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1. 发明申请

US20090239828A1 Adhesive preparation 审中-公开
标题翻译：粘合剂制备
公开(公告)号：US20090239828A1
公开(公告)日：2009-09-24
申请号：US12310876
申请日：2007-09-10
申请人： Yuuhiro Yamazaki , Noriyuki Hayashi , Yoshiki Sakai
发明人： Yuuhiro Yamazaki , Noriyuki Hayashi , Yoshiki Sakai
IPC分类号： A61K31/663 , A61P19/10 , A61P19/02 , A61P35/04 , A61P19/08 , A61P19/00
CPC分类号： A61K9/7053 , A61K9/7061 , A61K9/7069 , A61K9/7076 , A61K31/663
摘要： The present invention provides an adhesive preparation having a plaster layer disposed on a support, the adhesive preparation comprising at least one active ingredient selected from the group consisting of a bisphosphonic acid derivative, its salt thereof and a hydrate of either of the bisphosphonic acid derivative or the salt, a solubilizer for the active ingredient, propylene glycol, a hydrogenated terpene resin, an adhesive base, and a softening agent in the plaster layer.
摘要翻译：本发明提供了一种具有设置在支持体上的石膏层的粘合剂制剂，该粘合剂制剂包含至少一种选自双膦酸衍生物，其盐和双膦酸衍生物或其中任一种的水合物的活性成分盐，活性成分的增溶剂，丙二醇，氢化萜烯树脂，粘合剂基质和膏药层中的软化剂。

2. 发明申请

US20110071204A1 PERCUTANEOUS ABSORPTION PREPARATION 审中-公开
标题翻译： PERCUTANEOUS吸收制剂
公开(公告)号：US20110071204A1
公开(公告)日：2011-03-24
申请号：US11815499
申请日：2006-02-02
申请人： Koichi Takahashi , Yoshiki Sakai
发明人： Koichi Takahashi , Yoshiki Sakai
IPC分类号： A61K31/4164 , A61P11/06 , A61P13/10 , A61P9/00
CPC分类号： A61K9/7053 , A61K9/7069 , A61K31/4164
摘要： This present invention provides a percutaneous absorption type pharmaceutical preparation which includes 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide as the active ingredient and a backbone for transdermal system, and satisfies at least one of the following conditions (1) and (2). The pharmaceutical preparation of the present invention enables absorption of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide, which has a low ability to be absorbed from the skin, from the skin into the body continuously and efficiently. (1) The active ingredient content in one preparation or one time administration preparation is from about 0.1 mg to about 10 mg, (2) the size is from about 1 cm2 to about 300 cm2.
摘要翻译：本发明提供一种经皮吸收型药物制剂，其包含4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺作为活性成分，经皮系统的骨架，并满足以下条件中的至少一个（ 1）和（2）。本发明的药物制剂能够连续而有效地从皮肤吸收具有低的皮肤吸收能力的4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺。（1）一次制剂或一次给药制剂中的活性成分含量为约0.1mg至约10mg，（2）尺寸为约1cm 2至约300cm 2。

3. 发明申请

US20060188554A1 Transdermal absorption preparation 审中-公开
标题翻译：透皮吸收制剂
公开(公告)号：US20060188554A1
公开(公告)日：2006-08-24
申请号：US10566502
申请日：2004-08-03
申请人： Katashi Nakashima , Satoshi Ohmori , Norihiro Kanayama , Yoshiki Sakai
发明人： Katashi Nakashima , Satoshi Ohmori , Norihiro Kanayama , Yoshiki Sakai
IPC分类号： A61K31/445 , A61K31/4164 , A61F13/02
CPC分类号： A61K9/7053 , A61K9/7076 , A61K31/4174
摘要： (Object) A transdermal preparation is provided, which ensures stable and effective absorption of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutylamide (KRP-197) which has a low skin absorption and is a bladder-selective muscarinic M3 and M1 receptor antagonist, into body through the skin while causing little side effects and providing sustained pharmacological effect with less skin irritancy. (Solving means) A composition comprising KRP-197 and an external preparation base is deposited and dried onto a structural body or a small pool of the composition is deposited on the structural body to obtain a single adhesive layer-type transdermal preparation or a reservoir-type transdermal preparation. These preparations can ensure high permeation of KRP-197 through the skin and sustained absorption of KRP-197 into body while causing decreased skin irritancy.
摘要翻译：（对象）提供透皮制剂，其确保具有低皮肤吸收性并且是膀胱选择性的4-（2-甲基-1-咪唑基）-2,2-二苯基丁基酰胺（KRP-197）的稳定和有效的吸收毒蕈碱M3和M1受体拮抗剂通过皮肤进入体内，同时引起少量副作用，并提供持久的药理作用，皮肤刺激性较小。（解决方法）将包含KRP-197和外部制剂基质的组合物沉积并干燥到结构体上，或将组合物的小池沉积在结构体上，以获得单一粘合剂层型透皮制剂或储液器 - 型透皮制剂。这些制剂可以确保KRP-197通过皮肤的高渗透和KRP-197持续吸收到体内，同时引起皮肤刺激性降低。

