Substituted pyrazinone melanin concentrating hormone...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

Rate now

  [ 0.00 ] – not rated yet Voters 0   Comments 0

Details

C544S405000

Reexamination Certificate

active

08067420

ABSTRACT:
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula IwhereinR1, R2, R3, R8, and R9are defined herein.Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

REFERENCES:
patent: 3674836 (1972-07-01), Creger
patent: 3983140 (1976-09-01), Endo et al.
patent: 4027009 (1977-05-01), Grier et al.
patent: 4231938 (1980-11-01), Monaghan et al.
patent: 4346227 (1982-08-01), Terahara et al.
patent: 4379785 (1983-04-01), Weyer et al.
patent: 4448784 (1984-05-01), Glamkowski et al.
patent: 4450171 (1984-05-01), Hoffman et al.
patent: 4499289 (1985-02-01), Baran et al.
patent: 4613610 (1986-09-01), Wareing
patent: 4639436 (1987-01-01), Junge et al.
patent: 4647576 (1987-03-01), Hoefle et al.
patent: 4681893 (1987-07-01), Roth
patent: 4686237 (1987-08-01), Anderson
patent: 4759923 (1988-07-01), Buntin et al.
patent: 4871721 (1989-10-01), Biller
patent: 4904769 (1990-02-01), Rauenbusch
patent: 4924024 (1990-05-01), Biller
patent: 5006530 (1991-04-01), Angerbauer et al.
patent: 5011930 (1991-04-01), Fujikawa et al.
patent: 5177080 (1993-01-01), Angerbauer et al.
patent: 5260440 (1993-11-01), Hirai et al.
patent: 5273995 (1993-12-01), Roth
patent: 5354772 (1994-10-01), Kathawala
patent: 5385929 (1995-01-01), Bjorge et al.
patent: 5447954 (1995-09-01), Gribble et al.
patent: 5488064 (1996-01-01), Sher
patent: 5491134 (1996-02-01), Sher et al.
patent: 5506219 (1996-04-01), Robl
patent: 5541204 (1996-07-01), Sher et al.
patent: 5594016 (1997-01-01), Ueno et al.
patent: 5595872 (1997-01-01), Wetterau et al.
patent: 5612359 (1997-03-01), Murugesan
patent: 5691322 (1997-11-01), Robl
patent: 5698527 (1997-12-01), Kim
patent: 5712396 (1998-01-01), Magnin et al.
patent: 5753675 (1998-05-01), Wattanasin
patent: 5770615 (1998-06-01), Cheng et al.
patent: 5776983 (1998-07-01), Washburn et al.
patent: 6043265 (2000-03-01), Murugesan et al.
patent: 6159980 (2000-12-01), Arvanitis et al.
patent: 6414002 (2002-07-01), Cheng et al.
patent: 0 221 025 (1987-05-01), None
patent: 0 142 146 (1988-08-01), None
patent: 0 675 714 (1999-01-01), None
patent: 0 818 448 (2003-11-01), None
patent: 1 022 272 (2004-05-01), None
patent: 0 992 496 (2005-08-01), None
patent: 2 596 393 (1986-04-01), None
patent: 2 205 837 (1988-12-01), None
patent: 2 304 106 (1996-08-01), None
patent: WO 86/03488 (1986-06-01), None
patent: WO 86/07054 (1986-12-01), None
patent: WO 97/46226 (1997-05-01), None
patent: WO 97/21993 (1997-06-01), None
patent: WO 97/48701 (1997-12-01), None
patent: WO 99/00353 (1999-01-01), None
patent: WO 00/01389 (2000-01-01), None
patent: WO 00/15201 (2000-03-01), None
patent: WO 00/30665 (2000-06-01), None
patent: WO 00/38722 (2000-07-01), None
patent: WO 00/39077 (2000-07-01), None
patent: WO 00/50574 (2000-08-01), None
patent: WO 2007/071646 (2007-06-01), None
patent: WO2009/001132 (2008-12-01), None
Borowsky, B. et al. “Antidepressant, anxiolytic and anorectic effects of a melanin-concentrating hormone-1 receptor antagonist”, Nature Medicine vol. 8, No. 8:825-830, (2002).
Biller et al., “Isoprenoid (Phosphinylmethyl)phosphonates as inhibitor of Squalene Synthetase”, J. Med. Chem., vol. 31, No. 10, pp. 1869-1871 (1988).
Biller et al., “Squalene Synthetase Inhibitors”, Curr. Pharm. Des, 2, pp. 1-40 (1996).
Capson, T.L., “Synthesis and Evaluation of Ammonium Analogs of Carbocationic Intermediates in Squalene Biosynthesis”, Dept. Med. Chem. U of Utah, Table of Contents pp. 16, 17, 40-43, 48-51, Summary, (1987).
Corey, E. J. et al, “Application of Unreactive Analogs of Terpenoid Pyrophosphates of Studies of Multistep Biosynthesis. Demonstration That ‘Presqualene Pyrophosphate’ is Essential Intermediate on the Path to Squalene”, J. Amer. Chem. Soc. 98, pp. 1291-1293 (1976).
