BR0308721A - composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, preparação farmacêutica acondicionada, e, métodos para inibir a atividade transdutora de sinal de um receptor de c5a celular, a ligação de c5a ao receptor de c5a, e quimiotaxia celular modulada por receptor de c5a, para tratar um paciente, e para localizar receptores de c5a em uma amostra de tecido - Google Patents

composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, preparação farmacêutica acondicionada, e, métodos para inibir a atividade transdutora de sinal de um receptor de c5a celular, a ligação de c5a ao receptor de c5a, e quimiotaxia celular modulada por receptor de c5a, para tratar um paciente, e para localizar receptores de c5a em uma amostra de tecido

Info

Publication number
BR0308721A
BR0308721A BRPI0308721-2A BR0308721A BR0308721A BR 0308721 A BR0308721 A BR 0308721A BR 0308721 A BR0308721 A BR 0308721A BR 0308721 A BR0308721 A BR 0308721A
Authority
BR
Brazil
Prior art keywords
receptor
ring system
receptors
cell
compounds
Prior art date
Application number
BRPI0308721-2A
Other languages
English (en)
Inventor
George P Luke
George Maynard
Scott Mitchell
Andrew Thurkauf
Linghong Xie
Lu Yan Zhang
Suoming Zhang
He Zhao
Bertrand L Chenard
Yang Gao
Bingsong Han
Xiao Shu He
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.)
Filing date
Publication date
Application filed by Neurogen Corp filed Critical Neurogen Corp
Publication of BR0308721A publication Critical patent/BR0308721A/pt

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    • 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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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07D233/66—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 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Immunology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
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  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
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Abstract

"COMPOSTO OU SAL FARMACEUTICAMENTE ACEITáVEL DO MESMO, COMPOSIçãO FARMACêUTICA, PREPARAçãO FARMACêUTICA ACONDICIONADA, E, MéTODOS PARA INIBIR A ATIVIDADE TRANSDUTORA DE SINAL DE UM RECEPTOR DE C5a CELULAR, A LIGAçãO DE C5a AO RECEPTOR DE C5a, E QUIMIOTAXIA CELULAR MODULADA POR RECEPTOR DE C5a, PARA TRATAR UM PACIENTE, E PARA LOCALIZAR RECEPTORES DE C5a EM UMA AMOSTRA DE TECIDO". A invenção fornece imidazóis, pirazóis, piridizinas e compostos relacionados substituídos por Arila da Fórmula (I) onde o sistema de anel representado pela Fórmula (A) é um sistema de anel de heteroarila de 5 membros, em que x é 0, A é escolhido de carbono e dos heteroátomos nitrogênio, oxigênio e enxofre e E e G são independentemente carbono ou nitrogênio, contanto que o sistema de anel de heteroarila de 5 membros não contenha mais do que 3 heteroátomos ou mais do que 1 átomo de oxigênio ou enxofre ou um sistema de anel de heteroarila de 6 membros, em que x é 1, A, B, E e G são independentemente escolhidos de carbono e nitrogênio, contanto que o sistema de anel de heteroarila de 6 membros não contenha mais do que 3 átomos de nitrogênio. As variáveis remanescentes, Ar~ 1~, Ar~ 2~, R, R~ 1~, R~ 2~, R~ 3~, R~ 4~, R~ 5~, R~ 6~, y e z são aqui definidas. Tais compostos são ligandos de receptores de C5a. Os compostos preferidos da invenção atuam ligando-se aos receptores de C5a com alta afinidade e exibem atividade de antagonista neutro ou agonista inverso nos receptores de C5a. Esta invenção também diz respeito a composições farmacêuticas que compreendem tais compostos. Ela ainda diz respeito ao uso de tais compostos no tratamento de uma variedade de distúrbios inflamatórios e do sistema imune.
BRPI0308721-2A 2002-03-29 2003-03-28 composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, preparação farmacêutica acondicionada, e, métodos para inibir a atividade transdutora de sinal de um receptor de c5a celular, a ligação de c5a ao receptor de c5a, e quimiotaxia celular modulada por receptor de c5a, para tratar um paciente, e para localizar receptores de c5a em uma amostra de tecido BR0308721A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36911202P 2002-03-29 2002-03-29
US39214502P 2002-06-26 2002-06-26
PCT/US2003/009938 WO2003082829A1 (en) 2002-03-29 2003-03-28 New aryl imidazoles and related compounds as c5a receptor modulators

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BR0308721A true BR0308721A (pt) 2007-01-09

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BRPI0308721-2A BR0308721A (pt) 2002-03-29 2003-03-28 composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica, preparação farmacêutica acondicionada, e, métodos para inibir a atividade transdutora de sinal de um receptor de c5a celular, a ligação de c5a ao receptor de c5a, e quimiotaxia celular modulada por receptor de c5a, para tratar um paciente, e para localizar receptores de c5a em uma amostra de tecido

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US (2) US7186734B2 (pt)
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BRPI0518096A (pt) 2004-12-01 2008-10-28 Kalypsys Inc composto, composição farmacêutica, uso de um composto para a preparação de um medicamento para o tratamento de uma condição resultante de uma anormalidade na produção de óxido nìtrico, uso de um composto para a preparação de um medicamento para o tratamento da dor em um indivìduo com necessidade do mesmo e uso de um composto para a preparação de um medicamento para o tratamento de inibição da dimerização de inos
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JP5527923B2 (ja) * 2007-03-28 2014-06-25 公益財団法人相模中央化学研究所 パーフルオロアルキル基を有する複素環化合物およびその製造方法
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US9289467B2 (en) 2011-08-10 2016-03-22 Case Western Reserve University Compositions and methods for treating bone conditions
CN106573894B (zh) * 2014-08-13 2020-10-13 日本曹达株式会社 二芳基咪唑化合物和有害生物防除剂
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US12012385B1 (en) 2023-12-12 2024-06-18 King Faisal University 4,5-bis(4-methoxyphenyl)-1-hexyl-2-phenyl-1H-imidazole as an antimicrobial compound
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US7186734B2 (en) 2007-03-06
MXPA04009419A (es) 2005-01-25
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US20040116424A1 (en) 2004-06-17
IL164355A0 (en) 2005-12-18

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