公开(公告)号：US20060199795A1

公开(公告)日：2006-09-07

申请号：US10543997

申请日：2004-01-27

申请人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Takashi Miki ,  Yuji Kawamata ,  Satoru Oi ,  Taisuke Tawaraishi ,  Yuji Ishichi ,  Mariko Hirohashi

发明人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Takashi Miki ,  Yuji Kawamata ,  Satoru Oi ,  Taisuke Tawaraishi ,  Yuji Ishichi ,  Mariko Hirohashi

IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/5513

CPC分类号： C07D267/14 ,  A61K31/4353 ,  A61K31/5513 ,  A61K31/553

摘要： The present invention provides a TGR5 receptor agonist comprising a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring; and ring B′ is a 5- to 8-membered ring having one or more substituents or a salt thereof or a prodrug thereof, which is useful for the treatment of various diseases.

摘要翻译： 本发明提供一种TGR5受体激动剂，其包含由下式表示的稠环化合物：其中环A为任选取代的芳环; 环B'是具有一个或多个取代基的5-至8-元环或其盐或其前药，其可用于治疗各种疾病。

公开(公告)号：US07625887B2

公开(公告)日：2009-12-01

申请号：US10543997

申请日：2004-01-27

申请人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yuji Kawamata ,  Taisuke Tawaraishi ,  Yuji Ishichi ,  Mariko Hirohashi

发明人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yuji Kawamata ,  Taisuke Tawaraishi ,  Yuji Ishichi ,  Mariko Hirohashi

IPC分类号： A61K31/553 ,  A61K45/00 ,  C07D267/22 ,  C07D281/02

CPC分类号： C07D267/14 ,  A61K31/4353 ,  A61K31/5513 ,  A61K31/553

摘要： It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B′ represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases.

摘要翻译： 本发明提供一种TGR5受体激动剂，其含有下述通式表示的稠环化合物，其盐或其前药：（1）其中环A表示任选取代的芳环; 环B'表示具有一个或多个取代基的5-至8-元环; 其用于治疗各种疾病。

公开(公告)号：US20070117840A1

公开(公告)日：2007-05-24

申请号：US10549889

申请日：2004-03-16

申请人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yoshihiro Banno ,  Hiromi Yoshida ,  Hirokazu Matsumoto

发明人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Yoshihiro Banno ,  Hiromi Yoshida ,  Hirokazu Matsumoto

IPC分类号： A61K31/4704

CPC分类号： A61K31/4704

摘要： A compound represented by the formula (I): wherein ring A represents an aromatic ring; X represents a bond, oxygen, NR4 (R4 represents hydrogen, a hydrocarbon group, or a heterocyclic group), or alkylene; R1 represents a hydrocarbon group, or a heterocyclic group; R2 represents —COYR5 (Y represents a bond, alkylene, oxygen, sulfur, or NR6 (R6 represents hydrogen, a hydrocarbon group, or a heterocyclic group), and R5 represents a hydrocarbon group, or a heterocyclic group), a hydrocarbon group, or a heterocyclic group; and R3 represents a hydrocarbon group, a heterocyclic group, optionally substituted hydroxy, optionally substituted amino, or —S(O)nR7 (R7 represents a hydrocarbon group, or a heterocyclic group, and n is 0 to 2), a salt of the compound, or a prodrug or either is useful as an agent for modulating the function of an RFRP receptor.

摘要翻译： 由式（I）表示的化合物：其中环A表示芳环; X表示键，氧，NR 4（R 4表示氢，烃基或杂环基）或亚烷基; R 1表示烃基或杂环基; R 2表示-COYR 5（Y表示键，亚烷基，氧，硫或NR 6（R 6） SUP>表示氢，烃基或杂环基），R 5表示烃基或杂环基），烃基或杂环基; 和R 3表示烃基，杂环基，任选取代的羟基，任选取代的氨基或-S（O）n R 7 （R 7表示烃基或杂环基，n为0〜2），化合物或前药的盐或其可用作调节其功能的试剂 RFRP受体。

公开(公告)号：US20090239839A1

公开(公告)日：2009-09-24

申请号：US12391520

申请日：2009-02-24

申请人： Fumio ITOH ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

发明人： Fumio ITOH ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

IPC分类号： A61K31/553 ,  A61P25/04

CPC分类号： C07D267/08

摘要： An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.

