Substituted arylpyrazines

Details Substituted arylpyrazines Substituted arylpyrazines

2007-04-10

2007-04-10

Tucker, Zachary C. (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

C544S405000

Reexamination Certificate

active

11107148

ABSTRACT:
Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1receptors, including human CRF1receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.

REFERENCES:
patent: 4211870 (1980-07-01), Barnett et al.
patent: 4293552 (1981-10-01), Miesel
patent: 4788197 (1988-11-01), Wakabayashi et al.
patent: 1499768 (1975-05-01), None
patent: 3048666 (1991-03-01), None
patent: WO 95/10506 (1995-04-01), None
patent: WO 99/38829 (1998-01-01), None
patent: WO 98/11075 (1998-03-01), None
patent: WO 98/38174 (1998-09-01), None
patent: WO 98/43641 (1998-10-01), None
patent: WO 00/12488 (2000-03-01), None
patent: WO 00/45800 (2000-08-01), None
Thompson et al, “An Efficient Synthesis of Arylpyrazines and Bipyridines” Journal of Organic Chemistry, vol. 53(9), pp. 2052-2055 (1988).
Nakamura et al, “Synthesis of 5- and 3-,5-disubstituted 2-aminopyrazines by Pd Mediated Stille Coupling” SYNLETT, vol. 12, pp. 1227-1228 (1995).
The Merck Index, 13thEd., p. 1082, Entry # 6088: “Methylene Chloride.” Merck & Co., Inc. Whitehouse Station, NJ © 2001.
Akita et al., “Cross-Coupling Reaction of Chloropyrazines with Acetylenes,”Chem. Pharm. Bull.34(4), 1447-1458(1986).
Alvernhe et al., “Action de L'acide Fluorhydrique Sure Les Azirines: Synthese D'a-fluorectones et de Difluoramines—Etude De L'orientation de la Reaction,”Tetrahedron Letters, vol. 21, 1437-1440, (1980).
Badiger et al., “Oxidative Cyclization Using Fetizone's Reagent,”Indian J. of Chem., vol. 16B, 71-75, (1978).
Benincori et al., “Studies on the Fischer Indole Synthesis: Rearrangements of Five-Six- and Seven-membered Cyclic Hydrazones of Pyrazoline, Tetrahydropyridazine and Tetrahydro-1,2-diazepin Series in Polyphosphoric Acid,”J. Chem. Soc. Perkin Trans., 2139-2145, (1991).
Bremner et al., “Elevated CSF Corticotropin-Releasing Factor Concentrations in Posttraumatic Stress Disorder,”Am. J. of Psychiatry, vol. 154(5), 624-629, (1997).
Chellappa et al., “PMR Spectra of Some Substituted Pyrazines & 2,3-Dihydropyrazines,”Indian J. of Chem., vol. 21B, 778-779, (1982).
Heinrichs et al., “Anti-Stress Action of a Corticotropin-Releasing Factor Antagonist on Behavioral Reactivity to Stressors of Varying Type and Intensity,”Neuropsychopharmacology, vol. 11(3), 179-186, (1994).
Iredale et al., “Differential Regulation of Corticotropin-Releasing Factor Receptor Expression by Stress and Agonist Treatments in Brain and Cultured Cells,”Mol. Pharm., vol. 50, 1103-1110, (1996).
Kalin et al., “Restraint stress increases corticotropin-releasing hormone mRNA content in the amygdala and paraventricular nucleus,”Brain Res., vol. 656, 182-186, (1994).
Menzaghi et al., “Characterization of a Novel and Potent Corticotropin-Releasing Factor Antagonist in Rats,”J. of Pharm. And Exp. Therapeutics, vol. 269(1), 564-572, (1994).
Mitchell et al., “The Role of Corticotropin Releasing Factor in Depressive Illness: a Critical Review,”Neuroscience and Biobehavioral Reviews, vol. 22(5), 635-651, (1998).
Ohta et al., “Anti-Platelet Aggregation Activity of Some Pyrazines,”Biol. Pharm. Bull., vol. 20(10), 1076-1081, (1997).
Ohta et al., “Coupling Reaction of Chloropyrazines and their N-Oxides with Tetraphenyltin,”Heterocycles, vol. 24(3), 785-792, (1986).
Schulz et al., “CP-14,26: A Potent and Selective Nonpeptide Antagonist of Corticotropin releasing factor Receptors,”Proc. Natl. Acad. Sci. USA, vol. 93, 10477-10482, (1996).
Smagin et al., “Corticotropin-Releasing Factor Receptor Antagonist infused into the locus coeruleus attenuates immobilization stress-induced defensive withdrawal in rats,”Neuroscience Letters, vol. 220, 167-170, (1996).
Smagin et al., “CRF Receptor Antagonists Attenuates Immobilization Stress-Induced Norepinephrine Release in the Prefrontal Cortex in Rats,”Brain Res. Bull., vol. 42(6), 431-434, (1997).
Taylor et al., “Intramolecular Diels-Alder Reactions of 1,2,4-Triazines. Route to Condensed Pyrazines via Cycloaddition of Nitrile Dienophiles,”J. Org. Chem., vol. 54, 1245-1249, (1989).
Taylor et al., “Synthesis of Pyridines by Diels-Alder Reactions of Hetero-Substituted 1,2,4-Triazines with Enamines and an Enaminone,”J. Org. Chem., vol. 54, 1249-1256, (1989).
Vinot and Pinson, “No. 797.—Synthese de pyrazines,”Bulletin de la Société Chimique de France, No. 12, 4970-4974, (1968).
Yamagami et al. “Measurement and Prediction of Hydrophobicity Parameters for Highly Lipophilic Compounds: Application of the HPLC Colum-Switching Technique to Measurement of log P of Diarylpyrazines,”J. of Pharm. Sciences, vol. 88(12), 1299-1304, (1999).
CAS Printout of Hamazaki et al., Chem. Abs. 100:5477, (1984).
CAS Printout of Hori et al., Chem. Abs. 80:890, (1974).
CAS Printout of McCapra et al., Chem. Abs. 79:125387, (1973).
CAS Printout of Miesel et al., Chem. Abs. 96:35307, (1982).
CAS Printout of Rees et al. (WO 98/43641), (1998).
CAS Printout of Teranishi et al. (JP 10077286) (1998).
CAS Printout of Teranishi et al., (JP 1998-184331), (1998).
CAS Printout of Teranishi et al., Chem. Abs. 114:101506, (1991).

Affiliated with

Also associated with

Rating

Substituted arylpyrazines 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 arylpyrazines, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Substituted arylpyrazines will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3804340