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1.发明公开2-(PYRIMIDIN-5-YL)-THIOPYRIMIDINE DERIVATIVES AS HSP70 AND HSC70 MODULATORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开作为HSP70和HSC70调节剂治疗增殖性疾病的2-（嘧啶-5-基） - 噻嘧啶衍生物
公开(公告)号：EP3205647A3
公开(公告)日：2017-09-27
申请号：EP16189468.8
申请日：2010-08-17
发明人： CHIOSIS, Gabriela , TALDONE, Tony , RODINA, Anna , PATEL, Pallav , KANG, Yanlong
IPC分类号： C07D239/60 , C07D239/38 , C07D239/56 , C07D239/47 , C07D495/04 , C07D403/12 , A61K31/54 , A61P35/00
摘要： The present invention relates to 2-(Pyrimidin-5-yl)-thiopyrimidine derivatives as Hsp70 and Hsc70 modulators for the treatment of proliferative disorders.
(Fig. 2)摘要翻译： 本发明涉及用于治疗增殖性疾病的作为Hsp70和Hsc70调节剂的2-（嘧啶-5-基） - 硫代嘧啶衍生物。 （图2）
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2.发明公开2-(PYRIMIDIN-5-YL)-THIOPYRIMIDINE DERIVATIVES AS HSP70 AND HSC70 MODULATORS FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开作为HSP70和HSC70调节剂治疗增殖性疾病的2-（嘧啶-5-基） - 噻嘧啶衍生物
公开(公告)号：EP3205647A2
公开(公告)日：2017-08-16
申请号：EP16189468.8
申请日：2010-08-17
发明人： CHIOSIS, Gabriela , TALDONE, Tony , RODINA, Anna , PATEL, Pallav , KANG, Yanlong
IPC分类号： C07D239/60 , C07D239/38 , C07D239/56 , C07D239/47 , C07D495/04 , C07D403/12 , A61K31/54 , A61P35/00
摘要： The present invention relates to 2-(Pyrimidin-5-yl)-thiopyrimidine derivatives as Hsp70 and Hsc70 modulators for the treatment of proliferative disorders.
摘要翻译： 本发明涉及用于治疗增殖性疾病的作为Hsp70和Hsc70调节剂的2-（嘧啶-5-基） - 硫代嘧啶衍生物。
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3.发明公开PROCESS FOR THE PREPARATION OF A PHARMACEUTICAL AGENT 审中-公开VERFAHREN ZUR HERSTELLUNG EINES PHARMAZEUTISCHEN WIRKSTOFFS
公开(公告)号：EP3133062A1
公开(公告)日：2017-02-22
申请号：EP15460045.6
申请日：2015-08-19
发明人： KOSIK, Kamil , SAGOL, Karol , GODZISZ, Mateusz
IPC分类号： C07D219/06 , C07D405/04 , C07D239/60 , C07C15/00 , C07F9/24
CPC分类号： C07D405/04 , C07D239/60 , C07F9/2445 , C07F9/65125 , C07F9/65127 , C07F9/65586 , C07H1/02 , C07H19/10
摘要： This invention provides a process for providing phosphoramidate derivatives, comprising performing a nucleophilic substitution reaction at phosphorous, where a phosphoryl chloride derivative is reacted with an oxime derivative to provide activated phosphoramidate intermediates, the intermediates find utility in a second nucleophilic substitution reaction where an activated phosphoramidate is reacted with a primary alcohol-containing sugar derivative, wherein the product of the reaction is sofosbuvir.
