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41.发明授权Piperazine derivatives as stearoyl-coa desaturase inhibitors and their use as therapeutic agents 有权哌嗪衍生物作为硬脂酰辅酶A去饱和酶抑制剂及其作为治疗剂的用途公开(公告)号：US08030488B2
公开(公告)日：2011-10-04
申请号：US12247792
申请日：2008-10-08
申请人： 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
发明人： 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分类号： C07D239/02
CPC分类号： A61K31/551 , A61K31/00 , A61K31/501 , C07D237/20 , C07D403/08 , C07D405/08 , C07D409/12 , C07D413/08
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20100233116A1
公开(公告)日：2010-09-16
申请号：US12377499
申请日：2007-08-13
申请人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
发明人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
IPC分类号： 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分类号： C07D409/04 , C07D417/04 , C07D417/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20060252767A1
公开(公告)日：2006-11-09
申请号：US10567009
申请日：2004-07-29
申请人： Serguei Sviridov , Vishnumurthy Kodumuru , Shifeng Liu , Melwyn Abreo , Michael Winther , Heins Gschwend , Rajender Kamboj , Shaoyi Sun , Mark Holladay , Wenbao Li , Chi Tu
发明人： Serguei Sviridov , Vishnumurthy Kodumuru , Shifeng Liu , Melwyn Abreo , Michael Winther , Heins Gschwend , Rajender Kamboj , Shaoyi Sun , Mark Holladay , Wenbao Li , Chi Tu
IPC分类号： A61K31/497 , C07D403/04
CPC分类号： A61K31/551 , A61K31/00 , A61K31/501 , C07D237/20 , C07D403/08 , C07D405/08 , C07D409/12 , C07D413/08
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US07456180B2
公开(公告)日：2008-11-25
申请号：US10567009
申请日：2004-07-29
申请人： 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
发明人： 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分类号： A61K31/497 , C07D241/02
CPC分类号： A61K31/551 , A61K31/00 , A61K31/501 , C07D237/20 , C07D403/08 , C07D405/08 , C07D409/12 , C07D413/08
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20120004164A1
公开(公告)日：2012-01-05
申请号：US13231075
申请日：2011-09-13
申请人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
发明人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
IPC分类号： 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分类号： C07D409/04 , C07D417/04 , C07D417/14
摘要： 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.
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公开(公告)号：US20060199802A1
公开(公告)日：2006-09-07
申请号：US10566193
申请日：2004-07-29
申请人： Melwyn Abreo , Daniel Harvey , Heins Gschwend , Wenbao Li , Chi Tu , Rajender Kamboj , Michael Winther , Vishnumurthy Kodumuru , Cindy Hudson , Mikhail Kondratenko , Shifeng Liu , Vandna Raina , Serguei Sviridov , Zaihui Zhang , Mehran Seid Bagherzadeh , Shaoyi Sun
发明人： Melwyn Abreo , Daniel Harvey , Heins Gschwend , Wenbao Li , Chi Tu , Rajender Kamboj , Michael Winther , Vishnumurthy Kodumuru , Cindy Hudson , Mikhail Kondratenko , Shifeng Liu , Vandna Raina , Serguei Sviridov , Zaihui Zhang , Mehran Seid Bagherzadeh , Shaoyi Sun
IPC分类号： A61K31/551 , A61K31/496
CPC分类号： C07D213/71 , A61K31/00 , A61K31/501 , C07D213/75 , C07D213/76
摘要： 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 (1): wherein: W is —O—, —N(R1)—, C(O), S(O)t ; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1) , C(O)N(R1) or N(R1)C(O)N(R1); and V is C(O), C(S), C(O)N(R1)—, C(O)O—, S(O)2—, S(O)2N(R1)— or C(R1)H; and 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.
摘要翻译： 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（1）化合物：其中：W是-O - ， - N （R 1） - ，C（O），S（O）t; （其中t为0,1或2），N（R1）S（O）2，S（O）2N（R1），C（O）N（R1）或N（R1）C（O） ）; 并且V是C（O），C（S），C（O）N（R 1） - ，C（O）O-，S（O）2 - ，S（O）2 N（R 1） - 或C ）H; 并且x，y，R1，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。
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公开(公告)号：US08293768B2
公开(公告)日：2012-10-23
申请号：US13231075
申请日：2011-09-13
申请人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
发明人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
IPC分类号： A61K31/425 , A61K31/433 , A61K31/4196 , C07D203/02 , C07D249/08 , C07D285/10
CPC分类号： C07D409/04 , C07D417/04 , C07D417/14
摘要： 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.
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公开(公告)号：US08153636B2
公开(公告)日：2012-04-10
申请号：US12552868
申请日：2009-09-02
申请人： Melwyn Abreo , Daniel F. Harvey , Heinz W. Gschwend , Wenbao Li , Chi Tu , Rajender Kamboj , Michael D. Winther , Vishnumurthy Kodumuru , Cindy J. Hudson , Mikhail A. Kondratenko , Shifeng Liu , Vandna Raina , Serguei Sviridov , Zaihui Zhang , Mehran Seid Bagherzadeh , Shaoyi Sun
发明人： Melwyn Abreo , Daniel F. Harvey , Heinz W. Gschwend , Wenbao Li , Chi Tu , Rajender Kamboj , Michael D. Winther , Vishnumurthy Kodumuru , Cindy J. Hudson , Mikhail A. Kondratenko , Shifeng Liu , Vandna Raina , Serguei Sviridov , Zaihui Zhang , Mehran Seid Bagherzadeh , Shaoyi Sun
IPC分类号： A61K31/497 , C07D401/00
CPC分类号： C07D213/71 , A61K31/00 , A61K31/501 , C07D213/75 , C07D213/76
摘要： 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 x, y, W, V, 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.
摘要翻译： 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 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。
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49.发明授权Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid levels 有权适用于治疗与脂质水平升高有关的疾病的杂环化合物公开(公告)号：US08063084B2
公开(公告)日：2011-11-22
申请号：US12377499
申请日：2007-08-13
申请人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
发明人： Natalie Dales , Julia Fonarev , Jianmin Fu , Rajender Kamboj , Vishnumurthy Kodumuru , Shifeng Liu , Natalia Pokrovskaia , Vandna Raina , Shaoyi Sun , Zaihui Zhang
IPC分类号： A61K31/415 , C07D233/00
CPC分类号： C07D409/04 , C07D417/04 , C07D417/14
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20090030008A1
公开(公告)日：2009-01-29
申请号：US12247792
申请日：2008-10-08
申请人： 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
发明人： 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分类号： A61K31/496 , C07D403/04 , A61P3/04 , A61P3/10
CPC分类号： A61K31/551 , A61K31/00 , A61K31/501 , C07D237/20 , C07D403/08 , C07D405/08 , C07D409/12 , C07D413/08
摘要： 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.
摘要翻译： 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。
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