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31. 发明申请

US20050100598A1 Quick disintegrating tablet in buccal cavity and production process thereof 审中-公开
标题翻译：颊腔快速崩解片及其制作方法
公开(公告)号：US20050100598A1
公开(公告)日：2005-05-12
申请号：US10961875
申请日：2004-10-07
申请人： Takao Mizumoto , Yoshinori Masuda , Atsushi Kajiyama , Masahiro Yanagisawa , Janaki Ram Nyshadham
发明人： Takao Mizumoto , Yoshinori Masuda , Atsushi Kajiyama , Masahiro Yanagisawa , Janaki Ram Nyshadham
IPC分类号： A61K9/00 , A61K9/20 , A61K47/26 , A61K47/36 , H04L12/44 , H04L29/06 , H04L29/08
CPC分类号： H04L12/44 , A61K9/0056 , A61K9/2018 , A61K9/2095 , H04L29/06 , H04L67/12 , H04L67/26 , H04L69/08 , H04L69/329
摘要： The present invention relates to a quick disintegrating tablet in buccal cavity, comprising: a mixture, comprising a drug, a sugar (A), and an amorphous sugar (B), and after it is forming a tablet, it is humidified and dried. In particularly, the present invention relates to a quick disintegrating tablet in buccal cavity comprising: a mixture; comprising a drug, a sugar (A), and an amorphous sugar (B) which an amorphous-forming sugar in crystalline state is dissolved in a medicinally permitted solvent, the amorphous sugar is obtained from this solution by removing the solvent, and after it is forming a tablet, and it is humidified and dried. The tablet in the present invention is to provide stability against moisture at preserved, because the amorphous sugar changed to the crystalline state in a nonreversible reaction after it is humidified and dried in a manufacturing process. The tablet in the present invention is to further provide a design for the pharmaceutical preparation with respect to the stability of a drug, because the tablet is manufactured by one kind of a sugar and an amorphous sugar. Furthermore, the tablet in the present invention is to provide a production process by utilizing a common granulating machine and by utilizing a common tablet machine.
摘要翻译：本发明涉及颊腔中的快速崩解片，其包含：包含药物，糖（A）和无定形糖（B）的混合物，在形成片剂之后，将其加湿干燥。特别地，本发明涉及颊腔中的快速崩解片剂，其包含：混合物; 包含药物，糖（A）和无定形糖（B），其中结晶状态的无定形形成糖溶解在药物允许溶剂中，通过除去溶剂从该溶液获得无定形糖，之后正在形成片剂，并且被加湿和干燥。本发明中的片剂是为了提供在保存的水分中的稳定性，因为无定形糖在制造过程中被加湿干燥后，在不可逆反应中变为结晶状态。本发明的片剂是为了进一步提供关于药物的稳定性的药物制剂的设计，因为片剂由一种糖和无定形糖制造。此外，本发明中的片剂是通过利用普通的造粒机和利用普通的压片机来提供制造方法。

32. 发明授权

US06878525B1 Peptide leukotriene receptor 有权
标题翻译：肽白三烯受体
公开(公告)号：US06878525B1
公开(公告)日：2005-04-12
申请号：US09979603
申请日：2000-09-13
申请人： Jun Takasaki , Masazumi Kamohara , Mitsuyuki Matsumoto , Tetsu Saito , Tohru Sugimoto , Toshio Ota , Takao Isogai , Tetsuo Nishikawa , Yuri Kawai
发明人： Jun Takasaki , Masazumi Kamohara , Mitsuyuki Matsumoto , Tetsu Saito , Tohru Sugimoto , Toshio Ota , Takao Isogai , Tetsuo Nishikawa , Yuri Kawai
IPC分类号： A61K38/00 , A61P9/08 , A61P43/00 , C07K14/705 , C12N15/12 , G01N33/68 , G01N33/567
CPC分类号： C07K14/705 , A61K38/00 , G01N33/6893 , G01N2500/00 , G01N2500/04
摘要： A cDNA encoding a novel LTC4 receptor has been isolated. Provision of the novel protein, an LTC4 receptor, enabled binding experiments using the LTC4. By screening for compounds that modulate LTC4 receptor activity based on these binding experiments, development of drugs targeting the LTC4 receptor becomes possible.
摘要翻译：已经分离出编码新的LTC4受体的cDNA。提供新的蛋白质LTC4受体，启用使用LTC4的结合实验。通过筛选基于这些结合实验调节LTC4受体活性的化合物，开发靶向LTC4受体的药物成为可能。

