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21. 发明授权

US09168265B2 Tetracycline derivatives with reduced antibiotic activity and neuroprotective benefits 有权
标题翻译：具有降低的抗生素活性和神经保护益处的四环素衍生物
公开(公告)号：US09168265B2
公开(公告)日：2015-10-27
申请号：US13714052
申请日：2012-12-13
申请人： Neumedics
发明人： Iain W. Duncan , Edward A. Kesicki , Carl G. Osborne , William D. Schwieterman , Irina Jacobson
IPC分类号： C07D265/34 , C07D263/52 , A61K31/65 , A61K31/423 , A61K31/536 , A61K45/06 , C07C323/60 , C07D263/62 , C07D498/10 , C07C233/58
CPC分类号： C07D265/34 , A61K31/423 , A61K31/536 , A61K31/65 , A61K45/06 , C07C233/58 , C07C323/60 , C07C2603/46 , C07D263/52 , C07D263/62 , C07D498/10
摘要： The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.
摘要翻译：本公开涉及利用四环素支架，优选四环素或米诺环素的支架并且显着缺乏抗生素活性的组合物和方法。这些化合物具有神经保护属性，而不会干扰药物通过血脑屏障的能力。这些化合物由于其神经元细胞周期进程的抑制而具有神经保护活性。化合物的特征在于第五环连接位置9和10。

22. 发明授权

US08518979B2 Alpha-halo- and alpha-alkyl-cyclopropylcarboxy compounds and uses thereof 有权
标题翻译： α-卤代 - 和α-烷基 - 环丙基羧基化合物及其用途
公开(公告)号：US08518979B2
公开(公告)日：2013-08-27
申请号：US12527707
申请日：2008-02-19
申请人： Meir Bialer , Boris Yagen , Neta Pessah
发明人： Meir Bialer , Boris Yagen , Neta Pessah
IPC分类号： A61K31/433 , A61K31/17 , A61K31/164 , C07D285/135 , C07C275/18 , C07C233/61 , C07C233/58
CPC分类号： C07C233/58 , C07C275/52 , C07C2601/02 , C07D285/135
摘要： Novel Alpha-halo- and Alpha-alkyl-cyclopropylcarboxy compounds, and uses of these and related compounds in the treatment of a variety of neurological diseases and disorders, and particularly epilepsy, are provided.
摘要翻译：提供了新的α-卤代和α-烷基 - 环丙基羧基化合物，以及这些和相关化合物在治疗各种神经疾病和病症，特别是癫痫中的应用。

23. 发明授权

US08487133B2 Substituted bicyclo [4.1.0] heptane-7-carboxylic acid amides and derivatives thereof as food flavor substances 有权
标题翻译：取代的双环[4.1.0]庚烷-7-羧酸酰胺及其衍生物作为食品香料物质
公开(公告)号：US08487133B2
公开(公告)日：2013-07-16
申请号：US12445842
申请日：2007-10-18
申请人： Jan Looft , Tobias Vössing , Michael Backes
发明人： Jan Looft , Tobias Vössing , Michael Backes
IPC分类号： C07C233/58
CPC分类号： C07C233/58 , A23L23/00 , A23L27/205 , A23L27/60 , A23L27/63 , A23L27/88 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/20
摘要： The present invention relates to the use of a compound of the Formula (I) wherein: R1, R2, R3, R4, R5, R6, R7 and R8 denote in each case independently of one another hydrogen, an alkyl radical with 1 to 6 C atoms, or an alkenyl radical with 2 to 6 C atoms, with the proviso that at least one of the radicals R1, R2, R7 and R8 and at least one further of the radicals R1, R2, R3, R4, R5, R6, R7 and R8 are not hydrogen, wherein independently of one another also two of the radicals R1, R2, R3, R4, R5, R6, R7 and R8 can together denote a bridge with one or more bridge C atoms; Y1 and Y2 denote independently of one another hydrogen, methyl or ethyl; and Ra and Rb denote independently of one another hydrogen, an alkyl radical with 1 to 6 C atoms, an alkenyl radical with 2 to 6 C atoms or a cycloalkyl radical with 3 to 6 C atoms as a food flavor substance.
摘要翻译：本发明涉及式（I）化合物的用途，其中：R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8各自独立地表示氢，具有1至6个 C原子或具有2至6个C原子的烯基，条件是基团R 1，R 2，R 7和R 8中的至少一个以及基团R 1，R 2，R 3，R 4，R 5，R 6中的至少一个 R 7和R 8不是氢，其中独立地彼此基团R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8中的两个可以一起表示具有一个或多个桥C原子的桥; Y1和Y2彼此独立地表示氢，甲基或乙基; 并且R a和R b彼此独立地表示氢，具有1至6个C原子的烷基，具有2至6个C原子的烯基或具有3至6个C原子的环烷基作为食品香料物质。

