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GB1532148A - 1-substituted enkepholin derivatives - Google Patents

1-substituted enkepholin derivatives

Info

Publication number
GB1532148A
GB1532148A GB33220/77A GB3322077A GB1532148A GB 1532148 A GB1532148 A GB 1532148A GB 33220/77 A GB33220/77 A GB 33220/77A GB 3322077 A GB3322077 A GB 3322077A GB 1532148 A GB1532148 A GB 1532148A
Authority
GB
United Kingdom
Prior art keywords
gly
phe
met
obzl
leu
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
GB33220/77A
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GD Searle LLC
Original Assignee
GD Searle LLC
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GD Searle LLC filed Critical GD Searle LLC
Publication of GB1532148A publication Critical patent/GB1532148A/en
Expired legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/665—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans derived from pro-opiomelanocortin, pro-enkephalin or pro-dynorphin
    • C07K14/70—Enkephalins
    • C07K14/702—Enkephalins with at least 1 amino acid in D-form
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1008—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Toxicology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1532148 1-Substituted encephalin G D SEARLE & CO 8 Aug 1977 [9 Aug 1976] 33220/77 Heading C3H Polypeptides of the Formula (I) wherein Y is Leu or Met; W is (C 1-8 alkyl) Phe (wherein C 1-8 alkyl substitutes the phenyl radical of Phe), D-Tyr, #-Ala, DOPA, Pyroglu, hexahydroPhe, desamino-Tyr or X<SP>1</SP>-Tyr (wherein X<SP>1</SP> is N-(C 1-8 ) alkyl, O-(C 1-8 ) alkyl, Pyroglu, D-Arg, Sar or Sue); provided that if Y is Met; W is other than Phe, DOPA, desamino-Tyr or Sar-Tyr; wherein the optically active amino acids have the D, DL or L configuration; and the pharmaceutically acceptable acid addition salts thereof. Polypeptides (I) prepared in the Examples are: H-(4-tBu)Phe-Gly-Gly-Phe-Met-OH; H- (4-tBu)Phe-Gly-Gly-Phe-Leu-OH; H-hexahydroPhe-Gly-Gly-Phe-Leu-OH; H-Tyr(Me)-Gly- Gly-Phe-Met-OH; H-D-Tyr-Gly-Gly-Phe-Met- OH; H-#-Ala-Gly-Gly-Phe-Met-OH; H-#-Ala- Gly-Gly-Phe-Leu-OH; H-Pyroglu-Gly-Gly- Phe-Met-OH; H-Pyroglu-Gly-Gly-Phe-Leu- OH; H-DOPA-Gly-Gly-Phe-Leu-OH; H-D- (4-tBu)Phe-Gly-Gly-D-Phe-D-Met-OH; H-DTyr-Gly-Gly-Phe-Leu-OH; H-Sar-Tyr-Gly-Phe- Leu-OH; OctTyr-Gly-Gly-Phe-Leu-OH. Polypeptide intermediates isolated are: HEXAPEPTIDE: Boc-Sar-Tyr-Gly-Gly-Phe- Leu-OBzl. PENTAPEPTIDES: Boc-(4-tBu)Phe-Gly- Gly-Phe-Met-OBzl and OH; Boc-(4-tBu)Phe- Gly-Gly-Phe-Leu-OBrl; Boc-hexahydroPhe-Gly- Gly-Phe-Met-OBzl; Boc-Tyr(Me) -Gly-Gly-Phe- Met-OBzl; Boc-D-Tyr-Gly-Gly-Phe-Met-OBzl; Boc-#-Ala-Gly-Gly-Phe-Met-OBzl; H-Pyroglu- Gly-Gly-Phe-Met-OBzl- H-Pyroglu-Gly-Gly-Phe- Leu-OBzl; Boc-D-(4-tBu)Phe-Gly-Gly-D-Phe-DMet-OBzl. TETRAPEPTIDES: Boc and H-Gly-Gly-Phe- Met-OBzl; Boc and H-Gly-Gly-Phe-Leu-OBzl. TRIPEPTIDES: Boc-Gly-Gly-Phe-OBzl and OH. DIPEPTIDES: Boc and H-Gly-Phe-OBzl. Pharmaceutical compositions, which may be in unit dosage form, comprise polypeptides (I) in admixture with a pharmaceutically-acceptable carrier therefor.
GB33220/77A 1976-08-09 1977-08-08 1-substituted enkepholin derivatives Expired GB1532148A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US71262676A 1976-08-09 1976-08-09

Publications (1)

Publication Number Publication Date
GB1532148A true GB1532148A (en) 1978-11-15

Family

ID=24862912

Family Applications (1)

Application Number Title Priority Date Filing Date
GB33220/77A Expired GB1532148A (en) 1976-08-09 1977-08-08 1-substituted enkepholin derivatives

Country Status (5)

Country Link
JP (1) JPS5321140A (en)
AU (1) AU2768977A (en)
DE (1) DE2735674A1 (en)
FR (1) FR2361349A1 (en)
GB (1) GB1532148A (en)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2655149A1 (en) * 1975-12-17 1977-06-23 Sandoz Ag Analgesic glycine-contg. peptide derivs. - e.g. tyrosyl-glycyl-glycyl-phenylalanyl-norleucine
FR2338925A1 (en) * 1976-01-26 1977-08-19 Wellcome Found NEW PEPTIDES AND MEDICINAL PRODUCTS CONTAINING THESE SUBSTANCES
FI770219A7 (en) * 1976-02-02 1977-08-03 Sandoz Ag

Also Published As

Publication number Publication date
AU2768977A (en) 1979-02-15
FR2361349A1 (en) 1978-03-10
DE2735674A1 (en) 1978-02-16
JPS5321140A (en) 1978-02-27

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Legal Events

Date Code Title Description
CSNS Application of which complete specification have been accepted and published, but patent is not sealed