Patent EP0384341A2 successfully refreshed from Google Patents.
EP0384341A2
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New proline derivatives
Assignee: Yakult Honsha Co Ltd
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Filing: 1990-02-19
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Granted: —
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Expires: 2010-02-19
Abstract
Abstract New proline derivatives of the general formula: <CHEM> wherein R stands for a lower alkyl group and X for a N-terminal protective group conventional in amino acid chemistry or an acyl group derived from an amino acid with a protective group at the N-terminal. They have inhibitory activity against prolylendopeptidase and are chemically relatively stable as compared with known compounds of this type.
Inventors
- 👤 Takayuki Shioiri
- 👤 Yasumasa Hamada
- 👤 Naoko Irako
- 👤 Kunio C/O K.K. Yakult Honsha Kado
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 22:00
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/08; A; A61; A61P; A61P25/00; A61P25/28; C07D207/10; C07D207/16; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
42 words
Proline derivatives of the general formula: wherein R stands for a lower alkyl group and X for a N-terminal protective group conventional in amino acid chemistry or an acyl group derived from an amino acid with a protective group at the N-terminal.
Claim 2
Dependent Claim
42 words
Proline derivatives of the general formula: wherein R stands for a lower alkyl group and X for a N-terminal protective group conventional in amino acid chemistry or an acyl group derived from an amino acid with a protective group at the N-terminal.
Claim 3
Dependent Claim
22 words
Proline derivatives according to claim 1, wherein the N-terminal protective group conventional in the amino acid chemistry is methoxybenzoyl, methoxyphenylbutyryl or tert-butyryl.
Claim 4
Dependent Claim
22 words
Proline derivatives according to claim 1, wherein the amino acid from which the acyl is derived is proline, sarcosine or pyroglutamic acid.
Claim 5
Dependent Claim
35 words
Proline derivatives according to claim 1 or 3, wherein the N-terminal protective group in the acyl group derived from an amino acid with a protective group at the N-terminal is p-toluenesulfonyl, benzyloxycarbonyl, benzyloxysuccinyl or succinyl.
Claim 6
Dependent Claim
39 words
Proline derivatives according to claim 1, wherein the amino acid in the acyl group derived from an amino acid with a protective group at the N-terminal is N-benzyloxycarbonylproline, N-benzyloxysuccinylproline, N-succinylproline, N-p-toluenesulfonylsarcosine, N-benzyloxycarbonylsarcosine, N-benzyloxysuccinylsarcosine, N- succinylsarcosine, N-benzyloxycarbonylpyroglutamine, N-benzyloxysuccinylpyroglutamine or N-succinylpyroglutamine.
Claim 7
Dependent Claim
17 words
A proline derivative of the general formula (I) according to claim 1 for use as a medicament.
Claim 8
Dependent Claim
26 words
A pharmaceutical composition for treating senile dementia, especially Alzheimer's disease,comprising a compound of the general formula (I) according to claim 1 and a physiologically acceptable carrier.
Claim 9
Dependent Claim
98 words
A process for preparing the proline derivatives of the general formula (I) which comprises treating a prolinal of the general formula: wherein X has the meanings as defined above in or in the presence of the corresponding alcohol (ROH), using an acid catalyst, or, alternatively, for the preparation of compounds of the general formula (I) wherein X stands for a N-terminal protective group conventional in amino acid chemistry subjecting a prolinal dialkyl acetal of the general formula: wherein R has the meaning as defined above, to an amino acid - N atom protection reaction known per se .
Claim 10
Dependent Claim
98 words
A process for preparing the proline derivatives of the general formula (I) which comprises treating a prolinal of the general formula: wherein X has the meanings as defined above in or in the presence of the corresponding alcohol (ROH), using an acid catalyst, or, alternatively, for the preparation of compounds of the general formula (I) wherein X stands for a N-terminal protective group conventional in amino acid chemistry subjecting a prolinal dialkyl acetal of the general formula: wherein R has the meaning as defined above, to an amino acid - N atom protection reaction known per se .
References Cited (Backward Citations)
No citation records indexed.
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