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US4717727A Expired / Lapsed US ⏱️ 0.0 years remaining

Esters of pyridine-2,4- and 2,5-dicarboxylic acid as medicaments for the inhibition of proline hydroxylase and lysine hydroxylase

Assignee: Hoechst AG
•
Filing: 1985-08-29
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Granted: 1988-01-05
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Expires: 2005-08-29
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Abstract

Abstract Esters of pyridine-2,4- and -2,5-dicarboxylic acid act as inhibitors of proline hydroxylase and lysine hydroxylase and are suitable as fibrosuppressants and immunosuppressants, in particular for the treatment of disturbances of the metabolism of collagen and collagen-like substances and of the biosynthesis of Cl q .

Inventors

  • 👤 Volkmar Gunzler
  • 👤 Hartmut Hanauske-Abel
  • 👤 Jurgen Mohr
  • 👤 Georg Tschank
  • 👤 Kari Kivirikko
  • 👤 Kari Majamaa
  • 👤 Dietrich Brocks

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-07 18:02
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/60; C07D213/78; C07D213/79; A; A61; A61P; A61P37/00; A61P37/02; A61P37/06; A61P43/00; C07D213/80

Claims Analysis

Total Claims: 18
Claim 1
Independent Claim 92 words
A pharmaceutical preparation for inhibiting proline hydroxylase and lysine hydroxylase and for use as a fibrosuppressant and immunosuppressant which comprises an effective inhibiting or suppressing amount of a compound of the formula I ##STR2## in which R 1 and R 2 , which are identical or different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring and a tolerated pharmaceutical vehicle.
Claim 2
Dependent Claim 92 words
A pharmaceutical preparation for inhibiting proline hydroxylase and lysine hydroxylase and for use as a fibrosuppressant and immunosuppressant which comprises an effective inhibiting or suppressing amount of a compound of the formula I ##STR2## in which R 1 and R 2 , which are identical or different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring and a tolerated pharmaceutical vehicle.
Claim 3
Dependent Claim 18 words
A preparation as claimed in claim 1, in which both R 1 and R 2 are said alkyl.
Claim 4
Dependent Claim 22 words
A preparation as claimed in claim 2, in which R 1 and R 2 are alkyl of 1 to 3 carbon atoms.
Claim 5
Dependent Claim 16 words
A preparation as claimed in claim 3, in which R 1 and R 2 are ethyl.
Claim 6
Dependent Claim 16 words
A preparation as claimed in claim 3, in which R 1 and R 2 are methyl.
Claim 7
Independent Claim 105 words
A method for affecting the metabolism of collagen and collagen-like substances and the biosynthesis of C1 q which comprises administering to a patient suffering from disturbances of the metabolism of collagen and collagen-like substances and of the biosynthesis of C1 q an effective amount of a compound of the formula I ##STR3## in which R 1 and R 2 , which are identical or different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring.
Claim 8
Independent Claim 105 words
A method for affecting the metabolism of collagen and collagen-like substances and the biosynthesis of C1 q which comprises administering to a patient suffering from disturbances of the metabolism of collagen and collagen-like substances and of the biosynthesis of C1 q an effective amount of a compound of the formula I ##STR3## in which R 1 and R 2 , which are identical or different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring.
Claim 9
Dependent Claim 22 words
A method as claimed in claim 6, wherein in the compound of formula I R 1 and R 2 are said alkyl.
Claim 10
Dependent Claim 16 words
A method as claimed in claim 7, wherein said alkyl has 1 to 3 carbon atoms.
Claim 11
Dependent Claim 15 words
A method as claimed in claim 7, wherein R 1 and R 2 are ethyl.
Claim 12
Dependent Claim 15 words
A method as claimed in claim 7, wherein R 1 and R 2 are methyl.
Claim 13
Independent Claim 101 words
A method for inhibiting proline hydroxylase and lysine hydroxylase and for treatment with a fibrosuppressant or immunosuppressant which comprises administering to a patient in need of such treatment an effective inhibiting or suppressing amount of a compound of the formula I ##STR4## in which R 1 and R 2 , which are identical and different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring, together with a tolerated pharmaceutical vehicle.
Claim 14
Independent Claim 101 words
A method for inhibiting proline hydroxylase and lysine hydroxylase and for treatment with a fibrosuppressant or immunosuppressant which comprises administering to a patient in need of such treatment an effective inhibiting or suppressing amount of a compound of the formula I ##STR4## in which R 1 and R 2 , which are identical and different, both are alkyl of 1 to 6 carbon atoms, or one of R 1 and R 2 is hydrogen and the other said alkyl, the group R 2 OCO being bonded in the 4- or 5-position of the pyridine ring, together with a tolerated pharmaceutical vehicle.
Claim 15
Dependent Claim 21 words
A method as claimed in claim 11, in which both R 1 and R 2 of said compounds are said alkyl.
Claim 16
Dependent Claim 23 words
A method as claimed in claim 12, in which both R 1 and R 2 are alkyl of 1 to 3 carbon atoms.
Claim 17
Dependent Claim 16 words
A method as claimed in claim 13, in which R 1 and R 2 are ethyl.
Claim 18
Dependent Claim 16 words
A method as claimed in claim 13, in which R 1 and R 2 are methyl.

References Cited (Backward Citations)

US2809146A Cited
US2852519A Cited
FR2123141A6 Cited
US4457936A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-01-04 1991-07-06 1992-01-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-01-04 1995-07-06 1996-01-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-01-04 1999-07-06 2000-01-05 $7700.00 Window Closed / Lapsed

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