DERIVATIVES OF THIOXANTHINE AS MYELOPEROXIDASE INHIBITORS Russian patent published in 2008 - IPC C07D473/22 C07D473/20 A61K31/522 A61P25/28 A61P11/06 

Abstract RU 2323219 C2

FIELD: organic chemistry, medicine, biochemistry, pharmacy.

SUBSTANCE: invention relates to novel derivatives of thioxanthine of the formula (Ia): or (Ib): and their pharmaceutically acceptable salts, and to their using for preparing a drug and pharmaceutical composition based on thereof. Proposed compounds inhibit myeloperoxidase activity and can be used in treatment of diseases or states wherein inhibition of myeloperoxidase activity is useful, in particular, in neuroinflammatory diseases. In compounds of the general formula (Ia) or (Ib) X represents sulfur atom (S); Y represents oxygen atom (O); R1 represents hydrogen atom or (C1-C6)-alkyl; R2 represents (C1-C6)-alkyl substituted with saturated or partially unsaturated 3-7-membered ring comprising possibly one or two heteroatoms chosen independently from O, S and nitrogen atom (N) and wherein indicated ring is substituted possibly with one or more substitutes chosen from halogen atom, hydroxy, (C1-C6)-alkoxy and (C1-C6)-alkyl; R3 and R4 represent independently hydrogen atom or (C1-C6)-alkyl.

EFFECT: valuable medicinal and biochemical properties of compounds and pharmaceutical composition.

9 cl, 4 tbl, 22 ex

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RU 2 323 219 C2

Authors

Khanson Sverker

Nordvall' Gunnar

Tiden Anna-Karin

Dates

2008-04-27Published

2003-04-15Filed