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EP0197571A2 Expired / Lapsed EP ⏱️ 0.0 years remaining

Novel derivatives of gamma-cyclodextrin

Assignee: Janssen Pharmaceutica NV
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Filing: 1986-03-04
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Granted: —
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Expires: 2006-03-04
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Abstract

Abstract Novel gamma -cyclodextrin derivatives which are gamma -cyclodextrin substituted with C1-C6 alkyl, hydroxy C1-C6 alkyl, carboxy C1-C6 alkyl or C1-C6 alkyloxycarbonylC1-C6 alkyl or mixed ethers thereof and their preparation. Compositions comprising such cyclodextrin derivatives and an active ingredient which is preferably a drug and the preparation of such compositions.

Inventors

  • 👤 Bernd Willi Werner Müller

Bibliographic Details

Application Number —
Jurisdiction EP
Data Source google_patents
Last Synchronized 2026-11-10 02:20
CPC Classifications
C; C07; C07H; C07H3/00; C07H3/06; B; B82; B82Y; B82Y5/00; A; A61; A61K; A61K47/00; A61K47/50; A61K47/69; A61K47/6949; A61K47/6951; C08; C08B; C08B37/00; C08B37/0006; C08B37/0009; C08B37/0012

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 38 words
A y-cyclodextrin ether or mixed ether wherein the ether substituents are C 1 -C 6 alkyl, hydroxy C 1 -C 6 alkyl, carboxy C 1 -C 6 alkyl or (C 1 -C 6 alkyloxycarbonyl)C 1 -C 6 alkyl.
Claim 2
Dependent Claim 38 words
A y-cyclodextrin ether or mixed ether wherein the ether substituents are C 1 -C 6 alkyl, hydroxy C 1 -C 6 alkyl, carboxy C 1 -C 6 alkyl or (C 1 -C 6 alkyloxycarbonyl)C 1 -C 6 alkyl.
Claim 3
Dependent Claim 35 words
2 . A y-cyclodextrin ether or mixed ether according to claim 1 wherein the ether substituents are C 1 -C 3 alkyl, hydroxy C 2 -C 4 alkyl or carboxy C 1 -C 2 alkyl.
Claim 4
Dependent Claim 20 words
A γ-cyclodextrin derivative according to claim 1, wherein the substituents are methyl, ethyl, isopropyl, hydroxyethyl, hydroxypropyl, hydroxybutyl, carboxymethyl and carboxyethyl.
Claim 5
Dependent Claim 33 words
A y-cyclodextrin derivative according to any of claims 1-3 wherein the degree of substitution is in the range of 0.125 to 3 and the M.S. is in the range of 0.125 to 10.
Claim 6
Dependent Claim 33 words
A y-cyclodextrin derivative according to any of claims 1-3, wherein the degree of substitution is in the range of 0.3 to 2 and the M.S. is in the range of 0.3 to 3.
Claim 7
Dependent Claim 22 words
A process for preparing a compound as defined in any of the claims 1-5, characterized by reacting y-cyclodextrin with an O-alkylating agent.
Claim 8
Dependent Claim 32 words
A process according to claim 6, wherein the process is conducted in a reaction-inert solvent in the presence of a base and at a temperature in the range from 30° to 200°.
Claim 9
Dependent Claim 17 words
A composition comprising an active ingredient and a γ-cyclodextrin derivative as claimed in any of claims 1-5.
Claim 10
Dependent Claim 13 words
A composition according to claim 8, wherein the active ingedient is a drug.
Claim 11
Dependent Claim 42 words
A composition according to claim 9, wherein the drug is a non-steroid anti-rheumatic agent, a steroid, a cardiac glycoside or a derivative of benzodiazepine, benzimidazole, piperidine, piperazine, imidazole, triazole, pyridazine, 1,2,4-triazinedione, 2,3,5,6-tetra- hydroimidazo[2,1-b]thiazole or hydratropic acid, or an amide or trialkylamine derivative.
Claim 12
Dependent Claim 11 words
A composition according to claim 8 wherein the drug is etomidate.
Claim 13
Dependent Claim 11 words
A composition according to claim 8 wherein the drug is ketoconazole.
Claim 14
Dependent Claim 11 words
A composition according to claim 8 wherein the drug is itraconazole.
Claim 15
Dependent Claim 11 words
A composition according to claim 8 wherein the drug is flunarizine.
Claim 16
Independent Claim 38 words
A method of preparing a composition according to anyone of the claims 8-14, characterized in that the y-cyclodextrin ether is dissolved in water and that the active ingredient is added whereafter the thus obtained solution is optionally dried.
Claim 17
Dependent Claim 30 words
A method according to claim 15, wherein the residue after removal of the solvent is pulverized and, optionally after addition of further ingredients, converted into a solid form for administration.
Claim 18
Independent Claim 18 words
A method according to claims 15 or 16, wherein further physiologically acceptable substances are added to the water.
Claim 19
Dependent Claim 24 words
A method according to claim 17, wherein sodium chloride, glucose, mannitol. sorbitol, xylitol or a phosphate or citrate buffer are added to the water.

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