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1. 发明授权

EP2009012B1 NOVEL COMPOUND HAVING HETEROCYCLIC RING 有权
标题翻译： WITH杂环新连接
公开(公告)号：EP2009012B1
公开(公告)日：2014-06-25
申请号：EP07740496.0
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi Co., Ltd.
发明人： SUZUKI, Hideyuki , HIZATATE, Shoji , UTSUNOMIYA, Iwao , SHUDO, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55

2. 发明公开

EP2700645A1 SILICON-CONTAINING CARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：碳化硅碳化硅
公开(公告)号：EP2700645A1
公开(公告)日：2014-02-26
申请号：EP12774607.1
申请日：2012-04-19
申请人： Research Foundation Itsuu Laboratory , Kemphys Ltd.
发明人： MURATAKE, Hideaki , ITO, Ai , SHUDO, Koichi
IPC分类号： C07F7/10
CPC分类号： C07F7/0818 , C07F7/0816 , C07F7/082
摘要： A compound represented by the formula (I) [R 1 to R 3 represent an alkyl group, an alkenyl group, and the like; n represents 0 or 1; R 4 represents an amino group or - (CX 2 ) m -COOH (m represents 0 to 3, and X represents hydrogen atom); R 5 represents-(CY 2 ) p -COOR 6 (p represents an 0 to 3, Y represents hydrogen atom, and R 6 represents hydrogen atom or an alkyl group)], or a salt thereof.
摘要翻译：由式（I）表示的化合物[R 1至R 3表示烷基，烯基等] n表示0或1; R 4表示氨基或 - （CX 2）m -COOH（m表示0〜3，X表示氢原子）。 R 5表示 - （CY 2）p -COOR 6（p表示0〜3，Y表示氢原子，R 6表示氢原子或烷基）]或其盐。

3. 发明公开

EP2669283A1 Oxazolidinone derivative having 7-membered hetero ring 审中-公开
标题翻译：恶唑烷酮衍生物7-gliedrigem Heteroring
公开(公告)号：EP2669283A1
公开(公告)日：2013-12-04
申请号：EP13178030.6
申请日：2008-10-01
申请人： Shionogi & Co., Ltd. , Research Foundation Itsuu Laboratory
发明人： Suzuki, Hideyuki , Utsunomiya, Iwao , Shudo, Koichi , Iwaki, Tsutomu , Yasukata, Tatsuro
IPC分类号： C07D413/10 , C07D413/14 , C07D471/14 , C07D487/04 , A61K31/553 , A61P31/04
CPC分类号： C07D413/14 , C07D271/02 , C07D413/10 , C07D471/14 , C07D487/04 , Y02P20/55
摘要： A compound of the formula:

or a pharmaceutically acceptable salt or solvate thereof wherein
Y 1 is NP 2 or O;
P 1 and P 2 are independently hydrogen, or a substituent selected from Substituent Group S1 and amino protecting group;
R 11 is hydrogen, or a substituent selected from Substituent Group S1 and amino protecting group, with the proviso that R 11 is not -CO(CH 2 ) 3 -CO 2 H, -Ph, -CH 2 Ph, and -(CH 2 ) 3 CH(4-F-Ph) 2 wherein Ph is phenyl;
Substituent Group S1 consists of optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted cycloalkyl, optionally substituted formyl, optionally substituted (lower alkyl) carbonyl, optionally substituted cycloalkylcarbonyl, optionally substituted (lower alkyl) oxycarbonyl, optionally substituted (lower alkyl) oxythiocarbonyl, optionally substituted arylcarbonyl, optionally substituted aryloxycarbonyl, optionally substituted heterocyclecarbonyl, optionally substituted heterocycleoxycarbonyl, optionally substituted carbamoyl, optionally substituted carbamoylcarbonyl, optionally substituted thiocarbamoyl, optionally substituted (lower alkyl) thiocarbonyl, optionally substituted cycloalkylthiocarbonyl, optionally substituted arylthiocarbonyl, optionally substituted heterocyclic thiocarbonyl, optionally substituted (lower alkyl) sulfonyl, optionally substituted phenylsulfonyl, optionally substituted aromatic heterocyclesulfonyl, optionally substituted aminosulfonyl, optionally substituted aryl, optionally substituted heterocyclic group, cyano, optionally substituted thioformyl, optionally substituted (lower alkenyl) carbonyl, and optionally substituted heterocycleoxycarbonyl;
with the proviso that the compound is not the following compound:

