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1. 发明授权

US08232447B2 Animal having modification in MGAT2 gene 失效
标题翻译：具有MGAT2基因修饰的动物
公开(公告)号：US08232447B2
公开(公告)日：2012-07-31
申请号：US12525410
申请日：2007-11-30
申请人： Katsumi Aragane , Katsuya Ohbuchi , Yoshitaka Tamai , Naomoto Harada , Naomi Murai , Yoshiki Ito , Jun Kusunoki , Yukina Tokushima , Takaharu Maruyama
发明人： Katsumi Aragane , Katsuya Ohbuchi , Yoshitaka Tamai , Naomoto Harada , Naomi Murai , Yoshiki Ito , Jun Kusunoki , Yukina Tokushima , Takaharu Maruyama
IPC分类号： A01K67/027 , A01K67/00 , C07H21/02 , C07H21/04
CPC分类号： G01N33/5088 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/0362 , C12N9/1051 , C12N15/8509 , C12N2800/30 , G01N2333/91051 , G01N2500/00 , G01N2800/044
摘要： It is an object to provide a gene-modified non-human animal having inactivated MGAT2 gene and a gene-modified non-human animal cell, which are useful for the search of the function of MGAT2 in vivo. It is another object to provide a method for screening of a compound capable of inhibiting the activity of MGAT2 and a compound capable of inhibiting the activity of MGAT2. It is further another object to provide a method for detecting a disease induced by abnormal lipid metabolism based on the expression level or activity of MGAT2. A method for screening of a compound by using a gene-modified non-human mammal having the artificially inhibited expression of MGAT2 gene and a cell thereof enable to prevent or treat a disease induced by abnormal lipid metabolism. Also a screening of a compound capable of inhibiting or enhancing the function of MGAT2 enables to prevent or treat a disease induced by abnormal lipid metabolism.
摘要翻译：本发明的目的是提供具有失活的MGAT2基因和基因修饰的非人动物细胞的基因修饰的非人动物，其可用于在体内搜索MGAT2的功能。另一个目的是提供一种筛选能够抑制MGAT2活性的化合物和能抑制MGAT2活性的化合物的方法。另一个目的是提供一种基于MGAT2的表达水平或活性来检测由脂质代谢异常引起的疾病的方法。通过使用人体抑制MGAT2基因表达的基因修饰的非人哺乳动物及其细胞筛选化合物的方法能够预防或治疗由脂质代谢异常引起的疾病。另外，能够抑制或增强MGAT2功能的化合物的筛选能够预防或治疗由脂质代谢异常引起的疾病。

2. 发明授权

US07935712B2 Spirochromanone derivatives as acetyl coenzyme A carboxylase (ACC) inhibitors 有权
标题翻译：螺吡色酮衍生物作为乙酰辅酶A羧化酶（ACC）抑制剂
公开(公告)号：US07935712B2
公开(公告)日：2011-05-03
申请号：US11988588
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A01N43/42 , A61K31/44 , A61K31/535
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

3. 发明申请

US20070021453A1 Novel spirochromanone derivatives 有权
标题翻译：新型螺二色酮衍生物
公开(公告)号：US20070021453A1
公开(公告)日：2007-01-25
申请号：US11487029
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/4747 , C07D471/14
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

