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1. 发明授权

US06506797B1 Substituted phenylpropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor (PPAR) &agr; 失效
标题翻译：取代的苯丙酸衍生物作为人类过氧化物酶体增殖物激活受体（PPAR）α的激动剂
公开(公告)号：US06506797B1
公开(公告)日：2003-01-14
申请号：US10009175
申请日：2001-12-10
申请人： Masahiro Nomura , Yukie Takahashi , Takahiro Tanase , Hiroyuki Miyachi , Masaki Tsunoda , Tomohiro Ide , Koji Murakami
发明人： Masahiro Nomura , Yukie Takahashi , Takahiro Tanase , Hiroyuki Miyachi , Masaki Tsunoda , Tomohiro Ide , Koji Murakami
IPC分类号： A01N3712
CPC分类号： C07D263/26 , A61K31/195 , C07C235/60 , C07C323/60
摘要： The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor &agr; (PPAR&agr;), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride). It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.
摘要翻译：本发明提供新的取代苯丙酸衍生物，其通过与作为人过氧化物酶体增生物激活受体α（PPARα）的配体的受体结合而活化，并且对血液中的脂质（胆固醇和甘油三酸酯）表现出有效的降低作用。涉及取代的苯丙酸由通式（1）表示的衍生物，其药学上可接受的盐及其水合物及其制备方法。

2. 发明授权

US06730687B1 Substituted benzylthiazolidine-2, 4-dione derivatives 失效
标题翻译：取代的苄基噻唑烷-2,4-二酮衍生物
公开(公告)号：US06730687B1
公开(公告)日：2004-05-04
申请号：US10049645
申请日：2002-02-25
申请人： Hiroyuki Miyachi , Masahiro Nomura , Takahiro Tanase , Koji Murakami , Masaki Tsunoda
发明人： Hiroyuki Miyachi , Masahiro Nomura , Takahiro Tanase , Koji Murakami , Masaki Tsunoda
IPC分类号： A61K31426
CPC分类号： C07D277/34
摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives that bind to receptor to activate as ligands of human peroxisome proliferator-activated receptor (PPAR) and exhibit blood glucose-decreasing action and lipid-decreasing action, and processes for preparing them. It relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein the bond mode of A denotes —CH2CONH—, —NHCONH—, —CH2CH2CO— or —NHCOCH2—, and B denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, halogen atom, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and processes for preparing them.
摘要翻译：本发明提供了新的取代的苄基噻唑烷-2,4-二酮衍生物，其结合受体以作为人类过氧化物酶体增殖物激活受体（PPAR）的配体活化并显示出血糖降低作用和降脂作用，以及制备它们的方法。它涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A的键合模式表示-CH 2 CONH-，-NHCONH-，-CH 2 CH 2 CO-或-NHCOCH 2 - ，B表示低级烷基具有1至4个碳原子的烷基，具有1至3个碳原子的低级烷氧基，卤素原子，三氟甲基，三氟甲氧基，未取代或可具有取代基的苯基，未被取代或可具有取代基的苯氧基或可具有取代基的苯氧基未取代或可具有取代基的基团]，它们的药学上可接受的盐，它们的水合物及其制备方法。

3. 发明授权

US06734199B1 Substituted benzylthiazolidine-2, 4-dione derivatives 失效
标题翻译：取代的苄基噻唑烷-2,4-二酮衍生物
公开(公告)号：US06734199B1
公开(公告)日：2004-05-11
申请号：US10049904
申请日：2002-02-20
申请人： Hiroyuki Miyachi , Masahiro Nomura , Takahiro Tanase , Koji Murakami , Masaki Tsunoda
发明人： Hiroyuki Miyachi , Masahiro Nomura , Takahiro Tanase , Koji Murakami , Masaki Tsunoda
IPC分类号： A61K31426
CPC分类号： C07D277/34
摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation action of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents], their medicinally acceptable salts, their hydrates and a process for preparing them.
摘要翻译：本发明提供新的取代的苄基噻唑烷-2,4-二酮衍生物，其增加受体作为人过氧化物酶体增殖物激活受体（PPAR）的配体的反式激活作用，并显示出降血糖作用和降脂作用，本发明涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A表示未取代或可具有取代基的苯基，未取代或可具有取代基的苯氧基或未取代或可具有取代基的苄氧基，其药学上可接受的盐，它们的水合物及其制备方法。

