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1. 发明授权

US5559102A Adenosine and guanosine-3'-5'-cyclic methylphosphonate derivatives 失效
标题翻译：腺苷和鸟苷-3'5'-环甲基膦酸衍生物
公开(公告)号：US5559102A
公开(公告)日：1996-09-24
申请号：US181231
申请日：1994-01-13
申请人： Junichi Yano , Tadaaki Ohgi , Koichi Ishiyama , Kazuko Hirabayashi
发明人： Junichi Yano , Tadaaki Ohgi , Koichi Ishiyama , Kazuko Hirabayashi
IPC分类号： C07H19/20 , A61K31/70 , C07H19/167 , C07H19/173
CPC分类号： C07H19/20
摘要： Cyclic AMP and cyclic GMP derivatives, such as 8-bromoadenosine-3', 5'-cyclic methylphosphonate, are effective in inhibiting phosphodiesterases.
摘要翻译：环状AMP和环状GMP衍生物，如8-溴腺苷-3'，5'-环状甲基膦酸酯，对抑制磷酸二酯酶有效。

2. 发明授权

US5298614A Size limited double stranded poly I poly(cytidylate/4-thiouridylate) 失效
标题翻译：尺寸有限的双链poly I poly（胞苷酸/ 4-硫脲酸酯）
公开(公告)号：US5298614A
公开(公告)日：1994-03-29
申请号：US319062
申请日：1989-04-06
申请人： Junichi Yano , Tadaaki Ohgi
发明人： Junichi Yano , Tadaaki Ohgi
IPC分类号： C07H21/00 , C07H21/02
CPC分类号： C07H21/00 , C07H21/02
摘要： Nucleic acid derivatives and pharmaceutical compositions containing such derivatives are produced containing one 4-thiouridylic acid for every 6 to 39 cytidylic acids present, which has a length of from 50 to 10,000 base pairs. Methods of treatment using these nucleic acid derivatives to treat viral infections is also described.
摘要翻译：制备含有这样的衍生物的核酸衍生物和药物组合物，每六至三十九个胞苷酸含有一个4-硫尿酸，其具有50至10,000个碱基对的长度。还描述了使用这些核酸衍生物治疗病毒感染的方法。

3. 发明授权

US5703224A Antiviral c-nucleoside derivatives 失效
标题翻译：抗病毒c-核苷衍生物
公开(公告)号：US5703224A
公开(公告)日：1997-12-30
申请号：US652584
申请日：1996-08-26
申请人： Tadaaki Ohgi , Junichi Yano
发明人： Tadaaki Ohgi , Junichi Yano
IPC分类号： C07D405/06 , C07D473/00 , C07D473/18 , C07D473/30 , C07H19/04 , C07H19/00
CPC分类号： C07D473/00 , C07D405/06 , C07D473/18 , C07D473/30 , C07H19/04
摘要： The present invention is composed of a nucleoside derivative of the following general formula �I!: ##STR1## (wherein B represents adenin-9-ylmethyl, guanin-9-ylmethyl, hypoxanthin-9-ylmethyl, thymin-1-ylmethyl, uracil-1-ylmethyl, or cytosin-1-ylmethyl; X and Y may be the same or different and each represents hydrogen or hydroxy, exclusive of the case in which X is hydrogen and Y is hydroxy). The compound of the present invention is useful as an antiviral agent or an antimalignant-tumoral agent.
摘要翻译： PCT No.PCT / JP94 / 02059 Sec。 371日期：1996年8月26日 102（e）日期1996年8月26日PCT 1994年12月9日PCT公布。公开号WO95 / 15964 日期：1995年6月15日本发明由以下通式[I]的核苷衍生物组成：其中B表示腺嘌呤-9-基甲基，胍胍-9-基甲基，次黄嘌呤-9-基甲基，甲氨基-1-基甲基，尿嘧啶-1-基甲基或细胞蛋白-1-基甲基; X和Y可以相同或不同，各自表示氢或羟基，不包括X为氢且Y为羟基的情况）。本发明的化合物可用作抗病毒剂或抗恶性肿瘤剂。