24. 发明授权

US08222454B2 Process for preparing optical pure milnacipran and its pharmaceutically accepted salts 失效
标题翻译：制备光学纯米那普仑及其药学上可接受的盐的方法
公开(公告)号：US08222454B2
公开(公告)日：2012-07-17
申请号：US12517379
申请日：2007-11-28
申请人： Lin Ai , Xiao Liu
发明人： Lin Ai , Xiao Liu
IPC分类号： C07C233/58
CPC分类号： C07C231/20 , C07B2200/07 , C07C2601/02 , C07C237/24
摘要： The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.
摘要翻译：本发明公开了一种制备光学纯米那普仑及其药学上可接受的盐的方法，其采用外消旋米那普兰作为起始原料，酒石酸衍生物及其组合物作为分离剂进行分解。

25. 发明授权

US08115031B2 Anti-inflammatory quinic acid derivatives for oral administration 有权
标题翻译：用于口服给药的抗炎奎尼酸衍生物
公开(公告)号：US08115031B2
公开(公告)日：2012-02-14
申请号：US12268432
申请日：2008-11-10
申请人： Charles R. Yates , Duane D. Miller , Kui Zeng , Karin Emmons Thompson
发明人： Charles R. Yates , Duane D. Miller , Kui Zeng , Karin Emmons Thompson
IPC分类号： C07C233/58
CPC分类号： C07C235/40 , C07C271/20 , C07C2601/14
摘要： Disclosed are compounds comprising analogs of quinic acids or shikimic acids having anti-inflammatory properties. The compounds are suitable for oral administration, stable, and demonstrate significant efficacy in inhibiting NF-kB, inhibiting leukocyte adhesion, and inhibiting other factors and cytokines known to be involved in inflammatory disease.
摘要翻译：公开了包含具有抗炎特性的奎尼酸或莽草酸类似物的化合物。该化合物适合于口服给药，稳定，并且在抑制NF-kB，抑制白细胞粘附和抑制已知与炎症性疾病有关的其它因子和细胞因子方面具有显着疗效。

26. 发明申请

US20100010220A1 Process for Preparing Amidrazones 审中-公开
标题翻译：制备阿米嗪的方法
公开(公告)号：US20100010220A1
公开(公告)日：2010-01-14
申请号：US12376007
申请日：2007-07-25
申请人： Thomas Zierke , Christopher Koradin
发明人： Thomas Zierke , Christopher Koradin
IPC分类号： C07D239/42 , C07D237/20 , C07C251/00 , C07C233/57 , C07C233/58
CPC分类号： C07C257/22 , C07C233/58 , C07C257/02 , C07C2601/02
摘要： The present invention relates to a novel process for preparing amidrazones of the formula (I) wherein R, R1, R2, A, B, W, Y and n have the meanings as indicated in the description. Further, the invention relates to novel compounds used as intermediates in this process and to processes for their preparation.
摘要翻译：本发明涉及一种制备式（I）的氨基腙的新方法，其中R，R 1，R 2，A，B，W，Y和n具有如说明书中所示的含义。此外，本发明涉及在该方法中用作中间体的新化合物及其制备方法。

27. 发明授权

US07179943B2 Bicyclic derivatives that modulate voltage-gated potassium channels and methods of use thereof 失效
标题翻译：调节电压门控钾通道的双环衍生物及其使用方法
公开(公告)号：US07179943B2
公开(公告)日：2007-02-20
申请号：US11151624
申请日：2005-06-13
申请人： Wayne E. Childers , Jerome C. Wu , Callain Y. Kim , Edward J. Podlesny
发明人： Wayne E. Childers , Jerome C. Wu , Callain Y. Kim , Edward J. Podlesny
IPC分类号： C07C233/58 , C07C45/27 , A61K31/165
CPC分类号： C07C235/82
摘要： Bicyclic amide derivatives of formula (I) or tautomers or pharmaceutically acceptable salts thereof or both are provided: Also provided are processes for preparing the bicyclic amide derivatives as well as pharmaceutical compositions containing the same and therapeutic uses. The bicyclic amide derivatives are useful for treating a variety of conditions associated with the abnormal modulation of one or more Kv1.1 voltage-gated potassium channels.
摘要翻译：提供式（I）的二环酰胺衍生物或其互变异构体或其药学上可接受的盐或两者：还提供了制备双环酰胺衍生物的方法以及含有其的治疗用途的药物组合物。双环酰胺衍生物可用于治疗与一种或多种Kv1.1电压门控钾通道的异常调节相关的多种病症。

