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公开(公告)号：US06696464B2
公开(公告)日：2004-02-24
申请号：US10094760
申请日：2002-03-11
IPC分类号： A61K3144
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; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)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五元杂环，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的整数 -5;用于制备的中间体，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。
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公开(公告)号：US07186742B2
公开(公告)日：2007-03-06
申请号：US10844251
申请日：2004-05-12
IPC分类号： A61K31/415 , C07D231/12 , C07D231/14 , A61K31/4192 , A61K31/4164 , A61K31/42 , C07D249/06 , C07D261/12 , C07D233/68 , C07D233/70
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 P2X7 receptor of the formula: wherein R1–R3 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.
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公开(公告)号：US07176202B2
公开(公告)日：2007-02-13
申请号：US11260075
申请日：2005-10-27
IPC分类号： C07D253/075 , A61K31/53 , A61P19/02
CPC分类号： C07D253/075 , C07D401/06 , C07D405/06
摘要： The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 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： 本发明提供下式的P2X 7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。
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公开(公告)号：US07071223B1
公开(公告)日：2006-07-04
申请号：US10748342
申请日：2003-12-30
IPC分类号： A61K31/41 , C07D249/12
CPC分类号： C07D249/12
摘要： The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1–R3 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： 本发明提供下式的P2X 7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。
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公开(公告)号：US06974812B2
公开(公告)日：2005-12-13
申请号：US10748340
申请日：2003-12-30
IPC分类号： A61K20060101 , A61K31/53 , A61K31/5377 , A61P19/02 , C07D20060101 , C07D253/02 , C07D253/06 , C07D253/075 , C07D295/02 , C07D401/06 , C07D405/06
CPC分类号： C07D253/075 , C07D401/06 , C07D405/06
摘要： The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 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： 本发明提供下式的P2X 7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。
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公开(公告)号：US07671053B2
公开(公告)日：2010-03-02
申请号：US12147212
申请日：2008-06-26
IPC分类号： C07D253/075 , A61K31/53 , A61P11/06
CPC分类号： C07D253/075 , C07D401/06 , C07D405/06
摘要： The present invention provides benzamide inhibitors of the P2X7 receptor of the formula: wherein R1-R3 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： 本发明提供下式的P2X7受体的苯甲酰胺抑制剂：其中R1-R3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。
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公开(公告)号：US07553972B2
公开(公告)日：2009-06-30
申请号：US11673246
申请日：2007-02-09
IPC分类号： C07D211/70 , C07D241/02 , C07D237/00
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 P2X7 receptor of the formula: wherein R1-R3 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： 本发明提供下式的P2X7受体的苯甲酰胺抑制剂：其中R1-R3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。
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公开(公告)号：US20080280933A1
公开(公告)日：2008-11-13
申请号：US11780579
申请日：2007-07-20
申请人： Ivan Efremov , Bruce N. Rogers , Allen J. Duplantier , Lei Zhang , Qian Zhang , Noha S. Maklad , Edelweiss Evrard , Michael A. Brodney
发明人： Ivan Efremov , Bruce N. Rogers , Allen J. Duplantier , Lei Zhang , Qian Zhang , Noha S. Maklad , Edelweiss Evrard , Michael A. Brodney
IPC分类号： C07D401/02 , A61K31/454 , A61K31/438 , C07D487/10 , A61P25/00
CPC分类号： C07D401/06 , C07D405/14 , C07D413/14 , C07D471/10 , C07D491/052 , C07D491/107
摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
摘要翻译： 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。
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公开(公告)号：US07235549B2
公开(公告)日：2007-06-26
申请号：US11253112
申请日：2005-10-18
IPC分类号： C07D279/16 , A61K31/5415 , A61P19/02
CPC分类号： C07D405/12 , C07D211/76 , C07D213/64 , C07D241/08 , C07D249/12 , C07D263/24 , C07D279/16 , C07D409/12
摘要： The present invention relates to novel to P2X7 inhibitors of formula I and to processes for their preparation, intermediates useful in their preparation, pharmaceutical compositions containing them, and their use in therapy. The active compounds of the present invention are potent inhibitors of P2X7 and as such are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.
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公开(公告)号：US06380218B1
公开(公告)日：2002-04-30
申请号：US09308956
申请日：1999-05-27
申请人： Anthony Marfat , Robert J. Chambers , John W. Watson , John B. Cheng , Allen J. Duplantier , Edward F. Kleinman
发明人： Anthony Marfat , Robert J. Chambers , John W. Watson , John B. Cheng , Allen J. Duplantier , Edward F. Kleinman
IPC分类号： A61K314436
CPC分类号： C07D213/64 , C07D213/643 , C07D213/75 , C07D213/82 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12
摘要： A compound of formula (I) wherein m, n, o, p, q, r, A, B, D, E, R1, R2,R3, R4, R5, R6, R7 and R8 are as defined in the description, useful in the treatment of respiratory, allergic, rheumatoid, body weight regulation, inflammatory and central nervous system disorders such as asthma, chronic obstructive pulmonary disease, adult respiratory diseases syndrome, shock, fibrosis, pulmonary hypersensitivity, allergic rhinitis, atopic dermatitis, psoriasis, weight control, rheumatoid arthritis, cachexia, crohn's disease, ulcerative colitis, arthritic conditions and other inflammatory diseases, depression, multi-infarct dementia and AIDS.
摘要翻译： 其中m，n，o，p，q，r，A，B，D，E，R1，R2，R3，R4，R5，R6，R7和R8如式中所定义， 可用于治疗呼吸道，过敏性，类风湿，体重调节，炎症和中枢神经系统疾病如哮喘，慢性阻塞性肺疾病，成人呼吸道疾病综合征，休克，纤维化，肺过敏，过敏性鼻炎，特应性皮炎，牛皮癣， 重症控制，类风湿关节炎，恶病质，克罗恩病，溃疡性结肠炎，关节炎等炎症性疾病，抑郁症，多发性梗塞性痴呆和艾滋病。
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