公开(公告)号：US08415370B2

公开(公告)日：2013-04-09

申请号：US13557833

申请日：2012-07-25

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Yurevna Zenova ,  Qi Jia ,  Jean-Jacques Cadieux ,  Simon J. Gauthier ,  Amy Frances Douglas ,  Tom Hsieh ,  Nagasree Chakka ,  Zoran Cikojevic

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Yurevna Zenova ,  Qi Jia ,  Jean-Jacques Cadieux ,  Simon J. Gauthier ,  Amy Frances Douglas ,  Tom Hsieh ,  Nagasree Chakka ,  Zoran Cikojevic

IPC: A61K31/44 ,  C07D213/02

CPC classification number: C07D513/22 ,  C07D491/10 ,  C07D491/107 ,  C07D491/20 ,  C07D491/22 ,  C07D495/20 ,  C07D498/20 ,  C07D513/20 ,  C07D519/00

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及螺 - 羟吲哚化合物，作为立体异构体，对映体，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：US08101647B2

公开(公告)日：2012-01-24

申请号：US12577799

申请日：2009-10-13

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Zenova

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Zenova

IPC: C07D491/10 ,  A61K31/404

CPC classification number: C07D491/107 ,  C07D491/20

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

公开(公告)号：US20120014906A1

公开(公告)日：2012-01-19

申请号：US13238081

申请日：2011-09-21

Applicant: Sultan Chowdhury ,  Natalie Dales ,  Julia Fonarev ,  Jianmin Fu ,  Duanjie Hou ,  Qi Jia ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun ,  Zaihui Zhang

Inventor： Sultan Chowdhury ,  Natalie Dales ,  Julia Fonarev ,  Jianmin Fu ,  Duanjie Hou ,  Qi Jia ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun ,  Zaihui Zhang

IPC: A61K31/785 ,  C07D417/14 ,  C07D471/04 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501 ,  A61K31/437 ,  C12N9/99 ,  A61K38/28 ,  A61K38/26 ,  A61K31/455 ,  A61K31/616 ,  A61P3/00 ,  A61P3/10 ,  A61P3/08 ,  A61P3/06 ,  A61P9/12 ,  A61P7/02 ,  A61P3/04 ,  A61P17/00 ,  A61P17/06 ,  A61P17/10 ,  A61P17/02 ,  C07D417/04

CPC classification number: C07D417/04 ,  C07D417/14

Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.

Abstract translation: 本发明提供调节硬脂酰辅酶A去饱和酶活性的杂环衍生物。 还包括使用这些衍生物调节硬脂酰辅酶A去饱和酶活性的方法和包含这些衍生物的药物组合物。

公开(公告)号：US20110269788A1

公开(公告)日：2011-11-03

申请号：US13142375

申请日：2009-12-29

Applicant: Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Amy Frances Douglas ,  Jianmin Fu ,  Jonathan Langille ,  Shaoyi Sun ,  Mark Wood

Inventor： Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Amy Frances Douglas ,  Jianmin Fu ,  Jonathan Langille ,  Shaoyi Sun ,  Mark Wood

IPC: A61K31/4355 ,  A61K31/437 ,  A61P25/00 ,  A61P25/24 ,  A61P9/00 ,  A61P11/00 ,  A61P13/10 ,  A61P1/04 ,  A61P25/06 ,  A61P1/00 ,  A61P25/02 ,  A61P19/02 ,  A61P29/00 ,  A61P9/10 ,  A61P21/04 ,  A61P21/00 ,  A61P3/00 ,  A61P9/12 ,  A61P5/16 ,  A61P25/22 ,  A61P25/18 ,  A61P35/00 ,  A61P25/08 ,  A61P7/00 ,  A61P13/08 ,  A61P17/04 ,  C07D491/20

CPC classification number: C07D491/20 ,  C07D471/04

Abstract: This invention is directed to spiro-oxindole compounds of formulas (I), (II), (III), as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Abstract translation: 本发明涉及式（I），（II），（III）的螺 - 羟吲哚化合物，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：US20100099728A1

公开(公告)日：2010-04-22

申请号：US12577799

申请日：2009-10-13

Applicant: Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Zenova

Inventor： Mikhail Chafeev ,  Sultan Chowdhury ,  Lauren Fraser ,  Jianmin Fu ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov ,  Mark Wood ,  Alla Zenova

IPC: A61K31/407 ,  C07D491/107 ,  C07D491/20 ,  A61P25/00 ,  A61P9/00 ,  A61P11/00

CPC classification number: C07D491/107 ,  C07D491/20

Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

公开(公告)号：US07700641B2

公开(公告)日：2010-04-20

申请号：US11402310

申请日：2006-04-11

Applicant: 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

Inventor： 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: A61K31/407 ,  C07D491/107

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：US20090131447A1

公开(公告)日：2009-05-21

申请号：US11815739

申请日：2006-02-08

Applicant: 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

Inventor： 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: A61K31/501 ,  A61K31/4436 ,  A61K31/496 ,  A61P3/04

CPC classification number: A61K31/64 ,  A61K31/00 ,  A61K31/4439 ,  A61K38/28 ,  A61K45/06 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20060252758A1

公开(公告)日：2006-11-09

申请号：US11402200

申请日：2006-04-11

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: A61K31/519 ,  A61K31/4747 ,  A61K31/407 ,  C07D498/14 ,  C07D487/14

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, 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, 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，R 1，R 3a，R 3b， 作为其立体异构体，对映异构体，互变异构体或其混合物; R 3，R 3，R 3和R 3如本文所定义。 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：US08742109B2

公开(公告)日：2014-06-03

申请号：US13620391

申请日：2012-09-14

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: C07D213/36

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：US08466188B2

公开(公告)日：2013-06-18

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: A61K31/40 ,  A61K31/5377

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。