FR2416883A2 - Tri:fluoro:acetyl oligopeptide derivs. - useful as elastase inhibitors - Google Patents

Tri:fluoro:acetyl oligopeptide derivs. - useful as elastase inhibitors

Info

Publication number
FR2416883A2
FR2416883A2 FR7901410A FR7901410A FR2416883A2 FR 2416883 A2 FR2416883 A2 FR 2416883A2 FR 7901410 A FR7901410 A FR 7901410A FR 7901410 A FR7901410 A FR 7901410A FR 2416883 A2 FR2416883 A2 FR 2416883A2
Authority
FR
France
Prior art keywords
lys
ala
derivs
oligopeptide
fluoro
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.)
Pending
Application number
FR7901410A
Other languages
French (fr)
Inventor
J Bieth
J L Dimicoli
C G Wermuth
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.)
Synthelabo SA
Original Assignee
Delalande SA
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
Priority claimed from FR7704713A external-priority patent/FR2381023A1/en
Application filed by Delalande SA filed Critical Delalande SA
Priority to LU80829A priority Critical patent/LU80829A1/en
Priority to SE7900797A priority patent/SE7900797L/en
Publication of FR2416883A2 publication Critical patent/FR2416883A2/en
Priority to GR60859A priority patent/GR73130B/el
Priority to GB7944621A priority patent/GB2040291A/en
Priority to ZA00800079A priority patent/ZA8079B/en
Priority to IT19070/80A priority patent/IT1149281B/en
Priority to ES487622A priority patent/ES8202786A1/en
Priority to AU54749/80A priority patent/AU5474980A/en
Priority to JP447080A priority patent/JPS55100347A/en
Priority to NL8000345A priority patent/NL8000345A/en
Priority to DE19803001825 priority patent/DE3001825A1/en
Priority to BE0/199023A priority patent/BE881227R/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06086—Dipeptides with the first amino acid being basic
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • General Health & Medical Sciences (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Oligopeptide derivs. of formula (I) are claimed: (where (i) X-Y is L-Ala-L-Ala, n = O and R is H, m-NO2 p-Cl, p-CF3, p -MeO, p-isopropyl, p-CN or p-COOH; (ii) X-Y is L-Lys-L-Ala, n = O and R is H, p-CF3, p-Me, p-isopropyl, p-Nme2, p-COMe, p-isobutyl, plcyclohexyl, p-F or p-NET2; (iii) X-Y is L-Lys-L-Ala, n = 1 and R = H; (iv) X-Y is L-Ala-Dl-NHCH(CF3)CO, n = O and R = H; (v) X-Y is L-Lys-L-Lys or L-Ala-L-Lys, n = O and R = p-CF3; or (vi) X-Y is L-Lys-L-Pro, L-Lys-L-Phe, L-Lys-L-ValorL-Lys-L-Leu, n = O and R = isopropyl). Also claimed are new intermediates for the prepn. of (I). Cpds. (I) are reversible pancreatic and leucocytic elastase inhibitors. They can be used, e.g. in the treatment of emphysema.
FR7901410A 1977-02-18 1979-01-19 Tri:fluoro:acetyl oligopeptide derivs. - useful as elastase inhibitors Pending FR2416883A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
LU80829A LU80829A1 (en) 1977-02-18 1979-01-26 NOVEL TRIFLUOROMETHYL OLIGOPEPTIDES, THEIR PREPARATION PROCESS AND THEIR APPLICATION IN THERAPEUTICS
SE7900797A SE7900797L (en) 1978-02-09 1979-01-30 NEW TRIFLOURMETHILATED OLIGOPEPTIDS AND WAYS TO PRODUCE THESE
GR60859A GR73130B (en) 1979-01-19 1979-12-27
GB7944621A GB2040291A (en) 1979-01-19 1979-12-31 Trifluoromethylated dipeptides
ZA00800079A ZA8079B (en) 1979-01-19 1980-01-07 Trifluorethylated oligopeptides,a process of preparing same and their application in therapeutics
IT19070/80A IT1149281B (en) 1979-01-19 1980-01-08 TRIFLUOROMETHYLATED OLIGOPEPTIDES, THEIR PREPARATION PROCEDURE AND THEIR THERAPEUTIC APPLICATION
ES487622A ES8202786A1 (en) 1979-01-19 1980-01-11 Trifluoromethylated dipeptides
AU54749/80A AU5474980A (en) 1979-01-19 1980-01-18 Trifluorethylated oligopeptides
BE0/199023A BE881227R (en) 1977-02-18 1980-01-18 NOVEL TRIFLUOROMETHYLATED OLIGOPEPTIDES, THEIR PREPARATION PROCESS AND THEIR APPLICATION IN THERAPEUTICS
DE19803001825 DE3001825A1 (en) 1977-02-18 1980-01-18 Tri:fluoromethyl oligopeptide(s) - useful for treating emphysema
JP447080A JPS55100347A (en) 1979-01-19 1980-01-18 Trifluoromethylated oligopeptides and manufacture
NL8000345A NL8000345A (en) 1979-01-19 1980-01-18 NEW TRIFLUORMETHYL OLIGOPEPTIDES, PROCESS FOR THEIR PREPARATION AND USE IN MEDICINES.

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR7704713A FR2381023A1 (en) 1977-02-18 1977-02-18 NEW L-ALANINE-DERIVED TRIFLUOROMETHYL OLIGOPEPTIDES, THEIR PREPARATION PROCESS AND THEIR THERAPEUTIC APPLICATION
CH146478 1978-02-09

Publications (1)

Publication Number Publication Date
FR2416883A2 true FR2416883A2 (en) 1979-09-07

Family

ID=25687724

Family Applications (1)

Application Number Title Priority Date Filing Date
FR7901410A Pending FR2416883A2 (en) 1977-02-18 1979-01-19 Tri:fluoro:acetyl oligopeptide derivs. - useful as elastase inhibitors

Country Status (1)

Country Link
FR (1) FR2416883A2 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2183188A1 (en) * 1972-05-02 1973-12-14 Bofors Ab
FR2294715A1 (en) * 1974-12-17 1976-07-16 Inst Rech Scient Antibacterial and antifungal peptides with lysine-lysine gp - e.g. methyl N-alpha 2,2-dimethyl-palmitoyl L-lysyl-L-lysyl hydrochloride

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2183188A1 (en) * 1972-05-02 1973-12-14 Bofors Ab
FR2294715A1 (en) * 1974-12-17 1976-07-16 Inst Rech Scient Antibacterial and antifungal peptides with lysine-lysine gp - e.g. methyl N-alpha 2,2-dimethyl-palmitoyl L-lysyl-L-lysyl hydrochloride

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
CA1974 *
CA1975 *

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