Endothelin antagonistic cyclic pentapeptides

Details Endothelin antagonistic cyclic pentapeptides Endothelin antagonistic cyclic pentapeptides

C - Chemistry, Metallurgy

07

K

530/7.64, 167/10

C07K 7/64 (2006.01) A61K 38/12 (2006.01) C07K 14/575 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2032559

1. A cyclic pentapeptide of the formula: cyclo (-X1-X2-X3-X4-X5-)~ (I) wherein X n (n = 1-5) represent amino acid residues, respectively, and X1 is DPhe, DTyr, DTha, DTza, DNal, DBta, DTrp, DTrp(O), DTrp(CHO) or DTrp((CH2)m COR1) (wherein m is from 0 to 6, and R1 is a hydroxyl group, a C1-C6 alkoxy group, an amino group or a C1-C6 monoalkylamino group, provided that when m = 0, R1 is not a hydroxyl group), X2 is DAsp, DGlu or DCys(O3H), X3 is Pro, Hyp, Pip, Thz, .beta.Ala, Or Gly, Ala, .alpha.Aba, Aib, Val, Nva, Leu, Ile, aIle, Nle, Met, Met(O), Met(O2), Phe, Tza, Tha, Tyr, Trp, His, Arg, Lys, Lys(CHO), Orn, Orn(CHO), Asn, Gln, Asp, Glu, Cys(O3H), Cys, Ser or Thr wherein a hydrogen atom on the .alpha.-amino group may be substituted by a C1-C6 alkyl or C3-C7 cycloalkyl group which may have an optional group selected from the group consisting of an imidazolyl group, a carboxyl group, a sulfo group and a hydroxyl group, X4 is DAla, DThr, D.alpha.Aba, DVal, DNva, DLeu, DIle, DaIle, DNle, DtertLeu, DCpg, DChg, DDpg, DPen, Aib, Ac3c, Ac4c, Ac5C, Ac6c, Ac7c, or DPhg, DThg, DFug, DTzg or DItg wherein a hydrogen atom at the .alpha.- position may be substituted by a C1-C3 alkyl group, X5 is Pro, Pip, Thz, or His, Ala, aAba, Val, Nva, Leu, Ile, aIle, Nle, Met, C3al, Coal, C5a1 or C6al wherein a hydrogen atom on the .alpha.-amino group may be substituted by a C1-C6 alkyl group; or a pharmaceutically acceptable salt thereof.

Affiliated with

Also associated with

Rating

Endothelin antagonistic cyclic pentapeptides does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Endothelin antagonistic cyclic pentapeptides, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Endothelin antagonistic cyclic pentapeptides will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1981778