Melanocyte-stimulating hormone inhibitors

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

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C514S002600, C514S019300, C530S300000, C530S331000, C530S333000, C530S334000, C530S345000, C424S009100

Reexamination Certificate

active

09926391

ABSTRACT:
In the present specification is disclosed a melanocyte-stimulating hormone inhibitory composition which comprises, as the active ingredient, a di- or tripeptide derivative having a certain naphthyl group or the salts thereof, or a melanocyte-stimulating hormone inhibitory compound having a 50% inhibitory concentration of cAMP production (IC50) of 100 nM or less, which composition can prevent pigmentation, or can prevent, improve or recover from immune abnormality or immunodeficiency, or regulate body weight by appetite control, and also can be used as cosmetics or external preparations for the skin, and in addition, can be produced easily, and are excellent in the stability during storage.

REFERENCES:
patent: 2179979 (1939-11-01), Isler
patent: 3619196 (1971-11-01), Iwama et al.
patent: 4548926 (1985-10-01), Matsueda et al.
patent: 5861529 (1999-01-01), Baudoin et al.
patent: 6162828 (2000-12-01), Fukuda et al.
patent: 0 093 551 (1983-11-01), None
patent: WO 90/12814 (1990-11-01), None
patent: WO 95/12611 (1995-05-01), None
patent: WO 98/21229 (1998-05-01), None
patent: WO 00/11022 (2000-03-01), None
Etzkorn et al., J. Am. Chem. Soc. 1994, 116, 10412-10425.
Janecka et al. , J. Med. Chem. 38, 2922-2924 (1995).
J. M. Quillan, et al., vol. 92, pp. 2894-2898, “Combinatorial Diffusion Assay Used to Identify Topically Active Melanocyte-Stimulating Hormone Receptor Antagonists”, Mar. 1995.
A. Janecka, et al., “Reduced-Size Antogonists of Luteinizing Hormone-Releasing Hormone Active in Vitro”, J. Med. Chem., 38, 1995, XP-002125914, first page only.
F.A. Etzkoru, et al., “Cyclic Hexapeptides and Chimeric Peptides as Mimics of Tendamistat”, J. Am. Chem. Soc., 116, 1994, XP-002362517, first page only.
C.R. Noe, et al., “Studies on Cyclic Dipeptides, I: Aryl Modifications of Cyclo-(PHE-HIS)#”, Monatshefle Fuer Chemi, 127, 1996, XP-009059933, first page only.
M.D. Erion, et al., “Inhibition of Peptidylglycine Alpha-Amidating Monooxygenase by N-Substituted Homocysteine Analogs”, J. Med. Chem., 37, 1994, XP-002362519, first page only.
H. Harada, et al., “Synthesis of Human Renin Inhibitory Peptides, Angiotensinogen Transition-State Analogs Containing a Retro-Inverso Amide Bond”, Chem. Pharm. Bull., 38 (11), 1990, XP-000919337, first page only.
J.R. Luly, et al., “New Inhibitors of Human Renin That Contain Novel Leu-Val Replacements”, Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 30, No. 9, 1987, XP-001053395, first page only.
S. Gerisch, et al., “Enzymatic Peptide Synthesis in Frozen Aqueous Systems: Use of Nalpha-Unprotected Unusual Acyl Donors”, Tetrahedron: Asymmetry, vol. 6, No. 12, 1995, XP-004047955, first page only.
M. Akazome, et al., “Enantiomeric Inclusion of Alpha-Hydroxy Esters by (R)-(1-Naphtyl)Glycyl-(R)-Phenylglycine and the Crystal Structures of the Inclusion Cavities”, J. Org. Chem., 64, 1999, XP-002362520, first page only.
Y. Inai, et al., “Distance and Orientation Dependence of Electron Transfer and Exciplex Formation of Naphthyl and P-Dimethylanilino Groups Fixed on a Helical Polylpeptide Chain”, J. Phys. Chem., 94, 1990, XP-002362521, first page only.
A. Janecka, et al., “Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone Active in Vitro”, J. Med. Chem., 38, 1995, XP-002125914, pp. 2922-2924.
F.A. Etzkorn, et al., “Cyclic Hexapeptides and Chimeric Peptides as Mimics of Tendamistat”, J. Am. Chem. Soc., 116, 1994, XP-002362517, pp. 10412-10425.
C.R. Noe, et al., “Studies on Cyclic Dipeptides, I: Aryl Modifications of Cyclo-(PHE-HIS)#”, Monatshefte Fuer Chemi, 127, 1996, XP-009059933, pp. 1081-1097.
M.D. Erion, et al., “Inhibition of Peptidylglycine Alpha-Amidating Monooxygenase by N-Substituted Homocysteine Analogs”, J. Med. Chem., 37, 1994, XP-002362519, pp. 4430-4437.
H. Harada, et al., “Synthesis of Human Renin Inhibitory Peptides, Angiotensinogen Transition-State Analogs Containing a Retro-Inverso Amide Bond”, Chem. Pharm. Bull., 38 (11), 1990, XP-000919337, pp. 3042-3047.
