Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Reexamination Certificate
2006-06-20
2006-06-20
Berch, Mark L. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
C544S091000, C544S048000, C206S570000, C549S068000
Reexamination Certificate
active
07064122
ABSTRACT:
The subject invention features compounds having the structure:wherein X is O, S, CH2or NR5; Y is O or S; R1is H, substituted or unsubstituted C1-C15alkyl, C1-C8alkylaryl, —C(O)OR4, —C(O)NR4R5, —CR6R6′OR4, —CR6R6′OC(O)R4, —CR6R6′OC(O)NHR7, —C(O)NR10R11, —C(O)NR8R9NR8R9, —N(R5)C(O)NHR5, or CH2R4; R2is a substituted or unsubstituted, straight chain C1—C30alkyl or branched C3-C30alkyl, aryl, alkylaryl, arylalkyl, heteroarylalkyl or cycloalkyl; R3is H or substituted or unsubstituted C1-C6alkyl or C3-C10cycloalkyl; R4is H or a substituted or unsubstituted, straight chain or branched, C6-C30alkyl, aryl, —CH2-aryl, aryl —C1-C15alkyl, heteroaryl-C1-C15alkyl or C3-C10cycloalkyl; R5is H or a substituted or unsubstituted, straight chain or branched, C6-C30alkyl, aryl C1-C30alkyl, heteroarylalkyl or cycloalkyl; R6and R6′are each independently H, substituted or unsubstituted C1-C6alkyl, dialkyl or C3-C10cycloalkyl or together form a 3-7 membered ring system; R7is H or substituted or unsubstituted C1-C12alkyl or C3-C10cycloalkyl; R8and R9are each independently H, substituted or unsubstituted C1-C6alkyl, C1-C6alkoxy, C1-C6alkylaryl, or NR8R9together form a substituted piperazine or piperidine ring or a dihydro-1H-isoquinoline ring system, or a specific enantiomer thereof, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating diabetes or obesity by administering a therapeutically effective amount of the compounds of the invention.
REFERENCES:
patent: 4598089 (1986-07-01), Hadvary et al.
patent: 4760063 (1988-07-01), Hallenbach et al.
patent: 5422335 (1995-06-01), Hagen et al.
patent: 6037340 (2000-03-01), Castelhano et al.
patent: 0129748 (1985-01-01), None
patent: WO9619482 (1996-06-01), None
patent: WO9727200 (1997-07-01), None
patent: WO9748707 (1997-12-01), None
patent: WO9845298 (1998-10-01), None
patent: WO9854192 (1998-12-01), None
patent: WO0030646 (2000-06-01), None
patent: WO0040247 (2000-07-01), None
patent: WO0040569 (2000-07-01), None
patent: WO0320282 (2003-03-01), None
Gutschow et al. {J. Med. Chem. (1999) 42:5437-5447}.
Gutschow, M. et al. “2-(Diethylamino)thieno[1,3]oxazin-4-ones as Stable Inhibitors of Human Leukocyte Elastase”J. Med. Chem. (1999) 42: 5437-5447 (Exhibit 2).
McKibben, B.P. et al., “Practical Synthesis of Tetrasubstituted Thiophenes for Use in Compound Libraries”Terrahedron Lett. (1999) 40: 5471-5474 (Exhibit 13).
Yoshisuke, T. et al.,Chem. Pharm. Bull. (1991) 39(1): 18-22 (Exhibit 14).
Tinney, F.J. et al., “Synthesis and antiallergy activity of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines”J. Med. Chem. (1981) 24: 878-882 (Exhibit 15).
Hadvary, P. et al., “Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin”Biochem. J. (1988) 256: 357-361 (Exhibit 16).
Hadvary, P. et al., “Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin”Biochem. J. (1988) 256: 357-361 (Exhibit 17).
Gutschow, M. and Neumann, U. “Novel Thieno[2,3-d][1,3]oxazin-4-ones as Inhibitors of Human Leukocyte Elastase”J. Med. Chem. (1998) 41(10):1729-1740 (Exhibit 18).
Wang, Z. et al., “A New Approach to the Synthesis of Heteroannulated 3,1-Oxazin-4-ones from β-Enamino Esters and Phosgeneiminium Salts”Synthesis(2000) 2: 255-258 (Exhibit 19); and.
Achakzi, D. et al., “Synthesis of Heterocondensed 6H-1,3-Oxazin-6-ones from N-Acylenamino Esters in the System Triphenylphosphane/Hexachloroethane/Triethylamine”Chem. Ber. (1981) 1 14(9): 3188-3194 (Exhibit 20).
Castelhano Arlindo
Witter David
Berch Mark L.
Cooper & Dunham LLP
Habte Kahsay
OSI Pharmaceuticals, Inc.
White, Esq. John P.
LandOfFree
Pancreatic lipase inhibitor compounds, their synthesis and use does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Pancreatic lipase inhibitor compounds, their synthesis and use, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Pancreatic lipase inhibitor compounds, their synthesis and use will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3636551