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1. 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。

2. 发明申请

WO2007079199A2 SUBSTITUTED BIS-AMIDE METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：取代的双胺金属蛋白酶抑制剂
公开(公告)号：WO2007079199A2
公开(公告)日：2007-07-12
申请号：PCT/US2006/049521
申请日：2006-12-28
申请人： ALANTOS PHARMACEUTICALS, INC. , SUCHOLEIKI, Irving , POWERS, Timothy , GEGE, Christian , BLUHM, Harald , DODD, Rory , DENG, Hongbo , WU, Xinyuan , STEENECK, Christoph
发明人： SUCHOLEIKI, Irving , POWERS, Timothy , GEGE, Christian , BLUHM, Harald , DODD, Rory , DENG, Hongbo , WU, Xinyuan , STEENECK, Christoph
IPC分类号： C07D239/28 , C07D403/12 , C07D409/12 , C07D417/12
CPC分类号： C07D403/12 , C07D239/28 , C07D409/12 , C07D417/12
摘要： This invention relates to substituted bis-amide pyrimidine compounds of Formula (I), which are useful for the treatment of metalloprotease mediated diseases, in particular MMP-13 related diseases.
摘要翻译：本发明涉及式（I）的取代双酰胺嘧啶化合物，其可用于治疗金属蛋白酶介导的疾病，特别是MMP-13相关疾病。

3. 发明申请

WO2006128184A3 PYRIMIDINE OR TRIAZINE FUSED BICYCLIC METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：吡嗪二酮或二亚磷酸双金属金属蛋白酶抑制剂
公开(公告)号：WO2006128184A3
公开(公告)日：2007-03-08
申请号：PCT/US2006020970
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

WO2011107248A1 NOVEL COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (RORγ GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASE 审中-公开
标题翻译：用于调节ORPHAN核受体RAR相关ORPAN受体 - 游离（ROR？GAMMA，NR1F3）活性和治疗慢性炎症和自身免疫疾病的新型化合物
公开(公告)号：WO2011107248A1
公开(公告)日：2011-09-09
申请号：PCT/EP2011/000976
申请日：2011-02-28
申请人： PHENEX PHARMACEUTICALS AG , KINZEL, Olaf , STEENECK, Christoph , KLEYMANN, Gerald , ALBERS, Michael , HOFFMANN, Thomas , KREMOSER, Claus , PEROVIC-OTTSTADT, Sanja , SCHLÜTER, Thomas
发明人： KINZEL, Olaf , STEENECK, Christoph , KLEYMANN, Gerald , ALBERS, Michael , HOFFMANN, Thomas , KREMOSER, Claus , PEROVIC-OTTSTADT, Sanja , SCHLÜTER, Thomas
IPC分类号： C07D245/06 , C07D267/22 , C07D413/10 , C07D413/12 , C07D417/12 , A61P29/00 , A61P37/00 , A61K31/395 , C07D281/18 , C07D403/12 , C07D487/04 , C07D498/04
CPC分类号： C07D267/22 , C07D245/06 , C07D281/18 , C07D403/12 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04
摘要： The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administrating these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
摘要翻译：本发明提供了用于孤儿核受体ROR的调节剂？和治疗ROR的方法？通过管理这些新的ROR来介导疾病？对需要其的人或哺乳动物的调节剂。具体地说，本发明提供式（1）的化合物及其对映异构体，非对映异构体，互变异构体，溶剂合物及其药学上可接受的盐。

5. 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.

6. 发明申请

WO2003033437A3 A METHOD OF FORMING NEURAMINIDASE INHIBITORS BY DYNAMIC COMBINATORIAL CHEMISTRY AND COMPOUNDS OBTAINED 审中-公开
公开(公告)号：WO2003033437A3
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
摘要： The present invention relates to compounds according to the formula (I) (I) 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.

7. 发明申请

WO2011020615A1 NOVEL FXR (NR1H4 ) BINDING AND ACTIVITY MODULATING COMPOUNDS 审中-公开
标题翻译：新型FXR（NR1H4）结合和活性调节化合物
公开(公告)号：WO2011020615A1
公开(公告)日：2011-02-24
申请号：PCT/EP2010/005093
申请日：2010-08-19
申请人： PHENEX PHARMACEUTICALS AG , KREMOSER, Claus , ABEL, Ulrich , STEENECK, Christoph , KINZEL, Olaf
发明人： KREMOSER, Claus , ABEL, Ulrich , STEENECK, Christoph , KINZEL, Olaf
IPC分类号： C07D249/06 , C07D261/08 , C07D413/04 , C07D413/12 , C07D413/14 , A61K31/4192 , A61K31/42 , A61K31/443 , A61K31/4439 , A61P1/16 , A61P3/10 , A61P35/00
CPC分类号： C07D261/08 , A61K31/4192 , A61K31/42 , A61K31/422 , A61K31/423 , A61K31/4439 , C07D249/06 , C07D413/04 , C07D413/12 , C07D413/14 , Y02A50/409 , Y02A50/414 , Y02A50/415
摘要： The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
摘要翻译：本发明涉及结合NR1H4受体（FXR）并作为NR1H4受体（FXR）的激动剂的化合物。本发明还涉及该化合物在制备用于通过所述化合物与所述核受体结合来治疗疾病和/或病症的药物的用途，以及合成所述化合物的方法中的用途。

8. 发明申请

WO2008063671A2 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：WO2008063671A2
公开(公告)日：2008-05-29
申请号：PCT/US2007/024368
申请日：2007-11-20
申请人： ALANTOS PHARMACEUTICALS HOLDING, INC. , NOLTE, Bert , SUCHOLEIKI, Irving , FEUERSTEIN, Tim , GALLAGHER, JR., Brian M. , WU, Xinyuan , STEENECK, Christoph , GEGE, Christian , DENG, Hongbo , VAN VELDHUIZEN, Joshua , TAVERAS, Arthur
发明人： NOLTE, Bert , SUCHOLEIKI, Irving , FEUERSTEIN, Tim , GALLAGHER, JR., Brian M. , WU, Xinyuan , STEENECK, Christoph , GEGE, Christian , DENG, Hongbo , VAN VELDHUIZEN, Joshua , TAVERAS, Arthur
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention relates generally to heterobicyclic containing pharmaceutical agents, and in particular, to heterobicyclic metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of heterobicyclic metalloprotease inhibiting compounds that exhibit an increased potency in relation to currently known metalloprotease inhibitors.
摘要翻译：本发明一般涉及含杂环的药物，特别是涉及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金属蛋白酶抑制化合物，其与当前已知的金属蛋白酶抑制剂相比表现出增加的效力。

9. 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。

10. 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。

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