WATER-SOLUBLE DERIVATIVES OF PHENYLGLYCINE Russian patent published in 2006 - IPC C07D211/22 C07D211/42 C07D211/46 A61K31/4465

Abstract RU 2283305 C2

FIELD: organic chemistry, amino acids, medicine, pharmacy.

SUBSTANCE: invention relates to compounds of the formula (I): wherein R¹ means (lower)-alkoxy-group; R² means halogen atom; R³ means piperidinyl optionally substituted with group (lower)-alkyl, hydroxy-(lower)-alkyl, carboxy-(lower)-alkyl or (lower)-alkoxycarbonyl-(lower)-alkyl; R⁴ means hydrogen atom or (lower)-alkyl; n = 0-3, and group -(CH₂)_n- is substituted optionally with group (lower)-alkyl, and to their pharmaceutically acceptable salts. Also, invention proposes a method for preparing compounds of the formula (I). Invention proposes compound of the formula (II) given in the invention description. Also, invention proposes a pharmaceutical composition possessing inhibitory activity with respect to formation of coagulation factors Xa, IXa and thrombin comprising compound of the formula (I) and a pharmaceutically acceptable carrier and/or adjuvant. Invention provides preparing water-soluble derivatives of phenylglycine inhibiting formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor.

EFFECT: valuable medicinal properties of compounds and pharmaceutical composition.

15 cl, 18 ex

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RU 2 283 305 C2

Authors

Alig Leo

Grebke Tsbinden Katrin

Obst Ul'Rike

Dates

2006-09-10—Published

2003-01-30—Filed