公开(公告)号：US20060252812A1

公开(公告)日：2006-11-09

申请号：US11402310

申请日：2006-04-11

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/407 ,  C07D491/10

CPC分类号： C07D491/10

摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

摘要翻译： 本发明涉及式（I）的螺 - 羟吲哚化合物：其中k，j，Q，R 1，R 2a，R 2b， >，R 2c，R 2d，R 3a，R 3b，R 3c， >和R“>如本文所定义，作为其立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。 还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

公开(公告)号：US20100173967A1

公开(公告)日：2010-07-08

申请号：US12445264

申请日：2007-10-12

申请人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

发明人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

IPC分类号： A61K31/404 ,  A61P9/10 ,  A61P17/04 ,  A61P35/00

CPC分类号： A61K31/407 ,  A61K31/437

摘要： This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.

摘要翻译： 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。

公开(公告)号：US07700641B2

公开(公告)日：2010-04-20

申请号：US11402310

申请日：2006-04-11

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/407 ,  C07D491/107

CPC分类号： C07D491/10

摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

摘要翻译： 本发明涉及式（I）的螺 - 羟吲哚化合物：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义，作为立体异构体， 其互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。 还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

公开(公告)号：US20100125072A1

公开(公告)日：2010-05-20

申请号：US12650196

申请日：2009-12-30

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/5377 ,  C07D491/10 ,  A61K31/407 ,  A61K31/4439 ,  A61K31/506

CPC分类号： C07D491/10

摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

公开(公告)号：US08466188B2

公开(公告)日：2013-06-18

申请号：US12445264

申请日：2007-10-12

申请人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

发明人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

IPC分类号： A61K31/40 ,  A61K31/5377

CPC分类号： A61K31/407 ,  A61K31/437

摘要： This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.

摘要翻译： 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。

公开(公告)号：US20070105820A1

公开(公告)日：2007-05-10

申请号：US11408269

申请日：2006-04-20

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/404 ,  A61K31/675 ,  C07D403/02 ,  C07F9/572

CPC分类号： C07D409/06 ,  C07D209/34 ,  C07D209/38 ,  C07D209/40 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D403/10 ,  C07D405/04 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04

摘要： This invention is directed to oxindole compounds that are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of using the compounds are also disclosed.

摘要翻译： 本发明涉及可用于治疗和/或预防钠通道介导的疾病或病症（例如疼痛）的羟吲哚化合物。 还公开了包含该化合物的药物组合物和使用该化合物的方法。

公开(公告)号：US08106087B2

公开(公告)日：2012-01-31

申请号：US12650196

申请日：2009-12-30

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/407 ,  A61K31/5377

CPC分类号： C07D491/10

摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

摘要翻译： 本发明涉及式（I）的螺 - 羟吲哚化合物：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义，作为立体异构体， 其互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。 还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

公开(公告)号：US20110172282A9

公开(公告)日：2011-07-14

申请号：US12445264

申请日：2007-10-12

申请人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

发明人： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Duanjie Hou ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Shaoyi Sun ,  Jianyu Sun ,  Nagasree Chakka ,  Tom Hsieh ,  Vandna Raina

IPC分类号： A61K31/404 ,  A61P9/10 ,  A61P17/04 ,  A61P35/00

CPC分类号： A61K31/407 ,  A61K31/437

摘要： This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.

摘要翻译： 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 立体异构体，对映异构体，互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。

公开(公告)号：US20100130487A1

公开(公告)日：2010-05-27

申请号：US12650218

申请日：2009-12-30

申请人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

发明人： Mikhail Chafeev ,  Nagasree Chakka ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Duanjie Hou ,  Tom Hsieh ,  Rajender Kamboj ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC分类号： A61K31/407 ,  C07D491/20 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/5377 ,  A61P25/24 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00

CPC分类号： C07D491/10

摘要： This invention is directed to spiro-oxindole compounds of formula (I): wherein k, j, Q, R1, R2a, R2b, R2c, R2d, R3a, R3b, R3c, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.

摘要翻译： 本发明涉及式（I）的螺 - 羟吲哚化合物：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义，作为立体异构体， 其互变异构体或其混合物; 或其药学上可接受的盐，溶剂合物或前药，其可用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。 还公开了包含化合物的药物组合物以及制备和使用化合物的方法。

公开(公告)号：US20090131447A1

公开(公告)日：2009-05-21

申请号：US11815739

申请日：2006-02-08

申请人： Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

发明人： Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

IPC分类号： A61K31/501 ,  A61K31/4436 ,  A61K31/496 ,  A61P3/04

CPC分类号： A61K31/64 ,  A61K31/00 ,  A61K31/4439 ,  A61K38/28 ,  A61K45/06 ,  A61K2300/00

摘要： This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.

摘要翻译： 本发明涉及式（I）的SCD-1抑制剂的用途：其中x，y，V，W，G，J，L，M，R2，R3，R5，R5a，R6，R6a，R7， 本文定义R7a，R8和R8a与其他药物治疗组合以治疗不利的体重增加。