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1.发明授权Collagenase-1 and stromelysin-1 inhibitors, pharmaceutical compositions comprising same and methods of their use 失效胶原酶-1和基质溶素-1抑制剂，包含其的药物组合物及其使用方法公开(公告)号：US06271232B1
公开(公告)日：2001-08-07
申请号：US09350878
申请日：1999-07-09
IPC分类号： A61K31495
CPC分类号： C07D241/08
摘要： Novel inhibitors of metalloproteases, in particular collagenase-1 and stromelysin-1, are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.
摘要翻译： 公开了新型金属蛋白酶抑制剂，特别是胶原酶-1和基质溶素-1。 这些化合物可用于治疗或控制涉及组织分解的疾病状态或病症的药物组合物和方法，例如类风湿性关节炎。
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2.发明授权
公开(公告)号：US5817751A
公开(公告)日：1998-10-06
申请号：US731362
申请日：1996-10-11
IPC分类号： C07B61/00 , C07D241/08 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , G01N33/543 , G01N33/68 , C07K1/04 , C07K5/12
CPC分类号： C07D401/06 , C07D241/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , C40B40/00 , G01N33/54353 , G01N33/68
摘要： The present invention relates to the areas of organic and medicinal chemistry. More specifically, the present invention is concerned with combinatorial and solid phase methods for the synthesis of diverse diketopiperazine derivatives, and the use of such methods to create libraries of diverse diketopiperazine derivatives. The present invention has application in the areas of chemical synthesis, the screening for new diketopiperazine derivatives having beneficial medical properties and the use of such screening to provide compositions and methods including diketopiperazine derivatives for treating disease.
摘要翻译： 本发明涉及有机和药物化学领域。 更具体地，本发明涉及用于合成各种二酮哌嗪衍生物的组合和固相方法，以及使用这些方法来制备多种二酮哌嗪衍生物的文库。 本发明可用于化学合成，筛选具有有益医学性质的新型二酮哌嗪衍生物的领域，以及使用这种筛选来提供包括用于治疗疾病的二酮哌嗪衍生物的组合物和方法。
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3.发明授权Inhibitors of metalloproteases pharmaceutical compositions comprising same and methods of their use 失效金属蛋白酶抑制剂包含其的药物组合物及其使用方法
公开(公告)号：US5990112A
公开(公告)日：1999-11-23
申请号：US670713
申请日：1996-06-18
IPC分类号： C07B61/00 , C07D241/08 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , A61K31/495
CPC分类号： C07D401/06 , C07D241/08 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D409/06 , C07D409/14 , C40B40/00
摘要： Novel inhibitors of metalloproteases are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis.
摘要翻译： 公开了新的金属蛋白酶抑制剂。 这些化合物可用于治疗或控制涉及组织分解的疾病状态或病症的药物组合物和方法，例如类风湿性关节炎。
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4.发明授权Collagenase-1 and stromelysin-1 inhibitors, pharmaceutical compositions comprising same and methods of their use 失效胶原酶-1和基质溶素-1抑制剂，包含其的药物组合物及其使用方法
公开(公告)号：US5932579A
公开(公告)日：1999-08-03
申请号：US665603
申请日：1996-06-18
IPC分类号： C07D241/08 , A61K31/495 , C07D237/00 , C07D241/04 , C07D241/36
CPC分类号： C07D241/08
摘要： Novel inhibitors of metalloproteases, in particular collagenase-1 and stromelysin-1, are disclosed. Such compounds are useful in pharmaceutical compositions and methods for treating or controlling disease states or conditions which involve tissue breakdown, such as rheumatoid arthritis. ##STR1##
摘要翻译： 公开了金属蛋白酶的新型抑制剂，特别是胶原酶-1和基质溶素-1。 这些化合物可用于治疗或控制涉及组织分解的疾病状态或病症的药物组合物和方法，例如类风湿性关节炎。
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公开(公告)号：US08691187B2
公开(公告)日：2014-04-08
申请号：US13035405
申请日：2011-02-25
申请人： Anna Katrin Szardenings , Wei Zhang , Dhanalakshmi Kasi , Anjana Sinha , Umesh B. Gangadharmath , Joseph C. Walsh
发明人： Anna Katrin Szardenings , Wei Zhang , Dhanalakshmi Kasi , Anjana Sinha , Umesh B. Gangadharmath , Joseph C. Walsh
IPC分类号： A61K49/00
CPC分类号： C07D235/04 , A61K51/04 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/02 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D471/04 , C07D487/04
摘要： Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
摘要翻译： 式（I） - （V）的成像剂和用于检测神经障碍的方法包括向需要的患者施用能够结合tau蛋白和＆amp;淀粉样蛋白肽的式（I） - （V）化合物。 本发明还涉及成像A＆bgr的方法; 和tau聚集体，其包括引入可检测量的包含放射性标记的式（I） - （V）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。
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6.发明授权Compounds with matrix-metalloproteinase inhibitory activity and imaging agents thereof 有权具有基质金属蛋白酶抑制活性的化合物及其成像剂公开(公告)号：US09023318B2
公开(公告)日：2015-05-05
申请号：US13849646
申请日：2013-03-25
申请人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
发明人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
IPC分类号： A61K51/00 , A61M36/14 , C07D403/14 , C07D405/14 , C07D249/04 , C07D309/12 , C07D213/42
CPC分类号： C07D403/14 , C07D213/42 , C07D249/04 , C07D309/12 , C07D405/14
摘要： Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.