33. 发明申请

US20050031587A1 Immune response induction method 审中-公开
标题翻译：免疫反应诱导方法
公开(公告)号：US20050031587A1
公开(公告)日：2005-02-10
申请号：US10674581
申请日：2003-09-29
申请人： Yuuki Tsutsui , Kiyo Nakanishi , Shunsuke Watanabe , Shigeo Takemura
发明人： Yuuki Tsutsui , Kiyo Nakanishi , Shunsuke Watanabe , Shigeo Takemura
IPC分类号： A61K38/21 , A61K39/00
CPC分类号： A61K39/39 , A61K38/212 , A61K2039/543 , A61K2039/55522 , A61K2300/00
摘要： The present invention proposes a method of inducing both vaccine antigen-specific antibody in blood and vaccine antigen-specific antibody secreted at the mucosal surface using vaccine antigen and adjuvant of said vaccine antigen.
摘要翻译：本发明提出了使用疫苗抗原和所述疫苗抗原的佐剂诱导血液中的疫苗抗原特异性抗体和分泌在粘膜表面的疫苗抗原特异性抗体的方法。

34. 发明申请

US20040253309A1 Enteric sustained-release fine particles of tamsulosin and its salt and manufacturing method thereof 审中-公开
标题翻译：肠溶缓慢释放的坦索罗辛缓释微粒及其盐及其制备方法
公开(公告)号：US20040253309A1
公开(公告)日：2004-12-16
申请号：US10766201
申请日：2004-01-27
申请人： Yamanouchi Pharmaceutical Co., Ltd.
发明人： Yoji Tanijiri , Akira Ito , Hiroya Sugao , Tetsuya Tamura , Mare Nishura , Shigeru Yamazaki , Takao Mizumoto
IPC分类号： A61K009/26
CPC分类号： A61K9/0056 , A61K9/1652 , A61K9/5026 , A61K31/18
摘要： The present invention relates to enteric sustained-release fine particles of tamsulosin or its salt that can be contained in tablets that disintegrate in the buccal cavity and a manufacturing method thereof. In further detail, the present invention relates to enteric sustained-release fine particles for tablets that disintegrate in the buccal cavity, which comprise (1) tamsulosin or its salt and at least (2) an enterosoluble substance, and when necessary contain (3) a water-insoluble substance, and which have the following characteristics: 1) a particle diameter of approximately 5 to 250 nullm 2) when dissolution tests are performed on tablets that disintegrate in the buccal cavity containing these particles by dissolution testing methods cited in the Japanese Pharmacopoeia, a) the dissolution rate of tamsulosin or its salt at a pH of 1.2 two hours after starting tests is 25% or less b) the time when 50% of the tamsulosin or its salt has dissolved at a pH of 6.8 is 0.5 to 5 hours, and a manufacturing method thereof.
摘要翻译：本发明涉及可以包含在颊腔中分解的片剂中的坦索罗辛或其盐的肠溶缓释微粒及其制造方法。更详细地说，本发明涉及在颊腔中崩解的片剂的肠溶缓释微粒，其包含（1）坦洛新或其盐和至少（2）肠溶性物质，并且在必要时包含（3）一种水不溶性物质，具有以下特征：1）粒径约5〜250μm2）当对含有这些颗粒的颊腔分解的片剂进行溶解试验时，通过日本的溶出试验方法药典，a）在开始试验后两小时pH2.2时，坦索罗辛或其盐的溶解速率为25％以下b）当pH值为6.8时，坦索罗辛或其盐50％溶解的时间为0.5〜 5小时及其制造方法。

