Immunomodulation with novel pharmaceutical compositions

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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Details

C564S454000, C564S461000, C564S511000, C564S512000, C548S557000, C548S558000, C546S244000, C514S315000, C514S329000, C514S426000, C514S673000, C514S674000

Reexamination Certificate

active

06919483

ABSTRACT:
The synthesis and use of a novel class of tumor necrosis factor (TNFα) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNFα and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNFα and/or one or more other involved cytokines, alone or in combination with other agents. Examples of compounds of the present invention are those having the structures as shown below:wherein, a, b and c may be the same or different and are integers from 0 to 12, X equals NH or CHNH2, R1and R2can be the same or different and equal to a hydrogen or a straight or branched C1to C20saturated or unsaturated aliphatic; aliphatic amine; an alicyclic; single or multi-ring aromatic; a single or multi-ring aromatic heterocycle; a single or multi-ring saturated heterocycle and the halogenated forms thereof; andwherein, a, b and c may be the same or different and are integers from 0 to 12; R1, R2, R3, and R4can be the same or different and equal to a hydrogen or a straight or branched C1to C20saturated or unsaturated aliphatic; aliphatic amine; an alicyclic; single or multi-ring aromatic; a single or multi-ring aromatic heterocycle; a single or multi-ring saturated heterocycle and the halogenated forms thereof.

REFERENCES:
patent: 4507321 (1985-03-01), Raisfeld
The Merck Index, 12thed. (1996), Merck & Co., Inc., Whitehouse Station, NJ, p. 8899 entry No. 8894.

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