公开(公告)号：EP1293567A1

公开(公告)日：2003-03-19

申请号：EP01941117.2

申请日：2001-06-20

申请人： Takeda Chemical Industries, Ltd.

发明人： MORI, Masaaki ,  SHIMOMURA, Yukio ,  HARADA, Mioko ,  GOTO, Mika ,  KITADA, Chieko ,  ASAMI, Taiji ,  MATSUMOTO, Yoshio ,  ADACHI, Yuka ,  WATANABE, Takuya ,  SUGO, Tsukasa ,  ABE, Michiko

IPC分类号： C12N15/12 ,  C07K14/47 ,  C12N1/21 ,  C07K16/18 ,  G01N33/53 ,  G01N33/50 ,  G01N33/15 ,  C12P21/02 ,  C12P21/08 ,  A61K31/711 ,  A61K38/17 ,  A01K67/027 ,  A61P1/14 ,  A61P3/04

CPC分类号： C07K14/47 ,  A01K2217/05 ,  A61K38/00 ,  G01N2333/726 ,  G01N2500/04

摘要： The present invention aims at providing a ligand to GPR8, its DNA, etc., and more particularly, a polypeptide capable of binding to GPR8 or its amides or esters, or salts thereof, as well as its DNA, etc.
The ligand to GPR8 of the present invention is useful in developing a receptor-binding assay system with the use of a GPR8 expression system, screening candidate compounds for drugs such as preventive/therapeutic agents for obesity, appetite stimulants, prolactin production inhibitors, etc.

摘要翻译： 本发明旨在提供GPR8及其DNA等的配体，更具体地说，可以与GPR8或其酰胺或酯或其盐，以及其DNA等结合的多肽。GPR8的配体 本发明可用于开发使用GPR8表达系统的受体结合测定系统，筛选用于药物的候选化合物，例如用于肥胖的预防/治疗剂，食欲激素，催乳素产生抑制剂等。

公开(公告)号：EP1298439A1

公开(公告)日：2003-04-02

申请号：EP01947822.1

申请日：2001-07-04

申请人： Takeda Chemical Industries, Ltd.

发明人： MORI, Masaaki ,  SHIMOMURA, Yukio ,  HARADA, Mioko ,  SUGO, Tsukasa ,  SHINTANI, Yasushi

IPC分类号： G01N33/566 ,  G01N33/50 ,  G01N33/15

CPC分类号： G01N33/566 ,  A61K38/00 ,  G01N33/74 ,  G01N2333/726

摘要： The present invention relates to a screening method for a compound or a salt thereof that alters the binding property of MCH or a salt thereof to SLT or a salt thereof, or a partial peptide thereof, an amide or an ester thereof, or a salt thereof, characterized by using MCH, a derivative or a salt thereof and SLT or a salt thereof, or a partial peptide thereof, an amide or an ester thereof, or a salt thereof. The screening method of the present invention is useful for screening an SLT agonist, which can be used as an agent for promoting appetite (eating), and an SLT antagonist, which can be used as a prophylactic and/or therapeutic agent for obesity.

摘要翻译： 本发明涉及改变MCH或其盐与SLT或其盐或其部分肽，其酰胺或其酯或其盐的结合性的化合物或其盐的筛选方法 其特征在于使用MCH，其衍生物或其盐和SLT或其盐，或其部分肽，酰胺或其酯或其盐。 本发明的筛选方法可用于筛选可用作促进食欲的药物（进食）的SLT激动剂和可用作肥胖症的预防和/或治疗剂的SLT拮抗剂。

公开(公告)号：EP1344823A1

公开(公告)日：2003-09-17

申请号：EP01998185.1

申请日：2001-11-29

申请人： Takeda Chemical Industries, Ltd.

发明人： TERAO, Yasuko ,  SHINTANI, Yasushi ,  HARADA, Mioko ,  SHIMOMURA, Yukio ,  MORI, Masaaki

IPC分类号： C12N15/12 ,  C07K14/705 ,  C07K16/28 ,  C12P21/02 ,  C12Q1/68 ,  A61K45/00 ,  A61P25/00 ,  A61P29/00 ,  A61P9/00 ,  A61P35/00 ,  A61P3/00 ,  A61P37/02 ,  A61P1/00

CPC分类号： C07K14/47 ,  A01K2217/05 ,  A61K38/00 ,  C07K14/705

摘要： The present invention intends to provide a novel protein useful for a screening of agonists/antagonists. Specifically, the present invention provides rat- and mouse-derived protein or its salt, DNA encoding the protein, a determination method of ligand to the protein, a screening method and a screening kit for a compound that alters a binding property between ligand and the protein, a compound or its salt obtainable by the screening, and the like.
The protein of the present invention or the DNA encoding the same can be used for, (1) a determination of ligand to the protein of the present invention, (2) a prophylactic and/or therapeutic agent for diseases associated with dysfunction of the protein of the present invention, (3) a screening of a compound (agonist/antagonist) that alters a binding property between the protein of the present invention and ligand, and the like.

