公开(公告)号：US20190201432A1

公开(公告)日：2019-07-04

申请号：US16021103

申请日：2018-06-28

申请人： NuCana plc

发明人： Christopher McGuigan ,  Jan Balzarini ,  Magdalena Slusarczyk ,  Blanka Gonczy ,  Paola Murziani

IPC分类号： A61K31/7072 ,  A61K45/06 ,  C07H19/10 ,  C07F9/655 ,  C07F9/6558 ,  C07F9/6584

CPC分类号： A61K31/7072 ,  A61K45/06 ,  C07F9/65515 ,  C07F9/65586 ,  C07F9/65844 ,  C07H19/10

摘要： Phosphoramidate derivates of 5-fluoro-2′-deoxyuridine are disclosed for use in the treatment of cancer, especially in the treatment of cancer where the patient shows resistance, for example, in a patient with cells with a lowered level of nucleoside transporter proteins and/or with nucleoside kinase-deficient cells and/or with mycoplasma-infected cells and/or with cells with a raised level of thymidylate synthase.

公开(公告)号：US20190085014A1

公开(公告)日：2019-03-21

申请号：US16149114

申请日：2018-10-01

申请人： The Trustees of Columbia University in the City of New York

发明人： Jingyue Ju ,  Zengmin Li ,  John Robert Edwards ,  Yasuhiro Itagaki

IPC分类号： C07H19/14 ,  C12Q1/6869 ,  C07H21/00 ,  C12Q1/686 ,  C12Q1/6872 ,  C12Q1/6876 ,  C07H19/10 ,  C12Q1/68 ,  C12Q1/6874 ,  C40B40/00

CPC分类号： C12Q1/6869 ,  C07B2200/11 ,  C07H19/10 ,  C07H19/14 ,  C07H21/00 ,  C12Q1/68 ,  C12Q1/686 ,  C12Q1/6872 ,  C12Q1/6874 ,  C12Q1/6876 ,  C12Q2525/117 ,  C12Q2525/186 ,  C12Q2535/101 ,  C12Q2535/122 ,  C12Q2563/107 ,  C12Q2565/501 ,  C40B40/00

摘要： This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3′-position of the deoxyribose.

公开(公告)号：US20190031705A1

公开(公告)日：2019-01-31

申请号：US16150185

申请日：2018-10-02

申请人： The Trustees of Columbia University in the City of New York

发明人： Jingyue Ju ,  Zengmin Li ,  John Robert Edwards ,  Yasuhiro Itagaki

IPC分类号： C07H19/14 ,  C12Q1/6869 ,  C07H19/10 ,  C12Q1/6874 ,  C12Q1/6876 ,  C12Q1/6872 ,  C12Q1/68 ,  C12Q1/686

CPC分类号： C12Q1/6869 ,  C07B2200/11 ,  C07H19/10 ,  C07H19/14 ,  C07H21/00 ,  C12Q1/68 ,  C12Q1/686 ,  C12Q1/6872 ,  C12Q1/6874 ,  C12Q1/6876 ,  C12Q2525/117 ,  C12Q2525/186 ,  C12Q2535/101 ,  C12Q2535/122 ,  C12Q2563/107 ,  C12Q2565/501 ,  C40B40/00

摘要： This invention provides methods for attaching a nucleic acid to a solid surface and for sequencing nucleic acid by detecting the identity of each nucleotide analogue after the nucleotide analogue is incorporated into a growing strand of DNA in a polymerase reaction. The invention also provides nucleotide analogues which comprise unique labels attached to the nucleotide analogue through a cleavable linker, and a cleavable chemical group to cap the —OH group at the 3′-position of the deoxyribose.

公开(公告)号：US20180346506A1

公开(公告)日：2018-12-06

申请号：US15535879

申请日：2015-11-11

申请人： ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

发明人： Yanghui GUO ,  Shiguo ZHAO ,  Yue ZHANG ,  Liang ZHANG ,  Zhiqing YANG ,  Jian CHAI

IPC分类号： C07H19/10 ,  C07H1/06 ,  A61P31/14

CPC分类号： C07H1/06 ,  C07H19/06 ,  C07H19/10

摘要： The present invention relates to a method for preparing Sofosbuvir crystal form-6. The method is simple in operation, stable in process condition, good in reproducibility, high in yield rate and high in purity, viscous gel-type products are not formed during the process, the problem of blocking of a discharge port is solved, and the method is suitable for mass industrial production and has high economic value.

公开(公告)号：US20180346505A1

公开(公告)日：2018-12-06

申请号：US15534022

申请日：2015-12-10

申请人： SOLSTICE BIOLOGICS, LTD.

