公开(公告)号：US07514436B2

公开(公告)日：2009-04-07

申请号：US10566856

申请日：2004-07-29

Applicant: Heinz W. Gschwend ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Rajender Kamboj

Inventor： Heinz W. Gschwend ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Rajender Kamboj

IPC: A61K31/55 ,  C07D403/04 ,  A61P7/12

CPC classification number: C07D213/75 ,  A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D213/76 ,  C07D213/81 ,  C07D237/20 ,  C07D237/22

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 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：US07456180B2

公开(公告)日：2008-11-25

申请号：US10567009

申请日：2004-07-29

Applicant: Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael D. Winther ,  Heinz W. Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark W. Holladay ,  Wenbao Li ,  Chi Tu

Inventor： Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael D. Winther ,  Heinz W. Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark W. Holladay ,  Wenbao Li ,  Chi Tu

IPC: A61K31/497 ,  C07D241/02

CPC classification number: A61K31/551 ,  A61K31/00 ,  A61K31/501 ,  C07D237/20 ,  C07D403/08 ,  C07D405/08 ,  C07D409/12 ,  C07D413/08

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 G, J, L, M, x, y, W, V, R2, R3, R4, R5, R6, R7, R8, R8a, R9, R9a, R10, R10a, R11 and R11a 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G，J，L，M，x ，y，W，V，R 2，R 3，R 4，R 5，R SUP > 6，R 7，R 8，R 8a，R 9，R SUP， > 9a，R 10，R 10a，R 11和R 11是本文定义的 。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20080280916A1

公开(公告)日：2008-11-13

申请号：US12036685

申请日：2008-02-25

Applicant: Andreas Bilich ,  Michael D. Winther ,  Yigal Paul Goldberg

Inventor： Andreas Bilich ,  Michael D. Winther ,  Yigal Paul Goldberg

IPC: A61K31/501 ,  A61P17/00

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D473/00

Abstract: Methods of treating an SCD-mediated skin disorder or condition in a mammal, preferably a human include administering to a mammal in need thereof a compound of formula (I): where x, y, W, V, R2, R3, R4, R5, R6, R6a, R7, R7a, R8, R8a, R9 and R9a are defined herein.

Abstract translation: 在哺乳动物，优选人中治疗SCD介导的皮肤病症或病症的方法包括向有需要的哺乳动物施用式（I）化合物：其中x，y，W，V，R 2， R 3，R 3，R 4，R 5，R 6，R 6a， R S，R 7，R 7a，R 8，R 8a，R 9， SUP＆gt;和R 9a在本文中定义。

公开(公告)号：US20080207587A1

公开(公告)日：2008-08-28

申请号：US11575642

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Serguei Sviridov ,  Sultan Chowdhury ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jian-Min Fu ,  Serguei Sviridov ,  Sultan Chowdhury ,  Vishnumurthy Kodumuru

IPC: A61K31/501 ,  C07D237/06 ,  C07D403/02 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07D401/02

CPC classification number: C07D401/12 ,  A61K31/501 ,  C07D237/24 ,  C07D403/12

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 x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a arc 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x，y，G，J，K， L，M，Q，W，V，R2，R3，R5，R5a，R6，R6a，R7，R7a，R8和R8a。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20080194616A1

公开(公告)日：2008-08-14

申请号：US12026435

申请日：2008-02-05

Applicant: Shifeng Liu ,  Jianmin Fu ,  Rajender Kamboj ,  Sultan Chowdhury ,  Qi Jia ,  Mark Wood ,  Jianyu Sun

Inventor： Shifeng Liu ,  Jianmin Fu ,  Rajender Kamboj ,  Sultan Chowdhury ,  Qi Jia ,  Mark Wood ,  Jianyu Sun

IPC: A61K31/444 ,  C07D471/02 ,  A61P29/00

CPC classification number: C07D471/04

Abstract: This invention is directed to pyridopyrimidinone compounds of formula (I): wherein n, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, useful 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）的吡啶并嘧啶酮化合物：其中n，R 1，R 2和R 3如本文所定义， 作为立体异构体，其对映异构体，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。

公开(公告)号：US20080108629A1

公开(公告)日：2008-05-08

申请号：US11575636

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Shaoyi Sun ,  Nagasree Chakka

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Shaoyi Sun ,  Nagasree Chakka

IPC: A61K31/496 ,  C07D417/04 ,  C07D413/04 ,  C07D403/04 ,  A61P3/00

CPC classification number: C07D277/28 ,  A61K31/381 ,  A61K31/41 ,  A61K31/415 ,  C07D231/38 ,  C07D271/113 ,  C07D285/01

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 x, y, G, J, K, L, M, W, V, R2, R3, 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：其中x，y，G，J，K ，L，M，W，V，R 2，R 3，R 5，R 5a，R R 6，R 6a，R 7，R 7a，R 8和R 8，R 8， 本文定义了8a。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20070219211A1

公开(公告)日：2007-09-20

申请号：US11575643

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

Inventor： Rajender Kamboj ,  Jian-Min Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

IPC: A61K31/50 ,  A61K31/497 ,  C07D403/00 ,  C12N9/99

CPC classification number: A61K31/497 ,  A61K31/50 ,  C07D235/08 ,  C07D487/04

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise, for example, administering to a mammal in need thereof a compound of formula (I): where x, y, J, K, L, M, W, V, R2, R3, 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，其中所述方法包括例如向有需要的哺乳动物施用式（I）化合物：其中x，y，J ，K，L，M，W，V，R 2，R 3，R 5，R 5a， R 6，R 6a，R 7，R 7a，R 8， 和R 8a是本文定义的。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20060293308A1

公开(公告)日：2006-12-28

申请号：US10566857

申请日：2004-07-29

Applicant: Melwyn Abreo ,  Daniel Harvey ,  Mikhail Kondratenko ,  Wenbao Li ,  Rajender Kamboj ,  Vishnumurthy Rodumuru ,  Michael Winther ,  Heinz Gschwend ,  Nagasres Chakka ,  Shifeng Liu ,  Serguei Sviridov ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel Harvey ,  Mikhail Kondratenko ,  Wenbao Li ,  Rajender Kamboj ,  Vishnumurthy Rodumuru ,  Michael Winther ,  Heinz Gschwend ,  Nagasres Chakka ,  Shifeng Liu ,  Serguei Sviridov ,  Shaoyi Sun

IPC: A01N43/62

CPC classification number: C07D401/14 ,  A61K31/00 ,  A61K31/444 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76 ,  C07D213/81 ,  C07D401/04

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): wherein W, V, x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a 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W，V，x，y，R R 1，R 2，R 3，R 4，R 5，R 5，R 5， R 6，R 7，R 7，R 8，R 8，R 8， R 9，R 9，R 10和R 10 10a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：US20060252812A1

公开(公告)日：2006-11-09

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 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 Bagherzadeh ,  Jianyu Sun ,  Shaoyi Sun ,  Serguei Sviridov

IPC: A61K31/407 ,  C07D491/10

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，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：US20050065143A1

公开(公告)日：2005-03-24

申请号：US10901563

申请日：2004-07-29

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 Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz 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 Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz Gschwend

IPC: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  A61P3/06 ,  C07D237/20 ,  C07D237/24

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  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 (I): 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x，y，W，V，R R 2，R 3，R 4，R 5，R 6，R 6a，R 7，R 7a，R 8，R 8a，R 本文定义<9>和R 9a。 还公开了包含式（I）化合物的药物组合物。