公开(公告)号：US08217036B2

公开(公告)日：2012-07-10

申请号：US13218571

申请日：2011-08-26

申请人： Aranapakam Mudumbai Venkatesan ,  Zecheng Chen ,  Christoph Martin Dehnhardt ,  Osvaldo Dos Santos ,  Efren Guillermo Delos Santos ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Joshua Aaron Kaplan ,  David James Richard ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Ariamala Gopalsamy ,  Kevin Joseph Curran ,  Mengxiao Shi

发明人： Aranapakam Mudumbai Venkatesan ,  Zecheng Chen ,  Christoph Martin Dehnhardt ,  Osvaldo Dos Santos ,  Efren Guillermo Delos Santos ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Joshua Aaron Kaplan ,  David James Richard ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Ariamala Gopalsamy ,  Kevin Joseph Curran ,  Mengxiao Shi

IPC分类号： A61K31/535 ,  C07D413/14

CPC分类号： C07D401/12 ,  A61K31/5377 ,  A61K45/06 ,  C07D251/18 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/14 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  C07D451/06 ,  C07D453/02 ,  C07D491/113 ,  C07D498/08

摘要： Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

摘要翻译： 式I的化合物，其中：R1是和R2，R4和R6-9在本文中定义，及其药学上可接受的盐和酯。 这些化合物抑制PI3激酶和mTOR，并可用于治疗PI3激酶和mTOR介导的疾病，如多种癌症。 公开了制备和使用本发明化合物的方法。 还公开了含有本发明化合物的各种组合物。

公开(公告)号：US20090304692A1

公开(公告)日：2009-12-10

申请号：US12470525

申请日：2009-05-22

申请人： Aranapakam Mudumbai Venkatesan ,  Zecheng Chen ,  Christoph Martin Dehnhardt ,  Osvaldo dos Santos ,  Efren Guillermo Delos Santos ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Joshua Aaron Kaplan ,  David James Richard ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Ariamala Gopalsamy ,  Kevin Joseph Curran ,  Mengxiao Shi

发明人： Aranapakam Mudumbai Venkatesan ,  Zecheng Chen ,  Christoph Martin Dehnhardt ,  Osvaldo dos Santos ,  Efren Guillermo Delos Santos ,  Arie Zask ,  Jeroen Cunera Verheijen ,  Joshua Aaron Kaplan ,  David James Richard ,  Semiramis Ayral-Kaloustian ,  Tarek Suhayl Mansour ,  Ariamala Gopalsamy ,  Kevin Joseph Curran ,  Mengxiao Shi

IPC分类号： A61K31/5375 ,  C07D413/04 ,  C07D413/14 ,  C07D405/14 ,  C07D417/14 ,  C07D491/08 ,  C07D498/08 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/7068 ,  A61K31/675 ,  A61K33/24 ,  A61K39/395 ,  A61P19/00 ,  A61P35/00

摘要： Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

公开(公告)号：US20070276030A1

公开(公告)日：2007-11-29

申请号：US10567649

申请日：2004-08-13

申请人： Ariamala Gopalsamy

发明人： Ariamala Gopalsamy

IPC分类号： A61K31/381 ,  C07D495/02

CPC分类号： C07D495/04 ,  A61K31/381

摘要： The invention is directed to a compound of the formula: wherein substitutions fat R1, R2, R3-R12, and Y are set forth in the specification; pharmaceutical compositions comprising said compound, methods of treating or preventing a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of said compound or pharmaceutical compositions including said compound and methods of inhibiting replication of a Hepatitis C virus comprising contacting the HCV virus with an effective amount of said compound or pharmaceutical compositions including said compound.

