公开(公告)号：EP2017279A1

公开(公告)日：2009-01-21

申请号：EP07742848.0

申请日：2007-04-25

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： KATO, Tetsuya ,  KAWANISHI, Nobuhiko ,  MITA, Takashi ,  NAGAI, Keita ,  NONOSHITA, Katsumasa ,  OHKUBO, Mitsuru

IPC分类号： C07D487/08 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K45/08 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07D487/08

摘要： The present invention relates to a compound of general formula I:

wherein:
n 1 and n 2 are the same or different, and are 0 or 1; R is aryl, heteroaryl, etc.; R e is hydrogen atom or lower alkyl; two groups selected from four groups consisting of (i) either one of R a1 and R a1 ', (ii) either one of R a2 and R a2 ', (iii) either one of R b1 and R b1 ', and (iv) either one of R b2 and R b2 ', are combined to form -(CH 2 ) n - where n is 1, 2 or 3; and among R a1 , R a1 ', R a2 , R a2 ', R b1 , R b1 ', R b2 and R b2 ', the groups which do not form -(CH 2 ) n - are each independently hydrogen atom, etc.; X 1 , X 2 , X 3 and X 4 are each independently CH, N, etc.; Y 1 , Y 2 , Y 3 and Y 4 are the same or different and are CH or N, etc.; W is a 5-membered aromatic heterocyclic group,

or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及通式I的化合物：其中：n 1和n 2相同或不同，为0或1; R是芳基，杂芳基等; R e为氢原子或低级烷基; 从（a）R a1和R a1'中的任一个，（ii）R a2和R a2'中的任一个，（iii）R b1和R b1'中的任一个和（iv） ）R b2和R b2'中的任一个组合形成 - （CH 2）n - ，其中n为1,2或3; 在R a1，R a1'，R a2，R a2'，R b1，R b1'，R b2和R b2'中，不形成 - （CH 2）n - 的基团各自独立地为氢原子等 。 X 1，X 2，X 3和X 4各自独立地为CH，N等; Y 1，Y 2，Y 3和Y 4相同或不同，为CH或N等; W是5元芳杂环基，或其药学上可接受的盐或酯。

公开(公告)号：EP2016080A1

公开(公告)日：2009-01-21

申请号：EP07742843.1

申请日：2007-04-25

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： SAKAMOTO, Toshihiro ,  SUNAMI, Satoshi ,  YAMAMOTO, Fuyuki ,  NIIYAMA, Kenji ,  BAMBA, Makoto ,  TAKAHASHI, Keiji ,  FURUYAMA, Hidetomo ,  SAGARA, Takeshi ,  OTSUKI, Sachie ,  NISHIBATA, Toshihide ,  YOSHIZUMI, Takashi ,  HIRAI, Hiroshi

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P43/00

CPC分类号： C07D487/04 ,  A61K31/4162 ,  A61K31/519

摘要： The invention relates to compounds of a general formula (I): wherein A1 is selected from the following formula (aa1); R1 is a lower alkenyl group or a lower alkynyl group; R2 is a phenyl, pyridyl or thienyl group; R5 and R6 are a hydrogen atom, a lower alkyl group or a hydroxy-lower alkyl group, etc. The compounds of the invention have excellent Weel kinase-inhibitory effect and are therefore useful in the field of medicines, especially treatment of various cancers.

公开(公告)号：EP1944301A1

公开(公告)日：2008-07-16

申请号：EP06822742.0

申请日：2006-10-25

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： SASAKI, Takahide ,  SATO, Nagaaki ,  TAKAHASHI, Toshiyuki ,  MIZUTANI, Takashi

IPC分类号： C07D327/06 ,  A61K31/4025 ,  A61K31/4365 ,  A61K31/4535 ,  A61K31/454 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/00 ,  A61P9/04 ,  A61P9/10 ,  A61P9/12 ,  A61P13/12 ,  A61P19/06 ,  A61P25/00 ,  A61P25/08 ,  A61P25/16 ,  A61P25/20 ,  A61P25/22

CPC分类号： C07D327/06 ,  C07D497/04

摘要： Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof.

This compound is useful for treatment of obesity, diabetes and the like. [In the formula (I), Ar represents a benzene ring or the like; X 1 represents a nitrogen atom, a sulfur atom or the like; R1 represents an aryl group or the like; X 2 represents a group represented by the following formula (II): (wherein R 4 and R 5 respectively represent a lower alkyl group or the like, and m represents a number of 2-4) or the like; one of X and Y represents an oxygen atom and the other represents a sulfanyl group or the like; and X 3 -X 6 respectively represent -CH-, a nitrogen atom or the like.

