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1. 发明申请

WO2010043682A2 PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT 审中-公开
标题翻译：制备作为SGLT抑制剂的化合物的方法
公开(公告)号：WO2010043682A2
公开(公告)日：2010-04-22
申请号：PCT/EP2009063503
申请日：2009-10-15
申请人： JANSSEN PHARMACEUTICA NV , MITSUBISHI TANABE PHARMA CORP , FILLIERS WALTER FERDINAND MARI , BROECKX RUDY LAURENT MARIA , NIESTE PATRICK HUBERT J , HATSUDA MASANORI , YOSHINAGA MASAHIKO , YADA MITSUHIRO
发明人： FILLIERS WALTER FERDINAND MARIA , BROECKX RUDY LAURENT MARIA , NIESTE PATRICK HUBERT J , HATSUDA MASANORI , YOSHINAGA MASAHIKO , YADA MITSUHIRO
CPC分类号： C07D333/12 , C07D409/10 , C07H7/04 , C07H13/04
摘要： The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
摘要翻译：本发明涉及一种制备具有抑制活性的化合物的新方法，所述化合物对存在于肠或肾中的钠依赖性葡萄糖转运蛋白（SGLT）具有抑制活性。

2. 发明公开

EP1640373A4 PROCESS FOR PRODUCING 3-ACYLAMINOBENZOFURAN-2-CARBOXYLIC ACID DERIVATIVE 审中-公开
标题翻译：用于生产3- ACYLAMINOBENZOFURAN -2-羧酸衍生物
公开(公告)号：EP1640373A4
公开(公告)日：2008-07-02
申请号：EP04746957
申请日：2004-06-29
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： SEKI MASAHIKO , YOSHIDA SHIN-ICHI , YAGI NOBUHIRO , HATSUDA MASANORI , KIMURA MAYUMI , KONDO KAZUHIKO
IPC分类号： C07D405/14 , C07C209/04 , C07C211/45 , C07C227/16 , C07C229/48 , C07C253/14 , C07C255/49 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/81 , C07D213/85 , C07D265/32 , C07D307/85 , C07D333/62 , C07D333/68 , C07D405/12 , C07D413/14
CPC分类号： C07D405/14 , C07C253/14 , C07D207/27 , C07D211/76 , C07D213/57 , C07D213/85 , C07D265/32 , C07D295/192 , C07D333/62 , C07D333/68 , C07D405/12 , C07C255/50 , C07C255/51 , C07C255/53 , C07C255/54 , C07C255/56 , C07C255/57
摘要： An excellent process for efficiently producing a benzofuran derivative or pyridofuran derivative or a pharmacologically acceptable salt of either, the derivatives being represented by the general formula [I]: [I] (wherein X represents -N= or -CH=; R1 represents hydrogen, halogeno, lower alkyl, lower alkoxy, cyano, or amino optionally substituted by lower alkyl; ring A represents a nitrogenous heterocyclic group; ring B represents an optionally substituted benzene ring or pyridine ring; and R3 represents hydrogen or lower alkyl). The derivatives are useful as an inhibitor against an activated blood coagulation factor X.

3. 发明公开

EP2963048A4 METHOD FOR PRODUCING -HALO-TETRAACYL GLUCOSE 有权
标题翻译： VERFAHREN ZUR HERSTELLUNG VON HALO-TETRAACYL-GLUCOSE
公开(公告)号：EP2963048A4
公开(公告)日：2017-03-01
申请号：EP14756953
申请日：2014-02-25
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： UEDA KEITA , HATSUDA MASANORI , HYODO ISAO , TANIMOTO KOUICHI
IPC分类号： C07H5/02 , A61K31/381 , A61P3/10 , C07B61/00 , C07D409/10 , C07H13/02 , C07H13/04 , C07H13/08
CPC分类号： C07H13/08 , A61K31/381 , C07D409/10 , C07H5/02 , C07H7/04 , C07H13/04
摘要： There is provided an efficient and excellent preparation method of an ±-halo-tetraacyl-glucose which is suitable for industrial preparation, which comprises reacting D-glucose or lower alkyl D-glucoside with a reactive derivative of a carboxylic acid and a metal halide to prepare the ±-halo-tetraacyl-glucose represented by the formula (III): wherein R represents an optionally substituted lower alkyl group or an optionally substituted aryl group, and X represents a halogen atom, in one step, and the resulting ±-halo-tetraacyl-glucose (III) can be converted into a compound of the formula (I) or a salt thereof by subjecting to a conventional method.
摘要翻译：提供了适用于工业制备的±卤代四酰基 - 葡萄糖的有效而优异的制备方法，其包括将D-葡萄糖或低级烷基D-葡萄糖苷与羧酸和金属卤化物的活性衍生物反应制备由式（III）表示的±卤代四酰基葡萄糖：其中R表示任选取代的低级烷基或任选取代的芳基，X表示卤素原子，一步反应，得到的± - 四酰基 - 葡萄糖（III）可以通过常规方法转化为式（I）化合物或其盐。

