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11. 发明申请

WO2006028290A1 2-MORPHOLINO-4-PYRIMIDONE COMPOUND 审中-公开
标题翻译： 2-吗啉-4-基吡啶酮化合物
公开(公告)号：WO2006028290A1
公开(公告)日：2006-03-16
申请号：PCT/JP2005/017080
申请日：2005-09-09
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-AVENTIS , WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , KOHARA, Toshiyuki , FUKUNAGA, Kenji , YOKOSHIMA, Satoshi
发明人： WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , KOHARA, Toshiyuki , FUKUNAGA, Kenji , YOKOSHIMA, Satoshi
IPC分类号： C07D413/04 , C07D413/14 , A61K31/5377 , A61P25/28
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; 1 represents a C 1 -C 12 alkyl; R 2 represents a hydrogen atom, or the like; R' represents a C 1 -C 6 alkyl or the like; q represents 0 or an integer of 1 to 7; Y represents a C 1 -C 6 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;

12. 发明申请

WO2006016707A2 PYRAZOLONE COMPOUNDS USEFUL FOR TREATMENT OF CEREBROVASCULAR DISORDERS ASSOCIATED WITH ISCHEMIC STROKE 审中-公开
标题翻译：用于治疗与ISCHEMIC STROKE相关的脑血管疾病的吡唑啉酮化合物
公开(公告)号：WO2006016707A2
公开(公告)日：2006-02-16
申请号：PCT/JP2005/014969
申请日：2005-08-10
申请人： MITSUBISHI PHARMA CORPORATION , 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 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：一种用于治疗与缺血性脑卒中相关的脑血管疾病不足的药物，其包含药学有效量的结构式（I）的吡唑啉酮化合物或其药学上可接受的盐或其假多晶型物，以可控剂量施用，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。

13. 发明申请

WO2004089341A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2004089341A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003656
申请日：2004-04-06
申请人： NOVARTIS AG , NOVARTIS PHARMA GMBH , MITSUBISHI PHARMA CORPORATION , OOMURA, Tomoyuki , PUDIPEDDI, Madhusudhan , ROYCE, Alan, Edward , RUEGGER, Colleen , SASAKI, Masaki , TAMURA, Tokuhiro
发明人： OOMURA, Tomoyuki , PUDIPEDDI, Madhusudhan , ROYCE, Alan, Edward , RUEGGER, Colleen , SASAKI, Masaki , TAMURA, Tokuhiro
IPC分类号： A61K9/20
CPC分类号： A61K31/145 , A61K9/0053 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K31/135 , A61K31/137 , A61K31/138 , A61K45/06 , A61K47/10 , A61K47/26 , A61K2300/00
摘要： A solid pharmaceutical composition suitable for oral administration, comprising: (a) S 1 P receptor agonist; and (b) a sugar alcohol.
摘要翻译：一种适用于口服给药的固体药物组合物，其包含：（a）S 1 P受体激动剂; 和（b）糖醇。

14. 发明申请

WO2004085408A1 2, 3, 6-TRISUBSTITUTED-4-PYRIMIDONE DERIVATIVES 审中-公开
标题翻译： 2,3,6-取代的4-吡啶酮衍生物
公开(公告)号：WO2004085408A1
公开(公告)日：2004-10-07
申请号：PCT/JP2004/004320
申请日：2004-03-26
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-SYNTHELABO , WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , YOKOSHIMA, Satoshi , USUI, Yoshihiro , OKUYAMA, Masahiro , SHODA, Aya , ARITOMO, Keiichi , KOHARA, Toshiyuki , FUKUNAGA, Kenji
发明人： WATANABE, Kazutoshi , UEHARA, Fumiaki , HIKI, Shinsuke , YOKOSHIMA, Satoshi , USUI, Yoshihiro , OKUYAMA, Masahiro , SHODA, Aya , ARITOMO, Keiichi , KOHARA, Toshiyuki , FUKUNAGA, Kenji
IPC分类号： C07D239/47
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C 1 -C 12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C 1 -C 8 alkyl group, an optionally partially hydrogenated C 6 -C 10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each Y independently represents a halogen atom, a hydroxy group, a cyano group, a C 1 -C 6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C 2 -C 6 alkylene group.
摘要翻译：具有由式（I）表示的tau蛋白激酶1抑制活性的嘧啶酮衍生物或其盐或其溶剂合物或其水合物; 可用于疾病的预防和/或治疗性治疗，例如神经变性疾病（例如阿尔茨海默病）; 其中Q表示CH或氮原子; R代表C1-C12烷基; 式（I）的环表示哌嗪环或哌啶环; 每个X独立地表示C1-C8烷基，任选部分氢化的C 6 -C 10芳基环，茚满环等; m表示1〜3的整数，每个Y独立地表示卤素原子，羟基，氰基，C1-C6烷基等; n表示0〜8的整数，当X和Y或两个Y基团连接在同一个碳原子上时，它们可以彼此结合形成C 2 -C 6亚烷基。

