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1. 发明申请

WO2004055024A1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-4-ON-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 审中-公开
标题翻译： 3-取代的-3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：WO2004055024A1
公开(公告)日：2004-07-01
申请号：PCT/EP2003/014423
申请日：2003-12-17
申请人： ABBOTT GMBH & CO. KG , BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
发明人： BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
IPC分类号： C07D495/14
CPC分类号： C07D495/14
摘要： Die erfindung betrifft 3,4-Dihydro-thieno[2,3-d]pyrimidin-4-on-Derivate, die in 3-Position mit 5-gliedrigem Heteroaryl substituierte sind, das mit einem Aryl- oder Heteroarylrest kondensiert sein kann, wobei das Heteroaryl und gegebenenfalls der kondensierte Aryl- oder Heteroarylrest 1,2 oder 3 unabhängig voneinander unter C 1-5 -Alkyl, C 1-5 -Alkoxy, C 1-5 -Alkylthio, Halogen, CN, Halogen-C 1-5 -alkyl, Halogen-C 1-5 alkoxy, Hydroxy, -NH 2, -N(R6) 2 , -NH(R6), Aryl, Aryloxy, Aralkyl, Aralkyloxy und Heteroaryl ausgewählte Substituenten tragen können, wobei die Substituenten Aryl, Aryloxy, Aralkyl, Aralkyloxy und Heteroaryl 1,2 oder 3 unabhängig voneinander unter C 1-5 -Alkythio, Halogen, CN, Halogen-C 1-5 -alkyl, Halogen-C 1-5 alkoxy, Hydroxy, -NH 2 , -N(R6) 2 und -NH(R6) ausgewählte Substituenten tragen können. Die Herstellung und Verwendung dieser Derivate, insbesondere zu therapeutischen Zwecken, z.B. bei der Behandlulng von Depressionen, werden ebenfalls beschrieben.
摘要翻译：本发明涉及3,4-二氢 - 噻吩并[2,3-d]嘧啶-4-酮衍生物，已被在其中可以与芳基稠合或杂芳基的5元杂芳基的3-位被取代，其中从C 1-5烷基，C 1-5 - 烷氧基，C 1-5 - 烷硫基，卤素，CN，卤代C 1-5烷基，卤素独立地选自杂芳基和任选稠合的芳基或杂芳基被1,2或3个取代基 C 1-5烷氧基，羟基，-NH 2，-N（R 6）2，-NH（R 6），芳基，芳氧基，芳烷基，芳烷氧基和杂芳基可以带有一个取代基中选择，其中取代基的芳基，芳氧基，芳烷基，芳烷氧基和杂芳基1， 2个或3个选自C 1-5 - 烷基硫基，卤素，CN，卤代C 1-5烷基，卤代C 1-5烷氧基，羟基，-NH 2，-N（R 6）2和-NH（R 6）独立地选择的取代基携带选自取代基可以。制备和使用这些衍生物的，并且特别是用于治疗目的，例如在抑郁症的Behandlulng，也有所说明。

