1,4-Substituted piperidines as acetylcholinesterase inhibitors and their use for the treatment of Alzheimer's disease

Cyclic amine cpds. of formula (I) and their salts are new. - J is (a) a gp., opt. substd., of: phenyl, pyridyl, pyrazyl, cyclohexyl, quino(xa)lyl or furyl; (b) a monovalent or divalent gp., where the phenyl may have substit(s), of: indan(ol)yl, (iii) inden(on)yl, indan(edio)hyl, tetralonyl, benzosub...

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Hauptverfasser: KARIBE, NORIO, OGURA, HIROO, IIMURA, YUOICHI, HIGURASHI, KUNIZOU, ARAKI, SHIN, TSUCHIYA, YUTAKA, KOZASA, MICHIKO, SUGIMOTO, HACHIRO, KOSASA, TAKASHI, SASAKI, ATSUSHI, YAMANASHI, YOSHIHARU, YAMATSU, KIYOMI, KUSOTA, ATSUHIKO
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creator KARIBE, NORIO
OGURA, HIROO
IIMURA, YUOICHI
HIGURASHI, KUNIZOU
ARAKI, SHIN
TSUCHIYA, YUTAKA
KOZASA, MICHIKO
SUGIMOTO, HACHIRO
KOSASA, TAKASHI
SASAKI, ATSUSHI
YAMANASHI, YOSHIHARU
YAMATSU, KIYOMI
KUSOTA, ATSUHIKO
description Cyclic amine cpds. of formula (I) and their salts are new. - J is (a) a gp., opt. substd., of: phenyl, pyridyl, pyrazyl, cyclohexyl, quino(xa)lyl or furyl; (b) a monovalent or divalent gp., where the phenyl may have substit(s), of: indan(ol)yl, (iii) inden(on)yl, indan(edio)hyl, tetralonyl, benzosuberonyl, or C6H5-CO-CH(CH3)-; (c) a monovalent gp. derived from a cyclic amide cpd. (d) lower alkyl; or (e) R21-CH=CH- (R21 = H or (lower alkoxycarbonyl). B = (CHR22)r, CO(CHR22)r, NR4-(HCR22)r, CO-NR5-(CHR22)r, CH=CH-(CHR22)r, OCOO-(CHR22)r, OOC-NH-(CHR22)r, NH-CO-(CHR32)4, CH2CONH-(CHR22)r, (CH2)2CONH-(CHR22)r, CH(OH)-(CHR22)r, CH(OH)-(CHR22)r, = (CH-CH=CH)b, =CH-(CH2)c, =(CH-CH)d, COCH=CH-CH2, COCH2-CH(CH(OH)CH2, CH(CH3)CONHCH2, CH=CHCONH(CH2)2, NH, O, S, dialkylaminoalkylcarbonyl or lower alkoxycarbonyl; R4 = H, acyl, lower alkyl(sulphonyl), (substd.)phenyl, or (substd.)benzyl; R5 = H, lower alkyl or phenyl, r = 0-10; R22 = H or Me such that one alkylene may have no CH3 or one or more CH3; b = 1-3; c = 0-9; d = 0-5; T = N or C (i) Q = N, C or (i) q = 1-3; K = H, (substd.) phenyl, arylalkyl in which the phenyl may be substd. cinnamyl, lower alkyl, pyridylmethyl, cyclo(alkyl)alkyl, adamantanemethyl, furylmethyl, lower alkoxycarbonyl or acyl; and dotted lines is a single-or double-bond. - 1-benzyl-4-((5,6-dimethoxy -1-indanon)- 2-ylidenyl)methyl) piperidine hydrochlorideis and example.
