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1.发明授权Fused ring system containing indole as M4 selective aza-anthracene muscarinic receptor antagonists 失效含有吲哚作为M4选择性氮杂 - 蒽类毒蕈碱受体拮抗剂的稠环体系公开(公告)号：US06500837B2
公开(公告)日：2002-12-31
申请号：US09952735
申请日：2001-09-14
IPC分类号： A61K314745
CPC分类号： C07D471/14
摘要： Disclosed are compounds of the Formula I and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, wherein R1 is hydrogen, lower alkyl, COOR7, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl, or (un)substituted heteroarylalkyl; R3 is hydrogen or lower alkyl; R2, R4, R5, and R6 independently represent hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, cyano, nitro, amino, mono- or dialkylamino, carboxy, alkoxycarbonyl, carbamoyl, sulfamoyl, trifluoromethyl, or alkylthio; R7 is hydrogen or lower alkyl; and R8 is hydrogen or oxo. Also provided is a method for selectively antagonizing the M4 muscarinic receptor and a method for treating Parkinson's disease.
摘要翻译： 公开了式I化合物及其药学上可接受的盐，酯，酰胺和前药，其中R1是氢，低级烷基，COOR7，（未）取代的芳基，（未）取代的杂芳基，（未）取代的芳烷基或（未） 取代的杂芳基烷基; R 3是氢或低级烷基; R 2，R 4，R 5和R 6独立地表示氢，卤素，低级烷基，低级烷氧基，羟基，氰基，硝基，氨基，单或二烷基氨基，羧基，烷氧基羰基，氨基甲酰基， ，三氟甲基或烷硫基; R 7为氢或低级烷基; 并且R 8是氢或氧代。还提供了选择性拮抗M4毒蕈碱受体的方法和治疗帕金森病的方法。
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2.发明授权2-substituted-4H-3, 1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease for the treatment of inflammatory processes 失效2-取代-4H-3,1-苯并恶嗪-4-酮和苯并噻嗪-4-酮作为补体C1r蛋白酶的抑制剂，用于治疗炎症过程
公开(公告)号：US5652237A
公开(公告)日：1997-07-29
申请号：US501507
申请日：1995-08-10
申请人： Corinne Elizabeth Augelli-Szafran , Bradley William Caprathe , John Lodge Gilmore , Sheryl Jeanne Hays , Juan Carlos Jaen , Jan Ruth Penvose-Yi
发明人： Corinne Elizabeth Augelli-Szafran , Bradley William Caprathe , John Lodge Gilmore , Sheryl Jeanne Hays , Juan Carlos Jaen , Jan Ruth Penvose-Yi
IPC分类号： C07D265/24 , C07D279/08 , A61K31/54 , A61K31/535 , C07C279/08 , C07D265/12 , C07D279/16
CPC分类号： C07D265/24 , C07D279/08
摘要： This invention concerns certain 2-substituted-3,1-benzoxazin-4-ones and benzthiazinones as complement Clr protease inhibitors and antiinflammatory agents, pharmaceutical compositions containing them, methods of using them, and processes for their preparation.
摘要翻译： 本发明涉及某些2-取代-3,1-苯并恶嗪-4-酮和苯并噻嗪酮作为补体Clr蛋白酶抑制剂和抗炎剂，含有它们的药物组合物，使用它们的方法及其制备方法。
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公开(公告)号：US20100286164A1
公开(公告)日：2010-11-11
申请号：US12682660
申请日：2008-10-10
IPC分类号： A61K31/496 , C12N9/99 , A61K31/395 , A61K31/495 , A61K31/438 , A61K31/44 , A61K31/357 , A61K31/135 , C07D225/02 , C07D401/12 , C07D241/04 , C07D491/113 , C07D213/36 , C07D319/16 , C07C215/20 , A61P25/28
CPC分类号： C07C215/08 , C07C217/58 , C07C217/72 , C07C217/84 , C07C217/90 , C07C229/38 , C07C233/73 , C07C255/58 , C07C255/59 , C07C2601/02 , C07C2601/14 , C07D213/38 , C07D213/79 , C07D215/14 , C07D295/088 , C07D295/092 , C07D295/096 , C07D307/81 , C07D309/12 , C07D317/58 , C07D319/18 , C07D333/28 , C07D491/08
摘要： Aspects of the invention relate to substituted aryl propylamino-oxy-analogs and uses thereof. Aspects of the invention relate to compositions that are inhibitors of γ-secretase and uses thereof for treating subjects having, or at risk of developing, Alzheimer's disease.
