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US4340585A Expired / Lapsed US ⏱️ 0.0 years remaining

Salified anionic resin for cholesterol and lipid lowering

Assignee: Alfa Farmaceutici SpA
•
Filing: 1979-12-11
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Granted: 1982-07-20
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Expires: 1999-12-11
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Abstract

Abstract A non-toxic anionic resin selected from resins having a polymeric reticulated skeleton of styrenic or acrylic type, inert to the digestive enzymes, having a molecular weight higher than 1000 and containing ionizable amino groups, resins having a cellulosic reticulated skeleton modified by the introduction of free or substituted amino groups and resins having a polysaccharide reticulated skeleton modified by the introduction of free or substituted amino groups. The resin is capable of binding itself permanently to the biliary acids and is salified with an acid corresponding to the general formula: ##STR1## wherein: R' represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, R represents a chlorine atom or a group selected from p-chlorobenzoyl, p-bromobenzoyl and p-fluorobenzoyl, W represents a group selected from OH, --N(R"')--CH(R")-(CH 2 ) n --COOH and O--CH 2 --COOH wherein n represents a number from 0 to 5, R" represents a hydrogen atom, a benzyl, a phenyl or a phenyl substituted with an OH group, a lower alkyl, a lower alkoxyl or a lower hydroxyalkyl group and R"' represents a hydrogen atom or a lower alkyl.

Inventors

  • 👤 Valerio Borzatta
  • 👤 Manlio Cristofori
  • 👤 Angelo Brazzi

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 11:34
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/74; A61K31/785; A61K47/00; A61K47/50; A61K47/51; A61K47/56; A61K47/58; A61K47/585; A61P; A61P3/00; A61P3/06; C; C08; C08B; C08B15/00; C08B15/05; C08B15/06; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0021

Claims Analysis

Total Claims: 6
Claim 1
Independent Claim 138 words
A non-toxic cholestyramine resin, said resin being capable of binding itself permanently to the biliary acids, said resin being salified with an acid corresponding to the general formula: ##STR3## wherein: R' represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, R represents a chlorine atom or a group selected from the group consisting of p-chlorobenzoyl, p-bromobenzoyl and p-fluorobenzoyl, W represents a group selected from the group consisting of OH, --N(R"')--CH(R")--(CH 2 ) n --COOH and O--CH 2 --COOH wherein n represents a number from 0 to 5, R" represents a hydrogen atom, a benzyl, a phenyl or a phenyl substituted with an OH group, a lower alkyl, a lower alkoxyl or a lower hydroxyalkyl group and R"' represents a hydrogen atom or a lower alkyl.
Claim 2
Dependent Claim 138 words
A non-toxic cholestyramine resin, said resin being capable of binding itself permanently to the biliary acids, said resin being salified with an acid corresponding to the general formula: ##STR3## wherein: R' represents a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, a hydroxyalkyl group having 1 to 3 carbon atoms, R represents a chlorine atom or a group selected from the group consisting of p-chlorobenzoyl, p-bromobenzoyl and p-fluorobenzoyl, W represents a group selected from the group consisting of OH, --N(R"')--CH(R")--(CH 2 ) n --COOH and O--CH 2 --COOH wherein n represents a number from 0 to 5, R" represents a hydrogen atom, a benzyl, a phenyl or a phenyl substituted with an OH group, a lower alkyl, a lower alkoxyl or a lower hydroxyalkyl group and R"' represents a hydrogen atom or a lower alkyl.
Claim 3
Dependent Claim 21 words
The resin according to claim 1 wherein the salification degree is 0.7% to 100% of the exchange capacity of the resin.
Claim 4
Dependent Claim 13 words
The resin according to claim 2 wherein the salifying acid is 2-[4-(p-chlorobenzoylphenoxy]-2-methylpropionic acid.
Claim 5
Dependent Claim 22 words
The resin according to claim 3 is in the form of a polystyrenic resin reticulated with 2% of a divinyl benzene chloride.
Claim 6
Dependent Claim 38 words
A pharmaceutical preparation orally administrable to lower the cholesterol and lipid content in the blood, containing as an active substance the salified resin of any one of claims 1-4 in an effective dosage amount therefor, together with adjuvants.

References Cited (Backward Citations)

GB857194A Cited
GB929391A Cited
GB1099269A Cited
GB1286949A Cited
DE2151510A1 Cited
DE2427924A1 Cited
GB1460515A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1985-07-19 1986-01-18 1986-07-20 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1989-07-19 1990-01-18 1990-07-20 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1993-07-19 1994-01-18 1994-07-20 $7700.00 Window Closed / Lapsed

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