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1. 发明申请

WO2006080477A1 NORVALINE DERIVATIVE AND METHOD FOR PREPARATION THEREOF 审中-公开
标题翻译： NORVALINE DERIVATIVE AND METHOD FOR COMPEPARTING THEREOF
公开(公告)号：WO2006080477A1
公开(公告)日：2006-08-03
申请号：PCT/JP2006/301394
申请日：2006-01-24
申请人： TANABE SEIYAKU CO., LTD. , HARADA, Naoyuki , HIKOTA, Masataka
发明人： HARADA, Naoyuki , HIKOTA, Masataka
IPC分类号： C07C237/22 , C07D295/12 , C07D295/14 , C07C323/62 , C07C323/63 , C07D211/14 , C07D211/58 , A61K31/165 , A61K31/44 , A61P25/00 , A61P13/00
CPC分类号： C07D295/13 , C07C237/22 , C07C323/60 , C07C323/62 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D207/09 , C07D211/58 , C07D295/155
摘要： Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2). [wherein X is -CH 2 -, -O-, -S- or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R 1 and R 2 are (i) each is hydrogen or lower alkyl; (ii) R 1 and R 2 are combined to form lower alkylene; or (iii) R 1 is hydrogen or lower alkyl and R 2 is combined with R 4 or R 6 to form lower alkylene; R 3 and R 4 are (i) each is hydrogen or lower alkyl; (ii) R 3 and R 4 are combined to form lower alkylene; or (iii) R 3 is hydrogen or lower alkyl and R 4 is combined with R 2 or R 6 to form lower alkylene; R is or -OR 7 ; R 5 and R 6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R 5 and R 6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R 5 is optionally substituted lower alkyl or hydrogen and R 6 is combined with R 2 or R 4 to form lower alkylene; R 7 is lower alkyl.
摘要翻译：式[I]的诺瓦宁衍生物或其药学上可接受的盐，其制备方法，含有该化合物的药物组合物和所述化合物用于抑制甘氨酸转运蛋白2型（GlyT2）的转运活性的用途。 [其中X是-CH 2 - ， - O - ， - S-或单键; Ar是任选取代的芳基或低级环烷基; n为0〜2; R 1和R 2均为（i）各自为氢或低级烷基; （ii）R 1和R 2结合形成低级亚烷基; 或（iii）R 1是氢或低级烷基，R 2与R 4或R 6相结合，形成低级亚烷基; R 3和R 4是（i）各自为氢或低级烷基; （ii）R 3和R 4结合形成低级亚烷基; 或（iii）R 3是氢或低级烷基，R 4与R 2或R 6相结合，形成低级亚烷基; R是或-OR 7; R 5和R 6是（i）各自为任选取代的低级烷基或氢; （ii）R 5和R 6结合形成脂族5至6元杂环基; 或（iii）R 5是任选取代的低级烷基或氢，R 6与R 2或R 4相结合， SUP>以形成低级亚烷基; R 7是低级烷基。

2. 发明申请

WO2010039124A1 BENZENESULFONIC ACID SALT COMPOUNDS 审中-公开
标题翻译：苯甲酸盐化合物
公开(公告)号：WO2010039124A1
公开(公告)日：2010-04-08
申请号：PCT/US2008/078270
申请日：2008-09-30
申请人： MITSUBISHI TANABE PHARMA CORPORATION , HIKOTA, Masataka , IIJIMA, Toru , MCCLURE, Michael, S.
发明人： HIKOTA, Masataka , IIJIMA, Toru , MCCLURE, Michael, S.
IPC分类号： C07D207/16 , A61K31/40 , A61P3/10
CPC分类号： C07D207/16
摘要： Besylate salts of /rans-4-({2-[(2S)-2-cyanopyrrolidinyl]-2-oxoethyl}amino)- Λ/,Λ/-dimethylcyclohexanecarboxamide are described as well as methods of using the same in the treatment of disorders characterized by hyperglycemia.
摘要翻译：描述了/反-4 - （{2 - [（2S）-2-氰基吡咯烷基] -2-氧代乙基}氨基）-β-，α'-二甲基环己烷甲酰胺的甲磺酸盐以及用于处理以高血糖症为特征的疾病

3. 发明申请

WO0230890A8 NITROGENOUS FIVE-MEMBERED RING COMPOUNDS 审中-公开
标题翻译：氮五元环化合物
公开(公告)号：WO0230890A8
公开(公告)日：2002-05-16
申请号：PCT/JP0108802
申请日：2001-10-05
申请人： TANABE SEIYAKU CO , YASUDA KOSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKOTA MASATAKA , MATSUMOTO TAKESHI , ARAKAWA KENJI
发明人： YASUDA KOSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKOTA MASATAKA , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61K31/401 , A61K31/4025 , A61K31/4035 , A61K31/4178 , A61K31/422 , A61K31/423 , A61K31/426 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/517 , A61K31/5377 , C07D403/14
CPC分类号： C07D207/404 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/5375 , C07D207/16 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Aliphatic nitrogenous five-membered ring compounds of the general formula [I], or pharmacologically acceptable salts thereof: [I] wherein A is CH2- or S-; B is CH or N; R is H, lower alkyl, or the like; X is a single bond, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, or the like; R is H or lower alkyl; Alk is lower alkylene; and R is an optionally substituted cyclic group, substituted amino, or the like, with the proviso that when X is CO-, B is N.
摘要翻译：通式[I]的脂族含氮五元环化合物或其药理学上可接受的盐：[I]其中A是CH2-或S-; B是CH或N; R 1是H，低级烷基等; X是单键，-CO-，-Alk-CO-，-COCH 2 - ，-Alk-O-，-O-CH 2 - ，-SO 2 - ， - S - ， - COO - ， - CON（R 3 ，-Alk-CON（R 3） - ， - CON（R 3）CH 2 - ， - NHCH 2 - 等; R 3是H或低级烷基; Alk是低级亚烷基; 并且R 2是任选取代的环状基团，取代的氨基等，条件是当X是CO-时，B是N.

