公开(公告)号：US20130217723A1

公开(公告)日：2013-08-22

申请号：US13849733

申请日：2013-03-25

申请人： Nathalie TACCOEN

发明人： Francois SCHUTZE ,  Suzy CHARBIT ,  Herve FICHEUX ,  Michel HOMERIN ,  Alain TACCOEN ,  Yoshio INABA

IPC分类号： A61K31/444 ,  A61K31/415 ,  A61K31/192 ,  A61K31/196

CPC分类号： A61K31/444 ,  A61K31/192 ,  A61K31/196 ,  A61K31/365 ,  A61K31/405 ,  A61K31/407 ,  A61K31/415 ,  A61K31/4439 ,  A61K31/5415 ,  A61K31/616 ,  A61K31/635 ,  A61K45/06 ,  A61K2300/00

摘要： The invention relates to a novel pharmaceutical combination. The inventive pharmaceutical composition comprises a combination of tenatoprazole and one or more anti-inflammatory agents selected from non-steroid anti-inflammatory agents and cyclooxygenase-2 inhibitors. The invention is suitable for the treatment of painful and inflammatory manifestations.

摘要翻译： 本发明涉及一种新颖的药物组合。 本发明的药物组合物包含替硝唑和一种或多种选自非类固醇抗炎剂和环加氧酶-2抑制剂的抗炎剂的组合。 本发明适用于治疗疼痛和炎症表现。

公开(公告)号：US20090124618A1

公开(公告)日：2009-05-14

申请号：US11573476

申请日：2005-09-09

申请人： Kazutoshi WATANABE ,  Fumiaki UEHARA ,  Shinsuke HIKI ,  Toshiyuki KOHARA ,  Kenji FUKUNAGA ,  Satoshi YOKOSHIMA

发明人： Kazutoshi WATANABE ,  Fumiaki UEHARA ,  Shinsuke HIKI ,  Toshiyuki KOHARA ,  Kenji FUKUNAGA ,  Satoshi YOKOSHIMA

IPC分类号： A61K31/5377 ,  C07D413/14

CPC分类号： C07D413/14

摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein X represents CH or N; represents a C1-C12 alkyl; R2 represents a hydrogen atom, or the like; R′ represents a C1-C6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C1-C6 alkyl or the like; p represents 0 or an integer of 1 to 5; R represents a 2,3-dihydroindolyl 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，其光学活性异构体或其药学上可接受的盐：其中X表示CH或N; 表示C1-C12烷基; R2表示氢原子等; R'表示C1-C6烷基等; q表示0或1〜7的整数， Y表示C1-C6烷基等; p表示0或1〜5的整数， R表示2,3-二氢吲哚基等，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。

公开(公告)号：US07427615B2

公开(公告)日：2008-09-23

申请号：US10489606

申请日：2002-09-20

申请人： Fumiaki Uehara ,  Keiichi Aritomo ,  Aya Shoda ,  Shinsuke Hiki ,  Masahiro Okuyama ,  Yoshihiro Usui ,  Mitsuru Ooizumi ,  Kazutoshi Watanabe ,  Koichi Yamakoshi

发明人： Fumiaki Uehara ,  Keiichi Aritomo ,  Aya Shoda ,  Shinsuke Hiki ,  Masahiro Okuyama ,  Yoshihiro Usui ,  Mitsuru Ooizumi ,  Kazutoshi Watanabe ,  Koichi Yamakoshi

IPC分类号： C07D401/04 ,  C07D401/14 ,  A61K31/505

CPC分类号： C07D401/04 ,  C07D239/34 ,  C07D239/47 ,  C07D239/56 ,  C07D401/14 ,  C07D413/14

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof having inhibitory activity against tau protein kinase 1: wherein R1 represents a C1-C12 alkyl group which may be substituted; R represents, for example, a group represented by the following formula (II): wherein R2 and R3 independently represent a hydrogen atom or a C1-C8 alkyl group; R4 represents a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

摘要翻译： 由式（I）表示的嘧啶酮衍生物或其盐，或其溶剂合物或其水合物对tau蛋白激酶1具有抑制活性：其中R 1表示C 1〜 可以被取代的C 1 -C 12烷基; R表示例如由下式（II）表示的基团：其中R 2和R 3独立地表示氢原子或C 1〜 C 1 -C 8烷基; R 4表示可以被取代的苯环，可以被取代的萘环，可以被取代的茚满环，可被取代的四氢萘环，或具有1个的任选取代的杂环 至4个选自氧原子，硫原子和氮原子的杂原子，并且总共具有5至10个环构成原子。

公开(公告)号：US07396915B2

公开(公告)日：2008-07-08

申请号：US10546594

申请日：2004-02-27

申请人： Saiko Hosokawa ,  Masahiko Aoki ,  Yoko Hirakawa ,  Seima Itami ,  Hiroe Umeki ,  Yoshiro Saikawa ,  Koichiro Kumai ,  Kazumasa Fukuda

