公开(公告)号：US08466255B2

公开(公告)日：2013-06-18

申请号：US12525570

申请日：2008-02-04

申请人： Satoru Sonoke ,  Toshihiro Ueda

发明人： Satoru Sonoke ,  Toshihiro Ueda

IPC分类号： C08G65/04

CPC分类号： A61K31/7088 ,  A61K31/7105 ,  A61K31/711 ,  A61K31/713 ,  C08G65/3322 ,  C08G65/33306 ,  C08G2650/50 ,  C08L2203/02

摘要： The present invention includes a novel polyethylene glycol derivative; a drug carrier comprising the derivative; and a pharmaceutical composition comprising the drug carrier having a pharmacologically active substance included therein. Specifically disclosed are: a polyethylene glycol derivative represented by the general formula (I); a drug carrier comprising the derivative and 2-O-(2-diethylaminoethyl)carbamoyl-1,3-O-dioleoyl-glycerol; and a pharmaceutical composition comprising the drug carrier and a pharmacologically active substance (preferably double-stranded RNA, double-stranded DNA or an oligonucleic acid), wherein R represents a saturated or unsaturated aliphatic hydrocarbon group having 10 to 30 carbon atoms or a saturated or unsaturated fatty acid residue having 10 to 30 carbon atoms; and n represents an integer of 30 to 150.

摘要翻译： 本发明包括新型聚乙二醇衍生物; 包含该衍生物的药物载体; 以及包含其中包含药理活性物质的药物载体的药物组合物。 具体公开的是：由通式（I）表示的聚乙二醇衍生物; 包含该衍生物和2-O-（2-二乙基氨基乙基）氨基甲酰基-1,3-O-二油酰甘油的药物载体; 以及包含药物载体和药理活性物质（优选双链RNA，双链DNA或低聚核酸）的药物组合物，其中R表示具有10至30个碳原子的饱和或不饱和脂族烃基或饱和或不饱和的 10-30个碳原子的不饱和脂肪酸残基; n表示30〜150的整数。

公开(公告)号：US08282956B2

公开(公告)日：2012-10-09

申请号：US12304015

申请日：2007-06-12

申请人： Hironobu Kato ,  Hirokazu Sakamoto

发明人： Hironobu Kato ,  Hirokazu Sakamoto

IPC分类号： A61K9/20 ,  A61K9/28 ,  A61K9/30 ,  A61K9/42

CPC分类号： A61K9/284 ,  A61K9/2846 ,  A61K31/155 ,  A61K31/164 ,  A61K31/24 ,  A61K31/245 ,  A61K31/4178 ,  A61K31/431 ,  A61K31/5383

摘要： A main object of the present invention is to provide a novel coated tablet which contains a drug having a guanidino group and does not suffer an obvious color change even when packed in a one-dose pack together with a drug having a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DMDO) group. The present invention provides a coated tablet characterized in that an uncoated tablet containing a drug having a guanidino group has been coated with a polyvinyl alcohol for film coating which comprises polyvinyl alcohol, acrylic acid, and methyl methacrylate.

摘要翻译： 本发明的主要目的是提供一种包含胍基的药物的新颖的包衣片剂，即使当与含有（5-甲基-2-吡咯烷酮）的药物一起包装在一次包装中时也不会发生明显的变色， 2-氧代-1,3-二氧杂环戊烯-4-基）甲基（DMDO）。 本发明提供了一种包衣片，其特征在于，包含含有胍基的药物的未包衣片剂已经用包含聚乙烯醇，丙烯酸和甲基丙烯酸甲酯的薄膜包衣用聚乙烯醇涂覆。

公开(公告)号：US08217031B2

公开(公告)日：2012-07-10

申请号：US12593566

申请日：2008-03-28

申请人： Masato Matsuoka ,  Tatsuya Oyama

发明人： Masato Matsuoka ,  Tatsuya Oyama

IPC分类号： A61K31/55 ,  C07D223/16

CPC分类号： C07D491/048 ,  C07D495/04

摘要： The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: In formula [1], one of X and Y is CH and the other is oxygen or sulfur; R is hydrogen, etc.; Z is hydrogen, etc.; Ar is phenyl, etc.; and n is 1 or 2 and or m is 1 or 2, excluding compounds where n is 2 and m is 2 simultaneously. Also provided is a pharmaceutical composition comprising a compound of formula [1] or a pharmaceutically acceptable salt thereof as an active ingredient. The composition is usable as an agent for the prevention or treatment of depression, panic disorder, anxiety, obsessive-compulsive disorder, chronic pain, fibromyalgia, obesity, stress urinary incontinence, and overactive bladder.

