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71. 发明授权

EP3237416B1 POLYCYCLIC-CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE 有权
公开(公告)号：EP3237416B1
公开(公告)日：2019-05-01
申请号：EP15825729.5
申请日：2015-12-21
申请人： Gilead Sciences, Inc.
发明人： BACON, Elizabeth, M. , CAI, Zhenhong, R. , COTTELL, Jeromy, J. , JI, Mingzhe , JIN, Haolun , LAZERWITH, Scott, E. , MORGANELLI, Philip, Anthony , PYUN, Hyung-jung
IPC分类号： C07D471/04 , C07D491/147 , A61K31/4375 , A61P31/18

72. 发明公开

EP3378863A1 PYRANODIPYRIDINE COMPOUND 审中-公开
公开(公告)号：EP3378863A1
公开(公告)日：2018-09-26
申请号：EP16864249.4
申请日：2016-11-09
申请人： Eisai R&D Management Co., Ltd.
发明人： KUROKAWA Toshiki , YOSHIDA Yu , SHIN Kogyoku , KOBAYASHI Yoshihisa , FUKUMOTO Hironori , TAKEDA Kunitoshi , OHASHI Yoshiaki , KOTAKE Makoto , SHIBUGUCHI Tomoyuki , WATANABE Toru , KITA Yoichi , HIROTA Shinsuke , FUKUYAMA Takashi , KAMADA Yasuaki
IPC分类号： C07D491/147 , A61K31/4375 , A61K31/444 , A61K31/497 , A61K31/506 , A61P9/10 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30
CPC分类号： C07D491/147 , C07D491/052
摘要： Compounds represented by formulae (I) to (XXII) or pharmaceutically acceptable salts thereof:

73. 发明公开

EP3344629A1 THERAPEUTIC COMPOUND FOR PAIN AND SYNTHESIS THEREOF 无效
公开(公告)号：EP3344629A1
公开(公告)日：2018-07-11
申请号：EP16842981.9
申请日：2016-09-01
申请人： Janssen Pharmaceutica N.V.
发明人： DECORTE, Bart Lieven Daniel , RUSSCHER, Jacob Cornelis , MONNEE, Menno Cornelis Franciscus
IPC分类号： C07D471/12 , C07D471/18 , C07D317/46 , C07D491/147 , A61K31/437 , A61K31/36 , A61K31/336
CPC分类号： C07D471/18 , C07D451/00 , C07D451/04 , C07D451/06 , C07D451/10 , C07D451/12
摘要： and stereoisomers, pharmaceutically acceptable salts and derivatives thereof; and methods of making and using such compounds. The invention includes pharmaceutical compositions containing such compounds, and the use of such compounds in methods of treating conditions, diseases, or disorders.

