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1. 发明申请

US20060173014A1 Nobel compounds having selective inhibiting effect at gsk3 失效
标题翻译：诺贝尔化合物在gsk3具有选择性抑制作用
公开(公告)号：US20060173014A1
公开(公告)日：2006-08-03
申请号：US10539546
申请日：2003-12-15
申请人： Stefan Berg , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Sven Hellberg , Peter Soderman
IPC分类号： A61K31/497 , C07D403/02
CPC分类号： C07D295/073 , C07D211/56 , C07D241/26 , C07D295/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to new compounds, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.
摘要翻译：本发明涉及新化合物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途，例如提供在GSK3具有选择性抑制作用的化合物。

2. 发明申请

US20060116362A1 Nobel compounds having selective inhibiting effect at gsk3 失效
标题翻译：诺贝尔化合物在gsk3具有选择性抑制作用
公开(公告)号：US20060116362A1
公开(公告)日：2006-06-01
申请号：US10539543
申请日：2003-12-15
申请人： Stefan Berg , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Sven Hellberg , Peter Soderman
IPC分类号： A61K31/497 , A61K31/4965 , C07D403/02 , C07D241/26
CPC分类号： C07D401/12
摘要： The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclicc ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及新的式（I）化合物，其中：Z是N，X是CH或N; Y为CONR 5; P是苯基或含有一个或多个选自N，O或S的杂原子的5或6元杂芳环; Q是苯基或含有一个或多个氮原子的5或6元芳族杂环环; R是C 1-6烷基，R 10，或C 1-6烷基氮杂环丁烷; R 10是氢，C 1-6烷基，C 2-6 - 烯基，C 2-6 - 炔基，C 0-6-6烷基C 3-6环烷基，C 0-6烷基芳基，C 0-6-烷基杂芳基或C 1-6烷基N R 8 R 9; R 11是C 1-6烷基，R 8，R 9，C 0-6，烷基C 3-6环烷基或C 0-6-6烷基杂环烷基; 作为其盐的游离碱或其药学上可接受的盐，溶剂化物或溶剂化物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

3. 发明申请

US20100075989A1 Novel Compounds Having Selective Inhibiting Effect at GSK3 审中-公开
标题翻译：在GSK3上具有选择性抑制作用的新型化合物
公开(公告)号：US20100075989A1
公开(公告)日：2010-03-25
申请号：US12545213
申请日：2009-08-21
申请人： Stefan Berg , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Sven Hellberg , Peter Soderman
IPC分类号： A61K31/497 , C07D401/04 , A61P25/28
CPC分类号： C07D401/12
摘要： Compounds of formula I wherein Z, X, Y, ring P, ring Q, R, R3, R4, n and m are as defined in the specification, as a free base or a pharmaceutically acceptable salt, solvate or solvate of a salt; processes for their preparation and new intermediates used therein, pharmaceutical formulations containing said compounds, and the use of said compounds in therapy.
摘要翻译：其中Z，X，Y，环P，环Q，R，R 3，R 4，n和m如说明书中所定义的式I化合物作为盐的游离碱或其药学上可接受的盐，溶剂合物或溶剂合物; 其制备方法和其中使用的新中间体，含有所述化合物的药物制剂以及所述化合物在治疗中的用途。

4. 发明授权

US07595319B2 Compounds having selective inhibiting effect at GSK3 失效
标题翻译：在GSK3具有选择性抑制作用的化合物
公开(公告)号：US07595319B2
公开(公告)日：2009-09-29
申请号：US10539546
申请日：2003-12-15
申请人： Stefan Berg , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Sven Hellberg , Peter Soderman
IPC分类号： A61K31/497 , A61K31/50 , A61K31/501 , C07D241/02 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00
CPC分类号： C07D295/073 , C07D211/56 , C07D241/26 , C07D295/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： Selective phenyl substituted aminopyrazine inhibitors of GSK3 useful for the prevention and/or treatment of cognitive disorders.
摘要翻译：用于预防和/或治疗认知障碍的GSK3的选择性苯基取代的氨基吡嗪抑制剂。

