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1.发明授权Spiro-tricyclic ring compounds as beta-secretase modulators and methods of use 有权螺三环环化合物作为β-分泌酶调节剂和使用方法公开(公告)号：US08426447B2
公开(公告)日：2013-04-23
申请号：US12558426
申请日：2009-09-11
Applicant: Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
Inventor： Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
IPC: A61K31/44 , C07D311/82 , C07D401/00 , C07D413/00
CPC classification number: C07D498/10 , C07D513/10
Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中式I的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z如本文所定义。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。
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公开(公告)号：US07449581B2
公开(公告)日：2008-11-11
申请号：US11651302
申请日：2007-01-09
Applicant: Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl
IPC: C07D471/04
CPC classification number: C07D471/04 , C07D519/00
Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
Abstract translation: 本发明提供式I和II的化合物：其中R 1，R 3，W，Z，X 1，X SUP > 2，其中R 1，R 8和R 9如本文所定义，并且其制备和用途的方法和中间体 其中。
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公开(公告)号：US07449472B2
公开(公告)日：2008-11-11
申请号：US11202611
申请日：2005-08-12
Applicant: Jian Jeffrey Chen , Nolan James Dewdney , Christoph Martin Stahl
Inventor： Jian Jeffrey Chen , Nolan James Dewdney , Christoph Martin Stahl
IPC: A61K31/519 , A61P37/04 , C07D487/04 , C07D491/048 , C07D495/04 , C07D471/04 , C07D491/04 , A61K31/4355 , A61K31/4365 , A61K31/437
CPC classification number: C07D487/04 , C07D491/04 , C07D495/04
Abstract: The present invention discloses compounds corresponding to the formula wherein A, X, Y, R, R1 and R2 are as defined within, pharmaceutical formulations, methods of making and uses thereof.
Abstract translation: 本发明公开了对应于下式的化合物：其中A，X，Y，R，R 1和R 2定义如下，药物制剂，制备和用途的方法 其中。
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公开(公告)号：US07439247B2
公开(公告)日：2008-10-21
申请号：US11292217
申请日：2005-11-30
Applicant: Jian Jeffrey Chen , Nolan James Dewdney , Christoph Martin Stahl
Inventor： Jian Jeffrey Chen , Nolan James Dewdney , Christoph Martin Stahl
IPC: C07D471/04 , C07D491/048 , C07D495/04 , C07D487/04 , A61K31/519 , A61K31/4355 , A61K31/437
CPC classification number: C07D487/04 , C07D491/04 , C07D495/04
Abstract: The present invention discloses compounds corresponding to formula wherein A, R, X, Y, R, R1 and R2 are as defined above, pharmaceutical formulations, methods of making and uses thereof.
Abstract translation: 本发明公开了相应于下式的化合物：其中A，R，X，Y，R，R 1和R 2如上所定义，药物制剂，制备方法和 其用途。
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公开(公告)号：US07425631B2
公开(公告)日：2008-09-16
申请号：US10823377
申请日：2004-04-12
Applicant: Robert D. Groneberg , Benny C. Askew, Jr. , Derin C. D'Amico , James Zhan , Andras Toro , Youngboo Kim , David A. Mareska , Nianhe Han , Christopher H. Fotsch , Qingyian Liu , Babak Riahi , Kevin Yang , Aiwen Li , Chester Chenguang Yuan , Kaustav Biswas , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jian Jeffrey Chen , Rana Nomak
Inventor： Robert D. Groneberg , Benny C. Askew, Jr. , Derin C. D'Amico , James Zhan , Andras Toro , Youngboo Kim , David A. Mareska , Nianhe Han , Christopher H. Fotsch , Qingyian Liu , Babak Riahi , Kevin Yang , Aiwen Li , Chester Chenguang Yuan , Kaustav Biswas , Scott Harried , Thomas Nguyen , Wenyuan Qian , Jian Jeffrey Chen , Rana Nomak
IPC: C07D215/04
