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1. 发明公开

EP1820515A4 NITROGEN-CONTAINING FUSED RING COMPOUND AND USE THEREOF 审中-公开
标题翻译：含氮稠环的连接和使用
公开(公告)号：EP1820515A4
公开(公告)日：2009-11-25
申请号：EP05811303
申请日：2005-11-29
申请人： JAPAN TOBACCO INC
发明人： HIRATA KAZUYUKI , OGAWA NAOKI , SHINAGAWA YUKO , KIGUCHI TOSHIHIRO , INOUE TERUHIKO , MATSUO AKIRA , KOSUGI YOSHINORI , NOMURA YUKIHIRO , KAWAHARA IICHIRO , UEHARA HIDETO
IPC分类号： A61K45/00 , A61K31/498 , A61K31/538
CPC分类号： A61K45/06 , A61K31/395 , C07D209/08 , C07D223/16 , C07D241/42 , C07D241/44 , C07D243/12 , C07D263/56 , C07D265/36 , C07D265/38 , C07D267/02 , C07D267/14 , C07D279/16 , C07D413/06 , C07D413/12

2. 发明公开

EP1848686A2 9-SUBSTITUTED TETRACYCLINES 审中-公开
标题翻译： 9-取代的四环素
公开(公告)号：EP1848686A2
公开(公告)日：2007-10-31
申请号：EP06720553.4
申请日：2006-02-09
申请人： Wyeth
发明人： SUM, Phaik-Eng , MANSOUR, Tarek
IPC分类号： C07C237/26 , C07D265/06 , A61K31/65
CPC分类号： C07D265/02 , C07C237/26 , C07D267/02 , C07D409/12 , C07D413/12
摘要： This invention provides compounds of Formula (I); wherein: R1 is a moiety selected from the group: (II) and (III) n is an integer of 1 or 2; R2 is selected from hydrogen, amino, -NR6R7, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, alkynyl of 2 to 12 carbon atoms optionally substituted, halogen, and a 5 to 10 membered heteroaryl ring optionally substituted, having 1 to 4 heteroatoms independently selected from N, O and S; R3 is selected from hydrogen, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, vinyl, alkynyl of 2 to 12 carbon atoms optionally substituted and halogen; R4 is H, alkyl of 1 to 12 carbon atoms optionally substituted, cycloalkyl of 3 to 8 carbon atoms, bicycloalkyl of 5 to 10 carbon atoms or aralkyl optionally substituted; R5 is OH or -OH8; R6 and R7 are each independently H or alkyl of 1 to 12 carbon atoms or when optionally taken together with the nitrogen atom to which each is attached form a 3 to 8 membered saturated heterocyclyl ring; R8 is alkyl of 1 to 12 carbon atoms optionally substituted; or a tautomer or pharmaceutically acceptable salts thereof.

3. 发明公开

EP1553077A4 PROCESS FOR PRODUCTION OF HIGH-PURITY ENAMINES 审中-公开
标题翻译：工艺生产高纯度烯胺
公开(公告)号：EP1553077A4
公开(公告)日：2007-06-20
申请号：EP03765316
申请日：2003-07-17
申请人： SANKYO CO
发明人： OKAZAKI REI , KOJIMA SHUNSHI , YOKOKAWA HIDEHARU
IPC分类号： C07C209/60 , C07C209/84 , C07C211/21 , C07D267/02 , C07D279/12 , C07D281/02 , C07D285/14
CPC分类号： C07C209/60 , C07D267/02 , C07D279/12 , C07D281/02 , C07D285/14 , C07C211/21
摘要： A process for the production of compounds represented by the general formula (3) and having high purity: (3) [wherein R1 is C1-6 alkyl or the like and R2 is hydrogen or the like, or R1 and R2 may be united to form C1-6 alkylene; and R3 and R4 are each C1-6 alkyl or the like], which comprises the step of reacting a compound represented by the general formula (1): (1) [wherein R1 and R2 are each as defined above] with a compound represented by the general formula (2): (2) [wherein R3 and R4 are each as defined above] and the step of treating the obtained reaction mixture with acidic water at 0 to 30°C.

