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1.发明授权C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 有权C末端修饰（N-取代的）-2-吲哚基二肽作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂公开(公告)号：US06489353B2
公开(公告)日：2002-12-03
申请号：US09747317
申请日：2000-12-20
申请人： Donald S. Karanewsky , Xu Bai
发明人： Donald S. Karanewsky , Xu Bai
IPC分类号： A61K31404
CPC分类号： C07K5/0202 , A61K38/00
摘要： This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.
摘要翻译： 本发明涉及新的（N-取代的）吲哚ICE / ced-3抑制剂化合物。 本发明还涉及这种吲哚化合物的药物组合物，以及这些组合物在治疗患有炎性，自身免疫和神经变性疾病的患者中用于预防缺血性损伤的用途。
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2.发明授权Treatment of infectious disease using interleukin-1&bgr;-converting enzyme (ICE)/CED-3 family inhibitors 有权使用白细胞介素-1β转换酶（ICE）/ CED-3家族抑制剂治疗传染病公开(公告)号：US06610683B2
公开(公告)日：2003-08-26
申请号：US10007632
申请日：2001-11-13
IPC分类号： A61K3155
CPC分类号： A61Q17/00 , A01N1/0215 , A61K8/492 , A61K31/404 , A61K31/55 , A61K2800/75 , A61Q17/04 , C07K5/0202 , Y02A50/463
摘要： The present invention provides methods and compositions for treating infectious disease or suppressing inflammation associated therewith or ameliorating symptoms thereof by the suppression of the activity of a member of the interleukin-1&bgr;-converting enzyme (ICE)/CED-3 family of proteases. Also provided are compositions useful for these purposes. Exemplary compounds useful in the methods of the invention are provided herein.
摘要翻译： 本发明提供了通过抑制白细胞介素-1β转换酶（ICE）/ CED-3家族蛋白酶的活性来治疗感染性疾病或抑制与之相关的炎症或改善其症状的方法和组合物。 还提供了可用于这些目的的组合物。 本文提供了可用于本发明方法的示例性化合物。
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3.发明授权C-terminal modified (n-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 失效作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂的C-末端修饰（n-取代）-2-吲哚基二肽
公开(公告)号：US5869519A
公开(公告)日：1999-02-09
申请号：US767175
申请日：1996-12-16
申请人： Donald S. Karanewsky , Xu Bai
发明人： Donald S. Karanewsky , Xu Bai
IPC分类号： A01N1/02 , A61K38/00 , A61K38/55 , C07K5/02 , A61K31/40 , A61K31/405 , C07D209/14 , C07D209/42
CPC分类号： A61K38/55 , A01N1/0226 , C07K5/0202 , A61K38/00
摘要： This invention is directed to novel (N-substituted)indole ICE-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.
摘要翻译： 本发明涉及新的（N-取代）吲哚ICE-抑制剂化合物。 本发明还涉及这种吲哚化合物的药物组合物，以及这些组合物在治疗患有炎性，自身免疫性和神经变性疾病的患者中的用途，用于预防缺血性损伤，以及用于保存经受 移植手术。
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4.发明授权Treatment of inflammation-associated disorders using interleukin-1&bgr;-converting enzyme (ICE)/CED-3 family inhibitors 有权使用白细胞介素-1β转换酶（ICE）/ CED-3家族抑制剂治疗炎症相关疾病公开(公告)号：US06693096B2
公开(公告)日：2004-02-17
申请号：US10208729
申请日：2002-07-29
IPC分类号： A61K3155
CPC分类号： A61Q17/00 , A01N1/0215 , A61K8/492 , A61K31/404 , A61K31/55 , A61K2800/75 , A61Q17/04 , C07K5/0202 , Y02A50/463
摘要： The present invention provides methods and compositions for preventing and treating inflammation-associated disorders or ameliorating symptoms thereof by the suppression of the activity of a member of the interleukin-1&bgr;-converting enzyme (ICE)/CED-3 family of proteases. Also provided are compositions useful for these purposes. Exemplary compounds useful in the methods of the invention are provided herein.