摘要翻译： 本发明意图提供一种可用于筛选激动剂/拮抗剂的新型蛋白质。 具体地，本发明提供了大鼠和小鼠衍生的蛋白质或其盐，编码蛋白质的DNA，蛋白质配体的测定方法，筛选方法和用于改变配体与第 蛋白质，通过筛选获得的化合物或其盐等。 本发明的蛋白质或其编码的DNA可以用于：（1）测定本发明的蛋白质的配体，（2）与...相关的疾病的预防和/或治疗剂 本发明的蛋白质的功能障碍，（3）筛选改变本发明的蛋白质与配体之间的结合性质的化合物（激动剂/拮抗剂）等。

公开(公告)号：EP1218336A2

公开(公告)日：2002-07-03

申请号：EP00961075.9

申请日：2000-09-19

申请人： Takeda Chemical Industries, Ltd.

发明人： KATO, Kaneyoshi ,  TERAUCHI, Jun ,  MORI, Masaaki ,  SUZUKI, Nobuhiro ,  SHIMOMURA, Yukio ,  TAKEKAWA, Shiro ,  ISHIHARA, Yuji

IPC分类号： C07C235/00

CPC分类号： C07D207/277 ,  C07C217/74 ,  C07C219/28 ,  C07C233/29 ,  C07C233/44 ,  C07C233/80 ,  C07C235/42 ,  C07C235/50 ,  C07C235/56 ,  C07C235/64 ,  C07C235/84 ,  C07C237/40 ,  C07C271/28 ,  C07C275/42 ,  C07C311/21 ,  C07C2602/10 ,  C07C2602/12 ,  C07D209/18 ,  C07D209/22 ,  C07D209/42 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/26 ,  C07D211/32 ,  C07D211/52 ,  C07D211/62 ,  C07D211/70 ,  C07D213/56 ,  C07D213/81 ,  C07D213/82 ,  C07D215/14 ,  C07D215/38 ,  C07D233/24 ,  C07D239/28 ,  C07D239/30 ,  C07D261/18 ,  C07D263/14 ,  C07D263/34 ,  C07D265/28 ,  C07D271/06 ,  C07D295/096 ,  C07D295/13 ,  C07D295/185 ,  C07D307/68 ,  C07D307/81 ,  C07D311/58 ,  C07D317/60 ,  C07D319/20 ,  C07D333/24 ,  C07D333/28 ,  C07D333/38 ,  C07D335/16 ,  C07D405/04 ,  C07D405/12 ,  C07D413/04 ,  C07D413/12 ,  C07D493/04

摘要： A melanin-concentrating hormone antagonist which comprises a compound of formula (I) wherein Ar1 is a cyclic group which may have substituents; X is a spacer having a main chain of 1 to 6 atoms; Y is a bond or a spacer having a main chain of 1 to 6 atoms; Ar is a monocyclic aromatic ring which may be condensed with a 4 to 8 membered non-aromatic ring, and may have further substituents; R?1 and R2¿ are independently hydrogen atom or a hydrocarbon group which may have substituents; R?1 and R2¿, together with the adjacent nitrogen atom, may form a nitrogen-containing hetero ring which may have substituents; R2 may form a spiro ring together with Ar; or R2, together with the adjacent nitrogen atom and Y, may form a nitrogen-containing hetero ring which may have substituents; or a salt thereof; which is useful as an agent for preventing or treating obesity, etc.

摘要翻译： 一种黑色素浓缩激素拮抗剂，其包含下式化合物：其中Ar 1是可以具有取代基的环状基团; X是具有1至6个原子的主链的间隔物; Y是具有1至6个原子的主链的键或间隔基; Ar是可以与4至8元非芳族环稠合的单环芳族环，并且可以具有其它取代基; R 1和R 2独立地是氢原子或可以具有取代基的烃基; R 1和R 2以及相邻的氮原子可以形成可以具有取代基的含氮杂环; R 2可与Ar一起形成螺环; 或R 2与相邻的氮原子和Y一起形成可以具有取代基的含氮杂环; 或其盐; 其可用作预防或治疗肥胖症的药剂等。