Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai
Reexamination Certificate
2006-04-25
2006-04-25
Russel, Jeffrey Edwin (Department: 1654)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Peptide containing doai
C530S330000
Reexamination Certificate
active
07034004
ABSTRACT:
The subject invention provides novel peptides for use in treating mammals to control appetite and obesity. Disclosed is a peptide derivative having the formula:in-line-formulae description="In-line Formulae" end="lead"?X1-Z-Q-arg-trp-NH12in-line-formulae description="In-line Formulae" end="tail"?wherein: X1is an acyl group, Z is amino-2-naphthyl-carboxylic acid or histidine, Q is (D)phenylalanine or p-iodo-(D)phenylalanine, or a pharmacologically acceptable salt, complex or derivative thereof, the peptide derivative having melanocortin-4 receptor agonist activity.
REFERENCES:
patent: 5420109 (1995-05-01), Suto et al.
patent: 5726156 (1998-03-01), Girten et al.
patent: 5741774 (1998-04-01), Girten et al.
patent: 5760001 (1998-06-01), Girten et al.
patent: 5786332 (1998-07-01), Girten et al.
patent: 5888969 (1999-03-01), Girten et al.
patent: 5908609 (1999-06-01), Lee et al.
patent: 6245738 (2001-06-01), Suto et al.
patent: 6284735 (2001-09-01), Girten et al.
patent: 6613874 (2003-09-01), Mazur et al.
patent: 2001/0056179 (2001-12-01), Chen et al.
patent: WO 97/47316 (1997-12-01), None
Jerry Ryan Holder et al., “Structure-Activity Relationships of the Melanocortin Tetrapeptide Ac-His-Dphe-Arg-Trp-NH2at Mouse Melanocortin Receptors. I. Modifications at the His Position”, J. Med. Chem. 2002, 45, pp 2801-2810.
Jerry Ryan Holder et al., “Structure-Activity Relationships of the Melanocortin Tetrapeptide Ac-His-Dphe-Arg-Trp-NH2at Mouse Melanocortin Receptors:Part .Modifications at the Phe Position”, J. Med. Chem. 2002, 45, pp 3073-3081.
I. Lee et al., “Change in Body Weight and Longevity”, Oct. 21, 1992, JAMA, vol. 268, No. 15, pp 2045-2049.
J. McGinnis et al., “Actual Causes of Death in the United States”, Nov. 10, 1993, MA., vol. 270, No. 18, pp 2207-2212.
G. Colditz G., Economic Costs of Obesity1-3, 1992 AM J. Clin Nutr. 55, pp 503S-507S.
“Methods for Voluntary Weight Loss and Control”, NIH Technology Assessment Conference Panel, 1993, Ann Intern Med. vol. 119, No. 7, pp 764-770.
“Long-Term Pharmacotherapy in the Management of Obesity”, National Task Force on Obesity, 1996, JAMA, vol. 276, No. 23, pp 1907-1915.
F. Greenway, “Surgery for Obesity”, Endo Metab Clin N Amer., vol. 25, (4), Dec. 1996, pp 1005-1027.
S. Long et al., “Weight Loss in Severely Obese Subjects Prevents the Progression of Impaired Glucose Tolerance to Type II Diabetes”, May 1994, Diabetes Care, vol. 17, No. 5, pp 372-375.
“Gastrointestnal Surgery for Severe Obesity”, NIH Conference, Dec. 1991, Ann Intern Med., vol. 115, No. 12, pp 956-961.
C. Ezzell, “Fat Times for Obesity Research: Tons of New Information, But How Does it All Fit Together”, J. NIH Res. 7, pp 39-43(Oct. 1995).
Trish Gura, “Obesity Sheds Its Secrets”, Science, vol. 275, pp 751-753 (Feb. 7, 1997).
Jeffrey S. Flier, “Leptin Expression and Action: New Experimental Paradigms”, Proc. Natl. Acad. Sci. USA 94 (1997), pp 4242-4245 (Apr. 1997).
W. Chen et al., “Exocrine Gland Dysfunction in MC5-R-Deficient Mice: Evidence for Coordinated Regulation of Exocrine Gland Function by Melanocortin Peptides”, Cell, Dec. 1997, vol. 91, pp 789-798.
W. Fan et al., “Role of Melanocortinergic Neurons in Feeding and the Agouti Obesity Syndrome”, Nature, Jan. 1997, vol. 385, pp 165-168.
D. Huszar et al., “Targeted Disruption of the Melanocortin-4 Receptor Results in Obesity in Mice”, Cell, Jan. 1997, vol. 88, pp 131-141.
A.A. Butler et al., “A Unique Metabolic Syndrome Causes Obesity in the Melanocortin-3 Receptor-Deficient Mouse”, Endocrinology, 2000, vol. 141, No. 9, pp 3518-3521.
A.S. Chen et al., “Inactivation of the Mouse Melanocortin-3 Receptor Results in Increased Fat Mass and Reduced Lean Body Mass.”, Nat Genet, Sep. 2000, vol. 26, pp 97-102.
D. Lu et al., “Agouti Protein is an Antagonist of the Melanocyte-Stimulating-Hormone Receptor”, Nature, Oct. 1994, vol. 371, pp 799-802.
