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Details for Patent: 7,071,165

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Details for Patent: 7,071,165

Title:LHRH antagonist peptides
Abstract: Novel LHRH antagonist peptides, pharmaceutical compositions thereof, and methods of use thereof, are disclosed. The LHRH antagonist comprise a peptide compound, wherein a residue of the peptide compound corresponding to the amino acid at position 6 of natural mammalian LHRH comprises a hydrophilic N-acyl moiety, a dipolar moiety, a sulfonium moiety, a receptor-modifying moiety or a small polar moiety.
Inventor(s): Roeske; Roger W. (Indianapolis, IN)
Assignee: Indiana University Research and Technology Corporation (Indianapolis, IN)
Filing Date:Apr 05, 2002
Application Number:10/117,364
Claims:1. A method of rejuvenating the thymus in a subject, comprising administering to the subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comprises a structure: A-B-C-D-E-F-G-H-I-J wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal; B is His or 4-Cl-D-Phe; C is Trp, D-Pal, D-Nal, L-Nal, D-Pal(N--O), or D-Trp; D is Ser; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile; F is D-Asn or D-Gln; G is Leu or Trp; H is Lys(iPr), Gin, Met, or Arg; I is Pro; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof, thereby rejuvenating the thymus in the subject.

2. A method of rejuvenating the thymus in a subject comprising administering to the subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comPrises a structure: A-B-C-D-E-F-G-H-I-J wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal; B is His or 4-Cl-D-Phe; C is Trp, D-Pal, D-Nal, L-Nal, D-Pal(N--O), or D-Trp; D is Ser; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Arg or Ile; F is D-Asn; G is Leu or Trp; H is Lys(iPr), Gin, Met, or Arg; I is Pro; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof, thereby rejuvenating the thymus in the subject.

3. The method of any one of claims 1 or 2, wherein said peptide compound comprises a structure: Ac-D-Nal-4-Cl-Phe-D-Pal-Ser-N-Me-Tyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala-NH.sub.- 2; or a pharmaceutically acceptable salt thereof.

4. The method of any one of claim 1 or 2, wherein said peptide compound comprises a structure: Ac-D-Nal-4-Cl-D-Phe-D-Pal-Ser-Tyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof.

5. A method of rejuvenating the thymus in a subject, comprising administering to a subject an effective amount of a peptide compound which inhibits LHR.H activity, wherein the peptide compound comprises 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, thereby rejuvenating the thymus in the subject.

6. The method of claim 5, wherein the peptide compound comprises the 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, 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.

7. A method of rejuvenating the thymus in a subject, comprising administering to a subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comprises 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, thereby rejuvenating the thymus in the subject.

8. The method of claim 7, wherein the peptide compound comprises the 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, 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.

9. A method of rejuvenating the thymus in a subject, comprising administering to a subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comprises a structure: A-B-C-D-E-F-G-H-I 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, Mg 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, thereby rejuvenating the thymus in the subject.

10. The method of claim 9, wherein the peptide compound comprises the structure: A-B-C-D-E-F-G-H-I 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, Mg 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. The method of any one of claim 1 or 2, wherein said subject is an immunosuppressed subject.

12. A method of stimulating the production of T cells in a subject, comprising administering to the subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comprises a structure: A-B-C-D-E-F-G-H-I-J wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal; B is His or 4-Cl-D-Phe; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp; D is Ser; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Mg or Ile; F is D-Asn or D-Gln; G is Leu or Trp; H is Lys(iPr), Gln, Met, or Arg; I is Pro; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof, thereby stimulating the production of T cells in the subject.

13. A method of stimulating the production of T cells in a subject, comprising administering to the subject an effective amount of a peptide compound which inhibits LHRH activity, wherein the peptide compound comprises a structure: A-B-C-D-E-F-G-H-I-J wherein A is pyro-Glu, Ac-D-Nal , Ac-D-Qal, Ac-Sar, or Ac-D-Pal; B is His or 4-Cl-D-Phe; C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N--O), or D-Trp; D is Ser; E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, Asn, Met, Ala, Mg or Ile; F is D-Asn; G is Leu or Trp; H is Lys(iPr), Gln, Met, or Arg; I is Pro; and J is Gly-NH.sub.2 or D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof, thereby stimulating the production of T cells in the subject.

14. The method of any one of claim 12 or 13 wherein said peptide compound comprises a structure: Ac-D-Nal-4-Cl-D-Phe-D-Pal-Ser-Tyr-D-Asn-Leu-Lys(iPr)-Pro-D-Ala-NH.sub.2; or a pharmaceutically acceptable salt thereof.
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