公开(公告)号：US06500634B1

公开(公告)日：2002-12-31

申请号：US08164487

申请日：1993-12-10

Applicant: Robert Foldes ,  Rajender Kamboj

Inventor： Robert Foldes ,  Rajender Kamboj

IPC: C07K14705

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. DNA coding for EAA receptors of one family of human NMDA-binding type receptors has now been isolated and receptor proteins 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。 编码人类NMDA结合型受体的一个家族的EAA受体的DNA已经被分离并且受体蛋白质被表征。 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：US06399313B1

公开(公告)日：2002-06-04

申请号：US08439946

申请日：1995-05-12

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 ,  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 characterized 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。 该受体的结构特征在于，公开了表达这些受体的细胞系的构建和用途。

公开(公告)号：US06376200B1

公开(公告)日：2002-04-23

申请号：US08249241

申请日：1994-05-25

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

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

IPC: G01N33567

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：US6013768A

公开(公告)日：2000-01-11

申请号：US789478

申请日：1997-01-27

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

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 art 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EAA受体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：US5494792A

公开(公告)日：1996-02-27

申请号：US91569

申请日：1993-07-15

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

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

IPC: G01N33/53 ,  A61K38/00 ,  C07K14/705 ,  C07K16/28 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12R1/91 ,  C12N15/10 ,  C12Q1/00 ,  G01N33/50

CPC classification number: C07K14/70571 ,  A61K38/00 ,  Y10S530/839

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 commerical 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：US08258160B2

公开(公告)日：2012-09-04

申请号：US12520332

申请日：2007-12-19

Applicant: Natalie Dales ,  Zaihui Zhang ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun

Inventor： Natalie Dales ,  Zaihui Zhang ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun

IPC: A61K31/41 ,  A61K31/415 ,  C07D249/00 ,  C07D249/08 ,  C07D257/04

CPC classification number: C07D409/04 ,  C07D413/04 ,  C07D417/04

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：US08148378B2

公开(公告)日：2012-04-03

申请号：US12390117

申请日：2009-02-20

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

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

IPC: A61K31/501 ,  A61P3/06 ,  A61P9/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00

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

Abstract: A method of treating an SCD-mediated disease or condition in a mammal, preferably a human, includes administering to a mammal 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. The SCD-mediated disease or condition may be selected from the group consisting of Type II diabetes, impaired glucose tolerance, insulin resistance, obesity, fatty liver, non-alcoholic steatohepatitis, dyslipidemia, metabolic syndrome, acne, cardiovascular disease, hypertriglyceridemia, inflammation, cancer, and any combination of these.

Abstract translation: 在哺乳动物，优选人中治疗SCD介导的疾病或病症的方法包括向哺乳动物施用式（I）化合物：其中x，y，W，V，R 2，R 3，R 4，R 5，R 6 ，R6a，R7，R7a，R8，R8a，R9和R9a在本文中定义。 SCD介导的疾病或病症可以选自II型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖，脂肪肝，非酒精性脂肪性肝炎，血脂异常，代谢综合征，痤疮，心血管疾病，高甘油三酯血症，炎症， 癌症，以及这些的任何组合。

公开(公告)号：US08026360B2

公开(公告)日：2011-09-27

申请号：US12541005

申请日：2009-08-13

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Vandna Raina ,  Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Shifeng Lui ,  Shaoyi Sun ,  Duanjie Hou

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Vandna Raina ,  Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Shifeng Lui ,  Shaoyi Sun ,  Duanjie Hou

IPC: C07D401/00

CPC classification number: A61K31/501 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  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 x, y, G, J, K, L, M, W, 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，R 2，R 3，R 5，R 5a，R 6，R 6a，R 7，R 7a，R 8和R 8a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：US07951805B2

公开(公告)日：2011-05-31

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: C07D401/04 ,  A61K31/501 ,  A61P9/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  C07D213/26 ,  A61K31/45

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，R2，R3，R4，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：US20100125072A1

公开(公告)日：2010-05-20

申请号：US12650196

申请日：2009-12-30

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: A61K31/5377 ,  C07D491/10 ,  A61K31/407 ,  A61K31/4439 ,  A61K31/506

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.