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    Phthalimide derivatives that influence cellular vesicular systems, pharmaceutical compositions, and use thereof
    1.
    发明授权
    Phthalimide derivatives that influence cellular vesicular systems, pharmaceutical compositions, and use thereof 失效
    影响细胞水泡系统的邻苯二甲酰亚胺衍生物，药物组合物及其用途

    公开(公告)号：US08232299B2

    公开(公告)日：2012-07-31

    申请号：US12452206

    申请日：2008-06-20

    申请人： Laszlo Puskas ,  Liliana Feher ,  Eszter Molnar

    发明人： Laszlo Puskas ,  Liliana Feher ,  Eszter Molnar

    IPC分类号： A61K31/4035 ,  A61K31/4439 ,  A61K31/5377 ,  C07D413/12 ,  C07D407/12 ,  C07D209/48

    CPC分类号： C07D209/48 ,  C07D401/12

    摘要： The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C1-20-alkyl, —C2-20-alkenyl, —C2-20-alkinyl, —C5-6-cykloalkyl, aryl, aralkyl, adamantyl, heterocyclic, hydroxyl, hydroxyalkyl, Or —N—(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, —O—, —S—, —CH2-, or —NH—; Y is O or S; Z is O or S; R′ and R″ are each independently methyl, ethyl, isopropyl, isobuthyl, sec-butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R′, as well as R″ be isopropyl, and R1 and R2 be hydrogen at the same time. The present invention further relates to pharmaceutical compositions comprising such compounds and to use of such compounds for treatment of disease states.

    摘要翻译： 本发明涉及适用于治疗疾病状态并影响细胞囊泡系统，特别是脂滴形成和/或功能的化合物，所述化合物具有通式I（I），其中X各自独立地为氢，卤素， -C1-20-烷基，-C2-20-烯基，-C2-20-炔基，-C5-6-环烷基，芳基，芳烷基，金刚烷基，杂环，羟基，羟基烷基或-N-（R1，R2）基团 ; n为0,1,2,3或4; R 1和R 2可各自独立地为氢，直链或支链烷基，环烷基，芳基，芳烷基，杂环基，其中各自为未取代或卤素取代的; 或者R1和R2与它们之间的氮一起形成5或6元环; A是单键，-O - ， - S - ， - CH 2 - 或-NH-; Y为O或S; Z是O或S; R'和R“各自独立地为甲基，乙基，异丙基，异丁基，仲丁基或叔丁基; 其限制为：X（n）不能全部为氟，A为单键，Y为Z，O为R，R'为R“为异丙基，R 1和R 2为氢 同一时间。 本发明还涉及包含这些化合物的药物组合物和这些化合物用于治疗疾病状态。

    PHTHALIMIDE DERIVATIVES THAT INFLUENCE CELLULAR VESICULAR SYSTEMS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF
    2.
    发明申请
    PHTHALIMIDE DERIVATIVES THAT INFLUENCE CELLULAR VESICULAR SYSTEMS, PHARMACEUTICAL COMPOSITIONS, AND USE THEREOF 失效
    影响细胞体外系统，药物组合物及其用途的邻苯二甲酰亚胺衍生物

    公开(公告)号：US20100184762A1

    公开(公告)日：2010-07-22

    申请号：US12452206

    申请日：2008-06-20

    申请人： Laszlo Puskas ,  Liliana Feher ,  Eszter Molnar

    发明人： Laszlo Puskas ,  Liliana Feher ,  Eszter Molnar

    IPC分类号： A61K31/4035 ,  C07D209/48 ,  C07D401/12 ,  C07D413/12 ,  A61K31/4439 ,  A61K31/5377 ,  A61P35/00 ,  A61P29/00 ,  A61P9/10 ,  A61P31/04 ,  A61P31/12

    CPC分类号： C07D209/48 ,  C07D401/12

    摘要： The present invention relates to compounds that are suitable for treatment of disease states and influence cellular vesicular systems, especially the formation and/or function of lipid droplets, said compound having the general formula I (I) wherein X are each independently hydrogen, halogen, —C1-20-alkyl, —C2-20-alkenyl, —C2-20-alkinyl, —C5-6-cykloalkyl, aryl, aralkyl, adamantyl, heterocyclic, hydroxyl, hydroxyalkyl, Or —N—(R1, R2) group; n is 0, 1, 2, 3, or 4; R1 and R2 may each be independently hydrogen, straight or branching alkyl, cyclo-alkyl, aryl, aralkyl, heterocyclic group, wherein each is un-substituted or halogen substituted; or R1 and R2 together with the nitrogen in between them form a 5 or 6 member ring; A is a single bond, —O—, —S—, —CH2-, or —NH—; Y is O or S; Z is O or S; R′ and R″ are each independently methyl, ethyl, isopropyl, isobuthyl, sec-butyl or terc-butyl; with the restriction that: X(n) cannot all be fluorine, and A be a single bond, and Y, as well as Z be O, and R′, as well as R″ be isopropyl, and R1 and R2 be hydrogen at the same time. The present invention further relates to pharmaceutical compositions comprising such compounds and to use of such compounds for treatment of disease states.

