Dipeptide narcotic antagonists
Peptide, process for preparation thereof and use thereof
N-Acylpeptide compound, processes for the preparation thereof and the pharmaceutical compositions Patent #: 4436726
ApplicationNo. 06/452827 filed on 12/23/1982
US Classes:514/18, 3 or 4 peptide repeating units in known peptide chain514/19, 2 peptide repeating units in known peptide chain530/331, Tripeptides, e.g., tripeptide thyroliberin (TRH), melanostatin (MIF), etc.560/149, Sulfoxy in acid moiety560/169, Additional nitrogen in acid moiety560/170, Oxy, aldehyde or ketone group in acid moiety560/222, Phosphorus, sulfur or nitrogen in alcohol moiety560/251, Plural nitrogens in alcohol moiety560/252, Polyoxy alcohol moiety560/253Acyclic alcohol moiety
ExaminersPrimary: Phillips, Delbert R.
Attorney, Agent or Firm
International ClassesC07K 5/065 (20060101)
C07K 5/00 (20060101)
C07K 5/068 (20060101)
C07K 5/072 (20060101)
C07K 5/06 (20060101)
A61K 38/00 (20060101)
Foreign Application Priority Data1982-01-05 GB
AbstractN-acylpeptides are disclosed of the formula: ##STR1## wherein R1 is alkanoyloxy or alkenoyloxy; R2 is alkyl or alkenyl; R3 and R4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A1, A2 and A3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.