4. 发明申请

US20090292005A1 GALACTOSE DERIVATIVE, DRUG CARRIER AND MEDICINAL COMPOSITION 有权
标题翻译：糖醇衍生物，药物载体和药物组合物
公开(公告)号：US20090292005A1
公开(公告)日：2009-11-26
申请号：US12280778
申请日：2007-02-28
申请人： Tadaaki Ohgi , Toshihiro Ueda , Satoru Sonoke
发明人： Tadaaki Ohgi , Toshihiro Ueda , Satoru Sonoke
IPC分类号： A61K31/7088 , C07H15/04 , A61K47/30 , A61P35/00 , A61P31/12 , A61P29/00 , A61P25/00 , A61P3/00
CPC分类号： A61K47/26 , A61K9/10 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K31/713 , C07H15/04
摘要： The object of the present invention is to provide a novel and useful galactose derivative, which is a component of a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the drug carrier and a medicine.The present invention relates to a galactose derivative represented by the following general formula (I) a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, an oligo nucleic acid). wherein, R1 represents hydrogen, an alkyl having 1 to 10 carbons which may be substituted or 1-(D)-deoxylactito-1-yl; R2 represents a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms.
摘要翻译：本发明的目的是提供一种新颖有用的半乳糖衍生物，其是药物载体的组分，药物可以通过其有效转移到肝脏中，药物载体包含该衍生物，以及包含该药物的药物组合物载体和药物。本发明涉及由以下通式（I）表示的包含该衍生物和阳离子脂质的药物载体的半乳糖衍生物，以及包含该载体和药物（优选双链RNA，双链 DNA，寡核酸）。其中，R 1表示氢，可以被取代的具有1至10个碳的烷基或1-（D） - 脱氧葡糖基-1-基; R2表示具有10至30个碳原子的饱和或不饱和脂肪酸残基。

5. 发明授权

US07655768B2 Galactose derivative, drug carrier and medicinal composition 有权
标题翻译：半乳糖衍生物，药物载体和药用组合物
公开(公告)号：US07655768B2
公开(公告)日：2010-02-02
申请号：US11574302
申请日：2005-08-25
申请人： Tadaaki Ohgi , Toshihiro Ueda
发明人： Tadaaki Ohgi , Toshihiro Ueda
IPC分类号： C07G3/00 , C07G11/00 , C07H15/00 , C07H17/00 , A61K31/70 , A61K9/127 , A01N43/04
CPC分类号： C07H3/04 , A61K48/0025 , C07H15/04 , C07H15/08
摘要： The present invention relates to a novel and useful galactose derivative constituting a drug carrier by which a medicine can be efficiently transferred into the liver, a drug carrier comprising the derivative, and a pharmaceutical composition comprising the carrier and a medicine. The present invention also relates to a galactose derivative made up of galactose, a suitable spacer and a certain lipid, a drug carrier comprising the derivative and a cationic lipid, and a pharmaceutical composition comprising the carrier and a medicine (preferably a double-stranded RNA, a double-stranded DNA, or an oligo nucleic acid).
摘要翻译：本发明涉及一种构成药物载体的新型有用的半乳糖衍生物，通过该药物可将药物有效转移到肝脏中，包含该衍生物的药物载体和包含该载体和药物的药物组合物。本发明还涉及由半乳糖，合适的间隔基和某些脂质组成的半乳糖衍生物，包含该衍生物和阳离子脂质的药物载体，以及包含载体和药物（优选双链RNA ，双链DNA或寡核酸）。

6. 发明授权

US07163921B1 Peptide derivatives and medicinal compositions 有权
标题翻译：肽衍生物和药物组合物
公开(公告)号：US07163921B1
公开(公告)日：2007-01-16
申请号：US10257238
申请日：2001-04-16
申请人： Kouichi Ishiyama , Tomohiro Terada , Tatsuya Oyama , Tadaaki Ohgi
发明人： Kouichi Ishiyama , Tomohiro Terada , Tatsuya Oyama , Tadaaki Ohgi
IPC分类号： A61K38/07 , A61K38/05 , A61K38/06 , C07K5/08 , C07K7/04
CPC分类号： C07K5/1016 , A61K38/00 , C07K5/0812 , C07K5/1027 , C07K7/56
摘要： The present invention to novel nociceptin receptor agonists which are peptide derivatives represented by the following general formula (1): (in which A is alkylene, —CH2)nCO— or a group expressed by the following formula (2) or (3): wherein n represents an integer of 1 to 8; X and Y are same or different and each represents —CONH— or —CH2NH—; R1, R2 and R3 are same or different and each represents alkyl, aryl or heteroaryl; Z represents —CON(R4)R5 or —CH2N(R4)R5; R4 and R5 are same or different and each represents hydrogen, alkyl, aryl or heteroaryl) or a pharmaceutically acceptable salt thereof. A pharmaceutical composition according to the present invention is useful as a nociceptin receptor agonist.
摘要翻译：本发明涉及由以下通式（1）表示的肽衍生物的新的伤害感受激素受体激动剂：（其中A为亚烷基，-CH 2 O 2）n CO- 或由下式（2）或（3）表示的基团：其中n表示1至8的整数; X和Y相同或不同，各自表示-CONH-或-CH 2 NH-; R 1，R 2和R 3相同或不同，各自表示烷基，芳基或杂芳基; Z表示-CON（R 4）R 5或-CH 2 N（R 4）R SUP > 5 ; R 4和R 5相同或不同，各自表示氢，烷基，芳基或杂芳基）或其药学上可接受的盐。根据本发明的药物组合物可用作伤害感受肽受体激动剂。

