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US4123523A Expired / Lapsed US ⏱️ 0.0 years remaining

Analgesic and sedative polypeptides

Assignee: Imperial Chemical Industries Ltd
•
Filing: 1977-06-03
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Granted: 1978-10-31
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Expires: 1997-06-03
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Abstract

Abstract The disclosure relates to novel polypeptides which possess analgesic and sedative activity, to processes for their manufacture and to compositions containing them. Typical of the peptides disclosed is H-Tyr-D-Ala-Gly-Phe-Leu-Ala-Ile-Ile-Lys-Asn-Ala-Tyr-Lys-Lys-OH.

Inventors

  • 👤 Anand S. Dutta
  • 👤 James J. Gormley
  • 👤 Christopher F. Hayward
  • 👤 John S. Morley
  • 👤 Nigel N. Petter
  • 👤 Gilbert J. Stacey

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-29 20:42
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/675; C07K14/6755; A; A61; A61P; A61P25/00; A61P25/04; A61P29/00; C07K14/67; C07K14/672; A61K; A61K38/00

Claims Analysis

Total Claims: 11
Claim 1
Independent Claim 113 words
A polypeptide of the formula:- H-Tyr-A-Gly-Phe-B-P-E I in which A is selected from the group consisting of D-Ala, D-Ser, D-Met and Gly; B is selected from the group consisting of Leu and Met, E is selected from the group consisting of a hydroxy and amino radical and an alkoxy radical of 1 to 6 carbons; and P is a peptide residue selected from those of the formula:- Lys-Lys II asn-Ala-Y-Lys-Lys III ala-Ile-X-Lys-Asn-Ala-Y-Lys-Lys IV thr-Leu-Phe-Lys-Asn-Ala-Ile-X-Lys-Asn-Ala-Y-Lys-Lys V and ##STR7## in which X is Val or Ile and Y is Tyr or His; and the pharmaceutically-acceptable acid-addition salts thereof, and where the polypeptide of the formula I contains a free carboxygroup, the pharmaceutically-acceptable base-addition salts thereof.
Claim 2
Dependent Claim 113 words
A polypeptide of the formula:- H-Tyr-A-Gly-Phe-B-P-E I in which A is selected from the group consisting of D-Ala, D-Ser, D-Met and Gly; B is selected from the group consisting of Leu and Met, E is selected from the group consisting of a hydroxy and amino radical and an alkoxy radical of 1 to 6 carbons; and P is a peptide residue selected from those of the formula:- Lys-Lys II asn-Ala-Y-Lys-Lys III ala-Ile-X-Lys-Asn-Ala-Y-Lys-Lys IV thr-Leu-Phe-Lys-Asn-Ala-Ile-X-Lys-Asn-Ala-Y-Lys-Lys V and ##STR7## in which X is Val or Ile and Y is Tyr or His; and the pharmaceutically-acceptable acid-addition salts thereof, and where the polypeptide of the formula I contains a free carboxygroup, the pharmaceutically-acceptable base-addition salts thereof.
Claim 3
Dependent Claim 27 words
A polypeptide as claimed in claim 1 in which A is D-Ala, B is Leu, E is a hydroxy radical, X is Ile and Y is Tyr.
Claim 4
Dependent Claim 29 words
A polypeptide as claimed in claim 1 in which P is a peptide residue selected from those of the formula II, III, IV and V given in claim 1.
Claim 5
Dependent Claim 18 words
A polypeptide as claimed in claim 1 in which P has the formula VI given in claim 1.
Claim 6
Dependent Claim 12 words
A polypeptide as claimed in claim 1 in which A is D-Ala.
Claim 7
Dependent Claim 18 words
A polypeptide as claimed in claim 1 in which P has the formula IV given in claim 1.
Claim 8
Dependent Claim 39 words
A polypeptide as claimed in claim 1 in which A is D-Ala, B is Leu, E is a hydroxy radical and P has the formula IV given in claim 1 in which X is Ile and Y is Tyr.
Claim 9
Dependent Claim 32 words
A pharmaceutical composition which comprises as active ingredient an effective amount of a polypeptide as claimed in claim 1 in association with a major amount of a non-toxic pharmaceutically-acceptable diluent or carrier.
Claim 10
Dependent Claim 24 words
A method of producing analgesia in warm-blooded animals including man which comprises administering an analgesically-effective amount of a polypeptide as claimed in claim 1.
Claim 11
Dependent Claim 24 words
A method of producing sedation in warm-blooded animals including man which comprises administering a sedatively-effective amount of a polypeptide as claimed in claim 4.

References Cited (Backward Citations)

US4038222A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1981-10-30 1982-05-01 1982-10-31 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1985-10-30 1986-05-01 1986-10-31 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1989-10-30 1990-05-01 1990-10-31 $7700.00 Window Closed / Lapsed

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