摘要翻译： 本发明涉及由式[1]表示的化合物或其药学上可接受的盐：在式[1]中，X和Y之一是CH，另一个是氧或硫; R是氢等; Z是氢等; Ar是苯基等; n为1或2，m为1或2，不包括n为2，m为2的化合物。 还提供了包含式[1]化合物或其药学上可接受的盐作为活性成分的药物组合物。 该组合物可用作预防或治疗抑郁症，恐慌症，焦虑症，强迫症，慢性疼痛，纤维肌痛，肥胖，压力性尿失禁和膀胱过动症的药剂。

公开(公告)号：US07884116B2

公开(公告)日：2011-02-08

申请号：US10596827

申请日：2004-12-24

申请人： Naoyoshi Yamada

发明人： Naoyoshi Yamada

IPC分类号： A61K31/4425 ,  C07D213/56

CPC分类号： C07D213/40 ,  A61K31/047 ,  A61K31/075 ,  A61K31/16 ,  A61K31/19 ,  A61K31/215 ,  A61K31/4406 ,  C07C35/36 ,  C07C69/732 ,  C07C235/30 ,  C07C2602/28

摘要： It is an object of the invention to provide a novel octahydronaphthalene derivative with an activity of inhibiting ICAM-4 expression and a pharmaceutically acceptable salt thereof. The invention encompasses, for example, agents for suppressing ICAM-1, therapeutic agents for inflammatory diseases, therapeutic agents for rheumatoid arthritis, immunosuppressive agents, and agents for suppressing cell growth, comprising N-(pyridin-3-ylmethyl)-(2E,4E)-5-[(1S,2S,4aR,6R,7S,8S,8aS)-7-hydroxy-2,6,8-trimethyl-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl]-2-methylpenta-2,4-dienamide as an active ingredient.

摘要翻译： 本发明的目的是提供具有抑制ICAM-4表达活性的新的八氢萘衍生物及其药学上可接受的盐。 本发明包括例如用于抑制ICAM-1的药物，炎性疾病的治疗剂，类风湿性关节炎的治疗剂，免疫抑制剂和抑制细胞生长的试剂，其包括N-（吡啶-3-基甲基） - （2E， 4E）-5 - [（1S，2S，4aR，6R，7S，8S，8aS）-7-羟基-2,6,8-三甲基-1,2,4a，5,6,7,8,8a- 八氢萘-1-基] -2-甲基戊-2,4-二烯酰胺作为活性成分。

公开(公告)号：US20110015211A1

公开(公告)日：2011-01-20

申请号：US12919885

申请日：2009-02-26

申请人： Koji Murakami ,  Takuya Toramoto

发明人： Koji Murakami ,  Takuya Toramoto

IPC分类号： A61K31/4965 ,  C07D241/20 ,  A61P35/00 ,  A61P17/02 ,  A61P25/28 ,  A61P13/12 ,  A61P1/18 ,  A61P19/00

CPC分类号： C07D241/20 ,  A61K31/4965

摘要： [Object] The main object of the present invention is to provide a fibrosis inhibitor.[Solving Means] The present invention relates to a fibrosis inhibitor containing the heterocyclic derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof as an active ingredient; In the formula (1), R1 and R2 are the same or different and each represents an optionally substituted aryl; R3 and R4 are the same or different and each represents hydrogen atom or alkyl; R5 represents hydrogen atom, alkyl or halogen atom; Y represents N or N→O; A represents NR6, and R6 represents hydrogen atom, alkyl, etc.; D represents alkylene or alkenylene which is optionally substituted with hydroxy; E represents phenylene or a single bond; G represents O, S, etc.; and Q represents carboxy, alkoxycarbonyl, etc.

摘要翻译： 本发明的主要目的在于提供纤维化抑制剂。 本发明涉及含有下述通式（1）表示的杂环衍生物或其药学上可接受的盐作为有效成分的纤维化抑制剂。 在式（1）中，R 1和R 2相同或不同，表示任选取代的芳基; R3和R4相同或不同，各自表示氢原子或烷基; R5代表氢原子，烷基或卤素原子; Y表示N或N→O; A表示NR6，R6表示氢原子，烷基等; D表示任选被羟基取代的亚烷基或亚烯基; E表示亚苯基或单键; G代表O，S等; Q表示羧基，烷氧基羰基等。

公开(公告)号：US07820629B2

公开(公告)日：2010-10-26

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： A01N43/04 ,  A61K31/70

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。

公开(公告)号：US20090149645A1

公开(公告)日：2009-06-11

申请号：US12280764

申请日：2007-02-26

申请人： Yoshinobu Shiba

发明人： Yoshinobu Shiba

IPC分类号： C07H1/00

CPC分类号： C07H21/04 ,  C07H21/02 ,  Y02P20/55

摘要： A method is provided for removing a 2-cyanoethoxymethyl (CEM) group and substituting the 2′-hydroxyl group of each ribose of an oligonucleic acid derivative with good reproducibility and high efficiency.