7. 发明授权

US4593025A Triazine derivatives to treat pain, fever, inflammation, allergies and thrombosis 失效
标题翻译：三嗪衍生物治疗疼痛，发热，炎症，过敏和血栓形成
公开(公告)号：US4593025A
公开(公告)日：1986-06-03
申请号：US744047
申请日：1985-06-12
申请人： Kenji Sempuku , Yoshihisa Shibata , Tadaaki Ohgi
发明人： Kenji Sempuku , Yoshihisa Shibata , Tadaaki Ohgi
IPC分类号： A61K31/53 , A61P3/00 , A61P7/02 , A61P29/00 , A61P37/08 , C07D251/18 , C07D401/12
CPC分类号： C07D401/12 , C07C255/00 , C07D251/18
摘要： Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 and R.sup.2 are the same or different and each is hydrogen, hydroxy, halo, alkoxy of 1 to 4 carbon atoms or aralkyloxy of 1 to 4 carbon atoms and X and Y are each hydrogen or nicotinoyl are useful as anti-edema agents, anti-inflammatories, analgesics, anti-pyretics, anti-allergenics and anti-thrombosis agents.
摘要翻译：式（I）化合物：其中R 1和R 2相同或不同，各自为氢，羟基，卤素，1至4个碳原子的烷氧基或1至4个芳烷氧基碳原子和X和Y各自为氢或烟酰基，可用作抗浮肿剂，抗炎剂，止痛剂，抗热解剂，抗过敏原和抗血栓形成剂。

8. 发明申请

US20140100362A1 Process for Preparing Phosphate Compound Bearing Isotope 有权
标题翻译：制备磷酸盐化合物轴承同位素的方法
公开(公告)号：US20140100362A1
公开(公告)日：2014-04-10
申请号：US14116763
申请日：2012-05-07
申请人： Tomohiro Hamasaki , Tadaaki Ohgi
发明人： Tomohiro Hamasaki , Tadaaki Ohgi
IPC分类号： C12N15/10
CPC分类号： C12N15/10 , C07B59/00 , C07B59/005 , C07F9/06 , C07F9/08 , C07F9/09 , C07H21/00
摘要： The present invention provides a process for preparing an isotope-containing phosphate compound easily. The process for preparing an isotope-containing phosphate compound according to the present invention includes the step of oxidizing a trivalent phosphorus compound with an oxidizing agent containing an isotope to synthesize a pentavalent phosphate compound to which the isotope has been introduced. The present invention preferably is applied to the synthesis of nucleic acids such as DNA and RNA, for example. The isotope preferably is a stable isotope. The oxidizing agent preferably is H218O, 3H-1,2-benzodithiol 3-one 1,1-dioxide having 34S, or a diisopropylethylamine-borane complex having 10B, for example.
摘要翻译：本发明提供了容易地制备含同位素的磷酸盐化合物的方法。根据本发明的制备含同位素磷酸盐化合物的方法包括用含有同位素的氧化剂氧化三价磷化合物以合成已经引入同位素的五价磷酸盐化合物的步骤。本发明优选用于例如DNA和RNA等核酸的合成。同位素优选是稳定的同位素。氧化剂优选为具有34S的H 2 18 O，3H-1,2-苯并二硫酚3-酮1,1-二氧化物，或具有10B的二异丙基乙胺 - 硼烷络合物。