4. 发明公开

EP2749558A4 METHOD FOR PRODUCING OPTICALLY ACTIVE NAPHTHALENE COMPOUND 审中-公开
标题翻译：方法制备光学活性的萘
公开(公告)号：EP2749558A4
公开(公告)日：2014-11-19
申请号：EP12826351
申请日：2012-08-24
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： MATSUYAMA KOJI , HATSUDA MASANORI , YOSHINAGA MASAHIKO , YADA MITSUHIRO , TANIMOTO KOICHI
IPC分类号： C07D401/04 , A61K31/4709 , A61P17/00 , A61P17/02 , A61P17/04 , A61P29/00 , A61P43/00 , C07B61/00
CPC分类号： C07D401/04 , C07B53/00 , C07C25/06 , C07C255/03

5. 发明专利

JP2013216579A Method for producing trisubstituted indazoleacrylamide derivative 审中-公开
标题翻译：用于生产三唑丙基丙烯酰胺衍生物的方法
公开(公告)号：JP2013216579A
公开(公告)日：2013-10-24
申请号：JP2010153736
申请日：2010-07-06
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： UTSUGI MASAYUKI , HATSUDA MASANORI , MIYAKE TSUTOMU
IPC分类号： C07D231/56 , C07D471/04
CPC分类号： C07D231/56 , C07D471/04 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide an industrially advantageous method for producing an indazoleacrylic acid derivative useful as an IKur blocking agent.SOLUTION: In a method for producing a compound (4a), a compound (1) is reacted with a compound (2) or a compound (3) in the presence of a base, and then treated with an organic base. (In the formulae, ring X shows benzene or pyridine; Rshows hydrogen or alkyl; Rshows halogen or alkyl; Rshows a protecting group; Rand Rmay be the same or different, and each shows hydrogen or halogen; Rshows optionally substituted alkyl; Rshows hydrogen or optionally substituted alkyl; R shows optionally substituted aryl or optionally substituted alkyl; and Ar shows optionally substituted aryl).
摘要翻译：要解决的问题：提供一种工业上有利的制备用作IKur封端剂的吲唑丙烯酸衍生物的方法。溶液：化合物（4a）的制备方法使化合物（1）与化合物（2）反应，或化合物（3）在碱存在下反应，然后用有机碱处理。（式中，X表示苯或吡啶; Rs表示氢或烷基; R表示卤素或烷基; R表示保护基;兰德Rmay相同或不同，各自表示氢或卤素; R表示任选取代的烷基; R表示氢或任选取代的烷基; R表示任选取代的芳基或任选取代的烷基; Ar表示任选取代的芳基）。

6. 发明专利

JP2014167030A Process for preparation of compounds useful as inhibitors of sglt 有权
标题翻译：制备作为SGLT抑制剂的化合物的方法
公开(公告)号：JP2014167030A
公开(公告)日：2014-09-11
申请号：JP2014124295
申请日：2014-06-17
申请人： Janssen Pharmaceutica Nv , ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプJanssen Pharmaceutica Naamloze Vennootschap , Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： WALTER FERDINAND MARIA FILLIERS , RUDY LAURENT MARIA BROECKX , PATRICK HUBERT J NIESTE , HATSUDA MASANORI , YOSHINAGA MASAHIKO , YADA MITSUHIRO , CHRISTOPHER TELEHA
IPC分类号： C07D333/12
CPC分类号： C07D333/12 , C07D409/10 , C07H7/04 , C07H13/04
摘要： PROBLEM TO BE SOLVED: To provide a process of producing precursors for effectively producing compounds having inhibitory activity against sodium-glucose cotransporter (SGLT) present in the intestine or kidney, e.g., 1-glucopyranosyl-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene.SOLUTION: A process comprises a procedure of producing a compound (XVIII-S) according to the specified reaction scheme. The procedure comprises reacting a compound of the specified formula (XV-S) with a compound of the specified formula (XVII-S), in an organic solvent in the presence of a Ni or Pd catalyst, to produce a corresponding compound of the specified formula (XVIII-S).
摘要翻译：要解决的问题：提供一种制备用于有效生产对肠或肾中存在的钠 - 葡萄糖转运蛋白（SGLT）具有抑制活性的化合物的前体的方法，例如1-吡喃葡萄糖基-4-甲基-3- [5-（ 4-氟苯基）-2-噻吩甲基]苯。方法：一种方法包括根据规定的反应方案制备化合物（XVIII-S）的方法。该方法包括在有机溶剂中，在Ni或Pd催化剂的存在下，使规定式（XV-S）的化合物与规定的式（XVII-S）化合物反应，生成相应的化合物式（XVIII-S）。

