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1. 发明申请

US20060084702A1 (2S)-2-ethylphenylpropionic acid derivative 失效
标题翻译：（2S）-2-乙基苯基丙酸衍生物
公开(公告)号：US20060084702A1
公开(公告)日：2006-04-20
申请号：US10515176
申请日：2003-05-26
申请人： Jun Asano , Shigeki Isogai , Wataru Hori
发明人： Jun Asano , Shigeki Isogai , Wataru Hori
IPC分类号： A61K31/195 , C07C235/64
CPC分类号： C07D209/48 , C07C235/60 , C07D263/26
摘要： The invention provides novel (2S)-2-ethylphenylpropanoic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) α to activate and exhibit lipid-lowering effect, inhibitory effect on the arteriosclerosis, antiobesity effect, blood glucose-lowering effect, etc., their addition salts, and their medicinal compositions. (2S)-2-Ethylphenylpropanoic acid derivatives represented by a general formula (1) [wherein R1 denotes a halogen atom or trifluoromethyl group, R2 denotes a hydrogen atom, halogen atom or trifluoromethyl group, and, when R2 denotes a hydrogen atom, R3 denotes a halogen atom or trifluoromethyl group and, when R2 denotes a halogen atom or trifluoromethyl group, R3 denotes a hydrogen atom, halogen atom or trifluoromethyl group], and their addition salts.
摘要翻译：本发明提供了与受体作为人类过氧化物酶体增殖物激活受体（PPAR）α的配体结合的新型（2S）-2-乙基苯基丙酸衍生物，以激活并表现出降脂作用，对动脉硬化的抑制作用，抗肥胖作用，血液葡萄糖降低作用等，其加成盐及其药物组合物。（2S）-2-乙基苯基丙酸衍生物[其中R1表示卤素原子或三氟甲基，R2表示氢原子，卤素原子或三氟甲基，当R2表示氢原子时，R3 表示卤素原子或三氟甲基，当R 2表示卤素原子或三氟甲基时，R 3表示氢原子，卤素原子或三氟甲基]及其加成盐。

2. 发明授权

US07361783B2 (2S)-2-ethylphenylpropionic acid derivative 失效
标题翻译：（2S）-2-乙基苯基丙酸衍生物
公开(公告)号：US07361783B2
公开(公告)日：2008-04-22
申请号：US10515176
申请日：2003-05-26
申请人： Jun Asano , Shigeki Isogai , Wataru Hori
发明人： Jun Asano , Shigeki Isogai , Wataru Hori
IPC分类号： C07C409/44 , A01N37/12 , A01N25/00
CPC分类号： C07D209/48 , C07C235/60 , C07D263/26
摘要： The invention provides novel (2S)-2-ethylphenylpropanoic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor (PPAR) α to activate and exhibit lipid-lowering effect, inhibitory effect on the arteriosclerosis, antiobesity effect, blood glucose-lowering effect, etc., their addition salts, and their medicinal compositions.(2S)-2-Ethylphenylpropanoic acid derivatives represented by a general formula (1) [wherein R1 denotes a halogen atom or trifluoromethyl group, R2 denotes a hydrogen atom, halogen atom or trifluoromethyl group, and, when R2 denotes a hydrogen atom, R3 denotes a halogen atom or trifluoromethyl group and, when R2 denotes a halogen atom or trifluoromethyl group, R3 denotes a hydrogen atom, halogen atom or trifluoromethyl group], and their addition salts.
摘要翻译：本发明提供了与受体作为人类过氧化物酶体增殖物激活受体（PPAR）α的配体结合的新型（2S）-2-乙基苯基丙酸衍生物，以激活并表现出降脂作用，对动脉硬化的抑制作用，抗肥胖作用，血液葡萄糖降低作用等，其加成盐及其药物组合物。（2S）-2-乙基苯基丙酸衍生物[其中R1表示卤素原子或三氟甲基，R2表示氢原子，卤素原子或三氟甲基，当R2表示氢原子时，R3 表示卤素原子或三氟甲基，当R 2表示卤素原子或三氟甲基时，R 3表示氢原子，卤素原子或三氟甲基]及其加成盐。