摘要翻译： 用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n（n为0〜2的整数）或NR 3（R 3表示氢，任选取代的烃基或任意取代的杂环基）。 并且R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

公开(公告)号：US20070129348A1

公开(公告)日：2007-06-07

申请号：US10553273

申请日：2004-04-15

申请人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

发明人： Fumio Itoh ,  Shuji Hinuma ,  Naoyuki Kanzaki ,  Hiroshi Mabuchi ,  Hiromi Yoshida ,  Hirokazu Matsumoto ,  Takeshi Wakabayashi

IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/5513

CPC分类号： C07D267/08

摘要： An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I) [wherein ring A represents an optionally substituted aromatic ring; ring B represents an optionally substituted benzene ring; X represents oxygen, S(O)n (n is an integer of 0 to 2), or NR3 (R3 represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group); and R1 and R2 each represents hydrogen, an optionally substituted hydrocarbon group, or an optionally substituted heterocyclic group] or a salt of the compound.

摘要翻译： 用于调节RFRP受体功能的试剂，其特征在于含有由式（I）表示的化合物[其中环A表示任选取代的芳环; 环B表示任选取代的苯环; X表示氧，S（O）n N（n为0〜2的整数）或NR 3（R 3）表示氢， 任选取代的烃基或任选取代的杂环基）; 和R 1和R 2各自表示氢，任选取代的烃基或任选取代的杂环基]或该化合物的盐。

公开(公告)号：US06228984B1

公开(公告)日：2001-05-08

申请号：US08776971

申请日：1997-02-07

申请人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

发明人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

IPC分类号： C07K1447

CPC分类号： C07H21/04 ,  A61K38/00 ,  C07K14/575 ,  C07K14/705 ,  C07K14/72 ,  C07K16/28

摘要： The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervous system function modulators, and pancreatic function modulators, and (2) development of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

摘要翻译： 本发明涉及用于人垂体和小鼠胰腺衍生的G蛋白偶联受体蛋白质的配体多肽。 编码配体多肽的配体多肽或DNA可用于（1）开发药物如垂体功能调节剂，中枢神经系统功能调节剂和胰腺功能调节剂，以及（2）重组受体蛋白的发育和筛选 的药物候选化合物。 特别地，通过利用根据本发明的重组G蛋白偶联受体蛋白表达的受体结合测定系统，可以筛选对人类和其他温血动物特异性的G蛋白偶联受体的激动剂和拮抗剂， 获得的激动剂或拮抗剂可用作各种疾病的治疗和预防剂。

公开(公告)号：US6048711A

公开(公告)日：2000-04-11

申请号：US959381

申请日：1997-10-28

申请人： Shuji Hinuma ,  Shoji Fukusumi ,  Yuji Kawamata

发明人： Shuji Hinuma ,  Shoji Fukusumi ,  Yuji Kawamata

IPC分类号： G01N33/53 ,  A61K38/00 ,  A61K39/395 ,  A61K48/00 ,  A61P43/00 ,  C07H21/04 ,  C07K14/705 ,  C07K16/28 ,  C12N1/21 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12Q1/68 ,  C12R1/19 ,  G01N33/566

CPC分类号： C07K14/705 ,  A61K38/00

摘要： A novel G-protein coupled receptor protein, a partial peptide and their salts are disclosed. DNA encoding the receptor protein, production of the receptor protein, determination of a ligand to the receptor protein, a method for screening for compounds which inhibit ligand binding to the receptor protein, a kit for screening for such compounds are also disclosed. The receptor protein, its partial peptide and their salts are used for screening for candidate compounds of drugs and the like.

摘要翻译： 公开了一种新型的G蛋白偶联受体蛋白，部分肽及其盐。 编码受体蛋白质的DNA，受体蛋白质的产生，受体蛋白质的配体的测定，抑制配体与受体蛋白质结合的化合物的筛选方法，用于筛选这些化合物的试剂盒。 受体蛋白质，其部分肽及其盐用于筛选候选药物化合物等。

公开(公告)号：US06794491B1

公开(公告)日：2004-09-21

申请号：US09576290

申请日：2000-05-23

申请人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

发明人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

IPC分类号： C07K14475

CPC分类号： C07H21/04 ,  A61K38/00 ,  C07K14/575 ,  C07K14/705 ,  C07K14/72 ,  C07K16/28

摘要： The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervious system function modulators, and pancreatic function modulators, and (2) development of receptor binding assay systems using the expression of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.

