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1. 发明授权

US08759382B2 Propargyl-trifluoromethoxy-aminobenzothiazole derivatives, their preparation and use 失效
标题翻译：炔丙基 - 三氟甲氧基 - 氨基苯并噻唑衍生物，其制备和用途
公开(公告)号：US08759382B2
公开(公告)日：2014-06-24
申请号：US13823001
申请日：2011-09-29
申请人： Eliezer Falb , Jeffrey Sterling , Yaacov Herzig , Raphael Nudelman , Konstantin Ulanenko
发明人： Eliezer Falb , Jeffrey Sterling , Yaacov Herzig , Raphael Nudelman , Konstantin Ulanenko
IPC分类号： A01N43/78 , A61K31/425 , C07D277/60 , C07D277/62
CPC分类号： C07D277/64 , C07C309/04 , C07D277/82
摘要： Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.
摘要翻译：公开了炔丙基 - 三氟甲氧基 - 氨基 - 苯并噻唑的新衍生物，其有效治疗包括帕金森氏病和多发性硬化的神经障碍。

2. 发明申请

US20130172364A1 PROPARGYL-TRIFLUOROMETHOXY-AMINOBENZOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND USE 失效
标题翻译：衍生物 - 三氟甲基氨基苯并噻唑衍生物及其制备和使用
公开(公告)号：US20130172364A1
公开(公告)日：2013-07-04
申请号：US13823001
申请日：2011-09-29
申请人： Eliezer Falb , Jeffrey Sterling , Yaacov Herzig , Raphael Nudelman , Konstantin Ulanenko
发明人： Eliezer Falb , Jeffrey Sterling , Yaacov Herzig , Raphael Nudelman , Konstantin Ulanenko
IPC分类号： C07D277/64 , C07C309/04
CPC分类号： C07D277/64 , C07C309/04 , C07D277/82
摘要： Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.
摘要翻译：公开了炔丙基 - 三氟甲氧基 - 氨基 - 苯并噻唑的新衍生物，其有效治疗包括帕金森氏病和多发性硬化的神经障碍。

3. 发明申请

US20070021450A1 Indanylamino uracils and their use as antioxidants and neuroprotectants 审中-公开
标题翻译：茚基氨基尿嘧啶及其作为抗氧化剂和神经保护剂的用途
公开(公告)号：US20070021450A1
公开(公告)日：2007-01-25
申请号：US11182452
申请日：2005-07-15
申请人： Benjamin Sklarz , Eliezer Falb , Gyorgy Toth , Yaacov Herzig , Jeffrey Sterling
发明人： Benjamin Sklarz , Eliezer Falb , Gyorgy Toth , Yaacov Herzig , Jeffrey Sterling
IPC分类号： A61K31/513 , C07D239/545
CPC分类号： C07D239/545
摘要： Disclosed are compounds having the structure: wherein, R1 is H, NH2, NH—(C1-C4)alkyl, or N—[(C1-C4)alkyl]2; R2 and R3 are each independently H, (C1-C4)alkyl, or wherein R4 is H, (C1-C4)alkyl, halogen, hydroxy, (C1-C10)alkoxy, cyano, nitro, —NR5R6, or —OCONR7R8; wherein R5 and R6 are each independently H, or a substituted or unsubstituted (C1-C4)alkyl; and wherein R7 and R8 are each independently H, or substituted or unsubstituted (C1-C4)alkyl, or (C1-C10)aryl; and wherein only one of R2 and R3 is H, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds, pharmaceutical compositions containing such compounds or salts, and processes for their preparation. The subject invention also provides methods of alleviating symptoms of neurologic and inflammatory disorders, methods of preventing oxidation of lipids, proteins, or deoxyribonucleic acids on a cellular level, and methods of protecting human red blood cells from lysis by O2 radicals.
摘要翻译：公开了具有以下结构的化合物：其中R 1是H，NH 2，NH-（C 1 -C 4）或N - [（C 1 -C 4）烷基]亚烷基;或N - [（C 1 -C 4 - R 2和R 3各自独立地为H，（C 1 -C 4 -C 4）烷基，或其中R （C 1 -C 4）烷基，卤素，羟基，（C 1 -C 4）烷基，烷氧基，氰基，硝基，-NR 5 R 6或-CONR 7 R 13， 8

