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1.发明申请Novel compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORgamma, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune disease 有权用于调节孤儿核受体RAR相关孤儿受体-γ（RORgamma，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：US20130053380A1
公开(公告)日：2013-02-28
申请号：US13581961
申请日：2011-02-28
申请人： Olaf Kinzel , Christoph Steeneck , Gerald Klaymann , Michael Albers , Thomas Hoffman , Claus Kremoser , Sanja Perovic-Ottstadt , Thomas Schlüter
发明人： Olaf Kinzel , Christoph Steeneck , Gerald Klaymann , Michael Albers , Thomas Hoffman , Claus Kremoser , Sanja Perovic-Ottstadt , Thomas Schlüter
IPC分类号： A61K31/4709 , A61K31/395 , C07D413/12 , A61K31/4245 , C07D417/12 , A61K31/433 , A61K31/4178 , A61K31/4155 , C07D413/10 , A61K31/506 , A61K31/4427 , C07D498/04 , C07D413/14 , C07D401/12 , A61K31/5377 , C07D487/04 , A61K31/4188 , A61P17/00 , A61P29/00 , A61P37/00 , A61P17/06 , A61P11/06 , A61P19/02 , A61P1/00 , A61P1/04 , A61P3/10 , A61P25/00 , C07D267/22
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RORγ的调节剂和通过将这些新的RORγ调节剂施用于有需要的人或哺乳动物来治疗RORγ介导的疾病的方法。 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。
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2.发明授权Compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-gamma (RORγ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune disease 有权用于调节孤儿核受体RAR相关孤儿受体γ（RORγ，NR1F3）活性和治疗慢性炎症和自身免疫疾病的化合物公开(公告)号：US08940722B2
公开(公告)日：2015-01-27
申请号：US13581961
申请日：2011-02-28
申请人： Olaf Kinzel , Christoph Steeneck , Gerald Kleymann , Michael Albers , Thomas Hoffmann , Claus Kremoser , Sanja Perovic-Ottstadt , Thomas Schlüter
发明人： Olaf Kinzel , Christoph Steeneck , Gerald Kleymann , Michael Albers , Thomas Hoffmann , Claus Kremoser , Sanja Perovic-Ottstadt , Thomas Schlüter
IPC分类号： C07D245/06 , C07D267/22 , C07D413/10 , C07D413/12 , C07D417/12 , C07D487/04 , C07D498/04 , A61K31/395 , C07D281/18 , C07D403/12
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RORγ的调节剂和通过将这些新的RORγ调节剂施用于有需要的人或哺乳动物来治疗RORγ介导的疾病的方法。 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。
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公开(公告)号：US09139539B2
公开(公告)日：2015-09-22
申请号：US14232118
申请日：2012-07-12
申请人： Olaf Kinzel , Christoph Steeneck , Claus Kremoser
发明人： Olaf Kinzel , Christoph Steeneck , Claus Kremoser
IPC分类号： C07D261/08 , C07D413/12 , C07D413/14
CPC分类号： A61K31/4439 , A61K31/42 , A61K31/422 , C07D261/08 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of 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FXR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以及所述化合物的合成方法治疗疾病和/或病症的药物中的用途。
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公开(公告)号：US20140221659A1
公开(公告)日：2014-08-07
申请号：US14232118
申请日：2012-07-12
申请人： Olaf Kinzel , Christoph Steeneck , Claus Kremoser
发明人： Olaf Kinzel , Christoph Steeneck , Claus Kremoser
IPC分类号： C07D261/08 , C07D413/14 , C07D413/12
CPC分类号： A61K31/4439 , A61K31/42 , A61K31/422 , C07D261/08 , C07D413/12 , C07D413/14
摘要： The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of 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FXR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以及所述化合物的合成方法治疗疾病和/或病症的药物中的用途。
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公开(公告)号：US20120232116A1
公开(公告)日：2012-09-13
申请号：US13390499
申请日：2010-08-19
申请人： Claus Kremoser , Ulrich Abel , Christoph Steeneck , Olaf Kinzel
发明人： Claus Kremoser , Ulrich Abel , Christoph Steeneck , Olaf Kinzel
IPC分类号： A61K31/42 , A61K31/4439 , C07D249/06 , A61K31/4192 , C07D261/08 , C07D413/14 , C07D413/12 , A61K31/423 , A61P1/16 , A61P1/00 , A61P3/10 , A61P13/12 , A61P25/00 , A61P27/02 , A61K31/422 , A61P35/00 , A61P9/10 , C07D413/04
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。
