EP0089007B1
Expired / Lapsed
EP
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Process for the conversion of preproinsulin analogues into insulins
Assignee: Hoechst AG
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Filing: 1983-03-10
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Granted: 1986-07-30
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Expires: 2003-03-10
Abstract
Abstract The invention relates to a process for the preparation of insulins from analogs of preproinsulins, which comprises reacting preproinsulin analogs, at a pH below the isoelectric point of the insulins in the presence of trypsin or a trypsin-like endopeptidase, with an ester of natural amino acids or their derivatives and then cleaving off the ester group and other protective groups which may optionally be present.
Inventors
- 👤 Rainer Dr. Obermeier
- 👤 Rolf Prof. Dr. Geiger
- 👤 Ulrich Dr. Grau
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-29 14:24
CPC Classifications
C; C12; C12P; C12P21/00; C12P21/02; C07; C07K; C07K14/00; C07K14/435; C07K14/575; C07K14/62; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/26
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
73 words
A process for the production of insulins from analogs of preproinsulins, characterized in that preproinsulin analogs are reacted at a pH-value below the isoelectric point of the corresponding insulins in the presence of trypsin or a trypsin-like endopeptidase with an ester of natural amino acids or derivatives of such an ester which contain protective groups, and that the ester group and other protective groups which may optionally be present are then cleaved off.
Claim 2
Dependent Claim
73 words
A process for the production of insulins from analogs of preproinsulins, characterized in that preproinsulin analogs are reacted at a pH-value below the isoelectric point of the corresponding insulins in the presence of trypsin or a trypsin-like endopeptidase with an ester of natural amino acids or derivatives of such an ester which contain protective groups, and that the ester group and other protective groups which may optionally be present are then cleaved off.
Claim 3
Dependent Claim
21 words
A process as claimed in claim 1, characterized in that the amino acid derivatives used are Ala-OtBu or Thr (tBu) OtBu.
Claim 4
Dependent Claim
28 words
A process as claimed in claim 1 or 2, characterized in that it is carried out at a pH-value between 3.8 and 5.5, preferably between 3.8 and 5.0.
Claim 5
Dependent Claim
44 words
A process as claimed in one or more of claims 1 to 3, characterized in that the enzyme substrate ratio is from 1 : 1 to 1 : 100 parts by weigths, preferably from 1 : 4 to 1 : 10 parts by weight.
Claim 6
Dependent Claim
44 words
A process as claimed in one or more of claims 1 to 4, characterized in that the molar ratio between' the amino acid ester or its derivative containing protective groups to the preproinsulin analog is from 50 : 500, preferably from 100 : 250.
Claim 7
Dependent Claim
35 words
A process as claimed in one or more of claims 1 to 5, characterized in that the reaction temperature is between + 2 and + 37 °C, preferably between + 4 and + 10 °C.
Claim 8
Dependent Claim
69 words
A process as claimed in claim 1 or 2, characterized in that it is carried out at a pH-value between 3.8 and 5.5, the enzyme/substrate ratio is from 1 : 1 to 1 : 100 parts by weight, the molar ratio of amino acid ester or its derivative to the preproinsulin analog is from 50 : 500 and the reaction temperature is between + 2 and + 37 °C.
Claim 9
Dependent Claim
69 words
A process as claimed in claim 1 or 2, characterized in that it is carried out at a pH-value between 3.8 and 5.0, the enzyme/substrate ratio is from 1 : 4 to 1 : 10 parts by weight, the molar ratio of amino acid ester or its derivative to the preproinsulin analog is from 100 : 250, and the reaction temperature is between + 4 and + 10 °C.
References Cited (Backward Citations)
No citation records indexed.
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