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1. WO1996039449 - HYDROPHOBIC HETEROATOM-CONTAINING SEQUESTRANT FOR CHOLESTEROL DEPLETION

Publication Number WO/1996/039449
Publication Date 12.12.1996
International Application No. PCT/US1996/009101
International Filing Date 06.06.1996
Chapter 2 Demand Filed 30.12.1996
IPC
A61K 31/785 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
74Synthetic polymeric materials
785Polymers containing nitrogen
C08F 8/44 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
8Chemical modification by after-treatment
44Preparation of metal salts or ammonium salts
C08F 26/02 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
26Homopolymers or copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and at least one being terminated by a single or double bond to nitrogen or by a heterocyclic ring containing nitrogen
02by a single or double bond to nitrogen
CPC
A61K 31/785
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
74Synthetic polymeric materials
785Polymers containing nitrogen
A61K 31/787
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
74Synthetic polymeric materials
785Polymers containing nitrogen
787containing heterocyclic rings having nitrogen as a ring hetero atom
A61P 1/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
16for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
C08F 220/34
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride ester, amide, imide or nitrile thereof
02Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
10Esters
34Esters containing nitrogen ; , e.g. N,N-dimethylaminoethyl (meth)acrylate
Applicants
  • GELTEX PHARMACEUTICALS, INC. [US]/[US] (AllExceptUS)
  • MANDEVILLE, W., Harry, III [US]/[US] (UsOnly)
  • HOLMES-FARLEY, Stephen, Randall [US]/[US] (UsOnly)
  • PETERSEN, John, S. [US]/[US] (UsOnly)
Inventors
  • MANDEVILLE, W., Harry, III
  • HOLMES-FARLEY, Stephen, Randall
  • PETERSEN, John, S.
Agents
  • PIERCE, N., Scott
Priority Data
08/469,65906.06.1995US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) HYDROPHOBIC HETEROATOM-CONTAINING SEQUESTRANT FOR CHOLESTEROL DEPLETION
(FR) AGENT SEQUESTRANT HYDROPHOBE CONTENANT DES HETEROATOMES ET PERMETTANT UNE DEPLETION CHOLESTEROLIQUE
Abstract
(EN)
The present invention relates to a poly(allylamine) polymer and, more generally, a hydrocarbon amine polymer. Preferably, these polymers are cross-linked. The present invention also relates to methods of forming these polymers and methods for their use. Further, the present invention relates to alkylating agents that can be employed to form the polymers and to methods for forming the alkylating agents. Generally, the polymer sequestrant includes a substituent bound to an amine of the polymer. The substituent includes a quaternary amine-containing moiety having one, two or three terminal hydrophobic substituents. A method of preparing quaternary amine-containing alkylating agents includes reacting an unsymmetrical dihalide with a tertiary amine having at least one hydrophobic substituent. A method for binding bile salts of bile acids in a mammal includes orally administering to the mammal a therapeutically-effective amount of the polymer sequestrant.
(FR)
La présente invention se rapporte à un polymère de poly(allylamine) et, de manière plus générale, à un polymère d'amine hydrocarburée. De préférence, ces polymères sont réticulés. La présente invention se rapporte également à des procédés de fabrication de ces polymères et à des procédés d'utilisation de ces polymères. En outre, la présente invention se rapporte à des agents alkylants que l'on peut utiliser pour fabriquer ces polymères et à des procédés de fabrication de ces agents alkylants. De manière générale, l'agent séquestrant polymère comporte un substituant lié à une amine du polymère. Ce substituant comporte une fraction contenant une amine quaternaire pourvue d'un, de deux ou de trois substituants hydrophobes terminaux. Un procédé de préparation des agents alkylants contenant une amine quaternaire consiste à faire réagir un dihalogénure non symétrique avec une amine tertiaire ayant au moins un substituant hydrophobe. Un procédé permettant de lier les sels biliaires des acides biliaires chez un mammifère consiste à administrer oralement audit mammifère une quantité thérapeutiquement efficace de l'agent séquestrant polymère.
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