4. 发明授权

US08617614B2 Sustained release preparation for tissue regeneration therapy 有权
标题翻译：组织再生治疗的缓释制剂
公开(公告)号：US08617614B2
公开(公告)日：2013-12-31
申请号：US12446157
申请日：2007-10-18
申请人： Yoshiki Sakai , Takahiro Uchida
发明人： Yoshiki Sakai , Takahiro Uchida
IPC分类号： A61K9/50 , A61K31/44 , A01N43/40
CPC分类号： A61K31/4406 , A61K9/1647
摘要： The present invention provides a microsphere with a slow-release period from about two weeks to about four weeks following administration, to enable a higher content of a drug to be included, to suppress an initial burst of the drug, and to maintain an optimal, effective blood concentration during the slow-release period. In a microsphere containing a drug and polylactic acid/glycolic acid (PLGA) copolymer, the amount of PLGA copolymer per part by weight of the drug is from about 3 to about 10 parts by weight; the average particle size of the microsphere is from about 20 to about 50 μm; and (3) the PLGA copolymer has a weight-average molecular weight from about 10,000 to about 50,000 and a PLGA compositional ratio from about 75/25 to about 50/50. The microsphere promotes the production of various endogenous repair factors useful against various tissue disorders.
摘要翻译：本发明提供了一种在施用后约两周至约四周的缓释期的微球，以使得能够包含更高含量的药物以抑制药物的初始爆发，并保持最佳，缓释期有效血药浓度。在含有药物和聚乳酸/乙醇酸（PLGA）共聚物的微球中，每重量份药物的PLGA共聚物的量为约3至约10重量份; 微球的平均粒径为约20至约50μm; 和（3）PLGA共聚物的重均分子量为约10,000至约50,000，PLGA组成比为约75/25至约50/50。微球促进了各种可用于各种组织疾病的内源性修复因子的产生。

5. 发明授权

US07547715B2 Endogenous repair factor production accelerator 有权
标题翻译：内源性修复因子生产加速器
公开(公告)号：US07547715B2
公开(公告)日：2009-06-16
申请号：US10530685
申请日：2003-10-09
申请人： Yoshiki Sakai , Akio Nishiura , Teppei Ogata
发明人： Yoshiki Sakai , Akio Nishiura , Teppei Ogata
IPC分类号： A61K31/44
CPC分类号： A61K31/4406 , A61K9/1647 , A61K9/5031 , A61K31/19 , A61K31/343 , A61K31/403 , A61K45/06
摘要： It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) I2 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
摘要翻译：它涉及内源性修复因子产生促进剂，其包含选自前列腺素（PG）I2激动剂，EP2激动剂和EP4激动剂中的一种或至少两种。由于前列腺素（PG）I2激动剂，EP2激动剂或EP4激动剂具有各种内源性修复因子产生促进作用，血管生成加速作用和干细胞分化诱导作用，其可用作缺血性器官疾病（例如动脉硬化症）的预防和/或治疗剂闭塞性心脏病，勃起病，雷诺病，心肌梗死，心绞痛，糖尿病性神经病变，椎管狭窄，脑血管意外，脑梗塞，肺动脉高压，骨折，阿尔茨海默病等）和各种细胞和器官疾病。

6. 发明授权

US4464388A Use of prostaglandin analogues to treat cytodamage 失效
标题翻译：使用前列腺素类似物治疗细胞损伤
公开(公告)号：US4464388A
公开(公告)日：1984-08-07
申请号：US478031
申请日：1983-03-23
申请人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
发明人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
IPC分类号： A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557 , A61K31/5575 , A61P1/16 , A61P43/00 , C07C67/00 , C07C401/00 , C07C405/00 , C08B37/00 , A61K31/215 , A61K31/19
CPC分类号： C08B37/0015 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557
摘要： Prostaglandin analogue of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atom(s), R.sup.2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atom(s), the symbols------X--Y--Z-- in formula VB represent one of the groups: ##STR2## wherein in formulae (ii) and (iv), the configuration on C.sub.6 is S- or R-configuration or a mixture thereof and in formulae (iii) and (v) the double bond between C.sub.5 and C.sub.6 is in E- or Z-configuration or a mixture thereof) and n represents an integer of from 3 to 5 non-toxic salts thereof when R.sup.1 represents a hydrogen atom and cyclodextrin clathrates thereof are useful in the prevention or treatment of cytodamage associated with many diseases, especially liver damage.
摘要翻译：具有下式的前列腺素类似物：其中R 1表示氢原子或含有1至12个碳原子的直链或支链烷基，R 2表示氢原子原子或含有1至6个碳原子的直链或支链烷基，式VB中的符号--- XYZ-表示下列组之一：（i）（ii）（iv）其中在式（ii）和（iv）中，C6上的构型是S-或R-构型或其混合物，在式（ⅲ）中，和（v）C 5和C 6之间的双键为E-或Z-构型或其混合物），当R 1表示氢原子时，n表示3至5个无毒盐的整数，并且其环糊精包合物为可用于预防或治疗与许多疾病相关的细胞损伤，特别是肝损伤。

