-
公开(公告)号：US20090292125A1
公开(公告)日：2009-11-26
申请号：US12295618
申请日：2007-03-29
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
IPC分类号： C07D215/38
CPC分类号： C07D215/42 , C07D215/233
摘要： The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
摘要翻译： 本发明提供一种可用于治疗和/或预防动脉硬化疾病，血脂异常等疾病的光学活性四氢喹啉衍生物的方法及其合成中间体的制备方法。 具体地说，（2R，4S）-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐在不使用光学拆分的情况下以较少的步骤制备，并且光学活性的四氢喹啉衍生物 由胺化合物得到。
-
公开(公告)号：US08084611B2
公开(公告)日：2011-12-27
申请号：US12295618
申请日：2007-03-29
申请人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
发明人： Masaki Okamoto , Akira Sakuragi , Yoshikazu Mori , Takeshi Hamada , Hitoshi Kubota , Yoshinori Nakamura , Takanori Higashijima , Norimitsu Hayashi
IPC分类号： C07D215/38
CPC分类号： C07D215/42 , C07D215/233
摘要： The present invention is to provide a process for preparing optically active tetrahydroquinoline derivatives which can be used for the treatment and/or prevention of diseases such as arteriosclerotic diseases, dyslipidemia and the like, and a process for preparing synthetic intermediates thereof.Specifically, (2R,4S)-2-ethyl-6-trifluoromethyl-1,2,3,4-tetrahydroquinolin-4-ylamine or a salt thereof is prepared with fewer steps without using an optical resolution, and the optically active tetrahydroquinoline derivatives are obtained from the amine compound.
摘要翻译： 本发明提供一种可用于治疗和/或预防动脉硬化疾病，血脂异常等疾病的光学活性四氢喹啉衍生物的方法及其合成中间体的制备方法。 具体地说，（2R，4S）-2-乙基-6-三氟甲基-1,2,3,4-四氢喹啉-4-基胺或其盐在不使用光学拆分的情况下以较少的步骤制备，并且光学活性的四氢喹啉衍生物 由胺化合物得到。
-
公开(公告)号：US20090029994A1
公开(公告)日：2009-01-29
申请号：US12219775
申请日：2008-07-28
IPC分类号： A61K31/506 , A61P9/10 , A61P9/00 , A61P29/00 , A61P19/00 , A61P37/00 , C07D401/04 , C07D239/47 , C07D413/04 , A61K31/4412 , A61K31/444 , C07D413/14 , C07D401/12 , C07D239/48 , C07D403/12 , C07D213/72 , A61K31/5377 , A61K31/496
CPC分类号： C07D239/47 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D257/06 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
摘要翻译： 本发明涉及通式（1）的化合物：其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的苯基等; R1是任选取代的烷基等; 并且R 2是任选取代的氨基等; 或其药学上可接受的衍生物，其对胆固醇酯转移蛋白（CETP）具有抑制活性，因此可用于预防和/或治疗动脉硬化性疾病，高脂血症或血脂异常等。
-
公开(公告)号：US08076364B2
公开(公告)日：2011-12-13
申请号：US12973403
申请日：2010-12-20
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D239/47 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D257/06 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
摘要翻译： 本发明涉及通式（1）的化合物：其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的苯基等; R1是任选取代的烷基等; 并且R 2是任选取代的氨基等; 或其药学上可接受的衍生物，其对胆固醇酯转移蛋白（CETP）具有抑制活性，因此可用于预防和/或治疗动脉硬化性疾病，高脂血症或血脂异常等。
-
公开(公告)号：US07906517B2
公开(公告)日：2011-03-15
申请号：US12219775
申请日：2008-07-28
IPC分类号： A61K31/44 , C07D213/02
CPC分类号： C07D239/47 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D257/06 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
-
公开(公告)号：US20090023729A1
公开(公告)日：2009-01-22
申请号：US12219776
申请日：2008-07-28
IPC分类号： A61K31/506 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , A61K31/4155 , A61P9/10 , A61K31/4439 , C07D239/47 , C07D239/48 , A61K31/5377
CPC分类号： C07D401/12
摘要： The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted heterocyclic group, and the like; R1 is an optionally substituted alkyl group, wherein the alkyl group further may optionally be substituted by an optionally substituted homocyclic group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
