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1. 发明申请

WO2022175685A1 MODIFIED GUANINES 审中-公开
公开(公告)号：WO2022175685A1
公开(公告)日：2022-08-25
申请号：PCT/GB2022/050463
申请日：2022-02-21
申请人： NUCLERA NUCLEICS LTD
发明人： MCINROY, Gordon Ross , FOX, Martin Edward , SRIVASTAVA, Puneet , MATUSZEWSKI, Michal Robert
IPC分类号： C07H19/04 , C07H1/00 , C07H19/12 , C07H19/14 , C07H21/04 , C12P19/34
摘要： The present invention relates to a compound according to Formula (la) or (lb) wherein R1; R3; Y and X are defined herein, and their use in methods of nucleic acid synthesis. Disclosed herein is a method of reducing the deamination of the guanine base during oligonucleotide synthesis. The method is particularly applicable when nitrite is used to remove an aminooxy terminating moiety from the sugar hydroxyl.

2. 发明申请

WO2021211890A1 COMPOSITIONS COMPRISING 2'-DEOXYCYTIDINE ANALOGS AND USE THEREOF FOR THE TREATMENT OF SICKLE CELL DISEASE, THALASSEMIA, AND CANCERS 审中-公开
公开(公告)号：WO2021211890A1
公开(公告)日：2021-10-21
申请号：PCT/US2021/027548
申请日：2021-04-15
申请人： ADIMABIO LLC
发明人： VADIVELU, Santhosh
IPC分类号： A61K31/706 , C07H19/04 , A61P7/06 , A61P35/02
摘要： In one aspect, the disclosure relates to pharmaceutical compositions comprising 2'-deoxycytidine analogs, oral and other dosage formulations containing the same, and methods of making the same. In another aspect, the disclosure relates to methods of treating hematological disorders and diseases associated with abnormal cell proliferation using the same. In a still further aspect, the disclosure relates to kits comprising 2'-deoxycytidine analogs useful for treating hematological disorders and diseases associated with abnormal cell proliferation. In still another aspect, the disclosure relates to methods for increasing fetal hemoglobin levels in a subject. 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 disclosure.

3. 发明申请

WO2021001538A1 NOVEL GALACTOSIDE INHIBITOR OF GALECTINS 审中-公开
公开(公告)号：WO2021001538A1
公开(公告)日：2021-01-07
申请号：PCT/EP2020/068831
申请日：2020-07-03
申请人： GALECTO BIOTECH AB
发明人： ZETTERBERG, Fredrik , PETERSON, Kristoffer
IPC分类号： A61P29/00 , A61P35/00 , C07H19/04 , C07H19/052 , C07H19/24 , A61K31/7056
摘要： The present invention relates to a D-galactopyranose compound of formula (1) wherein the pyranose ring is α-D-galactopyranose, and these compounds are high affinity galectin-3 inhibitors for use in treatment of inflammation; Inflammation induced thrombosis; Atopic dermatitis; Acute coronary syndrome; fibrosis, such as pulmonary fibrosis, liver fibrosis, kidney fibrosis, ophthalmological fibrosis and fibrosis of the skin and heart; local fibrosis such as Dupuytren's disease and Peyronie's disease; fibrotic complications of other therapies such as coronary stents, bile duct stents, cerebral artery stents, ureter stents; scleroderma; scarring; keloid formation; covid-19; acute lung injury; ARDS; viral pneumonitis, aberrant scar formation; surgical adhesions; septic shock; cancer, such as colorectal cancer, other gastrointestinal carcinomas such as pancreatic cancer, gastric cancer, biliary tract cancer, lung cancers, mesothelioma, female cancers like breast cancer, ovarian cancer, uterine cancer, cancer of the cervix uteri, cancer of the salpingx, cerebral cancers such as medulloblastomao, glioma, meningioma, sarcomas of the bones and muscles and other sarcomas, leukemias and lymphomas, such as T-cell lymphomas; transplant rejection; metastasising cancers; ageing; Dementia; Alzheimers; TGFbeta driven bone disease such as osteogenesis imperfecta; Pulmonary hypertension; autoimmune diseases, such as psoriasis, rheumatoid arthritis, Rheumatoid lung; Crohn's disease, ulcerative colitis, ankylosing spondylitis, systemic lupus erythematosus; viral infections such as influenza virus, HIV, Herpes virus, Coronaviruses, Hepatitis C; metabolic disorders; heart disease; heart failure; pathological angiogenesis, such as ocular angiogenesis or a disease or condition associated with ocular angiogenesis, e.g. neovascularization related to cancer; and eye diseases, such as age-related macular degeneration and corneal neovascularization; atherosclerosis; metabolic diseases; diabetes; type I diabetes; type 2 diabetes; insulin resistens; obesity; Marfans syndrome; Loeys–Dietz syndrome; nephropathy; Diastolic HF; fibrotic lung complications of aPD1 and other CPI therapies; asthma and other interstitial lung diseases, including Hermansky-Pudlak syndrome, liver disorders, such as non- alcoholic steatohepatitis or non-alcoholic fatty liver disease; uterine disease such as uterine fibroids and uterine or cervical fibrosis.