4. 发明申请

US20050197365A1 Diamino thiazoloindan derivatives and their use 审中-公开
标题翻译：二氨基噻唑烷衍生物及其用途
公开(公告)号：US20050197365A1
公开(公告)日：2005-09-08
申请号：US11067110
申请日：2005-02-25
申请人： Jeffrey Sterling , Liat Hayardeny-Nisimov , David Lerner , Yaacov Herzig , Eliezer Falb , Gyorgy Toth , Sandor Molnar , Dalia Pinkert
发明人： Jeffrey Sterling , Liat Hayardeny-Nisimov , David Lerner , Yaacov Herzig , Eliezer Falb , Gyorgy Toth , Sandor Molnar , Dalia Pinkert
IPC分类号： A61K31/428 , C07D277/84
CPC分类号： A61K31/428 , C07C211/42 , C07C211/60 , C07C233/14 , C07C233/41 , C07C271/24 , C07C2602/08 , C07D277/60
摘要： The subject invention provides a compound having the structure: wherein Y is O, NR3R4 or NOR6; R3 is H, alkyl, aralkyl, alkynyl, trifluoroacetyl, t-butoxycarbonyl or an acyl group; R4 is H, alkyl, aralkyl, or alkynyl; R6 is H or C1-C4 alkyl; R1 and R2 are each independently H, alkyl, aralkyl, or alkynyl; the curved line drawn from S to the center of the phenyl ring and the straight line drawn from N to the center of the ring indicate that S and N are part of a 5 membered ring which shares two carbons with the phenyl ring; and the dashed line drawn from the carbon atom on the cyclopentyl ring to Y represents a bond when Y is O or NOR6 and is absent when Y is NR3R4, and wherein wherein X is H or O; and R5 is H, alkyl, trifluoroacetyl, t-butoxycarbonyl or an acyl group, or an enantiomer, or a tautomer, or a pharmaceutically acceptable salt thereof, a process for preparing the compounds and a method of treating Parknison's disease, multiple sclerosis or depression with the compounds of the invention.
摘要翻译：本发明提供具有以下结构的化合物：其中Y为O，NR 3 R 4或NOR 6; R 3是H，烷基，芳烷基，炔基，三氟乙酰基，叔丁氧基羰基或酰基; R 4是H，烷基，芳烷基或炔基; R 6是H或C 1 -C 4烷基; R 1和R 2各自独立地为H，烷基，芳烷基或炔基; 从S到苯环中心的曲线和从N到环的中心的直线表示S和N是与苯环共享两个碳的5元环的一部分; 在Y为O或NOR 6时，从环戊基环上的碳原子取代的虚线表示Y，当Y为NR 3 R时，不存在 > 4，并且其中X是H或O; R 5是H，烷基，三氟乙酰基，叔丁氧基羰基或酰基，或其对映体或其互变异构体或其药学上可接受的盐，该化合物的制备方法和用本发明的化合物治疗帕金森病，多发性硬化或抑郁症。

5. 发明申请

US20060025446A1 Propargyl nitroxides and indanyl nitroxides and their use for the treatment of neurologic diseases and disorders 审中-公开
标题翻译：炔丙基氮氧化物和二氢化茚基氮氧化物及其用于治疗神经系统疾病和病症的用途
公开(公告)号：US20060025446A1
公开(公告)日：2006-02-02
申请号：US11191212
申请日：2005-07-26
申请人： Jeffrey Sterling , Benjamin Sklarz , Yaacov Herzig , David Lerner , Eliezer Falb , Haim Ovadia
发明人： Jeffrey Sterling , Benjamin Sklarz , Yaacov Herzig , David Lerner , Eliezer Falb , Haim Ovadia
IPC分类号： C07D211/06 , A61K31/445
CPC分类号： C07D211/94
摘要： Disclosed are compounds having the structure: wherein Z is —OH or —O•; and A is: wherein X and Y are independently NR1 or O, where R1 is H or C1-C4 alkyl; and R2 is H, C1-C4 alkyl or t-butoxycarbonyl, wherein W is C3-C4 alkynyl; and R1 is H or C1-C4 alkyl, or wherein R1 is H, C1-C4 alkyl, or C3-C4 alkynyl; and R3 is H, OH, O(C1-C4 alkyl), or a halogen, optically active enantiomers, pharmaceutically acceptable salts of the compounds, pharmaceutical compositions containing such compounds or salts, and processes for their preparation. The subject invention also provides methods of alleviating symptoms of neurologic, autoimmune, and inflammatory disorders caused by the presence of reactive oxygen species, methods of preventing oxidation of lipids, proteins, or deoxyribonucleic acids on a cellular level, and methods of protecting human red blood cells from lysis by O2 radicals.
摘要翻译：公开了具有以下结构的化合物：其中Z是-OH或-O。 A是：其中X和Y独立地是NR 1或O，其中R 1是H或C 1 -C 4 烷基; R 2是H，C 1 -C 4烷基或叔丁氧基羰基，其中W是C 3 H 3， -C 4炔基; 且R 1是H或C 1 -C 4烷基，或其中R 1是H，C 1 -C 6烷基， C 1 -C 4烷基或C 3 -C 4炔基; C 1 -C 4烷基或C 3 -C 4炔基; 和R 3是H，OH，O（C 1 -C 4烷基）或卤素，旋光对映异构体，药学上可接受的盐的化合物，含有这些化合物或盐的药物组合物，及其制备方法。本发明还提供减轻由活性氧的存在引起的神经系统，自身免疫性和炎症性疾病的症状的方法，在细胞水平上防止脂质，蛋白质或脱氧核糖核酸的氧化的方法，以及保护人类红血液的方法细胞由O 2自由基裂解。

