公开(公告)号：US20240327444A1

公开(公告)日：2024-10-03

申请号：US18576587

申请日：2022-07-05

申请人： Japan Science and Technology Agency ,  National University Corporatjion Tokai National Higher Education and Research System

发明人： Hiroshi Abe ,  Naoko Abe ,  Masahito Inagaki ,  Yasuaki Kimura ,  Fumitaka Hashiya ,  Zhenmin Li ,  Yuko Nakashima

IPC分类号： C07H1/06 ,  A61K31/7105 ,  C07F9/24 ,  C07H17/02 ,  C07H21/00

CPC分类号： C07H1/06 ,  A61K31/7105 ,  C07F9/2458 ,  C07H17/02 ,  C07H21/00

摘要： A method for purifying a nucleotide-based substance; including a protecting group introduction step of introducing a hydrophobic protecting group represented by the following formula (P1) or (P2) into a nucleotide-based substance to produce a hydrophobic nucleotide-based substance; an isolation and purification step of isolating and purifying the hydrophobic nucleotide-based substance under a hydrophobic environment; and a deprotection step of deprotecting the hydrophobic protecting group from the hydrophobic nucleotide-based substance to produce the nucleotide-based substance,






wherein R1 represents a linear or branched alkyl group having 1 to 30 carbon atoms, R4 represents hydrogen or a linear or branched alkyl group having 1 to 10 carbon atoms, R2, R3, R5 and R6 represent hydrogen, a linear or branched alkyl group having 1 to 10 carbon atoms, or the like, and may be the same or different; and * means a bond with a nucleotide-based substance.

公开(公告)号：US20230144322A1

公开(公告)日：2023-05-11

申请号：US18149981

申请日：2023-01-04

申请人： Cancer Targeted Technology LLC ,  WASHINGTON STATE UNIVERSITY

发明人： Clifford Berkman ,  Svetlana A. Stekhova

IPC分类号： A61K51/04 ,  C07F9/24 ,  C07F9/58

CPC分类号： A61K51/0489 ,  C07F9/2458 ,  C07F9/58 ,  A61K51/0402 ,  C07F9/2404 ,  C07F9/2416

摘要： Compounds of Marlush formula (I) described in the claims are useful in diagnostic methods for detecting and/or identifying cells presenting PSMA. Disclosed are also methods for preparing the compounds. Representative compounds according to the application are:

公开(公告)号：US20190233367A1

公开(公告)日：2019-08-01

申请号：US16209744

申请日：2018-12-04

申请人： Techfields Pharma Co., Ltd.

发明人： Chongxi YU ,  Lina XU

IPC分类号： C07C233/47 ,  C07F9/24 ,  C07C229/42

CPC分类号： C07C233/47 ,  C07C229/42 ,  C07F9/242 ,  C07F9/2429 ,  C07F9/2458

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of mustards and mustard-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

公开(公告)号：US20180222930A1

公开(公告)日：2018-08-09

申请号：US15885258

申请日：2018-01-31

申请人： The Johns Hopkins University ,  Institute of Organic Chemistry and Biochemistry as CR V.V.I,

发明人： Barbara Slusher ,  Rana Rais ,  Lukas Tenora ,  Pavel Majer ,  Andrej Jancarik

IPC分类号： C07F9/24 ,  C07C245/18 ,  C07K5/083 ,  C07D317/38 ,  C07D263/04 ,  C07K5/062 ,  C07K5/078 ,  C07D309/10 ,  A61P35/00

CPC分类号： C07F9/2458 ,  A61K31/404 ,  A61K38/00 ,  A61P35/00 ,  C07C227/14 ,  C07C245/18 ,  C07C271/22 ,  C07D209/18 ,  C07D209/20 ,  C07D211/90 ,  C07D263/04 ,  C07D263/18 ,  C07D309/10 ,  C07D317/38 ,  C07D317/40 ,  C07D473/34 ,  C07F9/65616 ,  C07H15/203 ,  C07H19/207 ,  C07K5/06026 ,  C07K5/06156 ,  C07K5/0808

摘要： The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2′, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.