5. 发明授权

US07585853B2 Compounds having selective inhibiting effect at GSK3 失效
标题翻译：在GSK3具有选择性抑制作用的化合物
公开(公告)号：US07585853B2
公开(公告)日：2009-09-08
申请号：US10539543
申请日：2003-12-15
申请人： Stefan Berg , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Sven Hellberg , Peter Soderman
IPC分类号： A01N43/00 , A61K31/00 , A61K31/4965 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D241/02
CPC分类号： C07D401/12
摘要： The present invention relates to new compounds of formula (I) wherein: Z is N and X is CH or N; Y is CONR5; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S; Q is phenyl or a 5 or 6 membered aromatic heterocyclic ring containing one or more nitrogen atoms; R is C1-6alkylNR10R11 or C1-6alkylazetidine; R10 is hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C0-6alkylC3-6cycloalkyl, C0-6alkylaryl, C0-61alkylheteroaryl or C1-6alkylNR8R9; R11 is C1-6alkylNR8R9, C0-6alkylC3-6cycloalkyl or C0-6alkylheterocycloalkyl; as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及新的式（I）化合物，其中：Z是N，X是CH或N; Y是CONR5; P是苯基或含有一个或多个选自N，O或S的杂原子的5或6元杂芳环; Q是苯基或含有一个或多个氮原子的5或6元芳族杂环; R是C 1-6烷基NR 10 R 11或C 1-6烷基氮杂环丁烷; R 10是氢，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 0-6烷基C 3-6环烷基，C 0-6烷基芳基，C 0-6烷基杂芳基或C 1-6烷基NR 8 R 9; R 11是C 1-6烷基，R 8 R 9，C 0-6烷基C 3-6环烷基或C 0-6烷基杂环烷基; 作为其盐的游离碱或其药学上可接受的盐，溶剂化物或溶剂化物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途。

6. 发明申请

US20090018130A1 Derivatives of 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxamide or 5-Aryl-1H-Pyrrolo [2, 3B] Pyridine-3-Carboxylic Acid 审中-公开
标题翻译： 5-芳基-1H-吡咯并[2,3B]吡啶-3-甲酰胺或5-芳基-1H-吡咯并[2,3B]吡啶-3-羧酸的衍生物
公开(公告)号：US20090018130A1
公开(公告)日：2009-01-15
申请号：US11571183
申请日：2005-06-20
申请人： Stefan Berg , Johan Hedstrom , Sven Hellberg , Peter Soderman
发明人： Stefan Berg , Johan Hedstrom , Sven Hellberg , Peter Soderman
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , A61K31/496
CPC分类号： C07D471/04
摘要： The present invention relates to new compounds of formula I as a free base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy.
摘要翻译：本发明涉及作为其盐的游离碱或其药学上可接受的盐，溶剂合物或溶剂合物的新型式I化合物，其制备方法和其中使用的新中间体，含有所述治疗活性化合物的药物制剂以及使用所述活性化合物在治疗中。

7. 发明申请

US20090233930A9 Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia 审中-公开
标题翻译：新型2-氨基咪唑-4-酮化合物及其在制造用于治疗认知功能障碍，阿尔茨海默病，神经退行性和痴呆症药物中的应用
公开(公告)号：US20090233930A9
公开(公告)日：2009-09-17
申请号：US12094276
申请日：2006-11-20
申请人： Stefan Berg , Jeremy Burrows , Gianni Chessari , Miles Stuart Congreve , Johan Hedstrom , Sven Hellberg , Katharina Hogdin , Jacob Kihlstrom , Karin Kolmodin , Johan Lindstrom , Christopher Murray , Sahil Patel
发明人： Stefan Berg , Jeremy Burrows , Gianni Chessari , Miles Stuart Congreve , Johan Hedstrom , Sven Hellberg , Katharina Hogdin , Jacob Kihlstrom , Karin Kolmodin , Johan Lindstrom , Christopher Murray , Sahil Patel
IPC分类号： A61K31/5377 , C07D401/10 , A61K31/4725 , C07D339/08 , A61P25/28 , C07F7/08 , C12N9/99 , C07D413/12
CPC分类号： C07D233/88 , C07C25/22 , C07C25/24 , C07C39/373 , C07C43/1747 , C07C43/23 , C07C47/575 , C07C49/792 , C07C49/813 , C07C49/83 , C07C49/84 , C07D209/08 , C07D217/06 , C07D233/86 , C07D265/36 , C07D307/79 , C07D339/08 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/04 , C07F7/1804
摘要： This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有以下结构式I的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供了认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

