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US4007282A Expired / Lapsed US ⏱️ 0.0 years remaining

Lowering lipid and sugar levels in the blood with a bis(4-hydroxyphenyl)alkanoic acid or ester thereof

Assignee: Hoechst AG
•
Filing: 1973-06-07
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Granted: 1977-02-08
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Expires: 1993-06-07
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Abstract

Abstract Pharmaceutical compositions acting on the metabolism which contain as active substance bis(4-hydroxy-phenyl)alkanoic acids corresponding to the formulae I and II ##STR1## wherein R 1 and R 2 wich may be identical or different, each stands for a hydrogen or halogen atom or an alkyl group having 1 to 4 carbon atoms, R 3 stands for a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R 4 stands for hydroxy, alkoxy having 1 to 18 carbon atoms, phenyl-alkoxy having 1 to 4 alkyl carbon atoms, cycloalkoxy having 5 to 8 carbon atoms or a group of the formula ##STR2## in which Z and Z', which may be identical or different, each stands for hydrogen, alkyl of 1 to 18 carbon atoms, phenyl or cycloalkyl of 5 to 8 carbon atoms, or both together with the nitrogen atom may form a heterocyclic ring, R 6 stands for an alkylene radical having 2 to 12 atoms and n stands for zero or an integer of 1 to 6, and process for preparing them.

Inventors

  • 👤 Otto Mauz
  • 👤 Ernold Granzer

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-05 06:56
CPC Classifications
C; C07; C07C; C07C59/00; C07C59/40; C07C59/42; C07C59/52

Claims Analysis

Total Claims: 15
Claim 1
Independent Claim 143 words
A dry pharmaceutical composition for lowering lipid and sugar levels in the blood of a human or animal suffering from hyperlipemia, said composition being in dosage unit form suitable for oral administration and comprising a physiologically acceptable excipient and 0.1 to 1 g of a metabolically active bis(4-hydroxyphenyl) alkanoic acid or ester thereof corresponding to the formula ##STR14## wherein R 1 and R 2 , which are the same or different, are each hydrogen, halogen, or alkyl having 1 to 4 carbon atoms; R 3 is hydrogen or alkyl having 1 to 3 carbon atoms; R 4 is hydroxy, alkoxy having 1 to 8 carbon atoms, phenyl-alkoxy having 1 to 4 alkyl carbon atoms, or cycloalkyl-oxy having 5 to 8 carbon atoms; R 6 is alkylene having 2 to 12 carbon atoms; and n is zero or an integer from 1 to 6.
Claim 2
Dependent Claim 143 words
A dry pharmaceutical composition for lowering lipid and sugar levels in the blood of a human or animal suffering from hyperlipemia, said composition being in dosage unit form suitable for oral administration and comprising a physiologically acceptable excipient and 0.1 to 1 g of a metabolically active bis(4-hydroxyphenyl) alkanoic acid or ester thereof corresponding to the formula ##STR14## wherein R 1 and R 2 , which are the same or different, are each hydrogen, halogen, or alkyl having 1 to 4 carbon atoms; R 3 is hydrogen or alkyl having 1 to 3 carbon atoms; R 4 is hydroxy, alkoxy having 1 to 8 carbon atoms, phenyl-alkoxy having 1 to 4 alkyl carbon atoms, or cycloalkyl-oxy having 5 to 8 carbon atoms; R 6 is alkylene having 2 to 12 carbon atoms; and n is zero or an integer from 1 to 6.
Claim 3
Dependent Claim 16 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid is bis(4'-hydroxy-3',5'-di-tert.butyl-phenyl) ethanoic acid.
Claim 4
Dependent Claim 16 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid is 3,3-bis(4-hydroxy-3'-tert.butyl-phenyl) butanoic acid.
Claim 5
Dependent Claim 16 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid is bis(4'-hydroxy-3'-tert.butyl-phenyl) ethanoic acid.
Claim 6
Dependent Claim 19 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid ester is bis(4'-hydroxy-3'-tert.butyl-phenyl) ethanoic acid n-butyl ester.
Claim 7
Dependent Claim 19 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid ester is 3,3-bis(4'-hydroxy-3'-tert.butyl-phenyl) butanoic acid n-butyl ester.
Claim 8
Dependent Claim 16 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid is 4,4-bis(4'-hydroxy-3'-tert.butyl-phenyl) pentanoic acid.
Claim 9
Dependent Claim 19 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid ester is 4,4-bis(4'-hydroxy-3'-tert.butyl-phenyl) pentanoic acid n-butyl ester.
Claim 10
Dependent Claim 19 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid ester is bis[4,4-bis(4'-hydroxy-3'-tert.butyl-phenyl) pentanoic acid] glycol ester.
Claim 11
Dependent Claim 18 words
The pharmaceutical composition as in claim 1 wherein said bis(4-hydroxy-phenyl) alkanoic acid ester is bis[3,3-bis(4'-hydroxy-3'-tert.butyl-5'-bromophenyl)butanoic acid] glycol ester.
Claim 12
Dependent Claim 20 words
The pharmaceutical composition as in claim 1 which comprises 0.25 to 0.5 g of said active bis(4-hydroxyphenyl)alkanoic acid or ester.
Claim 13
Dependent Claim 13 words
The pharmaceutical composition as in claim 1 in the form of a capsule.
Claim 14
Independent Claim 125 words
A method for lowering lipid and sugar levels in the blood of a human or animal suffering from hyperlipemia, which method comprises orally administering an effective amount of a bis(4-hydroxyphenyl) alkanoic acid or ester thereof corresponding to the formula ##STR15## wherein R 1 and R 2 , which are the same or different, are each hydrogen, halogen, or alkyl having 1 to 4 carbon atoms; R 3 is hydrogen or alkyl having 1 to 3 carbon atoms; R 4 is hydroxy, alkoxy having 1 to 8 carbon atoms, phenyl-alkoxy having 1 to 4 alkyl carbon atoms, or cycloalkyl-oxy having 5 to 8 carbon atoms; R 6 is alkylene having 2 to 12 carbon atoms; and n is zero or an integer from 1 to 6.
Claim 15
Independent Claim 125 words
A method for lowering lipid and sugar levels in the blood of a human or animal suffering from hyperlipemia, which method comprises orally administering an effective amount of a bis(4-hydroxyphenyl) alkanoic acid or ester thereof corresponding to the formula ##STR15## wherein R 1 and R 2 , which are the same or different, are each hydrogen, halogen, or alkyl having 1 to 4 carbon atoms; R 3 is hydrogen or alkyl having 1 to 3 carbon atoms; R 4 is hydroxy, alkoxy having 1 to 8 carbon atoms, phenyl-alkoxy having 1 to 4 alkyl carbon atoms, or cycloalkyl-oxy having 5 to 8 carbon atoms; R 6 is alkylene having 2 to 12 carbon atoms; and n is zero or an integer from 1 to 6.

References Cited (Backward Citations)

US2933520A Cited
US3471554A Cited
US3043746A Cited
US3499008A Cited
GB1047039A Cited
NL6603418A Cited
GB1134337A Cited
US3471537A Cited
US3514472A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1980-02-08 1980-08-09 1981-02-08 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1984-02-08 1984-08-09 1985-02-08 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1988-02-08 1988-08-09 1989-02-08 $7700.00 Window Closed / Lapsed

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