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公开(公告)号:US20070173521A1
公开(公告)日:2007-07-26
申请号:US11599901
申请日:2006-11-14
申请人: Qiufen Xue , Brian Albrecht , Denise Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Bryant Yang , Wenge Zhong
发明人: Qiufen Xue , Brian Albrecht , Denise Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Bryant Yang , Wenge Zhong
IPC分类号: A61K31/513 , A61K31/506
CPC分类号: C07D405/12 , C07D413/12
摘要: 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 R1, W, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 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R 1,W,B,R 3,R 4,R 4, 5,i和j在本文中定义。 本发明还包括药物组合物,其包括一种或多种式I化合物,这些化合物的使用方法,包括治疗AD和相关疾病,通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案,可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US20070185144A1
公开(公告)日:2007-08-09
申请号:US11595187
申请日:2006-11-10
申请人: Wenge Zhong , Stephen Hitchcock , Brian Albrecht , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang
发明人: Wenge Zhong , Stephen Hitchcock , Brian Albrecht , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Dean Hickman , Daniel Horne , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Qiufen Xue , Bryant Yang
IPC分类号: A61K31/4747 , A61K31/4743 , A61K31/4741 , A61K31/4025 , A61K31/353 , A61K31/277 , A61K31/165 , C07D491/02
CPC分类号: C07D405/12 , C07D311/68 , C07D413/12 , C07D491/052
摘要: 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 A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 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A,B,W,R 3,R 4,R 5,i和 j在本文中定义。 本发明还包括药物组合物,其包括一种或多种式I化合物,这些化合物的使用方法,包括治疗AD和相关疾病,通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案,可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US20070185103A1
公开(公告)日:2007-08-09
申请号:US11600264
申请日:2006-11-14
申请人: Brian Albrecht , Denise Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Quifen Xue , Bryant Yang , Wenge Zhong
发明人: Brian Albrecht , Denise Andersen , Michael Bartberger , James Brown , Ryan Brown , Stuart Chaffee , Yuan Cheng , Michael Croghan , Russell Graceffa , Scott Harried , Stephen Hitchcock , Randall Hungate , Ted Judd , Matthew Kaller , Charles Kreiman , Daniel La , Patricia Lopez , Craig Masse , Holger Monenschein , Thomas Nguyen , Thomas Nixey , Vinod Patel , Lewis Pennington , Matthew Weiss , Quifen Xue , Bryant Yang , Wenge Zhong
IPC分类号: A61K31/538 , A61K31/503 , A61K31/4704 , A61K31/4745 , A61K31/4188 , A61K31/4162 , C07D487/02 , C07D471/02
CPC分类号: C07D405/12 , C07D413/12
摘要: 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 A, B, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 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A,B,R 3,R 4,R 5,i和j分别为 本文定义。 本发明还包括药物组合物,其包括一种或多种式I化合物,这些化合物的使用方法,包括治疗AD和相关疾病,通过给受试者施用式I化合物或包含它们的组合物。 本发明还包括式II和III的其它实施方案,可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US20070054916A1
公开(公告)日:2007-03-08
申请号:US11240590
申请日:2005-09-30
申请人: Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
