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(19)

(11)

2 268 258

(13)

(51)

IPC

C07C271/22(2006-01-01)

C07D307/80(2006-01-01)

A61K31/325(2006-01-01)

A61K31/44(2006-01-01)

A61P7/04(2006-01-01)

(21) (22)

Application

2002127781/04, 2001-03-08

(24)

Start date

2001-03-08

(22)

Actual filing date

2001-03-08

(45)

Published

2006-01-20

(72)

Inventor

Kornojer Richard LeoKejtts Pol FransisLauri Li EhduinMjul'Dorf Aleksander ViktorO`Jan KaundJasuda Dennis Mitsugu

(73)

Holder

F.Khoffmann-Lja Rosh Ag

DERIVATIVES OF CARBOXYLIC ACIDS AS ANTAGONISTS OF IP Russian patent published in 2006 - IPC C07C271/22 C07D307/80 A61K31/325 A61K31/44 A61P7/04

Abstract RU 2268258 C2

FIELD: organic chemistry, medicine, pharmacy.

SUBSTANCE: invention relates to compound of the formula (I): that are useful as antagonists of prostaglandin IP (I₂ or PGI₂). Invention proposes compound of the formula (I) wherein each R¹, R² and R³means independently in each case aryl or heteroaryl; R⁴ means -COOH or tetrazolyl; A, B, m, p, q, n and r are determined in the invention description. Also, invention relates to separated isomers, racemic or nonracemic mixtures of isomers and to their pharmaceutically acceptable salts or solvates also. Also, invention relates to pharmaceutical compositions comprising indicated compounds, to a method for their preparing and using as therapeutic agents. Invention provides the development of pharmaceutical composition possessing property of antagonists of IP wherein antagonists of these receptors can prevent states associated with excessive bleeding, for example, (but not only) hemophilia and hemorrhage and relieve septic shock-associated hypotension and diminish formation of edemas.

EFFECT: valuable medicinal properties of compounds.

28 cl, 15 sch, 29 ex

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RU 2 268 258 C2

Authors

Kornojer Richard Leo

Kejtts Pol Fransis

Lauri Li Ehduin

Mjul'Dorf Aleksander Viktor

O`Jan Kaund

Jasuda Dennis Mitsugu

Dates

2006-01-20—Published

2001-03-08—Filed