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公开(公告)号：EP2151438B1
公开(公告)日：2012-10-31
申请号：EP08764395.3
申请日：2008-05-20
发明人： NAKAMURA, Yoshikuni , HANANO, Ikuko , INOUE, Jun
IPC分类号： C07D263/32 , A61K31/421 , A61K31/426 , A61K31/427 , A61P27/02 , A61P27/04 , A61P27/14 , A61P37/08 , A61P43/00 , C07D277/24 , C07D417/06
CPC分类号： A61K31/427 , A61K31/421 , A61K31/426 , C07D263/32 , C07D277/24 , C07D417/06
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公开(公告)号：EP2151438A1
公开(公告)日：2010-02-10
申请号：EP08764395.3
申请日：2008-05-20
发明人： NAKAMURA, Yoshikuni , HANANO, Ikuko , INOUE, Jun
IPC分类号： C07D263/32 , A61K31/421 , A61K31/426 , A61K31/427 , A61P27/02 , A61P27/04 , A61P27/14 , A61P37/08 , A61P43/00 , C07D277/24 , C07D417/06
CPC分类号： A61K31/427 , A61K31/421 , A61K31/426 , C07D263/32 , C07D277/24 , C07D417/06
摘要： Provision of an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, and a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.
A preparation containing [3-[2-[4-isopropyl-2-(4-trifluoromethyl)phenyl-5-thiazolyl]ethyl]-5-methyl-1,2-benzisoxazol-6-yl]oxyacetic acid, [4-[3-[2-(4-trifluoromethyl)phenyl-4-isopropyl-5-thiazolyl]propionyl]-2-methylphenoxy]acetic acid or [4-[3-[2-(2-hydroxy-4-chlorophenyl)-5-isopropyl-4-oxazolyl]propionyl]-2-methylphenoxy]acetic acid, or a pharmacologically acceptable salt thereof as an active ingredient is used as an agent for promoting proliferation of meibomian gland epithelial cells or corneal epithelial cells, as well as a therapeutic agent for ocular diseases such as meibomian gland dysfunction, dry eye and the like.摘要翻译： 提供用于促进睑板腺上皮细胞或角膜上皮细胞增殖的药剂，以及眼部疾病如睑板腺功能障碍，干眼症等的治疗剂。 含有[3- [2- [4-异丙基-2-（4-三氟甲基）苯基-5-噻唑基]乙基] -5-甲基-1,2-苯并异恶唑-6-基]氧基乙酸[4- [3- [2-（4-三氟甲基）苯基-4-异丙基-5-噻唑基]丙酰基] -2-甲基苯氧基]乙酸或[4- [3- [2-（2-羟基-4-氯苯基） 5-异丙基-4-恶唑基〕丙酰基〕-2-甲基苯氧基〕乙酸或其药学上可接受的盐作为活性成分，用作促进睑板腺上皮细胞或角膜上皮细胞增殖的药剂，以及 诸如睑板腺功能障碍，干眼症等眼部疾病的治疗剂。
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3.发明授权2-chloro-6,7-dimethoxy-N-5 [5-(1)H- indazolyl]quinazoline-4-amine, N-(1-benzyl-4-piperidinyl)-1H-indazole-5-amine dihydrochloride, 4-[2-(2,3,4,5,6-pentafluorophenyl)acryloyl]cinnamic acid and fasudil hydrochloride for use in repairing corneal perception. 有权2-氯-6,7-二甲氧基 - N-5 [5-（1）H-吲唑基]喹唑啉-4-胺，N-（1-苄基-4-哌啶基）-1H-吲唑-5-胺二盐酸盐， 4- [2-（2,3,4,5,6-五氟苯基）丙烯酰基]肉桂酸和法舒地尔盐酸盐在角膜感知的恢复中使用。
公开(公告)号：EP1616577B1
公开(公告)日：2011-09-21
申请号：EP04728020.1
申请日：2004-04-16
IPC分类号： A61P25/00 , A61K31/517 , A61P27/00 , A61K38/43 , A61K31/00
CPC分类号： A61K38/45 , A61K31/454 , A61K31/517 , C12Y304/22054
摘要： It is intended to provide a novel drug repairing the corneal perception after a corneal surgery and improving the symptoms of dry eye. This drug, which contains an Rho protein inhibitor, is useful for treating depression in corneal perception after a cataract surgery, after an LASIK surgery, after a PRK surgery, or after corneal transplantation, or in association with neuroparalytic keratopathy, corneal ulcer, diabetic keratopathy, etc. and improving dry eye symptoms.
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公开(公告)号：EP1692098A1
公开(公告)日：2006-08-23
申请号：EP04807051.0
申请日：2004-12-08
IPC分类号： C07C271/22 , C07C275/16 , C07C317/40 , C07D295/20 , C07K5/02
CPC分类号： C07D213/30 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07C2602/08 , C07D295/215 , C07D307/20 , C07D309/12
摘要： The present invention provides a compound represented by the formula (I): (INSERT CHEMICAL FORMULA) (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.
