公开(公告)号：US20240139227A1

公开(公告)日：2024-05-02

申请号：US18511973

申请日：2023-11-16

Applicant: Gilead Sciences, Inc.

Inventor： Jinfa Du ,  Dhanapalan Nagarathnam ,  Michael Joseph Sofia ,  Peiyuan Wang

IPC: A61K31/7072 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K45/06 ,  C07D417/14 ,  C07H17/02 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/20

CPC classification number: A61K31/7072 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7076 ,  A61K45/06 ,  C07D417/14 ,  C07H17/02 ,  C07H19/04 ,  C07H19/06 ,  C07H19/10 ,  C07H19/20 ,  A61K31/7068 ,  Y02A50/30

Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure:




Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.

公开(公告)号：US20240084295A1

公开(公告)日：2024-03-14

申请号：US18331536

申请日：2023-08-29

Applicant: Hoffmann-La Roche Inc.

Inventor： Martin Bollmark ,  Walter Fernando Sehgelmeble Torrejon ,  Filippo Sladojevich ,  Ulf Tedebark

IPC: C12N15/11 ,  C07H19/10 ,  C07H19/20

CPC classification number: C12N15/111 ,  C07H19/10 ,  C07H19/20 ,  C12N2310/313 ,  C12N2310/3231 ,  C12N2330/30

Abstract: The invention provides the use of a compound of formula (I), as defined, for the preparation of an oligonucleotide comprising at least one phosphorodithioate internucleoside linkage. Various synthesis methods using compounds of formula (I) are provided.

公开(公告)号：US20230167142A1

公开(公告)日：2023-06-01

申请号：US17936970

申请日：2022-09-30

Applicant: Board of Regents, The University of Texas System

Inventor： Victoria YAN ,  Cong-Dat PHAM ,  Florian MULLER

IPC: C07F9/59 ,  C07F9/6558 ,  C07F9/24 ,  C07F9/58 ,  C07H19/20 ,  C07F9/6561 ,  A61K45/06 ,  A61P35/00

CPC classification number: C07F9/59 ,  C07F9/65583 ,  C07F9/24 ,  C07F9/58 ,  C07H19/20 ,  C07F9/65616 ,  A61K45/06 ,  A61P35/00

Abstract: Provided is a method for the preparation of mono-amidated phosphates or phosphonates as well as mono-amidated phosphates and phosphonates prepared by such method.

公开(公告)号：US11655502B2

公开(公告)日：2023-05-23

申请号：US17228477

申请日：2021-04-12

Applicant: ILLUMINA CAMBRIDGE LIMITED

Inventor： Elena Cressina ,  Antoine Francais ,  Xiaohai Liu

IPC: C12Q1/68 ,  C07H19/06 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6869 ,  C07H19/073 ,  C12Q1/6809 ,  C12Q1/6816

CPC classification number: C12Q1/6869 ,  C07H19/06 ,  C07H19/073 ,  C07H19/10 ,  C07H19/14 ,  C07H19/16 ,  C07H19/20 ,  C07H21/00 ,  C07H21/04 ,  C12Q1/6809 ,  C12Q1/6816 ,  C12Q1/6869 ,  C12Q2525/117 ,  C12Q2535/122

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

公开(公告)号：US20230138433A1

公开(公告)日：2023-05-04

申请号：US17974229

申请日：2022-10-26

Applicant: Southern Research Institute

Inventor： Omar Moukha-Chafiq ,  Corinne Elizabeth Augelli-Szafran ,  Rebecca Boohaker ,  Larry D. Bratton ,  Marina Fosso Yatchange ,  Anish K. Vadukoot

IPC: C07H19/16 ,  C07H19/20 ,  A61P35/00

Abstract: The present disclosure is concerned with Clofarabine analogs for the treatment of various cancers such as, for example, sarcomas, carcinomas, hematological cancers, solid tumors, breast cancer, cervical cancer, gastrointestinal cancer, colorectal cancer, brain cancer, skin cancer, prostate cancer, ovarian cancer, bladder cancer, thyroid cancer, testicular cancer, pancreatic cancer, endometrial cancer, melanomas, gliomas, leukemias, lymphomas, chronic myeloproliferative disorders, myelodysplastic syndromes, myeloproliferative neoplasms, and plasma cell neoplasms (myelomas). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US11597745B2