28. 发明授权

US07166746B2 N-bisaryl- and n-aryl-cycloakylidenyl-αhydroxy-and α-alkoxy acid amides 失效
标题翻译： N-二芳基 - 和正 - 芳基 - 亚环烷基 - α-羟基和α-烷氧基酰胺
公开(公告)号：US07166746B2
公开(公告)日：2007-01-23
申请号：US10522077
申请日：2003-07-23
申请人： Clemens Lamberth , Martin Zeller , Tibor Goegh
发明人： Clemens Lamberth , Martin Zeller , Tibor Goegh
IPC分类号： C07C233/58 , A01N37/18
CPC分类号： C07C235/36 , C07C215/64 , C07C215/74 , C07C217/74 , C07C217/80 , C07C235/38 , C07C2601/14 , C07F7/1804
摘要： The invention relates to N-bisaryl- and N-aryl-cycloalkylidenyl-a-hydroxy- and a-alkoxy acetic acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, C1–C12alkyl; C2–C12alkenyl; C2–C12alkynyl; C1–C12haloalkyl; R2 is hydrogen; optionally substituted alkyl; or optionally substituted alkynyl; R3 is optionally substituted aryl or optionally substituted heteroaryl; A is an optionally substituted saturated or unsaturated C3–C8-cycloalkylidene, optionally substituted phenylidene or optionally substituted saturated or unsaturated heterocyclylidene bridge, R4 and R5 are each independently hydrogen or an organic radical, and R6 is hydrogen; tri-C1–C4alkyl-silyl; di-C1–C4alkyl-phenylsilyl; C1–C4alkyl-diphenylsilyl; triphenylsilyl; optionally substituted alkyl; optionally substituted alkenyl or optionally substituted alkynyl. The compounds possess plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganism, especially fungi.
摘要翻译：本发明涉及通式（I）的N-双芳基 - 和N-芳基 - 环丙烯基-α-羟基 - 和α-烷氧基乙酰胺，其包括其旋光异构体和这些异构体的混合物，其中R 1 氢，C 1 -C 12烷基; C 2 -C 12链烯基; C 2 -C 12炔基; C 1 -C 12卤代烷基; R 2是氢; 任选取代的烷基; 或任选取代的炔基; R 3是任选取代的芳基或任选取代的杂芳基; A是任选取代的饱和或不饱和C 3 -C 8 - 亚烷基，任选取代的亚苯基或任选取代的饱和或不饱和杂环亚烷基桥，R 4 >和R 5各自独立地为氢或有机基团，并且R 6为氢; 三-C 1 -C 4烷基 - 甲硅烷基; 二-C 1 -C 4烷基 - 苯基甲硅烷基; C 1 -C 4烷基 - 二苯基甲硅烷基; 三苯基甲硅烷基; 任选取代的烷基; 任选取代的烯基或任选取代的炔基。该化合物具有植物保护性质，适用于保护植物免受植物病原微生物特别是真菌感染。

29. 发明授权

US06960687B2 Derivatives and pharmaceutical compositions of n-hydroxyalkyl tetramethylcyclopropane-carboxamide, having anti-epiletic, neurological, and CNS activity, and method for their preparation 失效
标题翻译：具有抗癫痫，神经系统和CNS活性的正羟基烷基四甲基环丙烷甲酰胺的衍生物和药物组合物及其制备方法
公开(公告)号：US06960687B2
公开(公告)日：2005-11-01
申请号：US10503235
申请日：2002-12-29
申请人： Meir Bialer , Nina Isoherranen , Boris Yagen
发明人： Meir Bialer , Nina Isoherranen , Boris Yagen
IPC分类号： A61K31/16 , C07C233/58 , A61K31/165
CPC分类号： A61K31/16
摘要： New derivatives of N-Hydroxyalkyl-tetramethylcyclopropane carboxamide, pharmaceutical compositions thereof, methods for their preparation, and use thereof for the treatment of epilepsy, neurological, affective and psychotic disorders and for the treatment of pain and migraine.
摘要翻译： N-羟基烷基 - 四甲基环丙烷甲酰胺的新衍生物，其药物组合物，其制备方法及其用于治疗癫痫，神经系统疾病，情感性和精神病性障碍以及治疗疼痛和偏头痛的用途。

