首页> 外国专利> ASSOCIATION OF AN ANTAGONIST OR REVERSE AGONIST OF THE H3 HISTAMINE RECEIVER WITH AN ANTIPSYCHOTIC OR AN ANTIDEPRESSIVE AND ITS USE TO PREPARE A MEDICINAL PRODUCT THAT AVOID THE INDESEABLE EFFECTS OF PSYCHOTROPIC DRUGS.

ASSOCIATION OF AN ANTAGONIST OR REVERSE AGONIST OF THE H3 HISTAMINE RECEIVER WITH AN ANTIPSYCHOTIC OR AN ANTIDEPRESSIVE AND ITS USE TO PREPARE A MEDICINAL PRODUCT THAT AVOID THE INDESEABLE EFFECTS OF PSYCHOTROPIC DRUGS.

机译：H3组胺受体的拮抗剂或逆转拮抗剂与抗精神病药或抗抑郁药的关联，并用于制备可避免精神病药物不可或缺的药物。

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摘要

Novel drug containing, in a pharmaceutically acceptable vehicle, an antipsychotic or an antidepressant (A), which alone presents an undesirable effect of increased body weight or sedation and an inverse antagonist and / or agonist (B) of the H3 receptor the histamine, said antipsychotic or antidepressant being present in the drug in a therapeutically effective amount for the antipsychotic or antidepressant sought, and said antagonist and / or inverse agonist of the histamine H3 receptor being present in a therapeutically effective amount to ensure one of the minus three following effects: suppression or at least limitation of the undesirable effect of weight gain, suppression or limitation of the undesirable effect on wakefulness, increase of the procognitive effect of the treatment, such that: - the agent (A) is selected from the agents that have an antagonistic effect of the histamine H1 receptor selected from olanzapine, clozapine, risperidone, quietapine, mirtazapine, aripiprazole; and - agent (B) responds to formula (II) in which: b = 0 or 1 i) R 1 and R 2, the same or different, each independently represents - a C1-C6 alkyl or a cycloalkyl , or taken together with the nitrogen atom to which they are attached, - a cyclic nitrogen compound saturated with m from 2 to 8 or a cyclic unsaturated unsaturated nitrogen compound being pyq independently from 0 to 3 and r from 0 to 4, with the proviso that pyq are not simultaneously 0 and that 2 = p + q + r = 8, where R ad is independently a hydrogen atom or a C1-C6 alkyl, cycloalkyl or carboalkoxy group or - a morpholino group or - an N-substituted piperazino group where R is a C1-C6 alkyl, cycloalkyl, carboalkoxy, aryl, arylalkyl, alkanoyl or an aroyl group group, ii) chain A "is selected from a linear, branched, saturated or unsaturated alkylene group - (CH2) n "- in which n" is an integer from 1 to 8; a linear or branched alkenylene group containing ne of 1 to 8 carbon atoms; and a linear or branched alkynylene group containing 1 to 4 carbon atoms; iii) group X "is selected from -OCONH-, OCON (alkyl) -, -OCON (alkene) -, - OCO-, -OCOSNH-, -CH2-, -O-, -OCH2CO-, -S-, -CO-, -CS-, an amine or a saturated or unsaturated alkyl; iv) the B chain "is selected from linear, branched, saturated or unsaturated alkylenes containing from 1 to 8 carbon atoms; and - (CH2) n "(heteroatom) - in which the heteroatom is preferably an oxygen or sulfur atom; n" being an integer from 1 to 5; ev) the group Y "represents an unsubstituted or mono or polysubstituted phenyl group by one or more identical or different substituents selected from halogen atoms, OCF3, CHO, CF3, SO2N (alkyl) 2 such as SO2N (CH3) 2, NO2 , S (aryl), SCH2 (phenyl), a linear or branched alkene, a linear or branched alkyne optionally substituted by a trialkyl silyl radical, -O (alkyl), -O (aryl), -CH2CN, a ketone, an aldehyde , a sulfone, an acetal, an alcohol, a C1-C6 alkyl, -CH = CHCHO, - C (alkyl) = N-OH, -C (alkyl) = NO (alkyl) and other ketone derivatives, -CH = NOH , - CH = NO (alkyl) and other aldehyde derivatives, -C (alkyl) = NH-CONH2, and O-phenyl or the group -OCH2 (phenyl), -C (cycloalkyl) -NOH, -C (cycloalkyl) = NO (alkyl); an optionally substituted heterocycle, a cycloalkyl; a bicyclic group and preferably a norbomyl group; a phenyl nucleus fused to a heterocycle containing a nitrogen hetero atom or a carbocycle or a heterocycle with a keto function na; a linear or branched C1-C6 alkyl; a linear or branched alkyne containing from 1 to 8 carbon atoms and especially 1 to 5 carbon atoms; a linear or branched mono or polysubstituted alkyl by unsubstituted or mono or polysubstituted phenyl groups; a phenylalkyl ketone in which the alkyl group is linear or branched or cyclic; a substituted or unsubstituted benzophenone; a substituted or unsubstituted, linear, branched or cyclic phenyl alcohol; a linear or branched alkene; a piperidyl group; a phenylcycloalkyl group; a polycyclic group, especially a fluorenyl group, a naphthyl or polyhydronaphthyl group or an indanyl group; an enol group; a ketone or a ketone derivative; a diphenyl group, a phenoxyphenyl group; a benzyloxyphenyl group, -CN, -alkyl, -aryl, -alkylCalkyl, -COOAlkyl, -COalkyl, -COaryl, -COaralkyl, -COcycloalkyl, -OH, -alkyl (OH), -alkyl (Oalkyl), -NHCOAlkyl, - NH2, or its pharmaceutically acceptable salts, hydrates, or hydrated salts, or the polymorphic crystalline structures of said compounds or their optical isomers, racemates, diastereoisomers or enantiomers.

