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1. 发明申请

WO2006036015A2 PYRIMIDONE COMPOUND 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2006036015A2
公开(公告)日：2006-04-06
申请号：PCT/JP2005018497
申请日：2005-09-29
申请人： MITSUBISHI PHARMA CORP , SANOFI AVENTIS , WATANABE KAZUTOSHI , FUKUNAGA KENJI , KOHARA TOSHIYUKI , UEHARA FUMIAKI , HIKI SHINSUKE , YOKOSHIMA SATOSHI
发明人： WATANABE KAZUTOSHI , FUKUNAGA KENJI , KOHARA TOSHIYUKI , UEHARA FUMIAKI , HIKI SHINSUKE , YOKOSHIMA SATOSHI
IPC分类号： C07D401/04 , A61K31/505 , A61K31/506 , A61P25/28 , C07D401/14 , C07D409/14 , C07D413/14
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14 , C07D413/14
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof:wherein R 1 represents a C 1 -C 12 alkyl; R 2 represents a hydrogen atom or the like; R 3 represents a halogen or the like; q represents an integer of 1 to 7; R 4 represents a halogen or the like; p represents 0 or an integer of 1 to 5; R 5 represents a C 6 -C 10 aryl, a heterocycle or the like; and X represents oxygen, NH, or the like, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
摘要翻译：由式（I）表示的化合物或其光学活性异构体或其药学上可接受的盐：其中R 1表示C 1 -C 12 烷基; R 2表示氢原子等; R 3表示卤素等; q表示1〜7的整数， R 4表示卤素等; p表示0或1〜5的整数， R 5表示C 6 -C 10芳基，杂环等; X代表氧，NH等，其用于预防和/或治疗由tau蛋白激酶1多动症如神经变性疾病（例如阿尔茨海默病）引起的疾病。

2. 发明申请

WO02062795A3 DIHYDROPYRAZOLOPYRIDINE COMPOUNDS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：二氢吡唑并吡啶化合物及其药物用途
公开(公告)号：WO02062795A3
公开(公告)日：2003-05-30
申请号：PCT/JP0200829
申请日：2002-02-01
申请人： MITSUBISHI PHARMA CORP , KOHARA TOSHIYUKI , FUKUNAGA KENJI , FUJIMURA MASATAKE , HANANO TOKUSHI , OKABE HIROTAKA
发明人： KOHARA TOSHIYUKI , FUKUNAGA KENJI , FUJIMURA MASATAKE , HANANO TOKUSHI , OKABE HIROTAKA
IPC分类号： A61K31/437 , A61P3/00 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P37/04 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides dihydropyrazolopyridine compounds represented by the formula (I): wherein each symbol is as defined in the specification,optically active forms thereof, and pharmaceutically acceptable salts thereof and hydrates thereof. The compounds of the present invention show a selective and strong inhibitory activity on glycogen synthase kinase-3 beta (GSK-3 beta ), and are useful as medicaments for prevention and/or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunopotentiators.
摘要翻译：本发明提供由式（I）表示的二氢吡唑并吡啶化合物：其中每个符号如本说明书中所定义，其光学活性形式及其药学上可接受的盐及其水合物。本发明的化合物对糖原合酶激酶-3β（GSK-3β）具有选择性和强抑制活性，可用作预防和/或治疗糖尿病，糖尿病并发症和神经变性疾病或作为免疫增强剂的药物。