发明人： Saiko Hosokawa ,  Masahiko Aoki ,  Yoko Hirakawa ,  Seima Itami ,  Hiroe Umeki ,  Yoshiro Saikawa ,  Koichiro Kumai ,  Kazumasa Fukuda

IPC分类号： C07K16/00

CPC分类号： G01N33/57442 ,  A61K47/6857 ,  A61K47/6913 ,  C07K16/30 ,  C07K2317/73 ,  G01N33/57423

摘要： A novel human monoclonal antibody specifically recognizing cancer cells such as non-small cell lung cancer, pancreatic cancer and gastric cancer cells is produced by hybridomas which are obtained by fusing lymphocytes derived from a cancer tissue of a cancer patient with mouse myeloma cells. An anti-cancer drug is obtained by using the antibody alone or anchoring the antibody on the surface of a liposome containing a toxin or an anti-cancer drug encapsulated therein. More specifically, an anti-cancer drug is obtained by using an antibody, in which variable region of its heavy chain comprises the amino acid sequence of SEQ ID NO: 115 and variable region of the light chain comprises the amino acid sequence of SEQ ID NO: 117, alone or anchoring the antibody on the surface of a liposome containing a toxin or an anti-cancer drug encapsulated therein.

摘要翻译： 通过将衍生自癌症患者的癌症组织的淋巴细胞与小鼠骨髓瘤细胞融合获得的杂交瘤产生特异性识别癌细胞例如非小细胞肺癌，胰腺癌和胃癌细胞的新型人单克隆抗体。 通过单独使用抗体或将抗体锚定在包含毒素或其中的抗癌药物的脂质体的表面上来获得抗癌药物。 更具体地，通过使用抗体，其重链的可变区包含SEQ ID NO：115的氨基酸序列并且轻链的可变区包含SEQ ID NO的氨基酸序列 ：117单独或将抗体锚定在包含其中的毒素或抗癌药物的脂质体的表面上。

公开(公告)号：US07388005B2

公开(公告)日：2008-06-17

申请号：US10490136

申请日：2002-09-19

申请人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Thierry Gallet ,  Patrick Lardenois ,  Alistair Lochead ,  Séverine Marguerie ,  Alain Nedelec ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： A61K31/551 ,  A61K31/519 ,  C07D487/04 ,  A61P25/28

CPC分类号： A61K31/519 ,  A61K31/551 ,  C07D487/04

摘要： The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C1-6 alkyl group optionally substituted by a C6,10 aryloxy or a C6,10 arylamino group; a C3-6 cycloalkyl group, a C1-4 alkylthio group, a C1-4 alkoxy group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represents each independently a hydrogen atom, C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom. 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 GSK3β3 or GSK3β3 and cdk5/p25, such as Alzheimer disease.

摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐，其中：X表示两个氢原子，硫原子，氧原子或C 1-12烷基和氢 原子; y表示键，亚乙烯基，亚乙炔基，氧原子，硫原子，磺酰基，亚砜基，羰基，任选的氮原子; 或任选取代的亚甲基; R1表示任选取代的嘧啶基团; R 2可以表示任选被C 6,10芳氧基或C 6,10芳基氨基取代的C 1-6烷基; C 3-6环烷基，C 1-4烷硫基，C 1-4烷氧基，C 1 -C 4烷氧基， 1-2个全卤代烷基，C 1-3卤代烷基，苯硫基，苄基，苯环，茚满环，5,6,7， 8-四氢萘环，萘环，吡啶环，吡咯环，噻吩环，呋喃环或咪唑环; R 3和R 4各自独立地表示氢原子，C 1-6烷基，羟基，C 1-4烷氧基或卤素原子; R5表示氢原子，C 1-6烷基或卤素原子。 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β3或GSK3β3和cdk5 / p25的异常活性引起的神经变性疾病，例如阿尔茨海默病 。

公开(公告)号：US20080027078A1

公开(公告)日：2008-01-31

申请号：US11841285

申请日：2007-08-20

申请人： Antonio ALMARIO GARCIA ,  Thierry GALLET ,  Adrien Tak LI ,  Alistair LOCHEAD ,  Severine MARGUERIE ,  Alain NEDELEC ,  Mourad SAADY ,  Philippe YAICHE

发明人： Antonio ALMARIO GARCIA ,  Thierry GALLET ,  Adrien Tak LI ,  Alistair LOCHEAD ,  Severine MARGUERIE ,  Alain NEDELEC ,  Mourad SAADY ,  Philippe YAICHE

IPC分类号： A61K31/519 ,  A61P25/00 ,  A61P25/28 ,  A61P3/04

CPC分类号： C07D487/04 ,  A61K31/519

摘要： The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3β such as Alzheimer's disease.

