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1. 发明申请

WO2008004698A3 PYRAZOLO [1, 5-A] PYRIMIDINE COMPOUNDS AS CB1 RECEPTOR ANTAGONIST 审中-公开
标题翻译： PYRAZOLO [1,5-A]吡嗪类化合物作为CB1受体拮抗剂
公开(公告)号：WO2008004698A3
公开(公告)日：2008-03-20
申请号：PCT/JP2007063762
申请日：2007-07-04
申请人： MITSUBISHI TANABE PHARMA CORP , TANIMOTO KOICHI , OI MARIKO , TSUBOI YASUNORI , MORITANI YASUNORI
发明人： TANIMOTO KOICHI , OI MARIKO , TSUBOI YASUNORI , MORITANI YASUNORI
IPC分类号： C07D487/04 , A61K31/519 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention provides a pyrazolo[1,5-a]pyrimidine compound, having CB1 receptor-antagonizing activity, of the following formula [I]: in which R 1 and R 2 are the same or different and each an optionally substituted aryl group etc, R 0 is hydrogen atom, an alkyl group etc, E is a group of the formula: -C(=O)- or -SO 2 -, R is a group of the following formula [i], [ii] or [iii] etc: Ring A is (a) a C 3-8 cycloalkyl group optionally fused to a benzene ring or (b) a benzene ring, Q is a single bond or a methylene group, Ring B is a 4- to 7-membered aliphatic heterocyclic group, said cyclic group binding via its ring-carbon atom to the adjacent nitrogen atom, X is sulfur atom etc, R 3 is an alkyl group optionally substituted by an alkylthio group, R 4 is hydrogen atom, an alkyl group etc, one of R A and R B is an alkyl group etc, and the other is hydrogen atom, an alkyl group etc, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有下式[I]的具有CB1受体拮抗活性的吡唑并[1,5-a]嘧啶化合物：其中R 1和R 2， SUP>相同或不同，各自为任选取代的芳基等，R 0为氢原子，烷基等，E为下式基团-C（= O） - 或 -SO 2 - ，R是下式[i]，[ii]或[iii]等的基团：环A是（a）C 3-8 任选地与苯环稠合的环烷基或（b）苯环，Q是单键或亚甲基，环B是4-至7-元脂族杂环基，所述环状基团通过其环碳结合原子与相邻的氮原子，X是硫原子等，R 3是任选被烷硫基取代的烷基，R 4是氢原子，烷基等 R A和R B之一是烷基等，另一个是氢原子，烷基等或药物其可接受的盐。

2. 发明申请

WO2004064721A2 A PYRAZOLOPYRIMIDINE COMPOUND AND A PROCESS FOR PREPARING THE SAME 审中-公开
标题翻译：一种吡唑并嘧啶化合物及其制备方法
公开(公告)号：WO2004064721A2
公开(公告)日：2004-08-05
申请号：PCT/JP2004000617
申请日：2004-01-23
申请人： TANABE SEIYAKU CO , TAKAMURO IWAO , SEKINE YASUO , TSUBOI YASUNORI , NOGI KOUJI , TANIGUCHI HIROYUKI
发明人： TAKAMURO IWAO , SEKINE YASUO , TSUBOI YASUNORI , NOGI KOUJI , TANIGUCHI HIROYUKI
IPC分类号： A61K20060101 , A61K6/00 , A61K31/519 , A61P1/00 , A61P25/00 , C07D487/04 , C07D519/00 , A61K
CPC分类号： C07D487/04
摘要： The present invention provides a novel pyrazolopyrimidine compound of the formula [I]: wherein R' is (A) a substituted aryl group, (B) an optionally substituted nitrogen-containing aliphatic heteromonocyclic group, (C) a substituted cyclo-lower alkyl group, (D) an optionally substituted amino group, or (E) a substituted heteroaryl group, R is (a) an optionally substituted heteroaryl group or (b) an optionally substituted aryl group, Y is a single bond, a lower alkylene group or a lower alkenylene group, Z is a group of the formula: -CO-, -CH2-, -S02- or a group of the formula[II]: Q is a lower alkylene group, and q is an integer of 0 or 1 or a pharmaceutically acceptable sait thereof, which has a small conductance potassium channel (SK channel) blocking activity and is useful as a medicament and a process for preparing the same.
摘要翻译：本发明提供式[I]的新型吡唑并嘧啶化合物：其中R'为（A）取代芳基，（B）任选取代的含氮脂族杂单环基团，（C）取代的环低级烷基，（D）任选取代的氨基或（E）取代的杂芳基，R 2是（a）任选取代的杂芳基或（b）任选取代的芳基，Y是单键，低级亚烷基或低级亚烯基，Z是下式基团：-CO-，-CH 2 - ， - SO 2 - 或式[II]基团：Q是低级亚烷基，q是 0或1或其药学可接受的盐，其具有小电导钾通道（SK通道）阻断活性，并且可用作药物及其制备方法。