J.R. Luly, et al., “New Inhibitors of Human Renin That Contain Novel Leu-Val Replacements”, Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 30, No. 8, 1987, XP-001053395, pp. 1609-1616.
S. Gerisch, et al., “Enzymatic Peptide Synthesis in Frozen Aqueous Systems: Use of Nalpha-Unprotected Unusual Acyl Donors”, Tetrahedron: Asymmetry, vol. 6, No. 12, 1995, XP-004047955, pp. 3039-3045.
M. Akazome, et al., “Enantiomeric Inclusion of Alpha-Hydroxy Esters by (R)-(1-Naphtyl)Glycyl-(R)-Phenylglycine and the Crystal Structures of the Inclusion Cavities”, J. Org. Chem., 64, 1999, XP-002362520, pp. 2293-2300.
Y. Inai, et al., “Distance and Orientation Dependence of Electron Transfer and Exciplex Formation of Naphthyl and P-Dimethylanilino Groups Fixed on a Helical Polylpeptide Chain”, J. Phys. Chem., 94, 1990, XP-002362521, pp. 6237-6243.
Abdel-Malek, Z., et al., “Mitogenic and Melanogenic Stimulation of Normal Human Melanocytes by Melanotropic Peptides,” Proc. Natl. Acad. Sci., Cell Biology, vol. 92, Feb. 1995, pp. 1789-1793.
Taylor, A. W., et al., “Alpha-Melanocyte-Stimulating Hormone Suppresses Antigen-Stimulated T Cell Production of Gamma-Interferon,” Neuroimmunomodulation 1994, vol. 1, pp. 188-194.
Hiltz, M. E., et al., “α-MSH Peptides Inhibit Acute Inflammation Induced in Mice by rIL-1β, rIL-6, rTNF-α and Endogenous Pyrogen but Not That Caused by LTB4, PAF and rIL-8,” Cytokine, vol. 4, No. 4, Jul. 1992, pp. 320-328.
Ludwig, D. S., et al., “Melanin-Concentrating Hormone: A Functional Melanocortin Antagonist in the Hypothalamus,” American Physiological Society, 1998, vol. 274, pp. E627-E633.
A. Janecka, et al., “Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone Active in Vitro”, J. Med. Chem., 38, 1995, XP-002125914, first page only, p. 2922-2924.
F.A. Etzkoru, et al., “Cyclic Hexapeptides and Chimeric Peptides as Mimics of Tendamistat”, J. Am. Chem. Soc., 116, 1994, XP-002362517, first page only, p. 10412-10423.
C.R. Noe, et al., “Studies on Cyclic Dipeptides, I: Aryl Modifications of Cyclo-(PHE-HIS)#”, Monatshefte Fuer Chemi, 127, 1996, XP-009059933, first page only p. 1081-1097.
M.D. Erion, et al., “Inhibition of Peptidylglycine Alpha-Amidating Monooxygenase by N-Substituted Homocysteine Analogs”, J. Med. Chem., 37, 1994, XP-002362519, first page only, p. 4430-4437.
H. Harada, et al., “Synthesis of Human Renin Inhibitory Peptides, Angiotensiogen Transition-State analogs Containing a Retro-Inverso Amide Bond”, Chem. Pharm. Bull., 38 (11), 1990, XP-000919337, first page only, p. 3042-3047.
J.R. Luly, et al., “New Inhibitors of Human Renin That Contain Novel Leu-Val Replacements”, Journal of Medicinal Chemistry, American Chemical Society. Washington, US, vol. 30, No. 9, 1987, XP-001053395, first page only, p. 1609-1616.
S. Gerisch, et al., “Enzymatic Peptide Synthesis in Frozen Aqueous Systems: Use of Nalpha-Unprotected Unusual Acyl Donors”, Tetrehedron: Asymmetry, vol. 6, No. 12, 1995, XP-004047955, first page only, p. 3039-3045.
M. Akazome, et al., “Enantiomeric Inclusion of Alpha-Hydroxy Esters by (R)-(1-Naphtyl)Glycyl-(R)-Phenylglycine and the Crystal Structures of the Inclusion Cavities”, J. Org. Chem., 64, 1999, XP-002362520, first page only, p. 2293-2300.
Y. Inai, et al., “Distance and Orientation Dependence of electron Transfer and Exciplex Formation of Naphthyl and P-Dimethylanilino Groups Fixed on a Helical Polylpeptide Chain”, J. Phys. Chem., 94, 1990, XP-002362521, first page only, p. 6237-6243.

LandOfFree

Say what you really think

Search LandOfFree.com for the USA inventors and patents. Rate them and share your experience with other people.

Rating

Melanocyte-stimulating hormone inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Melanocyte-stimulating hormone inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Melanocyte-stimulating hormone inhibitors will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-3920930

  Search
All data on this website is collected from public sources. Our data reflects the most accurate information available at the time of publication.