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1. 发明申请

WO2011045383A2 2,6-DIAMINOPYRIDINE COMPOUNDS SUITABLE FOR TREATING DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS OR FOR TREATING OR PREVENTING OCULAR DISEASES OR CONDITIONS ASSOCIATED WITH A PATHOLOGICAL ABNORMALITY/CHANGE IN THE TISSUE OF THE VISUAL SYSTEM 审中-公开
标题翻译：用于治疗与淀粉样蛋白或类淀粉样蛋白相关的疾病的2,6-二氨基吡啶化合物或用于治疗或预防与视觉异常组织相关的病理学异常/变化相关的眼睛疾病或病症
公开(公告)号：WO2011045383A2
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065439
申请日：2010-10-14
申请人： AC IMMUNE S.A. , KROTH, Heiko , FROESTL, Wolfgang , PFEIFER, Andrea , MUHS, Andreas
发明人： KROTH, Heiko , FROESTL, Wolfgang , PFEIFER, Andrea , MUHS, Andreas
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , A61K31/444 , C07D471/04 , G01N33/6896 , G01N2333/4709 , G01N2800/28
摘要： The present invention relates to 2.6-diaminopyridine compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
摘要翻译：本发明涉及可用于治疗与淀粉样蛋白相关的一组疾病和异常以及与淀粉样蛋白相关的疾病或病症的2.6-二氨基吡啶化合物。本发明的化合物还可以用于治疗与视觉系统的组织中的病理学异常/变化相关的眼部疾病。

2. 发明申请

WO2011128455A1 NOVEL COMPOUNDS FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS 审中-公开
标题翻译：用于治疗与淀粉样蛋白或类淀粉样蛋白相关的疾病的新型化合物
公开(公告)号：WO2011128455A1
公开(公告)日：2011-10-20
申请号：PCT/EP2011/056068
申请日：2011-04-15
申请人： AC IMMUNE S.A. , KROTH, Heiko , HAMEL, Cotinica , BENDERITTER, Pascal , FROESTL, Wolfgang , SREENIVASACHARY, Nampally , MUHS, Andreas
发明人： KROTH, Heiko , HAMEL, Cotinica , BENDERITTER, Pascal , FROESTL, Wolfgang , SREENIVASACHARY, Nampally , MUHS, Andreas
IPC分类号： C07D209/14 , C07D401/14 , C07D471/04 , C07D495/04 , A61K31/437 , A61P25/28
CPC分类号： A61K31/5377 , A61K31/404 , A61K31/437 , A61K31/496 , A61K45/06 , C07D209/14 , C07D401/14 , C07D471/04 , C07D495/04 , G01N33/6893 , G01N2333/4709 , G01N2800/52
摘要： The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.
摘要翻译：本发明涉及可用于治疗与淀粉样蛋白相关的一组疾病和异常的新型化合物，例如阿尔茨海默病，以及与淀粉状蛋白样蛋白相关的疾病或病症。本发明的化合物还可以用于治疗与视觉系统的组织中的病理学异常/变化相关的眼部疾病。本发明还涉及包含这些化合物的药物组合物和这些化合物用于制备用于治疗或预防与淀粉样蛋白和/或淀粉样蛋白样蛋白相关的疾病或病症的药物的用途。还公开了治疗或预防与淀粉样蛋白和/或淀粉样蛋白样蛋白相关的疾病或病症的方法。

3. 发明申请

WO2017009454A1 NOVEL IMAGING COMPOUNDS 审中-公开
标题翻译：新型成像化合物
公开(公告)号：WO2017009454A1
公开(公告)日：2017-01-19
申请号：PCT/EP2016/066901
申请日：2016-07-15
申请人： AC IMMUNE S.A. , PIRAMAL IMAGING SA
发明人： KROTH, Heiko , NAMPALLY, Sreenivasachary , MOLETTE, Jérôme , GABELLIERI, Emanuele , SCHIEFERSTEIN, Hanno , MÜLLER, Andre , SCHMITT-WILLICH, Heribert , BERNDT, Mathias
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28
CPC分类号： C07D471/14 , A61K51/0455 , C07B59/002
摘要： The present invention relates to novel compounds that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
摘要翻译：本发明涉及可用于选择性Tau检测与Tau聚集体如阿尔茨海默氏病和其他tau蛋白病相关的疾病和异常的新型化合物，其使用正电子发射断层扫描（PET）成像。