摘要翻译： 本发明提供了一种提供氨基磷酸酯衍生物的方法，包括在磷处进行亲核取代反应，其中磷酰氯衍生物与肟衍生物反应以提供活化的氨基磷酸酯中间体，中间体可用于第二亲核取代反应，其中活化的氨基磷酸酯 与含伯醇的糖衍生物反应，其中反应的产物是sofosbuvir。
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公开(公告)号：EP2729453B1
公开(公告)日：2015-05-06
申请号：EP12735316.7
申请日：2012-07-05
IPC分类号： C07D239/54 , C07D239/60 , A61P25/18 , A61K31/513
CPC分类号： A61K31/513 , A61K45/06 , C07D239/22 , C07D239/54 , C07D239/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , C07D471/04
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公开(公告)号：EP2497768A4
公开(公告)日：2013-08-28
申请号：EP10827174
申请日：2010-11-02
发明人： KIM SUNGHOON , HAN JUNG MIN , KIM HYEONG RAE , JEON DONG JU , SONG JONG HWAN , PARK KYUNG EUN
IPC分类号： C07D401/12 , A61K31/513 , A61P29/00 , C07D239/52 , C07D239/60
CPC分类号： C07D239/60 , C07D239/52 , C07D401/12
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公开(公告)号：EP2021324A1
公开(公告)日：2009-02-11
申请号：EP07729447.8
申请日：2007-05-23
申请人： NicOx S.A.
IPC分类号： C07D209/20 , C07D239/34 , C07D239/52 , C07D239/60 , C07D261/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/06 , C07D413/12 , C07D417/04 , A61K31/40 , A61K31/41 , A61K31/435
CPC分类号： C07D239/52 , C07D209/20 , C07D239/34 , C07D239/60 , C07D261/14 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/04 , C07D405/06 , C07D413/12 , C07D417/04 , C07K5/0821
摘要： Endothelin receptor antagonist nitroderivatives of general formula (I) having an improved pharmacological activity compared with their parent compounds. They can be employed for treating or preventing endothelial-related disorders, renal, pulmonary, cardiac and vascular diseases, and inflammatory processes.
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7.发明授权
公开(公告)号：EP1539713B1
公开(公告)日：2007-12-19
申请号：EP03792486.7
申请日：2003-08-20
申请人： AstraZeneca AB
发明人： EBDEN, Mark, Richard AstraZeneca R & D Charnwood , MEGHANI, Premji AstraZeneca R & D Charnwood , COOK, Antony, Ronald AstraZeneca R & D Charnwood , STEELE, John AstraZeneca R & D Charnwood , CHEEMA, Lal L. S., AstraZeneca R & D Charnwood
IPC分类号： C07D239/56 , C07D239/60 , C07D417/12 , C07D403/12 , C07D401/04 , C07D401/12 , C07D413/14 , C07D413/12 , C07D413/04 , A61K31/513 , A61P37/08 , A61P37/06 , A61P19/02 , A61P9/10 , A61P19/10
CPC分类号： C07D239/56 , C07D239/60 , C07D401/04 , C07D401/12 , C07D403/12 , C07D413/04 , C07D413/12 , C07D413/14 , C07D417/12
摘要： Compounds of formula (1), pharmaceutically acceptable salts, solvates and in vivo hydrolysable esters thereof, have activity as pharmaceuticals, in particular as modulators of chemokine receptor (especially CXCR2) activity, and may be in the treatment (therapeutic or prophylactic) of conditions/diseases in human and non-human animals which are exacerbated or caused by excessive or unregulated production of chemokines.
