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1.发明公开NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 有权硬脂酰辅酶AΔ9去饱和酶的新螺环化合物作为抑制剂
公开(公告)号：EP2398809A1
公开(公告)日：2011-12-28
申请号：EP10743365.8
申请日：2010-02-16
申请人： Merck Canada Inc.
IPC分类号： C07D491/107 , A61K31/438 , A61P3/00 , C07D417/14
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.
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2.发明公开HETEROAROMATIC COMPOUNDS AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 审中-公开杂芳族化合物如硬脂酰 - 辅酶AΔ9去饱和酶的抑制剂
公开(公告)号：EP2334666A1
公开(公告)日：2011-06-22
申请号：EP09810959.8
申请日：2009-09-02
申请人： Merck Canada Inc.
IPC分类号： C07D401/14 , A61K31/4192 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/506 , A61P3/06 , C07D403/14 , C07D413/14 , C07D417/14
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.
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3.发明授权NOVEL SPIRO COMPOUNDS USEFUL AS INHIBITORS OF STEAROYL-COENZYME A DELTA-9 DESATURASE 有权硬脂酰辅酶AΔ9去饱和酶的新螺环化合物作为抑制剂
公开(公告)号：EP2398809B1
公开(公告)日：2015-07-08
申请号：EP10743365.8
申请日：2010-02-16
申请人： Merck Canada Inc.
IPC分类号： C07D491/107 , A61K31/438 , A61P3/00 , C07D417/14
CPC分类号： A61K31/438 , C07D491/107
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公开(公告)号：EP2552902B1
公开(公告)日：2015-03-11
申请号：EP11761856.1
申请日：2011-03-28
申请人： Merck Canada Inc.
发明人： BURCH, Jason , COTE, Bernard , NGUYEN, Natalie , LI, Chun, Sing , ST-ONGE, Miguel , GAUVREAU, Danny
IPC分类号： C07D401/06 , A61K31/4439 , A61P31/18
CPC分类号： C07D401/06 , A61K31/4439 , A61K45/06
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公开(公告)号：EP2552902A1
公开(公告)日：2013-02-06
申请号：EP11761856.1
申请日：2011-03-28
申请人： Merck Canada Inc.
发明人： BURCH, Jason , COTE, Bernard , NGUYEN, Natalie , LI, Chun, Sing , ST-ONGE, Miguel , GAUVREAU, Danny
IPC分类号： C07D401/06 , A61K31/4439 , A61P31/18
CPC分类号： C07D401/06 , A61K31/4439 , A61K45/06
摘要： Heteroaromatic compounds of Formula I: (I) are HIV reverse transcriptase inhibitors, wherein R
1 , R
2 , R
3 ; R
4 and R
5 are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.摘要翻译： 式I的杂芳族化合物：（I）是HIV逆转录酶抑制剂，其中R 1，R 2，R 3; R 4和R 5如本文所定义。 式I化合物及其药学上可接受的盐可用于抑制HIV逆转录酶，预防和治疗HIV感染以及预防，延缓AIDS的发作或进展以及治疗。 化合物及其盐可以用作药物组合物中的成分，任选地与其他抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。
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公开(公告)号：EP1817276B1
公开(公告)日：2012-08-08
申请号：EP05808098.7
申请日：2005-11-18
申请人： Merck Canada Inc.
IPC分类号： C07C255/46 , A61K31/275 , A61P19/10
CPC分类号： C07C255/46 , C07C2601/02
摘要： This invention relates to a novel class of compounds, diagrammed below, wherein R1, R2, R3, R4, R5, R6, R7, D and n are defined therein, which are cysteine protein 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 reportion is indicated, such as osteoporosis.
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