发明人: Vinod Patel , Joseph Kim , Stephanie Geuns-Meyer , Stuart Chaffee , Victor Cee , Brian Hodous , Steven Bellon , Jean-Christophe Harmange , Philip Olivieri , Maya Thaman , Erin DiMauro , John Buchanan , David McGowan , Brian Albrecht , Holly Deak , Jean Bemis , Ryan White , Matthew Martin , Gregory Habgood , Paul Tempest , Craig Masse , William Buckner , Bradley Herberich , Russell Graceffa , Dawei Zhang , Shimin Xu , Kelvin Sham , Robert Rzasa , James Falsey , Partha Chakrabarti , Guo-Qiang Cao , Susan Tomlinson , Liping Pettus , Adrian Smith , Nick Paras , Gang Liu , Frenel DeMorin , Andrew Tasker , Anthony Reed
IPC分类号: A61K31/525 , A61K31/519 , A61K31/517
CPC分类号: C07D215/38 , C07C205/37 , C07D215/12 , C07D217/12 , C07D217/22 , C07D217/26 , C07D239/26 , C07D239/84 , C07D239/94 , C07D239/95 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译: 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病,包括炎症,癌症和相关病症的化合物。 化合物具有通式I,其中A 1,A 2,A 3,B,R 1, R 2,R 3和R 4在本文中定义。 因此,本发明还包括含有本发明化合物的药物组合物,使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法,以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号:US20060009453A1
公开(公告)日:2006-01-12
申请号:US11126000
申请日:2005-05-09
申请人: Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
发明人: Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
IPC分类号: A61K31/53 , A61K31/506 , C07D43/14
CPC分类号: C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
摘要翻译: 本发明涉及具有通式I的化合物,其中A,B,D,E,G,H 1-5和R 1-4如本文所定义, 和合成中间体,其能够调节各种蛋白激酶受体酶,从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如,这些化合物能够调节激酶,从而影响血管生成过程并治疗血管生成相关疾病和其它包括癌症和炎症的复发性疾病。 本发明还包括药物组合物,包括该化合物,以及治疗与蛋白激酶活性有关的疾病状态的方法。
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公开(公告)号:US20070185171A1
公开(公告)日:2007-08-09
申请号:US11584151
申请日:2006-10-20
申请人: Julie Germain , Benny Askew , David Bauer , Deborah Choquette , Lucian Dipietro , Russell Graceffa , Jean-Christophe Harmange , Qi Huang , Joseph Kim , Daniel La , Aiwen Li , Nobuko Nishimura , Rana Nomak , Vinod Patel , Michele Potashman , Babak Riahi , Thomas Storz , Simon Van Der Plas , Kevin Yang , Chester Yuan
发明人: Julie Germain , Benny Askew , David Bauer , Deborah Choquette , Lucian Dipietro , Russell Graceffa , Jean-Christophe Harmange , Qi Huang , Joseph Kim , Daniel La , Aiwen Li , Nobuko Nishimura , Rana Nomak , Vinod Patel , Michele Potashman , Babak Riahi , Thomas Storz , Simon Van Der Plas , Kevin Yang , Chester Yuan
IPC分类号: C07D209/04 , C07D213/16
CPC分类号: C07D471/04 , C07D487/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新颖的化合物,类似物,前药和药学上可接受的盐,用于预防和治疗疾病和其它疾病或涉及癌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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公开(公告)号:US20070049592A1
公开(公告)日:2007-03-01
申请号:US11506693
申请日:2006-08-18
申请人: Stephanie Geuns-Meyer , Stuart Chaffee , Rebecca Johnson , Joseph Kim , Joseph Nunes , Vinod Patel
发明人: Stephanie Geuns-Meyer , Stuart Chaffee , Rebecca Johnson , Joseph Kim , Joseph Nunes , Vinod Patel
IPC分类号: A61K31/5377 , A61K31/53 , A61K31/506 , A61K31/4709 , C07D413/02 , C07D403/02 , C07D401/02
CPC分类号: C07D213/81 , C07D213/75 , C07D239/42 , C07D239/48 , C07D239/74 , C07D239/94 , C07D251/18 , C07D251/48 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要: The present invention relates to compounds of Formulas I and II, wherein A1, A2, B1, B2, Q, X1, X2, Y and R3 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.