摘要翻译： 本发明提供了通过抑制白细胞介素-1β转换酶（ICE）/ CED-3家族蛋白酶的活性来预防和治疗炎症相关疾病或改善其症状的方法和组合物。 还提供了可用于这些目的的组合物。 本文提供了可用于本发明方法的示例性化合物。
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5.发明授权公开(公告)号：US06531467B2
公开(公告)日：2003-03-11
申请号：US09982123
申请日：2001-10-16
申请人： Lawrence C. Fritz , Kevin J. Tomaselli , Donald S. Karanewsky , Steven D. Linton , Xu Bai , Dominic F. Montisano , David Higgins
发明人： Lawrence C. Fritz , Kevin J. Tomaselli , Donald S. Karanewsky , Steven D. Linton , Xu Bai , Dominic F. Montisano , David Higgins
IPC分类号： A61K3155
CPC分类号： A61K31/404 , A01N1/0226 , A61K8/492 , A61K38/55 , A61K2800/75 , A61Q19/00 , C07K5/0202
摘要： The present invention provides methods for expanding and increasing survival of hematopoietic cell populations, for prolonging viability of an organ for transplantation, and enhancing bioproduction, using interleukin-1&bgr;-converting enzyme (ICE)/CED-3 family inhibitors. Exemplary compounds useful in the methods of the invention are provided herein.
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6.发明授权C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 失效C末端修饰（N-取代的）-2-吲哚基二肽作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂
公开(公告)号：US5877197A
公开(公告)日：1999-03-02
申请号：US928989
申请日：1997-09-12
申请人： Donald S. Karanewsky , Xu Bai
发明人： Donald S. Karanewsky , Xu Bai
IPC分类号： A01N1/02 , A61K38/00 , A61K38/55 , C07K5/02 , A61K31/405 , C07D209/14 , C07D231/02 , C07F9/28
CPC分类号： A61K38/55 , C07K5/0202
摘要： This invention is directed to novel (N-substituted)indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, and for the treatment of ischemic injury.
摘要翻译： 本发明涉及新的（N-取代的）吲哚ICE / ced-3抑制剂化合物。 本发明还涉及这种吲哚化合物的药物组合物，以及这些组合物在治疗患有炎症，自身免疫和神经变性疾病的患者中的用途以及用于治疗缺血性损伤。
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7.发明授权C-terminal modified (N-substituted)-2-indolyl dipeptides as inhibitors of the ICE/ced-3 family of cysteine proteases 失效C末端修饰（N-取代的）-2-吲哚基二肽作为ICE / ced-3家族半胱氨酸蛋白酶的抑制剂公开(公告)号：US06184244B2
公开(公告)日：2001-02-06
申请号：US09345724
申请日：1999-06-30
申请人： Donald S. Karanewsky , Xu Bai
发明人： Donald S. Karanewsky , Xu Bai
IPC分类号： A61K3140
CPC分类号： C07K5/0202 , A61K38/00
摘要： This invention is directed to novel (N-substituted) indole ICE/ced-3-inhibitor compounds. The invention is also directed to pharmaceutical compositions of such indole compounds, plus the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury.
摘要翻译： 本发明涉及新的（N-取代的）吲哚ICE / ced-3抑制剂化合物。 本发明还涉及这种吲哚化合物的药物组合物，以及这些组合物在治疗患有炎性，自身免疫和神经变性疾病的患者中用于预防缺血性损伤的用途。
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8.发明授权Method of improving stability of sweet enhancer and composition containing stabilized sweet enhancer 有权提高甜味增强剂和含有稳定的甜味增强剂的组合物的稳定性的方法公开(公告)号：US09000054B2
公开(公告)日：2015-04-07
申请号：US13208594
申请日：2011-08-12
CPC分类号： A23L1/22678 , A23L2/56 , A23L27/2054 , A23L27/88 , A23V2002/00 , A61K47/22 , A61K47/26
摘要： The present invention includes methods of stabilizing one or more sweet enhancers when they are exposed to a light source as well as liquid compositions containing one or more sweet enhancers and one or more photostabilizers.
