VARIOUS N-SUBSTITUTED AMINO HETEROCYCLICS HAVING CARDIVASCULAR ANTIINFLAMMATORY EFFECTS

(1) N-Aryl-pyrrolidine, -piperidine and -homopiperidine derivs. of formula (I) and their acid-addn. and quat. salts and their hydrates and alcoholates are new. p = 0, 1 or 2; A = H, OR1, CN, CONR1R2, COR1, COOR1, OCOR1, CH2OR1 or CH2NR1R2; m = 0-6; Q = CH, CH2 or CH(OH); d, n = 0 or 1 and the dotted...

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Hauptverfasser: PROAKIS, ANTHONY GEORGE, SHANKLIN, JAMES ROBERT JR
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description (1) N-Aryl-pyrrolidine, -piperidine and -homopiperidine derivs. of formula (I) and their acid-addn. and quat. salts and their hydrates and alcoholates are new. p = 0, 1 or 2; A = H, OR1, CN, CONR1R2, COR1, COOR1, OCOR1, CH2OR1 or CH2NR1R2; m = 0-6; Q = CH, CH2 or CH(OH); d, n = 0 or 1 and the dotted lines are opt. double bonds; Ar = X,Y,ZC6H2, pyridyl, thienyl, furyl or naphthyl; R = Ar gp., X,Y,ZC6H2CH2, cycloalkyl or 1-8C alkyl; D = Ar gp., quinolyl, Ar(CH2)5 or a gp. of formulae (II)-(IV). In (III) when X = H, bond a may be a single bond; s = 1-4; t = 0, 1 or 2; X,Y,Z = H, 1-8C alkyl, halogen, NO2, OR1, COR1, CF3, CN, CONR1R1, NR1R1, COOR1, SO2R2, SR2, SOR2, NR1-COR2, CH2COOM, SO2NR1R2, NR1-SO2Me, NR1-CONR1R2 or NR1-COOR2; B = O, S, SO, SO2, NR1 or N-COOR1; z = 0 or 1, but it is not 0 when n = 0 and D = opt. substd. Ph, or (A)d = H or CN or aminocarbonyl, or a there is a double bond between the alpha C atom and a C atom of the pyrrolidino etc. ring; R1 = H, 1-8C alkyl, Ph or Ph-(1-8C)alkyl; R2 = 1-8C alkyl, Ph or Ph-(1-8C) alkyl; M = metal ion. (2) Pharm. compsn. for use as a Ca antagonist in the treatment of hypertension comprises a cpd. (I) but without the proviso about (B)z. (3) Pharm. compsn. for use as an antihistamine or for the redn. of gastric secretion comprises a cpd. (I) but without the proviso about (B)z.
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In (III) when X = H, bond a may be a single bond; s = 1-4; t = 0, 1 or 2; X,Y,Z = H, 1-8C alkyl, halogen, NO2, OR1, COR1, CF3, CN, CONR1R1, NR1R1, COOR1, SO2R2, SR2, SOR2, NR1-COR2, CH2COOM, SO2NR1R2, NR1-SO2Me, NR1-CONR1R2 or NR1-COOR2; B = O, S, SO, SO2, NR1 or N-COOR1; z = 0 or 1, but it is not 0 when n = 0 and D = opt. substd. Ph, or (A)d = H or CN or aminocarbonyl, or a there is a double bond between the alpha C atom and a C atom of the pyrrolidino etc. ring; R1 = H, 1-8C alkyl, Ph or Ph-(1-8C)alkyl; R2 = 1-8C alkyl, Ph or Ph-(1-8C) alkyl; M = metal ion. (2) Pharm. compsn. for use as a Ca antagonist in the treatment of hypertension comprises a cpd. (I) but without the proviso about (B)z. (3) Pharm. compsn. for use as an antihistamine or for the redn. of gastric secretion comprises a cpd. (I) but without the proviso about (B)z.