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11.发明授权Phosphonic acid biaryl derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) 失效作为蛋白酪氨酸磷酸酶1B（PTP-1B）的抑制剂的膦酸联芳衍生物公开(公告)号：US06486141B2
公开(公告)日：2002-11-26
申请号：US09745199
申请日：2000-12-21
申请人： Cheuk Kun Lau , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Chun Sing Li , Patrick Roy , Michel Therien , Zhaoyin Wang
发明人： Cheuk Kun Lau , Christopher Bayly , Jacques Yves Gauthier , Yves Leblanc , Chun Sing Li , Patrick Roy , Michel Therien , Zhaoyin Wang
IPC分类号： A61K31663
CPC分类号： C07F9/65583 , C07F9/65188
摘要： The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.
摘要翻译： 本发明包括作为PTP-1B酶抑制剂的由式I表示的新一类化合物。本发明还包括治疗或预防PTP-1B介导的疾病的药物组合物和方法，包括糖尿病，肥胖症和糖尿病相关病症 。
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公开(公告)号：US09896447B2
公开(公告)日：2018-02-20
申请号：US15023145
申请日：2014-09-17
申请人： MERCK SHARP & DOHME CORP. , Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
发明人： Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
IPC分类号： C07D471/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D239/42 , C07D213/16 , C07D261/14 , C07D231/40
CPC分类号： C07D471/04 , C07D213/16 , C07D231/40 , C07D239/42 , C07D261/14 , C07D401/12 , C07D401/14 , C07D403/12
摘要： The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
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公开(公告)号：US20160229804A1
公开(公告)日：2016-08-11
申请号：US15023634
申请日：2014-09-17
申请人： Andrew J. COOKE , Craig A. STUMP , Xu-Fang ZHANG , Chun Sing LI , Qinghua MAO , MERCK SHARP & DOHME CORP
发明人： Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Chun Sing Li , Qinghua Mao
IPC分类号： C07D213/75 , C07D405/12 , C07D239/42 , C07D498/04 , C07D231/40 , C07D261/14 , C07D471/04 , C07D233/88 , C07C275/28 , C07D257/04 , C07D249/08 , C07D295/135 , C07D401/04 , C07D487/04 , C07D271/10 , C07D285/12 , C07D405/04 , C07D263/32 , C07D403/04 , C07D277/48
CPC分类号： C07D213/75 , C07C275/28 , C07D231/40 , C07D233/88 , C07D239/42 , C07D249/08 , C07D257/04 , C07D261/14 , C07D263/32 , C07D271/10 , C07D277/44 , C07D277/48 , C07D285/12 , C07D295/135 , C07D311/88 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/12 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04
摘要： The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.
摘要翻译： 本发明涉及式（I）的苄基脲化合物，其是原肌球蛋白相关激酶（Trk）家族蛋白激酶抑制剂，因此可用于治疗疼痛，炎症，癌症，再狭窄，动脉粥样硬化，牛皮癣，血栓形成 与神经生长因子（NGF）受体Trk-A，Trk-B和/或Trk-C的异常活动相关的疾病，失调，损伤或与异常髓鞘或脱髓鞘相关的疾病或障碍。
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14.发明申请NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 有权新型螺旋体化合物作为硬脂酸苄酯的一种抑制剂公开(公告)号：US20110312952A1
公开(公告)日：2011-12-22
申请号：US13148985
申请日：2010-02-16
IPC分类号： A61K31/438 , C07D498/10 , A61P3/06 , C07D417/14 , A61P3/10 , A61K31/537 , C07D491/107
CPC分类号： A61K31/438 , C07D491/107
摘要： Heteroaromatic compounds of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译： 结构式（I）的杂芳族化合物是相对于其他已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。
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公开(公告)号：US20110230446A1
公开(公告)日：2011-09-22
申请号：US13115462
申请日：2011-05-25
申请人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Chirstophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
发明人： Christopher I. Bayly , Cameron Black , Serge Leger , Chun Sing Li , Dan McKay , Chirstophe Mellon , Jacques Yves Gauthier , Vouy-Linh Truong , Cheuk Lau , Michel Therien , Michael J. Green , Bernard L. Hirschbein , James William Janc , James T. Palmer , Chitra Baskaran
IPC分类号： A61K31/277 , A61K31/495 , A61K31/4418 , A61K31/426 , A61K31/4174 , A61K31/663 , A61P19/08 , A61P19/10 , A61P1/02 , A61P19/02 , A61P35/00 , A61P19/00
CPC分类号： C07C237/20 , A61K31/165 , A61K31/18 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4418 , A61K31/495 , C07C255/25 , C07C255/29 , C07C255/46 , C07C255/58 , C07C259/10 , C07C311/37 , C07C317/32 , C07C2601/02 , C07C2601/14 , C07D209/08 , C07D213/38 , C07D213/57 , C07D213/64 , C07D213/70 , C07D213/89 , C07D215/12 , C07D231/12 , C07D233/64 , C07D239/26 , C07D241/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/28 , C07D277/30 , C07D295/135 , C07D295/155 , C07D307/52 , C07D333/20 , C07D401/04 , C07D417/04
摘要： This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及一类新的化合物，它们是半胱氨酸蛋白酶抑制剂，包括但不限于组织蛋白酶K，L，S和B的抑制剂。这些化合物可用于治疗其中指示抑制骨吸收的疾病，例如 骨质疏松症
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16.发明申请HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开作为硬脂酸苄酯A DELTA-9去饱和酶抑制剂的异构化合物公开(公告)号：US20110166152A1
公开(公告)日：2011-07-07
申请号：US13119467
申请日：2009-09-30
IPC分类号： A61K31/4985 , C07D277/62 , C07D487/04 , C07D471/04 , A61K31/426 , A61K31/437 , A61P3/10 , A61P9/10
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D487/04 , C07D498/04 , C07D513/04
摘要： Heteroaromatic compounds of structural formula (I) are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; Type 2 diabetes; insulin resistance; hyperglycemia; Metabolic Syndrome; neurological disease; cancer; and liver steatosis.
