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21. 发明申请

US20100130454A1 9,10-SECOPREGNANE DERIVATIVES AND MEDICINE 审中-公开
标题翻译： 9,10-SECOPREGNANE衍生物和药物
公开(公告)号：US20100130454A1
公开(公告)日：2010-05-27
申请号：US11720789
申请日：2005-12-05
申请人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku
发明人： Hiroki Fujieda , Hironori Otsu , Shoji Yasufuku
IPC分类号： A61K31/59 , C07C401/00 , A61P17/12 , A61P17/06
CPC分类号： C07C401/00
摘要： A novel useful vitamin D3 derivative which is reduced in influence on systemic calcium metabolism while retaining excellent vitamin D3 activity. The derivative is a 9,10-secopregnane derivative represented by the following general formula [1]. Also provided is a medicinal composition containing the derivative as an active ingredient. In the general formula [1], Y represents (1) a single bond, (2) alkylene (3) alkenylene, or (4) phenylene; R1 and R2 are the same or different and each represents (1) hydrogen, (2) alkyl, or (3) cycloalkyl, or R1 and R2 in combination represent cycloalkyl in cooperation with the adjacent carbon atom; R3 represents hydrogen or methyl; and Z represents (1) hydrogen, (2) hydroxy, or (3) —NR11R12.
摘要翻译：一种新颖有用的维生素D3衍生物，其对全身钙代谢的影响减小，同时保持优异的维生素D3活性。该衍生物是由以下通式[1]表示的9,10-仲孕烷衍生物。还提供含有该衍生物作为活性成分的药物组合物。在通式[1]中，Y表示（1）单键，（2）亚烷基（3）亚烯基或（4）亚苯基; R1和R2相同或不同，各自表示（1）氢，（2）烷基或（3）环烷基，或者R1和R2组合表示与相邻碳原子配合的环烷基; R3表示氢或甲基; Z表示（1）氢，（2）羟基或（3）-NR11R12。

22. 发明申请

US20100074880A1 POLYETHYLENE GLYCOL DERIVATIVE 有权
标题翻译：聚乙二醇衍生物
公开(公告)号：US20100074880A1
公开(公告)日：2010-03-25
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： A61K38/43 , C07C271/06 , C07F9/02 , C07J9/00 , A61K31/7088 , A61K31/7105 , A61P17/02
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。

23. 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）。

24. 发明申请

US20100022566A1 QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权
标题翻译：喹诺酮衍生物及其药物组合物
公开(公告)号：US20100022566A1
公开(公告)日：2010-01-28
申请号：US12089087
申请日：2006-10-03
申请人： Masahiko Okano , Tatsuya Oyama
发明人： Masahiko Okano , Tatsuya Oyama
IPC分类号： A61K31/517 , C07D239/72 , A61P17/02 , A61P17/06
CPC分类号： C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14
摘要： The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 and R4 are the same or different and represent hydrogen, alkyl, alkoxy or halogen; R5 is combined with R6 to represent alkylene or represents hydrogen, hydroxy, alkyl, phenyl or alkoxy; R6 represents alkyl, cycloalkyl, phenyl, a 5- to 10-membered aromatic heterocyclic group containing one to three heteroatoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, or —N(R6-1)(R6-2).
摘要翻译：本发明涉及具有较少皮肤刺激性和强烈抑制划伤行为的优异作用的新型喹唑啉衍生物以及含有喹唑啉衍生物作为活性成分的药物组合物。本发明涉及由通式[1]表示的喹唑啉衍生物或其药学上可接受的盐。在通式[1]中，R 1表示氢等; R2表示氢等; R3和R4相同或不同，代表氢，烷基，烷氧基或卤素; R5与R6结合表示亚烷基或代表氢，羟基，烷基，苯基或烷氧基; R6表示烷基，环烷基，苯基，含有1至3个选自氮原子，氧原子和硫原子的杂原子的5至10元芳族杂环基或-N（R 6-1）（ R6-2）。

