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1. 发明申请

US20190216845A1 PATATIN-LIKE PHOSPHOLIPASE DOMAIN CONTAINING 3 (PNPLA3) iRNA COMPOSITIONS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：US20190216845A1
公开(公告)日：2019-07-18
申请号：US16267615
申请日：2019-02-05
申请人： Alnylam Pharmaceuticals, Inc.
发明人： Kevin Fitzgerald , Gregory Hinkle
IPC分类号： A61K31/7125 , C12N15/113 , C07H21/02 , C12P19/34
CPC分类号： A61K31/7125 , C07H19/067 , C07H19/167 , C07H21/02 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/321 , C12N2310/322 , C12N2310/3515 , C12P19/34 , C12N2310/3521 , C12N2310/3533
摘要： The present invention relates to RNAi agents, e.g., double stranded RNAi agents, targeting the Patatin-Like Phospholipase Domain Containing 3 (PNPLA3) gene, and methods of using such RNAi agents to inhibit expression of a PNPLA3 gene and methods of treating subjects having Nonalcoholic Fatty Liver Disease (NAFLD) and/or a PNPLA3-associated disorder.

2. 发明授权

US09920319B2 2′/3′/5′-(R/S)-serinyl functionalized oligonucleotides 有权
公开(公告)号：US09920319B2
公开(公告)日：2018-03-20
申请号：US14888794
申请日：2014-05-02
申请人： Council of Scientific & Industrial Research
发明人： Vaijayanti Anil Kumar , Venubabu Kotikam , Souvik Maiti , Smita Nahar
IPC分类号： C07H21/02 , C07H21/04 , C12N15/113 , C07H19/067 , C07H19/10 , C07H21/00
CPC分类号： C12N15/113 , C07H19/067 , C07H19/10 , C07H21/00 , C07H21/02 , C12N2310/113 , C12N2310/321
摘要： The present invention provides novel chiral serinyl functionalized tethered oligunucleotides i.e. R/S serinyl functionalized tethered oligonucleotides and the process of preparation thereof. Specifically, the present invention provides a modified nucleoside unit containing the R/S serinyl derivative at 2′ of the sugar unit which is introduced in a nucleotide sequence. Also, capping of the oligonucleotides with abasic serinyl derivative to render the nuclease stability to the oligonucleotiedds is also disclosed. The chiral serinyl functionalized tethered oligonucleotides, 2′-O-[R/S-(2-amino-3-methoxy)propyl] nucleic acids with both ′3- and 5′-ends capped with two units of abasic serine have antisense activity against the miRNA.

3. 发明授权

US09695210B2 C1-phostphonate analogue of UDP-GlcNAc for inhibition of O-GlcNAc transferase 有权
公开(公告)号：US09695210B2
公开(公告)日：2017-07-04
申请号：US14969136
申请日：2015-12-15
申请人： SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
发明人： Jungkyun Im
IPC分类号： C07H19/00 , C07H19/10 , C07H1/02 , C07H19/06 , C07H1/04 , C07H19/067
CPC分类号： C07H19/10 , C07H1/02 , C07H1/04 , C07H19/06 , C07H19/067
摘要： A novel C1-phosphate log of uridine-5′-diphosphate (UDP)-GlcNAc as an effective OGT (O-linked N-acetylglucosamine (O-GlcNAc) transferase) inhibitor, and a preparation method for the same provides a compound having an OGT inhibitory effect that can be used as a useful tool in the studies on various vital phenomena in association with the protein modification by O-GlcNAc within cells and furthermore as a candidate substance in the treatment or research of diseases related to the protein modification by O-GlcNAc, such as cancers, diabetes, or degenerative neurological diseases.

4. 发明申请

US20160289260A1 METHODS OF SYNTHESIZING SUBSTITUTED PURINE COMPOUNDS 有权
标题翻译：合成取代的嘌呤化合物的方法
公开(公告)号：US20160289260A1
公开(公告)日：2016-10-06
申请号：US14929736
申请日：2015-11-02
申请人： Epizyme, Inc.
发明人： Edward J. Olhava
IPC分类号： C07H19/16
CPC分类号： C07H19/16 , A61K31/4184 , A61K31/7076 , C07B2200/13 , C07D235/12 , C07H1/06 , C07H19/06 , C07H19/067 , C07H19/167 , Y02A50/401 , Y02A50/409 , Y02A50/411
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.
摘要翻译：本发明提供了合成（2R，3R，4S，5R）-2-（6-氨基-9H-嘌呤-9-基）-5 - （（（（1r，3S）-3- （2-（5-（叔丁基）-1H-苯并[d]咪唑-2-基）乙基）环丁基）（异丙基）氨基）甲基）四氢呋喃-3,4-二醇及其水合物和治疗疾病的方法通过将这些化合物和药物组合物施用于有需要的受试者，其中DOT1介导的蛋白质甲基化部分起作用，例如癌症和神经障碍。本发明还提供了（2R，3R，4S，5R）-2-（6-氨基-9H-嘌呤-9-基）-5 - （（（（1r，3S）-3- （5-（叔丁基）-1H-苯并[d]咪唑-2-基）乙基）环丁基）（异丙基）氨基）甲基）四氢呋喃-3,4-二醇及其水合物（A型，B型，和C型），其特征在于独特的X射线衍射图和差示扫描量热法，以及独特的晶体结构。