7. 发明专利

JP2012197291A Method for producing n-(n'-substituted glycyl)-2-cyanopyrrolidine derivative 有权
标题翻译：生产N-（N'-取代的甘氨酸）-2-氰基吡咯烷衍生物的方法
公开(公告)号：JP2012197291A
公开(公告)日：2012-10-18
申请号：JP2012126278
申请日：2012-06-01
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： KURODA TORU , HATSUDA MASANORI , TOSHIKAWA SHOTA
IPC分类号： C07D207/16 , C07B61/00
CPC分类号： C07D207/16 , Y02P20/55
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a high-quality N-(N'-substituted glycyl)-2-cyanopyrrolidine derivative by reducing formation of byproducts.SOLUTION: A substitution method for amino group protection includes (i) obtaining a primary or secondary amine compound by reacting an amine compound protected by a first amino group-protecting group except a benzyl group or a substituted benzyl group in the presence of a palladium catalyst to remove the first amino group-protecting group, (ii) successively reacting the primary or secondary amine compound with benzaldehyde or a substituted benzaldehyde in a nitrogen atmosphere in the same reaction system, and (iii) after replacing the reaction system with hydrogen, subjecting the resultant product to a reduction reaction in the presence of the palladium catalyst same as (i) above to afford the amine compound protected with a second amino group-protecting group selected from the benzyl group and the substituted benzyl group.
摘要翻译：待解决的问题：提供通过减少副产物的形成来生产高品质的N-（N'取代的甘氨酰基）-2-氰基吡咯烷衍生物的方法。解决方案：用于氨基保护的取代方法包括（i）通过使由除了苄基或取代的苄基之外的第一氨基保护基保护的胺化合物在存在下进行反应获得伯或仲胺化合物用于除去第一氨基保护基团的钯催化剂，（ii）在相同的反应体系中，在氮气气氛中使伯胺或仲胺化合物与苯甲醛或取代的苯甲醛相继反应，和（iii）在将反应体系用氢气，在与上述（i）相同的钯催化剂存在下使所得产物进行还原反应，得到用选自苄基和取代苄基的第二氨基保护基保护的胺化合物。版权所有（C）2013，JPO＆INPIT

8. 发明专利

JP2008056690A Method for producing grignard reagent 有权
标题翻译：生产格氏试剂的方法
公开(公告)号：JP2008056690A
公开(公告)日：2008-03-13
申请号：JP2007269951
申请日：2007-10-17
申请人： Mitsubishi Tanabe Pharma Corp , 田辺三菱製薬株式会社
发明人： SEKI MASAHIKO , SHIMIZU TOSHIAKI , YOSHIDA SHINICHI , HATSUDA MASANORI
IPC分类号： C07F3/02 , C07F3/06
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a Grignard reagent more efficient than the conventional method. SOLUTION: The method for producing the compound represented by general formula (IX): R-X-Y (wherein, X is zinc or magnesium; and Y is iodine, bromine or chlorine) includes reacting a compound represented by general formula (VIII): R-I (VIII) (wherein, R is an alkyl group which may have a substituent, a bicyclo group which may have a substituent, an alkenyl group which may have a substituent, a heterocyclic group which contains one to four atoms selected from nitrogen atoms, oxygen atoms and sulfur atoms, and may have a substituent, or an aryl group which may have a substituent) with zinc or magnesium treated with bromine, hydrogen chloride or hydrogen bromide. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供比常规方法更有效的格氏试剂的制备方法。解决方案：由通式（Ⅸ）表示的化合物的制备方法：RXY（其中，X为锌或镁，Y为碘，溴或氯）包括使通式（Ⅷ）表示的化合物： R 1（Ⅷ）（其中，R为可具有取代基的烷基，可具有取代基的二环基，可具有取代基的烯基，含有1〜4个选自氮原子的原子的杂环基，氧原子和硫原子，并且可以具有取代基或可具有取代基的芳基）与用溴，氯化氢或溴化氢处理的锌或镁。版权所有（C）2008，JPO＆INPIT

9. 发明专利

ES2835828T3 Procedimiento para producir a-halo-tetraacilglucosa 未知
公开(公告)号：ES2835828T3
公开(公告)日：2021-06-23
申请号：ES14756953
申请日：2014-02-25
申请人： MITSUBISHI TANABE PHARMA CORP
发明人： UEDA KEITA , HATSUDA MASANORI , HYODO ISAO , TANIMOTO KOUICHI
IPC分类号： C07H1/00 , C07H5/02
摘要： Un procedimiento para producir una α-halo-tetraacil-glucosa representada por la formula (III): **(Ver fórmula)** en la que R representa alquilo C1-6 opcionalmente sustituido o arilo opcionalmente sustituido, y X representa un atomo de halogeno, que comprende hacer reaccionar D-glucosa o D-glucosido de alquilo C1-6 con un haluro de acido representado por la formula (V): **(Ver fórmula)** en la que R representa alquilo C1-6 opcionalmente sustituido o un arilo opcionalmente sustituido, y X representa un atomo de halogeno, en presencia de una cantidad catalitica de un haluro metalico de acido de Lewis seleccionado del grupo que consiste en bromuro de cinc, bromuro de cobalto y bromuro de bismuto.

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