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1. 发明申请

WO2008078837A1 2-SUBSTITUTED-6-HETEROCYCLIC PYRIMIDONE DERIVATIVES AS TAU PROTEIN KINASE 1 INHBITORS 审中-公开
标题翻译： 2-取代的6-杂环基吡啶酮衍生物作为TAU蛋白激酶1抑制剂
公开(公告)号：WO2008078837A1
公开(公告)日：2008-07-03
申请号：PCT/JP2007/075380
申请日：2007-12-26
申请人： MITSUBISHI TANABE PHARMA CORPORATION , SANOFI-AVENTIS , WATANABE, Kazutoshi , KOHARA, Toshiyuki , FUKUNAGA, Kenji , UEHARA, Fumiaki
发明人： WATANABE, Kazutoshi , KOHARA, Toshiyuki , FUKUNAGA, Kenji , UEHARA, Fumiaki
IPC分类号： C07D413/14 , A61K31/513 , A61P25/00 , A61P19/00 , A61P33/00 , A61P35/00 , A61P3/00
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 each R 1 represents hydrogen atom or the like; X represents oxygen atom or the like; A represents a C 3 -C 7 cycloalkyl group, a C 6 -C 10 aryl group or a heterocyclic group; R 6 represents a halogen atom or the like; s represents 0 or an integer of 1 to 5; Q represents a pyridine ring which may be substituted or pyrimidine ring; and R 2 represents hydrogen atom or the like, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 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：其中每个R 1表示氢原子等; X表示氧原子等; A表示C 3 -C 7环烷基，C 6 -C 10芳基或杂环组; R 6表示卤素原子等; s表示0或1〜5的整数， Q表示可以被取代或嘧啶环的吡啶环; R 2表示氢原子等，其用于预防和/或治疗由tau蛋白激酶1的异常活性（例如神经变性疾病（例如阿尔茨海默病））引起的疾病。

2. 发明申请

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。

3. 发明申请

WO2005014525A2 BI-ARYL COMPOUND HAVING IMMUNOSUPPRESSIVE ACTIVITY 审中-公开
标题翻译：具有免疫抑制活性的双亚甲基化合物
公开(公告)号：WO2005014525A2
公开(公告)日：2005-02-17
申请号：PCT/JP2004/011860
申请日：2004-08-12
申请人： Mitsubishi Pharma Corporation , 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： C07C215/00
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：本发明涉及一种具有独特的免疫调节活性的双芳基化合物，其制备方法，含有该双组分化合物的药物组合物，以及通过将化合物给予该T细胞来预防或治疗由T淋巴细胞介导的疾病或疾病的方法需要治疗。

4. 发明申请

WO1998029397A1 FUSED PYRIMIDINE COMPOUNDS AND MEDICINAL USE THEREOF 审中-公开
标题翻译：熔融吡嗪化合物及其药物用途
公开(公告)号：WO1998029397A1
公开(公告)日：1998-07-09
申请号：PCT/JP1997004782
申请日：1997-12-22
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , TANAKA, Hiroshi , SEIO, Koji , KIMURA, Koreichi , MINOGUCHI, Masanori , UEHATA, Masayoshi , KOHARA, Toshiyuki , OHASHI, Yoshitaka , MORIO, Yasunori , YAMAGAMI, Keiji
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07D239/94
CPC分类号： C07D487/04 , C07D239/94 , C07D239/95 , C07D495/04
摘要： Fused pyrimidine compounds represented by general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, drugs containing the compounds of general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, and medicinal compositions containing the compounds of general formula (I), pharmaceutically acceptable salts thereof or hydrates of the same, wherein each symbol is as defined in the specification. Because of having an excellent CRF receptor antagonism, these compounds are useful as drugs, in particular, remedies for human depression, eating disturbance including dietary negativism and overeating, Alzheimer's disease, schizophrenia, Parkinson's disease, Huntington's chorea, amyotrophic lateral sclerosis, mania, psychophysiologic disorder, senile dementia, panic disorder, cerebral attack, inflammation in autoimmune diseases such as rheumatoid arthritis, pain, obesity, Gilles de la Tourette's disease, alcohol dependence, climacteric disturbance and premenstrual tension syndrome, cardiac circulatory drugs such as hypotensive drugs, immunopotentiators, immunosuppressors and drugs for improving the conditions of patients in intensive care units (ICU).
摘要翻译：由通式（I）表示的稠合嘧啶化合物，其药学上可接受的盐或其水合物，含有通式（I）的化合物的药物，其药学上可接受的盐或其水合物，以及含有一般化合物的药物组合物式（I），其药学上可接受的盐或其水合物，其中每个符号如说明书中所定义。由于具有优异的CRF受体拮抗作用，这些化合物可用作药物，特别是用于人类抑郁症，饮食障碍，饮食消极反应和暴饮暴食，阿尔茨海默病，精神分裂症，帕金森病，亨廷顿舞蹈病，肌萎缩性侧索硬化，躁狂症，心理生理疾病，老年性痴呆，恐慌症，脑部发作，自身免疫性疾病如类风湿性关节炎，疼痛，肥胖，杜伊勒图雷特氏病，酒精依赖性，更年期障碍和经前期紧张综合征，心脏循环药物如降血压药物，免疫增强剂，免疫抑制剂和药物，用于改善重症监护病房（ICU）患者的病情。