3. 发明申请

WO2007057790A2 SUBSTITUTED BICYCLIC PYRIMIDONE DERIVATIVES 审中-公开
标题翻译：取代的双环嘧啶酮衍生物
公开(公告)号：WO2007057790A2
公开(公告)日：2007-05-24
申请号：PCT/IB2006004046
申请日：2006-11-21
申请人： SANOFI AVENTIS , MITSUBISHI PHARMA CORP , CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
发明人： CHEREZE NATHALIE , LOCHEAD ALISTAIR , SAADY MOURAD , SLOWINSKI FRANCK , YAICHE PHILIPPE
CPC分类号： C07D239/00 , C07D471/04
摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1- 3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C- 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 2. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3ß, such as Alzheimer disease.
摘要翻译：式（I）代表的嘧啶酮衍生物或其盐，或其溶剂化物或其水合物：其中：Y代表两个氢原子，硫原子，氧原子或C 1-2- / >烷基和氢原子; Z表示键，氧原子，被氢原子或C 1〜3烷基取代的氮原子，硫原子，任选被取代的亚甲基; R1代表2,3或4-吡啶环或2,4或5-嘧啶环，所述环任选被取代; R2代表苯环或萘环; 该环任选被取代; R 3表示氢原子，C 1-6烷基或卤素原子; R4代表氢原子或C1-6烷基; R 5表示氢原子，任选取代的C 1-6烷基; R6代表氢原子，C1-6烷基或卤素原子; R 7代表氢原子或C 1-6烷基; n表示0至3; m代表0至1; o代表0至2.本发明还涉及一种药物，其包含所述衍生物或其盐作为活性成分，其用于预防和/或治疗由GSK3β的异常活性引起的神经退行性疾病，如阿尔茨海默病。

4. 发明申请

WO02062795A9 DIHYDROPYRAZOLOPYRIDINE COMPOUNDS AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译：二氢吡唑并吡啶化合物及其药物用途
公开(公告)号：WO02062795A9
公开(公告)日：2002-10-10
申请号：PCT/JP0200829
申请日：2002-02-01
申请人： MITSUBISHI PHARMA CORP , KOHARA TOSHIYUKI , FUKUNAGA KENJI , FUJIMURA MASATAKE , HANANO TOKUSHI , OKABE HIROTAKA
发明人： KOHARA TOSHIYUKI , FUKUNAGA KENJI , FUJIMURA MASATAKE , HANANO TOKUSHI , OKABE HIROTAKA
IPC分类号： A61K31/437 , A61P3/00 , A61P3/10 , A61P9/10 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/24 , A61P25/28 , A61P37/04 , A61P43/00 , C07D471/04
CPC分类号： C07D471/04
摘要： The present invention provides dihydropyrazolopyridine compounds represented by the formula (I): wherein each symbol is as defined in the specification,optically active forms thereof, and pharmaceutically acceptable salts thereof and hydrates thereof. The compounds of the present invention show a selective and strong inhibitory activity on glycogen synthase kinase-3 beta (GSK-3 beta ), and are useful as medicaments for prevention and/or treatment of diabetes, diabetic complications and neurodegenerative diseases or as immunopotentiators.
摘要翻译：本发明提供由式（I）表示的二氢吡唑并吡啶化合物：其中各符号如说明书中所定义，其光学活性形式及其药学上可接受的盐和其水合物。本发明化合物对糖原合成酶激酶-3β（GSK-3β）显示出选择性强的抑制活性，可用作预防和/或治疗糖尿病，糖尿病并发症和神经退行性疾病或作为免疫增强剂的药物。

5. 发明申请

WO02056026B1 NOVEL PROTEOME ANALYSIS METHOD AND DEVICES THEREFOR 审中-公开
标题翻译：新型保护分析方法及其设备
公开(公告)号：WO02056026B1
公开(公告)日：2002-09-19
申请号：PCT/JP0200029
申请日：2002-01-09
申请人： MITSUBISHI PHARMA CORP
发明人： TANAKA KENJI , LEE LYANG-JA , MUKAI HIROMICHI , MUNECHIKA KOJI , ARIKUNI HISASHI , SHIWA MIEKO , OCHIAI BUNGO
IPC分类号： G01N27/62 , C40B30/04 , G01N21/27 , G01N21/78 , G01N27/447 , G01N27/64 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/567 , G01N33/68 , H01J49/16 , G06F19/00
CPC分类号： C40B30/04 , G01N27/447 , G01N33/5436 , G01N33/567 , G01N33/6803 , G01N33/6845
摘要： The present invention provides a proteome analysis method including grouping a proteome into membrane proteins and compounds capable of interacting with the membrane proteins, while retaining their native structure and function, and analyzing both the membrane proteins and the compounds based on biological affinity, and devices therefor.
摘要翻译：本发明提供了一种蛋白质组分析方法，其包括将蛋白质组分成膜蛋白和能够与膜蛋白相互作用的化合物，同时保留其天然结构和功能，并且基于生物亲和力分析膜蛋白和化合物及其装置。