5. 发明公开

EP1254898A4 BENZENE-FUSED HETEROCYCLE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译：苯并杂环衍生物并将此作为有效成分含药物
公开(公告)号：EP1254898A4
公开(公告)日：2003-03-12
申请号：EP01946856
申请日：2001-01-25
申请人： ONO PHARMACEUTICAL CO
发明人： OHMOTO KAZUYUKI , ITAGAKI IORI
IPC分类号： A61K38/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P3/14 , A61P7/04 , A61P7/06 , A61P9/10 , A61P11/00 , A61P11/06 , A61P13/08 , A61P19/02 , A61P19/10 , A61P21/00 , A61P21/04 , A61P25/00 , A61P25/28 , A61P27/10 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D223/16 , C07D243/12 , C07D243/14 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D285/36 , C07D401/12 , C07D403/12 , C07D409/12 , C07D491/048 , C07D491/056 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/078 , A61K31/55 , A61K31/5513 , A61K31/553 , A61K31/554 , A61P9/00 , A61P33/00 , A61P37/00
CPC分类号： C07D223/16 , A61K38/00 , C04B35/632 , C07D243/12 , C07D243/14 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D285/36 , C07D401/12 , C07D403/12 , C07D409/12 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06191
摘要： Benzene-fused heterocycle derivatives of the general formula (I); and nontoxic salts thereof (wherein each symbol is as defined in the description). The compounds of the general formula (I) exhibit inhibitory activities against cysteine proteases and are useful as preventive and/or therapeutic drugs for immunopathy (such as autoimmune diseases and infectious diseases), inflammatory diseases (such as inflammatory diseases of intestine, multiple encephalosclerosis, and arthritis), nerve degeneration diseases (such as Alzheimer's disease and muscular dystrophy), bone resorptive diseases (such as osteoporosis), respiratory diseases, diabetes, shock, and so on.

6. 发明公开

EP1820515A1 NITROGEN-CONTAINING FUSED RING COMPOUND AND USE THEREOF 审中-公开
标题翻译：国际海事组织KONDENSIERTE RINGVERBINDUNG
公开(公告)号：EP1820515A1
公开(公告)日：2007-08-22
申请号：EP05811303.6
申请日：2005-11-29
申请人： Japan Tobacco, Inc.
发明人： HIRATA, Kazuyuki C.Pharm.Res.Inst. of Jp. Tobacco , OGAWA, Naoki C.Pharm.Res.Inst. of Jp. Tobacco , SHINAGAWA, Yuko C.Pharm.Res.Inst. of Jp. Tobacco , KIGUCHI, Toshihiro C.Pharm.Res.Inst. of Jp.Tobacco , INOUE, Teruhiko C.Pharm.Res.Inst. of Jp. Tobacco , MATSUO, Akira C.Pharm.Res.Inst. of Jp. Tobacco , KOSUGI, Yoshinori C.Pharm.Res.Inst. of Jp. Tobacco , NOMURA, Yukihiro C.Pharm.Res.Inst. of Jp. Tobacco , KAWAHARA, Iichiro C.Pharm.Res.Inst. of Jp. Tobacco , UEHARA, Hideto C.Pharm.Res.Inst. of Jp. Tobacco
IPC分类号： A61K45/00
CPC分类号： A61K45/06 , A61K31/395 , C07D209/08 , C07D223/16 , C07D241/42 , C07D241/44 , C07D243/12 , C07D263/56 , C07D265/36 , C07D265/38 , C07D267/02 , C07D267/14 , C07D279/16 , C07D413/06 , C07D413/12
摘要： A URAT1 activity inhibitor containing a nitrogen-containing fused ring compound represented by the following formula [1]:

wherein each symbol is as defined in the description. The present invention is useful for the prophylaxis or treatment of pathology showing involvement of uric acid, such as hyperuricemia, gouty tophus, acute gouty arthritis, chronic gouty arthritis, gouty kidney, urolithiasis, renal function disorder, coronary artery disease, ischemic heart disease and the like.
摘要翻译：含有由下式[1]表示的含氮稠环化合物的URAT1活性抑制剂：其中每个符号如说明书中所定义。本发明可用于预防或治疗显示尿酸例如高尿酸血症，痛风，急性痛风性关节炎，慢性痛风性关节炎，痛肾，尿石症，肾功能障碍，冠状动脉疾病，缺血性心脏病和类似。

