N-PHENYLARYLSULFONYLAMIDE, PHARMACEUTICAL COMPOSITION CONTAINING INDICATED SUBSTANCE AS ACTIVE COMPONENT, COMPOUND AS INTERMEDIATE IN SYNTHESIS OF INDICATED COMPOUND AND METHOD FOR ITS PREPARING Russian patent published in 2007 - IPC C07D277/36 C07D307/64 C07D213/70 C07D405/12 C07D417/12 C07D401/12 C07D413/12 A61K31/341 A61K31/426 A61K31/44 A61P29/00 A61P13/00 A61P35/00 

Abstract RU 2299202 C2

FIELD: organic chemistry, chemical technology, medicine, pharmacy.

SUBSTANCE: invention proposes compound of N-phenylarylsulfonylamide of the formula (I): wherein R1 represents -COOH and so on; R2 represents hydrogen atom, methyl and so on; R3 and R4 represent combination of methyl and methyl and so on; R5 represents isopropyl and so on; Ar represents thiazolyl, pyridyl, 5-methyl-2-furyl wherein each is substituted optionally with methyl; n = 0 or 1, intermediate compound used in synthesis of this compound and a method for its synthesis. Compound of the formula (I) binds with prostaglandin E2 receptors, in particular, with subtype of EP1 and shows antagonistic properties. This compound shows low binding with protein and therefore it possesses the satisfactory activity in vivo. Also, invention claims a method for preparing a pharmaceutical composition possessing antagonistic activity with respect to EP1 receptors that comprises compound of the formula (I) as active component and an inert excipient. Proposed pharmaceutical composition is designated for prophylaxis and/or treatment of pollakiuria (more frequent diuresis) or enuresis.

EFFECT: valuable medicinal properties of compound and pharmaceutical composition, improved method of synthesis.

16 cl, 4 tbl, 3 sch, 270 ex

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RU 2 299 202 C2

Authors

Naganava Atsusi

Saitokh Tetsudzi

Kobajasi Kaoru

Marujama Takajuki

Nakai Esikhiko

Khasimoto Sinsuke

Dates

2007-05-20Published

2002-03-11Filed