7. 发明申请

US20100323026A1 SUSTAINED RELEASE PREPARATION FOR TISSUE REGENERATION THERAPY 有权
标题翻译：用于组织再生治疗的持续释放准备
公开(公告)号：US20100323026A1
公开(公告)日：2010-12-23
申请号：US12446157
申请日：2007-10-18
申请人： Yoshiki Sakai , Takahiro Uchida
发明人： Yoshiki Sakai , Takahiro Uchida
IPC分类号： A61K9/14 , A61K31/4406 , A61P9/10 , A61P9/00 , A61P11/00 , A61P9/12 , A61P11/06 , A61P3/10 , A61P19/10 , A61P19/02
CPC分类号： A61K31/4406 , A61K9/1647
摘要： The object of the present invention is to provide a microsphere which has a slow-release period of from about two weeks to about four weeks following administration, enables a higher content of a drug to be included, suppresses an initial burst of the drug, and enables the drug to be maintained at an optimal, effective blood concentration during the slow-release period.In a microsphere containing a drug and PLGA, the above problems can be resolved by setting: (1) the amount of lactic acid/glycolic acid copolymer per part by weight of the drug to from about 3 to about 10 parts by weight; (2) the microsphere to an average particle size of from about 20 to about 50 μm; and (3) the lactic acid/glycolic acid copolymer to a weight-average molecular weight of from about 10,000 to about 50,000 and to a lactic acid/glycolic acid compositional ratio of from about 75/25 to about 50/50.In addition, the microsphere, by promoting the production of various endogenous repair factors, is useful against various tissue disorders.
摘要翻译：本发明的目的是提供一种微球，其在施用后具有约两周至约四周的缓释期，能够包含更高含量的药物，抑制药物的初始爆发，以及使药物在缓释期间保持在最佳的有效血药浓度。在含有药物和PLGA的微球中，上述问题可通过以下方式来解决：（1）每重量份药物的乳酸/乙醇酸共聚物的量为约3至约10重量份; （2）微球的平均粒度为约20至约50μm; 和（3）乳酸/乙醇酸共聚物，其重均分子量为约10,000至约50,000，乳酸/乙醇酸组成比为约75/25至约50/50。此外，微球通过促进各种内源性修复因子的产生，可用于各种组织疾病。

8. 发明申请

US20060122275A1 Agentfor reducing side effects of diclofenac 审中-公开
标题翻译：用于减少双氯芬酸副作用的药剂
公开(公告)号：US20060122275A1
公开(公告)日：2006-06-08
申请号：US10524857
申请日：2003-08-21
申请人： Yoshiki Sakai , Nobuo Katsube , Akio Nishiura , Masanobu Yamamoto , Ken-ichi Sugishita
发明人： Yoshiki Sakai , Nobuo Katsube , Akio Nishiura , Masanobu Yamamoto , Ken-ichi Sugishita
IPC分类号： A61K31/557 , A61K31/195 , A61K31/192
CPC分类号： A61K31/215 , A61K9/4808 , A61K31/196 , A61K31/216 , A61K31/5575 , A61K45/06 , A61K2300/00
摘要： The present invention relates to reduction of side effects of diclofenac or a salt thereof An agent for reducing side effects of diclofenac or a salt thereof which comprises ornoprostil. It is expected that a combination agent of diclofenac or a non-toxic salt thereof and ornoprostil is comparable to even superior to marketed diclofenac tablets or Arthrotec tables in effects and fast-acting property while showing little side effects (particularly digestive disorders, gastric ulcer, diarrhea/vomiting and renal disorder) and exerting excellent antipyretic, analgesic and antiinlfammatory effects. Also, by formulating the combination agent into a preparation of separation type pharmaceutical preparation, the stability of ornoprostil can be improved.
摘要翻译：本发明涉及降低双氯芬酸或其盐的副作用。本发明涉及降低双氯芬酸或其盐的副作用的药剂，其包含鸟苷前列腺素。预期双氯芬酸或其无毒盐和奥罗前列素的组合剂与甚至优于市售的双氯芬酸片剂或Arthrotec的效果和速效性能相当，但几乎没有副作用（特别是消化系统疾病，胃溃疡，腹泻/呕吐和肾脏疾病），并具有优异的解热，镇痛和抗炎作用。此外，通过将组合剂配制成分离型药物制剂的制剂，可以提高奥斯匹林的稳定性。

