公开(公告)号：US20090306090A1

公开(公告)日：2009-12-10

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: A61K31/501 ,  C12N9/99 ,  C07D403/04

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：US07592343B2

公开(公告)日：2009-09-22

申请号：US11575641

申请日：2005-09-20

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

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

IPC: A61K31/50

CPC classification number: A61K31/501 ,  C07D237/24 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

Abstract: Compounds of formula (Ia): where x, y, G, L, M, W, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, are disclosed, as well as pharmaceutical compositions comprising the compounds. These compounds and pharmaceutical compositions are useful in treating SCD-mediated diseases or conditions.

Abstract translation: 式（Ia）化合物：其中x，y，G，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， 包含该化合物的组合物。 这些化合物和药物组合物可用于治疗SCD介导的疾病或病症。

公开(公告)号：US20090156615A1

公开(公告)日：2009-06-18

申请号：US12303490

申请日：2007-06-04

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

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

IPC: A61K31/497 ,  C07D401/14 ,  A61K31/444 ,  C07D415/00 ,  A61K31/4439 ,  A61K31/4709

CPC classification number: A61K31/4436 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/497 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/04 ,  C07D417/14 ,  C07F7/0834

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：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：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：US20070166711A1

公开(公告)日：2007-07-19

申请号：US10552158

申请日：2004-04-08

Applicant: Mark Samuels ,  Erwin Ludwig ,  Marcia MacDonald ,  Patrick Franchini ,  Yigal Goldberg ,  Rajender Kamboj ,  George Papanikolaou

Inventor： Mark Samuels ,  Erwin Ludwig ,  Marcia MacDonald ,  Patrick Franchini ,  Yigal Goldberg ,  Rajender Kamboj ,  George Papanikolaou

IPC: A61K48/00 ,  A61K38/40 ,  C12Q1/68 ,  G01N33/567 ,  A61K39/395 ,  C12N5/08

CPC classification number: G01N33/5023 ,  A61K38/40 ,  A61K48/00 ,  C07K14/47 ,  C12Q1/6883 ,  C12Q1/6897 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/5008 ,  G01N33/5091 ,  G01N2500/10 ,  Y10T436/143333

Abstract: Polynucleotide and polypeptide sequences for HFE2A, as well as mutations associated with juvenile hemochromatosis, and methods of utilizing these for the screening and identification of agents for the treatment of diseases of iron metabolism, including small organic compounds, are disclosed along with methods of treating and/or ameliorating diseases of iron metabolism, especially in human patients are disclosed. Diagnostic compounds, kits and methods using HFE2A are also described.

Abstract translation: HFE2A的多核苷酸和多肽序列以及与幼年血色素沉着相关的突变，以及利用它们用于筛选和鉴定用于治疗铁代谢疾病（包括小有机化合物）的药剂的方法，以及治疗和 /或改善铁代谢疾病，特别是在人类患者中。 还描述了使用HFE2A的诊断化合物，试剂盒和方法。