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    PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINO TETRALIN DERIVATIVES AS BRAIN-SELECTIVE MAO INHIBITORS
    1.
    发明申请
    PROPARGYLAMINO INDAN DERIVATIVES AND PROPARGYLAMINO TETRALIN DERIVATIVES AS BRAIN-SELECTIVE MAO INHIBITORS 审中-公开
    丙氨酰胺衍生物和丙氨酰胺四环素衍生物作为脑选择性MAO抑制剂

    公开(公告)号：US20090131535A1

    公开(公告)日：2009-05-21

    申请号：US12357177

    申请日：2009-01-21

    申请人： Eran Blaugrund ,  Yaacov Herzig ,  Jeffrey Sterling

    发明人： Eran Blaugrund ,  Yaacov Herzig ,  Jeffrey Sterling

    IPC分类号： A61K31/135 ,  C07C211/42 ,  A61P25/24 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00

    CPC分类号： C07C219/26 ,  A61K31/24 ,  A61K31/375 ,  C07C215/64 ,  C07C271/40 ,  C07C2602/08 ,  C07C2602/10

    摘要： The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure: wherein R1 is OC(O)R9 and R2 is H, wherein R9 is branched or unbranched C1 to C6 alkyl, aryl, or aralkyl, or R1 is OC(O)R4 and R2 is OC(O)R4, wherein R4 is branched or unbranched C1 to C6 alkyl, aryl, aralkyl or NR5R6, wherein R5 and R6 are each independently H, C1 to C8 alkyl, C6 to C12 aryl, C6 to C12 aralkyl or C6 to C12 cycloalkyl, each optionally substituted; wherein R3 is H or C1 to C6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2, or a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.

    摘要翻译： 本发明提供了选择性抑制脑中单胺氧化酶（MAO）的炔丙基氨基茚满（PAI）和炔丙基氨基四氢萘的衍生物，其结构如下：其中R1是OC（O）R9且R2是H，其中R9是支链或非支链C1 或C 1 -C 6烷基，芳基或芳烷基，或R 1为OC（O）R 4且R 2为OC（O）R 4，其中R 4为支链或非支链C1至C6烷基，芳基，芳烷基或NR5R6，其中R5和R6各自独立地为 H，C 1至C 8烷基，C 6至C 12芳基，C 6至C 12芳烷基或C 6至C 12环烷基，各自任选取代; 其中R3是H或C1-C6烷基; 其中n为0或1; 并且其中m为1或2，或其药学上可接受的盐。 另外，本发明提供了使用这些化合物治疗神经障碍的方法，这些化合物用于制备用于治疗神经障碍的药物的用途和用于合成这些化合物的方法。

    Indanylamino uracils and their use as antioxidants and neuroprotectants
    2.
    发明申请
    Indanylamino uracils and their use as antioxidants and neuroprotectants 审中-公开
    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

    Diamino thiazoloindan derivatives and their use
    3.
    发明申请
    Diamino thiazoloindan derivatives and their use 审中-公开
    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。

    Propargyl nitroxides and indanyl nitroxides and their use for the treatment of neurologic diseases and disorders
    5.
    发明申请
    Propargyl nitroxides and indanyl nitroxides and their use for the treatment of neurologic diseases and disorders 审中-公开
    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。