Pyrrole and pyrazole DAAO inhibitors

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

Reexamination Certificate

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Details

C514S419000, C514S423000, C548S361100, C548S374100, C548S530000

Reexamination Certificate

active

07488747

ABSTRACT:
Methods for increasing D-Serine concentration and reducing concentration of the toxic products of D-Serine oxidation, for enhancing learning, memory and/or cognition, or for treating schizophrenia, Alzheimer's disease, ataxia or neuropathic pain, or preventing loss in neuronal function characteristic of neurodegenerative diseases involve administering to a subject in need of treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt or solvate thereof:whereinR1and R2are independently selected from hydrogen, halo, nitro, alkyl, acyl, alkylaryl, and XYR5;or R1and R2, taken together, form a 5, 6, 7 or 8-membered substituted or unsubstituted carbocyclic or heterocyclic group;X and Y are independently selected from O, S, NH, and (CR6R7)n;R3is hydrogen, alkyl or M+;M is aluminum, calcium, lithium, magnesium, potassium, sodium, zinc ion or a mixture thereof;Z is N or CR4;R4is from selected from hydrogen, halo, nitro, alkyl, alkylaryl, and XYR5;R5is selected from aryl, substituted aryl, heteroaryl and substituted heteroaryl;R6and R7are independently selected from hydrogen and alkyl;n is an integer from 1 to 6;at least one of R1, R2and R4is other than hydrogen; andat least one of X and Y is (CR6R7)n.D-serine or cycloserine may be coadministered along with the compound of formula I.

REFERENCES:
patent: 5859042 (1999-01-01), Lee et al.
patent: WO 03/039540 (2003-05-01), None
Ashton et al., Nonpeptide Angiotensin II Antagonists Derived from 1H-Pyrazole-5-carboxylates and 4-Aryl-1-H-imidazole-5-carboxylates;J. Med. Chem.,1993, 36, pp. 3595-3605.
van Herk et al., Pyrazole Derivatives as Partial Agonists for the Nicotinic Acid Receptor, Journal of Medicinal Chemistry, 46(18):3945-51 (2003).

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