C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/129, 530/15.
C07D 207/452 (2006.01) C07K 15/06 (1985.01)
Patent
CA 1236091
16777 TITLE OF THE INVENTION CONJUGATES OF LEUKOTRIENE C4 WITH PROTEINS ABSTRACT OF THE INVENTION Leukotriene C4 (LTC4) has been conjugated with Bovine Serum Albumin (BSA) and Hemocyanin from Giant Keyhole Limpets (KLH) using 1,5-difluoro-2,4-dinitrobenzene as coupling agent. A second LTC4-KLH conjugate was prepared using a new bifunctional coupling agent, 6-N-maleimidohexanoic acid chloride. Conjugates of some representative LTC4 component parts; S-p-chlorophenacylglutathione with BSA and of 2,4(E),6,9(z)-pentadecatetraen-1-ol with BSA were also prepared. These conjugates are useful as reagents in a newly developed immunoassay for Leukotriene C4, as well as having potential utility as chemical immunotherapeutic agents in the treatment various allergic and chronic inflammatory diseases of the skin, lung, and airways, including asthma, allergic - 2 - 16777 rhinitis, rheumatoid arthritis, and skin diseases such as psoriasis and eczema. Thus the conjugates can be used to raise antibodies to LTC4, LTD4, LTE4, in humans (in a manner similar to that employed herein in rabbits). The resulting circulating levels of antibodies would serve to diminish plasma levels of LTC4, and LTD4 and LTE4 released during an asthmatic anaphylactic response and thus serve to alleviate the symptoms. Since the antibodies would be present during long periods of time, this would represent a long term asthma therapy.
426031
Hayes Edward C.
Rokach Joshua
Young Robert N.
Goudreau Gage Dubuc
Merck & Co. Inc.
Merck Frosst Canada Inc.
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