BR9810619A - Compostos de amÈnio quaternário como antagonistas de taquicinina. - Google Patents

Compostos de amÈnio quaternário como antagonistas de taquicinina.

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Publication number
BR9810619A
BR9810619A BR9810619-8A BR9810619A BR9810619A BR 9810619 A BR9810619 A BR 9810619A BR 9810619 A BR9810619 A BR 9810619A BR 9810619 A BR9810619 A BR 9810619A
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BR
Brazil
Prior art keywords
alkyl
cycloalkyl
optionally substituted
fluoroalkoxy
fluoroalkyl
Prior art date
Application number
BR9810619-8A
Other languages
English (en)
Inventor
Sandra Marina Monaghan
David Alker
Christopher John Burns
Original Assignee
Pfizer
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of BR9810619A publication Critical patent/BR9810619A/pt

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    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
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    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
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    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
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    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems

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Abstract

Patente de Invenção: <B>"COMPOSTOS DE AMÈNIO QUATERNáRIO COMO ANTAGONISTAS DE TAQUICININA"<D>. A presente invenção proporciona um composto da fórmula: em que R é fenila, cicloalquila C~ 3~-C~ 7~ ou heteroarila, sendo cada um dos quais opcionalmente benzo- ou cicloalquila C~ 3~-C~ 7~-condensada e opcionalmente substituída, incluindo na porção benzo- ou cicloalquila C~ 3~-C~ 7~-condensada, por desde 1 até 3 substituintes cada um independentemente selecionado dentre alquila C~ 1~-C~ 4~, fluoroalquila C~ 1~-C~ 4~, alcóxi C~ 1~-C~ 4~, fluoroalcóxi C~ 1~-C~ 4~, fenóxi, alcanoílo C~ 2~-C~ 4~, halo, alcoxicarbonila C~ 1~-C~ 4~, cicloalquila C~ 3~-C~ 7~, -S(O)~ m~(alquila C~ 1~-C~ 4~), ciano, -NR R , -S(O)~ m~NR R , -NR^ 4^(alcanoílo C~ 1~-C~ 4~) e -CONR R ou R é 2,3-diidrobenzo[b]furanila ou cromanila. R é H ou alquila C~ 1~-C~ 6~; W é uma ligação direta, metileno ou etileno; X é alquileno C~ 2~-C~ 4~ não-ramificado; Y é fenila, naftila, benzila, piridila, tienila ou cicloalquila C~ 3~-C~ 7~, sendo cada uma das quais opcionalmente substituída por desde 1 até 3 substituintes cada um independentemente selecionado dentre alquila C~ 1~-C~ 4~, fluoroalquila C~ 1~-C~ 4~, alcóxi C~ 1~-C~ 4~, fluoroalcóxi C~ 1~-C~ 4~, halo e ciano; Ar é fenila, naftila, benzila, tienila, benzo[b]tienila ou indolila, sendo cada uma das quais opcionalmente substituída por desde 1 até 3 substituintes cada um independentemente selecionado dentre alquila C~ 1~-C~ 4~, fluoroalquila C~ 1~-C~ 4~, alcóxi C~ 1~-C~ 4~, fluoroalcóxi C~ 1~-C~ 4~, halo e ciano, ou Ar é 1,3-benzodioxolan-4 ou 5-ila ou 1,4-benzodioxolan-5 ou 6-ila; Z^ A^ é um ânion farmaceuticamente aceitável; com a condição de que quando W é uma ligação direta e R é hetero-arila opcionalmente condensada e opcionalmente substituída, a referida heteroarila está ligada por um átomo de carbono do anel ao grupo carbonila. Os compostos são antagonistas de taquicinina.
BR9810619-8A 1997-06-18 1998-06-05 Compostos de amÈnio quaternário como antagonistas de taquicinina. BR9810619A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9712882.1A GB9712882D0 (en) 1997-06-18 1997-06-18 Quaternary ammonium compounds
PCT/EP1998/003500 WO1998057972A1 (en) 1997-06-18 1998-06-05 Quaternary ammonium compounds as tachykinin antagonists

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BR9810619A true BR9810619A (pt) 2000-09-12

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BR9810619-8A BR9810619A (pt) 1997-06-18 1998-06-05 Compostos de amÈnio quaternário como antagonistas de taquicinina.