摘要翻译： 本发明涉及通式（1）的化合物：其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的杂环基等; R1是任选取代的烷基，其中烷基进一步可以任选地被任选取代的杂环基取代，等等; 并且R 2是任选取代的氨基等; 或其药学上可接受的衍生物，其具有对胆固醇酯转移蛋白（CETP）的抑制活性，从而可用于预防和/或治疗动脉硬化性疾病，高脂血症或血脂异常等。
-
公开(公告)号：US20110092506A1
公开(公告)日：2011-04-21
申请号：US12973403
申请日：2010-12-20
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/505 , A61K31/498 , A61K31/41 , A61K31/44 , A61P9/10 , A61P9/00 , A61P3/10 , A61P3/00 , A61P9/12 , A61P3/04 , A61P7/02 , A61P25/00 , A61P9/06 , A61P11/00 , A61P13/12 , A61P1/16 , A61P29/00 , A61P37/02 , A61P15/00 , A61P35/00 , A61P25/28
CPC分类号： C07D239/47 , C07D239/42 , C07D239/48 , C07D239/52 , C07D239/56 , C07D257/06 , C07D401/04 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The present invention relates to a compound of the general formula (1): wherein, Y is a methylene group, and the like; A is an optionally substituted heterocyclic group, and the like; B is an optionally substituted phenyl group, and the like; R1 is an optionally substituted alkyl group, and the like; and R2 is an optionally substituted amino group, and the like; or a pharmaceutically acceptable derivative thereof, which has an inhibitory activity against cholesteryl ester transfer protein (CETP), thereby being useful for prophylaxis and/or treatment of arteriosclerotic diseases, hyperlipemia or dyslipidemia, and the like.
摘要翻译： 本发明涉及通式（1）的化合物：其中Y为亚甲基等; A是任选取代的杂环基等; B是任选取代的苯基等; R1是任选取代的烷基等; 并且R 2是任选取代的氨基等; 或其药学上可接受的衍生物，其具有对胆固醇酯转移蛋白（CETP）的抑制活性，从而可用于预防和/或治疗动脉硬化性疾病，高脂血症或血脂异常等。
-
公开(公告)号：US09302996B2
公开(公告)日：2016-04-05
申请号：US13994543
申请日：2011-12-16
申请人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
发明人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
IPC分类号： A61K31/44 , C07D211/72 , C07D233/64 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
CPC分类号： C07D401/04 , C07D233/64 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
摘要： This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译： 这是提供具有DGAT1抑制活性的连续的芳环化合物，并且可用于预防和/或治疗由肥胖，高甘油三酯血症，脂质代谢障碍，脂肪肝，高血压，动脉硬化，糖尿病等引起的肥胖症或高脂血症，以及 以提供包含连续的芳环化合物或其药学上可接受的盐作为有效成分的DGAT1抑制剂。 公开了连续的芳环化合物由下式表示：其中式中的取代基与说明书中所定义的相同，或其药学上可接受的盐。
-
公开(公告)号：US20130261128A1
公开(公告)日：2013-10-03
申请号：US13994543
申请日：2011-12-16
申请人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
发明人： Osamu Sakurai , Kunio Saruta , Norimitsu Hayashi , Takashi Goi , Kenji Morokuma , Hidekazu Tsujishima , Hiroaki Sawamoto , Hiroaki Shitama , Ritsuo Imashiro
IPC分类号： C07D233/64 , C07D401/10 , C07D403/10 , C07D401/14 , C07D405/14 , C07D401/04 , C07D403/04
CPC分类号： C07D401/04 , C07D233/64 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/14
摘要： This is to provide a continuous arycyclic compound having a DGAT1 inhibitory activity, and useful for prophylaxis and/or treatment of obesity or hyperlipidemia caused by obesity, hypertriglyceridemia, lipid metabolism disorder, fatty liver, hypertension, arteriosclerosis, diabetes, etc., as well as to provide a DGAT1 inhibitor comprising the continuous arycyclic compound or a pharmaceutically acceptable salt thereof as an effective ingredient. Disclosed is the continuous arycyclic compound is represented by the formula: wherein the substituents in the formula are the same as defined in the specification, or a pharmaceutically acceptable salt thereof.
摘要翻译： 这是提供具有DGAT1抑制活性的连续的芳环化合物，并且可用于预防和/或治疗由肥胖，高甘油三酯血症，脂质代谢障碍，脂肪肝，高血压，动脉硬化，糖尿病等引起的肥胖症或高脂血症，以及 以提供包含连续的芳环化合物或其药学上可接受的盐作为有效成分的DGAT1抑制剂。 公开了连续的芳环化合物由下式表示：其中式中的取代基与说明书中所定义的相同，或其药学上可接受的盐。
-
-
-
-
-
-
-
-
搜索结果
9 条记录 (耗时 0.045 秒)