机译：在药学上可接受的媒介物中包含抗精神病药或抗抑郁药（A）的新药，其单独表现出增加体重或镇静的不良作用以及组胺H3受体的反向拮抗剂和/或激动剂（B），抗精神病药或抗抑郁药以所需的抗精神病药或抗抑郁药的治疗有效量存在，并且所述组胺H3受体拮抗剂和/或反向激动剂以治疗有效量存在，以确保负三种以下作用之一：抑制或至少限制体重增加的不良影响，抑制或限制对唤醒的不良影响，增加治疗的认知作用，使得：-药剂（A）选自具有拮抗作用的药剂选自奥氮平，氯氮平，利培酮，文雅平，米氮平，阿立哌唑的组胺H1受体的作用; -试剂（B）响应式（II），其中：b = 0或1 i）R 1和R 2相同或不同，各自独立地表示-C1-C6烷基或环烷基，或与-与它们相连的氮原子--饱和m的环状氮化合物2至8或环状不饱和不饱和氮化合物pyq独立于0至3和r从0至4，条件是pyq不同时0，且2 <= p + q + r <= 8，其中R ad独立地为氢原子或C1-C6烷基，环烷基或碳烷氧基或-吗啉代基团或-N-取代的哌嗪基，其中R为C 1 -C 6烷基，环烷基，碳烷氧基，芳基，芳基烷基，烷酰基或芳酰基基团，ii）链A“选自直链，支链，饱和或不饱和亚烷基-（CH 2）n-其中n”是1至8的整数;含有1至8个碳原子的ne的直链或支链亚烯基;以及直链或支链的亚炔基含有1至4个碳原子; iii）基团X”选自-OCONH-，OCON（烷基）-，-OCON（烯烃）-，-OCO-，-OCOSNH-，-CH2-，-O-，-OCH2CO-，-S-，- CO-，-CS-，胺或饱和或不饱和烷基; iv）“ B链”选自含有1至8个碳原子的直链，支链，饱和或不饱和亚烷基; -（CH 2）n“（杂原子）-，其中，杂原子优选为氧或硫原子; n”为1〜5的整数。 ev）“ Y基团通过一个或多个选自卤素原子，OCF3，CHO，CF3，SO2N（烷基）2如SO2N（CH3）2，NO2，S的相同或不同取代基表示未取代或单取代或多取代的苯基（芳基），SCH 2（苯基），直链或支链的烯烃，直链或支链的炔烃，其任选地被三烷基甲硅烷基，-O（烷基），-O（芳基），-CH2CN，酮，醛，砜，乙缩醛，醇，C1-C6烷基，-CH = CHCHO，-C（烷基）= N-OH，-C（烷基）= NO（烷基）和其他酮衍生物，-CH = NOH，- CH = NO（烷基）和其他醛衍生物，-C（烷基）= NH-CONH2，和O-苯基或基团-OCH2（苯基），-C（环烷基）-NOH，-C（环烷基）= NO（烷基）;任选取代的杂环，环烷基;双环基团，优选为降冰片基;与含氮杂原子或碳环或具有酮官能团的杂环的杂环稠合的苯基核;直链或支链C1- C6烷基; al含1至8个碳原子，尤其是1至5个碳原子的炔或支链炔烃;直链或支链的单或多取代的烷基，具有未取代或单或多取代的苯基;烷基为直链或支链或环状的苯基烷基酮;取代或未取代的二苯甲酮;取代或未取代的直链，支链或环状苯醇;直链或支链烯烃;哌啶基;苯基环烷基;多环基，特别是芴基，萘基或多氢萘基或茚满基;烯醇基团;酮或酮衍生物;二苯基，苯氧基苯基;苄氧基苯基，-CN，-烷基，-芳基，-烷基C烷基，-COOAlk基，-CO烷基，-CO芳基，-COar烷基，-CO环烷基，-OH，-烷基（OH），-烷基（O烷基），-NHCO烷基，- NH 2或其药学上可接受的盐，水合物或水合盐，或所述化合物或其旋光异构体，外消旋体，非对映异构体或对映异构体的多晶型晶体结构。

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公开/公告号ES2350103T3

专利类型
公开/公告日2011-01-18

原文格式PDF
申请/专利权人 BIOPROJET;
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申请/专利号ES20040767475T
发明设计人 LECOMTE JEANNE-MARIE;SCHWARTZ JEAN-CHARLES;
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申请日2004-06-25
分类号A61K31/551;A61K31/137;A61K31/40;A61K31/4025;A61K31/4164;A61K31/4412;A61K31/4453;A61K31/496;A61K31/513;A61K31/55;A61K31/554;A61K45/06;A61P25/18;A61P25/24;
国家 ES
入库时间 2022-08-21 18:02:52

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