4. 发明申请

WO2018015549A1 COMPOUNDS FOR IMAGING TAU PROTEIN AGGREGATES 审中-公开
标题翻译：用于成像TAU蛋白质聚集体的化合物
公开(公告)号：WO2018015549A1
公开(公告)日：2018-01-25
申请号：PCT/EP2017/068509
申请日：2017-07-21
申请人： AC IMMUNE S.A. , PIRAMAL IMAGING SA
发明人： KROTH, Heiko , MOLETTE, Jérôme , DARMENCY, Vincent , SCHIEFERSTEIN, Hanno , MÜLLER, Andre , SCHMITT-WILLICH, Heribert , BERNDT, Mathias , ODEN, Felix , GABELLIERI, Emanuele
IPC分类号： A61K51/04 , C07B59/00
摘要： The present invention relates to novel compounds of the formula (II) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
摘要翻译：本发明涉及新颖的式（II）化合物，其可用于使用正电子发射断层摄影术（positron Emission Tomography）的与Tau聚集体（例如阿尔茨海默病和其他tau蛋白病）相关的病症和异常的选择性Tau检测（ PET）成像。

5. 发明申请

WO2018015546A1 COMPOUNDS FOR IMAGING TAU PROTEIN AGGREGATES 审中-公开
标题翻译：用于成像TAU蛋白质聚集体的化合物
公开(公告)号：WO2018015546A1
公开(公告)日：2018-01-25
申请号：PCT/EP2017/068500
申请日：2017-07-21
申请人： AC IMMUNE S.A. , PIRAMAL IMAGING SA
发明人： KROTH, Heiko , MOLETTE, Jérôme , SCHIEFERSTEIN, Hanno , MÜLLER, Andre , SCHMITT-WILLICH, Heribert , BERNDT, Mathias , ODEN, Felix
IPC分类号： A61K51/04 , C07B59/00
摘要： The present invention relates to novel compounds of the formula (I) that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.
摘要翻译：本发明涉及新颖的式（I）化合物，其可用于使用正电子发射断层扫描术（positron Emission Tomography）对与Tau聚集体（例如阿尔茨海默病和其他tau蛋白病）相关的病症和异常进行选择性Tau检测（ PET）成像。

6. 发明申请

WO2006128184A2 HETEROBICYCLIC METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：异源环氧化酶抑制剂
公开(公告)号：WO2006128184A2
公开(公告)日：2006-11-30
申请号：PCT/US2006/020970
申请日：2006-05-22
申请人： ALANTOS-PHARMACEUTICALS, INC. , STEENECK, Christoph , GEGE, Christian , RICHTER, Frank , HOCHGUERTEL, Matthias , FEURSTEIN, Tim , BLUHM, Harald , SUCHOLEIKI, Irving , BOER, Jurgen , WU, Xinyuan , SCHNEIDER, Matthias , NOLTE, Bert , GALLAGHER, Brian , VAN VELDHUIZEN, Joshua , DENG, Hongbo , ESSERS, Michael , KROTH, Heiko , KIELY, Andrew , POWERS, Timothy , TAVERAS, Arthur, G.
发明人： STEENECK, Christoph , GEGE, Christian , RICHTER, Frank , HOCHGUERTEL, Matthias , FEURSTEIN, Tim , BLUHM, Harald , SUCHOLEIKI, Irving , BOER, Jurgen , WU, Xinyuan , SCHNEIDER, Matthias , NOLTE, Bert , GALLAGHER, Brian , VAN VELDHUIZEN, Joshua , DENG, Hongbo , ESSERS, Michael , KROTH, Heiko , KIELY, Andrew , POWERS, Timothy , TAVERAS, Arthur, G.
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 inhibitors.
摘要翻译：本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。更具体地，本发明提供了一类新型的杂双环MMP-13抑制化合物，其表现出与目前已知的MMP-13抑制剂相关的效力增加。

