Endothelin-antagonizing peptide

Details Endothelin-antagonizing peptide Endothelin-antagonizing peptide

C - Chemistry, Metallurgy

07

K

C07K 7/56 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/12 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/575 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2142985

Disclosed is a peptide compound represented by the following formula (I): R1-R2-R3-R4-R5-R6-R7-R8-R9-R10-R11-R12-Phe- (I) R14-R15-R16-Rl7-R18-Ile-R20-Z {wherein R1 represents X1-Gly, Image , X2-SCH2CH2CO or hydrogen; R2 represents Asn, Asp, Phe, Tyr, Ser, or a single bond; R3 represents Trp, Ile, Pro, Ala, or a single bond; R4 represents His, Lys, Gly, Trp, Ala, or a single bond; R5 represents Gly, Thr, Trp, Val, or a single bond; R6 represents Gly, Thr, Asn, Tyr, Asp, or a single bond; R7 represents Ala, Ser, Asn, Asp, Tyr, Phe, or a single bond; R8 represents Pro, Ala, Arg, or a single bond; R9 represents Image , Image or a single bond; R10 represents Trp or Ala; R11 represents Val, Pro, or a single bond; R12 represents Tyr or a single bond; R14 represents Ala, MeAla, Ser, or Cys; R15 represents His or Trp; R16 represents Leu or Nva; R17 represents Asp, Thr, Asn, Ser, Gly, or Glu; R18 represents Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg, or Nle; R20 represents Trp, Phe, or Tyr; and Z represents hydroxy, lower alkoxy, or amino (wherein X1 and X3 each represent hydrogen, benzyloxycarbonyl, t-butyloxycarbonyl, 9- fluorenylmethyloxycarbonyl, or carboxy-substituted or unsubstituted lower alkanoyl; X2 represents hydrogen or acetamidomethyl; Y1 represents hydroxy or lower alkoxy; Y2 represents hydrogen, or X1 and Y1 or X2 and Y2 are combined together to form a single bond as X1-Y1 or X2-Y2; and Nva represents a norvaline residue, Cha represents a .beta.- cyclohexylalanine residue, Abu represents a 2-aminobutanoic acid residue, Thi represents a .beta.-(2-thienyl)alanine residue, Phg represents a phenylglycine residue, Nle represents a norleucine residue, MeAla represents a N-methylalanine residue, MeLeu represents a N-methylleucine residue, Melle represents a N-methylisoleucine residue, and amino acid residues other than Gly each represent a D-, L-, or DL-amino acid residue)}, and a pharmaceutically acceptable salt thereof.

Composé peptidique à effet antagoniste de l'endothéline représenté par la formule générale (I) et sel pharmaceutiquement acceptable de ce composé: R<1>-R<2>-R<3>-R<4>-R<5>-R<6>-R<7>-R<8>-R<9>-R<10>-R<11>-R<12>-Phe-R<14>-R<15>-R<16>-R<17>-R<18>-Ile-R<20>-Z dans laquelle: R<1> est X<1>-Gly, X<3>(a), X<2>-SCH2CO ou de l'hydrogène; R<2> est Asn, Asp, Phe, Tyr, Ser ou une liaison unique; R<3> est Trp, Ile, Pro, Ala ou une liaison unique; R<4> est His, Lys, Gly, Trp, Ala ou une liaison unique; R<5> est Gly, Thr, Trp, Val ou une liaison unique; R<6> est Gly, Thr, Asn, Tyr, Asp ou une liaison unique; R<7> est Ala, Ser, Asn, Asp, Tyr, Phe ou une liaison unique; R<8> est Pro, Ala, Arg ou une liaison unique; R<9> est (b), (c) ou une liaison unique; R<10> est Trp ou Ala; R<11> est Val, Pro ou une liaison unique; R<12> est Tyr ou une liaison unique; R<14> est Ala, MeAla, Ser ou Cys; R<15> est His ou Trp; R<16> est Leu ou Nva; R<17> est Asp, Thr, Asn, Ser, Gly ou Glu; R<18> est Ile, Leu, Cha, Abu, Thi, Met, Tyr, MeLeu, MeIle, Phg ou Nle; R<20> est Trp, Phe ou Tyr; et Z est un hydroxy, un alcoxy inférieur, ou un amino.

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