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1. 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。

2. 发明申请

WO2008063670A1 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：WO2008063670A1
公开(公告)日：2008-05-29
申请号：PCT/US2007/024365
申请日：2007-11-20
申请人： ALANTOS PHARMACEUTICALS HOLDING, INC. , HOCHGÜRTEL, Matthias , BLUHM, Harald , ESSERS, Michael , KROTH, Heiko , GEGE, Christian , TAVERAS, Arthur
发明人： HOCHGÜRTEL, Matthias , BLUHM, Harald , ESSERS, Michael , KROTH, Heiko , GEGE, Christian , 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 provides a new class of heterobicyclic MMP-3 and/or MMP-13 inhibiting compounds, of Formula (I) that exhibit an increased potency and selectivity in relation to currently known MMP-13 and MMP-3 inhibitors. The heterobicyclic metalloprolease inhibiting compounds of the present invention may be used in the treatment of metalloprotease mediated diseases, such as rheumatoid arthritis, osteoarthritis, abdominal aortic aneurysm, cancer, inflammation, atherosclerosis, multiple sclerosis, chronic obstructive pulmonary disease, ocular diseases, neurological diseases, psychiatric diseases, thrombosis, bacterial infection, Parkinson's disease, fatigue, tremor, diabetic retinopathy, vascular diseases of the retina, aging, dementia, cardiomyopathy, renal tubular impairment, diabetes, psychosis, dyskinesia, pigmentary abnormalities, deafness, inflammatory and fibrotic syndromes, intestinal bowel syndrome, allergies, Alzheimer's disease, arterial plaque formation, periodontal, viral infection, stroke, cardiovascular disease, reperfusion injury, trauma, chemical exposure or oxidative damage to tissues, wound healing, hemorroid, skin beautifying, pain, inflammatory pain, bone pain and joint pain.
摘要翻译：本发明提供了与目前已知的MMP-13和MMP-3抑制剂相比显示增加的效力和选择性的新一类式（I）的杂双环MMP-3和/或MMP-13抑制化合物。本发明的杂双环金属蛋白酶抑制化合物可用于治疗金属蛋白酶介导的疾病，例如类风湿性关节炎，骨关节炎，腹主动脉瘤，癌症，炎症，动脉粥样硬化，多发性硬化，慢性阻塞性肺病，眼病，神经系统疾病精神疾病，血栓形成，细菌感染，帕金森病，疲劳，震颤，糖尿病性视网膜病变，视网膜血管疾病，衰老，痴呆，心肌病，肾小管损伤，糖尿病，精神病，运动障碍，色素异常，耳聋，炎性和纤维化综合征肠道综合征，过敏症，阿尔茨海默病，动脉斑块形成，牙周病，病毒感染，中风，心血管疾病，再灌注损伤，创伤，化学暴露或对组织的氧化损伤，伤口愈合，血红细胞，皮肤美化，疼痛，炎性疼痛，骨痛和关节疼痛。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明申请

WO2003033437A2 A METHOD OF FORMING NEURAMINIDASE INHIBITORS BY DYNAMIC COMBINATORIAL CHEMISTRY AND COMPOUNDS OBTAINED 审中-公开
标题翻译：通过动态组合化学和形成化合物形成神经酰胺糖苷酶抑制剂的方法
公开(公告)号：WO2003033437A2
公开(公告)日：2003-04-24
申请号：PCT/EP2002/011526
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： C07B61/00
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 compounds according to the formula (I), wherein the dotted line denotes a double bond which is present in one of the two possible positions; R 1 to R 4 are independently of each other selected from the group consisting of: hydrogen, C 1 -C 20 alkyl groups, C 2 -C 20 -alkenyl groups, C 4 -C 20 aryl groups, C 5 -C 20 -aralkyl groups and C 5 -C 20 -alkaryl groups, all of which groups all can contain one or more hetero atoms from the group consisting of N, O, and S, and which groups can carry one or more substituents from the group consisting of hydroxyl groups and C 1 -C 4 -alkyl ester groups; or one of the substituents NR 1 R 2 and NR 3 R 4 is a guanidino group of the formula NR 5 -C(NR 6 R 7 )=NR 8 in which the substituents R 5 to R 8 independently of each other have the meaning given above for the substituents R 1 to R 4 ; R 9 is a C 1 -C 4 -alkyl group, or a physiologically acceptable salt or solvate thereof in any stereoisomenc form or mixtures thereof in any ratio. A further object of the invention is a method of forming a library of components which are potentially capable of binding to neuraminidase, in particular influenza neuraminidase, which method comprises i) selecting a plurality of molecules carrying a functionality which may interact with a binding site of neuraminidase, said molecules furthermore having a linking group which is capable of interacting with other linking groups under the formation of reversible bonds; ii) reacting the molecules carrying the functionality with a molecule according to formula (I) as defined in claim 1 in the presence of the target, under conditions where a formation of reversible bonds between the linking groups on the molecule (I) and on the molecules carrying a functionality occurs.
摘要翻译：本发明涉及式（I）化合物，其中虚线表示存在于两个可能位置之一中的双键; R 1至R 4彼此独立地选自：氢，C 1 -C 20烷基，C 2 -C 20 - 烯基，C 4 -C 20芳基，C 5 -C 20 - 芳烷基和C 5 -C 20烷芳基，所有这些基团都可以含有一个或多个来自N，O和S的杂原子，并且哪些基团可以携带一个或多个取代基，其由羟基和C 1 -C 4 - 烷基酯基; 或取代基NR 1 R 2和NR 3 R 4之一是式NR 5 -C（NR 6 R 7）= NR 8的胍基，其中取代基R 5至R 8彼此独立地具有上面对取代基R 1至R 4给出的含义; R 9是以任何比例的任何立体异构形式或其混合物的C 1 -C 4 - 烷基或其生理上可接受的盐或溶剂合物。本发明的另一个目的是形成潜在地能够结合神经氨酸酶，特别是流感神经氨酸酶的组分文库的方法，该方法包括：i）选择携带官能团的多个分子，其可以与所述分子还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）在靶的存在下，在分子（I）上的连接基团和在分子（I）上形成可逆键的条件下，使带有官能团的分子与如权利要求1所定义的式（I）携带功能的分子发生。

8. 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。

9. 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。

10. 发明申请

WO2003034071A3 A METHOD OF FORMING A DYNAMIC COMBINATORIAL LIBRARY USING A SCAFFOLD 审中-公开
公开(公告)号：WO2003034071A3
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： C07B61/00
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.

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