摘要翻译： 本发明涉及下式化合物：其中取代脂肪R 1，R 2，R 3，R 12， / SUP>和Y在说明书中列出; 包含所述化合物的药物组合物，治疗或预防哺乳动物中丙型肝炎病毒感染的方法，包括使哺乳动物与有效量的所述化合物或包含所述化合物的药物组合物和抑制丙型肝炎病毒复制的方法接触，包括接触HCV 病毒与有效量的所述化合物或包含所述化合物的药物组合物。

公开(公告)号：US07300946B2

公开(公告)日：2007-11-27

申请号：US10538998

申请日：2003-12-08

申请人： Ping Ding ,  Robert N. Henrie, II ,  Daniel H. Cohen ,  John W. Lyga ,  David S. Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter H. Yeager ,  Stephen F. Donovan ,  Steven Shunxiang Zhang ,  Inna Shulman ,  Seong Jae Yu ,  Guozhi Wang ,  Y. Larry Zhang ,  Ariamala Gopalsamy ,  Dennis L. Warkentin ,  Paul E. Rensner ,  Ian R. Silverman ,  Thomas G. Cullen

发明人： Ping Ding ,  Robert N. Henrie, II ,  Daniel H. Cohen ,  John W. Lyga ,  David S. Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter H. Yeager ,  Stephen F. Donovan ,  Steven Shunxiang Zhang ,  Inna Shulman ,  Seong Jae Yu ,  Guozhi Wang ,  Y. Larry Zhang ,  Ariamala Gopalsamy ,  Dennis L. Warkentin ,  Paul E. Rensner ,  Ian R. Silverman ,  Thomas G. Cullen

IPC分类号： A61K31/44 ,  A61K31/445 ,  A61K31/4422 ,  C07D211/06 ,  C07D211/08 ,  C07D211/70 ,  C07D211/82

CPC分类号： C07D405/14 ,  A01N43/40 ,  A01N43/54 ,  A01N43/713 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/94 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D451/14 ,  C07D513/04

摘要： It has now been found that certain novel N-(substituted aryl)-4(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present

摘要翻译： 现在已经发现，某些新的N-（取代的芳基）-4（二取代的甲基）哌啶和吡啶衍生物已经提供了意想不到的杀虫活性。 这些化合物由式（I）表示：其中m，n，q，r和s独立地选自0或1; 且p为0,1,2或3; A是C或CH; 和B，D，E，R，R 1，R 2，R 3，R 4，R 本文中充分描述了本发明的第5，第6，第七和第八和第八。 此外，还公开了包含杀虫有效量的至少一种式I化合物和任选的有效量的至少一种第二化合物与至少一种与杀虫相容的载体的组合物; 以及控制昆虫的方法，包括将所述组合物施用于存在昆虫或预期存在的场所

公开(公告)号：US20060276464A1

公开(公告)日：2006-12-07

申请号：US11432788

申请日：2006-05-10

申请人： Ariamala Gopalsamy ,  William Moore ,  Jeffery Kern ,  Albert Molinari ,  Mengxiao Shi ,  Gregory Welmaker ,  Mathew Wilson ,  Girija Krishnamurthy ,  Thomas Commons ,  Michael Webb ,  Richard Woodworth

发明人： Ariamala Gopalsamy ,  William Moore ,  Jeffery Kern ,  Albert Molinari ,  Mengxiao Shi ,  Gregory Welmaker ,  Mathew Wilson ,  Girija Krishnamurthy ,  Thomas Commons ,  Michael Webb ,  Richard Woodworth

IPC分类号： A61K31/537 ,  A61K31/538 ,  A61K31/495 ,  A61K31/445 ,  A61K31/4172 ,  A61K31/40 ,  A61K31/18

CPC分类号： C07F9/3882 ,  C07C317/14 ,  C07C317/22 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D213/42 ,  C07D233/54 ,  C07D401/04 ,  C07F9/4056

摘要： Compounds of Formula 1, or pharmaceutically acceptable salts thereof, are provided: which are modulators of secreted frizzled related protein-1. The compounds, and compositions containing the compounds, can be used to treat a variety of disorders, including osteoporosis.