摘要翻译: 本发明涉及式I和II的化合物,其中A 1,A 2,B 1,B 2, 本文定义了本文所定义的含有这些化合物的合成中间体和药物组合物,其中,Q,X 1,X 2,Y和R 3, 。 化合物和组合物能够调节各种蛋白激酶受体如Tie-2,因此影响激酶相关的疾病状态和状况。 该化合物例如能够治疗由不受调节的血管发生,炎症以及其它增殖性疾病引起的癌症。
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公开(公告)号:US20060040956A1
公开(公告)日:2006-02-23
申请号:US11234713
申请日:2005-09-23
申请人: Guoqing Chen , Jeffrey Adams , Jean Bemis , Shon Booker , Guolin Cai , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Stephanie Geuns-Meyer , Michael Handley , Qi Huang , Joseph Kim , Tae-Seong Kim , Alexander Kiselyov , Xiaohu Ouyang , Vinod Patel , Leon Smith , Markian Stec , Andrew Tasker , Ning Xi , Shimin Xu , Chester Yuan , Michael Croghan
发明人: Guoqing Chen , Jeffrey Adams , Jean Bemis , Shon Booker , Guolin Cai , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Stephanie Geuns-Meyer , Michael Handley , Qi Huang , Joseph Kim , Tae-Seong Kim , Alexander Kiselyov , Xiaohu Ouyang , Vinod Patel , Leon Smith , Markian Stec , Andrew Tasker , Ning Xi , Shimin Xu , Chester Yuan , Michael Croghan
IPC分类号: A61K31/506 , C07D403/02
CPC分类号: C07D213/82 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5377 , A61K31/538 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/00 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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公开(公告)号:US20050153960A1
公开(公告)日:2005-07-14
申请号:US10996035
申请日:2004-11-22
申请人: Daniel Elbaum , Benny Askew , Shon Booker , Julie Germain , Gregory Habgood , Michael Handley , Tae-Seong Kim , Aiwen Li , Nobuko Nishimura , Vinod Patel , Chester Yuan , Joseph Kim , Guolin Cai , Guoqing Chen , Michael Croghan , Lucian Di Pietro , Celia Dominguez , Qi Huang , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu
发明人: Daniel Elbaum , Benny Askew , Shon Booker , Julie Germain , Gregory Habgood , Michael Handley , Tae-Seong Kim , Aiwen Li , Nobuko Nishimura , Vinod Patel , Chester Yuan , Joseph Kim , Guolin Cai , Guoqing Chen , Michael Croghan , Lucian Di Pietro , Celia Dominguez , Qi Huang , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/538 , A61P1/04 , A61P3/00 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/00 , A61P11/06 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P21/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P29/00 , A61P31/12 , A61P31/18 , A61P31/22 , A61P35/00 , A61P35/02 , A61P35/04 , A61P37/02 , A61P37/04 , A61P37/08 , A61P43/00 , C07D213/81 , C07D213/82 , C07D237/04 , C07D237/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , A61K31/4545 , C07D413/02 , C07D41/02
CPC分类号: C07D213/81 , C04B35/632 , C07D213/82 , C07D237/04 , C07D237/24 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis 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, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
摘要翻译: 所选化合物对于预防和治疗诸如血管生成介导的疾病等疾病是有效的。 本发明包括新型化合物,类似物,前药及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癌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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公开(公告)号:US20060194848A1
公开(公告)日:2006-08-31
申请号:US11417329
申请日:2006-05-02
申请人: Guoqing Chen , Jeffrey Adams , Jean Bemis , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Qi Huang , Joseph Kim , Xiaohu Ouyang , Vinod Patel , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu , Chester Yuan , Michael Croghan , Tae-Seong Kim
发明人: Guoqing Chen , Jeffrey Adams , Jean Bemis , Lucian Di Pietro , Celia Dominguez , Daniel Elbaum , Julie Germain , Qi Huang , Joseph Kim , Xiaohu Ouyang , Vinod Patel , Leon Smith , Andrew Tasker , Ning Xi , Shimin Xu , Chester Yuan , Michael Croghan , Tae-Seong Kim
CPC分类号: C07D401/14 , A61K31/00 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , Y02A50/401
摘要: Selected amines are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
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