9. 发明授权

US08691782B2 Single-stranded nucleic acid molecule having nitrogen-containing alicyclic skeleton 有权
标题翻译：具有含氮脂环骨架的单链核酸分子
公开(公告)号：US08691782B2
公开(公告)日：2014-04-08
申请号：US13254159
申请日：2011-07-28
申请人： Tadaaki Ohgi , Hirotake Hayashi , Hisao Shirohzu , Tomohiro Hamasaki , Akihiro Itoh , Hiroshi Suzuki
发明人： Tadaaki Ohgi , Hirotake Hayashi , Hisao Shirohzu , Tomohiro Hamasaki , Akihiro Itoh , Hiroshi Suzuki
IPC分类号： A01N43/04 , C07H19/044 , C12Q1/68 , C12N15/63 , C07H21/04
CPC分类号： C12N15/113 , A61K31/7105 , A61K31/7125 , C07F9/22 , C12N15/111 , C12N15/1136 , C12N2310/14 , C12N2310/318 , C12N2330/30 , C12N2310/531
摘要： Provided is a novel nucleic acid molecule that can be produced easily and efficiently and can inhibit the expression of a gene. The nucleic acid molecule is a single-stranded nucleic acid molecule including an expression inhibitory sequence that inhibits expression of a target gene. The single-stranded nucleic acid molecule includes: a region (X); a linker region (Lx); and a region (Xc). The linker region (Lx) is linked between the regions (Xc) and (Xc). The region (Xc) is complementary to the region (X). At least one of the regions (X) and (Xc) includes the expression inhibitory sequence. The linker region (Lx) has a non-nucleotide structure including at least one of a pyrrolidine skeleton and a piperidine skeleton. According to this single-stranded nucleic acid molecule, it is possible to inhibit the expression of the target gene.
摘要翻译：提供了可以容易且有效地产生并可以抑制基因表达的新型核酸分子。核酸分子是包含抑制靶基因表达的表达抑制性序列的单链核酸分子。单链核酸分子包括：区域（X）; 连接区（Lx）; 和区域（Xc）。连接区域（Lx）连接在区域（X）和（Xc）之间。区域（Xc）与区域（X）互补。区域（X）和（Xc）中的至少一个包括表达抑制序列。接头区（Lx）具有包含吡咯烷骨架和哌啶骨架中的至少一种的非核苷酸结构。根据该单链核酸分子，可以抑制靶基因的表达。

10. 发明申请

US20070282097A1 Phosphoramidite Compound And Method For Producing Oligo-Rna 有权
标题翻译：亚磷酰胺化合物及其制备方法
公开(公告)号：US20070282097A1
公开(公告)日：2007-12-06
申请号：US11574308
申请日：2005-08-25
申请人： Tadaaki Ohgi , Kouichi Ishiyama , Yutaka Masutomi
发明人： Tadaaki Ohgi , Kouichi Ishiyama , Yutaka Masutomi
IPC分类号： C07H21/02 , C07C43/12
CPC分类号： C07C255/13 , C07H19/067 , C07H19/167 , C07H21/02 , Y02P20/55 , Y02P20/582
摘要： An object of the present invention is to provide a useful and novel phosphoramidite compound for the synthesis of oligo-RNA. A phosphoramidite compound represented by general formula (1), wherein: BX represents a nucleobase optionally having a protecting group; and R1 is a substituent represented by general formula (2), wherein: R11, R12 and R13 are the same or different and each represents hydrogen or alkoxy; R2a and R2b are the same or different and each represents alkyl, or R2a and R2b taken together with the adjacent nitrogen atom may form a 5- to 6-membered saturated amino cyclic group, the amino cyclic group optionally having an oxygen or sulfur atom as a ring-composing member in addition to the adjacent nitrogen atom; and WG1 and WG2 are the same or different and each represents an electron-withdrawing group.
摘要翻译：本发明的目的是提供一种用于合成寡聚RNA的有用和新型的亚磷酰胺化合物。一种由通式（1）表示的亚磷酰胺化合物，其中：B X表示任选具有保护基团的核碱基; 和R 1是由通式（2）表示的取代基，其中：R 11，R 12和R 13， SUP>相同或不同，各自表示氢或烷氧基; R 2a和R 2b相同或不同，各自代表烷基，或R 2a取代R 2b和R 2b 与相邻的氮原子一起可以形成5至6元饱和的氨基环状基团，除了相邻的氮原子之外，氨基环状基团任选地具有作为环组成成分的氧或硫原子; 和WG ^{1和WG 2相同或不同，并且各自表示吸电子基团。}

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