7. 发明申请

WO2006116157A2 DIPEPTIDYL PEPTIDASE-IV INHIBITORS 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-IV抑制剂
公开(公告)号：WO2006116157A2
公开(公告)日：2006-11-02
申请号：PCT/US2006/015200
申请日：2006-04-21
申请人： ALANTOS PHARMACEUTICALS, INC. , KROTH, Heiko , FEUERSTEIN, Tim , RICHTER, Frank , BOER, Jürgen , ESSERS, Michael , NOLTE, Bert , SCHNEIDER, Matthias , HOCHGUERTEL, Matthias , FRICKEL, Fritz-Frieder , TAVERAS, Arthur
发明人： KROTH, Heiko , FEUERSTEIN, Tim , RICHTER, Frank , BOER, Jürgen , ESSERS, Michael , NOLTE, Bert , SCHNEIDER, Matthias , HOCHGUERTEL, Matthias , FRICKEL, Fritz-Frieder , TAVERAS, Arthur
IPC分类号： C07D403/12 , C07D207/16 , C07D413/12 , C07D401/12
CPC分类号： C07D207/16 , C07D209/02 , C07D209/52 , C07D401/12 , C07D403/12 , C07D413/12 , C07D487/08 , C07D495/04
摘要： The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
摘要翻译：本发明一般涉及吡咯烷和噻唑烷DPP-IV抑制剂化合物。本发明还提供了用于制备这种化合物的合成方法，使用这些化合物抑制DPP-IV的方法和含有它们的药物制剂用于治疗DPP-IV介导的疾病，特别是2型糖尿病。

8. 发明申请

WO2007139856A2 HETEROBICYCLIC METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：异源环氧化酶抑制剂
公开(公告)号：WO2007139856A2
公开(公告)日：2007-12-06
申请号：PCT/US2007/012337
申请日：2007-05-22
申请人： ALANTOS PHARMACEUTICALS, INC. , GEGE, Christian , KROTH, Heiko , STEENECK, Christoph , RICHTER, Frank , HOCHGUERTEL, Matthias , NOLTE, Bert , VAN VELDHUIZEN, Joshua , ESSERS, Michael , GALLAGHER, Brian , FEUERSTEIN, Tim , ARNDT, Torsten , SCHNEIDER, Matthias , WU, Xinyuan , TAVERAS, Arthur, G. , BLUHM, Harald , SUCHOLEIKI, Irving , BIESINGER, Ralf , DENG, Hongbo
发明人： GEGE, Christian , KROTH, Heiko , STEENECK, Christoph , RICHTER, Frank , HOCHGUERTEL, Matthias , NOLTE, Bert , VAN VELDHUIZEN, Joshua , ESSERS, Michael , GALLAGHER, Brian , FEUERSTEIN, Tim , ARNDT, Torsten , SCHNEIDER, Matthias , WU, Xinyuan , TAVERAS, Arthur, G. , BLUHM, Harald , SUCHOLEIKI, Irving , BIESINGER, Ralf , DENG, Hongbo
IPC分类号： C07D487/04 , A61K31/519 , A61P19/02
CPC分类号： C07D487/04
摘要： The present invention relates generally to amide group containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic MMP- 13 inhibiting and MMP-3 inhibiting compounds, that exhibit an increased potency in relation to currently known MMP- 13 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含酰胺基的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制剂化合物。更具体地说，本发明提供了一类新型的杂双环MMP-13抑制和MMP-3抑制化合物，其与当前已知的MMP-13和MMP-3抑制剂相比表现出增加的效力。

