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Title:
LIGANDS OF α-ADRENOCEPTORS AND OF DOPAMINE, HISTAMINE, IMIDAZOLINE AND SEROTONIN RECEPTORS AND THE USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2009/082268
Kind Code:
A3
Abstract:
The invention relates to novel ligands, the broad spectrum of which simultaneously comprises alpha-adrenoceptors, dopamine receptors, histamine receptors, imidazoline receptors and seratinin receptors, including 5-HT7 seratinin receptors, as compounds of general formula 1 in the form of free bases, geometrical isomers, racemic mixtures or individual optical isomers and also in the form of pharmaceutically acceptable salts and/or hydrates, wherein: R1 is an aminogroup substituent, optionally substituted C1-C2 alkyl, acyl, heterocyclyl, alkoxycarbonyl and substituted sulphonyl; R2 is a cyclic group substituent, including a hydrogen atom, a halogen atom, optionally substituted C1-C4 alkyl, CF3, CN, alkoxy, alkoxycarbonyl, carboxyl, heterocyclyl or substituted sulphonyl; Ar is optionally substituted aryl, possibly annelated with heterocyclyl, or optionally substituted heterocyclyl; W is an optionally substituted CH2-CH=CH group, an optionally substituted C≡C group, an SO2 group; n=1 or 2; m=1, 2 or 3; a continuous line together with a dotted line following it (---) represent a single or a double bonds. Medicinal substances, pharmaceutical compositions containing the novel ligands in the form of medicinal substances, novel medicinal agents which are used for treating diseases and states of the central nervous system of human beings and animals, are also disclosed.

Inventors:
IVASHCHENKO ANDREY ALEXANDROVICH (RU)
IVASHCHENKO ALEXANDER VASILIEV (US)
LAVROVSKY YAN VADIMOVICH (US)
MITKIN OLEG DMITRIEVICH (RU)
SAVCHUK NIKOLAY FILIPPOVICH (RU)
TKACHENKO SERGEY YEVGENIEVICH (RU)
OKUN ILYA MATUSOVICH (US)
Application Number:
PCT/RU2008/000780
Publication Date:
August 20, 2009
Filing Date:
December 19, 2008
Export Citation:
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Assignee:
IVASHCHENKO ANDREY ALEXANDROVI (RU)
ALLA CHEM LLC (US)
IVASHCHENKO ALEXANDER VASILIEV (US)
LAVROVSKY YAN VADIMOVICH (US)
MITKIN OLEG DMITRIEVICH (RU)
SAVCHUK NIKOLAY FILIPPOVICH (RU)
TKACHENKO SERGEY YEVGENIEVICH (RU)
OKUN ILYA MATUSOVICH (US)
International Classes:
C07D471/04; A61K31/43; A61K31/519; A61P25/00; C07D487/04
Foreign References:
US4754038A1988-06-28
US3409628A1968-11-05
DE1813229A11970-08-20
US3502688A1970-03-24
GB752668A1956-07-11
US3522262A1970-07-28
US3484449A1969-12-16
RU2283108C22006-09-10
RU2106864C11998-03-20
US4798896A1989-01-17
RU2036193C11995-05-27
Other References:
YU. YA. IVANOV ET AL.: "Kaltsy-antagonisticheskaya aktivnost nekotorykh gidrirovannykh proizvodnykh pirido[4,3-v]indolov.", KHIMIKO-FARMATSEVTICHESKY ZHURNAL., vol. 35, no. 7, 2001, pages 7, XP008145531
DATABASE ACS [online] VERKHOVSKII YU.G. ET AL: "Toxicological and antiserotonin properties of y-carboline derivatives.", accession no. STN Database accession no. 9497
DATABASE ACS [online] SHADURSKII K.S. ET AL: "Pharmacological properties and chemical structure of tetrahydro-y-carbolines", accession no. STN. Database accession no. 121995
DATABASE ACS [online] BOKSA JAN ET AL: "Synthesis in vitro and in vivo 5-HT1 A/5-HT2A serotonin receptor activity of new hybrid 1,2,3,4-tetrahydro-carbolines moiety", accession no. STN Database accession no. 74532
See also references of EP 2236511A4
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