BR0017338A - Composto, processo para preparar um composto, composição farmacêutica, e métodos para tratar um paciente, para inibir quimiotaxia celular promovida com c5a, para localizar receptores de c5a em um tecido, e para reduzir a gravidade ou frequência de uma ou mais sequelas inflamatórias de transplante de órgão - Google Patents

Composto, processo para preparar um composto, composição farmacêutica, e métodos para tratar um paciente, para inibir quimiotaxia celular promovida com c5a, para localizar receptores de c5a em um tecido, e para reduzir a gravidade ou frequência de uma ou mais sequelas inflamatórias de transplante de órgão

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Publication number
BR0017338A
BR0017338A BR0017338-0A BR0017338A BR0017338A BR 0017338 A BR0017338 A BR 0017338A BR 0017338 A BR0017338 A BR 0017338A BR 0017338 A BR0017338 A BR 0017338A
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BR
Brazil
Prior art keywords
compound
receptors
treating
pharmaceutical composition
sequelae
Prior art date
Application number
BR0017338-0A
Other languages
English (en)
Inventor
Andrew Thurkauf
Xiaoyan Zhang
Xia-Shu He
He Zhao
John Peterson
George Maynard
Robert Ohliger
Original Assignee
Neurogen Corp
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.)
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Publication date
Application filed by Neurogen Corp filed Critical Neurogen Corp
Publication of BR0017338A publication Critical patent/BR0017338A/pt

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    • C07D207/30—Heterocyclic 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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic 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 two 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
    • C07D207/325—Heterocyclic 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 two 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 with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
    • C07D207/327—Radicals substituted by carbon 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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Abstract

"COMPOSTO, PROCESSO PARA PREPARAR UM COMPOSTO, COMPOSIçãO FARMACêUTICA, E MéTODOS PARA TRATAR UM PACIENTE, PARA INIBIR QUIMIOTAXIA CELULAR PROMOVIDA COM C5a, PARA LOCALIZAR RECEPTORES DE C5a EM UM TECIDO, E PARA REDUZIR A GRAVIDADE OU FREQuêNCIA DE UMA OU MAIS SEQuELAS INFLAMATóRIAS DE TRANSPLANTE DE ORGãO". A invenção inclui moléculas orgânicas, não peptidomiméticas, não peptídicas, de baixo peso molecular, que podem atuar como moduladores de receptores de C5a de complemento mamífero, de preferência aquelas que atuam como ligandos de receptor de C5a com alta afinidade, e também ligandos de tipo que podem atuar como antagonistas ou agonistas inversos de receptores de C5a de complemento. Compostos preferidos da invenção possuem algumas ou todas as propriedades a seguir, que são: 1) estrutura multi-arila; 2) estrutura heteroarila; 3) uma dose oral farmaceuticamente aceitável pode proporcionar um efeito detectável in vivo; 4) compreender menos que quatro ligações amida ou, de preferência, nenhuma, e 5) capaz de HABITING/inibir* quimiotaxia de leucócitos a concentrações nanomolares ou sub-nanomolares. A invenção também inclui composição farmacêutica compreendendo esses compostos e o uso desses compostos no tratamento de uma variedade de distúrbios inflamatórios e do sistema imunológico.
BR0017338-0A 2000-09-29 2000-09-29 Composto, processo para preparar um composto, composição farmacêutica, e métodos para tratar um paciente, para inibir quimiotaxia celular promovida com c5a, para localizar receptores de c5a em um tecido, e para reduzir a gravidade ou frequência de uma ou mais sequelas inflamatórias de transplante de órgão BR0017338A (pt)

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EP1322309B1 (en) 2008-08-13
JP2004525873A (ja) 2004-08-26
DE60039921D1 (de) 2008-09-25
CN1454086A (zh) 2003-11-05
AU7622500A (en) 2002-07-01
YU23503A (sh) 2006-03-03
NO20031370D0 (no) 2003-03-26
WO2002049993A2 (en) 2002-06-27
EP1322309A4 (en) 2004-10-13
KR20030060887A (ko) 2003-07-16
ATE404553T1 (de) 2008-08-15
EP1322309A2 (en) 2003-07-02
WO2002049993A3 (en) 2003-02-20
MXPA03002788A (es) 2004-12-13
NO20031370L (no) 2003-05-30
JP5260818B2 (ja) 2013-08-14
IL154993A0 (en) 2003-10-31

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