公开(公告)日：2023-03-07

申请号：US16977525

申请日：2019-03-08

Applicant: Japan Science and Technology Agency

Inventor： Hiroshi Abe ,  Yasuaki Kimura

IPC: C07H19/20 ,  C07H19/16

Abstract: A β-modified phosphoric acid compound precursor that inhibits the progress of a phosphorylation reaction having a partial structure represented by where A1 represents —SR1, —S—S—R1, —SeR1, or —X, where X is a halogen selected from fluoro, chloro, bromo, and iodo; R1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L1 represents hydrogen, an alkyl group having 1 to 20 carbon atoms, or the like; L2 represents an alkyl group having 1 to 20 carbon atoms, or the like; L1 and L2 may be linked to each other to form a 4 to 6-membered ring structure; L1 and L2 may each have a substituent; and the symbol * represents a bond to be bonded to a phosphate group by phosphorylation. Further, provided are a reaction inhibitor and a medicine, each of which includes the β-modified phosphoric acid compound precursor.

公开(公告)号：US11566042B2

公开(公告)日：2023-01-31

申请号：US16940039

申请日：2020-07-27

Applicant: ZATA Pharmaceuticals, Inc

Inventor： David R. Tabatadze ,  Ivan B. Yanachkov

IPC: C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H19/10 ,  C07H19/20 ,  A61K31/7088

Abstract: Compositions and compounds of nucleoside phosphoramidites and modified oligonucleotides, each comprising one or more charge-neutralizing moieties according to the formula V The nucleoside phosphoramidites permit facile attachment of the neutralizing moieties on the backbones of the modified oligonucleotides. The modified oligonucleotides can be used as therapeutic agents (i.e., oligotherapeutics) for the treatment of cancer, autoimmune disorders, genetic diseases, infectious diseases, neurological diseases, inflammatory diseases, metabolic diseases and others.

公开(公告)号：US20230028388A1

公开(公告)日：2023-01-26

申请号：US17816555

申请日：2022-08-01

Applicant: The Trustees of Columbia University in the City of New york

Inventor： Jingyue Ju ,  Xiaoxu Li ,  Xin Chen ,  Zengmin Li ,  Shiv Kumar ,  Shundi Shi ,  Cheng Guo ,  Jianyi Ren ,  Min-Kang Hsieh ,  Minchen Chien ,  Chuanjuan Tao ,  Ece Erturk ,  Sergey Kalachikov ,  James J. Russo

IPC: C12Q1/6869 ,  C07H19/10 ,  C07H19/20 ,  C07H19/14

Abstract: Disclosed herein, inter alia, are compounds, compositions, and methods of use thereof in the sequencing of a nucleic acid.

公开(公告)号：US11440934B2

公开(公告)日：2022-09-13

申请号：US16768037

申请日：2018-12-11

Applicant: Yabao Pharmaceutical Group Co., Ltd.

Inventor： Fanghui Tang ,  Jiyu Bao ,  Junfeng Gao ,  Zhouhong Tan

IPC: C07H19/20 ,  C07H1/04

Abstract: The present application relates to a method for prepare a Cangrelor tetrasodium salt, comprising: using N-[2-(methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)sulfonyl]adenosine as a raw material to undergo two steps of reaction to obtain a reaction solution containing the Cangrelor tetrasodium salt; separating and purifying once by C18 silica gel column chromatography so as to obtain a Cangrelor tetrasodium salt pure product. The present application has the advantages of short synthesis route, mild reaction conditions, sufficient reaction, simple operation, high product yield, high purity, and environmental friendliness, and is suitable for large-scale preparation.

公开(公告)号：US20220220145A1

公开(公告)日：2022-07-14

申请号：US17604681

申请日：2020-04-21

Applicant: LIGAND PHARMACEUTICALS, INC.

Inventor： Lin Zhi

IPC: C07H19/10 ,  C07H19/20 ,  A61P1/16

Abstract: Provided herein are cyclic phosphate compounds, their preparation and their uses, such as treating liver diseases or conditions or a disease or condition in which the physiological or pathogenic pathways involve the liver.