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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：US07214677B2
公开(公告)日：2007-05-08
申请号：US10292887
申请日：2002-11-12
IPC分类号： C07D253/075 , A61K31/53 , 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.
摘要翻译： 本发明涉及新型的式I的P2X 7 N抑制剂及其制备方法，可用于其制备的中间体，含有它们的药物组合物及其在治疗中的用途。 本发明的活性化合物是P2X7的有效抑制剂，因此可用于治疗炎症，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。
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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：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：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：US20120252758A1
公开(公告)日：2012-10-04
申请号：US13433452
申请日：2012-03-29
申请人： Martin Youngjin Pettersson , Douglas Scott Johnson , Chakrapani Subramanyam , Christopher John O'Donnell , Christopher William Am Ende , Benjamin Adam Fish , Michael Eric Green , Patrick Bradley Mullins , Cory Michael Stiff , Tuan Phong Tran , Thayalan Navaratnam
发明人： Martin Youngjin Pettersson , Douglas Scott Johnson , Chakrapani Subramanyam , Christopher John O'Donnell , Christopher William Am Ende , Benjamin Adam Fish , Michael Eric Green , Patrick Bradley Mullins , Cory Michael Stiff , Tuan Phong Tran , Thayalan Navaratnam
IPC分类号： A61K31/4985 , C07F7/10 , A61K31/695 , C07D401/04 , A61P25/00 , A61P25/18 , A61P25/28 , C07D471/04 , A61K31/551
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/695 , A61K45/06 , C07D401/04 , C07D491/048 , C07F7/0812
摘要： Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. 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，其中所述化合物具有如本文所定义的式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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7.发明授权2-saccharinylmethyl aryl carboxylates useful as proteolytic enzyme inhibitors and compositions and method of use thereof 失效可用作蛋白水解酶抑制剂的2-糖基甲基芳基羧酸盐及其组合物及其使用方法
公开(公告)号：US5597841A
公开(公告)日：1997-01-28
申请号：US445118
申请日：1995-05-19
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Virendra Kumar , Chakrapani Subramanyam , Ranjit C. Desai , Dennis J. Hlasta , Manohar T. Saindane , Malcolm R. Bell , John J. Court , Robert P. Farrell
IPC分类号： C07D275/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541 , A61K31/425
CPC分类号： C07D275/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541
摘要： 4-R.sup.4 -R.sup.5 -2-Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-2-糖基甲基芳基羧酸盐通过在酸 - 受体存在下使4-R 4 -R 5 - 2-卤代甲基糖精与芳基羧酸反应来制备。
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8.发明授权Substituted heterocyclylisoquinolinium salts and compositions and method of use thereof 失效取代的杂环基异喹啉鎓盐及其组合物及其使用方法
公开(公告)号：US5569655A
公开(公告)日：1996-10-29
申请号：US283319
申请日：1994-07-29
申请人： John A. Dority, Jr. , William G. Earley , Virendra Kumar , John P. Mallamo , Matthew S. Miller , Chakrapani Subramanyam
发明人： John A. Dority, Jr. , William G. Earley , Virendra Kumar , John P. Mallamo , Matthew S. Miller , Chakrapani Subramanyam
IPC分类号： C07D491/22 , A61K31/435 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/535 , A61P25/18 , A61P25/28 , C07D471/18 , C07D498/18 , C07D498/22 , C07D513/18 , C07D513/22 , C07D519/00 , A61K31/54 , A61K31/415 , A61K31/425 , C07D415/00 , C07D417/02 , C07D463/22 , C07D471/02
CPC分类号： C07D471/18 , C07D498/18 , C07D513/18 , Y10S514/884
摘要： Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.
摘要翻译： 取代的杂环基异喹啉鎓盐，含有它们的药物组合物和用于治疗或预防神经变性疾病或利用它们的神经毒性损伤的方法。
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公开(公告)号：US5371074A
公开(公告)日：1994-12-06
申请号：US67637
申请日：1993-05-24
申请人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
发明人： Richard P. Dunlap , Neil W. Boaz , Albert J. Mura , Dennis J. Hlasta , Ranjit C. Desai , Chakrapani Subramanyam , Lee H. Latimer , Eric P. Lodge
IPC分类号： A61K31/425 , A61K31/415 , A61K31/428 , A61K31/47 , A61P29/00 , A61P43/00 , C07D275/04 , C07D275/06 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07F9/6541 , A61K31/535
CPC分类号： C07D275/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , C07F9/6541
摘要： Novel 2-substituted saccharins which inhibit the enzymatic activity of proteolytic enzymes, are useful in the treatment of degenerative diseases and have the formula 0010wherein:L is --O--, --S--, --SO-- or --SO.sub.2 --; m and n are each independently 0 or 1; R.sub.1 is halo, lower-alkanoyl, 1-oxophenalenyl, phenyl or substituted phenyl, heterocyclyl or substitued heterocyclyl or, when L is --O-- and n is 1, cycloheptatrienon-2-yl or, when L is --S-- and n is 1, cyano or lower-alkoxythiocarbonyl or, when L is --SO.sub.2 -- and n is 1, lower-alkyl or trifluoromethyl; R.sub.2 is hydrogen, lower-alkoxycarbonyl, phenyl or phenylthio; and R.sub.3 and R.sub.4 are each hydrogen or various substituents and processes for preparation and pharmaceutical compositions and method of use thereof are disclosed.
摘要翻译： 抑制蛋白水解酶的酶活性的新型2-取代糖精可用于治疗退行性疾病，并具有式0010其中：L是-O - ， - S - ， - SO-或-SO 2 - ; m和n各自独立地为0或1; R 1为卤素，低级烷酰基，1-氧代对苯二烯基，苯基或取代的苯基，杂环基或取代的杂环基，或当L为-O-并且n为1时，环庚三烯-2-基或当L为-S-且n为 1，氰基或低级烷氧基硫代羰基，或当L为-SO 2 - 且n为1时，为低级烷基或三氟甲基; R2是氢，低级烷氧基羰基，苯基或苯硫基; 并且R 3和R 4各自为氢或各种取代基和制备方法，并且公开了药物组合物及其使用方法。
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公开(公告)号：US5306818A
公开(公告)日：1994-04-26
申请号：US965593
申请日：1992-10-23
IPC分类号： A61K31/425 , A61K31/435 , A61P1/00 , A61P11/00 , A61P29/00 , A61P43/00 , C07D275/06 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541
CPC分类号： C07D275/06 , C07D413/10 , C07D413/12 , C07D417/04 , C07D417/12 , C07F9/6541
摘要： 4-R.sup.4 -R.sup.5 -Saccharinylmethyl aryl carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R.sup.4 -R.sup.5 -2-halomethylsaccharin with an arylcarboxylic acid in the presence of an acid-acceptor.
摘要翻译： 可用于治疗退行性疾病的4-R4-R5-糖基甲基芳基羧酸酯通过在酸 - 受体的存在下使4-R 4 -R 5 -2-卤代甲基糖精与芳基羧酸反应来制备。
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