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EP (1) EP0994876B1 (pt)
JP (1) JP3280993B2 (pt)
KR (1) KR100345389B1 (pt)
CN (1) CN1199971C (pt)
AP (1) AP947A (pt)
AR (1) AR012249A1 (pt)
AT (1) ATE275564T1 (pt)
AU (1) AU726027B2 (pt)
BG (1) BG63341B1 (pt)
BR (1) BR9810619A (pt)
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CO (1) CO4940478A1 (pt)
DE (1) DE69826129T2 (pt)
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EA (1) EA002424B1 (pt)
ES (1) ES2227856T3 (pt)
GB (1) GB9712882D0 (pt)
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WO (1) WO1998057972A1 (pt)
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KR100591027B1 (ko) * 1997-12-26 2006-06-22 아스텔라스세이야쿠 가부시키가이샤 서방성 의약 조성물
JP4546589B2 (ja) * 1998-04-23 2010-09-15 武田薬品工業株式会社 ナフタレン誘導体
AU7552401A (en) * 2000-06-12 2001-12-24 Univ Rochester Method of treating symptoms of hormonal variation, including hot flashes, using tachykinin receptor antagonist
AU2002230665A1 (en) * 2000-12-06 2002-06-18 Sepracor, Inc. 4,4-disubstituted piperidines for use as dopamine, serotonin and norepinephrine ligands
WO2003101459A1 (en) * 2002-05-29 2003-12-11 The Regents Of The University Of California Antagonizing nk1 receptors inhibits consumption of substances of abuse
WO2004091597A2 (en) * 2003-04-15 2004-10-28 Pharmacia & Upjohn Company Llc Method of treating irritable bowel syndrome (ibs)
JP2007536270A (ja) * 2004-05-07 2007-12-13 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ イミダゾール誘導体のスケールアップ可能な合成
CN101641099A (zh) 2007-01-24 2010-02-03 葛兰素集团有限公司 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物

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US3991201A (en) * 1974-06-27 1976-11-09 Janssen Pharmaceutica N.V. 1-(β-Aryl-β-R-ethyl)imidazoles as antimicrobial agents
US5583134A (en) * 1992-09-30 1996-12-10 Sanofi 1-azoniabicyclo[2.2.2] octanes and pharmaceutical compositions in which they are present
FR2696178B1 (fr) 1992-09-30 1994-12-30 Sanofi Elf Amides basiques quaternaires, procédé pour leur préparation et compositions pharmaceutiques en contenant.

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CA2291975A1 (en) 1998-12-23
KR100345389B1 (ko) 2002-07-24
PE80099A1 (es) 1999-08-25
HUP0003962A3 (en) 2001-12-28
AU726027B2 (en) 2000-10-26
HN1998000087A (es) 1998-10-22
GB9712882D0 (en) 1997-08-20
CA2291975C (en) 2004-02-10
WO1998057972A1 (en) 1998-12-23
NO995782D0 (no) 1999-11-25
EA199900986A1 (ru) 2000-06-26
US6207678B1 (en) 2001-03-27
TW479055B (en) 2002-03-11
EP0994876A1 (en) 2000-04-26
SK283346B6 (sk) 2003-06-03
PL337713A1 (en) 2000-08-28
AR012249A1 (es) 2000-09-27
UA62966C2 (en) 2004-01-15
YU64699A (sh) 2002-06-19
MA26509A1 (fr) 2004-12-20
UY25045A1 (es) 2000-09-29
DE69826129T2 (de) 2005-09-22
IL133079A (en) 2004-06-01
PT994876E (pt) 2005-01-31
TR199903135T2 (xx) 2000-04-21
BG63341B1 (bg) 2001-10-31
JP2000513030A (ja) 2000-10-03
AP947A (en) 2001-03-08
AP9801262A0 (en) 1998-06-30
US6380396B1 (en) 2002-04-30
CN1260795A (zh) 2000-07-19
ATE275564T1 (de) 2004-09-15
NO995782L (no) 2000-02-16
HRP980337B1 (en) 2003-02-28
PA8452501A1 (es) 2000-05-24
CO4940478A1 (es) 2000-07-24
IS5269A (is) 1999-11-23
NZ501286A (en) 2000-07-28
TNSN98089A1 (fr) 2005-03-15
SI0994876T1 (en) 2005-02-28
PL189557B1 (pl) 2005-08-31
DZ2524A1 (fr) 2003-02-01
AU8215398A (en) 1999-01-04
HUP0003962A2 (hu) 2001-04-28
ID23410A (id) 2000-04-20
ZA985239B (en) 1999-12-17
KR20010013909A (ko) 2001-02-26
EA002424B1 (ru) 2002-04-25
ES2227856T3 (es) 2005-04-01
EP0994876B1 (en) 2004-09-08
IL133079A0 (en) 2001-03-19
MY136376A (en) 2008-09-30
DE69826129D1 (de) 2004-10-14
JP3280993B2 (ja) 2002-05-13
HRP980337A2 (en) 1999-02-28
IL155621A0 (en) 2003-11-23
CN1199971C (zh) 2005-05-04
SK174499A3 (en) 2001-05-10
OA11235A (en) 2003-07-09

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