wherein Ph is phenyl.
摘要翻译：下式的化合物或其药学上可接受的盐或溶剂化物，其中Y 1是NP 2或O; P 1和P 2独立地为氢，或选自取代基组S1和氨基保护基的取代基; R 11是氢或选自取代基组S1和氨基保护基的取代基，条件是R 11不是-CO（CH 2）3 -CO 2 H，-Ph，-CH 2 Ph和 - （CH 2）3 CH（4-F-Ph）2，其中Ph是苯基; 取代基组S1由任选取代的低级烷基，任选取代的低级烯基，任选取代的环烷基，任选取代的甲酰基，任选取代的（低级烷基）羰基，任选取代的环烷基羰基，任选取代的（低级烷基）氧羰基，任选取代的（低级烷基）氧硫基羰基任选取代的芳基羰基，任选取代的芳基羰基，任选取代的杂芳基羰基，任选取代的杂环羰基，任选取代的氨基甲酰基，任选取代的氨基甲酰基，任选取代的氨基甲酰基，任选取代的硫代氨基甲酰基，任选取代的（低级烷基）硫代羰基，任选取代的环烷硫基羰基，任选取代的芳硫基羰基，任选取代的杂环硫代羰基，任选取代的（低级烷基）磺酰基，任选取代的苯磺酰基，任选取代的芳族杂环磺酰基，任选取代的氨基磺酰基，任选取代的芳基，任选取代的杂环基，氰基，任选取代的硫代甲酰基，任选取代的（低级烯基）羰基和任选取代的杂环氧羰基; 条件是该化合物不是以下化合物：其中Ph是苯基。

4. 发明授权

EP2189443B1 TRICYCLIC AMIDE COMPOUND 有权
标题翻译：三环酰胺
公开(公告)号：EP2189443B1
公开(公告)日：2013-10-23
申请号：EP08792457.7
申请日：2008-08-14
申请人： Research Foundation Itsuu Laboratory
发明人： AMANO, Yohei , NOGUCHI, Masayuki , SHUDO, Koichi
IPC分类号： C07C233/65 , A61K31/381 , A61K31/44 , A61K31/455 , A61P35/00 , A61P43/00 , C07C233/81 , C07C311/21 , C07D213/79 , C07D213/81 , C07D213/82
CPC分类号： C07C233/81 , C07C233/65 , C07C311/21 , C07C2603/28 , C07C2603/34 , C07D213/79 , C07D213/81 , C07D213/82 , C07D333/38 , C07D333/40

5. 发明公开

EP1798227A1 SEROTONIN 5-HT3 RECEPTOR AGONIST 审中-公开
标题翻译： AGONIST DES SEROTONIN-5-HT3-REZEPTORS
公开(公告)号：EP1798227A1
公开(公告)日：2007-06-20
申请号：EP05778615.4
申请日：2005-09-08
申请人： Research Foundation Itsuu Laboratory
发明人： JIKYO, Tamaki , SHUDO, Koichi
IPC分类号： C07D295/20 , C07D243/08 , A61K31/495 , A61K31/551 , A61K31/395 , A61P1/08 , A61P1/10 , A61P1/12 , A61P43/00
CPC分类号： C07D295/215 , A61K31/395 , A61K31/495 , A61K31/551 , C07D243/08
摘要： A serotonin 5-HT3 receptor agonist containing a compound represented by the general formula (1) [R 1 , R 3 and R 5 represent hydrogen atom, a lower alkyl group, a lower alkenyl group, a halogen atom, hydroxyl group, amino group, a lower alkoxy group, carboxyl group, carbamoyl group, or nitro group, R 2 and R 4 represent a halogen atom, hydroxyl group, or amino group, R 6 represents hydrogen atom, a lower alkyl group, or a lower alkenyl group, R 7 represents hydrogen atom, a lower alkyl group, a lower alkenyl group, or an aralkyl group, and m and n are integers of 1 to 3] or a physiologically acceptable salt thereof as an active ingredient and having both a serotonin 5-HT3 receptor antagonistic action and a serotonin 5-HT3 receptor activating action.
摘要翻译：含有通式（1）表示的化合物的5-羟色胺5-HT 3受体激动剂[R 1，R 3和R 5表示氢原子，低级烷基，低级烯基，卤素原子，羟基，氨基低级烷氧基，羧基，氨基甲酰基或硝基，R 2和R 4表示卤素原子，羟基或氨基，R 6表示氢原子，低级烷基或低级烯基， R 7表示氢原子，低级烷基，低级烯基或芳烷基，m和n为1〜3的整数]或其生理学上可接受的盐作为活性成分，同时具有5-羟色胺5-HT 3 受体拮抗作用和5-羟色胺5-HT 3受体激活作用。

