Cyclohexyl sulphone derivatives as gamma-secretase inhibitors

Details Cyclohexyl sulphone derivatives as gamma-secretase inhibitors Cyclohexyl sulphone derivatives as gamma-secretase inhibitors

2006-09-05

2006-09-05

Richter, Johann (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C514S424000, C514S557000, C514S562000, C514S602000, C514S613000, C514S210010, C514S210030, C548S542000, C544S124000, C544S158000

Reexamination Certificate

active

07101895

ABSTRACT:
Compounds of formula I:wherein Ar1and Ar2are optionally substituted aryl or heteroaryl, L is a bond, ═CH— or —(CHRa)n—, and X is SCN, SR1, S(O)R1, (CRaRb)mSO2R1, SO2N(R2)2, SO2NHCOR1, SO2NHN(R2)2, OSO2N(R2)2, OS(O)N(R2)2, OSO2NHCOR1, COR4, NHCOR1, NHCO2R1, NHCON(R2)2, NHSO2R1or NHSO2N(R2)2, inhibit the processing of APP by gamma secretase, and hence are useful in treatment of Alzheimer's disease.

REFERENCES:
patent: 2802013 (1957-08-01), Dodson
patent: 2812330 (1957-11-01), Dodson
patent: 2004/0082617 (2004-04-01), Harrison et al.
patent: 2004/0114496 (2004-06-01), Sogawa et al.
patent: 2004/0116404 (2004-06-01), Pineiro et al.
patent: 2004/0121995 (2004-06-01), Churcher et al.
patent: 2004/0171683 (2004-09-01), Pineiro
patent: 2004/0230054 (2004-11-01), Dinnell et al.
patent: 2005/0075320 (2005-04-01), Nadin et al.
patent: 2 473 374 (2003-07-01), None
patent: 0863134 (1998-09-01), None
patent: 1 466 898 (2004-10-01), None
patent: 56025149 (1981-03-01), None
patent: 56026847 (1981-03-01), None
patent: 56026866 (1981-03-01), None
patent: WO 00/50391 (2000-08-01), None
patent: WO 01/70677 (2001-09-01), None
patent: WO 02/081433 (2002-10-01), None
patent: WO 02/081435 (2002-10-01), None
patent: WO 03/018543 (2003-03-01), None
patent: WO 03/055850 (2003-07-01), None
patent: WO 03/059335 (2003-07-01), None
patent: WO 2004/013090 (2004-02-01), None
patent: WO 2004/031138 (2004-04-01), None
patent: WO 2004/048321 (2004-06-01), None
patent: WO 2004/101538 (2004-11-01), None
patent: WO 2004/101539 (2004-11-01), None
patent: WO 2005/000798 (2005-01-01), None
L. Capuano, et al., “Cyclische S-Oxide”, Chemische Berichte, vol. 112, pp. 1012-1022 (1979).
J.M. Decesare, et al.:, “Gamma- and Beta-epoxy sulfones. Formation of different ring-sized products upon reaction with CH3MgI or LiN[CH(CH3)2]2”, Canadian Journal of Chemistry., vol. 59, pp. 1415-1424 (1981).
O. Eisleb, “Neue Synthesen mittels Natriumamids”, Berichte der Deutschen Chemischen Gesellschaft, vol. 74, pp. 1433-1450 (1978).
J. Golinski, et al., “Reactions of Organic Anions; XVIV. Catalytic Two-Phase Alkylations of Benzyl Sulfones and Sulfonamides”, SYNTHESIS, No. 6, pp. 461-463 (1979).
P. Kisanga, et al., “Development, Synthetic Scope, and Mechanistic Studies of the Palladium-Catalyzed Cycloisomerization of Functionalized 1,6-Dienes in the Presence of Silane”, Journal of the American Chemical Society, vol. 122, No. 41, pp. 10017-10026 (2000).
C. Koradin, et al., “Cesium Catalyzed Addition of Nitriles to Alkynes”, SYNLETT, No. 10, pp. 1452-1454 (2000).
T. Oyuyama, et al., “Flash Photolytic Generation of a Dithio Carbocation from 1,3-Dithiolance Derivatives and Its Reaction with Nucleophiles”, Bulletin of the Chemical Society of Japan, vol. 64, No. 9, pp. 2751-2756 (1991).
M. Makosza, et al., “Ambiphilic Reactivity of 2,4-Djnitrobenzylp-Tolyl Sulfone Carbanion”, Polish Journal of Chemistry, vol. 72, pp. 1198-1201 (1998).
R. K. Norris, et al., “The Stereochemistry of the SRN1 Reaction In Some Cyclohexane Derivatives”, TETRAHEDRON, vol. 38, No. 8, pp. 1051-1057 (1982).
J. P. Scott et al., “Expedient Diels-Alder assembly of 4-aryl-4-phenylsulfonyl cyclohexanones”, Tetrahedron Letters, vol. 45, pp. 3345-3348 (2004).
E. W. Garbisch et al., “On the Mechanism of Benzylic Substituent Hydrogenolysis”, Journal of the American Chemical Society, vol. 89(16), pp. 4233-4235 (1967).
R. K. Norris et al., “An Example of Substitution proceeding with Retention in the SRN1 Reaction. Trapping of a Pyramidal Benzylic Radical by Benzenethiolate Ion”, J. of the Chem. Soc. Chem. Comm., Issue 3, pp. 79-80 (1981).

Affiliated with

Also associated with

Rating

Cyclohexyl sulphone derivatives as gamma-secretase inhibitors does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Cyclohexyl sulphone derivatives as gamma-secretase inhibitors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Cyclohexyl sulphone derivatives as gamma-secretase inhibitors will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3602276