DERIVATIVES OF 5-THIA-ω-SUBSTITUTED PHENYLPROSTAGLANDIN E, METHODS FOR ITS PREPARING, PHARMACEUTICAL COMPOSITION Russian patent published in 2003 - IPC

Abstract RU 2220135 C2

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new derivatives of prostaglandins, namely, to 5-thia-ω-substituted phenylprostaglandin E of the formula (I) -ω- wherein is OH or R1-alkoxy-group; C1-6 is oxygen or halogen atom; R2 is hydrogen atom or OH; R3 and R4a mean independently hydrogen atom or R4b-alkyl; C1-4 is phenyl substituted with R5-alkoxy-C1-4-alkyl, C1-4-alkenyloxy-C2-4-alkyl, phenyloxy-C1-4-alkyl and others. Compounds of the formula (I) can bind tightly with C1-4-receptors (especially with receptors of subtype PGE2). Therefore, these compounds are useful for prophylaxis and/or treatment of immunologic diseases (autoimmune diseases, such as amyotrophic lateral sclerosis, disseminated sclerosis, Sjogren's syndrome, chronic rheumoarthrosis, exanthematous (systemic) erythematosus and others, rejections after organs transplantation and others), asthma, pathology in bones formation, death of nerve cells, lung damage, liver injury, acute hepatitis, renal insufficiency, hypertension, myocardium ischemia, nephritis, general inflammatory response syndrome, burns pain, sepsis, hemophagus-syndrome, macrophages activation, Still's disease, Kawasaki's disease systemic granulomatosis, nonspecific ulcerous colitis, Crohn's disease, hypercytokinemia in dialysis, multiple organs injury, shock and others. Except for, receptor of subtype EP4 relates to sleep disorder and blood platelet aggregation. Therefore, it is believed that proposed compounds are useful in prophylaxis and/or treatment of above indicated diseases. EFFECT: improved preparing method, valuable medicinal properties of compounds. 21 cl, 4 tbl, 5 sch, 37 ex

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RU 2 220 135 C2

Authors

Marujama Toru

Okhutida Suiti

Dates

2003-12-27Published

1999-07-14Filed