2. 发明申请

WO2007006566A1 PYRIDAZINE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：吡咯烷酮化合物作为GLYCOGEN SYNTHASE KINASE 3抑制剂
公开(公告)号：WO2007006566A1
公开(公告)日：2007-01-18
申请号：PCT/EP2006/006826
申请日：2006-07-12
申请人： ABBOTT GMBH & CO. KG , TURNER, Sean, Colm , BAKKER, Margaretha , GRANDEL, Roland
发明人： TURNER, Sean, Colm , BAKKER, Margaretha , GRANDEL, Roland
IPC分类号： C07D487/04 , C07D471/14 , A61K31/551 , A61K31/55 , A61P25/28
CPC分类号： C07D487/04 , C07D471/14
摘要： Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula (I) indicates a single bond or a double bond; X is O, S or N-R 5 ; R 1 , R 2 are independently selected from the group consisting of H, NH 2 , NH-C 1 -C 6 -alkyl, OH, =O, (i.e. a carbonyl group), C 1 -C 6 -alkoxy, halogen, methyl, C 2 -C 4 -alkyl, C 3 - C 4 -cycloalkyl, C 3 -C 4 -alkenyl, fluorinated C 1 -C 4 -alkyl, fluorinated C 3 -C 4 -cycloalkyl, fluorinated C 3 -C 4 -alkenyl, formyl, C 1 -C 3 -alkylcarbonyl, and an aromatic radical Ar, R 1 and R 2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and O, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1 , 2 or 3 substituents selected, independently of each other, from the group of radicals R 4 as defined below; R 3 is hydrogen OH, halogen, CN, nitro, C 1 -C 6 -alkyl, fluorinated C 1 -C 6 -alkyl, C 1 -C 6 - hydroxyalkyl, C 1 -C 6 -alkoxy-C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, fluorinated C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 3 -C 7 -cycloalkyl, fluorinated C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkoxy, C 1 -C 6 - hydroxyalkoxy, C 1 C 6 -alkoxy-C 1 -C 6 -alkoxy, fluorinated C 1 -C 6 -alkoxy, C 1 -C 6 - alkylthio, fluorinated-C 1 -C 6 alkylthio, C 1 C 6 -alkylsulfinyl, fluorinated C 1 -C 6 - alkylsulfinyl, C 1 -C 6 -alkylsulfonyl, fluorinated C 1 -C 6 alkylsulfonyl, C 1 C 6 - alkylcarbonyl, fluorinated C 1 C 6 -alkylcarbonyl, C 1 - C 6 -alkylcarbonylamino, fluorinated C 1 -C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C 1 -C 6 -alkoxycarbonyl, NR a R b , C(O)-NR e R f , NH-C(O)-N R e R f , NR a R b -C 1 -C 6 -alkylene, O-NR a R b , etc. and wherein R 4 and R 5 are as defined in the specification and the claims.
摘要翻译：公开了可用于抑制糖原合成酶激酶3（GSK-3），制备该化合物的方法，含该化合物的组合物和使用该化合物的治疗方法的式I的哒嗪化合物。在式（I）中，债券或双重债券; X是O，S或N-R 5; R 1，R 2，R 2独立地选自H，NH 2，NH-C 1， -C 6 - 烷基，OH，= O（即羰基），C 1 -C 6 - 烷氧基，卤素，甲基，C 2 -C 4 - 烷基，C 3〜C 4 - 环烷基，C 3 氟化C 1 -C 4 - 亚烷基，氟化C 3 - 亚烷基，氟化C 1 -C 4 - C 4 - 4 - 环烷基，氟化C 3 -C 4 - 烯基，甲酰基，C 1 -C 3 - 亚烷基 - 烷基羰基和芳族基团Ar，R 1和R 2与它们所连接的碳原子一起形成稠合的饱和或不饱和的5-，6-或7-元C-结合的碳环或杂环，其包含选自氮，氧和硫作为环成员的1个杂原子，和0,1,2个另外的杂原子，独立地选自O，S和 N作为环成员，其中稠环是未取代的或可以携带1,2或3s 从如下定义的基团R 4中选择的取代基彼此独立地选自： R 3是氢OH，卤素，CN，硝基，C 1 -C 6 - 烷基，氟化C 1 C 1 -C 6 - 烷基，C 1 -C 6 - 羟基烷基，C 1 -C 6 - C 1 -C 6 - 烷氧基-C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，氟化C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C

