EP 1001800 A2 20000524 - BIOLOGICALLY ACTIVE PEPTIDES WITH REDUCED TOXICITY IN ANIMALS AND A METHOD FOR PREPARING SAME
Title (en)
BIOLOGICALLY ACTIVE PEPTIDES WITH REDUCED TOXICITY IN ANIMALS AND A METHOD FOR PREPARING SAME
Title (de)
BIOLOGISCH AKTIVE PEPTIDE MIT VERMINDERTER TOXIZITÄT IN TIEREN UND EIN VERFAHREN ZU DEREN HERSTELLUNG
Title (fr)
PEPTIDES BIOLOGIQUEMENT ACTIFS A TOXICITE REDUITE CHEZ L'ANIMAL ET PROCEDES D'ELABORATION
Publication
Application
Priority
- US 9814610 W 19980715
- US 89300697 A 19970715
Abstract (en)
[origin: WO9903488A2] The present invention relates to biologically active peptides with reduced toxicity and methods of preparing them. The peptides of the invention, which can be unsubstituted or N-terminal substituted have formula (I), wherein X is a biologically active amphiphilic ion channel-forming peptide or protein, T is a lipophilic moiety or hydrogen, and W is T or hydrogen. Preferably T is formula (II), wherein R is a hydrocarbon (alkyl or aromatic or alkylaromatic) having at least 2 and no more than 10 carbon atoms. T is preferably an octanoyl group. The peptides and proteins of the invention have improved antimicrobial and anti-tumor biological activity while exhibiting reduced toxicity. A preferred method of reducing toxicity involves the formation of related methane sulfonate derivatives or analogues. Additionally, the compounds of the invention may be used to treat sepsis, septic shock, and lung infections, such as those occuring in cystic fibrosis.
IPC 1-7
IPC 8 full level
A61K 38/00 (2006.01); A61P 31/00 (2006.01); A61P 35/00 (2006.01); C07K 1/02 (2006.01); C07K 14/435 (2006.01); C07K 14/46 (2006.01); C07K 14/47 (2006.01)
CPC (source: EP)
A61P 31/00 (2017.12); A61P 35/00 (2017.12); C07K 14/43563 (2013.01); C07K 14/46 (2013.01); A61K 38/00 (2013.01)
Citation (search report)
See references of WO 9903488A2
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9903488 A2 19990128; WO 9903488 A3 19990408; AU 8300598 A 19990210; CA 2294518 A1 19990128; EP 1001800 A2 20000524; JP 2001510164 A 20010731
DOCDB simple family (application)
US 9814610 W 19980715; AU 8300598 A 19980715; CA 2294518 A 19980715; EP 98933343 A 19980715; JP 2000502785 A 19980715