EP0352228A2
Expired / Lapsed
EP
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Novel proteins
Assignee: UCP Gen Pharma AG
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Filing: 1989-07-11
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Granted: —
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Expires: 2009-07-11
Abstract
Abstract Novel polypeptides are provided which differ from desulphatohirudin by simple or multiple mutations. The novel polypeptides have valuable pharmacological properties and can be prepared by recombinant DNA techniques.
Inventors
- 👤 Andrew Dr. Wallace
- 👤 Stanley Dr. Dennis
- 👤 Jan Dr. Hofsteenge
- 👤 Stuart R. Dr. Stone
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-23 21:42
CPC Classifications
C; C12; C12N; C12N15/00; C07; C07K; C07K14/00; C07K14/81; C07K14/815; A; A61; A61P; A61P7/00; A61P7/02; A61P9/00; A61K; A61K38/00
Claims Analysis
Total Claims: 24
Claim 1
Independent Claim
116 words
Mutants of desulphatohirudin having the amino acid sequence wherein Z o represents Val or the dipeptidyl radicals Gly-Val or Met-Val, Z₁ is Lys, Gln, Asn, Leu, Arg or Val, Z₂ represents Lys, Arg, Asn, Val, Leu or Gln, Z₃ represents Lys, Arg, Asn, Val or Leu, Z₄ represents Pro or Gly, Z₅ and Z₇ independently from each other represent Gln, Asn or Met, and Z₆ represents His, Gln or Asn, with the exception of compounds of the formula I in which Z o represents Val, Z₁ represents Lys or Gln, Z₂ represents Lys or Gln, Z₃ represents Lys, Z₄ represents Pro, Z₅ represents Gln, Z₆ represents Gln or His and Z₇ represents Asn, and salts thereof.
Claim 2
Dependent Claim
116 words
Mutants of desulphatohirudin having the amino acid sequence wherein Z o represents Val or the dipeptidyl radicals Gly-Val or Met-Val, Z₁ is Lys, Gln, Asn, Leu, Arg or Val, Z₂ represents Lys, Arg, Asn, Val, Leu or Gln, Z₃ represents Lys, Arg, Asn, Val or Leu, Z₄ represents Pro or Gly, Z₅ and Z₇ independently from each other represent Gln, Asn or Met, and Z₆ represents His, Gln or Asn, with the exception of compounds of the formula I in which Z o represents Val, Z₁ represents Lys or Gln, Z₂ represents Lys or Gln, Z₃ represents Lys, Z₄ represents Pro, Z₅ represents Gln, Z₆ represents Gln or His and Z₇ represents Asn, and salts thereof.
Claim 3
Dependent Claim
107 words
Desulphatohirudin mutants of the formula I according to claim 1 wherein Z o represents Val or the dipeptidyl radicals Gly-Val or Met-Val, Z₁ represents Lys, Gln, Asn or Arg, Z₂ represents Lys, Arg, Asn, Val or Gln, Z₃ represents Lys or Arg, Z₄ represents Pro or Gly, Z₅ represents Gln or Met, Z₆ represents His or Asn and Z₇ represents Asn or Met, with the exception of compounds of the formula I in which Z o represents Val, Z₁ represents Lys or Gln, Z₂ represents Lys or Gln, Z₃ represents Lys, Z₄ represents Pro, Z₅ represents Gln, Z₆ represents His and Z₇ represents Asn, and salts thereof.
Claim 4
Dependent Claim
5 words
[Asn²⁷]-desulphatohirudin according to claim 1.
Claim 5
Dependent Claim
5 words
[Asn³⁶]-desulphatohirudin according to claim 1.
Claim 6
Dependent Claim
5 words
[Val³⁶]-desulphatohirudin according to claim 1.
Claim 7
Dependent Claim
5 words
[Gly⁴⁸]-desulphatohirudin according to claim 1.
Claim 8
Dependent Claim
5 words
[Met⁴⁹]-desulphatohirudin according to claim 1.
Claim 9
Dependent Claim
5 words
[Met⁵²]-desulphatohirudin according to claim 1.
Claim 10
Dependent Claim
5 words
[Asn⁵¹]-desulphatohirudin according to claim 1.
Claim 11
Dependent Claim
6 words
[Gln²⁷, Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 12
Dependent Claim
7 words
[Gln²⁷, Gln³⁶, Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 13
Dependent Claim
6 words
[Arg³⁶, Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 14
Dependent Claim
6 words
[Arg²⁷, Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 15
Dependent Claim
7 words
Glycyl-[Gln²⁷, Gln³⁶, Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 16
Dependent Claim
5 words
Methionyl-[Gln²⁷,Arg⁴⁷]-desulphatohirudin according to claim 1.
Claim 17
Dependent Claim
11 words
A pharmaceutical composition comprising a desulphatohirudin mutant according to claim 1.
Claim 18
Dependent Claim
24 words
A desulphatohirudin mutant according to claim 1 for use in a method for the prophylactic or therapeutic treatment of the human or animal body.
Claim 19
Dependent Claim
99 words
Method for the production of a desulphatohirudin mutant according to claim 1 comprising culturing a microbial host strain which has been transformed with a hybrid vector comprising an expression cassette consisting of a promoter operably linked to a first DNA sequence encoding a signal peptide linked in the proper reading frame to a second DNA sequence coding for the desulphatohirudin mutant, and a DNA sequence containing transcription termination signals, and isolating the desulphatohirudin mutant, and, if desired, converting an obtained polypeptide having free carboxy and/or amino groups into a salt or converting a salt obtained into the free compound.
Claim 20
Dependent Claim
11 words
A desulphatohirudin mutant obtainable by the method according to claim 18.
Claim 21
Dependent Claim
50 words
A hybrid vector comprising an expression cassette consisting of a promoter operably linked to a first DNA sequence encoding a signal peptide linked in the proper reading frame to a second DNA sequence coding for a desulphatohirudin mutant according to claim 1, and a DNA sequence containing transcription termination signals.
Claim 22
Dependent Claim
84 words
Method for the production of a hybrid vector according to claim 20 comprising linking the expression cassette consisting of a promoter operably linked to a first DNA sequence encoding a signal peptide linked in the proper reading frame to a second DNA sequence coding for the desulphatohirudin mutant, and a DNA sequence containing transcription termination signals, or the constituents of the expression cassette to the DNA fragments containing selective genetic markers and origins of replication for the selection microbial host in the predetermined order.
Claim 23
Dependent Claim
59 words
A microbial host strain which has been transformed with a hybrid vector comprising an expression cassette consisting of a promoter operably linked to a first DNA sequence encoding a signal peptide linked in the proper reading frame to a second DNA sequence coding for a desulphatohirudin mutant according to claim 1, and a DNA sequence containing transcription termination signals.
Claim 24
Dependent Claim
28 words
Method for the production of the transformed microbial host strain according to claim 22 comprising transforming a microbial host strain with the hybrid vector according to claim 20.
References Cited (Backward Citations)
No citation records indexed.
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