摘要翻译： 本发明涉及由式（I）表示的嘧啶酮衍生物或其盐的治疗用途：其中X，Y，R 1，R 2，m和n如本文所定义。 具体地说，包含所述衍生物或其盐作为活性成分的药物用于预防和/或治疗由诸如阿尔茨海默病的GSK3β的异常活性引起的神经变性疾病。

公开(公告)号：US07312239B2

公开(公告)日：2007-12-25

申请号：US10643404

申请日：2003-08-18

申请人： Takayuki Tanaka ,  Tatsuhiko Mori

发明人： Takayuki Tanaka ,  Tatsuhiko Mori

IPC分类号： A61K31/4152 ,  A61K31/381 ,  A61K31/341

CPC分类号： A61K31/4152

摘要： An object of the present invention is to provide a medicament and method which is useful for prevention and/or therapy of arterial wall injury. According to the present invention, there is provided a method for prevention and/or therapy of arterial wall injury which comprises a step of administering the pyrazolone derivative represented by the following formula (I) or the physiologically acceptable salt thereof, or the hydrate or solvate thereof in a preventively or therapeutically effective amount to mammals including humans: wherein R1 represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R1 and R2 are combined with each other to represent an alkylene group; and R3 represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.

摘要翻译： 本发明的目的是提供一种可用于预防和/或治疗动脉壁损伤的药物和方法。 根据本发明，提供了一种预防和/或治疗动脉壁损伤的方法，包括给予由下式（I）表示的吡唑啉酮衍生物或其生理学上可接受的盐，或其水合物或溶剂化物 其具有预防或治疗有效量的哺乳动物包括人：其中R 1表示氢原子，芳基，烷基或烷氧基羰基烷基; R 2表示氢原子，芳氧基，芳基巯基，烷基或羟烷基; 或R 1和R 2彼此结合以表示亚烷基; R 3表示氢原子，烷基，环烷基，羟基烷基，苄基，萘基，苯基或被1〜3个取代基取代的苯基 由烷基，烷氧基，羟基烷基，烷氧基羰基，烷基巯基，烷基氨基，二烷基氨基，卤素原子，三氟甲基，羧基，氰基， 羟基，硝基，氨基和乙酰胺基。

公开(公告)号：US20070270589A1

公开(公告)日：2007-11-22

申请号：US10580283

申请日：2004-11-26

申请人： Hiroshi Iwamura ,  Takashi Naka

发明人： Hiroshi Iwamura ,  Takashi Naka

IPC分类号： C07D239/72

CPC分类号： C07D239/94

摘要： Object: To offer novel quinazoline derivatives, which are useful as intermediates in the production of agents for the treatment and prevention of cancer, and an industrially useful method for manufacture of the same. Means: The quinazoline derivative represented by general formula (I) below: (in the formula, each of the symbols is the same as described in the specification) or a salt thereof, or a hydrate or solvate thereof, and a method for using the same to produce novel quinazoline derivatives.

摘要翻译： 目的：提供新颖的喹唑啉衍生物，其可用作生产用于治疗和预防癌症的药剂的中间体，以及用于制备癌症的工业上有用的方法。 方法：由通式（I）表示的喹唑啉衍生物：（式中各符号与说明书中所述相同）或其盐或其水合物或溶剂合物，以及使用 同样产生新的喹唑啉衍生物。

公开(公告)号：US07247638B2

公开(公告)日：2007-07-24

申请号：US11225218

申请日：2005-09-13

申请人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

发明人： Alistair Lochead ,  Mourad Saady ,  Franck Slowinski ,  Philippe Yaiche

IPC分类号： C07D487/04 ,  A61K31/519

CPC分类号： A61K31/519 ,  C07D487/04

摘要： The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. 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 GSK3β, such as Alzheimer's disease.

摘要翻译： 本发明涉及由式（I）表示的取代嘧啶酮衍生物或其盐：其中X，Y，R 1，R 2，R 3，R 4，R 5，n，p和q如本文所定义。 本发明还涉及包含所述衍生物或其盐作为活性成分的药物，其用于预防和/或治疗由GSK3β如阿尔茨海默病异常活动引起的神经变性疾病。

公开(公告)号：US20070142409A1

公开(公告)日：2007-06-21

申请号：US10538766

申请日：2003-12-12

申请人： Yoshihiro Usui ,  Masahiro Okuyama ,  Tokushi Hanano

发明人： Yoshihiro Usui ,  Masahiro Okuyama ,  Tokushi Hanano

IPC分类号： A61K31/513 ,  C07D403/14

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

摘要： A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group which may be substituted; R2 represents a C?1#191-C?8#191 alkyl group which may be substituted, a benzene ring which may be substituted, a naphthalene ring which may be substituted, an indan ring which may be substituted, a tetrahydronaphthalene ring which may be substituted, or an optionally substituted heterocyclic ring having 1 to 4 hetero atoms selected from the group consisting of oxygen atom, sulfur atom, and nitrogen atom, and having 5 to 10 ring-constituting atoms in total.

摘要翻译： 用作tau蛋白激酶1抑制剂的由式（I）表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物：其中X表示CH或氮原子; R 1表示可被取代的C 1〜1 191〜C 12〜191烷基; R 2表示可以被取代的C 1〜191-C 18〜191烷基，可被取代的苯环，可被取代的萘环，可以被取代的萘环 可被取代的四氢萘环，或具有1-4个选自氧原子，硫原子和氮原子的杂原子的任意取代的杂环，并且总共具有5至10个环构成原子 。