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(d) lower alkyl; or (e) R21-CH=CH- (R21 = H or (lower alkoxycarbonyl). 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(d) lower alkyl; or (e) R21-CH=CH- (R21 = H or (lower alkoxycarbonyl). 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OGURA, HIROO ; IIMURA, YUOICHI ; HIGURASHI, KUNIZOU ; ARAKI, SHIN ; TSUCHIYA, YUTAKA ; KOZASA, MICHIKO ; SUGIMOTO, HACHIRO ; KOSASA, TAKASHI ; SASAKI, ATSUSHI ; YAMANASHI, YOSHIHARU ; YAMATSU, KIYOMI ; KUSOTA, ATSUHIKO</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_EP0296560B13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; fre ; ger</language><creationdate>1996</creationdate><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><topic>SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</topic><toplevel>online_resources</toplevel><creatorcontrib>KARIBE, NORIO</creatorcontrib><creatorcontrib>OGURA, HIROO</creatorcontrib><creatorcontrib>IIMURA, YUOICHI</creatorcontrib><creatorcontrib>HIGURASHI, KUNIZOU</creatorcontrib><creatorcontrib>ARAKI, SHIN</creatorcontrib><creatorcontrib>TSUCHIYA, YUTAKA</creatorcontrib><creatorcontrib>KOZASA, MICHIKO</creatorcontrib><creatorcontrib>SUGIMOTO, HACHIRO</creatorcontrib><creatorcontrib>KOSASA, TAKASHI</creatorcontrib><creatorcontrib>SASAKI, ATSUSHI</creatorcontrib><creatorcontrib>YAMANASHI, YOSHIHARU</creatorcontrib><creatorcontrib>YAMATSU, KIYOMI</creatorcontrib><creatorcontrib>KUSOTA, ATSUHIKO</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>KARIBE, NORIO</au><au>OGURA, HIROO</au><au>IIMURA, YUOICHI</au><au>HIGURASHI, KUNIZOU</au><au>ARAKI, SHIN</au><au>TSUCHIYA, YUTAKA</au><au>KOZASA, MICHIKO</au><au>SUGIMOTO, HACHIRO</au><au>KOSASA, TAKASHI</au><au>SASAKI, ATSUSHI</au><au>YAMANASHI, YOSHIHARU</au><au>YAMATSU, KIYOMI</au><au>KUSOTA, ATSUHIKO</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>1,4-Substituted piperidines as acetylcholinesterase inhibitors and their use for the treatment of Alzheimer's disease</title><date>1996-02-28</date><risdate>1996</risdate><abstract>Cyclic amine cpds. of formula (I) and their salts are new. - J is (a) a gp., opt. substd., of: phenyl, pyridyl, pyrazyl, cyclohexyl, quino(xa)lyl or furyl; (b) a monovalent or divalent gp., where the phenyl may have substit(s), of: indan(ol)yl, (iii) inden(on)yl, indan(edio)hyl, tetralonyl, benzosuberonyl, or C6H5-CO-CH(CH3)-; (c) a monovalent gp. derived from a cyclic amide cpd. (d) lower alkyl; or (e) R21-CH=CH- (R21 = H or (lower alkoxycarbonyl). B = (CHR22)r, CO(CHR22)r, NR4-(HCR22)r, CO-NR5-(CHR22)r, CH=CH-(CHR22)r, OCOO-(CHR22)r, OOC-NH-(CHR22)r, NH-CO-(CHR32)4, CH2CONH-(CHR22)r, (CH2)2CONH-(CHR22)r, CH(OH)-(CHR22)r, CH(OH)-(CHR22)r, = (CH-CH=CH)b, =CH-(CH2)c, =(CH-CH)d, COCH=CH-CH2, COCH2-CH(CH(OH)CH2, CH(CH3)CONHCH2, CH=CHCONH(CH2)2, NH, O, S, dialkylaminoalkylcarbonyl or lower alkoxycarbonyl; R4 = H, acyl, lower alkyl(sulphonyl), (substd.)phenyl, or (substd.)benzyl; R5 = H, lower alkyl or phenyl, r = 0-10; R22 = H or Me such that one alkylene may have no CH3 or one or more CH3; b = 1-3; c = 0-9; d = 0-5; T = N or C (i) Q = N, C or (i) q = 1-3; K = H, (substd.) phenyl, arylalkyl in which the phenyl may be substd. cinnamyl, lower alkyl, pyridylmethyl, cyclo(alkyl)alkyl, adamantanemethyl, furylmethyl, lower alkoxycarbonyl or acyl; and dotted lines is a single-or double-bond. - 1-benzyl-4-((5,6-dimethoxy -1-indanon)- 2-ylidenyl)methyl) piperidine hydrochlorideis and example.</abstract><edition>4</edition><oa>free_for_read</oa></addata></record>
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language eng ; fre ; ger
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title 1,4-Substituted piperidines as acetylcholinesterase inhibitors and their use for the treatment of Alzheimer's disease
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