摘要翻译： 公开了由下式（I）表示的化合物及其药学上可接受的盐。 该化合物可用于治疗肥胖症，糖尿病等。 [式（I）中，Ar表示苯环等; X1代表氮原子，硫原子等; R1代表芳基等; X2表示由下式（II）表示的基团：（其中R4和R5分别表示低级烷基等，m表示2-4的数）等等; X和Y中的一个代表氧原子，另一个代表硫烷基等; 和X 3 -X 6分别代表-CH-，氮原子等。

公开(公告)号：EP1420020B1

公开(公告)日：2008-05-28

申请号：EP02751627.7

申请日：2002-07-18

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： HASHIMOTO, M., c/o BANYU PHARMACEUTICAL CO., LTD. ,  OKAMOTO, Osamu,c/o BANYU PHARMACEUTICAL CO., LTD. ,  OZAKI, S. c/o BANYU PHARMACEUTICAL CO. LTD. ,  OHTA, H. c/o BANYU PHARMACEUTICAL CO. LTD.

IPC分类号： C07D471/10 ,  A61K31/438 ,  A61P1/00 ,  A61P3/04 ,  A61P7/12 ,  A61P11/06 ,  A61P11/08 ,  A61P11/14 ,  A61P15/10 ,  A61P23/00 ,  A61P25/04 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P43/00

CPC分类号： C07D471/10

摘要： A 4-oxoimidazolidine-2-spiropiperidine derivative represented by the general formula [I]: [I] (wherein A1, A2, A3, A4, and A5 each represents an optionally halogenated methine group or nitrogen; R1 and R2 each represents lower alkyl, etc.; R3 represents hydrogen or lower alkyl; and R4 and R5 each represents hydrogen or lower alkyl optionally substituted by hydroxy, etc.) or a salt of the derivative. The compound functions as a nociceptin receptor agonist and is useful as an analgesic, agent for overcoming tolerance to narcotic analgesics, agent for overcoming dependence on narcotic analgesics, analgesia enhancer, antiobestic agent, brain-function ameliorant, schizophrenia remedy, remedy for degenerative nerve diseases, anxiolytic or antidepressant agent, remedial agent for diabetes insipidus, polyuria remedy, etc.

公开(公告)号：EP1912642A2

公开(公告)日：2008-04-23

申请号：EP06788290.2

申请日：2006-07-24

申请人： Merck & Co., Inc. ,  BANYU PHARMACEUTICAL CO., LTD.

发明人： FERLITA, Russell, R. ,  HAGA, Yuji ,  ISHIKAWA, Makoto ,  KAMEI, Keisuke ,  KATO, Shinji ,  KOJIMA, Hisaki ,  MOMENT, Aaron ,  NONOYAMA, Nobuaki ,  SATAKE, Nobuya ,  SHIGEMORI, Kazuki ,  WADA, Toshihiro ,  WANG, Yaling ,  WEISSMAN, Steven, A. ,  WENSLOW, Robert, M.

IPC分类号： A61K31/4355 ,  C07D491/048

CPC分类号： C07D491/10

摘要： The present invention relates to a process for producing crystalline trans-N-[l-(2-fluorophenyl)- S-pyrazoly]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide and novel salts, hydrates and polymorphs thereof.

公开(公告)号：EP1905769A1

公开(公告)日：2008-04-02

申请号：EP06781274.3

申请日：2006-07-12

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： OGINO, Yoshio c/o Tsukuba Research Institute ,  NONOSHITA,Katsumasa c/o Tsukuba Research Institute ,  NISHIMURA, Teruyuki c/o Tsukuba Research Institute ,  EIKI, Jun-ichi c/o Tsukuba Research Institute

IPC分类号： C07D405/14 ,  A61K31/4439 ,  A61K31/497 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07D409/14 ,  C07D413/14

CPC分类号： C07D409/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： Compounds having glucokinase activating effects and being useful as treatments for diabetes, which are represented by the following formula (I):

(wherein X 1 to X 4 represent a carbon atom, etc., ring A represents a 5- or 6-membered heteroaryl having from 1 to 4 hetero atoms selected from the group consisting of a nitrogen atom, a sulfur atom and an oxygen atom, X 5 represent an oxygen atom, etc., X represent a carbon atom, etc., Het represents a 5- or 6-membered aliphatic hetero ring, R 1 represents aryl, etc., R 2 represents formyl, etc., R 3 represents -C 1-6 alkyl, etc.), as well as their pharmaceutically acceptable salts.

