公开(公告)号：US07919484B2

公开(公告)日：2011-04-05

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 ,  C07D211/34

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：US20100305138A1

公开(公告)日：2010-12-02

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: A61K31/496 ,  A61P3/10 ,  A61P3/04 ,  A61P17/10 ,  A61P3/00 ,  C07D401/04

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：US07547698B2

公开(公告)日：2009-06-16

申请号：US11575643

申请日：2005-09-20

Applicant: Rajender Kamboj ,  Jianmin Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

Inventor： Rajender Kamboj ,  Jianmin Fu ,  Vishnumurthy Kodumuru ,  Shifeng Liu ,  Kashinath Sadalapure ,  Nagasree Chakka ,  Duanjie Hou ,  Shaoyi Sun

IPC: A61K31/5025 ,  A61P3/04 ,  A61P3/10 ,  C07D487/04 ,  C07D403/04 ,  A61K31/437

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，R2，R3，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：US20090030008A1

公开(公告)日：2009-01-29

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: A61K31/496 ,  C07D403/04 ,  A61P3/04 ,  A61P3/10

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：US20080125434A1

公开(公告)日：2008-05-29

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: A61K31/501 ,  C07D403/14 ,  A61P3/10

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 SUP > 6，R 6a，R 7，R 7a，R 8和R SUP > 8a 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：US07335658B2

公开(公告)日：2008-02-26

申请号：US10901563

申请日：2004-07-29

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: C07D403/04 ,  C07D403/14 ,  A61K31/497

CPC classification number: A61K31/00 ,  A61K31/501 ,  A61K31/551 ,  C07D237/20 ,  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 (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 R 2，R 3，R 4，R 5，R 6，R 6，R 4， R 6a，R 7，R 7a，R 8，R 8a，R 8，R 7， 本文定义了9和9和9 9。 还公开了包含式（I）化合物的药物组合物。

公开(公告)号：US20080015230A1

公开(公告)日：2008-01-17

申请号：US11575638

申请日：2005-09-20

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

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

IPC: A61K31/44 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  C07D213/00 ,  C07D401/02

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, R4, 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，R 2，R 3，R 4，R 6，R 6a， R 7，R 7，R 8，R 8和R 8 8a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：US20130079354A1

公开(公告)日：2013-03-28

申请号：US13620151

申请日：2012-09-14

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: C07D401/14 ,  C07D401/04

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：US08318949B2

公开(公告)日：2012-11-27

申请号：US13238081

申请日：2011-09-21

Applicant: Sultan Chowdhury ,  Natalie Dales ,  Julia Fonarev ,  Jianmin Fu ,  Duanjie Hou ,  Qi Jia ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun ,  Zaihui Zhang

Inventor： Sultan Chowdhury ,  Natalie Dales ,  Julia Fonarev ,  Jianmin Fu ,  Duanjie Hou ,  Qi Jia ,  Vishnumurthy Kodumuru ,  Natalia Pokrovskaia ,  Shaoyi Sun ,  Zaihui Zhang

IPC: C07D417/12 ,  C07D277/20 ,  A01N43/54 ,  A61K31/4965 ,  A61K31/44 ,  A61K31/425

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：US20120004164A1

公开(公告)日：2012-01-05

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: A61K31/4439 ,  A61P3/00 ,  A61P3/10 ,  A61P5/48 ,  A61P3/08 ,  A61P3/04 ,  A61P3/06 ,  A61P9/12 ,  A61P7/00 ,  A61P19/06 ,  A61P7/02 ,  A61P17/00 ,  A61P17/10 ,  A61P17/06 ,  A61P17/02 ,  A61K38/28 ,  A61K38/26 ,  C07D417/14

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.