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1. 发明公开

EP2299825A1 INHIBITORS OF AKT ACTIVITY 有权
标题翻译： AKT活性抑制剂
公开(公告)号：EP2299825A1
公开(公告)日：2011-03-30
申请号：EP09759048.3
申请日：2009-05-27
申请人： Merck Sharp & Dohme Corp. , Banyu Pharmaceutical Co., Ltd.
发明人： FURUYAMA, Hidetomo , GOTO, Yasuhiro , KAWANISHI, Nobuhiko , LAYTON, Mark, E. , MITA, Takashi , OGINO, Yoshio , ONOZAKI, Yu , ROSSI, Michael, A. , SAKAMOTO, Toshihiro , SANDERSON, Philip, E. , WANG, Jiabing
IPC分类号： A01N43/90
CPC分类号： C07D471/14
摘要： The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供了抑制Akt活性的取代的[1,2,4]三唑并[4,3-a] -1,5-萘啶化合物。具体而言，所公开的化合物选择性地抑制一种或两种Akt同种型，优选Akt1。本发明还提供了包含这种抑制性化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性，特别是Akt1的方法。

2. 发明授权

EP1921065B1 PHENYLPYRIDONE DERIVATIVE 有权
标题翻译：苯基吡啶酮衍生物
公开(公告)号：EP1921065B1
公开(公告)日：2010-10-20
申请号：EP06797001.2
申请日：2006-08-23
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAYA, Akira , SAKAMOTO, Toshihiro , HAGA, Yuji , OTAKE, Norikazu
IPC分类号： C07D213/64 , A61K31/4412 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/5377 , A61P1/00 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P7/08 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/12 , A61P15/06
CPC分类号： C07D213/69 , C07D213/64 , C07D401/10 , C07D413/10
摘要： A compound represented by the formula (I) is contained as an active ingredient: wherein R1 and R2 independently represent a hydrogen atom, a lower alkyl group or the like, or R1 together with a nitrogen atom to which L, Z2 and R1 are attached may form an aliphatic nitrogenated heterocyclic group and R1 and R2 together with a nitrogen atom to which they are attached may form an aliphatic nitrogenated heterocyclic group; X represents a methine group or a nitrogen atom; Y represents -CH2-O-, -CH=CH- or the like; Z1 represents a single bond, a C1-4 alkylene group or the like; Z2 represents a single bond or a C1-4 alkylene group; L represents a methylene group, a C3-8 cycloalkylene group or the like; and Ar represents an aromatic carbocyclic group or the like. The compound is useful as a pharmaceutical for a central nerves system disease, a cardiovascular disease or a metabolic disease.
摘要翻译：含有由式（I）表示的化合物作为活性成分：其中R 1和R 2独立地表示氢原子，低级烷基等，或R 1与连接有L，Z 2和R 1的氮原子一起可以形成脂肪族含氮杂环基，并且R 1和R 2与它们所连接的氮原子一起可以形成脂肪族含氮杂环基; X代表次甲基或氮原子; Y表示-CH 2 -O - ， - CH = CH-等; Z1表示单键，C1-4亚烷基等; Z2表示单键或C1-4亚烷基; L表示亚甲基，C 3-8亚环烷基等; Ar表示芳族碳环基团等。该化合物可用作中枢神经系统疾病，心血管疾病或代谢疾病的药物。

3. 发明授权

EP1347052B1 A METHOD FOR SCREENING COMPOUNEDS USING THE GUANOSINE TRIPHOSPHATE (GTP) BINDING PROTEIN-COUPLED RECEPTOR PROTEIN, BG37 无效
标题翻译：法搜索对于其中GUANOSINTRIPHOSPHAT-（GTP）结合蛋白偶联型受体蛋白BG37中使用的部件
公开(公告)号：EP1347052B1
公开(公告)日：2010-05-05
申请号：EP01976875.3
申请日：2001-10-30
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： MARUYAMA, T., c/o BANYU PHARMACEUTICAL CO., LTD. , NAKAMURA, Takao, c/o BANYU PHARMACEUTICAL CO., LTD , ITADANI, Hiraku, c/o BANYU PHARMACEUTICAL CO., LTD , TANAKA, K., c/o BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C12N15/12 , C12N1/21 , C12N5/10 , C07K14/705 , C07K16/28 , C12P21/02 , C12Q1/02
CPC分类号： C07K14/705

