公开(公告)号：US11891655B2

公开(公告)日：2024-02-06

申请号：US17730004

申请日：2022-04-26

申请人： Battelle Memorial Institute

发明人： Aaron T. Wright ,  Susan Ramos-Hunter ,  Christopher Whidbey

IPC分类号： C12Q1/68 ,  C12Q1/6837 ,  C07K1/13 ,  C12Q1/6841 ,  C12Q1/48 ,  C07D311/16 ,  C07D405/04 ,  C07C233/33 ,  C07C233/20 ,  C07C247/00 ,  G01N33/58 ,  C07C305/22 ,  C07D203/26 ,  C07C247/12 ,  C07C203/04 ,  C07C271/28 ,  C07D405/12 ,  C07H19/067 ,  C07H15/203 ,  C12Q1/34 ,  C07C317/40

CPC分类号： C12Q1/6837 ,  C07C203/04 ,  C07C233/20 ,  C07C233/33 ,  C07C247/00 ,  C07C247/12 ,  C07C271/28 ,  C07C305/22 ,  C07C317/40 ,  C07D203/26 ,  C07D311/16 ,  C07D405/04 ,  C07D405/12 ,  C07H15/203 ,  C07H19/067 ,  C07K1/13 ,  C12Q1/34 ,  C12Q1/48 ,  C12Q1/6841 ,  G01N33/582 ,  G01N33/583 ,  C12Q2565/514 ,  C12Q2600/106 ,  G01N2333/91177

摘要： Activity-based probes that can be used to selectively identify and characterize enzymes that are involved in different phases of xenobiotic metabolism in a host and its microbiota population(s) are described. The activity-based probes described specifically label only their target active enzymes involved in xenobiotic metabolism and therefore provide a measurement of true protein functional activity rather than transcript or protein abundance. The activity-based probes also provide multimodal profiling of these active enzymes. Methods for preparing the activity based probes and exemplary methods for their use also are disclosed.

公开(公告)号：US20230399354A1

公开(公告)日：2023-12-14

申请号：US17999080

申请日：2022-09-16

申请人： BEIJING RIBIO PHARMA CO., LTD.

发明人： Yazhou LI ,  Yibiao LIU ,  Guanshen ZHOU ,  Zhenchang CHEN ,  Hongjuan ZHANG

IPC分类号： C07H19/067

CPC分类号： C07H19/067

摘要： The present disclosure provides a preparation method of a 2′-substituted pyrimidine nucleoside, including the following steps: subjecting a compound of Formula I or Formula II to a series of process including dehydration, selective 5′-protection, ring-opening reaction using magnesium alkoxide and deprotection to obtain a 2′-substituted pyrimidine nucleoside of Formula VII or Formula VIII. In the present disclosure, the preparation method has desirable universality for different substrates; the ring-opening with a protected anhydrous pyrimidine nucleoside improves a solubility of the substrate, with milder reaction conditions than those of a traditional synthetic route; the formation of a dimer is avoided during the ring-opening to improve the yield; in addition, an intermediate (5′-O-bis-p-methoxytrityl-protected 2′-substituted pyrimidine nucleoside) can be directly used in synthesis of a corresponding phosphoramidite monomer, with a wider potential for use.

公开(公告)号：US20230357304A1

公开(公告)日：2023-11-09

申请号：US18021907

申请日：2021-09-14

申请人： Wellstat Therapeutics Corporation

发明人： Reid Warren VON BORSTEL ,  SIMPSON David Michael ,  Rolando Alejandro GARCIA GARCIA

IPC分类号： C07H19/067

CPC分类号： C07H19/067

摘要： 5′-O-(Acetoacetyl)-2′,3′-di-O-acetyluridine is useful in the treatment or prevention of disorders characterized by cerebral metabolic energy failure or diminished mitochondrial energy reserve capacity.

公开(公告)号：US11753433B2

公开(公告)日：2023-09-12

申请号：US17222515

申请日：2021-04-05

申请人： Epizyme, Inc.