30. 发明申请

US20050215794A1 Copper-catalyzed formation of carbon heteroatom and carbon-carbon bonds 有权
标题翻译：铜催化形成碳杂原子和碳 - 碳键
公开(公告)号：US20050215794A1
公开(公告)日：2005-09-29
申请号：US11028500
申请日：2005-01-04
申请人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
发明人： Stephen Buchwald , Artis Klapars , Jon Antilla , Gabriel Job , Martina Wolter , Fuk Kwong , Gero Nordmann , Edward Hennessy
IPC分类号： B01J31/26 , C07B37/04 , C07B41/04 , C07B43/04 , C07B61/00 , C07C41/16 , C07C41/24 , C07C43/15 , C07C43/20 , C07C43/23 , C07C45/68 , C07C45/71 , C07C49/84 , C07C51/353 , C07C59/64 , C07C67/343 , C07C69/612 , C07C209/10 , C07C211/48 , C07C211/53 , C07C211/54 , C07C213/02 , C07C213/08 , C07C215/16 , C07C215/70 , C07C217/48 , C07C217/82 , C07C221/00 , C07C227/08 , C07C227/18 , C07C229/56 , C07C231/08 , C07C231/12 , C07C233/07 , C07C233/25 , C07C233/40 , C07C233/51 , C07C233/58 , C07C233/65 , C07C233/66 , C07C233/75 , C07C233/80 , C07C233/81 , C07C237/40 , C07C241/04 , C07C243/38 , C07C249/02 , C07C249/16 , C07C251/18 , C07C251/86 , C07C253/14 , C07C253/30 , C07C255/23 , C07C269/06 , C07C271/28 , C07C273/18 , C07C275/32 , C07C277/08 , C07C279/18 , C07C281/02 , C07C303/38 , C07C311/21 , C07C319/20 , C07C323/41 , C07D205/08 , C07D207/16 , C07D207/26 , C07D207/267 , C07D207/27 , C07D207/32 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/65 , C07D213/74 , C07D215/38 , C07D221/12 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/34 , C07D233/58 , C07D235/06 , C07D235/08 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D273/08 , C07D295/02 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07D521/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/4056 , C07B37/04 , C07B41/04 , C07B43/04 , C07C41/16 , C07C45/68 , C07C45/71 , C07C51/353 , C07C67/343 , C07C209/10 , C07C213/08 , C07C221/00 , C07C227/18 , C07C231/08 , C07C231/12 , C07C241/04 , C07C249/02 , C07C249/16 , C07C253/14 , C07C253/30 , C07C269/06 , C07C273/1854 , C07C277/08 , C07C281/02 , C07C303/38 , C07C319/20 , C07C2601/08 , C07C2601/14 , C07C2601/16 , C07D205/08 , C07D207/16 , C07D207/267 , C07D207/27 , C07D207/323 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/48 , C07D209/86 , C07D211/26 , C07D211/76 , C07D213/30 , C07D213/64 , C07D213/74 , C07D231/12 , C07D231/56 , C07D233/32 , C07D233/56 , C07D235/06 , C07D237/32 , C07D239/42 , C07D245/06 , C07D249/08 , C07D249/18 , C07D263/22 , C07D295/023 , C07D295/033 , C07D295/073 , C07D307/79 , C07D333/36 , C07D333/66 , C07D401/04 , C07D405/12 , C07D407/12 , C07D409/04 , C07D471/04 , C07D473/00 , C07C49/84 , C07C59/68 , C07C69/76 , C07C69/65 , C07C69/612 , C07C69/734 , C07C69/616 , C07C69/732 , C07C311/21 , C07C323/41 , C07C211/48 , C07C211/52 , C07C211/55 , C07C211/54 , C07C215/68 , C07C217/84 , C07C215/16 , C07C225/22 , C07C217/08 , C07C229/56 , C07C229/60 , C07C211/58 , C07C243/38 , C07C251/86 , C07C43/205 , C07C43/2055 , C07C43/235 , C07C43/23 , C07C43/16 , C07C43/215 , C07C43/225 , C07C237/30 , C07C255/58 , C07C233/07
摘要： The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-oxygen bond between the oxygen atom of an alcohol and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. The present invention also relates to copper-catalyzed methods of forming a carbon-carbon bond between a reactant comprising a nucleophilic carbon atom, e.g., an enolate or malonate anion, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. Importantly, all the methods of the present invention are relatively inexpensive to practice due to the low cost of the copper comprised by the catalysts.
摘要翻译：本发明涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。在某些实施方案中，本发明涉及在酰胺或胺部分的氮原子与芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在另外的实施方案中，本发明涉及在酰基肼的氮原子和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜催化方法。在其它实施方案中，本发明涉及在含氮杂芳族化合物（例如吲哚，吡唑和吲唑）的氮原子与芳基，杂芳基的活性炭之间形成碳 - 氮键的铜催化方法，或乙烯基卤化物或磺酸盐。在某些实施方案中，本发明涉及在醇的氧原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 氧键的铜催化方法。本发明还涉及在包含亲核性碳原子的反应物（例如烯醇化物或丙二酸酯阴离子）和芳基，杂芳基或卤乙烯或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。重要的是，由于催化剂所含的铜的低成本，本发明的所有方法都相对便宜。

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