6. 发明公开

EP1357104A1 TROPOLONE DERIVATIVE 审中-公开
标题翻译： TROPOLONDERIVAT
公开(公告)号：EP1357104A1
公开(公告)日：2003-10-29
申请号：EP01272512.3
申请日：2001-12-18
申请人： Research Foundation Itsuu Laboratory
发明人： KAGECHIKA, Hiroyuki
IPC分类号： C07C49/747
CPC分类号： C07D333/74 , C07C17/266 , C07C45/62 , C07C45/63 , C07C45/64 , C07C45/65 , C07C45/673 , C07C45/68 , C07C45/71 , C07C49/683 , C07C49/747 , C07C49/753 , C07C225/20 , C07C225/22 , C07C233/32 , C07C233/76 , C07C245/10 , C07C275/28 , C07C275/38 , C07C311/20 , C07C2601/18 , C07C2602/10 , C07D307/46 , C07D333/22 , C07C25/22 , C07C49/717
摘要： Tropolone derivatives represented by the formula (I), which have retinoid actions and are useful as active ingredients of medicaments [R 1 to R 4 represent hydrogen atom, an alkyl group, or an alkoxyl group; the ring represented by Ar represents an aryl ring or a heteroaryl ring; X represents a single bond, -N=N-,-CON(R 5 )-, -(C=C) n CON(R 6 )-, -N(R 7 )CON(R 8 )-, -SO 2 N(R 9 )-, -N(R 10 )- (R 5 to R 9 represent hydrogen atom or an alkyl group, n represents 1 to 3, R 10 represents hydrogen atom, an alkyl group, or an acyl group), an alkylene group, an aryldiyl group, or a heterocyclic diyl group; Y represents hydrogen atom, -OR 11 (R 11 represents hydrogen atom, an alkyl group, or an acyl group), -NHR 12 (R 12 represents hydrogen atom, an alkyl group, an acyl group, or amino group), or a halogen atom.
摘要翻译：具有类视黄醇作用并且可用作药物活性成分的式（I）的托洛酮衍生物代表氢原子，烷基或烷氧基; 由Ar表示的环表示芳基环或杂芳基环; X表示单键-N = N - ， - CON（R 5） - ， - （C = C）nCON（R 6） - ， - N（R 7）CON（R 8） - ） - ， - SO 2 N（R 9） - ， - N（R 10） - （R 5至R 9）表示氢原子或烷基，n表示1至3，R 10 >表示氢原子，烷基或酰基），亚烷基，芳基二基或杂环二基; Y表示氢原子，-OR 11（R 11表示氢原子，烷基或酰基），-NHR 12（R 12表示氢原子，烷基，酰基），或氨基）或卤素原子。

7. 发明授权

EP2181994B1 Antimicrobial compounds 有权
标题翻译：抗微生物化合物
公开(公告)号：EP2181994B1
公开(公告)日：2014-05-28
申请号：EP10001133.7
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi & Co., Ltd.
发明人： Suzuki, Hideyuki , Hizatate, Shoji , Utsunomiya, Iwao , Shudo, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55

8. 发明公开

EP2233484A3 Oxazolidinone derivatives having a 7-membered heterocyclic ring 审中-公开
标题翻译：具有7元杂环的恶唑烷酮衍生物
公开(公告)号：EP2233484A3
公开(公告)日：2012-04-04
申请号：EP10005451.9
申请日：2008-10-01
申请人： Research Foundation Itsuu Laboratory , Shionogi & Co., Ltd.
发明人： Suzuki, Hideyuki , Utsunomiya, Iwao , Shudo, Koichi , Iwaki, Tsutomu , Yasukata, Tatsuro
IPC分类号： C07D413/10 , C07D413/14 , C07D471/14 , C07D487/04 , A61K31/553 , A61P31/04
CPC分类号： C07D413/14 , C07D271/02 , C07D413/10 , C07D471/14 , C07D487/04 , Y02P20/55
摘要： The present invention provides a compound of the formula:

or a pharmaceutically acceptable salt or solvate thereof
wherein
Y 1 is NR a , O, S, SO or SO 2 ;
Ring B is optionally substituted carbocycle or optionally substituted heterocycle.