3. 发明公开

EP1772454A4 NITROGENOUS FUSED BICYCLIC COMPOUND 审中-公开
标题翻译：含氮稠合二环CONNECTION
公开(公告)号：EP1772454A4
公开(公告)日：2009-02-25
申请号：EP05766456
申请日：2005-07-22
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： TAKAMURO IWAO , KAWANAMI SABURO , TSUBOI YASUNORI , HIMIYAMA TOSHIYUKI , HASEGAWA YUKO , MOCHIDA HIDEKI , NOGI KOUJI
IPC分类号： C07D471/04 , A61K31/437 , A61K31/519 , A61P1/00 , A61P1/10 , A61P1/12 , A61P3/14 , A61P11/00 , A61P25/16 , A61P25/24 , A61P25/28 , A61P43/00 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： A novel nitrogenous fused bicyclic compound represented by the following general formula [I] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R0 represents hydrogen, halogeno, etc.; R1 represents a group represented by the formula (a) or (b) A represents a group represented by the formula (X) or (Y) D1, D2, and D3 each represents N or CH; R2 represents halogeno, optionally halogenated lower alkyl, etc.; R3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)

4. 发明专利

HK1069396A1 BENZOFURAN DERIVATIVE 未知
公开(公告)号：HK1069396A1
公开(公告)日：2005-05-20
申请号：HK05102768
申请日：2005-04-02
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： KAWAGUCHI TAKAYUKIA , AKATSUKA HIDENORI , IIJIMA TORU , TSUBOI YASUNORI , MITSUI TAKASHI , MURAKAMI JUN
IPC分类号： A61K20100101 , A61P20100101 , A61P7/02 , C07D20100101 , C07D307/85 , C07D405/04 , C07D405/12 , C07D405/14
摘要： The present invention provides a benzofuran derivative of the formula Ä1Ü: wherein x is a group of the formula: -N= or -CH=; Y is an optionally substituted amino group, an optionally substituted cycloalkyl group or an optionally substituted saturated heterocyclic group; A is a single bond, a carbon chain optionally having a double bond within or at the end(s) of the chain, or an oxygen atom; R is a hydrogen atom or a halogen atom; Ring B is an optionally substituted benzene ring; and R is a hydrogen atom, or a pharmaceutically acceptable salt thereof, which is useful as a medicament, especially as an activated blood coagulation factor X inhibitor.

5. 发明专利

JP2012020973A Medicinal composition 审中-公开
标题翻译：药物组合物
公开(公告)号：JP2012020973A
公开(公告)日：2012-02-02
申请号：JP2010160698
申请日：2010-07-15
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： TSUBOI YASUNORI , SHIRAI KIMIHIRO
IPC分类号： A61K31/519 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/08 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , C07D487/04
摘要： PROBLEM TO BE SOLVED: To provide a medicinal composition containing pyrrolo[2,3-d]pyrimidine compound having GPR119 receptor agonist activity or a pharmacologically acceptable salt thereof as an active ingredient.SOLUTION: The medicinal composition contains the compound represented by formula [I] [wherein, E is a group represented by the formula: -NH- or the like; ring A is a 6-membered aromatic ring which may contain one to two nitrogen atoms as hetero atoms (the aromatic ring may be substituted with a group represented by halogen, -CONRRor the like; and Rand Rare the same or different and each hydrogen, alkyl, hydroxyalkyl or the like); Ris acyl or the like; and Ris halogen or cyano], or the pharmacologically acceptable salt thereof as the active ingredient.
摘要翻译：待解决的问题：提供含有具有GPR119受体激动剂活性的吡咯并[2,3-d]嘧啶化合物或其药理学上可接受的盐作为有效成分的药物组合物。解决方案：药用组合物含有式[I]表示的化合物[其中，E为下式表示的基团：-NH-等; 环A是可以含有一至两个氮原子作为杂原子的六元芳环（芳环可以被卤素代表的基团取代，-CONR a R b 等; R a 和R b 是相同的或不同的，每个氢，烷基，羟基烷基等）; R 1是酰基等; 和R 2 是卤素或氰基]或其药理学上可接受的盐作为活性成分。版权所有（C）2012，JPO＆INPIT