3. 发明申请

WO2008154241A1 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的5-HETEROARYL取代的吲哚美辛
公开(公告)号：WO2008154241A1
公开(公告)日：2008-12-18
申请号：PCT/US2008/065727
申请日：2008-06-04
申请人： ABBOTT LABORATORIES , AKRITOPOULOU-ZANZE, Irini , WAKEFIELD, Brian D , MACK, Helmut , TURNER, Sean C , GASIECKI, Alan F , GRACIAS, Vijaya J , SARRIS, Kathy , KALVIN, Douglas M , MICHMERHUIZEN, Melissa J , SHUAI, Qi , PATEL, Jyoti R , BAKKER, Margaretha , TEUSCH, Nicole , JOHNSON, Eric T , KOVAR, Peter J , DJURIC, Stevan W , LONG, Andrew J , VASUDEVAN, Anil , HOBSON, Adrian , ST. JOHN MOORE, Nigel , WANG, Lu , GEORGE, Dawn , LI, Biqin , FRANK, Kristine
发明人： AKRITOPOULOU-ZANZE, Irini , WAKEFIELD, Brian D , MACK, Helmut , TURNER, Sean C , GASIECKI, Alan F , GRACIAS, Vijaya J , SARRIS, Kathy , KALVIN, Douglas M , MICHMERHUIZEN, Melissa J , SHUAI, Qi , PATEL, Jyoti R , BAKKER, Margaretha , TEUSCH, Nicole , JOHNSON, Eric T , KOVAR, Peter J , DJURIC, Stevan W , LONG, Andrew J , VASUDEVAN, Anil , HOBSON, Adrian , ST. JOHN MOORE, Nigel , WANG, Lu , GEORGE, Dawn , LI, Biqin , FRANK, Kristine
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R 1 , R 2 , R 3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中A，R 1，R 2，R 3和m在说明书中定义。本发明还涉及制备所述化合物的方法和含有所述化合物的组合物，其可用于抑制激酶如糖原合酶激酶3（GSK-3），Rho激酶（ROCK），Janus激酶（JAK），AKT，PAK4 ，PLK，CK2，KDR，MK2，JNK1，极光，pim1和nek2。

4. 发明授权

EP1572698B1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO¬2,3-D PYRIMIDIN-4-ONE-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 有权
标题翻译： 3-取代的-3,4-二氢THIENO¬2,3-D嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：EP1572698B1
公开(公告)日：2008-07-02
申请号：EP03813137.1
申请日：2003-12-17
申请人： Abbott GmbH & Co. KG
发明人： BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
IPC分类号： C07D495/14 , A61K31/519 , A61P25/00
CPC分类号： C07D495/14
摘要： The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidinde-4-one-derivatives which are substituted at 3-position with 5-membered heteroaryl which can be condensed with an aryl or heteroaryl radical. The heteroaryl and, optionally, the condensed aryl or heteroaryl radical 1,2 or 3 can independently include selected substitutents from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2, -NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl 1,2 or 3 independently include selected substituents from C1-5-alkythio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2 and -NH(R6). The invention also relates to the production and use of said derivatives, especially for therapeutical purposes, e.g. in the treatment of depression.