4. 发明公开

EP2120569A2 SPIROCHROMANON DERIVATIVES 有权
标题翻译：螺旋色素衍生物
公开(公告)号：EP2120569A2
公开(公告)日：2009-11-25
申请号：EP08705516.6
申请日：2008-01-08
申请人： Merck & Co., Inc. , BANYU PHARMACEUTICAL CO., LTD.
发明人： IINO, Tomoharu , JONA, Hideki , KURIHARA, Hideki , NAKAMURA, Masayuki , NIIYAMA, Kenji , SHIBATA, Jun , SHIMAMURA, Tadashi , WATANABE, Hitomi , YAMAKAWA, Takeru , YANG, Lihu
IPC分类号： A01N43/16 , A61K31/35
CPC分类号： C07D491/107 , C07D491/20 , C07D519/00
摘要： The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-b]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a nitrogen atom or a methine group; and V represents an oxygen atom or a sulfur atom. The compound of the invention is useful as therapeutical agents for various ACC-related diseases.
摘要翻译：本发明涉及通式（I）的化合物：其中Ar 1表示由选自苯，吡唑，异恶唑，吡啶，吲哚，1H-吲唑，1H-呋喃并[2,1- 1H-噻吩并[2,3-c]吡唑，苯并咪唑，1,2-苯并异恶唑，咪唑并[1,2-a]吡啶，咪唑并[1,5-a]吡啶和1H-吡唑并[ 3,4-b]吡啶，其具有Ar 2，并且任选地具有一个或两个或更多个选自R 3的取代基; R 1和R 2各自独立地表示氢原子，卤素原子，氰基，C 2 -C 6烯基，C 1 -C 6烷氧基，C 2 -C 7烷酰基，C 2 -C 7烷氧基羰基，芳烷氧基羰基，氨基甲酰基-C1-C6烷氧基，羧基-C2-C6链烯基或-Q1-N（Ra）-Q2-Rb的基团; 或任选具有取代基的C1-C6烷基; 或任选具有取代基的芳基或杂环基团; 或具有芳基或杂环基的C1-C6烷基或C2-C6烯基; T和U各自独立地表示氮原子或次甲基; V代表氧原子或硫原子。本发明的化合物可用作各种ACC相关疾病的治疗剂。

5. 发明公开

EP2116543A1 NOVEL AMINOPYRIMIDINE DERIVATIVE AS PLK1 INHIBITOR 审中-公开
标题翻译：使用氨基嘧啶衍生物ALS PLK1抑制剂
公开(公告)号：EP2116543A1
公开(公告)日：2009-11-11
申请号：EP07851126.8
申请日：2007-12-20
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： HASHIHAYATA, Takashi , KAWAMURA, Mikako , MITSUYA, Morihiro , SATOH, Yoshiyuki
IPC分类号： C07D471/04 , A61K31/506 , A61K45/00 , A61P35/00 , A61P43/00
CPC分类号： C07D471/04
摘要： The present invention relates to a compound represented by Formula [I]:

or a pharmaceutically acceptable salt or ester thereof, wherein R 1 and R 2 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, a cycloalkyl group, or the like; R 3 and R 4 , which may be the same or different, are each a hydrogen atom, a lower alkyl group, NR a R b , a phenyl group, a lower alkyl group substituted with a phenyl group, a 4- to 7-membered aliphatic heterocyclic group, a lower alkyl group substituted with a 4- to 7-membered aliphatic heterocyclic group, a 5- or 6-membered aromatic heterocyclic group, a lower alkyl group substituted with a 5- or 6-membered aromatic heterocyclic group, or the like; and R 5 is a hydrogen atom, a cyano group, a halogen atom, or a lower alkyl group.
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或酯，其中R 1和R 2可以相同或不同，分别为氢原子，低级烷基，环烷基等; R 3和R 4可以相同或不同，分别为氢原子，低级烷基，NR a R b，苯基，被苯基取代的低级烷基，4-至7- 被4至7元脂族杂环基取代的低级烷基，5或6元芳族杂环基，被5或6元芳族杂环基取代的低级烷基，或类似物; R 5为氢原子，氰基，卤素原子或低级烷基。

