公开(公告)号：US08501746B2

公开(公告)日：2013-08-06

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: A61K31/4965 ,  A61K31/47 ,  A61K31/44

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.

公开(公告)号：US08071603B2

公开(公告)日：2011-12-06

申请号：US11575646

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Serguei Sviridov ,  Vandna Raina ,  Duanjie Hou ,  Vishnumurthy Kodumuru ,  Mehran Seid Bagherzadeh

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Serguei Sviridov ,  Vandna Raina ,  Duanjie Hou ,  Vishnumurthy Kodumuru ,  Mehran Seid Bagherzadeh

IPC: A61K31/495 ,  C07D295/192 ,  A61K31/496

CPC classification number: C07D295/192

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, J, K, W, V, 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，其中x，y，J，K，W， V，R3，R4，R5，R5a，R6，R6a，R7，R7a，R8和R8a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：US08030488B2

公开(公告)日：2011-10-04

申请号：US12247792

申请日：2008-10-08

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: C07D239/02

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，R2，R3，R4，R5，R6，R7，R8，R8a，R9，R9a，R10，R10a，R11和R11a。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20110009414A9

公开(公告)日：2011-01-13

申请号：US12436665

申请日：2009-05-06

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: A61K31/5025 ,  C07D487/02 ,  C12N9/99 ,  C07D403/02 ,  A61K31/496 ,  A61P9/00 ,  A61P3/00

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 (II): where x, y, A, D, E, T, Q, G, Z, 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 (II) 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（II）化合物：其中x，y，A ，D，E，T，Q，G，Z，J，K，L，M，W，V，R2，R3，R5，R5a，R6，R6a，R7，R7a，R8和R8a。 还公开了包含式（II）化合物的药物组合物。

公开(公告)号：US20100233116A1

公开(公告)日：2010-09-16

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: A61K31/427 ,  A61K31/785 ,  C12N9/99 ,  A61K38/28 ,  A61K31/616 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61K31/513 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/454 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/423 ,  A61K31/4196 ,  A61K31/4178 ,  A61K31/4184 ,  C07D417/04 ,  C07D409/04 ,  C07D417/14 ,  A61P17/00 ,  A61P17/10 ,  A61P17/06 ,  A61P17/02 ,  A61P3/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/06 ,  A61P9/12

CPC classification number: C07D409/04 ,  C07D417/04 ,  C07D417/14

Abstract: The present invention provides heterocyclic derivatives hat 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: 本发明提供了调节硬脂酰辅酶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：US07763618B2

公开(公告)日：2010-07-27

申请号：US10566857

申请日：2004-07-29

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 ,  C07D241/04 ,  C07D295/00

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：US07700641B2

公开(公告)日：2010-04-20

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 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: A61K31/407 ,  C07D491/107

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。

公开(公告)号：US20090197890A1

公开(公告)日：2009-08-06

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 ,  A61P3/10

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：US20090131447A1

公开(公告)日：2009-05-21

申请号：US11815739

申请日：2006-02-08

Applicant: Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

Inventor： Rajender Kamboj ,  Michael D. Winther ,  Robert Fraser ,  Mikhail Chafeev ,  Sultan Chowdhury ,  Jian-Min Fu ,  Duanjie Hou ,  Shifeng Liu ,  Vandna Raina ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Kashinath Sadalapure ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Nagasree Chakka ,  Zaihui Zhang ,  Melwyn Abreo ,  Mikhail A. Kondratenko ,  Daniel F. Harvey ,  Cindy J. Hudson ,  Wenbao Li ,  Chi Tu ,  Sengen Sun ,  Mark W. Holladay ,  Heinz W. Gschwend

IPC: A61K31/501 ,  A61K31/4436 ,  A61K31/496 ,  A61P3/04

CPC classification number: A61K31/64 ,  A61K31/00 ,  A61K31/4439 ,  A61K38/28 ,  A61K45/06 ,  A61K2300/00

Abstract: This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain.

Abstract translation: 本发明涉及式（I）的SCD-1抑制剂的用途：其中x，y，V，W，G，J，L，M，R2，R3，R5，R5a，R6，R6a，R7， 本文定义R7a，R8和R8a与其他药物治疗组合以治疗不利的体重增加。

公开(公告)号：US20090069408A1

公开(公告)日：2009-03-12

申请号：US12044731

申请日：2008-03-07

Applicant: Mikhail Chafeev ,  Nagasree Chakka ,  Jean-Jacques Cadieux ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Serguei Sviridov ,  Zaihui Zhang

Inventor： Mikhail Chafeev ,  Nagasree Chakka ,  Jean-Jacques Cadieux ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Jonathan Langille ,  Shifeng Liu ,  Jianyu Sun ,  Serguei Sviridov ,  Zaihui Zhang

IPC: A61K31/381 ,  C07D333/76 ,  A61K31/343 ,  C07D307/91 ,  C07C257/10 ,  A61K31/155

CPC classification number: C07D337/10 ,  C07C335/32 ,  C07C2603/08 ,  C07C2603/18 ,  C07C2603/24 ,  C07D219/02 ,  C07D307/91 ,  C07D311/82 ,  C07D327/08 ,  C07D333/50

Abstract: This invention is directed to, for example, compounds of formula (I): wherein n, m, R1, R2, R3, R4, R5, R6, R7 and R8 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 of iron disorders. This invention is also directed to pharmaceutical compositions comprising the compounds and methods of using the compounds to treat iron disorders.

Abstract translation: 本发明涉及例如式（I）的化合物：其中n，m，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8如本文所定义，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，用于治疗铁疾病。 本发明还涉及包含该化合物的药物组合物和使用该化合物治疗铁疾病的方法。