6. 发明专利

MY144928A BENZOFURAN DERIVATIVES 未知
公开(公告)号：MY144928A
公开(公告)日：2011-11-30
申请号：MYPI20031170
申请日：2003-03-28
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： KAWAGUCHI TAKAYUKI , AKATSUKA HIDENORI , IIJIMA TORU , TSUBOI YASUNORI , MITSUI TAKASHI , MURAKAMI JUN
IPC分类号： A61P7/02 , C07D307/85 , C07D405/04 , C07D405/12 , C07D405/14
摘要： THE PRESENT INVENTION PROVIDES A BENZOFURAN DERIVATIVE OF THE FORMULA [1]; WHEREIN X IS A GROUP OF THE FORMULA: -N= OR -CH=; Y IS AN OPTIONALLY SUBSTITUTED AMINO GROUP, AN OPTIONALLY SUBSTITUTED CYCLOALKYL GROUP OR AN OPTIONALLY SUBSTITUTED SATURATED HETEROCYCLIC GROUP; A IS A SINGLE BOND, A CARBON CHAIN OPTIONALLY HAVING A DOUBLE BOND WITHIN OR AT THE END(s) OF THE CHAIN, OR AN OXYGEN ATOM; R1 IS A HYDROGEN ATOM OR A HALOGEN ATOM; RING B IS AN OPTIONALLY SUBSTITUTED BENZENE RING; AND R3 IS A HYDROGEN ATOM, OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, WHICH IS USEFUL AS A MEDICAMENT, ESPECIALLY AS AN ACTIVATED BLOOD COAGULATION FACTOR X INHIBITOR.

7. 发明专利

JP2013177319A Novel pyrrolo[2,3-d]pyrimidine compound 审中-公开
标题翻译：新型吡咯并[2,3-D]吡啶化合物
公开(公告)号：JP2013177319A
公开(公告)日：2013-09-09
申请号：JP2010160697
申请日：2010-07-15
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： TSUBOI YASUNORI , SHIRAI KIMIHIRO , HONJO TAKASHI
IPC分类号： C07D487/04 , A61K31/519 , A61K31/5377 , A61K31/54 , A61K31/5513 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D519/00
摘要： PROBLEM TO BE SOLVED: To provide a novel pyrrolo[2,3-d]pyrimidine compound which has GPR119 receptor agonistic activity and is useful as a drug.SOLUTION: There is provided a compound represented by formula [I] or a pharmacologically acceptable salt thereof. In formula [I], E is a group of the formula:-NH- or the like; ring A is a substituted benzene ring or the like; Ris a cyclic group or the like; and Ris a halogen.
摘要翻译：要解决的问题：提供具有GPR119受体激动活性并可用作药物的新型吡咯并[2,3-d]嘧啶化合物。溶液：提供由式[I]表示的化合物或药理学上可接受的盐其中。在式[I]中，E是下式的基团：-NH-等; 环A是取代的苯环等; R是环状基团等; 而R是卤素。

