公开(公告)号：US20200181186A1

公开(公告)日：2020-06-11

申请号：US16623263

申请日：2018-06-14

Applicant: NuCana plc

Inventor： Hugh Griffith ,  Gordon Kennovin ,  Venkata Lakshmi Narasimha Rao Dammalapati ,  Mani Bushan Kotala

IPC: C07H1/02 ,  C07H19/10 ,  C07H19/20

Abstract: The present invention generally relates to a process for the preparation of certain anticancer compounds as specific phosphate diastereoisomers.

公开(公告)号：US10669580B2

公开(公告)日：2020-06-02

申请号：US15684726

申请日：2017-08-23

Applicant: Roche Sequencing Solutions, Inc.

Inventor： Dmitriy Gremyachinskiy ,  Peter Crisalli ,  Andrew Trans ,  Ashwini Bhat

IPC: C12Q1/68 ,  C07H19/04 ,  C07H19/10 ,  C07H21/04 ,  C12Q1/6869 ,  C12Q1/6823 ,  C07H19/06 ,  C07K14/00

Abstract: The present disclosure relates to compounds comprising a negatively-charged polymer moiety which is capable of entering a nanopore and upon entering a nanopore in the presence of positive ions results in an increased flow of the positive ions through the nanopore. The present disclosure provides methods of preparing the compounds and for their use as nanopore-detectable tags, in particular, for nanopore-based nucleic acid detection and sequencing.

公开(公告)号：US10669538B2

公开(公告)日：2020-06-02

申请号：US15293102

申请日：2016-10-13

Applicant: NUEVOLUTION A/S

Inventor： Henrik Pedersen ,  Alex Haahr Gouliaev ,  Thomas Franch ,  Christian Klarner Sams ,  Eva Kampmann Olsen ,  Frank Abilgaard Slok ,  Gitte Nystrup Husemoen ,  Jakob Felding ,  Lene Hyldtoft ,  Mads Norregaard-Madsen ,  Michael Anders Godskesen ,  Sanne Schroder Glad ,  Thomas Thisted ,  Per-Ola Freskgard ,  Anette Holtmann

IPC: C12N15/10 ,  C07D405/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H23/00 ,  C12P19/34 ,  C40B40/00

Abstract: The present invention relates to a method for synthesising templated molecules. In one aspect of the invention, the templated molecules are linked to the template which templated the synthesis thereof. The invention allows the generation of libraries which can be screened for e.g. therapeutic activity.

公开(公告)号：US10669300B2

公开(公告)日：2020-06-02

申请号：US15514673

申请日：2015-09-29

Applicant: NuCana plc

Inventor： Hugh Griffith

IPC: C07H19/10

Abstract: Disclosed are methods of separating the diastereoisomers of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-phosphate (NUC-1031), or salts thereof, using crystallisation. In particular, crystallisation from isopropyl alcohol provides gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate in high diastereoisomeric purity: Also disclosed is a crystalline form of gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(S)-phosphate. Disclosed are methods of isolating gemcitabine-[phenyl-(benzoxy-L-alaninyl)]-(R)-phosphate in high diastereoisomeric purity:

公开(公告)号：US20200109161A1

公开(公告)日：2020-04-09

申请号：US16720693

申请日：2019-12-19

Applicant: Janssen Sciences Ireland Unlimited Company

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

IPC: C07H19/10 ,  C07H1/00 ,  C07H19/06 ,  C07H19/11 ,  A61K31/7072 ,  C07H19/24

Abstract: 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 thereofThe 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.

公开(公告)号：US10597422B2

公开(公告)日：2020-03-24

申请号：US16248273

申请日：2019-01-15

Applicant: Merck Sharp & Dohme Corp.

Inventor： Daniel DiRocco ,  Artis Klapars ,  Edward C. Sherer

IPC: C07D239/00 ,  C07D421/00 ,  C07D517/00 ,  C07H19/10 ,  C07H19/06 ,  C07H19/24 ,  C07D487/04 ,  C07H9/06 ,  C07H1/00 ,  C07H1/02

Abstract: The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

公开(公告)号：US20200080122A1

公开(公告)日：2020-03-12

申请号：US16465733

申请日：2017-11-30

Applicant: President and Fellows of Harvard College

Inventor： Kettner John Frederick Griswold, Jr. ,  Richie Kohman ,  George M. Church ,  Jonathan Rittichier

IPC: C12P19/34 ,  C07H19/20 ,  C07H19/10 ,  C07H21/02 ,  C07H21/04

Abstract: Cleavable nucleotide analogs are provided. The nucleotide analog includes a nucleotide molecule attached to a cleavable moiety wherein the cleavable moiety comprises a protective group and/or a linker attached to a fluorophore. The cleavable moiety is linked to the oxygen atom of the 3′-OH of the pentose of the nucleotide molecule. The nucleotide analogs can be used in making polynucleotide molecules using template independent polymerases. The nucleotide analogs can act as reversible terminators during DNA sequencing by synthesis. The cleavage of the cleavable moiety restores a free 3′-OH functional group allowing growth of the polynucleotide molecule. The general structures as well as proposed synthetic schemes for the nucleotide analogs are also provided.

公开(公告)号：US10526648B2

公开(公告)日：2020-01-07

申请号：US16033118

申请日：2018-07-11

Applicant: ILLUMINA CAMBRIDGE LIMITED

Inventor： Elena Cressina ,  Antoine Francais ,  Xiaohai Liu

IPC: C12Q1/68 ,  C07H19/10 ,  C12Q1/6869 ,  C07H19/073 ,  C07H19/14 ,  C07H21/04 ,  C12Q1/6809 ,  C12Q1/6816

Abstract: The present disclosure relates to new nucleotide and oligonucleotide compounds and their use in nucleic acid sequencing applications.

公开(公告)号：US10526363B2

公开(公告)日：2020-01-07

申请号：US15503776

申请日：2015-08-14

Applicant: Merck Sharp & Dohme Corp. ,  Merck Sharp & Dohme Limited ,  John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

Inventor： John Simon Edwards ,  Peter Richard Mullens ,  Edward Cleator ,  Bryon L. Simmons ,  Courtney K. Maguire ,  Jeremy Peter Scott ,  Nobuyoshi Yasuda ,  Yong-Li Zhong ,  Lisa F. Frey ,  Peter G. Dormer ,  Andrew Brunskill ,  Artis Klapars ,  Pu Qian ,  Yi Zhang ,  Baoqiang Wan ,  Eric Ashley

IPC: C07H19/10 ,  C07F9/58 ,  C07H19/06 ,  C07F9/24 ,  C07F9/6558

Abstract: The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.

公开(公告)号：US20190389897A1

公开(公告)日：2019-12-26

申请号：US16333673

申请日：2017-09-18

Applicant: LCB PHARMA INC. ,  UNIVERSITÉ D'OTTAWA

Inventor： Yvan GUINDON ,  Philippe MOCHIRIAN ,  Mona NEMER

IPC: C07H19/10 ,  C07H19/20 ,  C07H19/23 ,  A61P9/00

Abstract: Nucleoside and nucleotide analogues that can be used as cardioprotective agents are provided. The nucleosides and nucleotide analogues comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary stereogenic all-carbon centers at the 2′ position and a phosphonate ester at the 5′ position.