摘要翻译： 提供式1化合物或其药学上可接受的盐：其是分泌的卷曲相关蛋白-1的调节剂。 化合物和含有这些化合物的组合物可用于治疗多种疾病，包括骨质疏松症。

公开(公告)号：US20060264460A1

公开(公告)日：2006-11-23

申请号：US11436485

申请日：2006-05-18

申请人： Neal Green ,  Yonghan Hu ,  Neelu Kaila ,  Kristin Janz ,  Jennifer Thomason ,  Huan-Qiu Li ,  Rajeev Hotchandani ,  Junjun Wu ,  Ariamala Gopalsamy ,  Steve Tam ,  Lih-Ling Lin ,  John Cuozzo ,  Satenig Guler ,  Adrian Huang ,  Jeffrey condon

发明人： Neal Green ,  Yonghan Hu ,  Neelu Kaila ,  Kristin Janz ,  Jennifer Thomason ,  Huan-Qiu Li ,  Rajeev Hotchandani ,  Junjun Wu ,  Ariamala Gopalsamy ,  Steve Tam ,  Lih-Ling Lin ,  John Cuozzo ,  Satenig Guler ,  Adrian Huang ,  Jeffrey condon

IPC分类号： A61K31/4709 ,  A61K31/4706 ,  C07D401/02 ,  C07D215/38

CPC分类号： C07D215/42 ,  C07D215/44

摘要： The present invention provides compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, m and n are defined as described herein. The invention also provides methods of making the compounds of formula (I), and methods of treating inflammatory diseases, such as rheumatoid arthritis, in a mammal comprising administering a therapeutically effective amount of a compound of formula (I) to the mammal.

摘要翻译： 本发明提供式（I）化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7，R 8，M和 n定义如本文所述。 本发明还提供了在哺乳动物中制备式（I）化合物的方法和治疗炎性疾病如类风湿性关节炎的方法，包括向哺乳动物施用治疗有效量的式（I）化合物。

公开(公告)号：US07683070B2

公开(公告)日：2010-03-23

申请号：US11874015

申请日：2007-10-17

申请人： Ping Ding ,  Robert N. Henrie, II ,  Daniel H. Cohen ,  John W. Lyga ,  David S. Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter H. Yeager ,  Stephen F. Donovan ,  Stephen Shunxiang Zhang ,  Inna Shulman ,  Seong Jae Yu ,  Guozhi Wang ,  Y. Larry Zhang ,  Ariamala Gopalsamy ,  Dennis L. Warkentin ,  Paul E. Rensner ,  Ian R. Silverman ,  Thomas G. Cullen

发明人： Ping Ding ,  Robert N. Henrie, II ,  Daniel H. Cohen ,  John W. Lyga ,  David S. Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter H. Yeager ,  Stephen F. Donovan ,  Stephen Shunxiang Zhang ,  Inna Shulman ,  Seong Jae Yu ,  Guozhi Wang ,  Y. Larry Zhang ,  Ariamala Gopalsamy ,  Dennis L. Warkentin ,  Paul E. Rensner ,  Ian R. Silverman ,  Thomas G. Cullen

IPC分类号： A61K31/4523 ,  A61K31/4545 ,  C07D211/06 ,  C07D239/02

CPC分类号： C07D405/14 ,  A01N43/40 ,  A01N43/54 ,  A01N43/713 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/94 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D451/14 ,  C07D513/04

摘要： It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

摘要翻译： 现在已经发现某些新的N-（取代的芳基）-4-（二取代的甲基）哌啶和吡啶衍生物提供了意想不到的杀虫活性。 这些化合物由式（I）表示：其中m，n，q，r和s独立地选自0或1; 且p为0,1,2或3; A是C或CH; 本文完整地描述了B，D，E，R，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8。 此外，还公开了包含杀虫有效量的至少一种式I化合物和任选的有效量的至少一种第二化合物与至少一种与杀虫相容的载体的组合物; 以及控制昆虫的方法，包括将所述组合物施用于存在昆虫或预期存在的场所。

公开(公告)号：US20080312308A1

公开(公告)日：2008-12-18

申请号：US12168499

申请日：2008-07-07

申请人： Ariamala Gopalsamy ,  Scott Lee Kincaid

发明人： Ariamala Gopalsamy ,  Scott Lee Kincaid

IPC分类号： A61K31/403 ,  C07D209/04 ,  A61K31/195 ,  C07C59/74

CPC分类号： C07D209/24 ,  C07C251/60 ,  C07D209/14

摘要： The present invention relates generally to substituted acetic acid derivatives and methods of using them.