15. 发明申请

WO2004083210A1 SUBSTITUTED 8-PERFLUOROALKYL-6,7,8,9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES 审中-公开
标题翻译：取代的8-全氟代苄基-6,7,8,9-四氢吡啶并[1,2-a]吡咯烷-4-酮衍生物
公开(公告)号：WO2004083210A1
公开(公告)日：2004-09-30
申请号：PCT/EP2004/004013
申请日：2004-03-19
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D487/04
CPC分类号： A61K31/519 , C07D487/04
摘要： The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof, wherein: X represents two hydrogen atom, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted; R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted; R3 represents a hydrogen atour or a C 1-6 alkyl group; R4 represents a C 1-2 perhalogenated alkyl group or a C 1-3 halogenated alkyl group; R5 represents a hydrogen atour; a C 1-6 alkyl group or a halogen atom; n represents 0 to 3; and p+q=0 to 3. 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 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表示两个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2表示苯基或萘环; 苯基和萘环任选被取代; R 3表示氢环绕或C 1-6烷基; R4表示C1-2全卤代烷基或C1-3卤代烷基; R5表示氢气环绕; C 1-6烷基或卤素原子; n表示0〜3; 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的异常活性引起的神经变性疾病，例如作为阿尔茨海默病。

16. 发明申请

WO2004082577A2 8-SUBSTITUTED-6, 7, 8, 9-TETRAHYDROPYRIMIDO[1,2-a] PYRIMIDIN-4-ONE DERIVATIVES 审中-公开
标题翻译： 8-取代-6,7,8,9-四氢嘧啶并[1,2-a]吡啶并[4-a]衍生物
公开(公告)号：WO2004082577A2
公开(公告)日：2004-09-30
申请号：PCT/EP2004/004014
申请日：2004-03-19
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： A61K
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 represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted; R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted; R3 represents a hydrogen atom or a C 1-6 alkyl group; R4 represents a phenyl group, a pyridinyl group or a naphthalene ring, the groups and the ring being optionally substituted; R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; n represents 0 to 3; and p+q=0-3. 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 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表示两个氢原子，硫原子，氧原子或C 1-2烷基和氢原子; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2表示苯基或萘环; 苯基和萘环任选被取代; R3表示氢原子或C1-6烷基; R4表示苯基，吡啶基或萘环，所述基团和所述环任选被取代; R5表示氢原子，C1-6烷基或卤素原子; n表示0〜3; 和p + q = 0-3。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。

17. 发明申请

WO2004078760A1 SUBSTITUTED 8'-PYRIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE AND 8'-PYRIMIDINYL-DIHYDROSPIRO-[CYCLOALKYL]-PYRIMIDO [1,2-a] PYRIMIDIN-6-ONE DERIVATIVES AND THEIR USE AGAINST NEUROGENERATIVE DISEASES 审中-公开
标题翻译：取代的8'-吡啶基 - 二氢吡喃并[环己基] - 吡咯并[1,2-a]吡啶二酮-6-酮和8'-吡啶二基 - 二氢吡啶并[环己基] - 吡咯并[1,2-a]嘧啶-6-酮衍生物及其对抗神经病毒性疾病的使用
公开(公告)号：WO2004078760A1
公开(公告)日：2004-09-16
申请号：PCT/EP2004/003051
申请日：2004-03-05
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , GEORGE, Pascal , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
发明人： GEORGE, Pascal , LOCHEAD, Alistair , SAADY, Mourad , SLOWINSKI, Franck , YAICHE, Philippe
IPC分类号： C07D487/04
CPC分类号： C07D487/10
摘要： The invention relates to a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, 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; m represents 1 to 4 n represent 0 to 3 p represents 0 to 2 q represents 0 to 2, p+ q being inferior to 4. 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 disease.
摘要翻译：本发明涉及由式（I）表示的二氢螺环 - [环烷基] - 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 1-2烷基和氢原子 ; Y表示键，羰基，任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环，该环任选被取代; R2表示苯环或萘环; 所述环任选被取代; R3表示氢原子，C1-6烷基或卤素原子; m表示1〜4个n表示0〜3个p表示0〜2个q表示0〜2，p + q优于4.本发明还涉及含有上述衍生物或其盐作为有效成分的药物，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。