4. 发明申请

WO2020178768A1 3'3'-CYCLIC DINUCLEOTIDE ANALOGUE COMPRISING A CYCLOPENTANYL MODIFIED NUCLEOTIDE AS STING MODULATOR 审中-公开
公开(公告)号：WO2020178768A1
公开(公告)日：2020-09-10
申请号：PCT/IB2020/051883
申请日：2020-03-04
申请人： INSTITUTE OF ORGANIC CHEMISTRY AND BIOCHEMISTRY ASCR, V.V.I.
发明人： BIRKUS, Gabriel , BREHOVA, Petra , DEJMEK, Milan , NENCKA, Radim , PAV, Ondrej , SALA, Michal
IPC分类号： C07H19/213 , C07H19/04 , C07F9/6574 , A61K31/7076 , A61K31/665 , A61P37/02 , A61P37/08 , A61P31/12 , A61P35/00
摘要： The present disclosure relates to 3'3'-cyclic dinucleotides comprising a carbocyclic nucleotide and derivatives thereof, that can modulate the activity of the STING adaptor protein.

5. 发明申请

WO2019112567A1 METHODS AND COMPOSITIONS RELATED TO SELECTING VARIANT PROTEASES 审中-公开
公开(公告)号：WO2019112567A1
公开(公告)日：2019-06-13
申请号：PCT/US2017/064697
申请日：2017-12-05
申请人： THE SCRIPPS RESEARCH INSTITUTE
发明人： PAEGEL, Brian, M. , TRAN, Duc, T. , CAVETT, Valerie, J.
IPC分类号： C07H17/00 , C07H19/04 , C07H19/20 , C07H21/02
摘要： This invention provides protease activity screening matrices that contain a solid support conjugated to a substrate moiety that can be specifically cleaved by a specific protease. The invention also provides methods for utilizing the protease activity screening matrices described herein For identifying a variant protease that recognizes a desired substrate cleavage site. The invention additionally provides specific variant trypsin enzymes or enzymatic fragments that have citrulline-dependent proteolytic activities.

6. 发明申请

WO2018236814A2 NICOTINAMIDE RIBOSIDE DERIVATIVES AND THEIR USES 审中-公开
公开(公告)号：WO2018236814A2
公开(公告)日：2018-12-27
申请号：PCT/US2018/038201
申请日：2018-06-19
申请人： GANAPATI, Gangadhara , ARVIND, Atignal Shankara Rao
发明人： GANAPATI, Gangadhara , ARVIND, Atignal Shankara Rao
IPC分类号： C07H19/04 , C07H19/048 , A61K31/706 , A61K31/7064 , A61P29/00 , A61P35/00
摘要： The disclosure provides derivatives of both the oxidized form and the reduced form of nicotinamide riboside (NR) and nicotinic acid riboside (NAR). The NR and NAR derivatives have improved stability and bioavailability compared to NR and NAR, and can increase cellular NAD+ levels and improve mitochondrial function. Therefore, the NR and NAR derivatives are useful for treating mitochondrial diseases, mitochondria-related diseases and conditions, and other disorders and conditions.

