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1. 发明申请

WO2004099146A1 BENZAMIDE INHIBITORS OF THE P2X7 RECEPTOR 审中-公开
标题翻译： P2X7受体的苯扎嗪抑制剂
公开(公告)号：WO2004099146A1
公开(公告)日：2004-11-18
申请号：PCT/IB2004/001525
申请日：2004-05-10
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob , SUBRAMANYAM, Chakrapani
发明人： DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob , SUBRAMANYAM, Chakrapani
IPC分类号： C07D213/54
CPC分类号： C07D231/12 , C07D213/56 , C07D233/64 , C07D237/14 , C07D249/04 , C07D261/08 , C07D277/30 , C07D403/12 , C07D405/06
摘要： The present invention provides benzamide inhibitors of the P2X 7 receptor of the formula (I), wherein R 1 -R 3 are as defined herein. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明提供式（I）的P2X7受体的苯甲酰胺抑制剂，其中R 1 -R 3如本文所定义。本发明的化合物可用于治疗IL-1介导的病症，包括但不限于炎性疾病如骨关节炎和类风湿性关节炎; 过敏，哮喘，COPD，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

2. 发明申请

WO2004058270A1 3-(3,5-DIOXO-4,5-DIHYDRO-3H-(1,2,4)TRIAZIN-2-YL)-BENZAMIDE DERIVATIVES AS P2X7-INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： 3-（3,5-二氧代-4,5-二氢-3H-（1,2,4）三嗪-2-基） - 苯甲酰胺衍生物作为治疗炎症性疾病的P2X7-抑制剂
公开(公告)号：WO2004058270A1
公开(公告)日：2004-07-15
申请号：PCT/IB2003/006254
申请日：2003-12-19
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob
发明人： DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob
IPC分类号： A61K31/53
CPC分类号： C07D253/075 , C07D401/06 , C07D405/06
摘要： The present invention provides benzamide inhibitors of the P2X 7 receptor of the formula (I), wherein R 1 and R 2 are as defined in claim 1. R 3 is a nitrogen linked (C 1 -C 10 ) heterocyclyl of formula (II), wherein R 4 and R 7 are as defined in claim 1. The compounds of the invention are useful in the treatment of IL-1 mediated disorders, including, without limitation, inflammatory diseases such as osteoarthritis and rheumatoid arthritis; allergies, asthma, COPD, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明提供式（I）的P2X7受体的苯甲酰胺抑制剂，其中R 1和R 2如权利要求1中所定义。R 3是式（I）的氮连接的（C 1 -C 10）杂环基（II），其中R 4和R 7如权利要求1中所定义。本发明的化合物可用于治疗IL-1介导的病症，包括但不限于炎性疾病如骨关节炎和类风湿病关节炎; 过敏，哮喘，COPD，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

3. 发明申请

WO2002072579A1 TRIAZOLOPYRIDINES AS ANTI-INFLAMMATORY AGENTS 审中-公开
标题翻译：三唑并吡啶作为抗炎剂
公开(公告)号：WO2002072579A1
公开(公告)日：2002-09-19
申请号：PCT/IB2002/000424
申请日：2002-02-08
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob , LAIRD, Ellen, Ruth , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
发明人： DOMBROSKI, Mark, Anthony , DUPLANTIER, Allen, Jacob , LAIRD, Ellen, Ruth , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R 2 is selected from the group consisting of hydrogen, (C 1 -C 6 ) alkyl or other suitable substituents; R 3 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式I的新型三唑并 - 吡啶，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的5元杂环，其中至少一个所述杂原子必须是氮; R 2选自氢，（C 1 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s是0-5的整数; 制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫性疾病和其他疾病。

4. 发明申请

WO2003045400A1 COMBINATION OF AN IL-1/18 INHIBITOR WITH A TNF INHIBITOR FOR THE TREATMENT OF INFLAMMATION 审中-公开
标题翻译： IL-1/18抑制剂与用于治疗炎症的TNF抑制剂的组合
公开(公告)号：WO2003045400A1
公开(公告)日：2003-06-05
申请号：PCT/IB2002/004367
申请日：2002-10-18
申请人： PFIZER PRODUCTS INC. , GABEL, Christopher, Allen , DOMBROSKI, Mark, Anthony
发明人： GABEL, Christopher, Allen , DOMBROSKI, Mark, Anthony
IPC分类号： A61K31/64
CPC分类号： A61K45/06 , A61K31/00 , A61K31/34 , A61K31/64 , A61K2300/00
摘要： The invention relates to compositions and methods for treating or preventing inflammation, including rheumatoid arthritis (RA). The method comprises administering to mammals in need thereof an effective amount of a composition containing an agent that inhibits IL-1/18 combination with a TNF inhibitor.
摘要翻译：本发明涉及用于治疗或预防炎症的组合物和方法，包括类风湿性关节炎（RA）。该方法包括向有需要的哺乳动物施用有效量的含有抑制IL-1/18与TNF抑制剂组合的药剂的组合物。