74. 发明公开

EP3315501A1 DRUG WITH ANTIVIRAL ACTIVITY (VARIANTS) 有权
标题翻译：具有抗病毒活性的药物（变体）
公开(公告)号：EP3315501A1
公开(公告)日：2018-05-02
申请号：EP16773558.8
申请日：2016-04-06
申请人： Tets, Viktor Veniaminovich , Tets, Georgy Viktorovich
发明人： KRASNOV, Konstantin Andreevich
IPC分类号： C07D491/147 , C07D239/10 , C07H19/073 , A61K31/519 , A61K31/513 , A61P31/14 , A61P31/12
摘要： The invention relates to the field of organic chemistry and medicine, and more particularly to synthetic substances of the pyrimidine series, namely 2-chloro-5-phenyl-5 H- pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivatives, having antiviral activity. Claimed are a drug with antiviral activity against HIV infection and hepatitis B virus, containing 2-chloro-5-phenyl-5H-pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivatives of the general formula shown, where: X is selected from the group: H, NO 2 , Hal, OMe; R1 is selected from the group: Cl, OH; and R2 is selected from the group: Cl, SH, OH; and a drug with antiviral activity against HIV infection, containing a 2-chloro-5-phenyl-5H-pyrimido[5',4':5,6]pyrano[2,3-d]pyrimidine-4-ol derivative of the general formula shown, where: X is selected from the group: H, NO 2 , Hal, OMe; R1 is selected from the group: Cl, OH; and R2 is selected from the group: Cl, SH, OH in combination with a reverse transcriptase inhibitor selected from Retrovir, or in combination with a protease inhibitor selected from Lopinavir, in an effective amount. The result is an effective drug with antiviral activity.
摘要翻译：本发明涉及有机化学和医药领域，更具体地涉及嘧啶系列的合成物质，即2-氯-5-苯基-5H-嘧啶并[5'，4'：5,6]吡喃并[2,1- 3-d]嘧啶-4-醇衍生物，具有抗病毒活性。声称含有2-氯-5-苯基-5H-嘧啶并[5'，4'：5,6]吡喃并[2,3-d]嘧啶-4-酮的抗HIV感染和乙型肝炎病毒的抗病毒活性的药物，其中：X选自：H，NO 2，Hal，OMe; R1选自：Cl，OH; 并且R2选自：Cl，SH，OH; 和一种具有抗HIV感染的抗病毒活性的药物，该药物含有2-氯-5-苯基-5H-嘧啶并[5'，4'：5,6]吡喃并[2,3-d]嘧啶-4-醇衍生物所示通式表示，其中：X选自：H，NO 2，Hal，OMe; R1选自：Cl，OH; R2选自：Cl，SH，OH与选自Retrovir的逆转录酶抑制剂或与选自洛匹那韦的蛋白酶抑制剂组合的有效量的组合。其结果是具有抗病毒活性的有效药物。

75. 发明公开

EP3310784A1 TRICYCLIC COMPOUNDS AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS 有权
标题翻译：三环类化合物及其作为磷酸二酯酶抑制剂的用途
公开(公告)号：EP3310784A1
公开(公告)日：2018-04-25
申请号：EP16739563.1
申请日：2016-06-09
申请人： Pfizer Inc.
发明人： CHAPPIE, Thomas Allen , CHANDRASEKARAN, Ramalakshmi Yegna , HELAL, Christopher John , LACHAPELLE, Erik Alphie , PATEL, Nandini Chaturbhai , SCIABOLA, Simone , VERHOEST, Patrick Robert , WAGER, Travis T.
IPC分类号： C07D487/14 , C07D471/14 , C07D471/22 , C07D487/04 , C07D491/147 , C07D498/22 , C07D513/14 , A61K31/4985 , A61K31/506 , A61P25/28
摘要： or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

76. 发明公开

EP3044225A4 TRICYCLIC GYRASE INHIBITORS 审中-实审转让
标题翻译：三环旋转酶抑制剂
公开(公告)号：EP3044225A4
公开(公告)日：2017-03-08
申请号：EP14844214
申请日：2014-09-10
申请人： MERCK SHARP & DOHME , L LIVERMORE NAT SECURITY LLC
发明人： FINN JOHN , TARI LESLIE WILLIAM , CHEN ZHIYONG , ZHANG JUNHU , PHILLIPSON DOUGLAS , LEE SUK JOONG , TRZOSS MICHAEL , BENSEN DANIEL , LI XIAOMING , TENG MIN , ONG VOON , BORCHARDT ALLEN JOHN , LAM THANH TO , LIGHTSTONE FELICE C , WONG SERGIO E , NGUYEN TOAN B
IPC分类号： C07D487/04 , A61K31/519 , A61P31/04 , C07D487/16 , C07D487/22 , C07D491/147 , C07D515/22
CPC分类号： C07D487/04 , C07D491/147

77. 发明公开

EP3089984A1 NOVEL COMPOUNDS FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISEASES 无效
标题翻译：新化合物是治疗癌症和炎症疾病的治疗
公开(公告)号：EP3089984A1
公开(公告)日：2016-11-09
申请号：EP14876538.1
申请日：2014-12-22
申请人： Jin, Bohan
发明人： Jin, Bohan
IPC分类号： C07D491/147 , C07D491/22 , C07D471/04 , C07D471/14 , A61K31/4353 , A61K31/4375 , A61P35/00 , A61P29/00
CPC分类号： A61K31/437 , C07D471/04 , C07D471/14 , C07D491/147 , C07D491/22
摘要： The present invention relates to novel compounds and pharmaceutical compositions thereof which may be useful in the treatment and/or prevention of various conditions. The present invention also provides methods of preparing such compounds and compositions, and methods of using the same.

