公开(公告)号：US20080287544A1

公开(公告)日：2008-11-20

申请号：US12142652

申请日：2008-06-19

申请人： Kazuyoshi YAMAOKA ,  Kenichiro Takagi ,  Kenichiro Kataoka ,  Masanori Yamamoto ,  Toshihiro Chikanishi

发明人： Kazuyoshi YAMAOKA ,  Kenichiro Takagi ,  Kenichiro Kataoka ,  Masanori Yamamoto ,  Toshihiro Chikanishi

IPC分类号： A61K31/19 ,  A61P3/10 ,  A61P9/10

CPC分类号： G01N33/5079 ,  G01N33/6872

摘要： The present invention provides a method for screening a substance having a thermogenesis enhancing effect containing a compound having an effect activating PPARδ, an agent containing the compound, and an agent having antidiabetic, antiobestic or visceral accumulated fat-lowering function.The present invention provides an agent containing a compound having an effect activating PPARδ, which is a peroxisome proliferator activated receptor, and having effects which enhances nonshivering thermogenesis (nST), specifically enhances uncoupling respiration in mitochondria of cells in an adipose tissue or the like, or proton leak in inner membranes of mitochondria, and increases the amount of expression of UCP1, and provides an antidiabetic agent, an antiobestic gent and a visceral accumulated fat-lowering agent containing the compound. Further, the present invention provides a method for screening the compound by measuring a PPARδ activating effect.

摘要翻译： 本发明提供一种筛选具有生发促进效果的物质的方法，其含有具有活化PPARδ的作用的化合物，含有该化合物的药剂和具有抗糖尿病，抗胆固醇或内脏积累的降脂功能的药剂。 本发明提供含有具有激活PPARdta的作用的化合物的药剂，其是过氧化物酶体增殖物激活受体，并且具有增强非发热生成（nST）的作用，特别地增强脂肪组织等中的细胞的线粒体中的解偶联呼吸， 或线粒体内膜中的质子泄漏，并增加UCP1的表达量，并提供含有该化合物的抗糖尿病剂，抗胆碱剂和内脏积累的降脂剂。 此外，本发明提供了通过测量PPARδ激活效应来筛选化合物的方法。

公开(公告)号：US07396642B2

公开(公告)日：2008-07-08

申请号：US10483627

申请日：2002-07-17

申请人： Kazuyoshi Yamaoka ,  Kenichiro Takagi ,  Kenichiro Kataoka ,  Masanori Yamamoto ,  Toshihiro Chikanishi

发明人： Kazuyoshi Yamaoka ,  Kenichiro Takagi ,  Kenichiro Kataoka ,  Masanori Yamamoto ,  Toshihiro Chikanishi

IPC分类号： C12Q1/00 ,  C12Q1/68 ,  G01N33/53

CPC分类号： G01N33/5079 ,  G01N33/6872

摘要： The present invention provides a method for screening a substance having a thermogenesis enhancing effect containing a compound having an effect activating PPAR δ, an agent containing the compound, and an agent having antidiabetic, antiobestic or visceral accumulated fat-lowering function.The present invention provides an agent containing a compound having an effect activating PPAR δ, which is a peroxisome proliferator activated receptor, and having effects which enhances nonshivering thermogenesis (nST), specifically enhances uncoupling respiration in mitochondria of cells in an adipose tissue or the like, or proton leak in inner membranes of mitochondria, and increases the amount of expression of UCP1, and provides an antidiabetic agent, an antiobestic gent and a visceral accumulated fat-lowering agent containing the compound. Further, the present invention provides a method for screening the compound by measuring a PPAR δ activating effect.

摘要翻译： 本发明提供一种筛选具有生发增强效果的物质的方法，其含有具有活化PPARδ的作用的化合物，含有该化合物的药剂和具有抗糖尿病，抗胆固醇或内脏积累的降脂功能的药剂。 本发明提供了含有具有活化PPARδ作用的化合物的化合物，其是过氧化物酶体增殖物激活受体，并且具有增强非发热生成（nST）的作用，特别地增强脂肪组织等中的细胞的线粒体中的解偶联呼吸 或线粒体内膜中的质子泄漏，并增加UCP1的表达量，并提供含有该化合物的抗糖尿病药，抗胆碱剂和内脏累积降脂剂。 此外，本发明提供了通过测量PPARδ激活效应来筛选化合物的方法。

公开(公告)号：US5804410A

公开(公告)日：1998-09-08

申请号：US508448

申请日：1995-07-28

申请人： Kazuyoshi Yamaoka ,  Hiroko Ogawa ,  Yoshinori Sugimoto ,  Kenichi Masuda ,  Tetsuya Suga ,  Kenichiro Takagi ,  Susumu Yasuoka

发明人： Kazuyoshi Yamaoka ,  Hiroko Ogawa ,  Yoshinori Sugimoto ,  Kenichi Masuda ,  Tetsuya Suga ,  Kenichiro Takagi ,  Susumu Yasuoka

IPC分类号： C12N9/64 ,  C12N15/57 ,  C12P21/06 ,  C07H17/00 ,  C12N9/00

CPC分类号： C12N9/6424 ,  C12N2799/026

摘要： This invention provides a nucleic acid sequence encoding a trypsin-like enzyme which can be present at the trachea of human lungs, and can selectively digest a synthetic substrate for trypsin and a synthetic substrate for thrombin, and fibrinogen; and a process for producing the trypsin-like enzyme by genetic engineering utilizing the nucleic acid sequence.