5. 发明申请

US20160264611A1 4'-VINYL SUBSTITUTED NUCLEOSIDE DERIVATIVES AS INHIBITORS OF RESPIRATORY SYNCYTIAL VIRUS RNA REPLICATION 审中-公开
标题翻译：作为呼吸道同源病毒RNA复制的抑制剂的4'-乙烯基取代的核苷衍生物
公开(公告)号：US20160264611A1
公开(公告)日：2016-09-15
申请号：US14865135
申请日：2015-09-25
申请人： Riboscience LLC
发明人： Mark Smith , Klaus G. Klumpp
IPC分类号： C07H19/10 , C07H19/20 , C07H19/207
CPC分类号： C07H19/10 , A61P31/14 , C07H19/067 , C07H19/11 , C07H19/167 , C07H19/20 , C07H19/207 , C07H19/213
摘要： The application discloses compounds of Formula I wherein the variable substituents are as defined herein. The compounds of Formula I and pharmaceutical compositions comprising compounds of Formula I are useful for the treatment of diseases mediated by RSV.
摘要翻译：其中可变取代基如本文所定义。式I化合物和包含式I化合物的药物组合物可用于治疗由RSV介导的疾病。

6. 发明申请

US20160228562A1 MUTUAL PRODRUG COMPRISING SHORT CHAIN FATTY ACIDS AND ZEBULARINE OR 1'-CYANO-CYTARABINE FOR CANCER TREATMENT 审中-公开
标题翻译：包含短链脂肪酸和锌或用于癌症治疗的1'-氰基 - 氰尿酸的相似产品
公开(公告)号：US20160228562A1
公开(公告)日：2016-08-11
申请号：US15029852
申请日：2014-11-14
申请人： KAINOS MEDICINE, INC.
发明人： Sunmi SHIN , Hyangmi KIM , Su-Sung OH
IPC分类号： A61K47/48 , A61K31/7068
CPC分类号： A61K31/7068 , A61K47/542 , C07H19/06 , C07H19/067
摘要： The present invention provides mutual prodrugs comprising anti-cancer nucleosides and short chain fatty acids; methods for production of the mutual prodrugs; methods of treatment comprising administration of the mutual prodrugs; and pharmaceutical compositions comprising the mutual prodrugs. Further, the mutual prodrugs of the present invention can be used as therapeutic agents for the treatment of cancer diseases and conditions.
摘要翻译：本发明提供了包含抗癌核苷和短链脂肪酸的共同前体药物; 共同前药的生产方法; 治疗方法，包括联合前药的施用; 和包含相互前体药物的药物组合物。此外，本发明的联合前药可以用作治疗癌症疾病和病症的治疗剂。

7. 发明授权

US09221865B2 Synthetic intermediate of 1-(2-deoxy-2-fluoro-4-thio-β-D-arabinofuranosyl)cytosine, synthetic intermediate of thionucleoside, and method for producing the same 有权
标题翻译： 1-（2-脱氧-2-氟-4-硫代 - 乙酰-D-阿拉伯呋喃糖基）胞嘧啶的合成中间体，硫代核苷的合成中间体及其制备方法
公开(公告)号：US09221865B2
公开(公告)日：2015-12-29
申请号：US14621119
申请日：2015-02-12
申请人： FUJIFILM Corporation
发明人： Kouki Nakamura , Satoshi Shimamura , Junichi Imoto , Motomasa Takahashi , Katsuyuki Watanabe , Kenji Wada , Yuuta Fujino , Takuya Matsumoto , Makoto Takahashi , Hideki Okada , Takehiro Yamane , Takayuki Ito
IPC分类号： C07D409/04 , C07H19/06 , A61K31/7068 , C07C303/28 , C07C45/00 , C07B53/00 , C07C309/73 , C07C249/04 , C07C251/38 , C07H13/04 , C07H13/08 , C07H15/04 , C07H15/18 , C07H15/203 , C07H17/02 , C07H19/067 , C07H19/073 , C07H23/00 , C07C69/78 , C07H1/00 , C07H7/04 , C07C67/29 , C07C68/06 , C07C69/28 , C07C69/618 , C07C69/76 , C07C69/92 , C07C69/96
CPC分类号： C07D333/32 , A61K31/7068 , C07B53/00 , C07C45/00 , C07C47/277 , C07C67/29 , C07C68/06 , C07C69/28 , C07C69/618 , C07C69/76 , C07C69/78 , C07C69/92 , C07C69/96 , C07C249/04 , C07C251/38 , C07C251/40 , C07C303/28 , C07C309/66 , C07C309/73 , C07F7/1804 , C07H1/00 , C07H7/04 , C07H13/04 , C07H13/08 , C07H15/04 , C07H15/18 , C07H15/203 , C07H17/02 , C07H19/06 , C07H19/067 , C07H19/073 , C07H23/00 , Y02P20/55
摘要： A compound represented by a formula [1D] as shown below (wherein R1A, R1B, R2A, R2B, R3A and R3B represent a hydrogen atom, an optionally substituted C1-6 alkyl group, and the like) is useful as an intermediate for producing a thionucleoside, and the production method of the present invention is useful as a method for producing a thionucleoside.
摘要翻译：由下式（其中R1A，R1B，R2A，R2B，R3A和R3B表示氢原子，任选取代的C 1-6烷基等）表示的由式[1D]表示的化合物可用作生产中间体硫代核苷，本发明的制造方法可用作硫代核苷的制造方法。

