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1.发明授权
公开(公告)号：EP2107052B1
公开(公告)日：2011-10-12
申请号：EP07860141.6
申请日：2007-12-26
发明人： MOGI, Hiroyuki , TAJIMA, Hisashi , MISHINA, Noriko , YAMAZAKI, Yusuke , YONEDA, Shinji , WATANABE, Katsuhiko , FUJIKAWA, Junko , YAMAMOTO, Minoru
IPC分类号： C07C275/28 , C07D207/09 , C07D211/26 , C07D213/40 , C07D213/75 , C07D215/38 , C07D235/32 , C07D261/14 , C07D277/46 , C07D277/82 , C07D295/12 , C07D307/79 , A61K31/17 , A61K31/197 , A61K31/245 , A61K31/277 , A61K31/36 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61P27/02 , C07D317/50 , C07D319/18 , C07D333/36 , C07D405/12
CPC分类号： C07D207/09 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C275/42 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D207/27 , C07D211/26 , C07D213/40 , C07D213/75 , C07D215/38 , C07D235/32 , C07D261/14 , C07D277/46 , C07D277/82 , C07D295/12 , C07D307/79 , C07D317/50 , C07D319/18 , C07D333/36 , C07D405/12
摘要： Disclosed are: a study on the synthesis of a novel N-(2-aminophenyl)benzamide derivative having an urea structure and represented by the general formula (1); and the utilization of the pharmacological activity of the derivative. A compound represented by the general formula (1) or a salt thereof has an activity of changing the morphology of a trabecular cell and therefore is effective for the prevention and/or treatment of a disease associated with an ocular tension. In the formula, R1 and R2 independently represents a hydrogen atom, a lower alkyl group or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group or the like; R4 and R5 independently represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; X represents a lower alkylene group or the like; Y represents a single bond, a lower alkylene group or the like; l and m independently represent a number of 0, 1, 2 or the like.
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公开(公告)号：EP2292611A1
公开(公告)日：2011-03-09
申请号：EP09750683.6
申请日：2009-05-25
发明人： MOGI, Hiroyuki , TAJIMA, Hisashi , MISHINA, Noriko , YAMAZAKI, Yusuke , YONEDA, Shinji , WATANABE, Katsuhiko , FUJIKAWA, Junko , YAMAMOTO, Minoru
IPC分类号： C07D333/36 , A61K31/381 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02
CPC分类号： C07D333/36 , C07D409/12
摘要： The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R 3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R 4 and R 5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W 1 -W 2 represents N-CH, CH-N, etc. and l and m are the same or different and represent 0, 1, etc.
摘要翻译： 本发明涉及具有尿素结构的新型噻吩并二胺衍生物的合成研究及其药物作用。 本发明提供由下述通式（1）表示的化合物或其盐。 在式（1）中，R 1和R 2相同或不同，表示氢原子，可以具有取代基的低级烷基等。R 3表示羟基，可以具有羟基的低级烷氧基 取代基，可以具有取代基的低级环烷氧基等。R 4和R 5相同或不同，表示卤素原子，低级烷基，羟基等。X表示可以具有的低级亚烷基 取代基等.Y表示可以具有取代基的单键或低级亚烷基等.W 1 -W 2表示N-CH，CH-N等，l和m相同或不同，表示 0，1等
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公开(公告)号：EP2292611B1
公开(公告)日：2012-07-25
申请号：EP09750683.6
申请日：2009-05-25
发明人： MOGI, Hiroyuki , TAJIMA, Hisashi , MISHINA, Noriko , YAMAZAKI, Yusuke , YONEDA, Shinji , WATANABE, Katsuhiko , FUJIKAWA, Junko , YAMAMOTO, Minoru
IPC分类号： C07D333/36 , A61K31/381 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/00 , A61P7/06 , A61P9/00 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06 , A61P19/02 , C07D409/12 , A61P27/00
CPC分类号： C07D333/36 , C07D409/12
摘要： The present invention is related to study on synthesis of a novel thiophenediamine derivative having a urea structure and finding of a pharmacological action of the derivative. Specifically, the present invention provides a compound represented by formula (1) or a salt thereof. In the formula, R
1 and R
2 may be the same or different and each represents a hydrogen atom, an optionally substituted lower alkyl group or the like; R
3 represents a hydroxy group, an optionally substituted lower alkoxy group, an optionally substituted lower cycloalkyloxy group or the like; R
4 and R
5 may be the same or different and each represents a halogen atom, a lower alkyl group, a hydroxy group or the like; X represents an optionally substituted lower alkylene group or the like; Y represents a single bond, an optionally substituted lower alkylene group or the like; W
1 -W
2 represents N-CH, CH-N or the like; and l and m may be the same or different and each represents 0, 1 or the like.-
4.发明公开OCULAR HYPOTENSIVE AGENT COMPRISING COMPOUND CAPABLE OF INHIBITING HISTONE DEACETYLASE AS ACTIVE INGREDIENT 审中-公开MITTEL GEGENOKULÄREHYPOTONIE MIT EINER VERBINDUNG ZUR HISTONDEACETYLASEHEMMUNG ALS WIRKSTOFF
公开(公告)号：EP2135620A1
公开(公告)日：2009-12-23
申请号：EP08739138.9
申请日：2008-03-28
发明人： YONEDA, Shinji , FUJISAWA, Koushi , WATANABE, Katsuhiko , FUJIKAWA, Junko , SHIMAZAKI, Atsushi , KIRIHARA, Tomoko , TAJIMA, Hisashi
IPC分类号： A61K45/00 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/5377 , A61P27/02 , A61P43/00 , C07D213/81 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D213/81 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/5377 , C07D207/333 , C07D211/32 , C07D401/04 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.
