公开(公告)号：EP3137478A4

公开(公告)日：2018-03-07

申请号：EP15786514

申请日：2015-04-30

申请人： AGILENT TECHNOLOGIES INC

发明人： DELLINGER DOUGLAS J ,  MONFREGOLA LUCA ,  CARUTHERS MARVIN ,  ROY MITHUM

IPC分类号： C07H19/16 ,  C07H19/073 ,  C07H19/10 ,  C07H19/23 ,  C07H21/04

CPC分类号： C07H21/04 ,  C07H19/073 ,  C07H19/10 ,  C07H19/173 ,  C07H19/23 ,  Y02P20/55

摘要： Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.

公开(公告)号：EP3105243B1

公开(公告)日：2018-02-21

申请号：EP14716996.5

申请日：2014-03-04

申请人： Adam Mickiewicz University

发明人： CELEWICZ, Lech ,  KACPRZAK, Karol ,  BARANIAK, Dagmara ,  LEWANDOWSKA, Marta ,  RUSZKOWSKI, Piotr

IPC分类号： C07H19/073 ,  A61K31/7072 ,  A61P31/00

CPC分类号： C07H19/06 ,  A61K31/513 ,  A61K31/7072 ,  C07D453/04 ,  C07H19/073

摘要： 2′,3′-dideoxy-5-fluorouridine derivatives have general formula 1: wherein: R1 denotes cinchona alkaloid fragment with defined absolute configuration at C-8 and C-9 atoms. A process for the manufacture of 2′,3′-dideoxy-5-fluorouridine derivatives of general formula 1 and application of 2′,3′-dideoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer and hepatic cancer are also indicated.

公开(公告)号：EP3252066A1

公开(公告)日：2017-12-06

申请号：EP17176973.0

申请日：2014-09-02

申请人： MEDIVIR AB

发明人： KALAYANOV, Genadiy ,  TORSSELL, Staffan ,  WÄHLING, Horst

IPC分类号： C07H19/10 ,  C07H19/16 ,  C07H19/073 ,  C07H19/173 ,  A61K31/7072 ,  A61P31/14

CPC分类号： C07H19/06 ,  A61K31/7072 ,  A61K45/06 ,  C07H19/073 ,  C07H19/10 ,  C07H19/11 ,  C07H19/16 ,  C07H19/173 ,  C07H19/20 ,  C07H19/213 ,  C07H23/00

摘要： The invention provides compounds of the formula:

wherein B is a nucleobase:

and the other variables are as defined in the claims,
which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.

摘要翻译： 本发明提供了下式的化合物：其中B是核碱基，其它变量如权利要求中所定义，其用于治疗或预防丙型肝炎病毒感染及相关方面。

公开(公告)号：EP3140286A4

公开(公告)日：2017-09-27

申请号：EP15789510

申请日：2015-05-11

申请人： BIOSEARCH TECH INC

发明人： REDDINGTON MARK ,  COOK RONALD M ,  SOWERS BEN

IPC分类号： C07D455/04 ,  C07H19/04 ,  C07H19/073 ,  C12Q1/68

CPC分类号： C07D471/06 ,  C07D455/04 ,  C07F9/6561 ,  C07H17/02 ,  C07H21/00 ,  C12Q1/6818

摘要： The present invention provides quenchers of excited state energy, probes and other conjugates comprising these quenchers, and methods of their use.

摘要翻译： 本发明提供激发态能量的猝灭剂，包含这些猝灭剂的探针和其他缀合物，以及它们的使用方法。

公开(公告)号：EP3078671A4

公开(公告)日：2017-05-31

申请号：EP14867802

申请日：2014-12-04

申请人： HANGZHOU MINSHENG INST FOR PHARMA RES CO LTD ,  HANGZHOU MINSHENG PHARMACEUTICAL CO LTD

发明人： WU YAODONG ,  SHAN JIAQI ,  SHEN XIMING ,  WU CHUNXIA ,  HUANG BINNAN

IPC分类号： C07H19/073 ,  A61K31/7068 ,  A61P35/00 ,  C07H1/00

CPC分类号： C07H19/06 ,  A61K31/7068 ,  C07H1/00

摘要： The invention provides gemcitabine derivatives shown in the following formula (I) and preparation methods thereof. The invention further relates to a pharmaceutical composition which comprising the said gemcitabine derivatives in an effective amount and a pharmaceutically acceptable excipient or additive. The invention further provides use of the said derivatives for preparing anti-tumor drugs. The compound designed by the invention is novel in structure and has a remarkable anti-tumor activity. According to the compound designed by the invention, the preparation starting materials have extensive sources and are easily obtained, the preparation method is simple and easy to operate, and the yield of the product is high, so that industrial production on a large scale is facilitated.