Ghiselli, G., “The pharmacological profile of FCE 27677: a novel ACAT inhibitor with potent hypolipdemic activity mediated by selective suppression of the hepatic secretion of ApoB100-containing lipoprotein”, Cardiovasc. Drug Rev. 16(1):16-30(1998).
Hara, S., “Ileal Na+/bile acid Contransporter Inhibitors”, Drugs of the Future, 24(4), pp. 425-430 (1999).
Kowalski, T. et al., “Melanin-concentrating hormone-1 receptor antagonism decreases feeding by reducing meal size”, European Journal of Pharmacology 497:41-47 (2004).
Kowalski, T. et al., “Therapeutic potential of melanin-concentrating hormone-1 receptor antagonists for the treatment of obesity”, Expert Opin. Investing. Drugs 13(9):1113-1122 (2004).
Krause, B.R. et al. “ACAT Inhibitors: Physiologic Mechanisms for Hypolipidemic and Anti-Atherosclerotic Activities in Experimental Animals”, Inflammation: Mediators and Pathways, CRC Press Inc, publ., Ruffolo, Jr., R.R. et al., eds., pp. 173-198 (1995).
Ljung, B. et al., “AZ 242, a novel PPARα/γ agonist with beneficial effects on insulin resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats”, Journal of Lipid Research vol. 43:1855-1863 (2002).
McClard, R.W. et al., “Novel Phosphonylphosphinyl (P-C-P-C) Analogues of Biochemically Interesting Diphosphates. Syntheses and Properties of P-C-P-C Analogues of Isopentenyl Diphosphate and Dimethylallyl Diphosphate”, J. Am. Chem. Soc. 109, pp. 5544-5545 (1987).
Nicolosi et al., “The ACAT inhibitor, C1-1011 is effective in the prevention and regression of aortic fatty streak area in hamsters”, Atherosclerosis 137(1):77-85 (1998).
Ortiz de Montellano, P. et al., “Inhibition of Squalene Synthetase by Farnesyl Pyrophosphate Analogues”, J. Med. Chem., 20:243-249 (1977).
Rosenblum, S.B. et al., “Discovery of 1-(4-Fluorophenyl)-(3R)-[3-(4-fluorophenyl)-(3S)-hydroxypropyl]-(4S)-(4-hydroxyphenyl)-2-azetidinone (SCH 58235): A Designed, Potent, Orally Active inhibitor of Cholesterol Absorption”, J. Med. Chem. 41, pp. 973-980 (1998).
Salisbury, B.G. et al., “Hypocholesterolemic activity of a novel inhibitor of cholesterol absorption, SCH 48461”, Atherosclerosis, vol. 115, pp. 45-63 (1995).
Sliskovic, D.R. et al., “ACAT Inhibitors: Potential Anti-atherosclerotic Agents”, Current Medicinal Chemistry, vol. 1, No. 3, pp. 204-225 (1994).
Smith, C. et al., “RP 73163: A Bioavailable Alkylsulphinyl-diphenylimidazole ACAT inhibitor”, Bioorganic & Med. Chem. Lett., vol. 6, No. 1, pp. 47-50, (1996).
Stout, et al., “Inhibitors of acyl-CoA:cholesterol O-acyl transferase (ACAT) as hypocholeserolemic agents. 6. . . . ” Chemtracts: Org. Chem., 8(6):359-362 (1995).
Sorbera, L.A. et al., “Treatment of Lipoprotein Disorders ACAT Inhibitor”, Drugs of the Future, 24(1), pp. 9-15 (1999).
Takekawa, S. et al., “T226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist”, European Journal of Pharmacology 438, pp. 129-135 (2002).
Ulven, T. et al., “6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode”, J. Med. Chem. 48:5684-5697 (2005).
Yajima, K. et al., “Combination Therapy with PPARγ and PPARα agonists increases glucose-stimulate insulin secretion indb/dbmice”, Am. J. Physiol. Endocrinol. Metab. 284:E966-E971 (2003).
Database Registry [Online] Chemical Abstracts Service, Columbus, Ohio, US; Jul. 17, 2006, XP002512332 retrieved from STN see CAS Registry Nos. 893789-93-0; 893789-91-8 abstr

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

Substituted pyrazinone melanin concentrating hormone... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Substituted pyrazinone melanin concentrating hormone..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted pyrazinone melanin concentrating hormone... will most certainly appreciate the feedback.

Rate now

     

Profile ID: LFUS-PAI-O-4279906

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