摘要翻译： 具有葡糖激酶活化作用并且可用作糖尿病治疗的化合物，其由下式（I）表示：（其中X 1至X 4表示碳原子等，环A表示5-或6-元杂芳基 具有1至4个选自氮原子，硫原子和氧原子的杂原子，X 5表示氧原子等，X表示碳原子等，Het表示5-或 6元脂肪族杂环，R 1表示芳基等，R 2表示甲酰基等，R 3表示-C 1-6烷基等）及其药学上可接受的盐。

公开(公告)号：EP1878800A1

公开(公告)日：2008-01-16

申请号：EP06745973.5

申请日：2006-04-25

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： NAMBU, Hirohide, Tsukuba Res. Inst. of Banyo ,  OZAKI, Satoshi, Tsukuba Res. Inst. of Banyo ,  TANAKA, Takeshi, Tsukuba Res. Inst. of Banyo ,  OHTA, Hisashi, Tsukuba Research Inst. of Banyo

IPC分类号： C12Q1/02 ,  A61K45/00 ,  A61P3/04 ,  C12N15/09 ,  C12Q1/68

CPC分类号： G01N33/74 ,  C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158 ,  G01N2333/72 ,  G01N2500/10 ,  G01N2800/303

摘要： It is intended to provide a method for evaluating a compound which regulates eating or body weight characterized by comprising the steps of introducing a BARLP gene and preparing a cell expressing BARLP; bringing a test compound into contact with the cells and detecting a specific binding of the test compound to the BARLP and a method for evaluating a compound further comprising the step of evaluating a test compound using a non human genetically engineered animal in which the BARLP gene is inactivated. According to this invention, knowledge about a relationship between BARLP and biological functions is obtained and a method for evaluating a compound targeting BARLP and a BARLP ligand obtained by the evaluation can be provided.

摘要翻译： 它的目的是为其调节通过包括将基因BARLP和制备表达BARLP的细胞的步骤为特征的饮食或体重的化合物评价的方法; 使测试化合物与细胞接触，并检测特定的测试化合物与BARLP和进一步包括使用非人类遗传改造的动物，其中所述BARLP基因是评价测试化合物的步骤的化合物评价的方法的结合 灭活。 。根据本发明，约BARLP和生物学功能之间的关系的知识中获得，并且可以提供用于靶向BARLP的化合物评价的方法和由评估获得的BARLP配体。

公开(公告)号：EP1847603A1

公开(公告)日：2007-10-24

申请号：EP06712843.9

申请日：2006-02-01

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： KOTANI, Hidehito, c/o Banyu Pharmaceutical Co. Ltd ,  YAMANAKA, Kazunori, c/o Banyu Pharma. Co. Ltd. ,  MIZUARAI, Shinji, c/o Banyu Pharmaceutical Co. Ltd

IPC分类号： C12N15/09 ,  C12M1/00 ,  C12Q1/68 ,  G01N33/53 ,  G01N37/00

CPC分类号： G01N33/57484 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/178 ,  G01N33/574 ,  G01N2333/4748 ,  G01N2800/52

摘要： Detection of p53 dysfunction or molecular diagnosis of cancer is carried out by a method comprising the steps of measuring the expression level of at least one gene selected from the group consisting of CARS, MOCOS, TNFRSF9, LOC56901 and GEF-H1 or a gene which is functionally equivalent to the gene in a test tissue or a test cell; comparing the expression level of the gene with that of a corresponding gene in a normal tissue or a normal cell; and determining whether or not the expression level of the gene in the test tissue or the test cell is significantly higher than that of the corresponding gene in the normal tissue or the normal cell based on the comparison result. According to the method for molecular diagnosis of the present invention, regardless of the presence of p53 mutation or without directly detecting p53 mutation, it becomes possible to detect p53 dysfunction or to diagnose cancer caused by p53 dysfunction.

摘要翻译： p53的功能障碍或癌症的分子诊断检测是通过包括测量选自汽车，MOCOS，TNFRSF9，LOC56901和GEF-H1或基因的所有它是所选择的至少一种基因的表达水平的步骤的方法进行 功能上等效于在测试的组织或测试细胞的基因; 比较的确在正常组织或正常细胞中的相应基因的基因的表达水平; 和确定性采矿是否在测试组织或测试细胞中的基因的表达水平比在正常组织或基于该比较结果，正常细胞中的相应基因的显着更高。 。根据本发明的分子诊断的方法中，不管p53突变的或不直接检测p53基因突变的存在，有可能检测到p53的功能障碍或诊断癌症被p53功能障碍引起的。

公开(公告)号：EP1813613A1

公开(公告)日：2007-08-01

申请号：EP05803283.0

申请日：2005-11-07

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： SATO, Y., c/o BANYU PHARMACEUTICAL CO., LTD. ,  KURIHARA, H., c/o BANYU PHARMACEUTICAL CO., LTD. ,  KAMIJO, K., c/o BANYU PHARMACEUTICAL CO., LTD. ,  ONOZAKI, Y., c/o BANYU PHARMACEUTICAL CO., LTD. ,  TSUJINO, T., c/o BANYU PHARMACEUTICAL CO., LTD. ,  SUGIMOTO, T., c/o BANYU PHARMACEUTICAL Co., LTD. ,  WATANABE, A., c/o BANYU PHARMACEUTICAL CO., LTD. ,  MITSUYA, M., c/o BANYU PHARMACEUTICAL CO., LTD. ,  KOMATANI, H., c/o BANYU PHARMACEUTICAL CO., LTD