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公开(公告)号：US08952042B2
公开(公告)日：2015-02-10
申请号：US13390499
申请日：2010-08-19
申请人： Claus Kremoser , Ulrich Abel , Christoph Steeneck , Olaf Kinzel
发明人： Claus Kremoser , Ulrich Abel , Christoph Steeneck , Olaf Kinzel
IPC分类号： C07D413/04 , C07D413/14 , C07D413/12 , C07D261/08 , C07D249/06 , A61K31/4439 , A61K31/422 , A61K31/423 , A61K31/4192 , A61K31/42
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 of formula (1): where R, A, Q and Z are defined herein, or an enantiomer, diastereomer, tautomer, solvate, prodrug or pharmaceutical acceptable salt thereof. These compounds bind to the NR1H4 receptor (FXR) and act as agonists of the NR1H4 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： 本发明涉及式（1）化合物：其中R，A，Q和Z如本文所定义，或其对映异构体，非对映异构体，互变异构体，溶剂化物，前药或药学上可接受的盐。 这些化合物结合NR1H4受体（FXR）并充当NR1H4受体（FXR）的激动剂。 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。
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7.发明授权Pyrrolo sulfonamide compounds for modulation of orphan nuclear receptor RAR-related orphan receptor-γ (ROR-γ, NR1F3) activity and for the treatment of chronic inflammatory and autoimmune diseases 有权用于调节孤儿核受体RAR相关孤儿受体γ（ROR-γ，NR1F3）活性和治疗慢性炎症和自身免疫疾病的吡咯磺酰胺化合物公开(公告)号：US08946446B2
公开(公告)日：2015-02-03
申请号：US14110702
申请日：2012-04-13
IPC分类号： C07D209/02 , C07D207/00 , C07D215/00 , C07D401/00 , C07D413/00 , A61K31/44 , A61K31/535 , A61K31/397 , A61K31/445 , A61K31/40 , C07D209/30 , C07D207/36 , C07D401/04 , C07D403/04 , C07D403/10
CPC分类号： C07D209/30 , C07D207/36 , C07D401/04 , C07D403/04 , C07D403/10
摘要： The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide 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RORy的调节剂和通过将这些新型RORY调节剂施用于有需要的人或哺乳动物来治疗RORy介导的疾病的方法。 具体地说，本发明提供式（1）的吡咯磺酰胺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。
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8.发明申请PYRROLO SULFONAMIDE COMPOUNDS FOR MODULATION OF ORPHAN NUCLEAR RECEPTOR RAR-RELATED ORPHAN RECEPTOR-GAMMA (ROR-GAMMA, NR1F3) ACTIVITY AND FOR THE TREATMENT OF CHRONIC INFLAMMATORY AND AUTOIMMUNE DISEASES 有权用于调节ORFAN核受体RAR相关ORFAN受体 - 游离（ROR-GAMMA，NR1F3）活性和用于治疗慢性炎症和自身免疫疾病的吡罗莫磺酰胺化合物公开(公告)号：US20140142082A1
公开(公告)日：2014-05-22
申请号：US14110702
申请日：2012-04-13
IPC分类号： C07D403/04 , C07D401/04 , C07D209/30 , C07D207/36
CPC分类号： C07D209/30 , C07D207/36 , C07D401/04 , C07D403/04 , C07D403/10
摘要： The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide 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RORy的调节剂和通过将这些新型RORY调节剂施用于有需要的人或哺乳动物来治疗RORy介导的疾病的方法。 具体地说，本发明提供式（1）的吡咯磺酰胺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。
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公开(公告)号：US08076330B2
公开(公告)日：2011-12-13
申请号：US13006363
申请日：2011-01-13
申请人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochgürtel , Fritz-Frieder Frickel , Arthur G. Taveras , Christoph Steeneck
发明人： Heiko Kroth , Tim Feuerstein , Frank Richter , Jürgen Boer , Michael Essers , Bert Nolte , Matthias Schneider , Matthias Hochgürtel , Fritz-Frieder Frickel , Arthur G. Taveras , Christoph Steeneck
IPC分类号： A61K31/5377 , A61K31/41 , A61K31/40 , C07D257/02 , C07D413/14
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。
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公开(公告)号：US20080176870A1
公开(公告)日：2008-07-24
申请号：US11986622
申请日：2007-11-20
申请人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
发明人： Bert Nolte , Irving Sucholeiki , Tim Feuerstein , Brian M. Gallagher , Xinyuan Wu , Christoph Steeneck , Christian Gege , Hongbo Deng , Joshua Van Veldhuizen , Arthur Taveras
IPC分类号： A61K31/495 , C07D487/04 , A61P19/02 , A61P29/00 , A61P9/10
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。
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