CPC classification number: C07C311/19 , C07C311/13 , C07C311/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D207/12 , C07D207/16 , C07D207/20 , C07D209/14 , C07D209/16 , C07D209/40 , C07D209/52 , C07D211/38 , C07D211/44 , C07D211/46 , C07D211/60 , C07D211/70 , C07D213/42 , C07D213/56 , C07D213/64 , C07D215/38 , C07D215/40 , C07D215/42 , C07D217/22 , C07D233/54 , C07D239/74 , C07D271/08 , C07D277/64 , C07D279/02 , C07D285/14 , C07D295/125 , C07D295/13 , C07D295/135 , C07D307/14 , C07D307/28 , C07D307/79 , C07D307/81 , C07D311/68 , C07D317/58 , C07D333/20 , C07D333/24 , C07D333/58 , C07D333/62 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/06 , C07D407/12 , C07D409/06 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/08
Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Abstract translation: 所选化合物对于治疗疼痛和疾病如炎症介导的疾病是有效的。 本发明包括新的化合物，类似物，前药和其药学上可接受的衍生物，用于预防和治疗疾病和其它疾病或涉及疼痛，炎症等的病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。
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Patent Agency Ranking
公开(公告)号：US06696566B2
公开(公告)日：2004-02-24
申请号：US10073845
申请日：2002-02-11
Applicant: Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Christoph Martin Stahl
IPC: C07D47500
CPC classification number: C07D471/04 , C07D519/00
Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.
Abstract translation: 本发明提供式I和II的化合物：其中R 1，R 3，W，Z，X 1，X 2，Ar 1，R 8和R 9 >如本文所定义，以及其制备方法和中间体及其用途。
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公开(公告)号：US06518276B2
公开(公告)日：2003-02-11
申请号：US09943338
申请日：2001-08-30
Applicant: Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
Inventor： Humberto Bartolome Arzeno , Jian Jeffrey Chen , James Patrick Dunn , David Michael Goldstein , Julie Anne Lim
IPC: A61K31519
CPC classification number: C07D471/04 , C07D239/47
Abstract: The present invention provides compounds of the formula: wherein R1, R3, and Ar1 are those defined herein, and R2 is —CR′R″—Ra (where R′ and R″ are hydrogen, hydroxyalkyl or alkyl with at least one being alkyl or hydroxyalkyl and Ra is hydroxyalkyl), Rx—S—Ry— (where Rx is alkyl and Ry is alkylene), alkoxy-substituted alkyl, heterocyclylalkyl or C4-C5 cycloalkyl, wherein each of the hydroxy group present in R2 can be independently Ra—C(═O)—O, RaRbN—C(═O)—O, or Ra—S(O)2—O—, wherein Ra and Rb are independently hydrogen, alkyl, aryl, or aralkyl, and methods for preparation and uses thereof.
Abstract translation: 本发明提供下式的化合物：其中R1，R3和Ar1是本文定义的，R2是-CR'R'-Ra（其中R'和R“是氢，羟基烷基或具有至少一个 （其中R x是烷基，R y是亚烷基），烷氧基取代的烷基，杂环基烷基或C 4 -C 5环烷基，其中R 2中存在的每个羟基可以是 独立地是R a -C（= O）-O，R a R b N-C（= O）-O或R a -S（O）2-O-，其中R a和R b独立地是氢，烷基，芳基或芳烷基， 用于其制备和使用。
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公开(公告)号：US6130220A
公开(公告)日：2000-10-10
申请号：US369677
申请日：1999-08-05
Applicant: Chris Allen Broka , Jeffrey Allen Campbell , Arlindo Lucas Castelhano , Jian Jeffrey Chen , Robert Than Hendricks , Michael Joseph Melnick , Keith Adrian Murray Walker
Inventor： Chris Allen Broka , Jeffrey Allen Campbell , Arlindo Lucas Castelhano , Jian Jeffrey Chen , Robert Than Hendricks , Michael Joseph Melnick , Keith Adrian Murray Walker
IPC: C07C307/06 , C07D211/36 , C07D213/74 , C07D295/26 , C07D401/04 , C07D401/12 , A61K31/495 , A01N43/42 , C07D279/10 , C07D471/00 , C07D471/02
CPC classification number: C07D295/26 , C07C307/06 , C07D211/36 , C07D213/74 , C07D401/04 , C07D401/12
Abstract: This invention relates to sulfamides of formula (I) ##STR1## that are inhibitors of metalloproteases, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.
