Luteinizing hormone releasing hormone analogs

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

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514 2, 514800, 530313, 530328, 938110, A61K 3800, A61K 3824, A01N 3718, C04K 500

Patent

active

057835624

ABSTRACT:
A method is provided for the design and synthesis of Leuteinizing Hormone Releasing Hormone (LHRH) antagonists having exact amino acid sequences and containing 5-100 amino acids. This method can be used to produce peptides useful in treating disorders of the reproductive endocrine system, including endometriosis, precocious puberty, prostate cancer and breast cancer. Additionally, peptides produced by this method can be used as contraceptives for either males or females. Peptides produced by this method can further be employed in the diagnosis and treatment of infertility.

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Karl Folkers, et al., Increased Potency of Antagonists of the Luteinizing Releasing Hormone Which Have D-3-PAL in Position 6, Biochemical and Biophysical Research Communications, Jun. 13, 1986, vol. 137, No. 2, pp. 709-715.
Karl Folkers, et al., Activities of Antagonists of the Luteinizing Hormone Releasing Hormone with Emphasis on Positions 1, 5 and 6 and on Positions 1, 2 and 3. Z. Naturforsch. 42b, 101-106 (1987); received Jul. 18, 1986.
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Karl Folkers, et al., Increased Potency of Antagonists of the Luteinizing Hormone Releasing Hormone Which Have D-3-PAL in Position 6, Biochemical and Biophysical Research Communications, Jun. 13, 1986, vol. 137, No. 2, pp. 709-715.
R.W. Roeske et al., LHRH Antagonists with Low Histamine Releasing Activity, pp. 17-24.
Liu Ke-Liang et al., Synthesis and Bioactivities of New LHRH Antagonists Containing Novel Unnatural Amino Acids at Position File. vol. 34 No. 2 Received Jul. 3, 1989.
Marvin J. Karten et al., Gonadotropin-Releasing Hormone Analog Design. Structure-Function Studies toward the Development of Agonists and Antagonists: Rationale and Perspective. Vo. 7, No. 1.
Karl Folkers et al., Activities of Antagonists of the Luteinzing Hormone Releasing Hormone with Emphasis on Positions 1, 5 and 6 and on Positions 1, 2 and 3. Z. Naturforsch. 42b, 101-106 (1987); received Jul. 18, 1986.
Karl Folkers et al., Relative Potencies of Antagonists of the Luteinizing Hormone Releasing Hormone with Lys.sup.8 and Arq.sup.8 and Substitutions in Positions 3, 5, 6, 7 and 8. pp. 1087-1091 (1986); received Jun. 10, 1986.
Kelliang Liu et al., Antagonists of luteinizing hormone releasing hormone with novel unnatural amino acids at position six. Int. J. Peptide Protein Res. 35, 1990, 157-160.

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