摘要翻译： 本发明提供下式（I）所示的吉西他滨衍生物及其制备方法。 本发明还涉及包含有效量的所述吉西他滨衍生物和药学上可接受的赋形剂或添加剂的药物组合物。 本发明进一步提供了所述衍生物用于制备抗肿瘤药物的用途。 本发明设计的化合物结构新颖，具有显着的抗肿瘤活性。 根据本发明设计的化合物，制备原料来源广泛，易得，制备方法简单易操作，产品收率高，便于大规模工业化生产 。

公开(公告)号：EP2537839B1

公开(公告)日：2016-12-14

申请号：EP11742187.5

申请日：2011-02-07

申请人： NISSAN CHEMICAL INDUSTRIES, LTD.

发明人： IRIYAMA, Yusuke ,  HIGASHIYAMA, Tsutomu

IPC分类号： C07D307/32 ,  C07D405/04 ,  C07H19/073

CPC分类号： C07D405/04 ,  C07D307/32 ,  Y02P20/582

公开(公告)号：EP2921499A4

公开(公告)日：2016-04-27

申请号：EP13854700

申请日：2013-11-13

申请人： TAKEDA PHARMACEUTICAL

发明人： NONOGAWA MITSURU ,  NAGATA TOSHIAKI ,  SAITO HIDEKI ,  YASUMA TSUNEO

IPC分类号： C07H19/073 ,  C07H1/00 ,  C07H19/067 ,  C07H19/167 ,  C07H21/00 ,  C07H21/04

CPC分类号： C07H19/207 ,  C07H1/00 ,  C07H19/06 ,  C07H19/067 ,  C07H19/073 ,  C07H19/16 ,  C07H19/167 ,  C07H21/00 ,  C07H21/04

摘要： In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in Claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3'-direction but also in the 5'-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.

摘要翻译： 在该方法中，通过使用由式（I）表示的新型核苷单体化合物[其中X，R 1，Y，碱，Z，Ar，R 2，R 3和n为 如权利要求1所定义。 新型核苷单体化合物是一种核苷，其碱基部分被具有至少一个疏水基团的芳香烃 - 羰基 - 羰基或硫代羰基取代。 该方法可以避免每次反应中的色谱纯化，不仅能在3'方向而且在5'方向上进行碱基延伸，从而获得有效的液相合成寡核苷酸。

公开(公告)号：EP2816053A4

公开(公告)日：2015-07-01

申请号：EP13749023

申请日：2013-02-15

申请人： AJINOMOTO KK

发明人： HIRAI KUNIHIRO ,  KATAYAMA SATOSHI ,  TORII TAKAYOSHI ,  NAKAYA RYOTARO ,  TAKAHASHI DAISUKE

IPC分类号： C07H1/00 ,  C07H19/073 ,  C07H21/04

CPC分类号： C07H21/04 ,  C07H1/00

公开(公告)号：EP2303906A4

公开(公告)日：2014-12-03

申请号：EP09763709

申请日：2009-06-12

申请人： SCINOPHARM TAIWAN LTD

发明人： CHEN SHU-PING ,  SHIEH CHIA-LIN

IPC分类号： C07H19/073 ,  A61K31/522

CPC分类号： C07H19/073

公开(公告)号：EP2578578B1

公开(公告)日：2014-11-05

申请号：EP11789564.9

申请日：2011-04-25

申请人： Central Glass Company, Limited

发明人： ISHII, Akihiro ,  NAGURA, Hirokatsu ,  TSURUTA, Hideyuki

IPC分类号： C07D317/30 ,  A61K31/7068 ,  C07B61/00 ,  C07H19/073

CPC分类号： C07D317/30 ,  Y02P20/55