6. 发明授权

US07045592B2 Processes for coupling amino acids using bis-(trichloromethyl) carbonate 失效
标题翻译：使用碳酸二 - （三氯甲基）偶联氨基酸的方法
公开(公告)号：US07045592B2
公开(公告)日：2006-05-16
申请号：US10321648
申请日：2002-12-18
申请人： Eliezer Falb , Tamar Yechezkel , Yoseph Salitra
发明人： Eliezer Falb , Tamar Yechezkel , Yoseph Salitra
IPC分类号： C07K1/08 , C07K1/10 , C07C51/58
CPC分类号： C07K7/06 , A61K38/00 , C07K1/08 , C07K5/101 , C07K5/1016 , C07K5/1019
摘要： A process is disclosed for using bis-(trichloromethyl)carbonate (triphosgene), diphosgene or phosgene as efficient and effective coupling reagents during coupling of carbohydrates to peptide chains. This process is particularly useful for the coupling to sterically hindered amino acid residues, or for other difficult couplings. The reagents can be used for the derivatization of peptides by formation of a bond between a free amine on a peptide and a carbohydrate.
摘要翻译：公开了在将碳水化合物与肽链偶联期间使用双（（三氯甲基）碳酸酯（三光气），双光气或光气作为有效和有效的偶联试剂的方法。该方法对于与空间位阻氨基酸残基的偶联或其它困难的偶联特别有用。试剂可用于通过在肽上的游离胺和碳水化合物之间形成键来衍生肽。

7. 发明授权

US06512092B2 Processes for coupling amino acids using bis-(trichloromethyl) carbonate 失效
标题翻译：使用碳酸二 - （三氯甲基）偶联氨基酸的方法
公开(公告)号：US06512092B2
公开(公告)日：2003-01-28
申请号：US09756223
申请日：2001-01-09
申请人： Eliezer Falb , Tamar Yechezkel , Yoseph Salitra
发明人： Eliezer Falb , Tamar Yechezkel , Yoseph Salitra
IPC分类号： C07C110
CPC分类号： C07K7/06 , A61K38/00 , C07K1/08 , C07K5/101 , C07K5/1016 , C07K5/1019
摘要： A process is disclosed for using triphosgene as an efficient and effective coupling reagent during peptide synthesis, by in situ generation of amino acid chloride from a protected amino acid. This process is particularly useful for the coupling to sterically hindered amino acid residues, or for other difficult couplings. Furthermore, the same reagent can be used for the derivatization of peptides by formation of an amide bond between a free amine on a peptide and a carboxylic acid, or for the coupling of an amino acid to a solid support.
摘要翻译：公开了在肽合成期间通过原位从保护的氨基酸产生氨基酰氯来使用三光气作为有效和有效的偶联剂的方法。该方法对于与空间位阻氨基酸残基的偶联或其它困难的偶联特别有用。此外，相同的试剂可以用于通过在肽和羧酸上的游离胺之间形成酰胺键或将氨基酸与固体支持物偶联来使肽衍生化。

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