公开(公告)号：US20110251224A1

公开(公告)日：2011-10-13

申请号：US13078678

申请日：2011-04-01

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

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

IPC: A61K31/4747 ,  A61K31/407 ,  A61P25/24 ,  A61P25/04 ,  A61P9/00 ,  A61P11/00 ,  A61P25/18 ,  A61P29/00 ,  A61P25/06 ,  A61P25/00 ,  A61P43/00 ,  A61P25/22 ,  A61P9/10 ,  A61P19/02 ,  A61P35/00 ,  A61P25/08 ,  A61P9/06 ,  C07D491/20

CPC classification number: C07D491/10

Abstract: 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.

Abstract translation: 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：US20110087027A1

公开(公告)日：2011-04-14

申请号：US12904880

申请日：2010-10-14

Applicant: Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin Fu ,  Qi Jia ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

Inventor： Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin Fu ,  Qi Jia ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

IPC: C07D401/14 ,  C07D491/20

CPC classification number: C07D491/20 ,  C07D405/04

Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及制备某些螺 - 羟吲哚衍生物的方法，其可用于治疗和/或预防钠通道介导的疾病或病症如疼痛。

公开(公告)号：US20110034500A1

公开(公告)日：2011-02-10

申请号：US12855514

申请日：2010-08-12

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Serguei Sviridov

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Robert Fraser ,  Jianmin Fu ,  Rajender Kamboj ,  Shifeng Liu ,  Mehran Seid Bagherzadeh ,  Jianyu Sun ,  Serguei Sviridov

IPC: A61K31/438 ,  C07D491/22 ,  C07D495/22 ,  A61K31/407 ,  A61P29/00 ,  A61P25/24 ,  A61P9/00 ,  A61P11/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/04

CPC classification number: C07D491/22 ,  C07D495/22

Abstract: This invention is directed to spiroheterocyclic compounds of formula (I): wherein k, j, p, Q, R1, R3a, R3b, R3e, and R3d are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, 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.

Abstract translation: 本发明涉及式（I）的螺杂环化合物：其中k，j，p，Q，R1，R3a，R3b，R3e和R3d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，溶剂化物或前药，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：US07777036B2

公开(公告)日：2010-08-17

申请号：US11575638

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

IPC: C07D419/00 ,  C07D413/00 ,  C07D405/00 ,  C07D277/00

CPC classification number: C07D213/82

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where y, G, K, L, M, W, V, R2, R3, R4a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物，其中y，G，K，L，M， W，V，R2，R3，R4a，R6，R6a，R7，R7a，R8和R8a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US07754711B2

公开(公告)日：2010-07-13

申请号：US11055034

申请日：2005-02-09

Applicant: Nagasree Chakka ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Michael D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. Gschwend

Inventor： Nagasree Chakka ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Michael D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. Gschwend

IPC: A61K31/551 ,  A61K31/5513 ,  A61K31/50 ,  A61K31/502 ,  A61K31/501 ,  C07D245/02 ,  C07D243/04 ,  C07D243/08 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  A61P7/12

CPC classification number: C07D237/20 ,  A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/22 ,  C07D237/24

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了治疗哺乳动物，优选人类的SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（Ia）化合物：其中x，y，W，V，R 2 ，R3，R4，R5，R6，R6a，R7，R7a，R8，R8a，R9和R9a如本文所定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20100173967A1

公开(公告)日：2010-07-08

申请号：US12445264

申请日：2007-10-12

Applicant: 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

Inventor： 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: A61K31/404 ,  A61P9/10 ,  A61P17/04 ,  A61P35/00

CPC classification number: A61K31/407 ,  A61K31/437

Abstract: 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.

Abstract translation: 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：US20100160362A1

公开(公告)日：2010-06-24

申请号：US12445270

申请日：2007-10-12

Applicant: Jean-Jacques Cadieux ,  Sultan Chowdhury ,  Jianmin Fu ,  Rajender Kamboj ,  Tom Hsieh ,  Qi Jia ,  Shifeng Liu ,  Jianyu Sun

Inventor： Jean-Jacques Cadieux ,  Sultan Chowdhury ,  Jianmin Fu ,  Rajender Kamboj ,  Tom Hsieh ,  Qi Jia ,  Shifeng Liu ,  Jianyu Sun

IPC: A61K31/438 ,  C07D491/20

CPC classification number: C07D471/22 ,  C07D471/20

Abstract: This invention is directed to methods of using spiro-oxindole compounds of formula (I): wherein j, k, m, Q, X, R1, R2a, R2b, R2c, R2d and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, N-oxide, solvate or prodrug thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中j，k，m，Q，X，R1，R2a，R2b，R2c，R2d和R3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，N-氧化物，溶剂合物或前药，用于治疗和/或预防钠通道介导的疾病或病症，例如疼痛。

公开(公告)号：US20070299081A1

公开(公告)日：2007-12-27

申请号：US11575639

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Serguei Sviridov ,  Shaoyi Sun ,  Mehran Seid Bagherzadeh ,  Vandna Raina ,  Duanjie Hou ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru ,  Nagasree Chakka

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Serguei Sviridov ,  Shaoyi Sun ,  Mehran Seid Bagherzadeh ,  Vandna Raina ,  Duanjie Hou ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru ,  Nagasree Chakka

IPC: A61K31/501 ,  A61K31/445 ,  A61P3/00 ,  A61P3/10 ,  C07D237/02 ,  C07D401/04 ,  C07D211/94 ,  A61P3/04 ,  A61K31/50

CPC classification number: C07D213/82 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): Formula (I) where x, y, G, J, L, M, V, W, R2, R3, R4, R5, R5a, R6, R6a, R7, R7a, R8, and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract translation: 公开了在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法，其中所述方法包括向有需要的哺乳动物施用式（I）化合物：式（I）其中x，y，G ，J，L，M，V，W，R 2，R 3，R 4，R 5， R 5a，R 6，R 6a，R 7，R 7a， R 8，R 8a和R 8a在本文中定义。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20160009667A1

公开(公告)日：2016-01-14

申请号：US14772726

申请日：2014-03-14

Applicant: Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Shaoyi SUN ,  GENENTECH, INC. ,  XENON PHARMACEUTICALS INC.

Inventor： Chien-An CHEN ,  Sultan CHOWDHURY ,  Christoph Martin DEHNHARDT ,  Shaoyi SUN

IPC: C07D261/20 ,  C07D413/12

CPC classification number: C07D261/20 ,  C07D413/12

Abstract: The invention provides compounds having the general formula (I): and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, R1, R2, R3, R4, and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

Abstract translation: 本发明提供具有通式（I）的化合物及其药学上可接受的盐，其中变量RA，下标n，环A，X2，L，下标m，X1，R1，R2，R3，R4和RN具有 含有本文所述的含义，以及含有这些化合物的组合物和使用这些化合物和组合物的方法。

公开(公告)号：US08445696B2

公开(公告)日：2013-05-21

申请号：US12904880

申请日：2010-10-14

Applicant: Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin Fu ,  Qi Jia ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

Inventor： Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jianmin Fu ,  Qi Jia ,  Stefanie Abel ,  Emad El-Sayed ,  Elke Huthmann ,  Thomas Isarno

IPC: C07D491/20

CPC classification number: C07D491/20 ,  C07D405/04

Abstract: This invention is directed to methods of preparing certain spiro-oxindole derivatives, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及制备某些螺 - 羟吲哚衍生物的方法，其可用于治疗和/或预防钠通道介导的疾病或病症如疼痛。