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：US07052850B2

公开(公告)日：2006-05-30

申请号：US10084507

申请日：2002-02-28

Applicant: Donald G. Munroe ,  Rajender Kamboj ,  Diana Peters ,  Fatemeh Kooshesh ,  Tejal B. Vyas ,  Ashwani K. Gupta

Inventor： Donald G. Munroe ,  Rajender Kamboj ,  Diana Peters ,  Fatemeh Kooshesh ,  Tejal B. Vyas ,  Ashwani K. Gupta

IPC: G01N33/53 ,  G01N33/566 ,  C12N5/00 ,  C12N15/00 ,  C07K14/705

CPC classification number: C07K14/705 ,  A61K38/00

Abstract: A novel, isolated EDG receptor that upon activation results in increased induction of IL-8 or NF-κB. Preferably, the EDG receptor is a human EDG-4 receptor, which has an amino acid sequence shown in FIGS. 16A and 16B, or a variant of these sequences having at least 91% sequence identity.

Abstract translation: 一种新型的分离的EDG受体，其在激活时导致IL-8或NF-κB的诱导增加。 优选地，EDG受体是人EDG-4受体，其具有图1和图2所示的氨基酸序列。 16 A和16 B，或这些序列的变体具有至少91％的序列同一性。

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。

公开(公告)号：US06500624B1

公开(公告)日：2002-12-31

申请号：US08189738

申请日：1994-02-01

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

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

IPC: G01N3353

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 the kainate-binding type of EAA receptor, 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。 编码一种红藻氨酸结合型EAA受体家族的DNA已经被分离出来，其特征在于受体蛋白质。 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：US06489124B1

公开(公告)日：2002-12-03

申请号：US08217704

申请日：1994-03-25

Applicant: Robert Foldes ,  Robert Fantaske ,  Sally-Lin Adams ,  Rajender Kamboj

Inventor： Robert Foldes ,  Robert Fantaske ,  Sally-Lin Adams ,  Rajender Kamboj

IPC: G01N3353

CPC classification number: C07K14/705 ,  C07K14/70571 ,  G01N33/567 ,  G01N33/68

Abstract: Neurotransmission by excitatory amino acids (EAAs) such as glutamate is mediated via membrane-bound surface receptors. This neurotransmission has been found to be modulated by certain modulatory proteins. DNA coding for a family of such modulatory proteins has now been isolated and the modulatory proteins have been characterized. Herein described are recombinant cell lines which produce these modulatory proteins as heterologous membrane-bound products. Also described are related aspects of the invention, which are of commercial significance, including the use of cell lines which express the modulatory proteins either homomerically, or heteromerically in a complex with an NMDA receptor, as a tool for discovery of compounds which affect the function of the modulatory proteins.

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。 已经发现这种神经传递被某些调节蛋白调节。 已经分离了编码这种调节蛋白家族的DNA，并且已经表征了调节蛋白质。 本文描述了产生这些调节蛋白作为异源膜结合产物的重组细胞系。 还描述了具有商业意义的本发明的相关方面，包括使用在与NMDA受体的复合物中同源或异源地表达调节蛋白的细胞系作为发现影响功能的化合物的工具 的调节蛋白。

公开(公告)号：US06441155B1

公开(公告)日：2002-08-27

申请号：US08242344

申请日：1994-05-13

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 ,  C07K14/705

Abstract: Described herein are isolated polynucleotides which code for an AMPA-type human CNS receptor, designated the human GluR2B receptor. The receptor is charactereized structurally and the construction and use of cell lines expressing these receptor is disclosed.

Abstract translation: 本文描述的是编码AMPA型人CNS受体的分离的多核苷酸，其命名为人GluR2B受体。 受体在结构上具有特征性，并且公开了表达这些受体的细胞系的构建和用途。

公开(公告)号：US06403323B1

公开(公告)日：2002-06-11

申请号：US08257029

申请日：1994-06-08

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

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

IPC: C01N3353

CPC classification number: C07K14/705 ,  C07K14/70571

Abstract: Described herein are isolated polynucleotides which code for a family of AMPA-type human CNS receptors. The receptors are characterized structurally and the construction and use of cell lines expressing these receptors are disclosed.

Abstract translation: 本文描述了编码AMPA型人CNS受体家族的分离的多核苷酸。 所述受体在结构上表征，并且公开了表达这些受体的细胞系的构建和用途。

公开(公告)号：US6136544A

公开(公告)日：2000-10-24

申请号：US666221

申请日：1996-06-20

Applicant: Rajender Kamboj ,  Stephen Nutt

Inventor： Rajender Kamboj ,  Stephen Nutt

IPC: G01N33/566 ,  C07K14/705 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12R1/91

CPC classification number: C07K14/705

Abstract: Human CNS receptor-encoding DNA is provided from which more than one form of the receptor protein, an edited form and an unedited form, is expressed in vivo. The edited and unedited receptor forms are functionally distinct, and appear to be selectively expressed. Thus, a CNS receptor-encoding gene that is subject to such editing has value in screening compounds for potential therapeutic utility.

Abstract translation: 提供编码人类CNS受体编码DNA，其中多于一种形式的受体蛋白，编辑形式和未编辑的形式在体内表达。 编辑和未编辑的受体形式在功能上是不同的，并且似乎被选择性地表达。 因此，经受这种编辑的CNS受体编码基因在筛选化合物中具有潜在的治疗效用。

公开(公告)号：US6018023A

公开(公告)日：2000-01-25

申请号：US487691

申请日：1995-06-07

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

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

IPC: C07K14/435 ,  C07K14/00 ,  C07K14/705 ,  C07K16/00 ,  C07K16/28 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12R1/91 ,  G01N33/53 ,  G01N33/566

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 the kainate-binding type of EAA receptor, 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.