Compounds having 5-HT6 receptor antagonist activity

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S299000, C544S349000, C546S112000

Reexamination Certificate

active

06897215

ABSTRACT:
Novel 6-bicyclopiperazinyl-1-arylsulfonylindole and 6-bicyclopiperidinyl-1-arylsulfonylindole compounds are disclosed which are useful as 5-HT6receptor antagonists in the treatment of central nervous system disorders such as schizophrenia, depression, ADHD, and cognition and memory dysfunction The compounds are Formula Iwherein: R1 is H or C1-4alkyl; X is CH, —C—OR3, ═C, or —N and Y is C-R2 or N; R3 is H or —C(O)-R4; R4 is H or a labile prodrug group; n is 1 or 2; m and o are, independently, 0, 1, or 2 with the proviso that m+o is 1 or 2; and Ar is an aryl or heteroaryl group optionally substituted with 1-3 substitutents.

REFERENCES:
patent: 6251893 (2001-06-01), Maddaford et al.
Robichaud et al. in Annual Reports in Medicinal Chemistry, vol. 35, p. 11-20 (2000).*
Isaac M et al: “6-bicyclopiperazinyl-1-arylsulfonylindole s and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists” Bioorganic & Medicinal Chemistry Letters, Oxford, GB, vol. 10, No. 15, Aug. 7, 2000, pp. 1719-1721, XP004213231 ISSN: 0960-894X the whole document.
Ward R P et al: “Localization of Serotonin Subtype 6 Receptor Messenger RNA in the Rat Brain by in situ Hybridization Histochemistry” Neuroscience, New York, NY, US, vol. 64, No. 4, 1995, pp. 1105-1111, XP000943569 ISSN: 0306-4522 cited in the application p. 1107, right-hand column -p. 1110, right-hand column.
Hoyer D and Martin G: “5-HT receptor classification and nomenclature: towards a harmonization with the human genome” Neuropharmacology, GB, Pergamon Press, Oxford, No. 36, Apr. 1, 1997, pp. 419-428, XPOO2075372 ISSN: 0028-3908 cited in the application table 1.

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