4. 发明授权

US5120738A Pantothenic acid derivatives 失效
标题翻译：泛酸衍生物
公开(公告)号：US5120738A
公开(公告)日：1992-06-09
申请号：US598900
申请日：1990-10-05
申请人： Hiroshi Ikawa , Hajime Matsumoto , Nobuo Kobayashi , Jun Kusunoki
发明人： Hiroshi Ikawa , Hajime Matsumoto , Nobuo Kobayashi , Jun Kusunoki
IPC分类号： C07C235/12 , C07C237/22 , C07C323/41 , C07C327/30 , C07D295/185 , C07D319/06 , C07D405/12 , C07D407/12
CPC分类号： C07D295/185 , C07C235/12 , C07C237/22 , C07C323/41 , C07C327/30 , C07D319/06 , C07D405/12 , C07D407/12 , C07C2101/14 , Y02P20/55
摘要： Compounds represented by general formula (I) below ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, each represent a hydrogen atom or a protective group for a hydroxyl group;R.sup.3 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, or a group of formula ##STR2## where R.sup.4 represents a saturated or unsaturated, linear, branched or cyclic, monovalent C.sub.5 .about.C.sub.25 -aliphatic hydrocarbon group which may be substituted with an aromatic group, andR.sup.5 represents a hydrogen atom, or a saturated or unsaturated, linear, branched or cyclic, monovalent hydrovarbon group which may be substituted with an aromatic group;Q represents(a) a group of formula --X.sup.1 --A--Y.sup.1 --, where A represents a saturated or unsaturated, linear, branched or cyclic divalent C.sub.2 .about.C.sub.16 -aliphatic hydrocarbon group which may be substituted with an aromativ group, a divalent aromatic hydrocarbon group or a divalent aromatic heterocyclic group; one of X.sup.1 and Y.sup.1 represents ##STR3## and the other represents --O--, --S-- or ##STR4## in which R.sup.6 and R.sup.7 each represent a hydrogen atom or a lower alkyl group;(b) a group of formula --X.sup.2 --(CH.sub.2).sub.l --Y.sup.2 --, where one of X.sup.2 and Y.sup.2 represents a group of formula ##STR5## and the other represents --O--, --S-- or ##STR6## in which ##STR7## represents a 4.about.7-membered, divalent nitrogen-containing aromatic heterocyclic group, and R.sup.6 has the same meaning as defined above, and l is 0, 1 or 2; or(c) a group of formula ##STR8## where m is 2 or 3; n is an integer of from 1 to 4.The compounds have excellent inhibitory activity against acyl Co A-cholesterol-acyltransferase.

5. 发明申请

US20100074888A1 ANIMAL HAVING MODIFICATION IN MGAT2 GENE 失效
标题翻译：动物在MGAT2基因中的修饰
公开(公告)号：US20100074888A1
公开(公告)日：2010-03-25
申请号：US12525410
申请日：2007-11-30
申请人： Katsumi Aragane , Ktsuya Ohbuchi , Yoshitaka Tamai , Naomoto Harada , Naomi Murai , Yoshiki Ito , Jun Kusunoki , Yukina Tokushima , Takaharu Maruyama
发明人： Katsumi Aragane , Ktsuya Ohbuchi , Yoshitaka Tamai , Naomoto Harada , Naomi Murai , Yoshiki Ito , Jun Kusunoki , Yukina Tokushima , Takaharu Maruyama
IPC分类号： A61K39/395 , A01K67/027 , G01N33/50 , C12Q1/02 , A61K38/16 , A61K31/7052 , A61K36/00 , A61K35/00 , A61P3/06
CPC分类号： G01N33/5088 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/0362 , C12N9/1051 , C12N15/8509 , C12N2800/30 , G01N2333/91051 , G01N2500/00 , G01N2800/044
摘要： It is an object to provide a gene-modified non-human animal having inactivated MGAT2 gene and a gene-modified non-human animal cell, which are useful for the search of the function of MGAT2 in vivo. It is another object to provide a method for screening of a compound capable of inhibiting the activity of MGAT2 and a compound capable of inhibiting the activity of MGAT2. It is further another object to provide a method for detecting a disease induced by abnormal lipid metabolism based on the expression level or activity of MGAT2. A method for screening of a compound by using a gene-modified non-human mammal having the artificially inhibited expression of MGAT2 gene and a cell thereof enable to prevent or treat a disease induced by abnormal lipid metabolism. Also a screening of a compound capable of inhibiting or enhancing the function of MGAT2 enables to prevent or treat a disease induced by abnormal lipid metabolism.
摘要翻译：本发明的目的是提供具有失活的MGAT2基因和基因修饰的非人动物细胞的基因修饰的非人动物，其可用于在体内搜索MGAT2的功能。另一个目的是提供一种筛选能够抑制MGAT2活性的化合物和能抑制MGAT2活性的化合物的方法。另一个目的是提供一种基于MGAT2的表达水平或活性来检测由脂质代谢异常引起的疾病的方法。通过使用人体抑制MGAT2基因表达的基因修饰的非人哺乳动物及其细胞筛选化合物的方法能够预防或治疗由脂质代谢异常引起的疾病。另外，能够抑制或增强MGAT2功能的化合物的筛选能够预防或治疗由脂质代谢异常引起的疾病。