25. 发明申请

US20080299192A1 Intraorally Rapidly Disintergrating Tablets and Their Production 审中-公开
标题翻译：内部快速解淀粉片及其生产
公开(公告)号：US20080299192A1
公开(公告)日：2008-12-04
申请号：US12170859
申请日：2008-07-10
申请人： Tomoharu SUGA , Tomio NAKANO
发明人： Tomoharu SUGA , Tomio NAKANO
IPC分类号： A61K9/20
CPC分类号： A61K9/0056
摘要： The object of the present invention is to provide, as a solid preparation for making it easy to take, thus improving patient's compliance etc., an intraorally rapidly disintegrating tablet which can be produced easily without any particular problem by a usual method of producing tablets with a usual tabletting machine, has practically unproblematic hardness, and disintegrate rapidly in the oral cavity. This tablet is produced by tabletting cores coated with a pharmaceutical disintegrating agent, wherein the core is a granule containing a water-soluble medicament or containing a medicament and a sugar.
摘要翻译：本发明的目的是提供一种易于使用的固体制剂，从而提高患者的依从性等，可以容易地制造出口服快速崩解片剂，而不会产生任何特别的问题通常的压片机具有几乎没有问题的硬度，并且在口腔中快速分解。该片剂通过用药物崩解剂包衣的片剂制成，其中核心是含有水溶性药物或含有药物和糖的颗粒。

26. 发明申请

US20080020990A1 Oligo Double-Stranded Rna Inhibiting the Expression of Bcl-2 and Pharmaceutical Composition Containing the Same 审中-公开
标题翻译： Oligo双链Rna抑制Bcl-2的表达和含有它的药物组合物
公开(公告)号：US20080020990A1
公开(公告)日：2008-01-24
申请号：US10559083
申请日：2004-05-28
申请人： Junichi Yano , Kazuko Hirabayashi , Shinichiro Nakagawa
发明人： Junichi Yano , Kazuko Hirabayashi , Shinichiro Nakagawa
IPC分类号： A61K31/7105 , A61K48/00 , A61P35/00 , A61P7/00 , C07H21/02
CPC分类号： C12N15/1135 , A61K31/7105 , C12N2310/14
摘要： The present invention relates to oligo double-stranded RNAs for use in knockdown of the expression of Bcl-2 protein known as a suppressor for apoptosis, and pharmaceutical compositions containing them. It is known that Bcl-2 protein is over-expressed in diseases such as cancer, and by this over-expression, the growth of cancer cells is continued and the drug resistance to anti-cancer agents is caused. The present invention provides highly active oligo double-stranded RNAs cleaving bcl-2 mRNA and further provides pharmaceutical compositions comprising a complex of the oligo double-stranded RNA and a suitable carrier for inhibiting the expression of Bcl-2 protein.
摘要翻译：本发明涉及用于敲低已知为凋亡抑制剂的Bcl-2蛋白的表达的寡聚双链RNA，以及含有它们的药物组合物。已知Bcl-2蛋白在诸如癌症的疾病中过度表达，并且由于这种过度表达，癌细胞的生长继续进行，并且导致对抗癌剂的耐药性。本发明提供了切割bcl-2 mRNA的高活性寡聚双链RNA，并进一步提供了包含寡聚双链RNA和用于抑制Bcl-2蛋白表达的合适载体的复合物的药物组合物。

27. 发明授权

US07276525B2 Osteogenesis-promotion enhancer and method of screening the same 失效
标题翻译：造骨促进增强剂及其筛选方法
公开(公告)号：US07276525B2
公开(公告)日：2007-10-02
申请号：US10559155
申请日：2004-06-07
申请人： Kohei Miyazono , Takeshi Imamura , Shingo Maeda
发明人： Kohei Miyazono , Takeshi Imamura , Shingo Maeda
IPC分类号： A61K31/44 , A61K38/00
CPC分类号： G01N33/6863 , A61K31/4439 , A61K38/1875 , A61K45/06 , G01N2333/51 , G01N2500/00 , A61K2300/00
摘要： It is an object of the present invention to provide an excellent enhancer for an osteogenesis accelerator that can enhance the activity of BMP as an osteogenesis accelerator. Another object of the present invention is to provide a method of screening for a novel enhancer for an osteogenesis accelerator.The present invention relates to an enhancer for an osteogenesis accelerator, which comprises a compound having a TGF-β selective inhibitory activity as an active ingredient, the enhancer being administered with an osteogenesis accelerator containing BMP as an active ingredient either simultaneously or sequentially, and to a method of screening for an enhancer for an osteogenesis accelerator, comprising using a TGF-β inhibition as a measure for discovering the enhancer.
摘要翻译：本发明的目的是提供一种成骨促进剂的优异增强剂，其能够增强BMP作为成骨促进剂的活性。本发明的另一个目的是提供一种筛选用于成骨促进剂的新增强剂的方法。本发明涉及一种成骨促进剂的增强剂，其包含具有TGF-β选择性抑制活性作为活性成分的化合物，所述增强剂以含有BMP作为活性成分的成骨促进剂同时或依次施用，以及筛选增强子用于成骨促进剂的方法，包括使用TGF-β抑制作为发现增强子的量度。

