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1. 发明申请

WO03099793A8 1,2-AZOLE DERIVATIVES WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY 审中-公开
标题翻译：具有高血压和高血压活性的1,2-AZO衍生物
公开(公告)号：WO03099793A8
公开(公告)日：2004-12-29
申请号：PCT/JP0306389
申请日：2003-05-22
申请人： TAKEDA PHARMACEUTICAL , MAEKAWA TSUYOSHI , HARA RYOMA , ODAKA HIROYUKI , KIMURA HIROYUKI , MIZUFUNE HIDEYA , FUKATSU KOHJI
发明人： MAEKAWA TSUYOSHI , HARA RYOMA , ODAKA HIROYUKI , KIMURA HIROYUKI , MIZUFUNE HIDEYA , FUKATSU KOHJI
IPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/422 , A61K31/4439
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04
摘要： A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR4 (R4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.

2. 发明申请

WO03099793A9 1,2-AZOLE DERIVATIVES WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY 审中-公开
标题翻译：具有高血压和高血压活性的1,2-AZO衍生物
公开(公告)号：WO03099793A9
公开(公告)日：2005-02-10
申请号：PCT/JP0306389
申请日：2003-05-22
申请人： TAKEDA PHARMACEUTICAL , MAEKAWA TSUYOSHI , HARA RYOMA , ODAKA HIROYUKI , KIMURA HIROYUKI , MIZUFUNE HIDEYA , FUKATSU KOHJI
发明人： MAEKAWA TSUYOSHI , HARA RYOMA , ODAKA HIROYUKI , KIMURA HIROYUKI , MIZUFUNE HIDEYA , FUKATSU KOHJI
IPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04 , A61K31/415 , A61K31/4155 , A61K31/42 , A61K31/422 , A61K31/4439
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04
摘要： A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR (R is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：由式（1）表示的化合物，其中环A是任选具有1至3个取代基的环; 环B是可以进一步具有1至3个取代基的1,2-吡咯环; Xa，Xb和Xc相同或不同，各自为键，-O - ， - S-等; Ya是具有1至20个碳原子的二价脂族烃残基; Yb和Yc相同或不同，各自为键或碳原子数1〜20的二价脂肪族烃残基; 环C是可以进一步具有1至3个取代基的单环芳环; R表示-OR 4（R 4为氢原子或任意取代的烃基）等，或其盐或其前药可用作预防或治疗糖尿病等的药剂。

3. 发明申请

WO2003099793A1 1,2-AZOLE DERIVATIVES WITH HYPOGLYCEMIC AND HYPOLIPIDEMIC ACTIVITY 审中-公开
标题翻译：具有高分子和低分子活性的1,2-AZO衍生物
公开(公告)号：WO2003099793A1
公开(公告)日：2003-12-04
申请号：PCT/JP2003/006389
申请日：2003-05-22
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , MAEKAWA, Tsuyoshi , HARA, Ryoma , ODAKA, Hiroyuki , KIMURA, Hiroyuki , MIZUFUNE, Hideya , FUKATSU, Kohji
发明人： MAEKAWA, Tsuyoshi , HARA, Ryoma , ODAKA, Hiroyuki , KIMURA, Hiroyuki , MIZUFUNE, Hideya , FUKATSU, Kohji
IPC分类号： C07D231/12
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D231/22 , C07D261/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/12 , C07D417/04
摘要： A compound represented by the formula (1) wherein ring A is a ring optionally having 1 to 3 substituents; ring B is a 1,2-azole ring which may further have 1 to 3 substituents; Xa, Xb and Xc are the same or different and each is a bond, - O -, - S - and the like; Ya is a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; Yb and Yc are the same or different and each is a bond or a divalent aliphatic hydrocarbon residue having 1 to 20 carbon atoms; ring C is a monocyclic aromatic ring which may further have 1 to 3 substituents; and R represents -OR 4 (R 4 is hydrogen atom or optionally substituted hydrocarbon group) and the like, or a salt thereof or a prodrug thereof is useful as an agent for the prophylaxis or treatment of diabetes and the like.
摘要翻译：由下式表示的化合物其中环A是任选具有1至3个取代基的环; 环B是可以进一步具有1至3个取代基的1,2-吡咯环; Xa，Xb和Xc相同或不同，各自为键，-O - ， - S-等; Ya是具有1至20个碳原子的二价脂族烃残基; Yb和Yc相同或不同，各自为键或碳原子数1〜20的二价脂肪族烃残基; 环C是可以进一步具有1至3个取代基的单环芳环; 和R表示-OR4（R4是氢原子或任选取代的烃基）等，或其盐或其前药可用作预防或治疗糖尿病等的药剂。

4. 发明申请

WO2008016184A1 ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF 审中-公开
标题翻译： ALPHA-CARBOLINE衍生物及其制备方法
公开(公告)号：WO2008016184A1
公开(公告)日：2008-02-07
申请号：PCT/JP2007/065571
申请日：2007-08-02
申请人： TAKEDA PHARMACEUTICAL COMPANY LIMITED , MIZUNO, Masahiro , MIZUFUNE, Hideya , SERA, Misayo , MINENO, Masahiro , UEDA, Tsuyoshi
发明人： MIZUNO, Masahiro , MIZUFUNE, Hideya , SERA, Misayo , MINENO, Masahiro , UEDA, Tsuyoshi
IPC分类号： C07D471/04 , C07D213/74 , C07D213/75 , C07D405/12
CPC分类号： C07D471/04 , C07D213/74 , C07D213/75 , C07D405/12
摘要： To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein the symbols respectively represent the same meaning as defined in the present specification.
摘要翻译：提供在几个步骤中以及方便和工业上有利地制备α-咔啉衍生物的方法。一种制备由式（II）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下，将式（I）表示的化合物或其盐进行闭环反应基础; 一种制备由式（Ⅸ）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下使式（Ⅶ）表示的化合物或其盐进行闭环反应碱，然后进行芳构化反应; 以及由式（XV），（XVII）和（XIX）表示的化合物或其盐制备化合物或其盐的方法，包括使由式（Ⅱ）和（Ⅸ）表示的各种化合物或其盐进行引入在必要时离去基团，随后进行偶联反应：其中符号分别表示与本说明书中定义的相同的含义。

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