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1. 发明申请

US20190233367A1 HIGH PENETRATION PRODRUG COMPOSITIONS OF MUSTARDS AND MUSTARD-RELATED COMPOUNDS 审中-公开
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.

2. 发明申请

US20180222930A1 PRODRUGS OF GLUTAMINE ANALOGS 审中-公开
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.

3. 发明授权

US09896463B2 Preparation of purified phosphorodiamidite 有权
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.

4. 发明授权

US09879037B2 Fluorine-containing phosphate ester-amide, and flame retardant resin, flame retardant liquid and flame retardant solvent for organic synthesis containing same 有权
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.)

5. 发明申请

US20170275327A1 SUBSTITUTED PHOSPHORAMIDATE COMPOUNDS AND USES THEREOF 审中-公开
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.

6. 发明申请

US20170182181A1 PHOSPHATE BASED LINKERS FOR INTRACELLULAR DELIVERY OF DRUG CONJUGATES 审中-公开
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).

7. 发明授权

US09629862B2 Pantothenate derivatives for the treatment of neurologic disorders 有权
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.

8. 发明授权

US09447132B2 Highly active nucleoside derivative for the treatment of HCV 有权
标题翻译：用于治疗HCV的高活性核苷衍生物
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.

9. 发明申请

US20160215006A1 PEPTIDOMIMETIC INHIBITORS OF PSMA 审中-公开
标题翻译： PSMA的肽抑制剂
公开(公告)号：US20160215006A1
公开(公告)日：2016-07-28
申请号：US15088390
申请日：2016-04-01
申请人： Clifford E. BERKMAN , Henry F. VANBROCKLIN
发明人： Clifford E. BERKMAN , Henry F. VANBROCKLIN
IPC分类号： C07F9/24 , G01N33/574
CPC分类号： C07F9/2458 , A61K31/664 , A61K51/0489 , C07F9/24 , C07F9/2408 , C07F13/005 , G01N33/57434 , G01N33/57492 , G01N2333/705
摘要： Compounds of the formulae, (I), wherein each variable is as defined herein are provided which are useful in (i) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable carrier, excipient, and/or diluent; (3) methods for inhibiting or treating prostrate cancer; and (4) methods for blocking or destabilizing neovasculature of a tumor.
摘要翻译：提供式（I）化合物，其中每个变量如本文所定义，其可用于（i）用于检测和/或鉴定呈现PSMA的细胞的诊断方法; （2）包含本发明化合物与药学上可接受的载体，赋形剂和/或稀释剂的组合物; （3）抑制或治疗前列腺癌的方法; 和（4）阻断或破坏肿瘤新生血管的方法。

10. 发明申请

US20160207945A1 Novel chiral aryl or aryl-alkyl phosphoramidate dexamphetamine precursors having a regioisomeric purity >99% 有权
标题翻译：具有区域异质纯度> 99％的新型手性芳基或芳基 - 烷基氨基磷酸酯安非他明前体
公开(公告)号：US20160207945A1
公开(公告)日：2016-07-21
申请号：US15062872
申请日：2016-03-07
申请人： CHEMAPOTHECA, LLC
发明人： HAROLD MECKLER , BRIAN GREGG , JIE YANG
IPC分类号： C07F9/24
CPC分类号： C07F9/564 , C07B2200/07 , C07C209/62 , C07F9/2458 , C07F9/2475 , C07C211/27
摘要： The invention includes processes for the synthesis of amphetamine, dexamphetamine, methamphetamine, derivatives of these, including their salts, and novel precursors and intermediates obtained thereby, by synthesizing aziridine phosphoramidate compounds in specified solvents at specified temperatures, and then converting to a novel aryl or aryl-alkyl phosphoramidate precursors using an organometallic compound such as a copper salt, where the novel aryl or aryl-alkyl phosphoramidate precursor is then easily converted to the target compounds using known reactions,
摘要翻译：本发明包括合成苯丙胺，右旋苯丙胺，甲基苯丙胺，它们的衍生物，包括它们的盐的方法，以及由此获得的新型前体和中间体，通过在指定温度下合成特定溶剂中的氮丙啶氨基磷酸酯化合物，然后转化为新的芳基或使用有机金属化合物例如铜盐的芳基 - 烷基氨基磷酸酯前体，其中新的芳基或芳基 - 烷基氨基磷酸酯前体然后使用已知的反应容易地转化为目标化合物，

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