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9.发明授权Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use 失效金属蛋白酶抑制剂，含有它们的药物组合物及其用途
公开(公告)号：US6008243A
公开(公告)日：1999-12-28
申请号：US823962
申请日：1997-03-25
Applicant: Steven L. Bender , Arlindo L. Castelhano , Wesley K. M. Chong , Melwyn A. Abreo , Jian Jeffrey Chen , Judith G. Deal
Inventor： Steven L. Bender , Arlindo L. Castelhano , Wesley K. M. Chong , Melwyn A. Abreo , Jian Jeffrey Chen , Judith G. Deal
IPC: C07D233/58 , A61K31/00 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/4025 , A61K31/407 , A61K31/415 , A61K31/4164 , A61K31/4178 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/55 , A61K38/00 , A61P1/00 , A61P1/02 , A61P9/00 , A61P9/10 , A61P19/00 , A61P19/02 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D207/32 , C07D207/327 , C07D207/337 , C07D231/12 , C07D233/54 , C07D233/56 , C07D307/54 , C07D333/24 , C07D333/26 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/12 , C07D487/04 , C07D487/08 , C07D498/08 , C07D521/00 , C07K5/072
CPC classification number: C07D207/327 , C07D207/337 , C07D231/12 , C07D233/56 , C07D249/08 , C07D307/54 , C07D333/24 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D487/08 , C07K5/06104 , C07K5/06113 , A61K38/00
Abstract: The present invention is directed to compound of the formula I: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, X, Y, and ##STR2## are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
Abstract translation: 本发明涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5，X，Y和如本文所定义。 这些化合物可用于通过使金属蛋白酶与有效量的本发明化合物接触来抑制金属蛋白酶的活性。
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10.发明申请SPIRO-TRICYCLIC RING COMPOUNDS AS BETA-SECRETASE MODULATORS AND METHODS OF USE 有权SPIRO-TRICYCLIC环化合物作为β-分泌酶调节剂和使用方法公开(公告)号：US20100087429A1
公开(公告)日：2010-04-08
申请号：US12558426
申请日：2009-09-11
Applicant: Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
Inventor： Ryan White , Albert Amegadzie , Marian C. Bryan , Jian Jeffrey Chen , Alan C. Cheng , Thomas Dineen , Oleg Epstein , Vijay Keshav Gore , Zihao Hua , Jason Brooks Human , Hongbing Huang , Charles Kreiman , Daniel La , Qingyian Liu , Vu Van Ma , Isaac Marx , Vinod F. Patel , Wenyuan Qian , Matthew Weiss , Chester Chenguang Yuan
IPC: A61K31/421 , C07D498/10 , C07D513/10 , C07D498/20 , A61K31/506 , A61K31/4439 , A61K31/5377 , A61P25/00 , A61P25/28
CPC classification number: C07D498/10 , C07D513/10
Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, T1, T2, W, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
Abstract translation: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病（包括阿尔茨海默病（AD））和相关病症的新一类化合物。 在一个实施方案中，化合物具有通式I，其中式I的A1，A2，A3，A4，A5，A6，T1，T2，W，X，Y和Z如本文所定义。 本发明还包括在药物组合物中用于治疗，预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这种病症包括例如阿尔茨海默氏病，认知缺陷，认知障碍，精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案，可用于制备式I化合物的中间体和方法。
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