9. 发明申请

WO2008063669A1 HETEROBICYCLIC MATRIX METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：异源基质金属蛋白酶抑制剂
公开(公告)号：WO2008063669A1
公开(公告)日：2008-05-29
申请号：PCT/US2007/024364
申请日：2007-11-20
申请人： ALANTOS PHARMACEUTICALS HOLDING, INC. , BLUHM, Harald , HOCHGÜRTEL, Matthias , KROTH, Heiko , ESSERS, Michael , GEGE, Christian , RICHTER, Frank , TAVERAS, Arthur
发明人： BLUHM, Harald , HOCHGÜRTEL, Matthias , KROTH, Heiko , ESSERS, Michael , GEGE, Christian , RICHTER, Frank , TAVERAS, Arthur
IPC分类号： C07D487/04 , C07D495/04 , A61K31/495 , A61K31/53 , A61P35/00 , A61P29/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention relates generally to amide containing heterobicyclic containing pharmaceutical agents, and in particular, to amide containing heterobicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors.
摘要翻译：本发明一般涉及含酰胺的含杂双环的药剂，特别涉及含酰胺的杂双环金属蛋白酶抑制化合物。更具体地说，本发明提供了一类新型的杂双环MMP-3和/或MMP-13抑制化合物，与目前已知的MMP-13和MMP-3抑制剂相比，其表现出增加的效力和选择性。

10. 发明申请

WO2003034071A2 A METHOD OF FORMING A DYNAMIC COMBINATORIAL LIBRARY USING A SCAFFOLD 审中-公开
标题翻译：使用SCAFFOLD形成动态组合图书馆的方法
公开(公告)号：WO2003034071A2
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011520
申请日：2002-10-15
申请人： THERASCOPE AG , STEENECK, Christoph , ELISEEV, Alexey, V. , HOCHGUERTEL, Matthias , KROTH, Heiko
发明人： STEENECK, Christoph , ELISEEV, Alexey, V. , HOCHGUERTEL, Matthias , KROTH, Heiko
IPC分类号： G01N33/68
CPC分类号： C40B30/04 , C07C233/52 , C07C279/16 , C07C2601/16 , C07K1/047 , C07K7/64 , C12Q1/34 , G01N33/6845 , G01N2333/924 , G01N2500/20
摘要： The present invention relates to a method of forming a library of components which are potentially capable of binding to a target, which method comprises i) selecting a plurality of molecules carrying a functionality which may interact with a binding site of the said target, said molecules furthermore having a linking group which is capable of interacting with other linking groups under the formation of reversible bonds; ii) selecting a scaffold carrying two or more linking groups which are capable of interacting with the linking groups on the compound carrying a functionality; iii) reacting the scaffold and the molecules carrying the functionality in the presence of the target, under conditions where a formation of reversible bonds between the functionalities on the scaffold and on the molecules carrying a functionality occurs. In one embodiment of the present invention, the scaffold is designed to potentially interact with a binding site of known structure in a known target. The design, or pre-tailoring, of the scaffold will occur with respect to its size, three dimensional structure and/or flexibility. In a further embodiment of the present invention, the scaffold is designed to permit a screening against targets having a binding site of unknown structure, in particular to find components which are active in protein-protein-interactions.
摘要翻译：本发明涉及形成潜在能够结合靶标的组分文库的方法，该方法包括：i）选择携带可与所述靶的结合位点相互作用的官能团的多个分子，所述分子此外具有能够在可逆键形成下与其它连接基团相互作用的连接基团; ii）选择携带两个或更多个能够与携带功能的化合物上的连接基团相互作用的连接基团的支架; iii）在靶标存在下使支架和携带官能团的分子在支架上的官能团和携带官能团的分子之间形成可逆键的条件下进行反应。在本发明的一个实施方案中，支架被设计成潜在地与已知靶标中已知结构的结合位点相互作用。支架的设计或预先裁剪将相对于其尺寸，三维结构和/或柔性进行。在本发明的另一个实施方案中，支架被设计成允许筛选具有未知结构的结合位点的靶，特别是找到在蛋白质 - 蛋白质相互作用中有活性的成分。

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