摘要翻译： 本发明包括当一种或多种增甜剂暴露于光源时稳定一种或多种甜味增强剂的方法以及含有一种或多种甜味增强剂和一种或多种光稳定剂的液体组合物。
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公开(公告)号：US08633186B2
公开(公告)日：2014-01-21
申请号：US12663634
申请日：2008-06-03
申请人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Xiaodong Li , Feng Zhang , Guy Servant , Qing Chen , Vincent Darmohusodo , Richard Fine , Joseph R. Fotsing , Jeffrey Robert Hammaker , Xinshan Kang , Rachel D. A. Kimmich , Boris Klebansky , Haitian Liu , Goran Petrovic , Marketa Rinnova , Sara Adamski-Werner , Jeffrey Yamamoto , Hong Zhang , Albert Zlotnik , Karen Zoller
发明人： Catherine Tachdjian , Donald S. Karanewsky , Xiao-Qing Tang , Xiaodong Li , Feng Zhang , Guy Servant , Qing Chen , Vincent Darmohusodo , Richard Fine , Joseph R. Fotsing , Jeffrey Robert Hammaker , Xinshan Kang , Rachel D. A. Kimmich , Boris Klebansky , Haitian Liu , Goran Petrovic , Marketa Rinnova , Sara Adamski-Werner , Jeffrey Yamamoto , Hong Zhang , Albert Zlotnik , Mark Zoller
IPC分类号： C07D239/95 , C07D285/16 , A61K31/517 , A61K31/54
CPC分类号： A61K31/495 , A61K31/517 , A61K31/519 , C07D239/80 , C07D239/93 , C07D239/95 , C07D239/96 , C07D285/15 , C07D405/12 , C07D417/04 , C07D417/12 , C07D487/04 , C07D491/04 , C07D495/04 , C07D495/14 , C07D513/04 , C07D513/20 , C07H17/00 , G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2500/04 , G06F19/16 , G06F19/18
摘要： The present invention includes methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors, and modifiers capable of modulating chemosensory receptors and their ligands. The present invention also includes modifiers of chemosensory receptors and their ligands having Formula (I), its subgenus, and specific compounds. Furthermore, the present invention includes ingestible compositions comprising the modifiers of chemosensory receptors and their ligands and methods of using the modifiers of chemosensory receptors and their ligands to enhance the sweet taste of an ingestible composition or treat a condition associated with a chemosensory receptor. In addition, the present invention include processes for preparing the modifiers of chemosensory receptors and their ligands.
摘要翻译： 本发明包括用于鉴定化学感受器及其配体的调节剂的方法，例如通过确定测试实体是否适合与化学感应受体的金星蝇捕获区域内的一个或多个相互作用位点相互作用，以及能够调节化学感应受体 及其配体。 本发明还包括具有式（I），其亚属和特定化合物的化学感应受体及其配体的改性剂。 此外，本发明包括含有化学感应受体调节剂及其配体的可摄入组合物，以及使用化学感应受体及其配体改性剂增强可摄入组合物的甜味或治疗与化学感觉受体相关的病症的方法。 此外，本发明包括制备化学感受器及其配体的改性剂的方法。
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10.发明申请COMPOUNDS THAT INHIBIT (BLOCK) BITTER TASTE IN COMPOSITION AND METHODS OF MAKING SAME 审中-公开化合物组合物中的抑制（块状）双酚A的化合物及其制备方法公开(公告)号：US20130183252A1
公开(公告)日：2013-07-18
申请号：US13370832
申请日：2012-02-10
申请人： Xiaodong LI , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
发明人： Xiaodong LI , Andrew Patron , Catherine Tachdjian , Hong Xu , Qing Li , Alexey Pronin , Guy Servant , Lan Zhang , Thomas Brady , Vincent Darmohusodo , Melissa Arellano , Victor Selchau , Brett Weylan Ching , Donald S. Karanewsky , Paul Brust , Jing Ling , Wen Zhao , Chad Priest
IPC分类号： C07C311/17 , C07D223/18 , A61K8/46 , A61Q11/00 , C07D213/71 , C07D333/34 , C07D317/58 , A61K8/49 , C07C311/16 , C07C311/19 , C07C311/46 , C07C311/18 , C07C233/73 , C07D333/20 , C07D213/42 , C07D217/08 , A23L1/22 , C07D307/52
CPC分类号： C07C311/17 , A23L27/86 , A61K8/46 , A61K8/466 , A61K8/4933 , A61K8/494 , A61K8/4973 , A61K8/498 , A61K8/4986 , A61K31/135 , A61K31/4439 , A61K31/485 , A61K31/60 , A61K31/704 , A61K45/06 , A61Q11/00 , C07C233/73 , C07C311/04 , C07C311/13 , C07C311/16 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/21 , C07C311/29 , C07C311/46 , C07C323/49 , C07C335/16 , C07C335/18 , C07D213/42 , C07D213/71 , C07D217/08 , C07D223/18 , C07D307/14 , C07D307/52 , C07D317/58 , C07D333/20 , C07D333/34 , A61K2300/00
摘要： The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.
摘要翻译： 本发明涉及T2R味觉受体家族中的特定人类味觉受体对存在于例如咖啡中的特定苦味化合物的反应的发现。 此外，本发明涉及含有作为苦味抑制剂的特定化合物和组合物的发现，以及其作为例如咖啡和咖啡风味食品，饮料和药物中的苦味抑制剂或风味调节剂的用途。 此外，本发明涉及一种拮抗多种不同人类T2R的化合物的发现及其在测定中的用途以及用于摄取人类和动物的组合物中的苦味阻滞剂。
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