6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which provide...

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

C514S274000

Reexamination Certificate

active

07087615

ABSTRACT:
The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula:wherein R comprises ethers or amines;R1is:a) substituted or unsubstituted aryl; orb) substituted or unsubstituted heteroaryl;each R2unit is independently selected from the group consisting of:a) hydrogen;b) —(CH2)jO(CH2)nR8;c) —(CH2)jNR9aR9b;d) —(CH2)jCO2R10;e) —(CH2)jOCO2R10f) —(CH2)jCON(R10)2;g) —(CH2)jOCON(R10)2;h) two R2units can be taken together to form a carbonyl unit;i) and mixtures thereof;R8, R9a, R9b, and R10are each independently hydrogen, C1–C4alkyl, and mixtures thereof; R9aand R9bcan be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5, n is an index from 0 to 5;Z is O, S, NR11, or NOR11; R11is hydrogen or C1–C4alkyl.

REFERENCES:
patent: 3449359 (1969-06-01), Testa et al.
patent: 529153 (1972-10-01), None
patent: WO 01/57042 (2001-08-01), None
patent: WO 03/024971 (2003-03-01), None
Illei, G. G. et al., “Novel, non-antigen-specific therapeutic approaches to autoimmune/inflammatory diseases”,Current Opinion in Immunology, 2000, vol. 12, Issue 6, pp. 712-718.
Black, R. A. et al., “Agents that Block TNF-α Synthesis or Activity”,Annual Reports in Medicinal Chemistry-32, Chapter 24, Academic Press, Inc., 1997, pp. 241-250.

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