发明人： Edward James Olhava

IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H19/16 ,  A61K31/7076 ,  A61K31/4184 ,  C07D235/12 ,  C07H19/06 ,  C07H19/067 ,  C07H1/06 ,  C07H19/167

CPC分类号： C07H19/16 ,  A61K31/4184 ,  A61K31/7076 ,  C07D235/12 ,  C07B2200/13 ,  C07H1/06 ,  C07H19/06 ,  C07H19/067 ,  C07H19/167 ,  Y02A50/30

摘要： The present invention provides an efficient process for the synthesis of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof and methods for 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. The present invention also provides novel crystalline forms of (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol and hydrates thereof (Form A, Form B, and Form C), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.

公开(公告)号：US11655268B2

公开(公告)日：2023-05-23

申请号：US16963900

申请日：2019-01-24

申请人： ST Pharm Co., Ltd.

发明人： Kyungjin Kim ,  Meehyein Kim ,  Uk-Il Kim ,  Yun Young Go ,  Hwajung Nam ,  Hyung Tae Bang ,  Jin Soo Shin ,  Jihye Yoon ,  Yejin Jang

IPC分类号： C07H19/067

CPC分类号： C07H19/067

摘要： The present disclosure relates to a novel nucleoside or nucleotide derivative, a racemate thereof, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating viral infection-associated diseases, containing the same as an active ingredient.

公开(公告)号：US11628181B2

公开(公告)日：2023-04-18

申请号：US16921359

申请日：2020-07-06

申请人： Emory University

发明人： George R. Painter ,  David Guthrie ,  Gregory R. Bluemling ,  Michael G. Natchus

IPC分类号： A01N43/04 ,  A61K31/70 ,  A61K31/7068 ,  C07H19/067 ,  C07H19/11 ,  C07H19/10 ,  A61K9/00 ,  C07H19/073 ,  A61K45/06

摘要： This disclosure relates to N4-hydroxycytidine derivatives, compositions, and methods related thereto. In certain embodiments, the disclosure relates to the treatment and prophylaxis of viral infections.

公开(公告)号：US20220306679A1

公开(公告)日：2022-09-29

申请号：US17753336

申请日：2020-08-28

申请人： Dicerna Pharmaceuticals, Inc.

发明人： Weimin WANG ,  Naim NAZEF

IPC分类号： C07H21/02 ,  C07H19/167 ,  C07H19/067 ,  C07H1/00

摘要： The present invention relates to methods for synthesizing compounds useful as potent and stable RNA interference agents, derivatives thereof, and intermediates thereto.

公开(公告)号：US20220135611A1

公开(公告)日：2022-05-05

申请号：US17400515

申请日：2021-08-12

申请人： Tufts University

发明人： Philip G. Haydon ,  Jinbo Lee

IPC分类号： C07H19/06 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7064 ,  C07D413/14 ,  C07D405/14 ,  C07H19/067 ,  C07D405/04

摘要： This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.

公开(公告)号：US20220073916A1

公开(公告)日：2022-03-10

申请号：US17405708

申请日：2021-08-18

申请人： Roche Innovation Center Copenhagen A/S

发明人： Konrad BLEICHER ,  Jessica Marine Aurore BASTIEN

IPC分类号： C12N15/113 ,  C07H21/02 ,  C07H19/067

摘要： The invention relates to a compound of formula (II) wherein X, Y, R5, Rx, Ry and Nu are as defined in the description and in the claims. The compound of formula (II) can be used in the manufacture of medicaments.

公开(公告)号：US20220010309A1

公开(公告)日：2022-01-13

申请号：US17213852

申请日：2021-03-26

申请人： UNIVERSITY OF MASSACHUSETTS

发明人： Anastasia Khvorova ,  Loïc Maurice René Jean Roux ,  Ken Yamada

IPC分类号： C12N15/113 ,  C07H21/02 ,  C07H19/067

摘要： This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.