METHOD OF PRODUCING DERIVATIVES OF SUBSTITUTED BENZAMIDE OR THEIR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS

o-Substd.-N-morpholinyl alkylbenzamide derivs. and analogues of formula (I) and their acid-addn. or quat. ammonium salts and N-oxides are new. R is H, 2-5C alkoxycarbonyl, benzyloxycarbonyl, furyl-, thienyl-, pyridyl- or 1,2-benzisoxazolyl-(1-3C) alkyl, Ph-(3-5C) alkenyl or T-(Y)p-R6; T is single bo...

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Hauptverfasser: TATSUYA KON,JP, KAZUNORI OKHNO,JP, SIRO KATO,JP, TOSIYA MORIE,JP, KATSUKHIKO KHINO,JP, NAOYUKI ESIDA,JP, TADAKHIKO KARASAVA,JP
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creator TATSUYA KON,JP
KAZUNORI OKHNO,JP
SIRO KATO,JP
TOSIYA MORIE,JP
KATSUKHIKO KHINO,JP
NAOYUKI ESIDA,JP
TADAKHIKO KARASAVA,JP
description o-Substd.-N-morpholinyl alkylbenzamide derivs. and analogues of formula (I) and their acid-addn. or quat. ammonium salts and N-oxides are new. R is H, 2-5C alkoxycarbonyl, benzyloxycarbonyl, furyl-, thienyl-, pyridyl- or 1,2-benzisoxazolyl-(1-3C) alkyl, Ph-(3-5C) alkenyl or T-(Y)p-R6; T is single bond or 1-6C alkylene; X is O, S or CO; R6 is Ph opt. substd. by 1-5 halogen, 1-4C alkyl, CF3, 1-4C alkoxy, NO2, CN or NH2 or naphthyl or Ph2CH; p is 0 or 1, but it is 0 when T is single bond; R1 is halogen, OH, 1-12C alkoxy, 3-6C cycloalkoxy, 3-8C alkenyloxy, 3-8C alkynyloxy, 2-6C alk interrupted by 1 or 2 O or CO, 1-4C alkylthio, NH2, mono-substd. NH2 in which the substit. is 1-8C alkyl, Ph-(1-3)alkyl or 3-6C cycloalkyl, 2-6C alkoxy in which a C atom other than in the 1-position is substd. by one OH or NH2 or 1-6C alkoxy substd. by a halogen, CN, 2-5C alkoxycarbonyl, phthalimido, 3-6C cycloalkyl, Ph opt. substd. by one halogen, PhO opt. substd. by one halogen or PhCO opt. substd. by one halogen; R2 is H; R3 is H, halogen, NH2, mono- or di-(1-4C) alkylamino, 2-5C alkanoylamino or NO2; R4 is H, halogen, NO2, SO2NH2, mono- or di-(1-4C)alkylsulphamoyl; or 2 of R1-R4 form 1-3C alkylenedioxy and the other 2 are H; R5 is H or 1-4C alkyl; X is 1-3C alkylene, m, n are 1 or 2. If at least one of R2-R4 is other than H.