28. 发明授权

US07220751B2 Quinazoline derivatives and drugs 失效
标题翻译：喹唑啉衍生物和药物
公开(公告)号：US07220751B2
公开(公告)日：2007-05-22
申请号：US10399803
申请日：2001-11-01
申请人： Masahiko Okano , Kazuya Mori
发明人： Masahiko Okano , Kazuya Mori
IPC分类号： A61K31/517 , C07D413/02 , C07D209/36 , C07C29/20 , C07C275/00
CPC分类号： C07D401/06 , C07D239/94
摘要： The invention provides an excellent novel analgesic which acts on a nociceptin receptor to exhibit a wide range of the analgesic effect for example on a chronic pain as well as an allodynia accompanied with a herpes zoster.The invention relates to a nociceptin receptor agonist comprising as an active ingredient a compound represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or alkyl; A1 and A2 are the same or different and each represents a single bond or a divalent aliphatic hydrocarbon group; Q represents a single bond, cycloalkylene group, phenylene group or a divalent heterocyclic group; R2A and R2B are the same or different and each represents a hydrogen atom or alkyl; R3 represents an optionally substituted phenyl group or heterocyclic group; R4 and R5 are the same or different and each represents a hydrogen atom, alkyl, alkoxy, aralkyloxy, halogen, nitro, hydroxy, alkoxycarbonyl, —NR6R7 and the like.
摘要翻译：本发明提供了一种优异的新颖止痛剂，其作用于伤害感受肽受体以表现出广泛的止痛效果，例如慢性疼痛以及伴随带状疱疹的异常性疼痛。本发明涉及一种伤害感受肽受体激动剂，其包含作为活性成分的由式（I）表示的化合物或其盐：其中R 1表示氢原子或烷基; A 1和A 2相同或不同，各自表示单键或二价脂族烃基; Q表示单键，亚环烷基，亚苯基或二价杂环基; R 2A和R 2B相同或不同，各自表示氢原子或烷基; R 3表示任选取代的苯基或杂环基; R 4和R 5相同或不同，各自表示氢原子，烷基，烷氧基，芳烷氧基，卤素，硝基，羟基，烷氧基羰基，-NR 6＆lt; 7＆gt;等等。

29. 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。

30. 发明授权

US07030143B2 Heterocyclic compounds 失效
标题翻译：杂环化合物
公开(公告)号：US07030143B2
公开(公告)日：2006-04-18
申请号：US10781293
申请日：2004-02-17
申请人： Kenji Kuwabara , Tomiyoshi Aoki
发明人： Kenji Kuwabara , Tomiyoshi Aoki
IPC分类号： A61K31/421 , A61K31/4439 , C07D413/04
CPC分类号： A61K31/4439 , A61K31/4178 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/427 , C07D263/32 , C07D277/24 , C07D405/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention provides a preventive or therapeutic agent for hyperlipidemia, comprising as an active ingredient a heterocyclic compound of the formula [1], or a pharmaceutically acceptable salt thereof: wherein: R1 is optionally substituted aryl or aromatic heterocyclic group, Het is a divalent aromatic heterocyclic group, D is alkylene, alkenylene, alkynylene, or the like, and E is carboxy, or the like, and novel compounds among the heterocyclic compounds of the formula [1] above, which has blood triglyceride lowering effect, LDL-C lowering effect, and blood glucose lowering effect and blood insulin lowering effect, or HDL-C increasing effect or atherogenic index lowering effect all together, and hence is useful in the prevention or treatment of hyperlipidemia, arteriosclerosis, diabetes mellitus, hypertension, obesity, and the like.
摘要翻译：本发明提供高脂血症的预防或治疗剂，其包含作为活性成分的式[1]的杂环化合物或其药学上可接受的盐：其中：R 1是任选取代的芳基或芳族杂环基，Het为二价芳族杂环基，D为亚烷基，亚烯基，亚炔基等，E为羧基等，上述式[1]的杂环化合物中具有新化合物，其具有血液甘油三酯降低效果，降低LDL-C降低作用，血糖降低作用和血胰岛素降低作用，或HDL-C增加效果或致动脉粥样化指数降低作用，因此可用于预防或治疗高脂血症，动脉硬化，糖尿病，高血压，肥胖等。

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