8. 发明专利

JP2013107855A Pharmaceutical composition 审中-公开
标题翻译：药物组合物
公开(公告)号：JP2013107855A
公开(公告)日：2013-06-06
申请号：JP2011254826
申请日：2011-11-22
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： INOUE SHINYA , TSUBOI YASUNORI , IKEDA YOSUKE , NAKAJIMA TATSUO , FUJIMOTO NOBUAKI , IWASAKI SATOSHI , FUKANO YASUSHI
IPC分类号： A61K31/517 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D239/94 , C07D401/04 , C07D409/14 , C07D413/14 , C07D417/14
摘要： PROBLEM TO BE SOLVED: To provide a pharmaceutical composition which includes a quinazoline compound having a GPR119 receptor agonist action or its pharmaceutically acceptable salt as an active ingredient.SOLUTION: The pharmaceutical composition includes a compound represented by general formula [I]: [in the formula, Rdenotes hydrogen or halogen; a ring A denotes 5 to 6-membered aryl ring (the aryl ring may include the same or different 1 to 4 pieces of hetero atoms selected from O, S and N); Rand Rdenote independently a halogen atom, a cyano group or the like; a ring B denotes a 6 to 7-membered aliphatic nitrogen-containing heterocyclic group; Rdenotes hydrogen or alkyl; Rdenotes hydrogen or a hydroxyl group; and Rdenotes a hydroxyl group, a cyano group or the like] or its pharmaceutically acceptable salt as an active ingredient.
摘要翻译：待解决的问题：提供包含具有GPR119受体激动剂作用的喹唑啉化合物或其药学上可接受的盐作为活性成分的药物组合物。解决方案：药物组合物包含通式[I]表示的化合物：[式中，R 1表示氢或卤素; 环A表示5至6元芳环（芳环可包括相同或不同的1至4个选自O，S和N的杂原子）; R A1 ，并且R A2 独立地表示卤素原子，氰基等; 环B表示6至7元脂族含氮杂环基; R B1 表示氢或烷基; R B2 表示氢或羟基; 并且R B3 表示羟基，氰基等]或其药学上可接受的盐作为活性成分。版权所有（C）2013，JPO＆INPIT

9. 发明专利

JP2013177315A Novel pyrrolo[2,3-d]pyrimidine compound 审中-公开
标题翻译：新型吡咯并[2,3-D]吡啶化合物
公开(公告)号：JP2013177315A
公开(公告)日：2013-09-09
申请号：JP2010117021
申请日：2010-05-21
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： TSUBOI YASUNORI , SHIRAI KIMIHIRO , HONJO TAKASHI
IPC分类号： C07D487/04 , A61K31/519 , A61K31/541 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a compound having GPR119 receptor agonistic activity.SOLUTION: There is provided a compound represented by formula [I] or a pharmacologically acceptable salt thereof. In formula [I], E is a group represented by the formula: -NH-; ring A is a group represented by formulas (i) or (ii); Rand Rare each hydrogen or the like; Ris alkylthio or the like; Ris hydrogen or the like; Ris alkyl or alkoxy; Ris acyl represented by the formula: ROCO- [wherein Ris alkyl or the like]; Ris a halogen or the like; and Ris hydroxy or the like.
摘要翻译：要解决的问题：提供具有GPR119受体激动活性的化合物。解决方案：提供由式[I]表示的化合物或其药理学上可接受的盐。在式[I]中，E是下式表示的基团：-NH-; 环A是由式（i）或（ii）表示的基团; 兰稀有每个氢等; Ris烷硫基等; Ris氢等; Ris烷基或烷氧基; 由下式表示的R 1酰基：ROCO- [其中Ris烷基等]; R是卤素等; 和Ris羟基等。

10. 发明专利

JP2008285464A PYRAZOLO[1,5-a]PYRIMIDINE COMPOUND 有权
标题翻译：吡咯并[1,5-a]吡啶化合物
公开(公告)号：JP2008285464A
公开(公告)日：2008-11-27
申请号：JP2007175769
申请日：2007-07-04
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： TANIMOTO KOICHI , OI MARIKO , TSUBOI YASUNORI , MORITANI YASUNORI
IPC分类号： C07D487/04 , A61K31/519 , A61P25/18 , A61P25/20 , A61P25/32 , A61P25/34 , A61P25/36 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a pyrazolo[1,5-a]pyrimidine compound having a CB1 receptor antagonistic activity. SOLUTION: This compound is expressed by general formula [I] [wherein, R 1 , R 2 are each an aryl which may have a substituent, or the like; R 0 is H, an alkyl or the like; E is a group expressed by formula: -C(=O)- or -SO 2 -; and R is a group expressed by formula [i], [ii], [iii], or the like]. COPYRIGHT: (C)2009,JPO&INPIT

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