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Generated: July 25, 2017

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Title: LHRH antagonist peptides
Abstract:Methods of treating a subject having a disorder associated with LHRH activity are disclosed.
Inventor(s): Roeske; Roger W. (Indianapolis, IN)
Assignee: Advanced Research & Technology Institute (Indianapolis, IN)
Application Number:08/973,378
Patent Claims: 1. An LHRH analogue comprising the structure A--B--C--D--E--F--G--H--I--J, wherein A is D-Glu, L-Glu, or an analogue thereof; B is D-His, L-His, or an analogue thereof; C is D-Trp, L-Trp, or an analogue thereof; D is D-Ser, L-Ser, or an analogue thereof; E is D-Tyr, L-Tyr, or an analogue thereof; F is D-asparagine, L-asparagine, D-glutamine, or L-glutamine; G is D-Leu, L-Leu or an analogue thereof; H is D-Arg, L-Arg, or an analogue thereof; I is D-Pro, L-Pro, or an analogue thereof; and J is D-Gly, L-Gly, or an analogue thereof; or a pharmaceutically acceptable salt thereof.

2. An LHRH analogue comprising the structure A--B--C--D--E--F--G--H--I, wherein A is D-Glu, L-Glu, or an analogue thereof; B is D-His, L-His, or an analogue thereof; C is D-Trp, L-Trp, or an analogue thereof; D is D-Ser, L-Ser, or an analogue thereof; E is D-Tyr, L-Tyr, or an analogue thereof; F is D-asparagine, L-asparagine, D-glutamine, or L-glutamine; G is D-Leu, L-Leu or an analogue thereof; H is D-Arg, L-Arg, or an analogue thereof; and I is D-Pro, L-Pro, or an analogue thereof; or a pharmaceutically acceptable salt thereof.

3. An LHRH analogue comprising a structure:

A--B--C--D--E--F--G--H--I--J

wherein A is pyro-Glu, Ac-Nal , Ac-Qal, Ac-Sar, or Ac-Pal, or an analogue thereof; B is His or 4-Cl-Phe, or an analogue thereof; C is Trp, Pal, Nal, Nal-Pal(N--O), or Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is Asn or Gln; G is Leu or Trp, or an analogue thereof, H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; I is Pro, or an analogue thereof; and J is Gly-NH.sub.2 or Ala-NH.sub.2, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

4. The LHRH analogue of claim 3, wherein said LHRH analogue comprises the structure:

wherein A is pyro-Glu, Ac-Nal , Ac-Qal, Ac-Sar, or Ac-Pal, or an analogue thereof; B is His or 4-Cl-Phe, or an analogue thereof; C is Trp, Pal, Nal, L-Nal-Pal(N--O), or Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is Asn; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; I is Pro, or an analogue thereof; and J is Gly-NH.sub.2 or Ala-NH.sub.2, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

5. An LHRH analogue comprising a structure:

A--B--C--D--E--F--G--H--I

wherein A is pyro-Glu, Ac-Nal , Ac-Qal, Ac-Sar, or Ac-Pal, or an analogue thereof; B is His or 4-Cl-Phe, or an analogue thereof; C is Trp, Pal, Nal, Nal-Pal(N--O), or Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is Asn or Gln; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; and I is Pro, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

6. The LHRH analogue of claim 5, wherein said LHRH analogue comprises the structure:

wherein A is pyro-Glu, Ac-Nal , Ac-Qal, Ac-Sar, or Ac-Pal, or an analogue thereof; B is His or 4-Cl-Phe, or an analogue thereof; C is Trp, Pal, Nal, L-Nal-Pal(N--O), or Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is Asn; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; and I is Pro, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

7. An LHRH analogue comprising a structure:

wherein A is pyro-Glu, Ac-D-Nal, Ac-D-Qal, Ac-Sar, or Ac-D-Pal, or an analogue thereof; B is His or 4-Cl-D-Phe, or an analogue thereof; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4--Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is D-Asn or D-Gln; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; I is Pro, or an analogue thereof; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

8. The LHRH analogue of claim 7, wherein said LHRH analogue comprises the structure:

wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal, or an analogue thereof; B is His or 4-Cl-D-Phe, or an analogue thereof; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is D-Asn; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; I is Pro, or an analogue thereof; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

9. An LHRH analogue comprising a structure:

wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal, or an analogue thereof; B is His or 4-Cl-D-Phe, or an analogue thereof; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is D-Asn or D-Gln; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; and I is Pro, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

10. The LHRH analogue of claim 9, wherein said LHRH analogue comprises the structure:

wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal, or an analogue thereof; B is His or 4-Cl-D-Phe, or an analogue thereof; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp, or an analogue thereof; D is Ser, or an analogue thereof; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile, or an analogue thereof; F is D-Asn; G is Leu or Trp, or an analogue thereof; H is Lys(iPr), Gln, Met, or Arg, or an analogue thereof; and I is Pro, or an analogue thereof;

or a pharmaceutically acceptable salt thereof.

11. An LHRH analogue comprising the structure B--C--D--E--F--G--H--I--J, wherein B is D-His, L-His, or an analogue thereof; C is D-Trp, L-Trp, or an analogue thereof; D is D-Ser, L-Ser, or an analogue thereof; E is D-Tyr, L-Tyr, or an analogue thereof; F is D-asparagine, L-asparagine, D-glutamine, or L-glutamine; G is D-Leu, L-Leu or an analogue thereof; H is D-Arg, L-Arg, or an analogue thereof; I is D-Pro, L-Pro, or an analogue thereof; and J is D-Gly, L-Gly, or an analogue thereof; or a pharmaceutically acceptable salt thereof.

12. The LHRH analogue of anyone of claims, 1, 2, 3, 5, 7, 9, or 11, wherein F is D-asparagine.

13. The LHRH analogue of anyone of claims 1, 2, 3, 5, 7, 9, or 11, wherein F is D-glutamine.

14. The LHRH analogue of anyone of claims 1, 2, 3, 5, 7, 9, or 11, wherein the LHRH analogue inhibits ovulation in at least 50% of treated rats in a standard rat antiovulatory assay at a dose of 5 .mu.g/rat and has an ED.sub.50 for histamine release of at least 3 .mu.g/ml.

15. The LHRH analogue of claim 14, which inhibits ovulation in at least 50% of treated rats in a standard rat antiovulatory assay at a dose of 2 .mu.g/rat.

16. The LHRH analogue of claim 14, which inhibits ovulation in at least 50% of treated rats in a standard rat antiovulatory assay at a dose of 1 .mu.g/rat.

17. The LHRH analogue of claim 14, which has an ED.sub.50 for histamine release of at least 5 .mu.g/ml.

18. The LHRH analogue of claim 14, which has an ED.sub.50 for histamine release of at least 10 .mu.g/ml.
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