Novel compounds are disclosed that have the chemical structure of Formula
(IIB), and its prodrug esters and acid-addition salts, and that are useful
as Interleukin-1 and Tumor Necrosis Factor-.alpha. modulators, and thus
are useful in the treatment of various diseases.
##STR1##
wherein the R groups include the following: R.sub.1 is selected from the
group consisting of hydrogen, a halogen, COOH, C.sub.1 -C.sub.12
carboxylic acids, C.sub.1 -C.sub.12 acyl halides, C.sub.1 -C.sub.12 acyl
residues, C.sub.1 -C.sub.12 esters, C.sub.1 -C.sub.12 secondary amides,
(C.sub.1 -C.sub.12)(C.sub.1 -C.sub.12) tertiary amides, C.sub.1 -C.sub.12
alcohols, (C.sub.1 -C.sub.12)( C.sub.1 -C.sub.12) ethers, C.sub.1
-C.sub.12 alkyls, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12
alkenyls, C.sub.2 -C.sub.12 substituted alkenyls; R.sub.2 is selected from
hydrogen, a halogen, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12
substituted alkyls, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12
substituted alkenyl, C.sub.2 -C.sub.12 alkynyl, and C.sub.1 -C.sub.12
acyl, and C.sub.5 -C.sub.12 aryl. R.sub.3, R.sub.4, R.sub.5, R.sub.7,
R.sub.8, and R.sub.11 -R.sub.13 are each separately selected from
hydrogen, a halogen, C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12
substituted alkyls, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12
substituted alkenyl, C.sub.2 -C.sub.12 alkynyl, and C.sub.5 -C.sub.12
aryl. R.sub.6 is selected from hydrogen, a halogen, C.sub.1 -C.sub.12
alkyls, C.sub.1 -C.sub.12 substituted alkyls, C.sub.2 -C.sub.12 alkenyls,
C.sub.2 -C.sub.12 substituted alkenyl and C.sub.2 -C.sub.12 alkynyl.
R.sub.10 is selected from hydrogen, a halogen, CH.sub.2, C.sub.1 -C.sub.6
alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.2 -C.sub.6 alkenyl,
C.sub.2 -C.sub.6 substituted alkenyl, C.sub.1 -C.sub.12 alcohol, and
C.sub.5 -C.sub.12 aryl.
Показаны смеси романа имеют химическую структуру формулы (IIB), и свои эстеры prodrug и соли кислот-dobavlenih, и который полезно как Interleukin-1 и модуляторы/демодулятор некроза Factor-.alpha. тумора, и таким образом будьте полезно в обработке различных заболеваний. ## ## STR1 при котором группы р вклюают following: R.sub.1 выбрано от водопода группы consist of, галоида, COOH, C.sub.1 - C.sub.12 карбоновых кислот, C.sub.1 - галоиды ацила C.sub.12, C.sub.1 - выпарки ацила C.sub.12, C.sub.1 - C.sub.12 эстеры, C.sub.1 - вторичные амиды C.sub.12, (C.sub.1 - C.sub.12)(C.sub.1 - C.sub.12) третичные амиды, C.sub.1 - спирты C.sub.12, (C.sub.1 - C.sub.12)($$ET-C.sub.1 - C.sub.12) эфиры, C.sub.1 - C.sub.12 alkyls, C.sub.1 - C.sub.12 заменил alkyls, C.sub.2 - C.sub.12 алкенилы, C.sub.2 - C.sub.12 замененные алкенилы; R.sub.2 выбрано от водопода, галоида, C.sub.1 - C.sub.12 алкила, C.sub.1 - alkyls замененные C.sub.12, C.sub.2 - C.sub.12 алкенила, C.sub.2 - алкенил замененный C.sub.12, C.sub.2 - alkynyl C.sub.12, и C.sub.1 - ацил C.sub.12, и C.sub.5 - арила C.sub.12. R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.8, и R.sub.11 - R.sub.13 каждое отдельно выбранное от водопода, галоида, C.sub.1 - алкил C.sub.12, C.sub.1 - C.sub.12 замененные alkyls, C.sub.2 - алкенил C.sub.12, C.sub.2 - C.sub.12 замененный алкенил, C.sub.2 - alkynyl C.sub.12, и C.sub.5 - арил C.sub.12. R.sub.6 выбрано от водопода, галоида, C.sub.1 - C.sub.12 alkyls, C.sub.1 - alkyls замененные C.sub.12, C.sub.2 - C.sub.12 алкенилов, C.sub.2 - алкенил замененный C.sub.12 и C.sub.2 - alkynyl C.sub.12. R.sub.10 выбрано от водопода, галоида, CH.sub.2, C.sub.1 - C.sub.6 алкила, C.sub.1 - алкил замененный C.sub.6, C.sub.2 - C.sub.6 алкенил, C.sub.2 - алкенил замененный C.sub.6, C.sub.1 - спирт C.sub.12, и C.sub.5 - арил C.sub.12.
