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11.发明授权Heterocyclic derivatives and their use as mediators of stearoyl-CoA desaturase 失效杂环衍生物及其作为硬脂酰CoA去饱和酶介体的用途公开(公告)号：US07951805B2
公开(公告)日：2011-05-31
申请号：US11575639
申请日：2005-09-20
申请人： 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
发明人： 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分类号： C07D401/04 , A61K31/501 , A61P9/00 , A61P3/10 , A61P3/04 , A61P3/00 , C07D213/26 , A61K31/45
CPC分类号： C07D213/82 , C07D401/04 , C07D401/14 , C07D403/04
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): 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.
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：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。
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12.发明授权Pyridazine-piperazine compounds and their use as stearoyl-CoA desaturase inhibitors 失效哒嗪 - 哌嗪化合物及其作为硬脂酰辅酶A去饱和酶抑制剂的用途公开(公告)号：US07592343B2
公开(公告)日：2009-09-22
申请号：US11575641
申请日：2005-09-20
申请人： Rajender Kamboj , Zaihui Zhang , Jianmin Fu , Vandna Raina , Serguei Sviridov , Vishnumurthy Kodumuru , Nagasree Chakka , Shifeng Liu , Shaoyi Sun , Duanjie Hou
发明人： Rajender Kamboj , Zaihui Zhang , Jianmin Fu , Vandna Raina , Serguei Sviridov , Vishnumurthy Kodumuru , Nagasree Chakka , Shifeng Liu , Shaoyi Sun , Duanjie Hou
IPC分类号： A61K31/50
CPC分类号： A61K31/501 , C07D237/24 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20100173967A1
公开(公告)日：2010-07-08
申请号：US12445264
申请日：2007-10-12
申请人： Mikhail Chafeev , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Rajender Kamboj , Duanjie Hou , Shifeng Liu , Mehran Seid Bagherzadeh , Serguei Sviridov , Shaoyi Sun , Jianyu Sun , Nagasree Chakka , Tom Hsieh , Vandna Raina
发明人： Mikhail Chafeev , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Rajender Kamboj , Duanjie Hou , Shifeng Liu , Mehran Seid Bagherzadeh , Serguei Sviridov , Shaoyi Sun , Jianyu Sun , Nagasree Chakka , Tom Hsieh , Vandna Raina
IPC分类号： A61K31/404 , A61P9/10 , A61P17/04 , A61P35/00
CPC分类号： A61K31/407 , A61K31/437
摘要： This invention is directed to methods of using 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, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.
摘要翻译： 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 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，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。
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14.发明申请Heterocyclic Derivatives and Their Use as Strearoyl-Coa Desaturase Inhibitors 失效杂环衍生物及其作为Strearoyl-Coa去饱和酶抑制剂的用途公开(公告)号：US20080125434A1
公开(公告)日：2008-05-29
申请号：US11575641
申请日：2005-09-20
申请人： Rajender Kamboj , Zaihui Zhang , Jianmin Fu , Vandna Raina , Serguei Sviridov , Vishnumurthy Kodumuru , Nagasree Chakka , Shifeng Liu , Shaoyi Sun , Duanjie Hou
发明人： Rajender Kamboj , Zaihui Zhang , Jianmin Fu , Vandna Raina , Serguei Sviridov , Vishnumurthy Kodumuru , Nagasree Chakka , Shifeng Liu , Shaoyi Sun , Duanjie Hou
IPC分类号： A61K31/501 , C07D403/14 , A61P3/10
CPC分类号： A61K31/501 , C07D237/24 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
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 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.
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，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。
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公开(公告)号：US07700641B2
公开(公告)日：2010-04-20
申请号：US11402310
申请日：2006-04-11
申请人： 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
发明人： 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分类号： A61K31/407 , C07D491/107
CPC分类号： C07D491/10
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20100125072A1
公开(公告)日：2010-05-20
申请号：US12650196
申请日：2009-12-30
申请人： 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
发明人： 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分类号： A61K31/5377 , C07D491/10 , A61K31/407 , A61K31/4439 , A61K31/506
CPC分类号： C07D491/10
摘要： 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.
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公开(公告)号：US20060252812A1
公开(公告)日：2006-11-09
申请号：US11402310
申请日：2006-04-11
申请人： Mikhail Chafeev , Nagasree Chakka , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Duanjie Hou , Tom Hsieh , Rajender Kamboj , Shifeng Liu , Vandna Raina , Mehran Bagherzadeh , Jianyu Sun , Shaoyi Sun , Serguei Sviridov
发明人： Mikhail Chafeev , Nagasree Chakka , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Duanjie Hou , Tom Hsieh , Rajender Kamboj , Shifeng Liu , Vandna Raina , Mehran Bagherzadeh , Jianyu Sun , Shaoyi Sun , Serguei Sviridov
IPC分类号： A61K31/407 , C07D491/10
CPC分类号： C07D491/10
摘要： 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.
摘要翻译： 本发明涉及式（I）的螺 - 羟吲哚化合物：其中k，j，Q，R 1，R 2a，R 2b， >，R 2c，R 2d，R 3a，R 3b，R 3c， >和R“>如本文所定义，作为其立体异构体，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，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。
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公开(公告)号：US08466188B2
公开(公告)日：2013-06-18
申请号：US12445264
申请日：2007-10-12
申请人： Mikhail Chafeev , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Rajender Kamboj , Duanjie Hou , Shifeng Liu , Mehran Seid Bagherzadeh , Serguei Sviridov , Shaoyi Sun , Jianyu Sun , Nagasree Chakka , Tom Hsieh , Vandna Raina
发明人： Mikhail Chafeev , Sultan Chowdhury , Robert Fraser , Jianmin Fu , Rajender Kamboj , Duanjie Hou , Shifeng Liu , Mehran Seid Bagherzadeh , Serguei Sviridov , Shaoyi Sun , Jianyu Sun , Nagasree Chakka , Tom Hsieh , Vandna Raina
IPC分类号： A61K31/40 , A61K31/5377
CPC分类号： A61K31/407 , A61K31/437
摘要： This invention is directed to methods of using 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, for the treatment and/or prevention of hypercholesterolemia, benign prostatic hyperplasia, pruritis and cancer.
摘要翻译： 本发明涉及使用式（I）的螺 - 羟吲哚化合物的方法：其中k，j，Q，R1，R2a，R2b，R2c，R2d，R3a，R3b，R3c和R3d如本文所定义， 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，用于治疗和/或预防高胆固醇血症，良性前列腺增生，瘙痒症和癌症。
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公开(公告)号：US20070105820A1
公开(公告)日：2007-05-10
申请号：US11408269
申请日：2006-04-20
申请人： 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
发明人： 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分类号： A61K31/404 , A61K31/675 , C07D403/02 , C07F9/572
CPC分类号： C07D409/06 , C07D209/34 , C07D209/38 , C07D209/40 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/04 , C07D417/04
摘要： This invention is directed to oxindole compounds that 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 using the compounds are also disclosed.
摘要翻译： 本发明涉及可用于治疗和/或预防钠通道介导的疾病或病症（例如疼痛）的羟吲哚化合物。 还公开了包含该化合物的药物组合物和使用该化合物的方法。
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公开(公告)号：US08106087B2
公开(公告)日：2012-01-31
申请号：US12650196
申请日：2009-12-30
申请人： 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
发明人： 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分类号： A61K31/407 , A61K31/5377
CPC分类号： C07D491/10
摘要： 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.
摘要翻译： 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。
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