5. 发明公开

EP1902055A1 PYRIDAZINE COMPOUNDS AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：哒嗪抑制剂糖原合酶激酶3
公开(公告)号：EP1902055A1
公开(公告)日：2008-03-26
申请号：EP06754720.8
申请日：2006-07-12
申请人： Abbott GmbH & Co. KG
发明人： TURNER, Sean, Colm , BAKKER, Margaretha , GRANDEL, Roland
IPC分类号： C07D487/04 , C07D471/14 , A61K31/551 , A61K31/55 , A61P25/28
CPC分类号： C07D487/04 , C07D471/14
摘要： Disclosed are pyridazine compounds of the formula I which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds: In formula (I) indicates a single bond or a double bond; X is O, S or N-R5; R1, R2 are independently selected from the group consisting of H, NH2, NH-C1-C6-alkyl, OH, =O, (i.e. a carbonyl group), C1-C6-alkoxy, halogen, methyl, C2-C4-alkyl, C3- C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, formyl, C1-C3-alkylcarbonyl, and an aromatic radical Ar, R1 and R2 together with the carbon atoms, to which they are attached, form a fused, saturated or unsaturated 5-, 6- or 7-membered C-bound carbocyclic or heterocyclic ring comprising 1 heteroatom, selected from nitrogen, oxygen and sulfur as ring member and O, 1 or 2 further heteroatoms, independently selected from O, S and N, as ring members, wherein the fused ring is unsubstituted or may carry 1 , 2 or 3 substituents selected, independently of each other, from the group of radicals R4 as defined below; R3 is hydrogen OH, halogen, CN, nitro, C1-C6-alkyl, fluorinated C1-C6-alkyl, C1-C6- hydroxyalkyl, C1-C6-alkoxy-C1-C6-alkyl, C2-C6-alkenyl, fluorinated C2-C6-alkenyl, C2-C6-alkynyl, C3-C7-cycloalkyl, fluorinated C3-C7-cycloalkyl, C1-C6-alkoxy, C1-C6- hydroxyalkoxy, C1C6-alkoxy-C1-C6-alkoxy, fluorinated C1-C6-alkoxy, C1-C6- alkylthio, fluorinated-C1-C6 alkylthio, C1C6-alkylsulfinyl, fluorinated C1-C6- alkylsulfinyl, C1-C6-alkylsulfonyl, fluorinated C1-C6 alkylsulfonyl, C1C6- alkylcarbonyl, fluorinated C1C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, fluorinated C1-C6-alkylcarbonylamino, carboxy, C1-C6-alkyloxycarbonyl, fluorinated C1-C6-alkoxycarbonyl, NRaRb, C(O)-NReRf, NH-C(O)-N ReRf, NRaRb-C1-C6-alkylene, O-NRaRb, etc. and wherein R4 and R5 are as defined in the specification and the claims.

6. 发明公开

EP1572698A1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO[2,3-D]PYRIMIDIN-4-ONE-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 有权
标题翻译： 3-取代的-3,4-二氢THIENO¬2,3-D嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：EP1572698A1
公开(公告)日：2005-09-14
申请号：EP03813137.1
申请日：2003-12-17
申请人： Abbott GmbH & Co. KG
发明人： BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
IPC分类号： C07D495/14 , A61K31/519 , A61P25/00
CPC分类号： C07D495/14
摘要： The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidinde-4-one-derivatives which are substituted at 3-position with 5-membered heteroaryl which can be condensed with an aryl or heteroaryl radical. The heteroaryl and, optionally, the condensed aryl or heteroaryl radical 1,2 or 3 can independently include selected substitutents from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2, -NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl 1,2 or 3 independently include selected substituents from C1-5-alkythio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2 and -NH(R6). The invention also relates to the production and use of said derivatives, especially for therapeutical purposes, e.g. in the treatment of depression.

7. 发明公开

EP2167491A1 5-HETEROARYL SUBSTITUTED INDAZOLES AS KINASE INHIBITORS 审中-公开
标题翻译： 5-杂芳基取代的吲唑作为激酶抑制剂的
公开(公告)号：EP2167491A1
公开(公告)日：2010-03-31
申请号：EP08770094.4
申请日：2008-06-04
申请人： Abbott Laboratories , Abbott GmbH & Co. KG
发明人： AKRITOPOULOU-ZANZE, Irini , WAKEFIELD, Brian D , MACK, Helmut , TURNER, Sean C , GASIECKI, Alan F , GRACIAS, Vijaya J , SARRIS, Kathy , KALVIN, Douglas M , MICHMERHUIZEN, Melissa J , SHUAI, Qi , PATEL, Jyoti R , BAKKER, Margaretha , TEUSCH, Nicole , JOHNSON, Eric F. , KOVAR, Peter J , DJURIC, Stevan W , LONG, Andrew J , VASUDEVAN, Anil , HOBSON, Adrian , ST. JOHN MOORE, Nigel , WANG, Lu , GEORGE, Dawn , LI, Biqin , FRANK, Kristine
IPC分类号： C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D403/04 , C07D413/04 , C07D417/04
摘要： The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.

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