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1. 发明授权

US5599926A A.sub.4 B.sub.6 macrotricyclic enantioselective receptors for amino acid derivatives, and other compounds 失效
标题翻译：氨基酸衍生物的A4B6大分子对映体选择性受体和其他化合物
公开(公告)号：US5599926A
公开(公告)日：1997-02-04
申请号：US188146
申请日：1994-01-27
申请人： W. Clark Still , Julian A. Simon , Shawn D. Erickson , Seung S. Yoon , Jong-In Hong
发明人： W. Clark Still , Julian A. Simon , Shawn D. Erickson , Seung S. Yoon , Jong-In Hong
IPC分类号： C07B57/00 , C07B63/00 , C07B63/04 , C07D487/18 , C07D487/22 , C07D498/18 , C07D513/18
CPC分类号： C07D487/18 , C07B57/00 , C07B63/00 , C07B63/04 , C07D487/22 , C07D498/18 , C07D513/18 , Y02P20/55
摘要： The subject invention provides chiral receptor molecules having the structure: ##STR1## wherein A has the structure: ##STR2## and R.sub.1 and R.sub.2 are independently the same or different and are H, F, alkyl, aryl, etc.; X is CH.sub.2 or NH; Y is C.dbd.O or SO.sub.2 ; and n is 0 to about 3; which are useful for the purification of enantiomers of amino acid derivatives and other compounds. The subject invention also provides methods of preparing said receptor molecules.
摘要翻译：本发明提供具有以下结构的手性受体分子：其中A具有以下结构：R 1和R 2独立地相同或不同，为H，F，烷基，芳基等; X是CH 2或NH; Y为C = O或SO2; 且n为0至约3; 其可用于纯化氨基酸衍生物和其它化合物的对映异构体。本发明还提供了制备所述受体分子的方法。

2. 发明授权

US5571911A Method of purifying organic compounds using an enantioselective receptor 失效
标题翻译：使用对映选择性受体纯化有机化合物的方法
公开(公告)号：US5571911A
公开(公告)日：1996-11-05
申请号：US296814
申请日：1994-08-26
申请人： W. Clark Still , Julian A. Simon , Jong-In Hong
发明人： W. Clark Still , Julian A. Simon , Jong-In Hong
IPC分类号： C07B57/00 , C07B63/00 , C07B63/04 , C07D487/18 , C07D487/22 , C07D498/18 , C07D513/18
CPC分类号： C07D487/18 , C07B57/00 , C07B63/00 , C07B63/04 , C07D487/22 , C07D498/18 , C07D513/18 , Y02P20/55
摘要： The present invention relates to a composition having the general formula: ##STR1## wherein each of A, B, C, X, Y, and Z is independently O, NH, N(CH.sub.2).sub.m CH.sub.3, N(C.dbd.O) (CH.sub.2).sub.m CH.sub.3, CH.sub.2, S, or Se; each of R.sub.1, R.sub.2, and R.sub.3 is independently phenyl, 4-hydroxyphenyl, pyridyl, pyrrolyl, indolyl, naphthyl, thiophenyl, (C.dbd.O) (CH.sub.2).sub.p CH.sub.3, NH(C.dbd.O) (CH.sub.2).sub.p CH.sub.3, OH, COOH, NH.sub.2, or SH; and m, n, and p are integers between 0 and 5. The composition is a chiral receptor molecule useful for the purification of enantiomers of derivatives of amino acids and of compounds able to form hydrogen bonds. The preparation of the composition involves coupling a trifunctional aromatic molecule with three protected chiral molecules at the three aromatic groups, cleaving protecting groups, and joining adjacent chiral groups by multiple lactamizations. The receptor may be used in a form either bound to a solid support or dissolved in an immiscible phase to effect convenient purification of enantiomers or other compounds of interest.
摘要翻译：本发明涉及具有以下通式的组合物：其中A，B，C，X，Y和Z各自独立地为O，NH，N（CH 2）m CH 3，N（C = O））mCH 3，CH 2，S或Se; R 1，R 2和R 3各自独立地为苯基，4-羟基苯基，吡啶基，吡咯基，吲哚基，萘基，噻吩基，（C = O）（CH 2）pCH 3，NH（C = O）（CH 2）p CH 3，OH，COOH ，NH2或SH; 并且m，n和p是0和5之间的整数。该组合物是可用于纯化氨基酸衍生物和能够形成氢键的化合物的对映异构体的手性受体分子。组合物的制备包括将三官能芳族分子与三个芳族基团上的三个受保护的手性分子偶联，切割保护基团，并通过多次内酰胺化连接相邻的手性基团。受体可以以与固体支持物结合或溶解在不混溶相中的形式使用，以实现对映异构体或其它目的化合物的方便的纯化。