摘要翻译： 本发明涉及用于人垂体和小鼠胰腺衍生的G蛋白偶联受体蛋白质的配体多肽。配体多肽或编码配体多肽的DNA可用于（1）开发诸如垂体的药物 功能调节剂，中枢神经系统功能调节剂和胰腺功能调节剂，以及（2）使用重组受体蛋白质的表达和药物候选化合物的筛选开发受体结合测定系统。特别地，通过受体结合测定系统利用表达 根据本发明的重组G蛋白偶联受体蛋白质，可以筛选对人类和其他温血动物特异性的G蛋白偶联受体的激动剂和拮抗剂，并且所获得的激动剂或拮抗剂可用作治疗和预防 各种疾病的代理

公开(公告)号：US07214495B2

公开(公告)日：2007-05-08

申请号：US10504726

申请日：2003-02-13

申请人： Shuji Hinuma ,  Masaki Hosoya ,  Yasuaki Ito ,  Makoto Kobayashi ,  Hideyuki Tanaka ,  Shoichi Ohkubo ,  Ryo Fujii ,  Hideki Kizawa ,  Yuji Kawamata ,  Kazuhiro Ogi ,  Masataka Harada

发明人： Shuji Hinuma ,  Masaki Hosoya ,  Yasuaki Ito ,  Makoto Kobayashi ,  Hideyuki Tanaka ,  Shoichi Ohkubo ,  Ryo Fujii ,  Hideki Kizawa ,  Yuji Kawamata ,  Kazuhiro Ogi ,  Masataka Harada

IPC分类号： G01N33/566

CPC分类号： C07K14/705 ,  A61K38/00 ,  A61K39/00 ,  A61K48/00 ,  A61K2039/505 ,  C07K16/28 ,  C07K2319/60 ,  G01N2333/726 ,  G01N2500/00

摘要： By using (1) a G protein-coupled receptor protein having the same or substantially the same amino acid sequence as the amino acid sequence represented by SEQ ID NO: 1 or its salt and (2) a fatty acid or an eicosanoid, a compound or its salt that can change the binding properties of the receptor protein or its salt to the fatty acid or the eicosanoid can be screened efficiently.

摘要翻译： 通过使用（1）具有与SEQ ID NO：1所示的氨基酸序列相同或基本相同的氨基酸序列的G蛋白偶联受体蛋白质或其盐和（2）脂肪酸或类花生酸，化合物 或者可以有效地筛选能够将受体蛋白质或其盐与脂肪酸或类花生酸形成的结合性质改变的盐。

公开(公告)号：US20050170461A1

公开(公告)日：2005-08-04

申请号：US11054211

申请日：2005-02-08

申请人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

发明人： Shuji Hinuma ,  Yugo Habata ,  Yuji Kawamata ,  Masaki Hosoya ,  Ryo Fujii ,  Shoji Fukusumi ,  Chieko Kitada

IPC分类号： A61K38/00 ,  C07H21/04 ,  C07K14/575 ,  C07K14/705 ,  C07K14/72 ,  C07K16/28 ,  C12N1/21 ,  C12N15/12

CPC分类号： C07H21/04 ,  A61K38/00 ,  C07K14/575 ,  C07K14/705 ,  C07K14/72 ,  C07K16/28

摘要： The present invention relates to the ligand polypeptide for the human pituitary- and mouse pancreas-derived G protein-coupled receptor proteins. The ligand polypeptide or the DNA which codes for the ligand polypeptide can be used for (1) development of medicines such as pituitary function modulators, central nervious system function modulators, and pancreatic function modulators, and (2) development of receptor binding assay systems using the expression of recombinant receptor proteins and screening of pharmaceutical candidate compounds. In particular, by the receptor binding assay systems utilizing the expression of recombinant G protein-coupled receptor proteins in accordance with the invention, agonists and antagonists of G protein-coupled receptors which are specific to human and other warm-blooded animals can be screened and the agonists or antagonists obtained can be used as therapeutic and prophylactic agents for various diseases.