6. 发明公开

EP2065354A1 REACTION APPARATUS, AND REACTION METHOD 审中-公开
标题翻译： REAKTIONSAPPARAT UND REAKTIONSVERFAHREN
公开(公告)号：EP2065354A1
公开(公告)日：2009-06-03
申请号：EP07807353.3
申请日：2007-09-14
申请人： Banyu Pharmaceutical Co., Ltd.
发明人： YONEDA, Noriyuki , ODA, Yuichi , NAKANISHI, Yasuo
IPC分类号： C07B61/00 , B01J19/24 , C07C67/343 , C07C69/716
CPC分类号： C07D487/04 , B01J19/243 , B01J2219/00063 , C07C67/343 , C07C69/716
摘要： The present invention is directed at obtaining a high yield of a target substance and simultaneously securing high productivity.
A reaction apparatus 10 has: a main flow channel 12 having an inner diameter of 3 mm, in which a raw material M 1 flows; an introduction flow channel 14 in which a raw material M 2 that causes a chemical reaction with the raw material M 1 flows; and five branch introduction flow channels 16a to 16e which are branched from the introduction flow channel 14 and introduce the raw material M 2 to the main flow channel 12, at predetermined introduction points 12o to 12s in the main flow channel 12. Here, in the main flow channel 12, the flow channel lengths of the flow channels 12b to 12d between adjacent introduction points 12p to 12s are not longer than those of the flow channels 12a to 12c between the next previous adjacent introduction points 12o to 12r in a flow direction of the raw material M 1 . At least one length of the flow channels 12b to 12d between the adjacent introduction points 12p to 12s is shorter than lengths of the flow channels 12a to 12c between previous adjacent introduction points 12o to 12r in the flow direction of the raw material M 1 .
摘要翻译：本发明涉及获得高产率的目标物质并同时确保高生产率。反应装置10具有：原料M 1流入的内径为3mm的主流路12; 导入与原料M 1发生化学反应的原料M 2的导入流路14; 以及从导入流路14分支并将原料M 2引导到主流路12的5个分支导入流路16a〜16e，在主流路12的规定的导入点12o〜12s。这里，主流路12中，相邻导入点12p〜12s之间的流路12b〜12d的流路长度不比前一相邻导入点12o〜12r之间的流路12a〜12c的流路长度在流动方向原料M 1。相邻导入点12p〜12s之间的流路12b〜12d的至少一个长度比原料M 1的流动方向上的前一相邻导入点12o〜12r之间的流路12a〜12c的长度短。

7. 发明公开

EP1944301A1 NOVEL BENZOXATHIIN DERIVATIVE 审中-公开
标题翻译：新的苯并吖庚因衍生物
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。

8. 发明授权

EP1420020B1 4-OXOIMIDAZOLIDINE-2-SPIROPIPERIDINE DERIVATIVE 有权
标题翻译： 4-OXOIMIDAZOLIDIN-2-SPIRO PIPERIDIN DERIVAT
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.

9. 发明公开

EP1878800A1 METHOD FOR EVALUATING COMPOUND USING BARLP AND SUBSTANCE FOR SUPPRESSING EATING AND BODY WEIGHT 审中-公开
标题翻译：评估过程中连接使用BARLP和物质减少，食品和体重
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。

10. 发明公开

EP1847603A1 METHOD FOR DETECTING p53 DYSFUNCTION, METHOD FOR MOLECULAR DIAGNOSIS OF CANCER AND METHOD FOR EVALUATING COMPOUND EFFECTIVE IN TREATING CANCER 审中-公开
标题翻译：方法评估在癌症的有效连接的癌症治疗的分子诊断和方法的检出p53的运行失常，方法
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。

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