公开(公告)号：US20190100552A1

公开(公告)日：2019-04-04

申请号：US16134520

申请日：2018-09-18

申请人： Epizyme, Inc.

发明人： Edward J. OLHAVA ,  Richard CHESWORTH ,  Roy M. POLLOCK ,  Lei JIN

IPC分类号： C07H19/16 ,  C07H19/14 ,  C07D473/34 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7068 ,  A61K31/708 ,  A61K31/7064

摘要： The present invention relates to DOT1L inhibitors and methods of identifying, designing, or optimizing them. The present invention also relates to crystals of DOT1L-inhibitor complexes, the crystal structures thereof, and the use of the crystal structures. Also disclosed are pharmaceutical compositions containing these DOT1L inhibitors and methods of treating disorders in which DOT1-mediated protein methylation plays a part, such as cancer and neurological disorders, by administering these compounds and pharmaceutical compositions to subjects in need thereof.

公开(公告)号：US20190092806A1

公开(公告)日：2019-03-28

申请号：US16200564

申请日：2018-11-26

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 ,  C12Q1/686

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：US20190085015A1

公开(公告)日：2019-03-21

申请号：US16150180

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 ,  C12Q1/6872 ,  C12Q1/6876 ,  C07H19/10 ,  C12Q1/6869 ,  C12Q1/6874 ,  C12Q1/68 ,  C07H21/00 ,  C12Q1/686

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：US10214768B2

公开(公告)日：2019-02-26

申请号：US15851014

申请日：2017-12-21

申请人： Illumina Cambridge Limited

发明人： Nikolai Romanov

IPC分类号： C12Q1/6816 ,  C12Q1/6876 ,  C12Q1/6869 ,  C07D491/052 ,  C07H21/00 ,  C07H19/14 ,  C07H19/10 ,  C07D491/147 ,  C09K11/06 ,  C07D491/04

摘要： The present application relates to new coumarin compounds and their uses as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications.

公开(公告)号：US20190031704A1

公开(公告)日：2019-01-31

申请号：US16149098

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 ,  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：US10144961B2

公开(公告)日：2018-12-04

申请号：US15596379

申请日：2017-05-16

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

发明人： Jingyue Ju ,  Huanyan Cao ,  Zengmin Li ,  Qinglin Meng ,  Jia Guo ,  Shenglong Zhang ,  Lin Yu

IPC分类号： C12Q1/68 ,  C12Q1/6869 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20

摘要： This invention provides novel azido linkers for deoxynucleotide analogs having a detectable marker attached thereto.

公开(公告)号：US09988416B2

公开(公告)日：2018-06-05

申请号：US15465485

申请日：2017-03-21

申请人： NOVARTIS AG

发明人： Martijn Fenaux ,  Oliver Saunders ,  Fumiaki Yokokawa ,  Weidong Zhong

IPC分类号： C07H19/14 ,  A61K31/7064 ,  C07H19/04 ,  C07D487/04

CPC分类号： C07H19/14 ,  A61K31/7064 ,  C07D487/04 ,  C07H19/04

摘要： The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent, and methods of using the compounds and compositions for treatment of viral infections, especially HRV.

公开(公告)号：US20180111957A1

公开(公告)日：2018-04-26

申请号：US15575743

申请日：2016-05-23

申请人： ILLUMINA CAMBRIDGE LIMITED

发明人： Nikolai Romanov ,  Xiaolin Wu

IPC分类号： C07H19/10 ,  C09B23/06 ,  C09K11/06 ,  C07H19/14 ,  C09B69/10 ,  C12Q1/6876

CPC分类号： C07H19/10 ,  C07D401/06 ,  C07H19/14 ,  C09B23/06 ,  C09B69/105 ,  C09K11/06 ,  C12Q1/6876

摘要： The present disclosure relates to new compounds and their use as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications. The labels are advantageous due to their long Stokes shifts.

公开(公告)号：US09840532B2

公开(公告)日：2017-12-12

申请号：US15139370

申请日：2016-04-27

申请人： Eli Lilly and Company

发明人： Guillermo S Cortez ,  Zahid Quyoom Bonday

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H19/14 ,  C07D487/04 ,  A61K31/7068 ,  A61K31/706 ,  A61K31/7076

CPC分类号： C07H19/14 ,  A61K31/706 ,  A61K31/7068 ,  A61K31/7076 ,  C07D487/04

摘要： The present invention relates to novel 5′-substituted nucleoside compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, more particularly for the treatment of cancer, in particular glioblastomas, melanoma, sarcomas, gastric cancer, pancreatic cancer, cholangiocarcinoma, bladder cancer, breast cancer, non-small cell lung cancer, leukemias including acute myeloid leukemia, and lymphomas.

公开(公告)号：US20170240584A1

公开(公告)日：2017-08-24

申请号：US15453702

申请日：2017-03-08

申请人： Institute of Organic Chemistry and Biochemistry ASCR,V.V.I.

发明人： Aurelie Bourderioux ,  Michal Hocek ,  Petr Naus

IPC分类号： C07H19/14 ,  A61K45/06 ,  A61K31/7064

CPC分类号： C07H19/14 ,  A61K31/7064 ,  A61K45/06 ,  A61K2300/00

摘要： The invention provides compounds of formula I, wherein R1, R2 and R3 have values defined in the specification and a pharmaceutically acceptable salt thereof; or an optical isomer thereof; or a mixture of optical isomers, as well as compositions comprising such compounds and therapeutic methods that utilize such compounds and/or compositions.