摘要翻译： 结构式（I）的杂芳族化合物是硬脂酰辅酶A delta-9去饱和酶（SCD）的抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 2型糖尿病; 胰岛素抵抗; 高血糖症 代谢综合征; 神经系统疾病; 癌症; 和肝脂肪变性。
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17.发明申请HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开作为硬脂酸苄酯A DELTA-9去饱和酶抑制剂的异构化合物公开(公告)号：US20110152295A1
公开(公告)日：2011-06-23
申请号：US13060756
申请日：2009-09-02
IPC分类号： A61K31/506 , C07D277/30 , C07D401/14 , C07D257/04 , C07D271/06 , C07D417/14 , C07D261/06 , A61K31/4178 , A61K31/4439 , A61K31/41 , A61K31/4245 , A61K31/422 , A61P9/10
CPC分类号： A61K31/4192 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/506 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/14
摘要： Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
摘要翻译： 结构式I的杂芳族化合物是相对于其它已知的硬脂酰辅酶A去饱和酶的硬脂酰辅酶Aδ-9去饱和酶（SCD1）的选择性抑制剂。 本发明的化合物可用于预防和治疗与脂质合成和代谢异常有关的病症，包括心血管疾病，如动脉粥样硬化; 肥胖; 糖尿病; 神经系统疾病; 代谢综合征; 胰岛素抵抗; 和肝脂肪变性。
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公开(公告)号：US20100063013A1
公开(公告)日：2010-03-11
申请号：US12532652
申请日：2008-03-25
IPC分类号： A61K31/395 , C07D285/00 , A61K31/496 , A61P3/00 , A61P29/00 , A61K31/59 , A61K31/663
CPC分类号： C07D273/02 , C07D245/02 , C07D285/00
摘要： The present invention relates to novel compounds of the formula (I), wherein R′-R7, X, Y, D and n are as defined in the specification. These compounds are cysteine protease inhibitors which include but are not limited to inhibitors of cathepsms K, L, S and B and are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
摘要翻译： 本发明涉及式（I）的新化合物，其中R'-R7，X，Y，D和n如说明书中所定义。 这些化合物是半胱氨酸蛋白酶抑制剂，其包括但不限于组织蛋白酶K，L，S和B的抑制剂，并且可用于治疗其中指示骨吸收抑制的疾病，例如骨质疏松症。
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19.发明授权Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) 失效作为蛋白酪氨酸磷酸酶1B（PTP-1B）抑制剂的膦酸衍生物公开(公告)号：US06583126B2
公开(公告)日：2003-06-24
申请号：US09745222
申请日：2000-12-21
申请人： Yves Leblanc , Claude Dufresne , Scheigetz John , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michael Boyd , Zhaoyin Wang
发明人： Yves Leblanc , Claude Dufresne , Scheigetz John , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michael Boyd , Zhaoyin Wang
IPC分类号： C07F938
CPC分类号： C07F9/65318 , C07F9/3856 , C07F9/3869 , C07F9/3873 , C07F9/3882 , C07F9/4037 , C07F9/4056 , C07F9/4075 , C07F9/58 , C07F9/65188
摘要： The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
摘要翻译： 本发明包括作为PTP-1B酶抑制剂的由式I表示的新一类化合物。本发明还包括治疗或预防PTP-1B介导的疾病（包括糖尿病，肥胖症和糖尿病相关疾病）的药物组合物和方法 。
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20.发明授权Phosphonic acid derivatives as inhibitors of protein tyrosine phosphatase 1B (PTP-1B) 失效作为蛋白酪氨酸磷酸酶1B（PTP-1B）抑制剂的膦酸衍生物公开(公告)号：US06486142B2
公开(公告)日：2002-11-26
申请号：US09745211
申请日：2000-12-21
申请人： Yves Leblanc , Claude Dufresne , Jacques Yves Gauthier , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michel Therien , John Scheigetz , Zhaoyin Wang
发明人： Yves Leblanc , Claude Dufresne , Jacques Yves Gauthier , Cheuk Kun Lau , Chun Sing Li , Patrick Roy , Michel Therien , John Scheigetz , Zhaoyin Wang
IPC分类号： C07F938
CPC分类号： C07F9/6539 , C07F9/3882 , C07F9/4075 , C07F9/4087 , C07F9/65188 , C07F9/65318
摘要： The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.
摘要翻译： 本发明包括由式I表示的新型化合物，其是PTP-1B酶的抑制剂。本发明还包括治疗或预防PTP-1B介导的疾病的药物组合物和方法，包括糖尿病，肥胖症和与 糖尿病。
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