6. 发明申请

WO2004096208A9 COMPOSITION FOR ORAL ADMINISTRATION CONTAINING ALKYLENE DIOXYBENZENE DERIVATIVE 审中-公开
标题翻译：含有亚苄基二苯并噻吩衍生物的口服药物组合物
公开(公告)号：WO2004096208A9
公开(公告)日：2005-11-17
申请号：PCT/JP2004005864
申请日：2004-04-23
申请人： MITSUBISHI PHARMA CORP , SUZUKI TETSUYA
发明人： SUZUKI TETSUYA
IPC分类号： A61K9/16 , A61K9/50 , A61K9/52 , A61K31/36 , A61P25/22 , A61P25/24 , C07D407/12 , A61K9/14 , A61K9/48 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/32 , A61K47/34 , A61K47/38 , A61K47/42 , A61K47/44
CPC分类号： A61K31/36 , A61K9/1617 , A61K9/5026 , C07D407/12
摘要： The present invention relates to a composition for oral administration containing an alkylenedioxybenzene derivative represented by the general formula (I): (wherein m represents an integer of 2 to 5, and n represents an integer of 1 to 3) or an acid addition salt thereof, which allows for duration of the drug concentration in plasma. By dispersing a compound represented by the general formula (I) in a matrix containing a synthetic polymer and/or waxes, a safe and useful pharmaceutical preparation for oral administration having the stable drug releasing property in a living body was obtained.
摘要翻译：本发明涉及含有通式（I）表示的亚烷基二氧基苯衍生物或其酸加成盐（式中，m表示2〜5的整数，n表示1〜3的整数）的口服用组合物，，其允许血浆中药物浓度的持续时间。通过将由通式（I）表示的化合物分散在含有合成聚合物和/或蜡的基质中，获得了在生物体内具有稳定的药物释放性的口服安全有用的药物制剂。

7. 发明申请

WO2005014525A3 BI-ARYL COMPOUND HAVING IMMUNOSUPPRESSIVE ACTIVITY 审中-公开
标题翻译：双芳基化合物具有免疫抑制活性
公开(公告)号：WO2005014525A3
公开(公告)日：2005-04-21
申请号：PCT/JP2004011860
申请日：2004-08-12
申请人： MITSUBISHI PHARMA CORP , KOHARA TOSHIYUKI , ADACHI KUNITOMO , TANAKA YOSHIHITO , SUGAHARA KUNIO , TOMATSU AYUMI , KIUCHI MASATOSHI
发明人： KOHARA TOSHIYUKI , ADACHI KUNITOMO , TANAKA YOSHIHITO , SUGAHARA KUNIO , TOMATSU AYUMI , KIUCHI MASATOSHI
IPC分类号： A61P37/06 , C07C215/28 , C07C217/54 , C07C217/64 , C07C225/16 , C07D231/12 , C07D257/04 , C07D277/36 , C07D333/20 , C07D333/22 , C07F9/09 , C07F9/6553 , A61K31/137 , A61K31/381 , A61K31/415 , A61K31/426 , A61K31/661
CPC分类号： C07D231/12 , C07C215/28 , C07C217/64 , C07C225/16 , C07D257/04 , C07D277/36 , C07D333/20 , C07D333/22 , C07F9/094 , C07F9/655345
摘要： The invention is directed to a bi-aryl compound having a unique immunomodulating activity, a process for a preparation thereof, a pharmaceutical composition containing the same, and a method of preventing or treating disorders or diseases mediated by T lymphocytes by administering the compound to a subject in need of treatment.
摘要翻译：本发明涉及具有独特免疫调节活性的双芳基化合物，其制备方法，含有该化合物的药物组合物，以及预防或治疗由T淋巴细胞介导的病症或疾病的方法，需要治疗的主体。