发明人： Curt W. BRADSHAW ,  Sukumar SAKAMURI ,  Dingguo LIU

IPC分类号： C07H19/10 ,  A61P31/14

CPC分类号： C07H19/11 ,  A61K31/712 ,  A61K47/54 ,  A61K47/549 ,  C07H19/10 ,  C07H19/213

摘要： The invention features a mononucleotide comprising a nucleobase bonded to a sugar having a 3′-carbon and a 5′-carbon, where the 5′-carbon is bonded to a phosphorus (V) atom of a phosphate group through an oxygen atom, the phosphorus (V) atom being bonded to (i) a disulfide bioreversible group through an oxygen atom; and (ii) (a) optionally substituted amino, optionally substituted alkoxy, optionally substituted aryloxy, or optionally substituted heteroaryloxy; or (b) the 3′-carbon through an oxygen atom. The invention also features methods of delivering the mononucleotide to a cell and methods of treating a subject having Hepatitis C.

公开(公告)号：US10138514B2

公开(公告)日：2018-11-27

申请号：US15444826

申请日：2017-02-28

申请人： Illumina Cambridge Limited

发明人： Xiaohai Liu ,  Xiaolin Wu ,  Geoffrey Paul Smith

IPC分类号： C12Q1/68 ,  C07H19/073 ,  C12Q1/6869 ,  C07H19/10 ,  C07H19/14 ,  C07H19/173 ,  C07H19/20 ,  C12Q1/6876

CPC分类号： C12Q1/6869 ,  C07H19/073 ,  C07H19/10 ,  C07H19/14 ,  C07H19/173 ,  C07H19/20 ,  C12Q1/6876 ,  Y02P20/55

摘要： Some embodiments described herein relate to modified nucleotide and nucleoside molecules with novel 3′-hydroxy protecting groups. Also provided herein are methods to prepare such modified nucleotide and nucleoside molecules and sequencing by synthesis processes using such modified nucleotide and nucleoside molecules.

公开(公告)号：US20180265537A1

公开(公告)日：2018-09-20

申请号：US15460475

申请日：2017-03-16

申请人： Steven A. Benner

发明人： Steven A. Benner

IPC分类号： C07H19/10

CPC分类号： C07H19/10 ,  C07H19/20

摘要： This invention claims aqueous compositions that comprise triphosphates of 2′-deoxynucleoside derivatives that have, instead of a 3′-OH moiety, a 3′-ONH2 moiety; wherein said compositions contain less than 0.5 mole percent contaminating triphosphate having a 3′-OH moiety, as well as processes for providing such compositions. The compositions further must contain insubstantial amounts of hydroxylamine.

公开(公告)号：US10071112B2

公开(公告)日：2018-09-11

申请号：US15516657

申请日：2015-10-08

申请人： EPIGENETICS PHARMA LLC

发明人： Richard Daifuku

IPC分类号： C07H19/10 ,  C07H19/20 ,  A61K31/7068 ,  A61K47/54 ,  A61K47/55 ,  A61K31/355 ,  A61K47/48

CPC分类号： A61K31/7068 ,  A61K31/355 ,  A61K47/545 ,  A61K47/549 ,  A61K47/55 ,  A61K47/551 ,  C07H19/10 ,  C07H19/20

摘要： The present disclosure describes nucleoside and nucleoside analogs that are conjugated to a vitamin E derivative via a phosphate ester or a phosphoramidate linkage. The nucleoside or nucleoside analogs can provide enhanced therapeutic activity (e.g., antiproliferative activity against tumor cells) and/or greater chemical stability in aqueous solutions.

公开(公告)号：US10059734B2

公开(公告)日：2018-08-28

申请号：US15581834

申请日：2017-04-28

申请人： FUJIFILM Corporation

发明人： Hidenobu Kuniyoshi ,  Daisuke Nakagawa ,  Takuya Matsumoto ,  Yuji Yoshimitsu

IPC分类号： C07H19/10 ,  A61P35/02 ,  A61K31/7068 ,  A61P35/00

CPC分类号： C07H19/10 ,  A61K31/7068 ,  A61P35/00 ,  A61P35/02

摘要： Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General Formula [1] (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.

公开(公告)号：US10040814B2

公开(公告)日：2018-08-07

申请号：US15809730

申请日：2017-11-10

申请人： Janssen Sciences Ireland UC

发明人： Ioannis Nicolaos Houpis ,  Tim Hugo Maria Jonckers ,  Pierre Jean-Marie Bernard Raboisson ,  Abdellah Tahri

IPC分类号： C07H19/06 ,  C07H19/10 ,  C07H19/24 ,  A61K31/7072 ,  C07H19/11

CPC分类号： C07H19/10 ,  A61K31/7072 ,  C07H19/06 ,  C07H19/11 ,  C07H19/24

摘要： The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.