摘要翻译： 本发明提供编码胰蛋白酶样酶的核酸序列，其可以存在于人肺气管中，并且可以选择性地消化胰蛋白酶的合成底物和用于凝血酶和纤维蛋白原的合成底物; 以及利用核酸序列通过遗传工程生产胰蛋白酶样酶的方法。

公开(公告)号：US20130210781A1

公开(公告)日：2013-08-15

申请号：US13880637

申请日：2011-10-24

申请人： Hiroshi Saito ,  Masato Komiyama ,  Eiji Ochiai ,  Kenichiro Takagi ,  Takayuki Chida ,  Mariko Fujita ,  Keiichiro Imaizumi ,  Toshiyuki Kaneko

发明人： Hiroshi Saito ,  Masato Komiyama ,  Eiji Ochiai ,  Kenichiro Takagi ,  Takayuki Chida ,  Mariko Fujita ,  Keiichiro Imaizumi ,  Toshiyuki Kaneko

IPC分类号： C07C401/00 ,  C07F7/18

CPC分类号： C07C401/00 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/24 ,  C07F7/1804 ,  C07F7/1852 ,  Y02P20/55

摘要： To provide a novel vitamin D3 derivative useful as a therapeutic agent for osteoporosis.Provided is a vitamin D3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.

公开(公告)号：US20100216747A1

公开(公告)日：2010-08-26

申请号：US12671414

申请日：2008-08-01

申请人： Eiji Ochiai ,  Miyuki Nishiga ,  Kenichiro Takagi ,  Yoshiaki Azuma

发明人： Eiji Ochiai ,  Miyuki Nishiga ,  Kenichiro Takagi ,  Yoshiaki Azuma

IPC分类号： A61K31/663 ,  A61K31/675 ,  A61P19/08

CPC分类号： A61K45/06 ,  A61K31/426 ,  A61K31/663 ,  A61K31/675 ,  A61K2300/00

摘要： An object of the present invention is to provide a preventive drug and a therapeutic drug for diseases caused by abnormal bone metabolism, especially osteoporosis, which is more effective than conventional drugs. Combined use of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, or a salt thereof; and at least one compound selected from the group consisting of etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, minodronic acid, ibandronic acid, zoledronic acid, and salts thereof can exert higher bone resorption inhibitory effect and provide a preventive effect and a therapeutic effect for diseases caused by abnormal bone metabolism, especially osteoporosis as compared with administration of the respective agents respectively.

摘要翻译： 本发明的目的是提供一种用于由异常的骨代谢引起的疾病，特别是骨质疏松症的预防药物和治疗药物，其比常规药物更有效。 合并使用N-羟基-4- {5- [4-（5-异丙基-2-甲基-1,3-噻唑-4-基）苯氧基]戊氧基} - 苄脒或其盐; 并且选自依替膦酸，氯膦酸，帕米膦酸，替鲁膦酸，利塞膦酸，米诺膦酸，伊班膦酸，唑来膦酸及其盐中的至少一种化合物可以发挥更高的骨吸收抑制作用并提供预防效果 以及与分别给予各种试剂相比，由异常骨代谢引起的疾病，特别是骨质疏松症的治疗效果。

公开(公告)号：US09006220B2

公开(公告)日：2015-04-14

申请号：US13880637

申请日：2011-10-24

申请人： Hiroshi Saito ,  Masato Komiyama ,  Eiji Ochiai ,  Kenichiro Takagi ,  Takayuki Chida ,  Mariko Fujita ,  Keiichiro Imaizumi ,  Toshiyuki Kaneko

发明人： Hiroshi Saito ,  Masato Komiyama ,  Eiji Ochiai ,  Kenichiro Takagi ,  Takayuki Chida ,  Mariko Fujita ,  Keiichiro Imaizumi ,  Toshiyuki Kaneko

IPC分类号： C07C401/00 ,  C07F7/18

CPC分类号： C07C401/00 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/24 ,  C07F7/1804 ,  C07F7/1852 ,  Y02P20/55

摘要： To provide a novel vitamin D3 derivative useful as a therapeutic agent for osteoporosis.Provided is a vitamin D3 derivative represented by the following formula (1) or a medicinally acceptable solvate thereof: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkylcarbonyloxyalkyl group with each alkyl having 1 to 6 carbon atoms, or an arylcarbonyloxyalkyl group with the aryl having 6 to 10 carbon atoms and the alkyl having 1 to 6 carbon atoms; R2 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or, together with the other R2 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; R3 represents an alkyl group having 1 to 6 carbon atoms or, together with the other R3 and the carbon atom to which they are bound to, may form a cyclic alkyl group having 3 to 6 carbon atoms; X represents an oxygen atom or a methylene group; and n represents an integer of 1 or 2.

摘要翻译： 提供可用作骨质疏松症治疗剂的新型维生素D3衍生物。 本发明提供由下式（1）表示的维生素D3衍生物或其药学上可接受的溶剂合物：其中，R1表示氢原子，碳原子数1〜6的烷基，碳原子数1〜6的烷基的烷基羰氧基烷基 或芳基具有6至10个碳原子的芳基羰氧基烷基和具有1至6个碳原子的烷基; R 2表示氢原子或碳原子数1〜6的烷基，或者与其它的R 2和与它们相连的碳原子一起形成可以形成碳原子数为3〜6的环状烷基。 R 3表示碳原子数为1〜6的烷基，或者与另外的R 3及与它们相连的碳原子一起形成碳原子数为3〜6的环状烷基。 X表示氧原子或亚甲基; n表示1或2的整数。