4. 发明授权

US07049342B2 Substituted phenylpropionic acid derivatives 失效
标题翻译：取代苯基丙酸衍生物
公开(公告)号：US07049342B2
公开(公告)日：2006-05-23
申请号：US10296206
申请日：2001-05-25
申请人： Hiroyuki Miyachi , Masahiro Nomura , Yukie Takahashi , Takahiro Tanase , Kouji Murakami , Masahiro Suzuki
发明人： Hiroyuki Miyachi , Masahiro Nomura , Yukie Takahashi , Takahiro Tanase , Kouji Murakami , Masahiro Suzuki
IPC分类号： A61K31/195 , C07C235/52
CPC分类号： C07C229/34 , C07B2200/07 , C07C69/734 , C07C69/738 , C07C233/55 , C07C235/38
摘要： The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor α (PPARα) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.It relates to substituted phenylpropionic acid derivatives represented by a general formula (1) [wherein R1 denotes a lower alkyl group with carbon atoms of 1 to 4, lower alkoxy group with carbon atoms of 1 to 3, trifluoromethyl group, trifluoromethoxy group, phenyl group which is unsubstituted or may have substituents, phenoxy group which is unsubstituted or may have substituents or benzyloxy group which is unsubstituted or may have substituents, R2 denotes a hydrogen atom, lower alkyl group with carbon atoms of 1 to 4 or lower alkoxy group with carbon atoms of 1 to 3, R3 denotes a lower alkoxy group with carbon atoms of 1 to 3, and the binding mode of A portion denotes —CH2CONH—, —NHCOCH2—, —CH2CH2CO—, —CH2CH2CH2—, —CH2CH2O—, —CONHCH2—, —CH2NHCH2—, —COCH2O—, —OCH2CO—, —COCH2NH— or —CHCH2CO—], their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.
摘要翻译：本发明提供新的取代的苯基丙酸衍生物，其结合受体作为人类过氧化物酶体增殖物激活受体α（PPARα）的配体，以活化并显示出有力的降脂作用，以及制备它们的方法。它涉及由通式（1）表示的取代的苯基丙酸衍生物[其中R 1表示碳原子数为1〜4的低级烷基，碳原子数1〜3的低级烷氧基，三氟甲基，三氟甲氧基，未取代或可具有取代基的苯基，未取代或可具有取代基的苯氧基或未取代或可具有取代基的苄氧基，R 2表示氢原子，碳原子数为1〜3的碳原子数为1〜4的低级烷基，碳原子数1〜3的低级烷氧基，碳原子数为1〜3的低级烷氧基，A 部分表示-CH 2 CO 2，-NHCOCH 2 - ， - CH 2 CH 2 CO-， - CH 2 CH 2 CH 2 - ， - CH 2 CH 2 - O-（CH 2）2 CH 2 - ，-CONHCH 2 - ， - CH 2 NHCH 2 - ， - COCH 2 O - ， - OCH 2 - CO - ， - COCH 2 NH-或-CHCH 2 - CO-]，它们的药学上可接受的盐和它们的水合物，以及它们的制备方法。

5. 发明申请

US20130317215A1 STABLE SYNTHETIC INTERMEDIATE AND METHOD FOR MANUFACTURING SAME 审中-公开
标题翻译：稳定的合成中间体及其制备方法
公开(公告)号：US20130317215A1
公开(公告)日：2013-11-28
申请号：US13990382
申请日：2011-11-30
申请人： Takeshi Tsubuki , Takahiro Tanase , Masashi Suzuki
发明人： Takeshi Tsubuki , Takahiro Tanase , Masashi Suzuki
IPC分类号： C07C229/64 , C07C227/18 , C07D413/04
CPC分类号： C07C229/64 , C07C227/18 , C07D413/04
摘要： [Problem]To provide a stable industrially-manufactured intermediate, enabling an industrially stable supply of 2-pyridyl-benz[d][1,3]oxazine to be provided.[Solution]The compound represented by formula (6) (wherein M represents sodium or potassium).
摘要翻译： [问题]提供稳定的工业制造的中间体，使得能够工业上稳定地供应2-吡啶基 - 苯并[d] [1,3]恶嗪。 [溶液]由式（6）表示的化合物（其中M表示钠或钾）。

6. 发明授权

US06963012B2 Diaryl ether derivative, addition salt thereof, and immunosuppressant 失效
标题翻译：二芳基醚衍生物，其加成盐和免疫抑制剂
公开(公告)号：US06963012B2
公开(公告)日：2005-11-08
申请号：US10490345
申请日：2002-09-25
申请人： Yasushi Kohno , Naoki Ando , Takahiro Tanase , Kazuhiko Kuriyama , Satoru Iwanami , Shinji Kudou
发明人： Yasushi Kohno , Naoki Ando , Takahiro Tanase , Kazuhiko Kuriyama , Satoru Iwanami , Shinji Kudou
IPC分类号： A61P11/02 , A61P11/06 , A61P17/00 , A61P17/16 , A61P27/14 , A61P29/00 , A61P37/06 , A61P37/08 , C07C217/64 , C07D319/06 , C07C217/34 , C07C217/56 , C07C255/54 , C07C317/22
CPC分类号： C07D319/06 , C07C217/64
摘要： The present invention provides diaryl ether derivatives that exhibit significant immunosuppressive effects with less side effects.The diaryl derivatives of the present invention are represented by the following general formula (1): one example is 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propanediol.
摘要翻译：本发明提供了表现出显着的免疫抑制作用并具有较少副作用的二芳基醚衍生物。本发明的二芳基衍生物由以下通式（1）表示：一个实例是2-氨基-2- [4-（3-苄氧基苯氧基）-2-氯苯基]丙基-1,3-丙二醇。

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