    摘要翻译： 本发明涉及适用于治疗疾病状态并影响细胞囊泡系统，特别是脂滴形成和/或功能的化合物，所述化合物具有通式I（I），其中X各自独立地为氢，卤素， -C1-20-烷基，-C2-20-烯基，-C2-20-炔基，-C5-6-环烷基，芳基，芳烷基，金刚烷基，杂环，羟基，羟基烷基或-N-（R1，R2）基团 ; n为0,1,2,3或4; R 1和R 2可各自独立地为氢，直链或支链烷基，环烷基，芳基，芳烷基，杂环基，其中各自为未取代或卤素取代的; 或者R1和R2与它们之间的氮一起形成5或6元环; A是单键，-O - ， - S - ， - CH 2 - 或-NH-; Y为O或S; Z是O或S; R'和R“各自独立地为甲基，乙基，异丙基，异丁基，仲丁基或叔丁基; 其限制为：X（n）不能全部为氟，A为单键，Y为Z，O为R，R'为R“为异丙基，R 1和R 2为氢 同一时间。 本发明还涉及包含这些化合物的药物组合物和这些化合物用于治疗疾病状态。

    ACTIVE CARRIER, ITS PRODUCTION AND ITS USE
    3.
    发明申请
    ACTIVE CARRIER, ITS PRODUCTION AND ITS USE 审中-公开
    主动承运人，其生产及其使用

    公开(公告)号：US20100022415A1

    公开(公告)日：2010-01-28

    申请号：US12310306

    申请日：2007-08-21

    申请人： Laszlo Puskas ,  Eszter Molnar

    发明人： Laszlo Puskas ,  Eszter Molnar

    IPC分类号： C40B50/00 ,  C07F7/02

    CPC分类号： G01N33/54353

    摘要： Active carrier that consists of a carrier base (1) and attached linkers containing activated linker functional groups. The active carrier contains two or more different activated linker functional groups. A process for the production of the active carrier that comprises a carrier base (1) and linkers containing activated linker functional groups. Steps of the process: a) binding of a linker containing one or more linker functional groups to the carrier base (1), through the carrier functional groups; and b) reacting the linker functional groups of the linkers bound to the carrier base in step a) with two or more different activating reagents simultaneously. Use of the active carrier, during which the surface of the active carrier is contacted with one or more solution of small molecules.

    摘要翻译： 活性载体由载体碱基（1）和含有活化的接头官能团的连接基团组成。 活性载体含有两个或多个不同的活化的接头官能团。 一种制备活性载体的方法，其包含载体碱（1）和含有活化的连接官官团的连接体。 该方法的步骤：a）通过载体官能团将含有一个或多个连接基官能团的接头与载体基团（1）结合; 和b）使步骤a）中与载体碱结合的接头的接头官能团与两种或更多种不同的活化剂同时反应。 使用活性载体，在此期间活性载体的表面与一种或多种小分子溶液接触。

    8-HYDROXY-QUINOLINE DERIVATIVES
    4.
    发明申请
    8-HYDROXY-QUINOLINE DERIVATIVES 有权
    8-羟基喹啉衍生物

    公开(公告)号：US20130131096A1

    公开(公告)日：2013-05-23

    申请号：US13696541

    申请日：2011-05-06

    申请人： Laszlo Puskas ,  Csaba Szabo ,  Ivan Kanizsai ,  Mario Gyuris ,  Ramona Madacsi ,  Bela Ozsvari ,  Liliana Feher ,  Gabor Tamas

    发明人： Laszlo Puskas ,  Csaba Szabo ,  Ivan Kanizsai ,  Mario Gyuris ,  Ramona Madacsi ,  Bela Ozsvari ,  Liliana Feher ,  Gabor Tamas

    IPC分类号： C07D413/12 ,  C07D401/14 ,  C07D401/10 ,  C07D401/12 ,  C07D215/26

    CPC分类号： C07D413/12 ,  C07D215/26 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14

    摘要： The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2). The compounds according to the invention can be used in the medicine mainly for the treatment of diseases associated with neurological and/or oxidative stress.

