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1. RU94041210 - [(BENZODIOXANE, BENZOFURAN OF BENZOPYRAN) ALKYLAMINO] ALKYLSUBSTITUTED GUANIDINES AS SELECTIVE VASOCONSTRICTIVE AGENTS, PROCESS FOR PREPARATION THEREOF, INTERMEDIATES THEREFOR, COMPOSITION AND PROCESS FOR PREPARING THEREOF

Office Fédération de Russie
Numéro de la demande 94041210/04
Date de la demande 26.08.1994
Numéro de publication 94041210
Date de publication 10.07.1996
Type de publication A1
CIB
6C 07D 307/86 A
6C 07D 311/74 B
6C 07D 319/06 B
6C 07D 405/02 B
6 C 07 D 307/86, 311/74, 319/06, 405/02
CPC
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
A61P 9/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
A61P 25/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
A61P 25/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
04Centrally acting analgesics, e.g. opioids
C07D 307/81
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
307Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
77ortho- or peri-condensed with carbocyclic rings or ring systems
78Benzo [b] furans; Hydrogenated benzo [b] furans
79with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals directly attached to carbon atoms of the hetero ring
81Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 311/58
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
311Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
02ortho- or peri-condensed with carbocyclic rings or ring systems
04Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
58other than with oxygen or sulfur atoms in positions 2 or 4
Déposants Zhansen Farmasetika N.V. (BE)
Жансен Фармасетика Н.В. (BE)
Inventeurs Gi Rozalia Ozhen Van Lomman[BE]
Ги Розалиа Ожен Ван Ломман[BE]
Marsel' Fran Leopol'd de Brjujen[BE]
Марсель Фран Леопольд де Брюйен[BE]
Val'ter Zhakobjus Zhozef Zhanssen[BE]
Вальтер Жакобюс Жозеф Жанссен[BE]
Mandataires Matveeva N.A.
Матвеева Н.А.
Données relatives à la priorité 842,560 27.02.1992 US
Titre
(EN) [(BENZODIOXANE, BENZOFURAN OF BENZOPYRAN) ALKYLAMINO] ALKYLSUBSTITUTED GUANIDINES AS SELECTIVE VASOCONSTRICTIVE AGENTS, PROCESS FOR PREPARATION THEREOF, INTERMEDIATES THEREFOR, COMPOSITION AND PROCESS FOR PREPARING THEREOF
(RU) [/БЕНЗОДИОКСАН, БЕНЗОФУРАН ИЛИ БЕНЗОПИРАН/-АЛКИЛАМИНО]-АЛКИЛЗАМЕЩЕННЫЕ ГУАНИДИНЫ В КАЧЕСТВЕ СЕЛЕКТИВНЫХ СОСУДОСУЖИВАЮЩИХ СРЕДСТВ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРОМЕЖУТОЧНОЕ ДЛЯ НИХ, КОМПОЗИЦИЯ И СПОСОБ ЕЕ ПОЛУЧЕНИЯ
Abrégé
(EN)
FIELD: pharmaceutical industry. SUBSTANCE: present invention relates the vasoconstrictive (benzodioxane, benzofuran or benzopyran) alkylamino-alkyl-substituted quanidines of formula (1), pharmaceutically acceptable acid addition salts thereof and stereochemically isomeric forms thereof, wherein X is O, CH2 or single bond; R1 is hydrogen or C1-C6-alkyl; R2 is hydrogen, C1-C6-alkyl, C3-C6- alkenyl or C3-C6-alkynyl; R3 is hydrogen or C1-C6-alkyl; or R2 and R3 taken together form divalent radical of formula: (CH2)m- wherein m is 4 or 5; or R1 and R2 taken form divalent radical of formula: -CH=CH- or formula (CH2)n- wherein n is 2.3 or 4; or R3 is bond when R1 and R2 taken together form divalent radical of formula: -CH=CH=CH=, -CH=CH-N= or -CH=N-CH=; R4 is hydrogen or C1-C6-alkyl; Alk1 is divalent C1-C3-alkanediyl radical, A represents divalent radical of formula (a), (b), (c), (d) and (e) in which each R5 is hydrogen or C1-C4--alkyl, in which each R6 is hydrogen or C1-C4-alkyl Alk2 represents C2-C15- alkanediyl or C5-C7-- cycloalkanediyl, and each p is 0.1 or 2; provided that it is not [2-[(2,3-dihydro-1,4-benzodioxin-2-yl)-methyl] - amino] ethyl-guanidine. Pharmaceutical drugs are suitable as vasoconstrictive agents. The invention describes compositions comprising above-mentioned guanidine derivatives as active ingredients, processes for preparing said guanidine derivatives and novel N- cyanoguanidine intermediate compounds, and use thereof as drugs. EFFECT: improved properties of the title compounds.

(RU)
Изобретение относится к сосудосуживающим (бензодиоксан, бензофуран или бензопиран)-алкиламино-алкил-замещенным гуанидинам формулы I, приведенной в описании, их фармацевтически приемлемым солям присоединения кислот и их стереохимически изомерным формам. Фармацевтические препараты пригодны в качестве сосудосуживающих средств. Предложены композиции, содержащие указанные производные гуанидина в качестве активных ингредиентов, способы получения вышеуказанных производных гуанидина и новый N-цианогуанидин, промежуточные соединения и использование в качестве лекарственных средств.