5. 发明申请

WO2004020440A1 DI AND TRIFLUORO-TRIAZOLO-PYRIDINES ANTI-INFLAMMATORY COMPOUNDS 审中-公开
标题翻译： DI和三氟乙酸吡啶类抗炎化合物
公开(公告)号：WO2004020440A1
公开(公告)日：2004-03-11
申请号：PCT/IB2003/003847
申请日：2003-08-19
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
发明人： DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention relates to novel triazolo-pyridines of the formula (I) wherein R 1 is fluoro; s is an integer from two to three; R 2 is (C 3 -C 6 )cycloalkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C l -C 4 )alkyl, hydroxy, (C l -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C=O)-0-; or R 2 is (C l -C 6 )alkyl optionally substituted by one or two moieties independently selected from the group consisting of halo, (C 1 -C 6 )alkyl, hydroxy, (C 1 -C 6 )alkoxy and (C 1 -C 6 )alkyl-(C=O)-0-; with the proviso that said compound of formula (I) cannot be 6-[4-(2,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; or 6-[4-(3,4-Difluoro-phenyl)-oxazol-5-yl]-3-isopropyl-[1,2,4]triazolo[4,3-a]pyridine; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式（I）的新的三唑并 - 吡啶，其中R 1是氟; s是从2到3的整数; R 2是任选被一个或两个独立地选自卤素，（C 1 -C 4）烷基，羟基，（C 1 -C 4）烷基的部分取代的（C 3 -C 6）环烷基（C 1 -C 6）烷基 - （C = O）-O-;（C 1 -C 6）烷基 - （C = O）或R 2是任选被一个或两个独立地选自以下的部分取代的（C 1 -C 6）烷基：卤素，（C 1 -C 6）烷基，羟基，（C 1 -C 6）（C 1 -C 6）烷基 - （C = O）-O-;（C 1 -C 6）烷基 - （C = O）条件是所述式（I）化合物不能是6- [4-（2,4-二氟 - 苯基） - 恶唑-5-基] -3-异丙基 - [1,2,4]三唑并[4,5- 3-a]吡啶; 或6- [4-（3,4-二氟 - 苯基） - 恶唑-5-基] -3-异丙基 - [1,2,4]三唑并[4,3-a]吡啶; 制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作中的再灌注或缺血，自身免疫疾病和其他疾病。

6. 发明申请

WO2002072576A1 BENZIMIDAZOLE ANTI-INFLAMMATORY COMPOUNDS 审中-公开
标题翻译：苯并咪唑抗炎化合物
公开(公告)号：WO2002072576A1
公开(公告)日：2002-09-19
申请号：PCT/IB2002/000334
申请日：2002-01-30
申请人： PFIZER PRODUCTS INC. , DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
发明人： DOMBROSKI, Mark, Anthony , LETAVIC, Michael, Anthony , MCCLURE, Kim, Francis
IPC分类号： C07D403/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D487/04
摘要： The present invention relates to novel triazolo-pyridines of the formula (I) wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R 2 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; R 3 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion of ischemia in stroke or heart attack, autoimmune diseases and other disorders.
摘要翻译：本发明涉及式（I）的新型三唑并 - 吡啶，其中Het是含有一至二个选自氮，硫和氧的杂原子的任选取代的5元杂环，其中至少一个所述杂原子必须是氮; R 2选自氢，（C 1 -C 6）烷基或其它合适的取代基; R 3选自氢，（C 1 -C 6）烷基或其它合适的取代基; s是0-5的整数; 制备中间体，含有它们的药物组合物及其药物用途。本发明的化合物是MAP激酶的有效抑制剂，优选p38激酶。它们可用于治疗炎症，骨关节炎，类风湿性关节炎，癌症，中风或心脏病发作缺血再灌注，自身免疫疾病和其他疾病。

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