公开(公告)号：US5981704A

公开(公告)日：1999-11-09

申请号：US822238

申请日：1997-03-20

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 ,  C07K14/435 ,  A61K38/17

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 commercial significance. Included is use of the cell lines as a tool for discovery of compounds which modulate EAA receptor simulation.

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受体模拟的化合物的工具。

公开(公告)号：US5643785A

公开(公告)日：1997-07-01

申请号：US259164

申请日：1994-06-13

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

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

IPC: A61K38/00 ,  A61K48/00 ,  C07K14/00 ,  C07K14/705 ,  C07K16/00 ,  C12N5/10 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  G01N33/53 ,  G01N33/566 ,  C07H21/04 ,  C12N15/63 ,  C12N15/85

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：US5614406A

公开(公告)日：1997-03-25

申请号：US203676

申请日：1994-02-28

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 ,  C12N1/21 ,  C12N15/79

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 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：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。

公开(公告)号：US20130096056A1

公开(公告)日：2013-04-18

申请号：US13620339

申请日：2012-09-14

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

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：US08293768B2

公开(公告)日：2012-10-23

申请号：US13231075

申请日：2011-09-13

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

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

IPC: A61K31/425 ,  A61K31/433 ,  A61K31/4196 ,  C07D203/02 ,  C07D249/08 ,  C07D285/10

CPC classification number: C07D409/04 ,  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.

公开(公告)号：US08236835B2

公开(公告)日：2012-08-07

申请号：US12442279

申请日：2007-09-19

Applicant: Natalie Dales ,  Zaihui Zhang ,  Rajender Kamboj ,  Jianmin Fu ,  Shaoyi Sun ,  Natalia Pokrovskaia ,  Serguei Sviridov

Inventor： Natalie Dales ,  Zaihui Zhang ,  Rajender Kamboj ,  Jianmin Fu ,  Shaoyi Sun ,  Natalia Pokrovskaia ,  Serguei Sviridov

IPC: A61K31/426

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：US08153636B2

公开(公告)日：2012-04-10

申请号：US12552868

申请日：2009-09-02

Applicant: Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

Inventor： Melwyn Abreo ,  Daniel F. Harvey ,  Heinz W. Gschwend ,  Wenbao Li ,  Chi Tu ,  Rajender Kamboj ,  Michael D. Winther ,  Vishnumurthy Kodumuru ,  Cindy J. Hudson ,  Mikhail A. Kondratenko ,  Shifeng Liu ,  Vandna Raina ,  Serguei Sviridov ,  Zaihui Zhang ,  Mehran Seid Bagherzadeh ,  Shaoyi Sun

IPC: A61K31/497 ,  C07D401/00

CPC classification number: C07D213/71 ,  A61K31/00 ,  A61K31/501 ,  C07D213/75 ,  C07D213/76

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 x, y, W, V, 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x，y，W，V，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：US08063084B2

公开(公告)日：2011-11-22

申请号：US12377499

申请日：2007-08-13

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

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

IPC: A61K31/415 ,  C07D233/00

CPC classification number: C07D409/04 ,  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：US07919496B2

公开(公告)日：2011-04-05

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: A61K31/381 ,  C07D271/113 ,  C07D285/135 ,  A61K31/50 ,  A61K31/415 ,  C07D237/20 ,  C07D237/24 ,  C07D231/38 ,  C07D277/42

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，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。