8. 发明申请

US20090105252A1 Pyrimidine Derivatives and Their Use in Therapy as well as the Use of Pyrimidine Derivatives in the Manufacture of a Medicament for Prevention and/or Treatment of Alzheimer's Disease 审中-公开
标题翻译：嘧啶衍生物及其在治疗中的应用以及嘧啶衍生物在制造预防和/或治疗阿尔茨海默病药物中的应用
公开(公告)号：US20090105252A1
公开(公告)日：2009-04-23
申请号：US12089008
申请日：2006-10-02
申请人： Lars Andersson , Erwan Arzel , Stefan Berg , Jeremy Burrows , Sven Hellberg , Fernando Huerta , Torben Pedersen , Tobias Rein , Didier Rotticci , Karin Staaf , Dominika Turek
发明人： Lars Andersson , Erwan Arzel , Stefan Berg , Jeremy Burrows , Sven Hellberg , Fernando Huerta , Torben Pedersen , Tobias Rein , Didier Rotticci , Karin Staaf , Dominika Turek
IPC分类号： A61K31/5377 , C07D403/02 , A61K31/506 , C07D413/14 , A61P25/28 , C07D403/14 , A61K31/496
CPC分类号： C07D405/14 , A61K31/506 , C07D401/14 , C07D403/04 , C07D409/14
摘要： Compounds of formula I wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the specification as a base or a pharmaceutically acceptable salt, solvate or solvate of salt thereof, processes for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如说明书中所定义的式I化合物或其盐，溶剂化物或其盐的溶剂合物，其制备方法，新的其中使用的中间体，含有所述化合物的药物制剂和所述化合物在治疗中的用途。

9. 发明申请

US20060116385A1 Novel compounds having selective inhibiting effect at gsk3 失效
标题翻译：在gsk3具有选择性抑制作用的新型化合物
公开(公告)号：US20060116385A1
公开(公告)日：2006-06-01
申请号：US10539545
申请日：2003-12-15
申请人： Stefan Berg , Sven Hellberg
发明人： Stefan Berg , Sven Hellberg
IPC分类号： A61K31/4965 , A61K31/497 , A61K31/4439 , A61K31/44 , C07D401/02 , C07D403/02
CPC分类号： C07D403/06 , C07B2200/11 , C07D241/26 , C07D409/06
摘要： The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.
摘要翻译：本发明涉及新的式（I）化合物，其中Z是N; Y为CONR 5，NR 5 CO，SO 2 NR 5，NR 5 O， > SO 2，CH 2，NR 5，NR 5，NR 5 CONR CH 2 CO 2，CO，O或CH 2 O; X是CH或N; P是苯基或含有一个或多个选自N，O或S的杂原子的5或6元杂芳环，所述苯环或5或6元杂芳环可以任选地与5或6元饱和，部分饱和或不饱和的含有一个或多个选自C，N，O或S的原子的环; Q是C 1-6烷基，C 2-6链烯基或C 2-6-6炔基，其制备方法和使用的新中间体其中含有所述治疗活性化合物的药物制剂和所述活性化合物在治疗中的用途，例如提供在GSK3具有选择性抑制作用的化合物。

10. 发明申请

US20050075351A1 Use 审中-公开
标题翻译：使用
公开(公告)号：US20050075351A1
公开(公告)日：2005-04-07
申请号：US10499685
申请日：2002-12-18
申请人： Stefan Berg , Ratan Bhat , Sven Hellberg
发明人： Stefan Berg , Ratan Bhat , Sven Hellberg
IPC分类号： C07D487/04 , A61K31/517 , A61K31/5377 , A61P9/10 , A61P15/00 , A61P15/16 , A61P17/14 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , C07D471/04 , C07D43/02
CPC分类号： A61K31/517
摘要： The present invention relates to a new use of oxindole derivatives of formula I, as a free base or pharmaceutically acceptable salts thereof, in the manufacture of a medicament for the prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3. Formula (I) wherein R1, R2, R3, ring Z, m and n are as defined as in claim 1. The present invention further relates to a method of prevention and/or treatment of dementia related diseases, Alzheimer's Disease and conditions associated with glycogen synthase kinase-3, as well as a pharmaceutical composition for said use.
摘要翻译：本发明涉及式I的羟吲哚衍生物作为游离碱或其药学上可接受的盐在制备用于预防和/或治疗痴呆症相关疾病，阿尔茨海默病和与糖原相关的病症的药物中的新用途合酶激酶-3。式（I）其中R 1，R 2，R 3，环Z，m和n如权利要求1中所定义。本发明还涉及预防和/或治疗痴呆的方法相关疾病，阿尔茨海默病和与糖原合酶激酶-3相关的病症，以及用于所述用途的药物组合物。

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