发明名称 NOVEL IMMUNOTHERAPEUTIC COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF AND METHOD OF DECREASE OF LEVELS OF PHDE, TNF ALPHA AND NFKB
摘要 organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to novel immunotherapeutic compounds of the formula: alpha where X means O- or where n has value 0, 1, 2 or 3; -(CnH2n)- means alkyl containing from 1 to 10 carbon atoms or monocycloalkyl containing up to 10 carbon atoms; R1 means hydrogen atom, lower alkyl or lower alkoxy-group; R2 means: (1) unsubstituted phenyl or naphthalene or phenyl or naphthalene substituted with one or more substitutes being each is taken independently among nitro-group, halogen atom, amino-group, amino-group substituted with alkyl containing 1-5 carbon atoms, alkyl containing up to 10 carbon atoms, cycloalkyl containing up to 10 carbon atoms, alkoxy-group containing up to 10 carbon atoms, cycloalkoxy-group containing up to 10 carbon atoms, phenyl or methylenedioxy-group; (2) pyridine; each of R3 and R4 taken separately means hydrogen atom; or R5 and R4 taken in common mean a bond carbon-carbon; Y means COZ, R5 or lower alkyl containing from 1 to 5 carbon atoms; Z means OH, -C=N or NR6R6, -R7; -OR7 means hydrogen atom or lower alkyl; and R6 means alkyl. These compounds are inhibitors of tumor necrosis R7-factor, nuclear factor kB and phosphodiesterase and can be used for control of cachexia, endotoxic shock, replication of retroviruses, asthma and inflammatory states. Invention relates to also a pharmaceutical composition based on these compounds and a method of decrease of levels of PHDE (phosphodiesterase), tumor necrosis alpha-factor (TNFalpha) and nuclear factor kB (NFkB). EFFECT: new immunotherapeutic compounds indicated above, valuable medicinal properties. 9 cl, 1 tbl
申请公布号 RU2188819(C2) 申请公布日期 2002.09.10
申请号 RU19990104523 申请日期 1997.08.11
申请人 SELDZHIN KORPOREJSHN 发明人 MALLER DZHORDZH U.;SHAJR MEHRI
分类号 C07D317/58;A61K31/12;A61K31/16;A61K31/165;A61K31/19;A61K31/192;A61K31/216;A61K31/275;A61K31/277;A61K31/341;A61K31/345;A61K31/36;A61K31/40;A61K31/4174;A61K31/44;A61K31/4409;A61P11/06;A61P19/00;A61P29/00;A61P31/00;A61P31/14;C07C43/215;C07C43/235;C07C43/243;C07C45/00;C07C45/46;C07C45/69;C07C49/175;C07C49/255;C07C62/10;C07C67/343;C07C69/612;C07C69/618;C07C69/734;C07C205/45;C07C225/22;C07C235/34;C07C255/32;C07C255/34;C07C255/37;C07C255/42;C07C255/49;C07D207/04;C07D211/80;C07D213/57;C07D233/66;C07D307/54;C07D307/68;C07D317/60;C07D333/34;C07D333/78;C07D409/02;(IPC1-7):C07C255/32 主分类号 C07D317/58
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