公开(公告)号：US09896463B2

公开(公告)日：2018-02-20

申请号：US15110971

申请日：2015-01-15

申请人： RHODIA OPERATIONS

发明人： Gary Woodward

IPC分类号： C07F9/02 ,  C07F9/24

CPC分类号： C07F9/2412 ,  C07F9/2408 ,  C07F9/2458

摘要： The instant invention relates to a method of phosphorodiamidite production that comprises: (E1) preparing a purified solution of a dialkylamine in a polar solvent as follows: —the dialkylamine dissolved in a polar solvent is contacted with a quantity of phosphorus trihalide that is sufficient to react with the alcohol impurities contained in the dialkylamine but sufficiently low to leave a major part of the dialkylamine unreacted, whereby a mixture is obtained that contains the dialkylamine in the polar solvent and reaction products of the impurities with the phosphorous trihalide; —the unreacted dialkylamine and polar solvent present in the mixture obtained in step (E1.1.) are extracted from the solution S by their difference of volatility, typically by distillation, whereby the purified solution of the dialkylamine in the polar solvent is obtained; (E2) the purified solution of dialkylamine in a polar solvent as obtained in step (E1) is reacted with a phosphorus trihalide, whereby an intermediate compound is formed; (E3) the intermediate compound obtained in step (E2) is reacted with a hydroxyalkyl compound in the presence of a non-polar co-solvent.

公开(公告)号：US09879037B2

公开(公告)日：2018-01-30

申请号：US14385862

申请日：2013-03-22

申请人： TOSOH F-TECH, INC.

发明人： Hideyuki Mimura ,  Hiroaki Fujita ,  Hisao Eguchi

IPC分类号： C07F9/59 ,  H01M10/42 ,  H01M10/0567 ,  C08J9/00 ,  C09K21/12 ,  C07F9/24 ,  H01M10/0525 ,  C08G18/24 ,  C08G18/32 ,  C08G18/72

CPC分类号： C07F9/59 ,  C07F9/2408 ,  C07F9/2454 ,  C07F9/2458 ,  C08G18/24 ,  C08G18/32 ,  C08G18/72 ,  C08J9/0038 ,  C08J2375/04 ,  C09K21/12 ,  H01M10/0525 ,  H01M10/0567 ,  H01M10/4235

摘要： [Problem] To provide a fluorine-containing phosphate ester-amide which has high flame retardancy such as exhibiting flame retardant effects at a small quantity of addition, and sufficient hydrolysis resistance.[Solution] A fluorine-containing phosphate ester-amide represented by general formula (1). (In the formula, R1 and R2 are the same or different and represent a branched or linear alkyl group having 1 to 20 carbon atoms in which at least one carbon bonded to a nitrogen atom is a secondary or tertiary carbon, wherein R1 and R2 may have a substituent group selected from the group consisting of an alkoxy group, a hydroxy group, an amino group, a methyl amino group, an ethyl amino group, a dimethyl amino group, diethyl amino group and a fluorine atom. In addition, R1 and R2 may be bonded together to form a five- to eight-membered cyclic structure. X and Y are the same or different and represent a hydrogen atom or a fluorine atom, and n and m represent an integer of 1 to 6.)

公开(公告)号：US20170275327A1

公开(公告)日：2017-09-28

申请号：US15503776

申请日：2015-08-14

申请人： John Simon EDWARDS ,  Peter Richard MULLENS ,  Edward CLEATOR ,  Bryon L. SIMMONS ,  Courtney K. MAGUIRE ,  Jeremy Peter SCOTT ,  Nobuyoshi YASUDA ,  Yong ZHONG ,  Lisa F. FREY ,  Peter G. DORMER ,  Andrew BRUNSKILL ,  Artis KLAPARS ,  Eric ASHLEY ,  Pu QIAN ,  Yi ZHANG ,  Baoqiang WAN ,  MERCK SHARP & DOHME CORP. ,  MERCK SHARP & DOHME LIMITED

发明人： John Edwards ,  Peter Richard Mullens ,  Ed 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 ,  Puneet Qian ,  Yi Zhang ,  Baoqiang Wan

IPC分类号： C07H19/10 ,  C07F9/24 ,  C07F9/58

CPC分类号： C07H19/10 ,  C07F9/242 ,  C07F9/2458 ,  C07F9/2487 ,  C07F9/58 ,  C07F9/65586 ,  C07H19/06

摘要： 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：US20170182181A1

公开(公告)日：2017-06-29

申请号：US15301564

申请日：2015-03-30

申请人： MERCK SHARP & DOHME CORP. ,  AMBRX, INC.