摘要翻译： 本发明提供由式（I）表示的化合物：（INSERT CHEMICAL FORMULA）（其中R 1是被低级烷氧基或杂环基取代的低级烷基或杂环基; R 2是任选被 苯基;并且R3是任选被卤素，低级烷氧基或苯基或稠合多环烃基团取代的低级烷基），其口服吸收良好，表现出良好的血液水平的持久性并且具有有效的钙蛋白酶抑制活性。
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公开(公告)号：EP1489076B1
公开(公告)日：2008-08-13
申请号：EP03712708.1
申请日：2003-03-14
发明人： NAKAMURA, Masayuki , INOUE, Jun
IPC分类号： C07D307/22 , A61K31/341 , A61P9/00 , A61P9/10 , A61P19/02 , A61P21/04 , A61P25/28 , A61P27/12 , A61P43/00
CPC分类号： C07D307/22
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6.发明授权USE OF CYSTEINPROTEASE INHIBITORS FOR THE MANUFACTURE OF A MEDICAMENT FOR PREVENTION AND TREATMENT OF BRAIN TISSUE IMPAIRMENT DUE TO HYPERTENSIVE ENCEPHALOPATHY OR ENCEPHALOTHLIPSIS. 有权半胱氨酸抑制剂用于制备药物VORGBEUGUNG和治疗GEHIRNGEWEBEZERRÜTUNG而导致高血压脑病或ENCEPHALOTHLIPSIS使用
公开(公告)号：EP1064021B1
公开(公告)日：2004-09-08
申请号：EP99909212.5
申请日：1999-03-17
发明人： AZUMA, Mitsuyoshi , YOSHIDA, Yukuo , SAKAMOTO, Yuji , INOUE, Jun
摘要： A pharmaceutical composition for the prophylaxis and therapy of brain tissue impairment, which contains, as an active ingredient, a compound of formula (I) wherein R represents an alkyl group having 1-4 carbon atoms or an aryl group having 6-10 carbon atoms which is optionally substituted; R and R may be the same or different and each represents hydrogen or an alkyl group having 1-4 carbon atoms or R and R may jointly form a ring having 3-7 carbon atoms; and R represents a lower alkyl group which is optionally substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.
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公开(公告)号：EP0474874B1
公开(公告)日：1995-10-18
申请号：EP91903819.0
申请日：1991-02-08
发明人： INOUE, Jun
IPC分类号： A61K31/195
CPC分类号： A61K31/195
摘要： A Maillard reaction inhibitor containing a substance represented by general formula (I), a pharmaceutically acceptable ester thereof, and a pharmaceutically acceptable salt of the substance or the ester, wherein X represents hydroxyl or nitro. It is used for treating or preventing various complications of diabetes, such as coronary artery disease, peripheral circulatory disturbance, cerebrovascular disease, neurosis, nephropathy, arteriosclerosis, arthrosclerosis, cataract and retinitis, and similar diseases caused by aging, such as atherosclerosis, coronary heart disease, cerebrovascular disease, senile cataract, and so forth.
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公开(公告)号：EP1491537B1
公开(公告)日：2010-07-07
申请号：EP03745432.9
申请日：2003-03-27
发明人： NAKAMURA, Masayuki , INOUE, Jun
IPC分类号： C07D265/32 , A61K31/5375 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/12 , A61P37/02 , A61P43/00
CPC分类号： A61K31/5375 , C07D265/32
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公开(公告)号：EP1557407B1
公开(公告)日：2009-11-11
申请号：EP03765283.1
申请日：2003-07-11
发明人： NAKAMURA, Masayuki , INOUE, Jun
IPC分类号： C07C311/19 , A61K31/18 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P27/06 , A61P27/12 , A61P37/02 , A61P43/00
CPC分类号： C07C311/19
摘要： A compound of the general formula: (I) wherein each of R1, R2 and R3 represents a lower alkyl group, which compound exhibits a calpain inhibiting activity.
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公开(公告)号：EP1964575A1
公开(公告)日：2008-09-03
申请号：EP06833405.1
申请日：2006-11-27
发明人： NAKAMURA, Yoshikuni , HANANO, Ikuko , INOUE, Jun
IPC分类号： A61K45/00 , A61K31/216 , A61K31/426 , A61K31/505 , A61P27/02 , C07D239/38 , C07D277/26
CPC分类号： C07D239/47 , A61K31/216 , A61K31/426 , A61K31/505 , C07D277/26
摘要： An object of the present invention is to provide an agent for promoting proliferation of a meibomian gland epithelial cell and a corneal epithelial cell, as well as provide an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye.
There are provided an agent for promoting proliferation of a meibomian gland epithelial cell or a corneal epithelial cell, containing a PPARα or δ agonist as an active ingredient, as well as an agent for treating an ocular disease such as meibomian gland dysfunction or evaporative dry eye, containing a PPARα or δ agonist as an active ingredient.摘要翻译： 本发明的目的是提供一种用于促进睑板腺上皮细胞和角膜上皮细胞增殖的药剂，以及提供治疗诸如睑板腺功能障碍或蒸发干眼症的眼部疾病的药剂。 提供了用于促进睑板腺上皮细胞或角膜上皮细胞的增殖的试剂，其含有PPAR±或'激动剂作为活性成分，以及用于治疗眼部疾病如睑板腺功能障碍或蒸发干燥的药剂 眼睛，含有PPAR±或'激动剂作为活性成分。
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