摘要翻译： 本发明的方面涉及取代的芳基丙氨基 - 氧基 - 类似物及其用途。 本发明的方面涉及作为γ-分泌酶抑制剂的组合物及其用于治疗患有或有发展为阿尔茨海默氏病风险的受试者的用途。
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4.发明授权Method of inhibiting amyloid protein aggregation and imaging amyloid deposits 失效抑制淀粉样蛋白聚集和成像淀粉样沉积物的方法公开(公告)号：US06972287B1
公开(公告)日：2005-12-06
申请号：US10009611
申请日：2000-05-31
申请人： Corinne Elizabeth Augelli-Szafran , Mark Robert Barvian , Christopher Franklin Bigge , Shelly Ann Glase , Shunichiro Hachiya , John Steven Kiely , Takenori Kimura , Yingjie Lai , Annette Theresa Sakkab , Mark James Suto , Larry Craswell Walker , Tomoyuki Yasunaga , Nian Zhuang
发明人： Corinne Elizabeth Augelli-Szafran , Mark Robert Barvian , Christopher Franklin Bigge , Shelly Ann Glase , Shunichiro Hachiya , John Steven Kiely , Takenori Kimura , Yingjie Lai , Annette Theresa Sakkab , Mark James Suto , Larry Craswell Walker , Tomoyuki Yasunaga , Nian Zhuang
IPC分类号： A61K31/196 , A61K31/402 , A61K31/4164 , C07C229/58 , C07C229/62 , C07C229/64 , C07C233/43 , C07C311/51 , C07D209/44 , C07D213/82 , C07D217/02 , C07D233/88 , C07D257/04 , C07D295/135 , C07D317/58 , C07D413/06 , C07D401/10 , A61K31/41 , A61P25/28 , C07D403/10 , C07D413/10
CPC分类号： C07D213/82 , A61K31/196 , A61K31/402 , A61K31/4164 , C07C229/58 , C07C229/62 , C07C229/64 , C07C233/43 , C07C311/51 , C07D209/44 , C07D217/02 , C07D233/88 , C07D257/04 , C07D295/135 , C07D317/58 , C07D413/06
摘要： The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).
摘要翻译： 本发明提供使用式（I）的化合物治疗阿尔茨海默病的方法。 还提供了使用式（I）化合物和淀粉样沉积物成像方法以及式（I）的新化合物抑制淀粉样蛋白聚集的方法。
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公开(公告)号：US06812228B2
公开(公告)日：2004-11-02
申请号：US10275825
申请日：2002-11-08
IPC分类号： A61K315365
CPC分类号： C07D498/14
摘要： Benzoxazines of Formula (I) wherein R1 is C1-C6 alkyl, C2-C6 alkenyl, or (CH2)n phenyl, R2 is C3-C6 alkyl, R3 is hydrogen, halo, hydroxy, alkoxy, or alkylthio, R4 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof, are useful for treating movement disorders such as Parkinson's disease.
摘要翻译： 式（I）的苯并恶嗪其中R 1为C 1 -C 6烷基，C 2 -C 6烯基或（CH 2）n苯基，R 2为C 3 -C 6烷基，R 3为氢，卤素，羟基， 烷氧基或烷硫基，R 4是氢或烷基或其药学上可接受的盐，可用于治疗运动障碍如帕金森病。
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