3. 发明授权

US5342934A Enantioselective receptor for amino acid derivatives, and other compounds 失效
标题翻译：氨基酸衍生物的对映选择性受体和其他化合物
公开(公告)号：US5342934A
公开(公告)日：1994-08-30
申请号：US901401
申请日：1992-06-19
申请人： W. Clark Still , Julian A. Simon , Jong-In Hong
发明人： W. Clark Still , Julian A. Simon , Jong-In Hong
IPC分类号： C07B57/00 , C07B63/00 , C07B63/04 , C07D487/18 , C07D487/22 , C07D498/18 , C07D513/18
CPC分类号： C07D487/18 , C07B57/00 , C07B63/00 , C07B63/04 , C07D487/22 , C07D498/18 , C07D513/18 , Y02P20/55
摘要： The present invention relates to a composition having the general formula: ##STR1## wherein each of A, B, C, X, Y, and Z is independently O, NH, N(CH.sub.2).sub.m CH.sub.3 ], N(C.dbd.O) (CH.sub.2).sub.m CH.sub.3 ], CH.sub.2, S, or Se; each of R.sub.1, R.sub.2, and R.sub.3 is independently phenyl, 4-hydroxyphenyl, pyridyl, pyrrolyl, indolyl, naphthyl, thiophenyl, (C.dbd.O) (CH.sub.2).sub.p CH.sub.3, NH(C.dbd.O) (CH.sub.2).sub.p CH.sub.3 ], OH, COOH, NH.sub.2, or SH; and m, n, and p are integers between 0 and 5. The composition is a chiral receptor molecule useful for the purification of enantiomers of derivatives of amino acids and of compounds able to form hydrogen bonds. The preparation of the composition involves coupling a trifunctional aromatic molecule with three protected chiral molecules at the three aromatic groups, cleaving protecting groups, and joining adjacent chiral groups by multiple lactamizations. The receptor may be used in a form either bound to a solid support or dissolved in an immiscible phase to effect convenient purification of enantiomers or other compounds of interest.
摘要翻译：本发明涉及具有以下通式的组合物：其中A，B，C，X，Y和Z各自独立地为O，NH，N（CH 2）m CH 3]，N（C = O） CH2）mCH3]，CH2，S或Se; R 1，R 2和R 3各自独立地是苯基，4-羟基苯基，吡啶基，吡咯基，吲哚基，萘基，噻吩基，（C = O）（CH 2）pCH 3，NH（C = O）（CH 2）p CH 3] COOH，NH2或SH; 并且m，n和p是0和5之间的整数。该组合物是可用于纯化氨基酸衍生物和能够形成氢键的化合物的对映异构体的手性受体分子。组合物的制备包括将三官能芳族分子与三个芳族基团上的三个受保护的手性分子偶联，切割保护基团，并通过多次内酰胺化连接相邻的手性基团。受体可以以与固体支持物结合或溶解在不混溶相中的形式使用，以实现对映异构体或其它目的化合物的方便的纯化。

4. 发明申请

US20090203770A1 COMPOSITIONS AND METHODS FOR MODULATING APOPTOSIS IN CELLS OVER-EXPRESSING Bcl-2 FAMILY MEMBER PROTEINS 审中-公开
标题翻译：用于调节Bcl-2家族成员蛋白中细胞凋亡的组合物和方法
公开(公告)号：US20090203770A1
公开(公告)日：2009-08-13
申请号：US11768111
申请日：2007-06-25
申请人： David M. Hockenberry , Julian A. Simon , Shie-Pon Tzung
发明人： David M. Hockenberry , Julian A. Simon , Shie-Pon Tzung
IPC分类号： A61K31/357 , C07D321/00 , C12Q1/02
CPC分类号： C07D321/00 , A61K31/00 , A61K31/357 , G01N2510/00
摘要： The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family member protein. Further, the agents preferentially induce apoptosis in cells that over-express anti-apoptotic Bcl-2 family member proteins and typically exhibit reduced binding affinity for cytochrome B. Pharmaceutical uses of the agents and compositions include treating apoptosis-associated disease, such as neoplasia and drug resistance, are also disclosed.
摘要翻译：本发明提供用于调节细胞凋亡状态的药剂和组合物。这些试剂包括与抗凋亡Bcl-2家族成员蛋白结合的抗生素的衍生物。此外，所述药剂优先诱导细胞凋亡，其过表达抗凋亡Bcl-2家族成员蛋白并通常表现出对细胞色素B的降低的结合亲和力。药物和组合物的药物用途包括治疗凋亡相关疾病，例如瘤形成和耐药性也被披露。