摘要翻译： 本发明一般涉及取代的乙酸衍生物及其使用方法。

公开(公告)号：US07388016B2

公开(公告)日：2008-06-17

申请号：US11634601

申请日：2006-12-06

申请人： Ariamala Gopalsamy ,  Mengxiao Shi ,  Kristina Kutterer ,  Kim Timothy Arndt

发明人： Ariamala Gopalsamy ,  Mengxiao Shi ,  Kristina Kutterer ,  Kim Timothy Arndt

IPC分类号： A61K31/4745 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The present invention relates to Dibenzonaphthyridine Derivatives, compositions comprising an effective amount of a Dibenzonaphthyridine Derivative and methods for treating or preventing a proliferative disorder, comprising administering to a subject in need thereof an effective amount of a Dibenzonaphthyridine Derivative.

摘要翻译： 本发明涉及二苯并萘啶衍生物，包含有效量的二苯并萘啶衍生物和治疗或预防增殖性疾病的方法的组合物，包括向有需要的受试者施用有效量的二苯并萘啶衍生物。

公开(公告)号：US20080090828A1

公开(公告)日：2008-04-17

申请号：US11874015

申请日：2007-10-17

申请人： Ping Ding ,  Robert Henrie ,  Daniel Cohen ,  John Lyga ,  David Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter Yeager ,  Stephen Donovan ,  Stephen Zhang ,  Inna Shulman ,  Seong Yu ,  Guozhi Wang ,  Y. Zhang ,  Ariamala Gopalsamy ,  Dennis Warkentin ,  Paul Rensner ,  Ian Silverman ,  Thomas Cullen

发明人： Ping Ding ,  Robert Henrie ,  Daniel Cohen ,  John Lyga ,  David Rosen ,  George Theodoridis ,  Qun Zhang ,  Walter Yeager ,  Stephen Donovan ,  Stephen Zhang ,  Inna Shulman ,  Seong Yu ,  Guozhi Wang ,  Y. Zhang ,  Ariamala Gopalsamy ,  Dennis Warkentin ,  Paul Rensner ,  Ian Silverman ,  Thomas Cullen

IPC分类号： C07D453/02 ,  A61K31/4745 ,  A61K31/50

CPC分类号： C07D405/14 ,  A01N43/40 ,  A01N43/54 ,  A01N43/713 ,  C07D211/14 ,  C07D211/18 ,  C07D211/22 ,  C07D211/24 ,  C07D211/26 ,  C07D211/28 ,  C07D211/32 ,  C07D211/94 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D417/12 ,  C07D451/14 ,  C07D513/04

摘要： It has now been found that certain novel N-(substituted aryl)-4-(disubstituted methyl)piperidine and pyridine derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): wherein m, n, q, r, and s are independently selected from 0 or 1; and p is 0, 1, 2, or 3; A is C or CH; and B, D, E, R, R1, R2, R3, R4, R5, R6, R7 and R8 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.

摘要翻译： 现在已经发现某些新的N-（取代的芳基）-4-（二取代的甲基）哌啶和吡啶衍生物提供了意想不到的杀虫活性。 这些化合物由式（I）表示：其中m，n，q，r和s独立地选自0或1; 且p为0,1,2或3; A是C或CH; 和B，D，E，R，R 1，R 2，R 3，R 4，R 本文中充分描述了本发明的第5，第6，第七和第八和第八。 此外，还公开了包含杀虫有效量的至少一种式I化合物和任选的有效量的至少一种第二化合物与至少一种与杀虫相容的载体的组合物; 以及控制昆虫的方法，包括将所述组合物施用于存在昆虫或预期存在的场所。