摘要翻译： 提供了以高重现性和高效率除去2-氰基乙氧基甲基（CEM）基团并且取代低聚核酸衍生物的每个核糖的2'-羟基的方法。

公开(公告)号：US07494997B2

公开(公告)日：2009-02-24

申请号：US10519722

申请日：2003-06-27

申请人： Tetsuo Asaki ,  Taisuke Hamamoto ,  Yukiteru Sugiyama

发明人： Tetsuo Asaki ,  Taisuke Hamamoto ,  Yukiteru Sugiyama

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  A61K31/506 ,  A61K31/53 ,  A61P35/00

CPC分类号： C07D239/42 ,  A61K31/505 ,  A61K31/506 ,  C07D401/04

摘要： The present invention provides an amide derivative represented by the following general formula (1): wherein R1 represents a saturated cyclic amino group, R2 represents alkyl, halogen or haloalkyl, R3 represents hydrogen or halogen, Het 2 represents pyridyl or pyrimidinyl, and Het 1 represents a group of the formula [6], or a salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.

摘要翻译： 本发明提供由以下通式（1）表示的酰胺衍生物：其中R1表示饱和环状氨基，R2表示烷基，卤素或卤代烷基，R3表示氢或卤素，Het2表示吡啶基或嘧啶基，Het1 表示式[6]的基团，或其盐，以及包含该基团的药物组合物作为活性成分。 本发明的化合物可用作BCR-ABL酪氨酸激酶抑制剂。

公开(公告)号：US20090042879A1

公开(公告)日：2009-02-12

申请号：US11912179

申请日：2006-04-21

申请人： Kohei Kagayama ,  Xin Zhang

发明人： Kohei Kagayama ,  Xin Zhang

IPC分类号： A61K31/5377 ,  C07D413/10 ,  A61K31/502 ,  A61P11/00 ,  A61P17/00 ,  C07D403/10

CPC分类号： C07D237/32 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10 ,  C07D491/113

摘要： The present invention provides a novel compound having an excellent PDE4 inhibitory activity and TNF-α production-suppressing activity, and also provides a preventive and therapeutic agent for atopic dermatitis or the like. The present invention includes a novel phthalazinone derivative of the following general structural formula [1] or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising it as an active ingredient. In the structural formula [1], the partial structure bridging the 6-position and the 7-position represents a single bond or a double bond; R1 and R2 are the same or different and each represents alkyl or the like; Y represents phenylene or the like; Z represents alkylene or the like; and R3 represents a mono- to tri-cyclic saturated or unsaturated cyclic amino group or the like optionally substituted with R31 and R32, wherein R31 and R32 represent alkyl or the like.

摘要翻译： 本发明提供了具有优异的PDE4抑制活性和TNF-α产生抑制活性的新化合物，并且还提供特应性皮炎等的预防和治疗剂。 本发明包括以下通式[1]的新颖的2,3-二氮杂萘酮衍生物或其药学上可接受的盐，以及包含其作为活性成分的药物组合物。 在结构式[1]中，桥接6-位和7-位的部分结构表示单键或双键; R1和R2相同或不同，各自表示烷基等; Y表示亚苯基等; Z表示亚烷基等; 并且R 3表示任选被R 31和R 32取代的单 - 三环饱和或不饱和环氨基等，其中R 31和R 32表示烷基等。

公开(公告)号：US20070172925A1

公开(公告)日：2007-07-26

申请号：US10597445

申请日：2005-01-26

申请人： Tadaaki Ohgi ,  Toshihiro Ueda ,  Yasufumi Maruyama ,  Hirofumi Masuda

发明人： Tadaaki Ohgi ,  Toshihiro Ueda ,  Yasufumi Maruyama ,  Hirofumi Masuda

IPC分类号： C12P19/28 ,  C07H21/04 ,  C07H19/04

CPC分类号： C07H19/167 ,  A61K31/7068 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/7088 ,  C07H19/067 ,  C07H19/10 ,  C07H19/20 ,  C07H21/02 ,  C07H21/04 ,  Y02P20/55

摘要： A novel phosphotriesterified ribonucleic acid compound which is important for liquid-phase synthesis of oligo-RNA is provided. Examples of the ribonucleic acid compound of the invention may include ribonucleic acid compounds represented by the following general formula: (wherein B represents adenine, guanine, cytosine or uracil or a modified form thereof; R21 represents aryl which may be substituted or a monocyclic or bicyclic heterocyclic group which may be substituted; R20 represents H or alkyl which may be substituted; and R1 represents a protecting group which can be removed at 90% or more at a temperature in the range from 0° C. to 60° C. under acidic conditions at a pH value from 2 to 4 within 24 hours).

摘要翻译： 提供了一种对寡核苷酸的液相合成非常重要的新型磷酸酯化核糖核酸化合物。 本发明的核糖核酸化合物的实例可以包括由以下通式表示的核糖核酸化合物：其中B表示腺嘌呤，鸟嘌呤，胞嘧啶或尿嘧啶或其修饰形式; R 21表示 可以被取代或可以被取代的单环或双环杂环基; R 20表示H或可被取代的烷基; R 1表示可以被取代的保护基 在酸性条件下，在24小时内pH为2〜4的温度下，在0℃〜60℃的温度下，90％以上除去）。