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NH2 in which the substit. is 1-8C alkyl, Ph-(1-3)alkyl or 3-6C cycloalkyl, 2-6C alkoxy in which a C atom other than in the 1-position is substd. by one OH or NH2 or 1-6C alkoxy substd. by a halogen, CN, 2-5C alkoxycarbonyl, phthalimido, 3-6C cycloalkyl, Ph opt. substd. by one halogen, PhO opt. substd. by one halogen or PhCO opt. substd. by one halogen; R2 is H; R3 is H, halogen, NH2, mono- or di-(1-4C) alkylamino, 2-5C alkanoylamino or NO2; R4 is H, halogen, NO2, SO2NH2, mono- or di-(1-4C)alkylsulphamoyl; or 2 of R1-R4 form 1-3C alkylenedioxy and the other 2 are H; R5 is H or 1-4C alkyl; X is 1-3C alkylene, m, n are 1 or 2. 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R is H, 2-5C alkoxycarbonyl, benzyloxycarbonyl, furyl-, thienyl-, pyridyl- or 1,2-benzisoxazolyl-(1-3C) alkyl, Ph-(3-5C) alkenyl or T-(Y)p-R6; T is single bond or 1-6C alkylene; X is O, S or CO; R6 is Ph opt. substd. by 1-5 halogen, 1-4C alkyl, CF3, 1-4C alkoxy, NO2, CN or NH2 or naphthyl or Ph2CH; p is 0 or 1, but it is 0 when T is single bond; R1 is halogen, OH, 1-12C alkoxy, 3-6C cycloalkoxy, 3-8C alkenyloxy, 3-8C alkynyloxy, 2-6C alk interrupted by 1 or 2 O or CO, 1-4C alkylthio, NH2, mono-substd. NH2 in which the substit. is 1-8C alkyl, Ph-(1-3)alkyl or 3-6C cycloalkyl, 2-6C alkoxy in which a C atom other than in the 1-position is substd. by one OH or NH2 or 1-6C alkoxy substd. by a halogen, CN, 2-5C alkoxycarbonyl, phthalimido, 3-6C cycloalkyl, Ph opt. substd. by one halogen, PhO opt. substd. by one halogen or PhCO opt. substd. by one halogen; R2 is H; R3 is H, halogen, NH2, mono- or di-(1-4C) alkylamino, 2-5C alkanoylamino or NO2; R4 is H, halogen, NO2, SO2NH2, mono- or di-(1-4C)alkylsulphamoyl; or 2 of R1-R4 form 1-3C alkylenedioxy and the other 2 are H; R5 is H or 1-4C alkyl; X is 1-3C alkylene, m, n are 1 or 2. 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R is H, 2-5C alkoxycarbonyl, benzyloxycarbonyl, furyl-, thienyl-, pyridyl- or 1,2-benzisoxazolyl-(1-3C) alkyl, Ph-(3-5C) alkenyl or T-(Y)p-R6; T is single bond or 1-6C alkylene; X is O, S or CO; R6 is Ph opt. substd. by 1-5 halogen, 1-4C alkyl, CF3, 1-4C alkoxy, NO2, CN or NH2 or naphthyl or Ph2CH; p is 0 or 1, but it is 0 when T is single bond; R1 is halogen, OH, 1-12C alkoxy, 3-6C cycloalkoxy, 3-8C alkenyloxy, 3-8C alkynyloxy, 2-6C alk interrupted by 1 or 2 O or CO, 1-4C alkylthio, NH2, mono-substd. NH2 in which the substit. is 1-8C alkyl, Ph-(1-3)alkyl or 3-6C cycloalkyl, 2-6C alkoxy in which a C atom other than in the 1-position is substd. by one OH or NH2 or 1-6C alkoxy substd. by a halogen, CN, 2-5C alkoxycarbonyl, phthalimido, 3-6C cycloalkyl, Ph opt. substd. by one halogen, PhO opt. substd. by one halogen or PhCO opt. substd. by one halogen; R2 is H; R3 is H, halogen, NH2, mono- or di-(1-4C) alkylamino, 2-5C alkanoylamino or NO2; R4 is H, halogen, NO2, SO2NH2, mono- or di-(1-4C)alkylsulphamoyl; or 2 of R1-R4 form 1-3C alkylenedioxy and the other 2 are H; R5 is H or 1-4C alkyl; X is 1-3C alkylene, m, n are 1 or 2. If at least one of R2-R4 is other than H.</abstract><oa>free_for_read</oa></addata></record>
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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
title METHOD OF PRODUCING DERIVATIVES OF SUBSTITUTED BENZAMIDE OR THEIR PHARMACEUTICALLY ACCEPTABLE ACID-ADDITIVE SALTS
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