HUP0303347A2 - (R)-2-aril-propionsav-omega-aminoalkilamidok mint polimorf magvú és egymagvú sejtek kemotaxisának inhibitorai, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents

(R)-2-aril-propionsav-omega-aminoalkilamidok mint polimorf magvú és egymagvú sejtek kemotaxisának inhibitorai, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények

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Publication number
HUP0303347A2
HUP0303347A2 HU0303347A HUP0303347A HUP0303347A2 HU P0303347 A2 HUP0303347 A2 HU P0303347A2 HU 0303347 A HU0303347 A HU 0303347A HU P0303347 A HUP0303347 A HU P0303347A HU P0303347 A2 HUP0303347 A2 HU P0303347A2
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HU
Hungary
Prior art keywords
group
hydrogen atom
optionally
atom
groups
Prior art date
Application number
HU0303347A
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English (en)
Inventor
Marcello Allegretti
Valerio Berdini
Ricardo Bertini
Cinzia Bizzarri
Gianfranco Caselli
Maria Candida Cesta
Francesco Colotta
Vito Di Cioccio
Carmelo Gandolfi
Original Assignee
Dompé S.p.A.
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Application filed by Dompé S.p.A. filed Critical Dompé S.p.A.
Publication of HUP0303347A2 publication Critical patent/HUP0303347A2/hu
Publication of HUP0303347A3 publication Critical patent/HUP0303347A3/hu
Publication of HU230832B1 publication Critical patent/HU230832B1/hu

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Abstract

A találmány szerinti vegyületek (I) általános képletében Ar jelentéseadott esetben szubsztituált arilcsoport, R jelentése hidrogénatom,alkilcsoport, alkenilcsoport vagy alkinilcsoport, amelyek adottesetben CO2R3 csoporttal szubsztituálva lehetnek, ahol R3 jelentésehidrogénatom, alkilcsoport vagy alkenilcsoport, X jelentése 1-6szénatomos egyenes vagy elágazó szénláncú alkiléncsoport, 4-6szénatomos alkeniléncsoport vagy 4-6 szénatomos alkiniléncsoport,amelyet adott esetben CO2R3 vagy CONHR4 csoporttal szubsztituálvalehetnek, ahol R4 jelentése hidrogénatom, 2-6 szénatomos egyenes vagyelágazó szénláncú alkilcsoport vagy OR3 csoport, R3 jelentése a fenti,(CH2)m-B-(CH2)n csoport, amely adott esetben fent definiált CO2R3 vagyCONHR4 csoporttal szubsztituálva lehet, ahol B jelentése oxigénatomvagy kénatom, m értéke 0, 2 vagy 3 és n értéke 2 vagy 3, vagy Bjelentése CO, SO vagy CONH csoport és m értéke 1-3, és n értéke 2 vagy3, vagy X jelentése a kapcsolódó omega-aminocsoport nitrogénatomjávalés az R1 csoporttal együtt 3-7 tagú nem aromás nitrogéntartalmúheterociklusos csoport, monociklusos csoport vagy policiklusoscsoport, amely a nitrogénatomon Rc csoportot hordoz, ahol Rc jelentésehidrogénatom, alkilcsoport, hidroxialkilcsoport, acilcsoport, adottesetben szubsztituált fenilcsoport vagy difenilmetilcsoport, Rl és R2jelentése egymástól függetlenül hidrogénatom, egyenes vagy elágazószénláncú alkilcsoport, amely adott esetben oxigénatomot vagykénatomot tartalmaz, cikloalkilcsoport, alkenilcsoport,alkinilcsoport, arilalkilcsoport vagy hidroxialkilcsoport, vagy R1 ésR2 jelentése a kapcsolódó nitrogénatommal együtt (II) általánosképletű 3-7 tagú nitrogéntartalmú heterociklusos csoport, ahol Yjelentése közvetlen kötés, CH2, O, S vagy N-Rc csoport, p értéke 0-3,vagy R1 jelentése a fenti és R2 jelentése (III) általános képletűcsoport, ahol Ra jelentése hidrogénatom, Rb jelentése hidrogénatom,hidroxilcsoport, alkilcsoport vagy NRdRe csoport, ahol Rd és Rejelentése egymástól függetlenül hidrogénatom, alkilcsoport vagyfenilcsoport, vagy Ra és Rb jelentése a kapcsolódó nitrogénatomokkalegyütt 5-7 tagú heterociklusos csoport, amely adott esetbenbenzolgyűrűvel, piridingyűrűvel vagy pirimidingyűrűvel fuzionálva van,azzal a megszorítással, hogy ha Ar jelentése 4-difenilcsoport és Xjelentése etiléncsoport vagy propiléncsoport, akkor R1 és R2 jelentéseetilcsoporttól eltérő, ha Ar jelentése 4-(2-fluor)difenilcsoport és Xjelentése CO2H csoporttal szubsztituált butiléncsoport, akkor Ra és Rbjelentése hidrogénatomtól eltérő, ha Ar jelentése fenilcsoport és Xjelentése butiléncsoport, akkor R1 és R2 jelentése a kapcsolódónitrogénatommal együtt N-(2-metoxifenil)piperazinilcsoporttól eltérő.A találmány kiterjed a fenti vegyületek előállítására és gyógyszerkénttörténő alkalmazására és a vegyületeket
HU0303347A 2001-02-27 2002-02-25 (R)-2-aril-propionsav-omega-aminoalkilamidok mint polimorf magvú és egymagvú sejtek kemotaxisának inhibitorai HU230832B1 (hu)

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ITMI2001A000395 2001-02-27
PCT/EP2002/001974 WO2002068377A1 (en) 2001-02-27 2002-02-25 Omega-aminoalkylamides of r-2-aryl-propionic acids as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells

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