35. 发明申请

US20040068109A1 Diazepan derivatives or salts thereof 有权
标题翻译：二氮杂环庚烷衍生物或其盐
公开(公告)号：US20040068109A1
公开(公告)日：2004-04-08
申请号：US10656129
申请日：2003-09-08
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Fukushi Hirayama , Hiroyuki Koshio , Tsukasa Ishihara , Norio Seki , Shunichiro Hachiya , Keizo Sugasawa , Ryota Shiraki , Yuji Koga , Yuzo Matsumoto , Takeshi Shigenaga , Souichirou Kawazoe
IPC分类号： A61K031/551 , C07D243/08
CPC分类号： C07D401/04 , A61K31/551 , C07D243/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D471/04
摘要： To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-null(3-carbamimidoylphenylamino)methylnull-3-null4-(4-methyl-1,4-diazepan-1-yl)benzoylaminonullbenzoic acid and 3-hydroxy-4null-methoxy-2-nullnull4-(4-methyl-1,4-diazepan-1-yl)benzoylnullaminonullbenzanilide or a salt thereof is an effective ingredient.
摘要翻译：提供具有基于活化凝血因子X的抑制的抗凝作用的化合物，并且可用作抗凝血剂或用于预防和治疗由血栓或栓塞引起的疾病的药剂。二氮杂环丁烷衍生物如4 - [（3-氨甲酰氨基）甲基] -3- [4-（4-甲基-1,4-二氮杂环庚烷-1-基）苯甲酰基氨基]苯甲酸和3-羟基-4'-甲氧基 - 2 - {[4-（4-甲基-1,4-二氮杂环庚烷-1-基）苯甲酰基]氨基} -N-苯甲酰苯胺或其盐是有效成分。

36. 发明申请

US20030055092A1 Remedies for ischemic stroke 审中-公开
标题翻译：缺血性卒中的治疗方法
公开(公告)号：US20030055092A1
公开(公告)日：2003-03-20
申请号：US10282087
申请日：2002-10-29
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
发明人： Masamichi Okada , Masayasu Takahashi , Satoshi Hayashibe
IPC分类号： A61K031/428
CPC分类号： A61K31/429 , A61K31/00 , A61K31/428
摘要： This invention is to provide remedies for ischemic stroke which contain as an active ingredient a compound having mGluR1 antagonism, pharmaceutical compositions which are remedies for ischemic stroke at the acute stage, pharmaceutical compositions which contain as an active ingredient a compound having selective mGluR1 antagonism, and pharmaceutical compositions wherein the compound having selective mGluR1 antagonism is 6-amino-N-cyclohexyl-N,3 -dimethylthiazolonull3,2-anullbenzoimidazole-2-carboxamide dihydrochloride.
摘要翻译：本发明提供缺血性卒中的补救措施，其含有作为活性成分的具有mGluR1拮抗作用的化合物，作为急性期缺血性卒中的药物的药物组合物，含有选择性mGluR1拮抗作用的化合物作为活性成分的药物组合物，以及具有选择性mGluR1拮抗作用的化合物是6-氨基-N-环己基-N，3-二甲基噻唑并[3,2-a]苯并咪唑-2-甲酰胺二盐酸盐的药物组合物。

37. 发明申请

US20030039685A1 Bitterness-reduced intrabuccally quick disintegrating tablets and method for reducing bitterness 失效
标题翻译：苦味减少的脂肪内快速崩解片剂和减少苦味的方法
公开(公告)号：US20030039685A1
公开(公告)日：2003-02-27
申请号：US10096892
申请日：2002-03-14
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
发明人： Masahiro Yanagisawa , Takao Mizumoto
IPC分类号： A61K009/20
CPC分类号： A61K9/0056
摘要： The invention relates to a method for reducing bitterness of bitter drugs, which does not cause delay of release rate, does not show reduction of bioavailability in comparison with conventional pharmaceutical preparations and, due to the use of additives generally used in the field of pharmaceutical preparation, has high practical value, and to intrabuccally quick disintegrating tablets having reduced bitterness of bitter drugs. Illustratively, it relates to an intrabuccally quick disintegrating tablet which comprises a bitter drug and a water-insoluble substance having an average particle size of 30 nullm or less, wherein the water-insoluble substance disperses as particles on the tongue surface prior to the release of the bitter drug.
摘要翻译：本发明涉及一种降低苦味药物的方法，其不会导致释放速度的延迟，与常规药物制剂相比并不显示降低生物利用度，并且由于使用通常用于药物制剂领域的添加剂具有很高的实用价值，并且具有降低苦味苦味的快速崩解片剂。说明性地，本发明涉及一种包含苦味药物和平均粒径为30μm以下的水不溶性物质的肌内快速崩解片剂，其中所述水不溶性物质在释放之前作为颗粒分散在舌片表面上苦药。