    摘要翻译： 本发明涉及通式（I）的化合物及其药学上可接受的盐（式中R1表示氢原子，低级烷基，低级烯基，低级环烷基，芳基，芳烷基或杂环基，其中， 上述基团任选在邻位，间位和/或对位用1,2,3或4个吸电子基团或给电子基团取代; R 2表示氢原子，低级烷基，芳基，芳烷基或杂环基，其中 上述基团任选被一个或多个卤素原子取代; R 3表示低级烷基，芳基，芳烷基或杂环基，其中上述基团在邻位，间位或对位任选被取代1,2,3或4 吸电子基团或给电子基团; R 4表示氢原子，低级烷基或任何酸性官能团; n为1或2）。 根据本发明的化合物可用于药物中，主要用于治疗与神经和/或氧化应激有关的疾病。

    8-hydroxy-quinoline derivatives
    5.
    发明授权
    8-hydroxy-quinoline derivatives 有权
    8-羟基 - 喹啉衍生物

    公开(公告)号：US08871937B2

    公开(公告)日：2014-10-28

    申请号：US13696541

    申请日：2011-05-06

    申请人： Laszlo Puskas ,  Csaba Szabo ,  Ivan Kanizsai ,  Mario Gyuris ,  Ramona Madacsi ,  Bela Ozsvari ,  Liliana Feher ,  Gabor Tamas

    发明人： Laszlo Puskas ,  Csaba Szabo ,  Ivan Kanizsai ,  Mario Gyuris ,  Ramona Madacsi ,  Bela Ozsvari ,  Liliana Feher ,  Gabor Tamas

    IPC分类号： C07D215/38 ,  C07D401/10 ,  C07D401/06 ,  C07D401/14 ,  C07D413/12 ,  C07D401/12 ,  C07D215/26

    CPC分类号： C07D413/12 ,  C07D215/26 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14

    摘要： The invention relates to compounds of the general formula (I) and their pharmaceutically acceptable salts (in which formula R1 represents a hydrogen atom, lower alkyl group, lower alkenyl group, lower cycloalkyl group, aryl group, aralkyl group or heterocyclic group, wherein, the above groups are optionally substituted in ortho, meta and/or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R2 represents a hydrogen atom, lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted with one or more halogen atoms; R3 represents a lower alkyl group, aryl group, aralkyl group or heterocyclic group wherein the above groups are optionally substituted in ortho, meta or para position with 1, 2, 3 or 4 electron withdrawing groups or electron donating groups; R4 represents a hydrogen atom, lower alkyl group or any acidic functional group; n is 1 or 2). The compounds according to the invention can be used in the medicine mainly for the treatment of diseases associated with neurological and/or oxidative stress.

    摘要翻译： 本发明涉及通式（I）的化合物及其药学上可接受的盐（式中R1表示氢原子，低级烷基，低级烯基，低级环烷基，芳基，芳烷基或杂环基，其中， 上述基团任选在邻位，间位和/或对位用1,2,3或4个吸电子基团或给电子基团取代; R 2表示氢原子，低级烷基，芳基，芳烷基或杂环基，其中 上述基团任选被一个或多个卤素原子取代; R 3表示低级烷基，芳基，芳烷基或杂环基，其中上述基团在邻位，间位或对位任选被取代1,2,3或4 吸电子基团或给电子基团; R 4表示氢原子，低级烷基或任何酸性官能团; n为1或2）。 根据本发明的化合物可用于药物中，主要用于治疗与神经和/或氧化应激有关的疾病。

    Use Of Genes As Molecular Markers In Diagnosis Of Schizophrenia And Diagnostic Kit For The Same
    6.
    发明申请
    Use Of Genes As Molecular Markers In Diagnosis Of Schizophrenia And Diagnostic Kit For The Same 审中-公开
    使用基因作为精神分裂症诊断分子标记和诊断试剂盒

    公开(公告)号：US20080274455A1

    公开(公告)日：2008-11-06

    申请号：US11568467

    申请日：2005-05-02

    申请人： Laszlo Puskas ,  Agnes Zvara ,  Miklos Santha ,  Gyorgy Szekeres ,  Zoltan Janka

    发明人： Laszlo Puskas ,  Agnes Zvara ,  Miklos Santha ,  Gyorgy Szekeres ,  Zoltan Janka

