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    Process for the Isomerization of Semicarbazone Compounds
    2.
    发明申请
    Process for the Isomerization of Semicarbazone Compounds 审中-公开
    缩氨基脲化合物异构化方法

    公开(公告)号：US20110105794A1

    公开(公告)日：2011-05-05

    申请号：US13001063

    申请日：2009-06-22

    申请人： Thomas Zierke ,  Stefan Engel

    发明人： Thomas Zierke ,  Stefan Engel

    IPC分类号： C07C237/18

    CPC分类号： C07C281/14

    摘要： The present invention relates to a process for the isomerization of the Z-isomer I-Z of a semicarbazone compound of the general formula (I) into its E-isomer I-E wherein the variables in formula (I) have the meanings as defined in the description.

    摘要翻译： 本发明涉及将通式（I）的缩氨基脲化合物的Z-异构体I-Z异构化为其E-异构体I-E的方法，其中式（I）中的变量具有如说明书中所定义的含义。

    Method For Producing Semicarbazones
    3.
    发明申请
    Method For Producing Semicarbazones 有权
    生产缩氨基脲的方法

    公开(公告)号：US20070203356A1

    公开(公告)日：2007-08-30

    申请号：US10592271

    申请日：2005-03-16

    申请人： Thomas Zierke ,  Stefan Engel ,  Peter Otto

    发明人： Thomas Zierke ,  Stefan Engel ,  Peter Otto

    IPC分类号： C07C281/06

    CPC分类号： C07C281/14

    摘要： The invention relates to a process for preparing semicarbazone compounds of the formula I, where R1 and R2 are each independently hydrogen, halogen, CN, C1-C4-alkyl, C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, and R3 is C1-C4-alkoxy, C1-C4-haloalkyl or C1-C4-haloalkoxy, by reacting a hydrazone compound of the general formula II, where R is C1-C4-alkoxy, amino, C1-C4-alkylamino or di(C1-C4-alkyl)amino, and R1, R2 are each as defined above, with an aniline compound of the general formula III where R3 is as defined above.

    摘要翻译： 本发明涉及一种制备式I的缩氨基脲化合物的方法，其中R 1和R 2各自独立地为氢，卤素，CN，C 1， C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，C 1 -C 3 - 烷基，C 1 -C 4 - C 1 -C 4烷基或C 1 -C 4 - 卤代烷氧基，R 3是C 1 - C 1 -C 4 - 烷氧基，C 1 -C 4 - 卤代烷基或C 1 -C 3 通过使通式II的腙化合物反应，其中R是C 1 -C 4 - 烷氧基，氨基，C

    Halogenated antituberculosis agents
    5.
    发明申请
    Halogenated antituberculosis agents 失效
    卤化抗结核药

    公开(公告)号：US20030114531A1

    公开(公告)日：2003-06-19

    申请号：US10237416

    申请日：2002-09-09

    发明人： Farzad Kobarfard ,  Joel M. Kauffman

    IPC分类号： A61K031/175 ,  C07C337/06 ,  C07C281/12

    CPC分类号： C07C281/14 ,  C07C337/08

    摘要： Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized. In general, the halogenated compound has the structure of Structure I: 1 wherein X1 is a halogen and X2 is a second halogen or hydrogen, and Y is sulfur or oxygen; or, has the structure of Structure IV: 2 wherein X1 is a halogen and X2 is a second halogen or hydrogen. Alternatively, the halogenated compounds may be pharmaceutically acceptable salts of these compounds. These halogenated derivatives possess anti-mycobacterial activity and are particularly useful for the treatment of Mycobacterium tuberculosis infections. In particular, fluorinated analogs of thioacetazone and p-amino-salicylic acid have been synthesized for use as anti-tuberculosis therapeutic agents either alone or in combination with other conventional anti-tuberculosis therapeutic agents.

    摘要翻译： 已经合成了两种合成抗结核药物硫代乙酮和对氨基水杨酸的卤代衍生物。 通常，卤代化合物具有结构I的结构：其中X1是卤素，X2是第二个卤素或氢，Y是硫或氧; 或具有结构IV的结构：其中X1是卤素，X2是第二个卤素或氢。 或者，卤化化合物可以是这些化合物的药学上可接受的盐。 这些卤代衍生物具有抗分枝杆菌活性，特别可用于治疗结核分枝杆菌感染。 特别地，已经合成硫代乙酮和对氨基水杨酸的氟化类似物单独使用或与其它常规抗结核治疗剂组合用作抗结核治疗剂。

    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    6.
    发明申请
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 失效
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US20020183321A1

    公开(公告)日：2002-12-05

    申请号：US10178477

    申请日：2002-06-25

    发明人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F.W. Keana ,  Victor I. Ilyin

    IPC分类号： A61K031/535 ,  A61K031/495 ,  A61K031/445 ,  A61K031/175

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1 or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基-82-。 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。

    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof
    7.
    发明授权
    Carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones and the use thereof 有权
    碳环和杂环取代的缩氨基脲和缩氨基硫脲和其用途

    公开(公告)号：US06458843B1

    公开(公告)日：2002-10-01

    申请号：US09421403

    申请日：1999-10-21

    申请人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    发明人： Yan Wang ,  Sui Xiong Cai ,  Nancy C. Lan ,  John F. W. Keana ,  Victor I. Ilyin ,  Eckard Weber

    IPC分类号： A61K3117

    CPC分类号： C07D213/643 ,  A61K31/17 ,  A61K31/175 ,  A61K31/44 ,  A61K31/445 ,  A61K31/47 ,  A61K31/505 ,  C07C281/12 ,  C07C281/14 ,  C07C2601/14 ,  C07D209/14 ,  C07D211/46 ,  C07D213/68 ,  C07D215/12 ,  C07D307/91 ,  C07D309/12 ,  C07D317/50 ,  C07D317/58 ,  C07D317/62 ,  C07D317/64 ,  C07D319/18

    摘要： This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl. The invention also is directed to the use of carbocycle and heterocycle substituted semicarbazones and thiosemicarbazones for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), for the treatment and prevention of otoneurotoxicity and eye diseases involving glutamate toxicity and for the treatment, prevention or amelioration of pain, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy and urinary incontinence.

    摘要翻译： 本发明涉及由式I表示的碳环和杂环取代的缩氨基脲和缩氨基硫脲或其药学上可接受的盐或前药，其中：Y是氧或硫; R1，R21，R22和R23独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基; 或R 22和R 23与N一起形成杂环; A1和A2独立地是芳基，杂芳基，饱和或部分不饱和的碳环或饱和或部分不饱和的杂环，其中任何一个任选被取代; X是1或O，S，NR 24，CR 25 R 26，C（O），NR 24 C（O），C（O）NR 24，SO，SO 2或共价键; 其中R 24，R 25和R 26独立地是氢，烷基，环烷基，烯基，炔基，卤代烷基，芳基，氨基烷基，羟基烷基，烷氧基烷基或羧基烷基。 本发明还涉及使用碳环和杂环取代的缩氨基脲和缩氨基硫脲来治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS），用于治疗和预防 涉及谷氨酸毒性和治疗，预防或改善疼痛，作为抗惊厥药，以及作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病和尿失禁的抗疟药抑制剂。