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。

公开(公告)号：US20060252767A1

公开(公告)日：2006-11-09

申请号：US10567009

申请日：2004-07-29

Applicant: Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael Winther ,  Heins Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark Holladay ,  Wenbao Li ,  Chi Tu

Inventor： Serguei Sviridov ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Melwyn Abreo ,  Michael Winther ,  Heins Gschwend ,  Rajender Kamboj ,  Shaoyi Sun ,  Mark Holladay ,  Wenbao Li ,  Chi Tu

IPC: A61K31/497 ,  C07D403/04

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 11a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：US20160289191A1

公开(公告)日：2016-10-06

申请号：US14879583

申请日：2015-10-09

Applicant: Natalie Dales ,  Zaihui Zhang ,  Jianmin Fu ,  Duanjie Hou ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia

Inventor： Natalie Dales ,  Zaihui Zhang ,  Jianmin Fu ,  Duanjie Hou ,  Shaoyi Sun ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia

IPC: C07D213/81 ,  C07D401/04 ,  C07D409/12 ,  C07D401/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D405/12 ,  C07D213/89

CPC classification number: C07D213/81 ,  A61K31/4439 ,  A61K31/444 ,  C07D213/89 ,  C07D401/04 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/04 ,  C07D413/14 ,  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：US08541457B2

公开(公告)日：2013-09-24

申请号：US11916243

申请日：2006-06-05

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: A01N43/78 ,  A61K31/425

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: 公开了治疗哺乳动物，优选人类的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：US08383628B2

公开(公告)日：2013-02-26

申请号：US12816076

申请日：2010-06-15

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 ,  C07D401/00

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：US20100240713A1

公开(公告)日：2010-09-23

申请号：US12663104

申请日：2008-06-05

Applicant: Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Serguei Sviridov ,  Zaihui Zhang

Inventor： Jean-Jacques Cadieux ,  Mikhail Chafeev ,  Julia Fonarev ,  Jianmin Fu ,  Rajender Kamboj ,  Vishnumurthy Kodumuru ,  Serguei Sviridov ,  Zaihui Zhang

IPC: A61K31/44 ,  C07C211/50 ,  C07C261/04 ,  C07C22/04 ,  C07C33/26 ,  C07D333/12 ,  C07D333/16 ,  C07D495/02 ,  C07D249/14 ,  C07D213/53 ,  A61K31/135 ,  A61K31/165 ,  A61K31/03 ,  A61K31/047 ,  A61K31/381 ,  A61K31/4196 ,  A61P43/00

CPC classification number: A61K31/155 ,  A61K31/275 ,  A61K31/381 ,  A61K31/4196 ,  A61K31/44 ,  Y02A50/411

Abstract: This invention is directed to compounds of formula (I), wherein m, formula (II), 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, 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: 本发明涉及式（I）化合物，其中m，式（II），R 1，R 2和R 3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。

公开(公告)号：US07777036B2

公开(公告)日：2010-08-17

申请号：US11575638

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

Inventor： Rajender Kamboj ,  Zaihui Zhang ,  Jianmin Fu ,  Mehran Seid Bagherzadeh ,  Serguei Sviridov ,  Sultan Chowdhury ,  Shifeng Liu ,  Vishnumurthy Kodumuru

IPC: C07D419/00 ,  C07D413/00 ,  C07D405/00 ,  C07D277/00

CPC classification number: C07D213/82

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 y, G, K, L, M, W, V, R2, R3, R4a, 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y，G，K，L，M， W，V，R2，R3，R4a，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：US07754711B2

公开(公告)日：2010-07-13

申请号：US11055034

申请日：2005-02-09

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 D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. 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 D. Winther ,  Zaihui Zhang ,  Melwyn Abreo ,  Mark W. Holladay ,  Wenbao Li ,  Sengen Sun ,  Chi Tu ,  Heinz W. Gschwend

IPC: A61K31/551 ,  A61K31/5513 ,  A61K31/50 ,  A61K31/502 ,  A61K31/501 ,  C07D245/02 ,  C07D243/04 ,  C07D243/08 ,  C07D403/04 ,  C07D401/14 ,  C07D403/14 ,  A61P7/12

CPC classification number: C07D237/20 ,  A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/22 ,  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 (Ia): 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: 公开了治疗哺乳动物，优选人类的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（Ia）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：US20100152187A1

公开(公告)日：2010-06-17

申请号：US11916243

申请日：2006-06-05

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: A61K31/5377 ,  C12N9/99 ,  A61K31/4439 ,  A61K31/426 ,  A61P3/10 ,  A61P3/04 ,  A61P9/10

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: 公开了治疗哺乳动物，优选人类的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。