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BR9807858A - Derivados de amida do ácido heteroaril-hexanóico, suas preparaçÊes e seus usos como inibidores seletios de mip-1.alfa ligando aos seus receptores ccr1 - Google Patents

Derivados de amida do ácido heteroaril-hexanóico, suas preparaçÊes e seus usos como inibidores seletios de mip-1.alfa ligando aos seus receptores ccr1

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Publication number
BR9807858A
BR9807858A BR9807858-5A BR9807858A BR9807858A BR 9807858 A BR9807858 A BR 9807858A BR 9807858 A BR9807858 A BR 9807858A BR 9807858 A BR9807858 A BR 9807858A
Authority
BR
Brazil
Prior art keywords
alkyl
optionally substituted
heteroaryl
mip
selective inhibitors
Prior art date
Application number
BR9807858-5A
Other languages
English (en)
Inventor
Matthew Frank Brown
John Charles Kath
Christopher Stanley Poss
Original Assignee
Pfizer
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of BR9807858A publication Critical patent/BR9807858A/pt

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    • C07D213/02Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D213/82Amides; Imides in position 3
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Abstract

Patente de Invenção: <B>"DERIVADOS DE AMIDA DO áCIDO HETEROARIL-HEXANóICO, SUAS PREPARAçõES E SEUS USOS COMO INIBIDORES SELETIVOS DE MIP-1.ALFA LIGANDO AOS SEUS RECEPTORES CCR1"<D>. Compostos da fórmula em que R^ 1^ é (C~ 2~- C~ 9~) heteroarila opcionalmente substituída; R^ 2^ é fenil -(CH~ 2~)~ m~-, naftil-(CH~ 2~)~ m~-, (C~ 3~ -C~ 10~) cicloalquil- (CH~ 2~)~ m~, (C~ 1~ - C~ 6~) alquila ou (C~ 2~- C~ 9~) heteroaril-(CH~ 2~)~ m~-, opcionalmente substituídos, m é um inteiro de zero a quatro; R^ 3^ é hidrogênio, ou (C~ 1-C~ 10~)ciclo alquil-(CH~ 2)~ n-, (C~ 2~-C~ 9~)heterociclo-alquil-(CH~ 2)~ n~-, (C~ 2~-C~ 9~)heteroaril-(CH~ 2~)~ n~- ou aril-(CH~ 2~)~ n~-, opcionalmente substituídos, n é um inteiro de zero a seis; ou R^ 3^ e o carbono ao qual está ligado formam um anel de cinco a sete membros fundido e/ou opcionalmente substituído; R^ 4^ é hidrogênio, (C~ 1~-C~ 6~)alquila, hidróxi, (C~ 1~-C~ 6~)alcóxi, hidróxi (C~ 1~-C~ 6~)alquila, (C~ 1~-C~ 6~) alcoxiCO, (C~ 3~-C~ 10~)cicloalquil-(CH~ 2~)~ p~-, ou (C~ 2~-C~9~)heterocicloalquil-(CH~ 2~)~ p~-, (C~ 2~-C~ 9~)heteroaril-(CH~ 2~)~ p~-, fenil-(CH~ 2~)~ p~- ou naftil-(CH~ 2~)~ p~-, opcionalmente substituídos, p é um inteiro de zero a quatro; ou R^ 4^ e R^ 5^ juntos com o átomo de nitrogênio ao qual estão ligados formam um grupo (C~ 2~-C~ 9~) heterocicloalquila opcionalmente substituído; R^ 5^ é hidrogênio, (C~ 1~-C~ 6~)alquila ou amino. Os presentes compostos são inibidores potentes e seletivos de MIP-1-alfa ligando os sesu inibidores CCR1, e são úteis para tratar inflamações e outros distúrbios imunológicos.
BR9807858-5A 1997-02-26 1998-02-05 Derivados de amida do ácido heteroaril-hexanóico, suas preparaçÊes e seus usos como inibidores seletios de mip-1.alfa ligando aos seus receptores ccr1 BR9807858A (pt)

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US3916997P 1997-02-26 1997-02-26
PCT/US1998/001568 WO1998038167A1 (en) 1997-02-26 1998-02-05 Heteroaryl-hexanoic acid amide derivatives, their preparation and their use as selective inhibitors of mip-1-alpha binding to its ccr1 receptor

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