6. 发明申请

US20090131464A1 SPIROCHROMANONE DERIVATIVES AS ACETYL COENZYME A CARBOXYLASE (ACC) INHIBITORS 有权
标题翻译：甲氧基酮衍生物作为乙酰丙酮羧酸酶（ACC）抑制剂
公开(公告)号：US20090131464A1
公开(公告)日：2009-05-21
申请号：US11988588
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/438 , A61P3/00
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

7. 发明授权

US07410976B2 Spirochromanone derivatives 有权
标题翻译：螺二色酮衍生物
公开(公告)号：US07410976B2
公开(公告)日：2008-08-12
申请号：US11487029
申请日：2006-07-14
申请人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
发明人： Takeru Yamakawa , Hideki Jona , Kenji Niiyama , Koji Yamada , Tomoharu Iino , Mitsuru Ohkubo , Hideaki Imamura , Jun Shibata , Jun Kusunoki , Lihu Yang
IPC分类号： A61K31/438 , C07D491/107
CPC分类号： C07D491/10 , C07D495/10
摘要： The invention relates to a compound of a formula (I): or a pharmaceutically acceptable salt or ester thereof, useful as a therapeutic agent for various ACC-related disorders.
摘要翻译：本发明涉及可用作各种ACC相关疾病的治疗剂的式（I）化合物或其药学上可接受的盐或酯。

8. 发明授权

US5149834A 4-Hydroxytetrahydropyran-2-one derivatives 失效
标题翻译： 4-羟基四氢吡喃-2-酮衍生物
公开(公告)号：US5149834A
公开(公告)日：1992-09-22
申请号：US665666
申请日：1991-03-07
申请人： Masakatsu Matumoto , Nobuko Watanabe , Eiko Mori , Jun Kusunoki
发明人： Masakatsu Matumoto , Nobuko Watanabe , Eiko Mori , Jun Kusunoki
IPC分类号： C07C46/06 , C07C46/08 , C07C50/02 , C07C50/06 , C07D307/79 , C07D311/58 , C07D405/14 , C07D407/06 , C07D407/14
CPC分类号： C07D307/79 , C07C46/06 , C07C46/08 , C07C50/02 , C07C50/06 , C07D311/58 , C07D405/14 , C07D407/06 , C07D407/14
摘要： 4-hydroxytetrahydropyran-2-one derivatives with general formula (I) are useful as cholesterol reducing agents as well as lipid reducing agents, serving as inhibitors of HMG-CoA reductase, and capable of inhibiting the biosynthesis of peroxidized lipids, and therefore effective for curing arteriosclerosis: ##STR1## wherein R.sub.1 represent hydrogen or a 2-tetrahydropyranyl group; R.sub.2 and R.sub.3 each represent hydrogen or an alkyl group having 1 to 6 carbon atoms; R.sub.4 represents hydrogen, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an aryl group, an aralkyl group, an acyl group, an aroyl group or a substituted sulfonyl group; A represents --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--; and n is an integer of 1 or 2, and intermediates for synthesizing the 4-hydroxytetrahydropyran-2-one derivatives are disclosed.

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