N-substituted-(Dihydroxyboryl)alkyl purine, indole and pyrimidin

Details N-substituted-(Dihydroxyboryl)alkyl purine, indole and pyrimidin N-substituted-(Dihydroxyboryl)alkyl purine, indole and pyrimidin

1994-06-22

1997-07-01

Bernhardt, Emily

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Boron containing doai

544229, 548405, 562 7, A61K 3169, C07F 502, C07F 504

Patent

active

056438931

ABSTRACT:
Novel N-substituted-(dihydroxyboryl)alkyl purine, indole and pyrimidine derivatives have been found to be useful as inhibitors of inflammatory cytokines. They can be used, inter alia, in the therapy of septic shock, cachexia, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and AIDS. The compounds are typically prepared by reaction of an bromoalkyl boronic acid with the purine, indole or pyrimidine base.

REFERENCES:
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patent: 5306732 (1994-04-01), Norris et al.
Ruddle et al., 1990, "An antibody to lymphotoxin and tumor necrosis factor prevents transfer of experimental allergic encephalomyelitis" J. Exp. Med. 172:1193-1200.
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Sood et al., 1990, "Boron-containing nucleic acids. 2. Synthesis of oligonucleoside boranophosphaates" J. Am. Chem. Soc. 112:9000-1.
Sood et al., 1989, "Boron-containing nucleic acids. 2. Synthesis of cyanoborane adducts of 2'deoxy-nucleosides" J. Am. Chem. Soc. 111:9234-5.
Spielvogel et al., 1991, "From boron analogues of amino acids to boronated DNA: potential new pharmaceuticals and neutron capture agents" Pure & Appl. Chem. 63:415-8.

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