38. 发明申请

US20020031547A1 IMMEDIATELY DISINTEGRABLE MEDICINAL COMPOSITION 无效
标题翻译：立即消毒药物组合物
公开(公告)号：US20020031547A1
公开(公告)日：2002-03-14
申请号：US09331235
申请日：1999-06-18
申请人： YAMANOUCHI PHARMACEUTICAL CO., LTD.
发明人： HIROKAZU TAKAGI , ATSUSHI KAJIYAMA , MASAHIRO YANAGISAWA
IPC分类号： A61K009/20
CPC分类号： A61K9/2009 , A61K9/1617 , A61K9/1652 , A61K9/2018 , A61K9/2022 , A61K9/2054
摘要： The present invention relates to a pharmaceutical composition useful for rapid disintegration, which comprises a sparingly soluble medicament held on a gel-forming water-soluble polymer as a solid dispersion, wherein it contains a salt substance that comprises an alkali and a weak or strong acid and has an endothermic standard enthalpy of solution or heat of solution. Since rapid disintegration of the pharmaceutical composition of the present invention and rapid dissolution of the medicament contained in the preparation can be made in the digestive tracts pH-independently, good bioavailability can be attained.
摘要翻译：本发明涉及用于快速崩解的药物组合物，其包含保持在形成凝胶的水溶性聚合物作为固体分散体的微溶性药物，其中其含有包含碱和弱或强酸的盐物质并且具有吸热标准溶液溶液或溶液热。由于本发明的药物组合物的快速崩解和制剂中包含的药物的快速溶解可以在消费道中独立地进行，可以获得良好的生物利用度。

39. 发明授权

US6133258A Inhibitor of kainic acid neurotoxicity and pyridothiazine derivative 失效
标题翻译：红藻氨酸神经毒性抑制剂和吡啶并噻嗪衍生物
公开(公告)号：US6133258A
公开(公告)日：2000-10-17
申请号：US68534
申请日：1998-05-13
申请人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
发明人： Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
IPC分类号： A61K31/5415 , A61K31/542 , C07D513/04
CPC分类号： A61K31/5415
摘要： Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
摘要翻译： PCT No.PCT / JP96 / 03339 Sec。 371日期1998年5月13日 102（e）日期1998年5月13日PCT 1996年11月14日PCT PCT。出版物WO97 / 17970 日期1997年5月22日基于抑制红藻氨酸神经毒性的神经保护剂和基于抑制红藻氨酸神经毒性作用的神经保护剂的化合物。作为活性成分的红藻氨酸神经毒性抑制剂，含有下述通式（I）所示的吡哆噻嗪衍生物或其药学上可接受的盐，以及下述通式（I）表示的吡哒嗪衍生物或其药学上可接受的盐其中式中的符号具有以下各自的含义：环A：吡啶环; R 1，R 2，R 3，R 4和R 5可以相同或不同，各自表示氢原子或可以具有取代基或不存在的低级烷基，环烷基，烯基，芳基，羧基或低级烷氧基羰基，条件是R2和R3可以一起形成可以具有氮原子作为另一个杂原子的含氮杂环基，可以与苯环稠合并且可以具有低级烷基作为取代基。

40. 发明授权

US5795736A Genes coding for a protein having human MACIF activity, expression vectors containing said genes, transformant cells and proteins having human macif activity 失效
标题翻译：编码具有人MACIF活性的蛋白质的基因，含有所述基因的表达载体，转化体细胞和具有人类macif活性的蛋白质
公开(公告)号：US5795736A
公开(公告)日：1998-08-18
申请号：US514183
申请日：1995-08-11
申请人： Motowo Tomita , Yuji Sugita , Toshiyuki Takemoto , Kiyoshi Furuichi , Makoto Takayama , Ko Yasukawa , Katsuhisa Ito , Noboru Yamaji , Shinya Yano
发明人： Motowo Tomita , Yuji Sugita , Toshiyuki Takemoto , Kiyoshi Furuichi , Makoto Takayama , Ko Yasukawa , Katsuhisa Ito , Noboru Yamaji , Shinya Yano
IPC分类号： A61K38/00 , C07K4/12 , C07K14/705 , C12N15/12
CPC分类号： C07K14/70596 , A61K38/00 , Y10S530/808
摘要： Genes coding for a protein having human MACIF activity, expression vectors containing the genes, transformed cells with the vectors and proteins having human MACIF activity.
摘要翻译：编码具有人MACIF活性的蛋白质的基因，含有该基因的表达载体，具有载体的转化细胞和具有人MACIF活性的蛋白质。

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