J.R. Shutter et al., “Hypothalamic Expression of ART, a Novel Gene Related to Agouti, is Up-Regulated in Obese and Diabetic Mutant Mice”, Genes & Development, 1997, vol. 11, pp 593-602.
M.M. Ollman et al., “Antagonism of Central Melanocortin Receptors in Vitro and in Vivo by Agouti-Related Protein”, Science, Oct. 1997, vol. 278, pp 135-138.
C. Haskell-Luevano et al., “Characterization of Melanocortin NDP-MSH Agonist Peptide Fragments at the Mouse Central and Peripheral Melanocortin Receptors”, J. Med. Chem., 2001, vol. 44, pp 2247-2252.
Y. Yang et al., “Molecular Determinants of Ligand Binding to the Human Melanocortin-4 Receptor”, Biochemistry 2000, vol. 39, pp 14900-14911.
P. Grieco et al., “New Dimensions in the Design of Potent and Receptor Selective Melanotropin Analogues”.In Peptides for the New Millenium, Proceedings of the 16thAmerican Peptide Symposium, pp 541-542, not dated.
P. Grieco et al., Design and Synthesis of Highly Potent and Selective Melanotropin Analogues of SHU9119 Modified at Position 6, Biochemical and Biophysical Research Communications, vol. 292, No. 4, pp 1075-1080 (2002).
W. Danho et al., Highly Selective Cyclic Peptides for Human Melanocortin-4 Receptor (MC-4 R): Design, Synthesis, Bioactive Conformation, and Pharmacological Evaluation as an Anti-obesity Agent. InProceedings of the 2ndInternational /17thAmerican Peptide Symposium, pp 701-703 (2001).
M.J. Kavaranq et al., The Development of a Novel Highly Selective and Potent Agonist for Human Melanocortin 4 Receptor InProceedings of the 2ndInternational/17thAmerican PeptideSymposium, pp 708-709 (2001).
E. Kaiser et al., “Color Test for Detection of Free Terminal Amino Groups in the Solid-Phase Synthesis of Peptides”, Anal. Biochem., 1970, vol. 34, pp 595-598.
C. Haskell-Luevano et al., “Structure Activity Studies of the Melanocortin-4 Receptor by In Vitro Mutagenesis: Identification of Agouti-Related Protein (AGRP), Melanocortin Agonist and Synthetic Peptide Antagonist Interaction Determinants”, Biochemistry 2001, vol. 40, No. 20, pp 6164-6179.
H. Schild, pA2, A New Scale for the Measurement of Drug Antagonism.,Brit. J. Pharmacol.1947, vol. 2, pp 189-206.
L. Roselli-Rehfuss et al., “Identification of a Receptor for γMelanotropin and Other Proopiomelanocortin Peptides in the Hypothalamus and Limbic System”,Proc. Natl. Acad. Sci.USA, Oct. 1993, vol. 90, pp 8856-8860.
I. Gantz et al., “T. Molecular Cloning of a Novel Melancortin Receptor”,J. Biol. Chem., Apr. 1993, vol. 268, No. 11, pp 8246-8250.
I. Gantz et al., “Molecular Cloning, Expression, and Gene Localization of a Fourth Melanocortin Receptor”,J. Biol. Chem., Jul. 1993, vol. 268, No. 20, pp 15174-15179.
K.G. Mountjoy et al., “Localization of the Melanocortin-4 Receptor (MC4-R) in Neuroendocrine and Automated Control Circuits in the Brain”,Mol. Endo.1994, 8, pp 1298-1308.
F. Al-Obeidi et al., “Design of a New Class of Superpotent Cyclic α-Melanotropins Based on Quenched Dynamic Simulations”,J. Am. Chem. Soc.1989, vol. 111, No. 9, pp 3413-3416.
F. Al-Obeidi et al. Potent and Prolonged Acting Cyclic Lactam Analogues of α-Melanotropin: Design Based on Molecular Dynamics.,J. Med. Chem.1989, vol. 32, No. 12, pp 2555-2561.
V.J. Hruby et al., “Cyclic Lactam α-Melanotropin Analogues of Ac-Nle4-c(Asp5,Dphe7, Lys10)-α-MSH(4-10)-NH2with Bulky Aromatic Amino Acids at Position 7 Show High Antagonist Potency and Selectivity at Specific Melanocortin Receptors”,J. Med Chem.1995, vol. 38, No. 18, pp. 3454-3461.
S.C. Benoit et al., “A Novel Selective melanocortin-4 Receptor Agonist Reduces Food Intake in Rats and Mice Without Producing Aversive Consequences”, J. Neurosci May 2000, 20(9), pp 3442-3448.
M.A. Bednarek et al., Analogs of MTII, Lactan Derivatives of α-Melanotropin, Modified at the N-T
Haskell-Luevano Carrie
Holder Jerry Ryan
Russel Jeffrey Edwin
Saliwanchik Lloyd & Saliwanchik
University of Florida
LandOfFree
Peptides and methods for the control of obesity does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Peptides and methods for the control of obesity, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Peptides and methods for the control of obesity will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3563732