3. 发明申请

US20090036489A1 Novel Cyclic Aminophenylalkanoic Acid Derivative 审中-公开
标题翻译：新型环状氨基苯基链烷酸衍生物
公开(公告)号：US20090036489A1
公开(公告)日：2009-02-05
申请号：US11886909
申请日：2006-03-22
申请人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Kyoko Okada , Takehiro Shinozaki , Shigeki Isogai
发明人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Kyoko Okada , Takehiro Shinozaki , Shigeki Isogai
IPC分类号： A61K31/4535 , C07D401/12 , A61P3/04 , A61P3/10
CPC分类号： C07D417/12 , C07D409/12
摘要： The present invention provides cyclic aminophenylalkanoic acid derivatives that act as agonists for human peroxisome proliferator-activated receptors (PPARs), in particular human PPARα isoform, and are effective in the treatment of abnormal lipid metabolism, diabetes and other disorders. The present invention also provides addition salts of such cyclic aminophenylalkanoic acid derivatives and pharmaceutical compositions containing these compounds.Specifically, the present invention provides cyclic aminophenylalkanoic acid derivatives represented by the following general formula (1): , or pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供了作为人类过氧化物酶体增殖物激活受体（PPAR），特别是人PPARα同种型的激动剂的环状氨基苯基链烷酸衍生物，并且有效治疗脂质代谢异常，糖尿病等疾病。本发明还提供了这种环状氨基苯基链烷酸衍生物的加成盐和含有这些化合物的药物组合物。具体地说，本发明提供由以下通式（1）表示的环状氨基苯基链烷酸衍生物或其药学上可接受的盐。

4. 发明申请

US20070249580A1 Novel Cyclic Amino Benzoic Acid Derivative 失效
标题翻译：新型环状氨基苯甲酸衍生物
公开(公告)号：US20070249580A1
公开(公告)日：2007-10-25
申请号：US11659854
申请日：2005-08-11
申请人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Takehiro Shinozaki , Shigeki Isogai , Koji Murakami
发明人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Takehiro Shinozaki , Shigeki Isogai , Koji Murakami
IPC分类号： A61K31/426 , A61K31/445 , A61K31/5375 , A61K31/55 , A61P3/10 , C07D211/36 , C07D223/00 , C07D277/02 , C07D413/00
CPC分类号： C07D417/12 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60
摘要： The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds. A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及作为人类过氧化物酶体增殖物激活受体（PPAR）激动剂的脂质代谢异常的治疗有效的环状氨基苯甲酸衍生物，特别是作为对人PPARα同种型的激动剂的添加其盐，以及含有这些化合物的药物组合物。由通式（1）表示的环状氨基苯甲酸衍生物[其中环Ar表示可具有取代基的芳基等; Y表示C 1 -C 4亚烷基，C 2 -C 4亚烯基，C 2 C 3 -C 4亚炔基等; Z表示氧原子，硫原子或 - （CH 2 CH 2）n - （n表示0,1或2）。 X表示氢原子，卤素原子，可被卤素原子取代的低级烷基等; R代表氢原子或低级烷基，-COOR代替环W的结合位置的邻位或甲基位置]或其药学上可接受的盐。

5. 发明授权

US07902367B2 Cyclic amino benzoic acid derivative 失效
标题翻译：环状氨基苯甲酸衍生物
公开(公告)号：US07902367B2
公开(公告)日：2011-03-08
申请号：US11659854
申请日：2005-08-11
申请人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Takehiro Shinozaki , Shigeki Isogai , Koji Murakami
发明人： Masahiro Nomura , Yasuo Takano , Kazuhiro Yumoto , Takehiro Shinozaki , Shigeki Isogai , Koji Murakami
IPC分类号： C07D401/00 , A01N43/40
CPC分类号： C07D417/12 , C07D211/22 , C07D211/26 , C07D211/42 , C07D211/56 , C07D211/60
摘要： The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds.A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及有效治疗脂质代谢异常的环状氨基苯甲酸衍生物，作为人类过氧化物酶体增殖物激活受体（PPAR）激动剂的糖尿病等，特别是作为对人PPARα同种型的激动剂的添加其盐，以及含有这些化合物的药物组合物。由通式（1）表示的环状氨基苯甲酸衍生物[其中环Ar表示可具有取代基的芳基等; Y表示C1-C4亚烷基，C2-C4亚链烯基，C2-C4亚炔基等; Z表示氧原子，硫原子或 - （CH 2）n - （n表示0,1或2）; X表示氢原子，卤素原子，可被卤素原子取代的低级烷基等; R代表氢原子或低级烷基，-COOR代替环W的结合位置的邻位或甲基位置]或其药学上可接受的盐。

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