发明人： Robert M. Garbaccio ,  Jeffrey Kern ,  Philip E. Brandish ,  Sanjiv Shah ,  Linda Liang ,  Ying Sun ,  Jianing Wang ,  Nick Knudsen ,  Andrew Beck ,  Anthony Manibusan ,  Dennis Gately

IPC分类号： A61K47/48 ,  C07K16/28 ,  C07J41/00 ,  C07J43/00

CPC分类号： C07K16/2866 ,  A61K47/6803 ,  A61K47/6817 ,  A61K47/6849 ,  A61K47/6889 ,  A61K51/1045 ,  C07F9/091 ,  C07F9/098 ,  C07F9/12 ,  C07F9/2458 ,  C07F9/572 ,  C07F9/65517 ,  C07F9/65583 ,  C07F9/65586 ,  C07F9/6561 ,  C07H19/10

摘要： Phosphate-based linkers with tunable stability for intracellular delivery of drug conjugates are described. The phosphate-based linkers comprise a monophosphate, diphosphate, triphosphate, or tetraphosphate group (phosphate group) and a linker arm comprising a tuning element and optionally a spacer. A payload is covalently linked to the phosphate group at the distal end of the linker arm and the functional group at the proximal end of the linker arm is covalently linked to a cell-specific targeting ligand such as an antibody. These phosphate-based linkers have a differentiated and tunable stability in blood vs. an intracellular environment (e.g. lysosomal compartment).

公开(公告)号：US09629862B2

公开(公告)日：2017-04-25

申请号：US14871450

申请日：2015-09-30

申请人： Retrophin, Inc.

发明人： Andrew Vaino ,  Marek Biestek ,  Martin Shkreli

IPC分类号： A61K31/685 ,  C07F9/24 ,  C07F9/572 ,  C07F9/22 ,  C07F9/09 ,  C07F9/6561

CPC分类号： A61K31/685 ,  C07F9/09 ,  C07F9/222 ,  C07F9/2458 ,  C07F9/5728 ,  C07F9/65616

摘要： The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.

公开(公告)号：US09447132B2

公开(公告)日：2016-09-20

申请号：US14252290

申请日：2014-04-14

申请人： Achillion Pharmaceuticals, Inc.

发明人： Milind Deshpande ,  Jason Allan Wiles ,  Akihiro Hashimoto ,  Avinash Phadke

IPC分类号： A61K31/70 ,  C07H19/10 ,  C07H19/048 ,  A01N43/04 ,  C07H1/00 ,  A61K31/7072 ,  A61K45/06 ,  C07F9/24 ,  C07H19/067 ,  C07F9/58 ,  C07B59/00 ,  A61K31/4709

CPC分类号： C07H1/00 ,  A61K31/4709 ,  A61K31/7072 ,  A61K45/06 ,  C07B59/005 ,  C07F9/2429 ,  C07F9/2458 ,  C07F9/58 ,  C07H19/067 ,  Y02A50/385 ,  Y02A50/387 ,  Y02A50/393 ,  Y02A50/463 ,  A61K2300/00

摘要： A deuterated nucleoside analog of the formula and the pharmaceutically acceptable salts thereof are provided by this disclosure. The disclosure also includes pharmaceutical compositions comprising a compound or salt of the formula and a carrier. Compounds and salts of this formula are useful for treating viral infections, including HCV infections. A method for treating a host afflicted with hepatitis C or other disorders is also presented that includes administering an effective treatment amount of a nucleoside or nucleotide that has deuterium with at least 50% enrichment at the 5′-position of the nucleoside or nucleotide.