8. 发明申请

WO0219993A8 GRANULAR PREPARATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：用于口腔管理的格式准备
公开(公告)号：WO0219993A8
公开(公告)日：2003-11-13
申请号：PCT/JP0107697
申请日：2001-09-05
申请人： MITSUBISHI PHARMA CORP , NOMURA TATSUO
发明人： NOMURA TATSUO
IPC分类号： A61K9/36 , A61K9/50 , A61K31/74 , A61K31/787 , A61K47/38
CPC分类号： A61K9/5073 , A61K9/5042 , A61K9/5047 , A61K31/74 , A61K31/787
摘要： Granular preparations for oral administration wherein an anion exchange resin is contained as the active ingredient and cores of 3 to 4 mm in diameter are coated with a water-soluble polymeric cellulose as an inner coating layer and an aqueous dispersion of ethyl cellulose as an outer coating layer. Owing to this constitution, these preparations show no sliminess characteristic to cellulose, are free from adhesion of grains in the mouth and have a favorable texture at administration without any unacceptable feel as in large tablets.
摘要翻译：作为活性成分含有阴离子交换树脂的粒状制剂，直径为3〜4mm的核心，以作为内层的水溶性聚合纤维素和作为外涂层的乙基纤维素水分散体层。由于这种结构，这些制剂表现出纤维素不具有粘性，在口中没有颗粒附着，并且在大片剂中具有良好的施用质地，没有任何不可接受的感觉。

9. 发明申请

WO2007011065A3 INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF 审中-公开
标题翻译：用于合成药物的中间体化合物及其生产方法
公开(公告)号：WO2007011065A3
公开(公告)日：2007-08-16
申请号：PCT/JP2006314932
申请日：2006-07-21
申请人： MITSUBISHI PHARMA CORP , SANOFI AVENTIS , OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
发明人： OKUYAMA MASAHIRO , UEHARA FUMIAKI , IWAMURA HIROSHI , WATANABE KAZUTOSHI
IPC分类号： C07D265/30 , C07D265/32
CPC分类号： C07D265/30 , C07D265/32
摘要： The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.
摘要翻译：本发明涉及由式10表示的光学活性吗啉化合物的制备方法，其包括以下步骤：其中各符号如说明书中所定义。本发明还涉及由式55表示的化合物的制备方法，其包括以下步骤：其中每个符号如说明书中所定义。根据本发明的制备方法，可以使用作为2-（2-芳基吗啉）合成原料的重要的光学活性2-芳基取代的吗啉化合物和3-氧代-3-（嘧啶-4-基）丙酸酯 -4-基）-1-甲基-1H- [4,4']联嘧啶基-6-酮，可用作阿尔茨海默病等的治疗药物，具有τ蛋白激酶1抑制活性，通过工业上有利的方法获得产量。

10. 发明申请

WO2006016707A3 PYRAZOLONE COMPOUNDS FOR TREATING CEREBROVASCULAR DISORDERS 审中-公开
标题翻译：用于治疗脑血管病的吡唑啉酮化合物
公开(公告)号：WO2006016707A3
公开(公告)日：2006-09-14
申请号：PCT/JP2005014969
申请日：2005-08-10
申请人： MITSUBISHI PHARMA CORP , YUKI SATOSHI , NAKANO TAKUMA , SUZUKI HIROKO
发明人： YUKI SATOSHI , NAKANO TAKUMA , SUZUKI HIROKO
IPC分类号： A61K31/4152 , A61P25/00
CPC分类号： A61K31/4152 , A61K2039/545
摘要： A drug including edaravone for the treatment of cerebrovascular disorders associated with insufficient cerebral circulation such as ischemic stroke, which comprises a pharmaceutically effective amount of a pyrazolone compound of structural Formula (I): or a pharmaceutically acceptable salt thereof, or a pseudo-polymorphic form thereof, administered at a controlled dose so that the plasma concentration of unchanged form is kept constant for a predetermined period of time and so that the compound may exhibit a higher effect.
摘要翻译：一种药物，包括依达拉奉治疗与缺血性脑卒中相关的脑血管不良相关的脑血管障碍，其包含药学上有效量的结构式（I）的吡唑啉酮化合物或其药学上可接受的盐或假多形态其以受控剂量施用，使得不变形式的血浆浓度在预定时间段内保持恒定，并且使得化合物可以表现出更高的效果。

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