公开(公告)号：US20060252767A1

公开(公告)日：2006-11-09

申请号：US10567009

申请日：2004-07-29

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

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

IPC: A61K31/497 ,  C07D403/04

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 11a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：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：US06358693B1

公开(公告)日：2002-03-19

申请号：US08403663

申请日：1995-03-14

Applicant: Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

Inventor： Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

IPC: C12N1512

CPC classification number: C07K14/70571 ,  A61K48/00

Abstract: Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR4B receptor. The receptor is characterized structurally and the construction and use of cell lines expressing the receptor is disclosed.

Abstract translation: 本文描述了编码AMPA型人CNS受体的分离的多核苷酸，其命名为人GluR4B受体。 该受体的结构特征在于，公开了表达受体的细胞系的构建和用途。

公开(公告)号：US06322999B1

公开(公告)日：2001-11-27

申请号：US08377503

申请日：1995-01-24

Applicant: Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

Inventor： Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

IPC: C12P2106

CPC classification number: C07K14/70571 ,  F02B2075/027

Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors of the kainate-binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.

Abstract translation: 兴奋性氨基酸（EAAs）如谷氨酸的神经传递通过膜结合表面受体介导。 已经分离了编码红藻氨酸结合型EAA受体的这些受体的一个家族的DNA，并且以受体蛋白为特征。 本文描述了产生作为异源膜结合产物的EAA受体的重组细胞系。 还描述了具有商业意义的本发明的相关方面。 包括使用细胞系作为发现调节EAA受体刺激的化合物的工具。

公开(公告)号：US5830712A

公开(公告)日：1998-11-03

申请号：US597249

申请日：1996-02-06

Applicant: Vikarna Rampersad ,  Roman Zastawny ,  Rajender Kamboj

Inventor： Vikarna Rampersad ,  Roman Zastawny ,  Rajender Kamboj

IPC: C12Q1/68 ,  C12P19/34 ,  C07H21/02 ,  C07H21/04

CPC classification number: C12Q1/6848

Abstract: A novel method for inactivating undesirable members in a nucleic acid sample which comprises undesirable and desirable members of a nucleic acid family. The method includes the step of adding a blocker to the sample which selectively associates with the undesirable members such that they are unable to participate in any further processing of the sample. The method advantageously provides a means whereby desirable members of the nucleic acid family can be processed, i.e. identified, amplified and/or isolated, without interference from undesirable sequence-related members.

Abstract translation: 一种用于灭活核酸样品中不期望的成员的新方法，其包含核酸家族的不期望的和期望的成员。 该方法包括将样品添加到选择性地与不期望的成员相关联的样品的步骤，使得它们不能参与样品的任何进一步处理。 该方法有利地提供了一种方法，其中核酸家族的理想成员可以被加工，即鉴定，扩增和/或分离，而不受不期望的序列相关成员的干扰。

公开(公告)号：US5610032A

公开(公告)日：1997-03-11

申请号：US254573

申请日：1994-06-06

Applicant: Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

Inventor： Rajender Kamboj ,  Candace E. Elliott ,  Stephen L. Nutt

IPC: C07K14/705 ,  C12N15/00

CPC classification number: C07K14/70571 ,  C07K14/705

Abstract: Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR1B receptor. The receptor is characterized structurally and the construction and use of cell lines expressing the receptor is disclosed.

Abstract translation: 本文描述了编码AMPA型人CNS受体的分离的多核苷酸，其命名为人GluR1B受体。 该受体的结构特征在于，公开了表达受体的细胞系的构建和用途。

公开(公告)号：US5576205A

公开(公告)日：1996-11-19

申请号：US185232

申请日：1994-01-24

Applicant: Rajender Kamboj ,  Stephen L. Nutt ,  Lee Shekter ,  Michael A. Wosnick

Inventor： Rajender Kamboj ,  Stephen L. Nutt ,  Lee Shekter ,  Michael A. Wosnick

IPC: C07K16/00 ,  C07K14/00 ,  C07K14/705 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12R1/91 ,  G01N33/53 ,  C12N1/21 ,  C12N15/79

CPC classification number: C07K14/70571

Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. DNA coding for one family of these receptors, of the kainate binding type of EAA receptors, has now been isolated and the receptor protein characterized. Herein described are recombinant cell lines which produce the EAA receptor as a heterologous membrane-bound product. Also described are related aspects of the invention, which are of commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor stimulation.

Abstract translation: 兴奋性氨基酸（EAAs）如谷氨酸的神经传递通过膜结合表面受体介导。 已经分离了编码这些受体的一个家族的类红景天结合型EAA受体的DNA，并且以受体蛋白为特征。 本文描述了产生作为异源膜结合产物的EAA受体的重组细胞系。 还描述了具有商业意义的本发明的相关方面。 包括使用细胞系作为发现调节EAA受体刺激的化合物的工具。

公开(公告)号：US08541457B2

公开(公告)日：2013-09-24

申请号：US11916243

申请日：2006-06-05

Applicant: Jianmin Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Zaihui Zhang

Inventor： Jianmin Fu ,  Duanjie Hou ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Vandna Raina ,  Shaoyi Sun ,  Serguei Sviridov ,  Zaihui Zhang

IPC: A01N43/78 ,  A61K31/425

CPC classification number: C07D277/587 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/616 ,  A61K38/26 ,  A61K38/28 ,  A61K45/06 ,  C07D277/56 ,  C07D417/06 ,  C07D417/12

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 V, W, R1, R2, R3 and R4 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（I）化合物，其中V，W，R 1，R 2，R 3 和R4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：US08383628B2

公开(公告)日：2013-02-26

申请号：US12816076

申请日：2010-06-15

Applicant: Melwyn Abreo ,  Daniel F. Harvey ,  Mikhail A. Kondratenko ,  Wenbao Li ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Michael D. Winther ,  Heinz W. Gschwend ,  Nagasree Chakka ,  Shifeng Liu ,  Serguei Sviridov ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel F. Harvey ,  Mikhail A. Kondratenko ,  Wenbao Li ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Michael D. Winther ,  Heinz W. Gschwend ,  Nagasree Chakka ,  Shifeng Liu ,  Serguei Sviridov ,  Shaoyi Sun

IPC: A61K31/497 ,  C07D401/00

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 1 ，R2，R3，R4，R5，R6，R7，R7a，R8，R8a，R9，R9a，R10和R10a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：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。