18. 发明申请

WO2003072580A1 1-[ALKYL], 1-[HETEROARYL)ALKYL] AND 1-[ARYL)ALKYL]-7-(PYRIMIDIN-4-YL)-IMADAZO[1,2-a]PYRIMIDIN-5(1H)-ONE DERIVATIVES 审中-公开
标题翻译： 1- [烷基] -1- [异丁基]烷基]和1- [芳基]烷基] -7-（吡咯烷-4-基） - 咪唑并[1,2-a]吡啶-5（1H） - 酮衍生物
公开(公告)号：WO2003072580A1
公开(公告)日：2003-09-04
申请号：PCT/EP2003/002652
申请日：2003-02-26
申请人： SANOFI-SYNTHELABO , MITSUBISHI PHARMA CORPORATION , LOCHEAD, Alistair , SAADY, Mourad , YAICHE, Philippe
发明人： LOCHEAD, Alistair , SAADY, Mourad , YAICHE, Philippe
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: R 1 wherein X represents a bond, an ethenylene group, an ethenylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R 1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R 2 represents a C 1-6 alkyl group, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted; and n represents 0 to 3. 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：本发明涉及由式（I）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐：R1其中X表示键，亚乙烯基，亚乙烯基，任选取代的亚甲基; 羰基，氧原子，硫原子，磺酰基，亚砜基或任选取代的氮原子; R1表示任选取代的2,4或5-嘧啶基; R2表示C1-6烷基，C1-2全卤代烷基，C1-3卤代烷基，苄基，苯环，萘环，5,6,7,8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或咪唑环，所述苄基和所述环任选被取代; 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的异常活性引起的神经变性疾病，例如阿尔茨海默氏症疾病。

19. 发明申请

WO2003027080A1 3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES 审中-公开
标题翻译： 3-取代-4-吡啶酮衍生物
公开(公告)号：WO2003027080A1
公开(公告)日：2003-04-03
申请号：PCT/JP2002/009684
申请日：2002-09-20
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-SYNTHELABO , UEHARA, Fumiaki , ARITOMO, Keiichi , SHODA, Aya , HIKI, Shinsuke , OKUYAMA, Masahiro , USUI, Yoshihiro , OOIZUMI, Mitsuru , WATANABE, Kazutoshi
发明人： UEHARA, Fumiaki , ARITOMO, Keiichi , SHODA, Aya , HIKI, Shinsuke , OKUYAMA, Masahiro , USUI, Yoshihiro , OOIZUMI, Mitsuru , WATANABE, Kazutoshi
IPC分类号： C07D239/46
CPC分类号： A61K31/535 , C07D239/34 , C07D239/47 , C07D239/56 , C07D401/04 , 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 R 1 represents a C 1 -C 12 alkyl group which may be substituted;R represents, for example, a group represented by the following formula (II):wherein R 2 and R 3 independently represent a hydrogen atom or a C 1 -C 8 alkyl group; R 4 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，或其对tau蛋白激酶1具有抑制活性的溶剂合物或其水合物：其中R b1表示C <1 / 可以被取代的烷基; R表示例如由下式（II）表示的基团：其中R s2>和R > 3 独立地表示氢原子或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，或可以具有取代基的任意取代的杂环至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。

20. 发明申请

WO2002062795A2 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：WO2002062795A2
公开(公告)日：2002-08-15
申请号：PCT/JP2002/000829
申请日：2002-02-01
申请人： MITSUBISHI PHARMA CORPORATION , 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： 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-3β), 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。

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