IPC分类号： C07D471/04 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/5377 ,  A61P35/00 ,  A61P43/00 ,  C07D487/04

CPC分类号： C07D471/04 ,  C07D487/04

摘要： The present invention relates to a compound represented by the Formula [I]:

Wherein:
the A ring is a 5-membered aromatic heterocyclic group containing at least one hetero atom selected from a nitrogen atom, and the like; A 1 and A 2 , are each a nitrogen atom, and the like; X 2 , X 3 , X 4 , and X 5 are all carbon atoms, or alternatively any one of X 2 , X 3 , X 4 , and X 5 is a nitrogen atom and the rest are all carbon atoms; R 1 is a hydrogen atom, or the like; R 2 , R 3 , R 4 , and R 5 , are each a hydrogen atom, or the like; R 6 and R 6 ', are each a hydrogen atom, and the like; R 7 is an aryl group and the like; and R 8 is an amino group or a hydroxy group,
or a pharmaceutically acceptable salt or ester thereof.

摘要翻译： 本发明涉及由式[I]表示的化合物：其中：A环是含有至少一个选自氮原子的杂原子的5元芳族杂环基等; A 1和A 2各自为氮原子等; X 2，X 3，X 4和X 5都是碳原子，或者任选地，X 2，X 3，X 4和X 5是氮原子，其余全部是碳原子; R 1是氢原子等; R 2，R 3，R 4和R 5各自为氢原子等; R 6和R 6'各自为氢原子等; R 7是芳基等; R 8为氨基或羟基，或其药学上可接受的盐或酯。

公开(公告)号：EP1764362A1

公开(公告)日：2007-03-21

申请号：EP05758117.5

申请日：2005-06-29

申请人： BANYU PHARMACEUTICAL CO., LTD.

发明人： KAWAMOTO, Hiroshi, Tsukuba Research Institute ,  ITO, Satoru, Tsukuba Research Institute ,  SATOH, Atsushi, Tsukuba Research Institute ,  NAGATOMI, Yasushi, Tsukuba Research Institute ,  HIRATA, Yukari, Tsukuba Research Institute ,  KIMURA, Toshifumi, Tsukuba Research Institute ,  SUZUKI, Gentaroh, Tsukuba Research Institute ,  SATO, Akio, Tsukuba Research Institute ,  OHTA, Hisashi, Tsukuba Research Institute

IPC分类号： C07D249/06 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61P9/10 ,  A61P25/04 ,  A61P25/08 ,  A61P25/10 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/36 ,  A61P29/00 ,  A61P43/00 ,  C07D271/06 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D413/04

CPC分类号： C07D401/14 ,  C07D249/06 ,  C07D271/04 ,  C07D401/04 ,  C07D417/04

摘要： The present invention relates to a compound represented by the formula (I):

or a pharmaceutically acceptable salt thereof, whrein:
R 1 is a linear or branched alkoxy group, a cycloalkoxy group, a linear or branched lower alkyl group, etc.; R 2 is halogen atom, a lower alkyl group, etc.; Q 1 is carbon atom or nitrogen atom; Q 2 is carbon atom which may be substituted with oxo group; the formula (III) :

is a single bond or a double bond; A is a group selected from the group consisting of the substituent group α; and R 5 is hydrogen atom, a lower alkyl group, cyano group, an alkoxy group or a trialkylsilyl group; having an mGluR1 inhibiting action and being useful as treatment and/or prevention of convulsion, acute pain, cerebral disturbance such as cerebral infarction or transient cerebral ischemia onset, anxiety, chemical dependency or Parkinson's disease.

摘要翻译： 本发明涉及由式（I）表示的化合物或其药学上可接受的盐，其中：R 1为直链或支链烷氧基，环烷氧基，直链或支链低级烷基等; R 2为卤素原子，低级烷基等; Q 1是碳原子或氮原子; Q 2是可被氧代基取代的碳原子; 式（III）：是单键或双键; A是选自由取代基组成的组的组; R 5为氢原子，低级烷基，氰基，烷氧基或三烷基甲硅烷基; 具有mGluR1抑制作用，并且可用作治疗和/或预防惊厥，急性疼痛，脑梗塞如脑梗死或暂时性脑缺血发作，焦虑，化学依赖或帕金森病。