5. 发明申请

WO1996006068A1 BENZENE COMPOUND AND MEDICINAL USE THEREOF 审中-公开
标题翻译：苯并噻唑类化合物及其药物用途
公开(公告)号：WO1996006068A1
公开(公告)日：1996-02-29
申请号：PCT/JP1995001654
申请日：1995-08-22
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , FUJITA, Tetsuro , ADACHI, Kunitomo , KOHARA, Toshiyuki , KIUCHI, Masatoshi , CHIBA, Kenji , TESHIMA, Koji , MISHINA, Tadashi
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD.
IPC分类号： C07C215/28
CPC分类号： C07C217/64 , C07C215/28 , C07C215/30 , C07C215/56 , C07C217/72 , C07C219/22 , C07C225/16 , C07C233/18 , C07C233/31 , C07C233/36 , C07C233/73 , C07C271/16 , C07C271/18 , C07C2601/02
摘要： A benzene compound represented by general formula (I) (wherein each symbol is as defined in the specification), an optical isomer or salt thereof, a medicinal composition containing the same, and an immunosuppressant containing the same as the active ingredient. The compound, isomer or salt has an excellent immunosuppressive effect and is useful as an inhibitor for the rejection reaction occurring in organ or bone marrow transplantation and as a preventive or remedy for articular rheumatism, atopic eczema (dermatitis), Behcet's disease, uveal disease, systemic lupus erythematosus, Sjögren's syndrome, multiple sclerosis, myasthenia gravis, type I diabetes, endocrine ophthalmopathy, primary biliary cirrhosis, Crohn's disease, glomerulonephritis, sarcoidosis, psoriasis, pemphigus, aplastic anemia, idiopathic thrombocytopenic purpura, allergy, polyarteritis nodosa, progressive systemic sclerosis, mixed connective tissue disease, aortitis syndrome, polymyositis, dermatomyositis, Wegener's granuloma, ulcerative colitis, active chronic hepatitis, autoimmune hemolytic anemia, Evans' syndrome, bronchial asthma, and pollinosis. It is useful also as an antifungal agent and hair growth stimulant.
摘要翻译：由通式（I）表示的苯化合物（其中各符号如说明书中所定义），光学异构体或其盐，含有该化合物的药物组合物和含有该有机成分的免疫抑制剂。化合物，异构体或盐具有优异的免疫抑制作用，可用作器官或骨髓移植中发生的排斥反应的抑制剂，并且作为关节风湿病，特应性湿疹（皮炎），贝切特氏病，葡萄膜病，系统性红斑狼疮，Sjögren综合征，多发性硬化症，重症肌无力，I型糖尿病，内分泌眼病，原发性胆汁性肝硬化，克罗恩病，肾小球性肾炎，结节病，牛皮癣，天疱疮，再生障碍性贫血，特发性血小板减少性紫癜，变态反应，结节性多动脉炎，进行性系统性硬化，混合性结缔组织病，主动脉炎综合征，多发性肌炎，皮肌炎，韦格纳肉芽肿，溃疡性结肠炎，活动性慢性肝炎，自身免疫性溶血性贫血，伊文思综合征，支气管哮喘和花粉症。它也可用作抗真菌剂和毛发生长兴奋剂。

