公开(公告)号：US20060009459A1

公开(公告)日：2006-01-12

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

IPC: A61K31/501 ,  C07D403/02

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 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：US08258160B2

公开(公告)日：2012-09-04

申请号：US12520332

申请日：2007-12-19

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

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

IPC: A61K31/41 ,  A61K31/415 ,  C07D249/00 ,  C07D249/08 ,  C07D257/04

CPC classification number: C07D409/04 ,  C07D413/04 ,  C07D417/04

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：US08148378B2

公开(公告)日：2012-04-03

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 ,  A61P3/06 ,  A61P9/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00

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：US08026360B2

公开(公告)日：2011-09-27

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: C07D401/00

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：US07951805B2

公开(公告)日：2011-05-31

申请号：US11575639

申请日：2005-09-20

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

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

IPC: C07D401/04 ,  A61K31/501 ,  A61P9/00 ,  A61P3/10 ,  A61P3/04 ,  A61P3/00 ,  C07D213/26 ,  A61K31/45

CPC classification number: C07D213/82 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04

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): Formula (I) where x, y, G, J, L, M, V, W, R2, 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：式（I）其中x，y，G ，J，L，M，V，W，R2，R3，R4，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：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。