摘要翻译： 本发明的目的是找到具有HDAC抑制作用的化合物的新药理作用。 具有本发明的HDAC抑制作用的化合物对小梁细胞细胞的细胞形态学变化和/或眼压降低的作用具有优异的效果，因此可用作被认为是相关的疾病的预防和/或治疗剂 具有房水循环和/或眼内压，特别是作为青光眼或高眼压症的预防和/或治疗剂。
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5.发明公开NOVEL (2-AMINOPHENYL)PYRIDINECARBOXAMIDE DERIVATIVE HAVING UREA STRUCTURE 审中-公开神经元（2-氨基戊酸）吡啶羧酰胺衍生物麻醉剂HARNSTOFFSTRUKTUR
公开(公告)号：EP2133339A1
公开(公告)日：2009-12-16
申请号：EP08739136.3
申请日：2008-03-28
发明人： MOGI, Hiroyuki , TAJIMA, Hisashi , MISHINA, Noriko , YAMAZAKI, Yusuke , YONEDA, Shinji , WATANABE, Katsuhiko , FUJIKAWA, Junko , YAMAMOTO, Minoru
IPC分类号： C07D213/81 , A61K31/44 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/04 , A61P9/10 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/00 , A61P17/06
CPC分类号： C07D213/81 , C07D401/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/12
摘要： Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R 1 and R 2 represent a hydrogen atom, a lower alkyl group or the like; R 3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, -OCONR a R b , -NR c R d or the like; R 4 and R 5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; R a and R b represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; R c and R d represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W 1 -W 2 represents N-C or C-N; and l and m represent 0, 1, 2 or 3.
摘要翻译： 本发明的目的是研究具有新型尿素结构的新型吡啶羧酸（2-氨基苯基）酰胺衍生物的合成并找到该衍生物的药理作用。 本发明提供由式（1）表示的化合物或其盐。 在该式中，R 1和R 2表示氢原子，低级烷基等; R 3表示羟基，低级烷氧基，低级环烷氧基，芳氧基，羧基，低级烷氧基羰基，-OCONR a R b，-NR c R d等; R 4和R 5表示卤素原子，低级烷基，羟基，低级烷氧基等; R a和R b表示氢原子，低级烷基，低级环烷基，芳基，杂环基等; R c和R d表示氢原子，低级烷基，低级环烷基，芳基等; X表示低级亚烷基; Y表示单键，低级亚烷基; W 1 -W 2表示N-C或C-N; l和m表示0,1,2或3。
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6.发明公开
公开(公告)号：EP2107052A1
公开(公告)日：2009-10-07
申请号：EP07860141.6
申请日：2007-12-26
发明人： MOGI, Hiroyuki , TAJIMA, Hisashi , MISHINA, Noriko , YAMAZAKI, Yusuke , YONEDA, Shinji , WATANABE, Katsuhiko , FUJIKAWA, Junko , YAMAMOTO, Minoru
IPC分类号： C07C275/28 , A61K31/17 , A61K31/196 , A61K31/197 , A61K31/216 , A61K31/245 , A61K31/277 , A61K31/36 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/4409 , A61K31/443 , A61K31/4433 , A61K31/4465 , A61K31/495 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61P27/02 , A61P43/00
CPC分类号： C07D207/09 , C07C275/24 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/40 , C07C275/42 , C07C2601/08 , C07C2602/08 , C07C2602/10 , C07D207/27 , C07D211/26 , C07D213/40 , C07D213/75 , C07D215/38 , C07D235/32 , C07D261/14 , C07D277/46 , C07D277/82 , C07D295/12 , C07D307/79 , C07D317/50 , C07D319/18 , C07D333/36 , C07D405/12
摘要： The present invention relates to a study on the sy nthesis of a novel N-(2-aminophenyl)benzamide derivativ e having an urea structure and represented by the genera l formula (1); and the utilization of a pharmacological effect of the derivative. A compound represented by the general formula (1) or a salt thereof has an effect of cellular morphological change on trabecular meshwork ce lls and is effective in the prevention and/or treatment of a disease considered to be related to intraocular pre ssure. In the formula, R 1 and R 2 represent a hydrogen a tom, a lower alkyl group, or the like; R 3 represents a h ydroxy group, a lower alkoxy group, a lower cycloalkylo xy group, an aryloxy group, or the like; R 4 and R 5 repre sent a halogen atom, a lower alkyl group, a hydroxy grou p, a lower alkoxy group, or the like; X represents a low er alkylene group or the like; Y represents a single bon d, a lower alkylene group, or the like; l and m represen t 0, 1, 2, or the like.
摘要翻译： 本发明涉及具有脲结构并由式（1）表示的新型N-（2-氨基苯基）苯甲酰胺衍生物的合成的研究; 并利用衍生物的药理作用。 由通式（1）表示的化合物或其盐具有细胞形态改变对小梁网状细胞的作用，并且在预防和/或治疗被认为与眼内伤口有关的疾病方面是有效的。 式中，R 1和R 2表示氢或低级烷基等; R3表示羟基，低级烷氧基，低级环烷基氧基，芳氧基等; R4和R5表示卤原子，低级烷基，羟基，低级烷氧基等; X代表较低的亚烷基等; Y表示单键，低级亚烷基等; l和m表示0,1,2等。
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