7. 发明申请

WO2018200859A1 MULTITARGETED NUCLEOSIDE DERIVATIVES 审中-公开
公开(公告)号：WO2018200859A1
公开(公告)日：2018-11-01
申请号：PCT/US2018/029631
申请日：2018-04-26
申请人： KALMAN, Thomas, I.
发明人： KALMAN, Thomas, I.
IPC分类号： A61K31/712 , A61K48/00 , C07H19/04
摘要： Multitargeted pyrimidlne nucleoside carbamates, substituted with fluorine at both the base and the sugar moieties, are disclosed (see Formula I) where R =linear or branched alkyl (C1-7); R' = H, hydroxy protecting group; R" = H, phosphate ester, amino acid alkyl (C1- ester phoshoramidate, or phosphorodiamidate. The disclosed compounds are fluoropyrimidine prodrugs that are characterized by a novel combination of structural components that provide intracellular metabolites capable of 1 ) inhibiting several cellular enzymes required for the synthesis and proper functioning of DNA, and 2) causing DNA damage by misincorporation into DNA. By acting on multiple targets with different mechanisms of action, compounds of Formula I reduce the likelihood of the emergence of drug resistance, a major drawback of the use of nucleoside-based anticancer and antiviral drugs.

8. 发明申请

WO2017184885A1 USE OF NICOTINIC ACID RIBOSIDE OR NICOTINAMIDE RIBOSITE DERIVATIVES, AND REDUCED DERIVATIVES THEREOF, AS NAD+INCREASING PRECURSORS 审中-公开
标题翻译：尼妥珠酸或烟酰胺半乳糖衍生物及其还原衍生物的用途，作为NAD +增加的前体
公开(公告)号：WO2017184885A1
公开(公告)日：2017-10-26
申请号：PCT/US2017/028673
申请日：2017-04-20
申请人： CHROMADEX INC.
发明人： DELLINGER, Ryan , RHONEMUS, Troy , MORRIS, Mark , ERICKSON, Aron , CASSER, Hadi , MIGAUD, Marie, E.
IPC分类号： A61K31/44 , A61K31/706 , A61K31/7052 , C07H19/00 , C07H19/04 , C07H19/048
摘要： Compositions are provided including nicotinic acid riboside ("NAR"), and derivatives thereof including l -(2',3 ',5'-triacetyl-beta-D-ribofuranosyl)-nicotinic acid ("NAR triacetate" or "NARTA"); or derivatives of a reduced form of nicotinic acid riboside ("NARH"), including 1 - (2',3',5 '-triacetyl-beta-D-ribofuranosyl)-1,4-dihydronicotinic acid ("NARH triacetate" or "NARJT-TA"); or derivatives of nicotinamide riboside ("NR"), including 1 -(2',3',5'-triacetyl- beta-D-ribofuranosyl)-nicotinamide ("NR triacetate" or "NRTA"); derivatives of a reduced form of nicotinamide riboside ("NRH"), including 1-(2',3 ',5'-triacetyl-beta-D-ribofuranosyl)- 1,4- dihydronicotinamide ("NRH triacetate" or "NRH-TA"); or salts or prodrugs thereof, for use in food or beverage applications, pharmaceutical formulations, or as a dietary supplement. Methods of using the compounds above to promote the increase of intracellular levels of nicotinamide adenine dinuc!eotide ("NAD+") or NADH in cells and tissues for improving cell and tissue survival or overall cell and tissue health are provided.
摘要翻译：提供了包括烟酸核糖核苷（“NAR”）及其衍生物的组合物，包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基） - 烟酸（ “NAR三乙酸酯”或“NARTA”）; 或烟酸核苷（“NARH”）还原形式的衍生物，包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基）-1,4-二氢烟酸（“NARH triacetate” ;或“NARJT-TA”）; （“NR”）或包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基） - 烟酰胺（“NR三乙酸酯”或“NRTA”）的烟酰胺核糖核苷（“NR” 包括1-（2'，3'，5'-三乙酰基-β-D-呋喃核糖基）-1,4-二氢烟酰胺（“三乙酸NRH”或“NRH”）的还原形式的烟酰胺核糖核苷（“NRH” ; NRH-TA＆QUOT）; 或其盐或前药，用于食品或饮料应用，药物制剂或作为膳食补充剂。提供了使用上述化合物促进细胞和组织中细胞内烟酰胺腺嘌呤二核苷酸（“NAD +”）或NADH的增加以改善细胞和组织生存或整体细胞和组织健康的方法。 p>