    IPC分类号： C12Q1/68 ,  C40B30/04 ,  C12Q1/02 ,  G01N33/53 ,  C07H21/04

    CPC分类号： C12Q1/6883 ,  C12Q2600/136 ,  C12Q2600/158

    摘要： Drug-naive and drug-free schizophrenic PBL were screened to identify additional markers that are differentially expressed compared to healthy individuals using microarray and quantitative real-time PCR (QRT-PCR) techniques. Genes for dopamine D2 receptor (DRD2) and inwardly rectifying potassium channel (Kir2.3) were found to be overexpressed in microarray analysis. Increased mRNA levels were confirmed by QRT-PCR using SybrGreen method and dual labeled TaqMan probes.The invention relates to a method for diagnosing schizophrenia in a subject comprising assessing the level or the expression level of at least one of the following genes or proteins: Kir2.3 or DRD2 or a gene encoding Kir2.3 or DRD2. The invention further relates to agents and uses thereof, said agents specifically binding to said proteins or nucleic acids encoding them, diagnostic kits and screening methods.Use of both molecular markers allow prediction of schizophrenia and help to follow efficiency of drugs in therapy in order to provide a more tailored medication for schizophrenic patients.

    摘要翻译： 筛选无天真和无药物精神分裂症的PBL，以鉴定与使用微阵列和定量实时PCR（QRT-PCR）技术的健康个体差异表达的其他标志物。 发现多巴胺D 2受体（DRD2）和内向整流钾通道（Kir2.3）的基因在微阵列分析中过表达。 使用SybrGreen方法和双重标记的TaqMan探针通过QRT-PCR证实增加的mRNA水平。 本发明涉及用于诊断受试者中精神分裂症的方法，包括评估至少一种以下基因或蛋白质的水平或表达水平：Kir2.3或DRD2或编码Kir2.3或DRD2的基因。 本发明还涉及其药剂及其用途，所述药剂特异性结合所述蛋白质或编码它们的核酸，诊断试剂盒和筛选方法。 使用两种分子标记物可以预测精神分裂症，并有助于追踪药物在治疗中的效率，以便为精神分裂症患者提供更定制的药物。

    Synergistically active veterinary compositions and process for preparing same
    9.
    发明授权
    Synergistically active veterinary compositions and process for preparing same 失效
    合成活性兽药组合物及其制备方法

    公开(公告)号：US5120711A

    公开(公告)日：1992-06-09

    申请号：US616813

    申请日：1990-11-20

    申请人： Karoly Magyar ,  Ferenc Simon ,  Janos Varga ,  Attila Nagy ,  Laszlo Puskas ,  Pal Fekete ,  Janos Egri ,  Katalin Zukovics

    发明人： Karoly Magyar ,  Ferenc Simon ,  Janos Varga ,  Attila Nagy ,  Laszlo Puskas ,  Pal Fekete ,  Janos Egri ,  Katalin Zukovics

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61P15/00 ,  A61P15/14

    CPC分类号： A61K38/04

    摘要： The invention relates to synergistically active veterinary compositions useful particularly for the treatment of mastitis and metritis. The invention further relates to a process for preparing these compositions. The compositions according to the invention comprise, based on 1 part by weight of 6,9,18-tris(2-aminoethyl) -15-benzyl-21-[.sup.- 2,8-bis(2-aminoethyl)-5-(1-hydroxyethyl) -15-methyl-4,7,10-trioxo-3,6,9-triazaheptadecanamido]-3-(1-hydroxyethyl)-12-isobutyl-1,4,7,10,13,16,19-heptaazacyclotricosane-2, 5,8,11,14,17,20-heptaone or a pharmaceutically acceptable acid addition salt thereof, 1 to 1000 parts by weight of 1-(2-chlorophenyl)-diphenylmethyl-1H-imidazole or 1 to 400 parts by weight of 2-methyl-5,7-dichloro-8-hydroxyquinoline, respectively, optionally in admixture with carriers and/or additives commonly used in the pharmaceutical industry.

    摘要翻译： 本发明涉及特别用于治疗乳腺炎和子宫炎的协同作用的兽医学组合物。 本发明还涉及制备这些组合物的方法。 根据本发明的组合物包含基于1重量份的6,9,18-三（2-氨基乙基）-15-苄基-21 - [ - 2,8-双（2-氨基乙基）-5-（ 1-羟乙基）-15-甲基-4,7,10-三氧代-3,6,9-三氮杂十七烷酰胺基] -3-（1-羟基乙基）-12-异丁基-1,4,7,10,13,16 ，19-七氮杂环五烷-2,5,8,11,14,17,20-七酮或其药学上可接受的酸加成盐，1〜1000重量份的1-（2-氯苯基） - 二苯基甲基-1H-咪唑或 1至400份（重量）的2-甲基-5,7-二氯-8-羟基喹啉，分别任选与制药工业中通常使用的载体和/或添加剂混合。