78. 发明授权

EP2649078B1 4-AZA-2, 3-DIDEHYDROPODOPHYLLOTOXIN COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF 有权
标题翻译： 4-AZA-2,3-二羟基叶立德毒素化合物及其制备方法
公开(公告)号：EP2649078B1
公开(公告)日：2016-07-27
申请号：EP11719638.6
申请日：2011-03-25
申请人： Council of Scientific & Industrial Research
发明人： AHMED, Kamal , PAIDAKULA, Suresh , BANALA, Ashwini, Kumar , ADLA, Mallareddy , PAPAGARI, Venkat, Reddy , JAKI, Rasheed, Tamboli
IPC分类号： C07D491/147 , C07D498/14 , C07D491/04 , C07D498/04 , C07D513/04
CPC分类号： C07D498/14 , C07D491/04 , C07D491/147 , C07D498/04 , C07D513/04

79. 发明授权

EP2721034B1 N-HETEROTRICYCLIC ANTIBIOTICS 有权
标题翻译： N-异三环抗生素
公开(公告)号：EP2721034B1
公开(公告)日：2016-07-20
申请号：EP12728438.8
申请日：2012-06-11
申请人： Basilea Pharmaceutica AG
发明人： GAUCHER, Bérangère , DANEL, Franck Hubert , XIE, Tong , XU, Lin
IPC分类号： C07D491/14 , C07D491/147 , C07D491/052 , C07D495/04 , C07D498/04 , A61K31/4375 , A61K31/436 , A61K31/4365 , A61P31/04
CPC分类号： C07D498/04 , C07D491/052 , C07D491/14 , C07D491/147 , C07D495/04

80. 发明公开

EP2955184A1 METHOD FOR PREPARING (+)-TRICYCLIC HYDROXYL LACTONE 审中-公开
标题翻译： VERFAHREN ZUR HERSTELLUNG VON（+） - TRICYCLISCHEM HYDROXYLLONON
公开(公告)号：EP2955184A1
公开(公告)日：2015-12-16
申请号：EP14749294.6
申请日：2014-01-10
申请人： Fudan University
发明人： CHEN, Fener , HE, Qiuqin , XIONG, Fangjun , CHEN, Wenxue , WANG, Xinlong
IPC分类号： C07D491/22 , C07D491/147
CPC分类号： C07D491/147
摘要： The invention belongs to the technical field of organic chemistry, in particular being a method for preparing (+)-tricyclic hydroxyl lactone. The preparation of the (+)-tricyclic hydroxyl lactone compound in the prior art has lengthy steps, low stereoselectivity and high costs. The (+)-tricyclic hydroxyl lactone of the invention is obtained by an asymmetric oxidation reaction of prochiral tricyclic lactones in an organic solvent with an optically active Davis oxidant in the presence of an organic base. The method of the invention uses easily available raw materials, has low costs, good selectivity, and is suitable for large-scale preparation.
摘要翻译：本发明属于有机化学技术领域，特别是制备（+） - 三环羟基内酯的方法。现有技术中（+） - 三环羟基内酯化合物的制备具有漫长的步骤，低立体选择性和高成本。本发明的（+） - 三环羟基内酯通过在有机溶剂中的前手性三环内酯与光学活性的戴维斯氧化剂在有机碱的存在下的不对称氧化反应获得。本发明的方法使用容易获得的原料，成本低，选择性好，适用于大规模制备。

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