BRPI9811688A - benzamidas bicíclicas gastrocinéticas de derivados de piperidina 3- ou 4- substituídos com 4-aminometil), processo para preparação das mesmas, composições farmacêuticas compreendendo as mesmas e processo para preparação das referidas composições. - Google Patents

benzamidas bicíclicas gastrocinéticas de derivados de piperidina 3- ou 4- substituídos com 4-aminometil), processo para preparação das mesmas, composições farmacêuticas compreendendo as mesmas e processo para preparação das referidas composições.

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Publication number
BRPI9811688A
BRPI9811688A BRPI9811688A BRPI9811688A BRPI9811688A BR PI9811688 A BRPI9811688 A BR PI9811688A BR PI9811688 A BRPI9811688 A BR PI9811688A BR PI9811688 A BRPI9811688 A BR PI9811688A BR PI9811688 A BRPI9811688 A BR PI9811688A
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Prior art keywords
hydrogen
alkyl
alk
cycloalkyl
preparing
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BRPI9811688A
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English (en)
Inventor
Jean-Paul Rene Marie A Bosmans
Michel Anna Jozef De Cleyn
Michel Surkyn
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Janssen Pharmaceutica Nv
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Publication of BRPI9811688A publication Critical patent/BRPI9811688A/pt
Publication of BRPI9811688B1 publication Critical patent/BRPI9811688B1/pt
Publication of BRPI9811688B8 publication Critical patent/BRPI9811688B8/pt

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/42Oxygen atoms attached in position 3 or 5
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    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/46Oxygen atoms attached in position 4 having a hydrogen atom as the second substituent in position 4
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10Laxatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12Antidiarrhoeals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07ORGANIC CHEMISTRY
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    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
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    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D211/44Oxygen atoms attached in position 4
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    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/40Oxygen atoms
    • C07D211/44Oxygen atoms attached in position 4
    • C07D211/48Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
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    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/12Halogen atoms or nitro radicals
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    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D307/10Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
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    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

patente de invenção: <b>"benzamidas bicíclicas gastrocinéticas de derivados de piperidina 3- ou 4- substituídos com 4-(amimo-metil)"<d>. a presente invenção de compostos da fórmula (i) uma forma estereoquimicamente isomérica dos mesmos, uma forma de n-óxido dos mesmos ou um sal de adição ácido dos mesmos, r¹ e r² tomados em conjunto formam um radical bivalente da fórmula, em que no referido radical bivalente um ou dois átomos de hidrogênio podem ser substituídos com c~ 1-6~ alquila; r³ é hidrogênio ou halo; r^ 4^ é hidrogênio ou c~ 1-6~ alquila; l é c~ 3-6~ cicloalquila, c~ 5-6~ cicloalcanona, c~ 2-6~ alquenila, ou l é um radical da fórmula -alk-r^ 6^, -alk-x-r^ 7^, -alk-y-c(=o)-r^ 9^, ou -alk-y-c(=o)-nr^ 11^r^ 12^ em que cada alk é c~ 1-12~ alcanodiíla; e r~ 6~ é hidrogênio, ciano, c~ 1-6~ alquilsulfonilamino, c~ 3-6~ cicloalquila, c~ 5-6~ cicloalcanona ou um sistema de anel heterocíclico; r^ 7^ é hidrogênio, c~ 1-6~ alquila, hidróxic~ 1-6~ alquila, c~ 3-6~ cicloalquila, ou um sistema de anel heterocíclico; x é o, s, so~ 2~ ou nr^ 8^, o referido r^ 8^ sendo hidrogênio ou c~ 1-6~ alquila; r^ 9^ é hidrogênio, c~ 1-6~ alquila, c~ 3-6~ cicloalquila, c~ 1-6~ alquilóxi ou hidróxi; y é nr^ 10^ ou uma ligação direta; o referido r^ 10^ sendo hidrogênio, ou c~ 1-6~ alquila; r^ 11^ e r^ 12^ cada um, de forma independente são hidrogênio, c~ 1-6~ alquila, c~ 3-6~ cicloalquila, ou r^ 11^ e r^ 12^ combinados com o átomo de nitrogênio podem formar um anel de pirrolidinila, piperidinila, piperazinila ou 4-morfolinila opcionalmente substituído. são descritos processos para a preparação dos referidos produtos, formulações que compreendem os referidos e o uso dos mesmos como um medicamento, de forma específica para o tratamento de condições que estão relacionadas com a dificuldade de esvaziamento gástrico.
BRPI9811688 1997-07-11 1998-07-07 benzamidas bicìclicas gastrocinéticas de derivados de piperidina 3- ou 4- substituìdos com 4-aminometil), processo para preparação das mesmas, composições farmacêuticas compreendendo as mesmas e processo para preparação das referidas composições. BRPI9811688B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP97202180 1997-07-11
EP98200624 1998-02-27
PCT/EP1998/004190 WO1999002156A1 (en) 1997-07-11 1998-07-07 Gastrokinetic bicyclic benzamides of 3- or 4-substituted 4-(aminomethyl)-piperidine derivates

Publications (3)

Publication Number Publication Date
BRPI9811688A true BRPI9811688A (pt) 2000-09-26
BRPI9811688B1 BRPI9811688B1 (pt) 2011-10-18
BRPI9811688B8 BRPI9811688B8 (pt) 2021-07-06

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BRPI9811688 BRPI9811688B8 (pt) 1997-07-11 1998-07-07 benzamidas bicìclicas gastrocinéticas de derivados de piperidina 3- ou 4- substituìdos com 4-aminometil), processo para preparação das mesmas, composições farmacêuticas compreendendo as mesmas e processo para preparação das referidas composições.
BR9811687-8A BR9811687A (pt) 1997-07-11 1998-07-07 Benzamidas monocìclicas gastrocinéticas de derivados de 4-(aminometil) piperidina 3 ou 4-substituìda

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BR9811687-8A BR9811687A (pt) 1997-07-11 1998-07-07 Benzamidas monocìclicas gastrocinéticas de derivados de 4-(aminometil) piperidina 3 ou 4-substituìda

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US (10) US6452013B1 (pt)
EP (3) EP1206938A1 (pt)
JP (2) JP4530530B2 (pt)
KR (2) KR100500372B1 (pt)
CN (2) CN1195736C (pt)
AR (2) AR013361A1 (pt)
AT (2) ATE255092T1 (pt)
AU (2) AU734475B2 (pt)
BG (2) BG63709B1 (pt)
BR (2) BRPI9811688B8 (pt)
CA (2) CA2295088C (pt)
CZ (2) CZ297298B6 (pt)
DE (2) DE69820065T2 (pt)
DK (2) DK0991410T3 (pt)
EA (1) EA002619B1 (pt)
EE (1) EE04178B1 (pt)
ES (2) ES2212330T3 (pt)
HK (2) HK1025047A1 (pt)
HR (2) HRP20000006B1 (pt)
HU (2) HUP0004564A3 (pt)
ID (2) ID24481A (pt)
IL (2) IL133918A (pt)
MY (2) MY123199A (pt)
NO (2) NO317467B1 (pt)
NZ (2) NZ502209A (pt)
PL (2) PL190310B1 (pt)
PT (2) PT1000028E (pt)
RU (1) RU2213089C2 (pt)
SI (2) SI1000028T1 (pt)
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TR (2) TR200000022T2 (pt)
TW (2) TW402591B (pt)
UA (1) UA67745C2 (pt)
WO (2) WO1999002156A1 (pt)

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