5. 发明授权

US07241804B1 Compositions and methods for modulating apoptosis in cells over-expressing Bcl-2 family member proteins 有权
标题翻译：用于调节细胞过度表达Bcl-2家族蛋白的细胞凋亡的组合物和方法
公开(公告)号：US07241804B1
公开(公告)日：2007-07-10
申请号：US10069431
申请日：2000-08-18
申请人： David M. Hockenberry , Julian A. Simon , Shie-Pon Tzung
发明人： David M. Hockenberry , Julian A. Simon , Shie-Pon Tzung
IPC分类号： A61K31/35
CPC分类号： A61K31/35 , C12N2501/48
摘要： The present invention provides agents and compositions for modulating the apoptotic state of a cell. The agents comprise derivatives of antimycins which bind to an anti-apoptotic Bcl-2 family member protein. Further, the agents preferentially induce apoptosis in cells that over-express anti-apoptotic Bcl-2 family member proteins and typically exhibit reduced binding affinity for cytochrome B. Pharmaceutical uses of the agents and compositions include treating apoptosis-associated disease, such as neoplasia and drug resistance, are also disclosed.
摘要翻译：本发明提供用于调节细胞凋亡状态的药剂和组合物。这些试剂包括与抗凋亡Bcl-2家族成员蛋白结合的抗生素的衍生物。此外，所述药剂优先诱导细胞凋亡，其过表达抗凋亡Bcl-2家族成员蛋白并通常表现出对细胞色素B的降低的结合亲和力。药物和组合物的药物用途包括治疗凋亡相关疾病，例如瘤形成和耐药性也被披露。

6. 发明授权

US08232314B2 Compounds that protect against sensory hair cell death 失效
标题翻译：防止感觉毛细胞死亡的化合物
公开(公告)号：US08232314B2
公开(公告)日：2012-07-31
申请号：US12014470
申请日：2008-01-15
申请人： Henry C. Ou , Felipe Santos , Edwin W. Rubel , David W. Raible , Julian A. Simon
发明人： Henry C. Ou , Felipe Santos , Edwin W. Rubel , David W. Raible , Julian A. Simon
IPC分类号： A01N43/12
CPC分类号： A61K49/0006
摘要： The present invention provides methods of identifying compounds that protect against ototoxicity induced by one or more noxious stimuli, and methods of treating an individual with compounds identified using the present screening methods. Also provided are compounds demonstrated to have otoprotective effects.
摘要翻译：本发明提供了确定防止由一种或多种毒性刺激引起的耳毒性的化合物的方法，以及使用本筛选方法鉴定的化合物治疗个体的方法。还提供了证明具有保护作用的化合物。

7. 发明申请

US20110135756A1 COMPOSITIONS AND METHODS FOR PROTECTING SENSORY HAIR CELLS 审中-公开
标题翻译：用于保护感染性毛发细胞的组合物和方法
公开(公告)号：US20110135756A1
公开(公告)日：2011-06-09
申请号：US12963396
申请日：2010-12-08
申请人： Kelly N. Owens , Anna L. Corke , Henry C. Ou , Edwin W. Rubel , David W. Raible , Julian A. Simon
发明人： Kelly N. Owens , Anna L. Corke , Henry C. Ou , Edwin W. Rubel , David W. Raible , Julian A. Simon
IPC分类号： A61K33/24 , A61K31/522 , A61K31/122 , A61K31/4965 , A61K31/546 , A61K31/4706 , A61K31/138 , A61K31/438 , A61K31/7036 , A61P17/00 , A61P27/16
CPC分类号： A61K31/546 , A61K31/122 , A61K31/138 , A61K31/438 , A61K31/4706 , A61K31/522 , A61K31/7036 , A61K33/24 , A61K45/06 , A61K2300/00
摘要： The invention provides compounds, compositions and methods that can be used for the attenuation of damage to sensory hair cells and symptoms thereof. More particularly, the invention identifies drugs that can be used to protect sensory hair cells from ototoxic medications, noise-induced damage and age-related loss.
摘要翻译：本发明提供可用于减轻感觉毛细胞损伤及其症状的化合物，组合物和方法。更具体地，本发明鉴定可用于保护感觉毛细胞免受耳毒性药物，噪声诱发的损伤和与年龄有关的损失的药物。

8. 发明申请

US20090023751A1 COMPOUNDS THAT PROTECT AGAINST SENSORY HAIR CELL DEATH 失效
标题翻译：保护感染发炎细胞死亡的化合物
公开(公告)号：US20090023751A1
公开(公告)日：2009-01-22
申请号：US12014470
申请日：2008-01-15
申请人： Henry C. Ou , Felipe Santos , Edwin W. Rubel , David W. Raible , Julian A. Simon
发明人： Henry C. Ou , Felipe Santos , Edwin W. Rubel , David W. Raible , Julian A. Simon
IPC分类号： A61K31/381 , A61K31/473 , A61K31/138 , A61K31/4965 , A61K31/403
CPC分类号： A61K49/0006
摘要： The present invention provides methods of identifying compounds that protect against ototoxicity induced by one or more noxious stimuli, and methods of treating an individual with compounds identified using the present screening methods. Also provided are compounds demonstrated to have otoprotective effects.
摘要翻译：本发明提供了确定防止由一种或多种毒性刺激引起的耳毒性的化合物的方法，以及使用本筛选方法鉴定的化合物治疗个体的方法。还提供了证明具有保护作用的化合物。

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