8. 发明申请

US20150337002A1 NUCLEOSIDE AND NUCLEOTIDE HAVING SULFONAMIDE STRUCTURE 审中-公开
标题翻译：具有磺酰胺结构的核苷和核苷酸
公开(公告)号：US20150337002A1
公开(公告)日：2015-11-26
申请号：US14759099
申请日：2014-01-14
申请人： OSAKA UNIVERSITY , SHIONOGI & CO., LTD.
发明人： Satoshi OBIKA , Yasunori MITSUOKA
IPC分类号： C07H19/10 , C07H19/20
CPC分类号： C07H19/067 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/167 , C07H19/20 , C07H21/04 , Y02P20/55
摘要： The present invention provides compounds shown by the formula: wherein Y1-Y2 is S(═O)2—NR6, NR6—S(═O)2 or the like, R6 is a hydrogen atom, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.
摘要翻译：本发明提供下式所示的化合物：其中Y1-Y2是S（= O）2-NR6，NR6-S（= O）2等，R6是氢原子，取代或未取代的烷基等， Bx是核酸碱基部分，Z1和Z2各自独立地为氢原子，羟基保护基或反应性磷基，R1至R5各自独立地为氢原子，卤素，氰基，取代或未取代的烷基或类似，n为0〜3的整数，或其盐，其可用作合成核酸药物的材料的新型核苷或核苷酸。

9. 发明申请

US20150315229A1 METHOD FOR LIQUID-PHASE SYNTHESIS OF NUCLEIC ACID 审中-公开
标题翻译：用于液相酸的合成方法
公开(公告)号：US20150315229A1
公开(公告)日：2015-11-05
申请号：US14442601
申请日：2013-11-13
申请人： Takeda Pharmaceutical Company Limited
发明人： Mitsuru NONOGAWA
IPC分类号： C07H19/207 , C07H19/16 , C07H19/06
CPC分类号： C07H19/207 , C07H1/00 , C07H19/06 , C07H19/067 , C07H19/073 , C07H19/16 , C07H19/167 , C07H21/00 , C07H21/04
摘要： In this method, an oligonucleotide is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R1, Y, Base, Z, Ar, R2, R3 and n are each as defined in Claim 1]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method cars dispense with columm-chromalographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
摘要翻译：在该方法中，通过使用由式（I）表示的新型核苷单体化合物作为合成单元制备寡核苷酸[其中X，R 1，Y，碱，Z，Ar，R 2，R 3和n各自如上所定义在权利要求1中]。该新型核苷单体化合物是一种核苷，其碱基部分被具有至少一个疏水基团的芳烃 - 羰基 - 羰基或硫代羰基取代。方法汽车在每次反应中均没有色谱 - 色谱纯化，不仅能在3'方向而且在5'方向上实现碱伸长，从而实现寡核苷酸的有效的液相质量合成。

10. 发明授权

US09102938B2 2′ and 5′ modified monomers and oligonucleotides 有权
标题翻译： 2'和5'修饰的单体和寡核苷酸
公开(公告)号：US09102938B2
公开(公告)日：2015-08-11
申请号：US13638891
申请日：2011-03-31
申请人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Eric E. Swayze , Thazha P. Prakash
发明人： Kallanthottathil G. Rajeev , Muthiah Manoharan , Eric E. Swayze , Thazha P. Prakash
IPC分类号： C07H21/02 , C12N15/113 , C07H19/067 , A61K48/00 , C07H19/06 , C07H19/16
CPC分类号： C12N15/113 , A61K48/00 , C07H19/06 , C07H19/067 , C07H19/16
摘要： The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.
摘要翻译：本发明提供式（1）的核苷和至少包含式（2）核苷的寡核苷酸：式（1）和式（2）。本发明的另一方面涉及一种抑制基因表达的方法，所述方法包括（a）使本发明的寡核苷酸与细胞接触; 和（b）将来自步骤（a）的细胞维持足以获得靶基因的mRNA降解的时间。

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