7. 发明公开

EP1553077A1 PROCESS FOR PRODUCTION OF HIGH-PURITY ENAMINES 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON HOCHREINEN ENAMINEN
公开(公告)号：EP1553077A1
公开(公告)日：2005-07-13
申请号：EP03765316.9
申请日：2003-07-17
申请人： Sankyo Company, Limited
发明人： OKAZAKI, Rei c/o SANKYO COMPANY, LIMITED , KOJIMA, Shunshi c/o SANKYO COMPANY, LIMITED , YOKOKAWA, Hideharu c/o Res. Lab., SANKYO CHEM. IND
IPC分类号： C07C209/60
CPC分类号： C07C209/60 , C07D267/02 , C07D279/12 , C07D281/02 , C07D285/14 , C07C211/21
摘要： A method for producing highly pure enamines, which comprises a step of reacting an aldehyde or ketone with an amine and a step of treating the resulting reaction mixture with an acidic aqueous solution at between 0°C and 30°C.
摘要翻译：一种制备高纯度烯胺的方法，其包括使醛或酮与胺反应的步骤和在0℃至30℃之间用酸性水溶液处理所得反应混合物的步骤。

8. 发明公开

EP1254898A1 BENZENE-FUSED HETEROCYCLE DERIVATIVES AND DRUGS CONTAINING THE SAME AS THE ACTIVE INGREDIENT 审中-公开
标题翻译： BENZOKONDENSIERTE HETEROCYCLISCHE DERIVATE SOWIE DIESE ALS WIRKSTOFFE ENTHALTENDE MEDIKAMENTE
公开(公告)号：EP1254898A1
公开(公告)日：2002-11-06
申请号：EP01946856.0
申请日：2001-01-25
申请人： ONO PHARMACEUTICAL CO., LTD.
发明人： OHMOTO, Kazuyuki Minase Research Institute , ITAGAKI, Iori Minase Research Institute
IPC分类号： C07D223/16
CPC分类号： C07D223/16 , A61K38/00 , C04B35/632 , C07D243/12 , C07D243/14 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D285/36 , C07D401/12 , C07D403/12 , C07D409/12 , C07K5/06052 , C07K5/06078 , C07K5/06086 , C07K5/06139 , C07K5/06191
摘要： A benzene-fused heteroring derivative of formula (I)
wherein all symbols are the same as described in the specification, and a non-toxic salt thereof.
The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of immune diseases (autoimmune diseases, infectious diseases, etc.), inflammatory diseases (inflammatory bowel diseases, multiple cerebrosclerosis, arthritis, etc.), nerve degeneration diseases (Alzheimer's disease, muscular dystrophy, etc.), bone resorption diseases (osteoporosis, etc.), respiratory system diseases, diabetes, shock, etc.
摘要翻译：其中所有符号与说明书中所述相同的式（I）苯基稠合杂环衍生物及其无毒盐。式（I）化合物对半胱氨酸蛋白酶具有抑制活性，因此可用作预防和/或治疗免疫疾病（自身免疫性疾病，感染性疾病等），炎症性疾病（炎性肠病，多发性脑血管病，关节炎等），神经变性疾病（阿尔茨海默病，肌营养不良等），骨吸收疾病（骨质疏松症等），呼吸系统疾病，糖尿病，休克等

9. 发明公开

EP1093372A1 CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING $g(b)-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 审中-公开
标题翻译：氨基化合物，药物组合物时AND METHOD FOR抑制（B）淀粉样肽释放和/或其合成这些化合物的使用
公开(公告)号：EP1093372A1
公开(公告)日：2001-04-25
申请号：EP99930600.4
申请日：1999-06-22
申请人： Elan Pharmaceuticals, Inc. , Eli Lilly & Company
发明人： AUDIA, James, E. , DRESSMAN, Bruce, A. , SHI, Qing
IPC分类号： A61K31/55 , C07D223/14 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/24 , C07D267/02 , C07D281/02 , C07D487/02 , C07D487/12 , C07D498/02 , C07D513/02
CPC分类号： A61K31/55 , A61K38/00 , C07D223/14 , C07D223/16 , C07D223/18 , C07D243/06 , C07D243/10 , C07D243/12 , C07D243/14 , C07D243/24 , C07D267/02 , C07D267/14 , C07D281/02 , C07D281/10 , C07D401/04 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D417/04 , C07D471/04 , C07D471/06 , C07D471/08 , C07D487/02 , C07D487/04 , C07D487/12 , C07D498/02 , C07D513/02 , C07K4/00
摘要： Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

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