9. 发明授权

US4503068A Use of prostaglandin analogues to treat cytodamage 失效
标题翻译：使用前列腺素类似物治疗细胞损伤
公开(公告)号：US4503068A
公开(公告)日：1985-03-05
申请号：US497052
申请日：1983-05-23
申请人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
发明人： Yoshiki Sakai , Katsuhiro Imaki , Takashi Muryobayashi
IPC分类号： A61K31/045 , A61K31/23 , A61K31/275 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557 , A61K47/48 , A61P43/00 , C08B37/00 , A61K31/19
CPC分类号： B82Y5/00 , A61K31/34 , A61K31/38 , A61K31/40 , A61K31/557 , A61K47/48969 , C08B37/0015
摘要： The prostaglandin analogues16S-methyl-6-oxo-PGE.sub.1 methyl ester,17S,20-dimethyl-6-oxo-PGE.sub.1 methyl ester,15S-methyl-6-oxo-PGE.sub.1 and non-toxic salts thereof,17S,20-dimethyl-13,14-dihydro-6-oxo-PGE.sub.1 methyl ester,17S,20-dimethyl-6-oxo-PGE.sub.1 alcohol,17S,20-dimethyl-6S-PGI.sub.1 methyl ester,17S,20-dimethyl-trans-.DELTA..sup.2 -6RS-PGI.sub.1 methyl ester,17S,20-dimethyl-6,9.alpha.-nitrilo-PGI.sub.1 methyl ester,2-decarboxy-2-glycoloyl-17S,20-dimethyl-6S-PGI.sub.1,2-decarboxy-2-glycoloyl-15-cyclopentyl-16,17,18,19,20-pentanor-6S-PGI.sub.117S,20-dimethyl-6S-PGI.sub.1 alcohol,15-cyclopentyl-16,17,18,19,20-pentanor-6S-PGI.sub.1 alcohol and15-(3-propylcyclopentyl)-16,17,18,19,20-pentanor-6,9.alpha.-nitrilo-PGI.sub.1 alcohol,and cyclodextrin clathrates thereof are useful in the prevention or treatment of cytodamage.
摘要翻译：前列腺素类似物16S-甲基-6-氧代-PGE1甲酯，17S，20-二甲基-6-氧代-GE-PGE1甲酯，15S-甲基-6-氧代-PGE1及其无毒盐，17S，20-二甲基 -13,14-二氢-6-氧代-GE-PGE1甲酯，17S，20-二甲基-6-氧代-PPE1醇，17S，20-二甲基-6S-PGI1甲酯，17S，20-二甲基 - 反式-TATA 2 -6RS-PGI1甲酯，17S，20-二甲基-6,9α-二硝基-GII1甲酯，2-脱羧-2-乙酰基-17S，20-二甲基-6S-PGI1,2-脱羧-2-乙酰基 - 15-环戊基-16,17,18,19,20-戊酰-6S-PGI1,17S，20-二甲基-6S-PGI1醇，15-环戊基-16,17,18,19,20-戊酰-6S-PGI1 醇和15-（3-丙基环戊基）-16,17,18,19,20-戊醇-6,9α-亚硝基-PGI1醇及其环糊精包合物可用于预防或治疗细胞损伤。

10. 发明授权

US08436026B2 Endogeneous repair factor production promoters 有权
标题翻译：内生修复因子生产启动子
公开(公告)号：US08436026B2
公开(公告)日：2013-05-07
申请号：US12034614
申请日：2008-02-20
申请人： Yoshiki Sakai , Akio Nishiura , Teppei Ogata
发明人： Yoshiki Sakai , Akio Nishiura , Teppei Ogata
IPC分类号： A61K31/04
CPC分类号： A61K31/4406 , A61K9/1647 , A61K9/5031 , A61K31/19 , A61K31/343 , A61K31/403 , A61K45/06
摘要： It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) 12 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) 12 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases.
摘要翻译：其涉及内源性修复因子产生促进剂，其包含选自前列腺素（PG）12激动剂，EP2激动剂和EP4激动剂中的一种或至少两种。由于前列腺素（PG）12激动剂，EP2激动剂或EP4激动剂具有各种内源性修复因子产生促进作用，血管生成加速作用和干细胞分化诱导作用，其可用作缺血性器官疾病（例如动脉硬化症）的预防和/或治疗剂闭塞性心脏病，勃起病，雷诺病，心肌梗死，心绞痛，糖尿病性神经病变，椎管狭窄，脑血管意外，脑梗塞，肺动脉高压，骨折，阿尔茨海默病等）和各种细胞和器官疾病。

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