Abstract: Electrochemical methods, preferably the Kolbe coupling reaction, are utilized to create intramolecularly bridged peptides, segments or peptide isosteres which are conformationally restricted and preferably, biologically active. Preferably, the peptide analogues contain methylene groups bridging particular amino acid side chains. Analogues of a variety of peptide hormones, including insulin, insulin-like growth factors, somatostatin, melanocyte stimulating hormone, and the like are prepared by the above methods. Such peptides are useful as agonists or antagonists for treatment of diseases associated with deficiency of the hormone or dysregulation of hormone activity, as well as for mechanistic studies to understand the interactions between peptide hormones and cells.
Abstract: New glycopeptide antibiotics MM 49728, MM 55266, MM 55267/1, MM 55267/2 and MM 55268 are produced by fermentation of Amycolatopsis sp. NCIB 40089.
Type:
Grant
Filed:
December 18, 1991
Date of Patent:
March 9, 1993
Assignee:
Beecham Group PLC
Inventors:
Nigel J. Coates, Rachel Sykes, Christopher J. Davis, Lawrence M. Curtis
Abstract: The invention relates to new peptide derivatives of the general Formula I ##STR1## wherein R is a group derived from any oligopeptide by removing a terminal amino group, or--if the oligopeptide comprises a diamino carboxylic acid--the amino group in the .omega.-position, or the terminal and .omega.-amino groups; andstands for the integral number 1 or 2and acid addition slats thereof and a process for the preparation thereof.The new compounds of the general Formula I exhibit antitumor activity.
Type:
Grant
Filed:
April 19, 1985
Date of Patent:
August 21, 1990
Assignee:
Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
Abstract: A complex of a therapeutic agent is disclosed in which the therapeutic agent is complexed to an ammonium ion selected from the group consisting of ##STR1## where R.sup.1 and R.sup.2 are the same or different and are alkyl or hydroxy substituted alkyl containing 1 to 6 carbon atoms; andR, R' and R" are the same or different and are saturated or unsaturated aliphatics containing at least 10 carbon atoms, ##STR2## where R.sup.1, R.sup.2 and R" are as defined above, ##STR3## where R.sup.3 is independently alkyl or hydroxy substituted alkyl containing at least 10 carbon atoms; and R.sup.1, R.sup.2, R.sup.3 and R' having the meanings given above; and ##STR4## where R.sup.1, R.sup.2 and R.sup.3 have the meanings given above. The therapeutic agent is heparin, a biologically active peptide or protein or an antineoplastic drug. The therapeutic agent may also be covalently bonded to a triglyceride type backbone to form a compound.