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8.发明授权Substituted phenylpyrimidine derivatives, useful in the treatment or prevention of CNS disorders 失效取代的苯基嘧啶衍生物，CNS病症的治疗或预防
公开(公告)号：EP0727213B9
公开(公告)日：2007-11-07
申请号：EP95120378.5
申请日：1989-12-06
IPC分类号： A61K31/505 , A61K31/535 , C07D239/48 , C07D239/50 , C07D239/60 , C07D239/42 , C07D239/46
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5355 , A61K31/5377 , C07C255/54 , C07C255/56 , C07D239/47 , C07D239/48 , C07D239/50 , C07D239/56 , C07D239/58
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9.发明公开THIOAMIDES AND SALTS THEREOF AND CYTOKINE PRODUCTION INHIBITORS CONTAINING BOTH 有权硫唑酸钠在不同浓度范围内的细胞因子 - BILDUNGSINHIBITOREN
公开(公告)号：EP1716851A4
公开(公告)日：2007-10-17
申请号：EP05719200
申请日：2005-02-16
发明人： KATO FUMINORI , KIMURA HIROHIKO , TAMAI KIYOSHI , YAMAMOTO KAZUHIRO , SANO MITSUO , MORI SHINYA , OKADA TAKASHI , UEKI TOSHIHIKO , AZUMA KUMIKO
IPC分类号： A61K31/166 , C07D237/20 , A61K31/18 , A61K31/352 , A61K31/401 , A61K31/404 , A61K31/4045 , A61K31/41 , A61K31/415 , A61K31/4192 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/428 , A61K31/437 , A61K31/44 , A61K31/4409 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/47 , A61K31/4965 , A61K31/50 , A61K31/505 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/541 , A61P3/10 , A61P5/14 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P19/02 , A61P21/04 , A61P25/00 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07C233/66 , C07C233/69 , C07C233/71 , C07C233/78 , C07C311/17 , C07C323/42 , C07C327/48 , C07D207/09 , C07D209/04 , C07D209/08 , C07D209/42 , C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/81 , C07D213/82 , C07D213/83 , C07D215/20 , C07D215/22 , C07D231/18 , C07D231/20 , C07D235/08 , C07D237/04 , C07D239/30 , C07D239/34 , C07D239/42 , C07D239/60 , C07D241/12 , C07D241/18 , C07D249/18 , C07D257/04 , C07D263/58 , C07D277/20 , C07D277/36 , C07D277/74 , C07D311/08 , C07D311/46 , C07D401/12 , C07D471/04
CPC分类号： C07D239/34 , C07C233/66 , C07C233/69 , C07C233/71 , C07C233/78 , C07C323/42 , C07C327/48 , C07C2603/74 , C07D213/83 , C07D239/42
摘要： The invention provides cytokine production inhibitors useful as preventive or therapeutic agents for diseases accompanied with abnormally enhanced immune function. Cytokine production inhibitors containing as the active ingredient thioamides represented by the general formula (I) or salts thereof: wherein A is N, NO, C-NO2, or C-CN; Hal is halogeno; M1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, a heterocycle, amino, O, S, SO, or SO2; M2 is amino, O, S, or a single bond; R1 is halogeno, alkyl, or the like; R2 R3, R4 and R5 are each independently H, alkyl, or the like; R6 is halogeno, alkyl, or the like; Cy is cycloalkyl, cycloalkenyl, aryl, or a heterocycle; k, p and q are each independently an integer of 0 to 3; and r is an integer of 0 to 5.
摘要翻译： 提供细胞因子产生抑制剂，作为伴有过度活化免疫功能的疾病的预防或治疗药物。 含有式（I）所示的硫代酰胺化合物或其盐作为活性成分的细胞因子产生抑制剂：其中A为N，NO，C-NO 2或C-CN; 卤素是卤素; M 1是烷基，烯基，炔基，环烷基，环烯基，芳基，杂环基，氨基，O，S，SO或SO 2; M 2是氨基，O，S或单键; R 1是卤素，烷基等; R 2，R 3，R 4和R 5各自独立地为H，烷基等; R 6是卤素，烷基等; Cy是环烷基，环烯基，芳基或杂环基; k，p和q各自独立地为0〜3的整数; r为0〜5的整数。
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公开(公告)号：EP0834074B2
公开(公告)日：2005-11-16
申请号：EP96921410.5
申请日：1996-06-06
IPC分类号： G01N33/50 , G01N33/52 , C07D239/60 , C07D209/08 , C07F5/00 , C07F5/02
CPC分类号： G01N33/582 , C07D209/08 , C07D239/60 , C07D239/62 , C07D239/66 , C07D311/16 , C07F5/003 , C07F5/02 , C07F5/027 , C07F9/10 , C07F9/5728 , C09B23/02 , G01N33/5005 , G01N33/5008 , G01N33/502 , G01N33/5041 , G01N33/5044 , G01N33/5047 , G01N33/5058 , G01N33/5061 , G01N33/5076 , G01N33/52 , G01N33/542 , G01N33/6872 , G01N2500/10 , Y02P20/55 , Y10S436/805
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