9. 发明申请

WO2017163186A1 ALKYNYL NUCLEOSIDE ANALOGS AS INHIBITORS OF HUMAN RHINOVIRUS 审中-公开
标题翻译：炔诺酮核苷类似物作为人类鼻病毒的抑制剂
公开(公告)号：WO2017163186A1
公开(公告)日：2017-09-28
申请号：PCT/IB2017/051638
申请日：2017-03-21
申请人： NOVARTIS AG
发明人： FENAUX, Martijn , SAUNDERS, Oliver , YOKOKAWA, Fumiaki , ZHONG, Weidong
IPC分类号： C07D487/04 , C07H19/04 , A61K31/7064 , A61P31/16
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.
摘要翻译：本发明提供了式（I）的化合物或其盐; 和这些化合物的治疗用途。本发明进一步提供了包含这些化合物的药物组合物，以及包含这些化合物与治疗性辅助剂的组合物，以及使用所述化合物和组合物治疗病毒感染，特别是HRV的方法。

10. 发明申请

WO2017127357A1 DNA APTAMERS TARGETING THE CHOLECYSTOKININ B RECEPTOR AND METHODS OF USING SAME 审中-公开
标题翻译：靶向胆囊收缩素B受体的DNA APTAMERS及其使用方法
公开(公告)号：WO2017127357A1
公开(公告)日：2017-07-27
申请号：PCT/US2017/013769
申请日：2017-01-17
申请人： THE PENN STATE RESEARCH FOUNDATION
发明人： CLAWSON, Gary A. , MATTERS, Gail, L. , ADAIR, James H. , KESTER, Mark , MCGOVERN, Christopher , SMITH, Jill P. , TANG, Xiaomeng , LOC, Welley S. , LINTON, Samuel S.
IPC分类号： A61K51/00 , A61K49/00 , C12Q1/68 , G01N33/566 , C07H21/04 , C07H19/04
CPC分类号： G01N33/566 , A61K47/549 , A61K47/62 , A61K47/6923 , A61K47/6929 , A61K49/0034 , A61K49/0093 , C12N15/115 , C12N2310/16 , C12N2310/3517
摘要： A DNA aptamer is provided that binds to a cholecystokinin B receptor (CCBKR), allowing for delivery of therapeutic agents or imaging agents to cells having the CCBKR. Compositions and methods of use are provided where the aptamer binds to CCBKR and the agent is delivered such that it may be detected within the cytoplasm of the cell. Further provided are sequences of the nucleic acid molecules that bind to the amino acid residues 5-21 and/or 40-57 of the CCBKR polypeptide, and methods of delivery of a therapeutic agent to pancreatic adenocarcinoma cells.
摘要翻译：提供结合胆囊收缩素B受体（CCBKR）的DNA适体，允许将治疗剂或成像剂递送至具有CCBKR的细胞。提供使用的组合物和使用方法，其中适体与CCBKR结合并且递送药剂以使其可以在细胞的细胞质内被检测到。进一步提供了与CCBKR多肽的氨基酸残基5-21和/或40-57结合的核酸分子的序列，以及将治疗剂递送至胰腺癌细胞的方法。

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