</description><edition>4</edition><language>eng</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; 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</subject><creationdate>1990</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19900327&amp;DB=EPODOC&amp;CC=NZ&amp;NR=217408A$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25542,76290</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=19900327&amp;DB=EPODOC&amp;CC=NZ&amp;NR=217408A$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>PROAKIS, ANTHONY GEORGE</creatorcontrib><creatorcontrib>SHANKLIN, JAMES ROBERT JR</creatorcontrib><title>VARIOUS N-SUBSTITUTED AMINO HETEROCYCLICS HAVING CARDIVASCULAR ANTIINFLAMMATORY EFFECTS</title><description>(1) N-Aryl-pyrrolidine, -piperidine and -homopiperidine derivs. of formula (I) and their acid-addn. and quat. salts and their hydrates and alcoholates are new. p = 0, 1 or 2; A = H, OR1, CN, CONR1R2, COR1, COOR1, OCOR1, CH2OR1 or CH2NR1R2; m = 0-6; Q = CH, CH2 or CH(OH); d, n = 0 or 1 and the dotted lines are opt. double bonds; Ar = X,Y,ZC6H2, pyridyl, thienyl, furyl or naphthyl; R = Ar gp., X,Y,ZC6H2CH2, cycloalkyl or 1-8C alkyl; D = Ar gp., quinolyl, Ar(CH2)5 or a gp. of formulae (II)-(IV). In (III) when X = H, bond a may be a single bond; s = 1-4; t = 0, 1 or 2; X,Y,Z = H, 1-8C alkyl, halogen, NO2, OR1, COR1, CF3, CN, CONR1R1, NR1R1, COOR1, SO2R2, SR2, SOR2, NR1-COR2, CH2COOM, SO2NR1R2, NR1-SO2Me, NR1-CONR1R2 or NR1-COOR2; B = O, S, SO, SO2, NR1 or N-COOR1; z = 0 or 1, but it is not 0 when n = 0 and D = opt. substd. Ph, or (A)d = H or CN or aminocarbonyl, or a there is a double bond between the alpha C atom and a C atom of the pyrrolidino etc. ring; R1 = H, 1-8C alkyl, Ph or Ph-(1-8C)alkyl; R2 = 1-8C alkyl, Ph or Ph-(1-8C) alkyl; M = metal ion. (2) Pharm. compsn. for use as a Ca antagonist in the treatment of hypertension comprises a cpd. (I) but without the proviso about (B)z. (3) Pharm. compsn. for use as an antihistamine or for the redn. of gastric secretion comprises a cpd. 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In (III) when X = H, bond a may be a single bond; s = 1-4; t = 0, 1 or 2; X,Y,Z = H, 1-8C alkyl, halogen, NO2, OR1, COR1, CF3, CN, CONR1R1, NR1R1, COOR1, SO2R2, SR2, SOR2, NR1-COR2, CH2COOM, SO2NR1R2, NR1-SO2Me, NR1-CONR1R2 or NR1-COOR2; B = O, S, SO, SO2, NR1 or N-COOR1; z = 0 or 1, but it is not 0 when n = 0 and D = opt. substd. Ph, or (A)d = H or CN or aminocarbonyl, or a there is a double bond between the alpha C atom and a C atom of the pyrrolidino etc. ring; R1 = H, 1-8C alkyl, Ph or Ph-(1-8C)alkyl; R2 = 1-8C alkyl, Ph or Ph-(1-8C) alkyl; M = metal ion. (2) Pharm. compsn. for use as a Ca antagonist in the treatment of hypertension comprises a cpd. (I) but without the proviso about (B)z. (3) Pharm. compsn. for use as an antihistamine or for the redn. of gastric secretion comprises a cpd. (I) but without the proviso about (B)z.</abstract><edition>4</edition><oa>free_for_read</oa></addata></record>
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
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 VARIOUS N-SUBSTITUTED AMINO HETEROCYCLICS HAVING CARDIVASCULAR ANTIINFLAMMATORY EFFECTS
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