9. 发明公开

EP2181994A1 Antimicrobial compounds 有权
标题翻译： Antimikrobielle Verbindungen
公开(公告)号：EP2181994A1
公开(公告)日：2010-05-05
申请号：EP10001133.7
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi&Co., Ltd.
发明人： Suzuki, Hideyuki , Hizatate, Shoji , Utsunomiya, Iwao , Shudo, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55
摘要： A compound of the formula:

or a pharmaceutically acceptable salt or solvate thereof,
wherein
Y 1 is NP 2 or O;
P 1 and P 2 are independently hydrogen, acyl group or an amino protecting group;
R 11 is hydrogen, acyl group or an amino protecting group, provided that -CO(CH 2 ) 3 -CO 2 H, -Ph and -CH 2 Ph (Ph: phenyl) are excluded.
摘要翻译：下式的化合物或其药学上可接受的盐或溶剂化物，其中Y 1是NP 2或O; P 1和P 2独立地为氢，酰基或氨基保护基; R 11为氢，酰基或氨基保护基，条件是排除-CO（CH 2）3 -CO 2 H，-Ph和-CH 2 Ph（Ph：苯基）。

10. 发明公开

EP2181993A1 Antimicrobial oxazolidinone derivatives 审中-公开
标题翻译：抗恶唑烷恶唑烷酮
公开(公告)号：EP2181993A1
公开(公告)日：2010-05-05
申请号：EP10001092.5
申请日：2007-03-30
申请人： Research Foundation Itsuu Laboratory , Shionogi&Co., Ltd.
发明人： Suzuki, Hideyuki , Hizatate, Shoji , Utsunomiya, Iwao , Shudo, Koichi
IPC分类号： C07D413/10 , A61K31/55 , A61K31/553 , A61P31/04 , C07D413/14 , C07D417/14 , C07D471/14
CPC分类号： C07D273/06 , C07D255/02 , C07D413/10 , C07D413/14 , C07D417/14 , C07D471/14 , Y02P20/55
摘要： A compound of the formula:

or a pharmaceutically acceptable salt or solvate thereof, wherein
Ring A is
(A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms;
(A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or
(A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom, wherein said monocyclic hetero ring is optionally substituted, and said monocyclic hetero ring is optionally condensed with another ring,

X 1 is a single bond, or a hetero atom-containing group selected from the group consisting of -O-, -S-, -NR 2 -, -CO-, -CS-, -CONR 3 -, -NR 4 CO-, -SO 2 NR 5 -, and -NR 6 SO 2 -, wherein R 2 , R 3 , R 4 , R 5 and R 6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said hetero atom-containing group;
Ring B is optionally substituted carbocycle or optionally substituted heterocycle;
R 1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent.
摘要翻译：下式的化合物或其药学上可接受的盐或溶剂化物，其中环A是含有至少三个N原子的至少7元单环杂环的（A-1）（A-2）至少含有至少两个N原子和至少一个O原子的6元单环杂环; 或（A-3）至少含有至少两个N原子和至少一个S原子的7元单环杂环，其中所述单环杂环任选被取代，并且所述单环杂环任选地与另一个环X 1缩合或选自-O - ， - S - ， - NR 2 - ， - CO - ， - CS - ， - CONR 3 - ， - NR 4 CO - ， - -SO 2 NR 5 - 和-NR 6 SO 2 - ，其中R 2，R 3，R 4，R 5和R 6独立地为氢或低级烷基，或低级亚烷基或低级亚烯基，各自任意地被所述杂原子包含组; 环B是任选取代的碳环或任选取代的杂环; R 1是氢，或者可以在恶唑烷酮抗微生物剂中结合恶唑烷酮环的5-位的有机残基。

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