6. 发明申请

WO2007119463A1 2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS 审中-公开
标题翻译： 2-（环丙氨基） - 吡啶酮衍生物作为TPK1抑制剂
公开(公告)号：WO2007119463A1
公开(公告)日：2007-10-25
申请号：PCT/JP2007/055787
申请日：2007-03-14
申请人： MITSUBISHI PHARMA CORPORATION , SANOFI-AVENTIS , FUKUNAGA, Kenji , KOHARA, Toshiyuki , WATANABE, Kazutoshi , USUI, Yoshihiro , UEHARA, Fumiaki , YOKOSHIMA, Satoshi , SAKAI, Daiki , KUSAKA, Shin-ichi , NAKAYAMA, Kazuki
发明人： FUKUNAGA, Kenji , KOHARA, Toshiyuki , WATANABE, Kazutoshi , USUI, Yoshihiro , UEHARA, Fumiaki , YOKOSHIMA, Satoshi , SAKAI, Daiki , KUSAKA, Shin-ichi , NAKAYAMA, Kazuki
IPC分类号： C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D453/06 , C07D471/18 , C07D493/04 , C07D498/04 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/513 , A61P25/28
CPC分类号： C07D413/14 , C07D401/04 , C07D401/14 , C07D403/14 , C07D409/14 , C07D453/06 , C07D493/04
摘要： A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R 2 represents a hydrogen or the like; R 3 represents methyl group or the like; R 20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R 4 represents hydrogen or the like; R 5 represents hydrogen or the like; R 6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH 2 , oxygen atom, NH, or the like; any one or more of R 5 and R 6 , R 5 and R 4 , R 6 and R 4 , X and R 5 , X and R 4 , X and R 6 , and R 6 and R 6 may combine to each other to form a ring, 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（I）其中R 2表示氢等; R 3表示甲基等; R 20表示卤素原子等; q表示0〜3的整数， Z表示氮原子，CH等; R 4表示氢等; R 5表示氢等; R 6表示取代的烷氧基等; p表示0〜3的整数， X表示键，CH 2，氧原子，NH等; R 5和R 6，R 5和R 4，R 6中的任何一个或多个 X和R 5，X和R 4，X和R 6，，并且R 6和R 6可以彼此结合形成环，其用于预防和/或治疗治疗由tau蛋白激酶1引起的疾病多动症如神经退行性疾病（如阿兹海默症）。

7. 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。

8. 发明申请

WO2004014910A1 DIHYDROPYRAZOLOPYRIDINE COMPOUNDS 审中-公开
标题翻译：二氢吡唑并吡啶化合物
公开(公告)号：WO2004014910A1
公开(公告)日：2004-02-19
申请号：PCT/JP2003/009787
申请日：2003-08-01
申请人： MITSUBISHI PHARMA CORPORATION , KOHARA, Toshiyuki , FUKUNAGA, Kenji , HANANO, Tokushi
发明人： KOHARA, Toshiyuki , FUKUNAGA, Kenji , HANANO, Tokushi
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。

9. 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。

10. 发明申请

WO1993022327A1 2'-METHYLIDENENUCLEOSIDE COMPOUND AND PHARMACEUTICAL USE THEREOF 审中-公开
标题翻译： 2'-甲基二烯化合物及其药物用途
公开(公告)号：WO1993022327A1
公开(公告)日：1993-11-11
申请号：PCT/JP1993000514
申请日：1993-04-19
申请人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , YAMASA CORPORATION , MATSUDA, Akira , ARITA, Masafumi , YASUOKA, Joji , KOHARA, Toshiyuki , SAKATA, Shinji , MIYASHITA, Takanori
发明人： YOSHITOMI PHARMACEUTICAL INDUSTRIES, LTD. , YAMASA CORPORATION
IPC分类号： C07H19/06
CPC分类号： C07H19/06 , C07H19/10
摘要： A 2'-methylidenenucleoside compound represented by general formula (I) or a salt thereof, a process for the production thereof, and an antineoplastic or antiviral agent containing the same as the active ingredient, wherein one of R and R represents hydrogen, halogen, alkyl, cyano, optionally substituted carboxy or optionally substituted carbamoyl, and the other represents halogen, alkyl, cyano, optionally substituted carboxyl or optionally substituted carbamoyl; R and R may be the same or different from each other and each represents hydrogen, an in vivo hydrolyzable group, or a residue of mono-, di- or triphosphoric acid or an ester thereof; R represents hydrogen or an in vivo hydrolyzable group; and R represents hydrogen, halogen, alkyl, alkenyl, alkynyl or haloalkyl. The compound and the salts have enhanced antineoplastic and antiviral effects and an improved bioavailability and are reduced in side effects such as gastrointestinal diseases.
摘要翻译：由通式（I）表示的2'-亚甲基亚硝基核苷化合物或其盐，其制备方法和含有该活性成分的抗肿瘤抗病毒剂，其中R 1和R 2之一烷基，氰基，任选取代的羧基或任选取代的氨基甲酰基，另一个表示卤素，烷基，氰基，任选取代的羧基或任选取代的氨基甲酰基; R 3和R 4可以彼此相同或不同，并且各自表示氢，体内可水解基团，或单 - ，二 - 或三磷酸或其酯的残基; R 5表示氢或体内可水解基团; R 6表示氢，卤素，烷基，烯基，炔基或卤代烷基。化合物和盐具有增强的抗肿瘤和抗病毒作用和改善的生物利用度，并减少副作用如胃肠道疾病。

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