摘要翻译： 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。
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7.发明申请Compounds With Matrix-Metalloproteinase Inhibitory Activity and Imaging Agents Thereof 有权具有基质金属蛋白酶抑制活性和成像剂的化合物公开(公告)号：US20130217887A1
公开(公告)日：2013-08-22
申请号：US13849646
申请日：2013-03-25
申请人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
发明人： Gang Chen , Umesh B. Gangadharmath , Dhanalakshmi Kasi , Harmuth C. Kolb , Changhui Liu , Anjana Sinha , Anna Katrin Szardenings , Joseph C. Walsh , Eric Wang , Chul Yu , Wei Zhang , Klaus Kopka , Guenter Haufe , Michael Schaefers , Verena Hugenberg , Stefan Wagner , Sven Hermann , Hans-Joerg Breyholz , Andreas Faust
IPC分类号： C07D403/14 , C07D249/04 , C07D405/14
CPC分类号： C07D403/14 , C07D213/42 , C07D249/04 , C07D309/12 , C07D405/14
摘要： Novel compounds and pharmaceutical compositions having MMP inhibitory activity are disclosed, which have been found to be particularly useful in the prevention, treatment and diagnostic imaging of diseases associated with an unpaired activity of MMP, amongst others MMP-2, MMP-8, MMP-9 and/or MMP-13 to name a few. The compounds of the present invention are useful for the prevention, the treatment and the in vivo diagnostic imaging of a range of disease states (inflammatory, malignant and degenerative diseases) where specific matrix metalloproteinases are known to be involved.
摘要翻译： 已经公开了具有MMP抑制活性的新型化合物和药物组合物，其已经被发现特别可用于预防，治疗和诊断成像与MMP的非配对活性相关的疾病，其中MMP-2，MMP-8，MMP- 9和/或MMP-13等等。 本发明的化合物可用于预防，治疗和体内诊断成像的一系列疾病状态（炎性，恶性和退行性疾病），其中已知特定的基质金属蛋白酶涉及。
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公开(公告)号：US08491869B2
公开(公告)日：2013-07-23
申请号：US12661777
申请日：2010-03-23
申请人： Umesh B. Gangadharmath , Hartmuth C. Kolb , Peter J. H. Scott , Joseph C. Walsh , Wei Zhang , Anna Katrin Szardenings , Anjana Sinha , Gang Chen , Eric Wang , Vani P. Mocharia , Chul Yu , Changhui Liu , Daniel Kurt Cashion , Dhanalakshmi Kasi
发明人： Umesh B. Gangadharmath , Hartmuth C. Kolb , Peter J. H. Scott , Joseph C. Walsh , Wei Zhang , Anna Katrin Szardenings , Anjana Sinha , Gang Chen , Eric Wang , Vani P. Mocharia , Chul Yu , Changhui Liu , Daniel Kurt Cashion , Dhanalakshmi Kasi
CPC分类号： A61K51/0455 , A61K51/04 , A61K51/0453 , A61K51/0459 , A61K51/0463 , C07B59/002 , C07D215/06 , C07D235/14 , C07D277/62 , C07D401/04 , C07D403/06 , C07D413/10 , C07D413/14 , C07D487/04
摘要： Imaging agents of formula (I) and methods for detecting neurological disorders comprising administering ti a patient in need compounds of formula (I) capable of binding to tau proteins and β-amyloid peptides are presented herein. The invention also relates to methods of imaging Aβ and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formula (I) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.
摘要翻译： 式（I）的成像剂和用于检测神经障碍的方法包括给予需要能够结合tau蛋白和β-淀粉样肽的式（I）化合物的化合物。 本发明还涉及成像Abeta和tau聚集体的方法，包括引入可检测量的包含放射性标记的式（I）化合物的药物制剂，并检测患者中与淀粉样蛋白沉积物和/或tau蛋白相关的标记化合物。 这些方法和组合使得临床前诊断和监测AD和其他神经障碍的进展。
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9.发明授权公开(公告)号：US08389514B2
公开(公告)日：2013-03-05
申请号：US12677789
申请日：2008-09-11
申请人： Bei Li , Anna Katrin Szardenings
发明人： Bei Li , Anna Katrin Szardenings
IPC分类号： C07D498/06 , A61K31/5383
CPC分类号： C07D498/06
摘要： Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.
摘要翻译： 本文提供氨基喹诺酮及其药学上可接受的衍生物。 在某些实施方案中，本文提供了用于治疗，预防或改善GSK-3介导的疾病的化合物，组合物和方法。
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公开(公告)号：US08367673B2
公开(公告)日：2013-02-05
申请号：US12412837
申请日：2009-03-27
申请人： Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
发明人： Alan David Borthwick , Richard Jonathan Hatley , Deirdre Mary Bernadette Hickey , John Liddle , David George Hubert Livermore , Andrew McMurtrie Mason , Neil Derek Miller , Fabrizio Nerozzi , Steven Leslie Sollis , Anna Katrin Szardenings , Paul Graham Wyatt
IPC分类号： A61K31/497 , A61K31/4965
CPC分类号： C07D241/08 , A61K38/00 , C07D401/10 , C07D403/06 , C07D413/10 , C07D417/06 , C07K5/06078 , C07K5/06191
摘要： A method of treating or preventing diseases or conditions mediated through the action of oxytocin which comprises administering to a human in need thereof of an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
摘要翻译： 一种治疗或预防通过催产素作用介导的疾病或病症的方法，其包括向有需要的人施用有效量的式（I）化合物或其药学上可接受的盐。
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