EP0009609A2
Expired / Lapsed
EP
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Adjuvant for promoting absorption of therapeutically active substances through the digestive tract, pharmaceutical composition comprising said adjuvant and process for preparing said pharmaceutical composition; enamine derivatives
Assignee: Kyoto Pharmaceutical Industries Ltd
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Filing: 1979-08-24
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Granted: —
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Expires: 1999-08-24
Abstract
Abstract An adjuvant for promoting absorption of therapeutically active substances through the digestive tract having the formula <CHEM> and pharmaceutical compositions comprising said adjuvant in combination with a therapeutically active substane together with a process for preparing said pharmaceutical composition. The adjuvant is able to effectively elevate the concentration of such active substances in the blood stream even when said active substances are usually absorbable through the digestive tract only with considerable difficulty.
Inventors
- 👤 Kamada Akira
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-04 11:00
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026; A; A61; A61K; A61K47/00; A61K47/06; A61K47/16; A61K47/18; A61K47/183; A61K9/00; A61K9/02; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16; C07D307/00; C07D307/02; C07D307/34; C07D307/56; C07D307/58; A61K38/00; A61K9/0012; A61K9/0031; A61K9/48; A61K9/4841; A61K9/4858; Y; Y10; Y10S; Y10S424/00; Y10S424/15
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
204 words
An adjuvant for promoting absorption of therapeutically active substances through the digestive tract, which comprises one or more enamine derivatives having the general formula wherein R 1 -N-R 2 is the residue of an organic amino- carboxylic acid or organic aminosulfonic acid with a hydrogen atom removed from the amino group thereof, the carboxyl or sulfo group in said residue being optionally in the form of an alkali metal salt or ester; R 1 and R 2 may as taken together form a ring structure; R 3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; R 4 is a hydrogen atom, a lower alkyl group or a lower alkoxycarbonyl group; R 5 is a lower alkyl group; a lower alkoxy group which may optionally be substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; or a lower alkylamino group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; with the proviso that when R 3 and R 4 are both lower alkyl groups, the two may as taken together form a carbocyclic group; and that when R 4 is a lower alkyl group and R 3 is a lower alkoxy group, the two may as taken together form an oxygen-containing ring.
Claim 2
Dependent Claim
204 words
An adjuvant for promoting absorption of therapeutically active substances through the digestive tract, which comprises one or more enamine derivatives having the general formula wherein R 1 -N-R 2 is the residue of an organic amino- carboxylic acid or organic aminosulfonic acid with a hydrogen atom removed from the amino group thereof, the carboxyl or sulfo group in said residue being optionally in the form of an alkali metal salt or ester; R 1 and R 2 may as taken together form a ring structure; R 3 is a hydrogen atom, a lower alkyl group or a lower alkoxy group; R 4 is a hydrogen atom, a lower alkyl group or a lower alkoxycarbonyl group; R 5 is a lower alkyl group; a lower alkoxy group which may optionally be substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; or a lower alkylamino group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; with the proviso that when R 3 and R 4 are both lower alkyl groups, the two may as taken together form a carbocyclic group; and that when R 4 is a lower alkyl group and R 3 is a lower alkoxy group, the two may as taken together form an oxygen-containing ring.
Claim 3
Dependent Claim
29 words
The adjuvant according to claim 1, wherein R 1 -N-R 2 is the residue of an organic amino-carboxylic acid with a hydrogen atom removed from the amino group thereof.
Claim 4
Dependent Claim
14 words
The adjuvant according to claim 1, wherein R 3 is a lower alkyl group.
Claim 5
Dependent Claim
11 words
The adjuvant according to claim 3, wherein R 3 is methyl.
Claim 6
Dependent Claim
13 words
The adjuvant according to claim 1, wherein R 4 is a hydrogen atom.
Claim 7
Dependent Claim
14 words
The adjuvant according to claim 1, wherein R 5 is ethoxy, 1-ethoxycarbonylethoxy or 1-glyceryl.
Claim 8
Dependent Claim
27 words
A pharmaceutical composition for absorption through the digestive tract, which comprises a therapeutically active substance and an enamine derivative according to any of claims 1 to 6.
Claim 9
Dependent Claim
15 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N-(1-methyl-2-ethoxycarbonylvinyl)glycine sodium salt.
Claim 10
Dependent Claim
15 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative in N-(1-methyl-2-ethoxycarbonylvinyl)-L-leucine sodium salt.
Claim 11
Dependent Claim
15 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N-(1-methyl-2-ethoxycarbonylvinyl)-L-phenylglycine sodium salt.
Claim 12
Dependent Claim
15 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N-(1-methyl-2-ethoxycarbonylvinyl)-DL-phenylglycine sodium salt.
Claim 13
Dependent Claim
16 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N,N'-bis(1-methyl-2- ethoxycarbonylvinyl)-L-lysine sodium salt.
Claim 14
Dependent Claim
15 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N-[1-methyl-2-(2,3-dihydroxypropoxycarbonyl)vinyljglycine sodium salt.
Claim 15
Dependent Claim
16 words
The pharmaceutical composition according to claim 7, wherein said enamine derivative is N-[1-methyl-2-(1- ethoxycarbonyl-ethoxycarbonyl)vinyl]glycine sodium salt.
Claim 16
Dependent Claim
14 words
The pharmaceutical composition according to claim 7, wherein said therapeutically active substance is insulin.
Claim 17
Dependent Claim
16 words
The pharmaceutical composition according to claim 7, wherein said therapeutically active substance is a B-lactam antibiotic.
Claim 18
Dependent Claim
16 words
The pharmaceutical composition according to claim 7, characterized in that it is formulated for rectal administration.
Claim 19
Dependent Claim
99 words
A compound of the formula wherein R 1 -N-R 2 is the residue of an organic aminocarboxylic acid or organic aminosulfonic acid with a hydrogen atom removed from the amino group thereof, the carboxyl or sulfe group in said residue being optionally in the form of an alkali metal salt or ester; R 1 and R 2 may as taken together form a ring structure; R' 5 is a lower alkyl group; a lower alkoxy group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; or a lower alkylamino group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl.
Claim 20
Dependent Claim
99 words
A compound of the formula wherein R 1 -N-R 2 is the residue of an organic aminocarboxylic acid or organic aminosulfonic acid with a hydrogen atom removed from the amino group thereof, the carboxyl or sulfe group in said residue being optionally in the form of an alkali metal salt or ester; R 1 and R 2 may as taken together form a ring structure; R' 5 is a lower alkyl group; a lower alkoxy group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl; or a lower alkylamino group which is substituted by hydroxyl, carboxyl or lower alkoxycarbonyl.
Claim 21
Dependent Claim
29 words
A process for preparing the pharmaceutical composition according to claim 7, which comprises mixing a therapeutically active substance and one or more enamine derivatives as claimed in claim 1.
References Cited (Backward Citations)
No citation records indexed.
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