4. 发明申请

WO0230891A8 ALIPHATIC NITROGENOUS FIVE-MEMBERED RING COMPOUNDS 审中-公开
标题翻译：偶氮硝基五元环化合物
公开(公告)号：WO0230891A8
公开(公告)日：2002-05-16
申请号：PCT/JP0108803
申请日：2001-10-05
申请人： TANABE SEIYAKU CO , YASUDA KOSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKOTA MASATAKA , MATSUMOTO TAKESHI , ARAKAWA KENJI
发明人： YASUDA KOSUKE , MORIMOTO HIROSHI , KAWANAMI SABURO , HIKOTA MASATAKA , MATSUMOTO TAKESHI , ARAKAWA KENJI
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61K31/401 , A61K31/4025 , A61K31/4035 , A61K31/41 , A61K31/4155 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4365 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , C07D277/06 , C07D277/42 , C07D277/82 , C07D405/14 , C07D409/12 , C07D495/04
CPC分类号： C07D207/404 , A61K31/40 , A61K31/425 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/5375 , C07D207/16 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04
摘要： Aliphatic nitrogenous five-membered ring compounds of the general formula [I] or pharmacologically acceptable salts thereof; a process for the preparation of the compounds or the salts; and pharmaceutical compositions containing the compounds or the salts as the active ingredient: [I] wherein A is CH2- or S-; R is hydrogen, lower alkyl, hydroxy-lower alkyl, or lower alkoxy-lower alkyl; X is N(R )-, -O-, or CO-; R is hydrogen or lower alkyl; and R is an optionally substituted cyclic group or optionally substituted amino.
摘要翻译：通式[I]的脂肪族含氮五元环化合物或其药理学上可接受的盐; 一种制备化合物或其盐的方法; 以及含有化合物或其盐作为活性成分的药物组合物：[I]其中A是CH 2 - 或S-; R 1是氢，低级烷基，羟基 - 低级烷基或低级烷氧基 - 低级烷基; X是N（R 3） - ， - O-或CO-; R 3是氢或低级烷基; 并且R 2是任选取代的环状基团或任选取代的氨基。

5. 发明申请

WO1995014668A1 2-OXOINDOLINE DERIVATIVE 审中-公开
标题翻译： 2-氧杂吲哚衍生物
公开(公告)号：WO1995014668A1
公开(公告)日：1995-06-01
申请号：PCT/JP1994001990
申请日：1994-11-25
申请人： TANABE SEIYAKU CO., LTD. , YAMADA, Koichiro , HIKOTA, Masataka , SHIKANO, Toshiro , NAGASAKI, Masaaki
发明人： TANABE SEIYAKU CO., LTD.
IPC分类号： C07D209/40
CPC分类号： C07D401/06 , C07D209/40 , C07D209/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/06 , C07D409/12 , C07D471/06
摘要： A 2-oxoindoline derivative represented by general formula (I) and a pharmacologically acceptable salt thereof, wherein ring A represents (un)substituted benzene; R represents hydrogen, cycloalkyl, aryl, nitrogenous heterocycle, oxygenous heterocycle, sulfurous heterocycle, heterocycle containing nitrogen and oxygen, heterocycle containing nitrogen and sulfur, lower alkoxy, carboxy, cyano, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, oxiranyl, or 2-(lower alkylthio)-1-hydroxyethyl; R represents aryl, a group represented by formula (a), (un)substituted nitrogenous heteromonocycle, (un)substituted nitrogenous heterobicycle, a group represented by formula (b), (wherein n represnts 1 or 2), oxygenous heterocycle, sulfurous heterocycle, heterocyle containing nitrogen and oxygen or heterocycle containing nitrogen and sulfur; R represents (un)substituted lower alkyl; Q represents a single bond or lower alkylene; and Y represents a single bond, lower alkylene or lower alkinylene.
摘要翻译：由通式（I）表示的2-氧代二氢吲哚衍生物及其药理学上可接受的盐，其中环A表示（未）取代的苯; R 1表示氢，环烷基，芳基，含氮杂环，含氧杂环，亚硫杂环，含氮和氧的杂环，含氮和硫的杂环，低级烷氧基，羧基，氰基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，环氧乙烷基，或2-（低级烷硫基）-1-羟乙基; R 2表示芳基，由式（a）表示的基团，（un）取代的含氮异单环，（un）取代的含氮异双环，由式（b）表示的基团，（其中n表示1或2），氧杂环，亚硫杂环，含有氮和氧的杂环，或含有氮和硫的杂环; R 3表示（un）取代的低级烷基; Q表示单键或低级亚烷基; Y表示单键，低级亚烷基或低级亚烷基。

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