hydroxyl group; and R 4 is hydrogen, C 1-4 alkyl, OH or C 1-4 alkoxy; n is 0 or 1 to 7; or a pharmaceutically acceptable acid addition salt thereof.
Claim 3
Dependent Claim 22 words
The compound of claim 1, wherein said salt is an acetate, hydrochloride, hydrobromide, sulfate, citrate, tartrate, succiinate, maleinate, fumarate, lactate or benzoate.
Claim 4
Dependent Claim 34 words
The compound of claim 1, wherein A is --CH 2 --, --CH(OH)--(CH 2 ) n -- or --C(CH 3 ) 2 --(CH 2 ) n --, wherein n is 0 or 1 to 7.
Claim 5
Dependent Claim 21 words
A pharmaceutical composition comprising a pharmaceutically effective amount of the compound of claim 1 in combination with a pharmaceutically effective carrier.
Claim 6
Dependent Claim 34 words
A method of achieving an anti-arrhythmic, cardioprotective, antihypertensive, anti-potassium uretic or diuretic efficacy effect, comprising: administering a therapeutically effective amount of the composition of claim 4 to a subject in need of such effect.
Claim 7
Dependent Claim 20 words
The method of claim 5, wherein the dose of active agent ranges from 1 to 100 mg/kg of body weight.

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USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1995-06-23 1995-12-23 1996-06-23 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1999-06-23 1999-12-23 2000-06-23 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2003-06-23 2003-12-23 2004-06-23 $7700.00 Window Closed / Lapsed

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