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    NOVEL HELQUATS, THEIR PRECURSORS AND METHOD OF PREPARATION THEREOF
    2.
    发明申请
    NOVEL HELQUATS, THEIR PRECURSORS AND METHOD OF PREPARATION THEREOF 审中-公开
    新的帮助，他们的前提及其准备方法

    公开(公告)号：WO2010118711A2

    公开(公告)日：2010-10-21

    申请号：PCT/CZ2010000047

    申请日：2010-04-14

    Applicant: USTAV ORGANICKE CHEMIE A BIOCH ,  TEPLY FILIP ,  SEVERA LUKAS ,  ADRIAENSSENS LOUIS ,  VAVRA JAN

    Inventor： TEPLY FILIP ,  SEVERA LUKAS ,  ADRIAENSSENS LOUIS ,  VAVRA JAN

    CPC classification number: C07D471/04 ,  C07D401/06

    Abstract: Described are new helquats of general.formula I, their precursors of general formula II and III and methods of their preparation from compound of. general formula IV, where symbols S12, S1`2`, T23, T2`3` , R1 , R 2, X- have the meaning defined in description and claims. According to this invention it is possible e.g. from one non-symmetric compound of general formula IV (tether S1,2 is different from tether S1`2`) and 10 different alkylation agents to prepare 100 various helquats of general1, formula I and 90 various helquats without repetition of the alkylation agent. From symmetric compound of general formula IV (tether S1,2 is the same as tether S1`2` ) and 10 different alkylation agents it is possible to prepare 55 various helquats of general formula I and 45 various helquats without repetition of the alkylation agent.

    Abstract translation: 描述的是一般化合物I的新型，其通式II和III的前体及其由化合物制备的方法。 通式IV，其中符号S12，S1`2`，T23，T2`3`，R1，R2，X-具有在说明书和权利要求书中限定的含义。 根据本发明， 从一种不对称的通式IV化合物（系链S1,2不同于系链S1`2'）和10种不同的烷基化剂，以制备100种各种通用化合物1，式I和90种各种helquats而不重复烷基化试剂。 从通式IV的对称化合物（系链S1,2与系链S1`2`相同）和10种不同的烷基化试剂，可以制备55种各种通式I和45的各种helquats，不用重复烷基化试剂。

    NOVEL ANTIMICROBIAL PEPTIDES AND THEIR APPLICATION
    6.
    发明申请
    NOVEL ANTIMICROBIAL PEPTIDES AND THEIR APPLICATION 审中-公开
    新型抗微生物肽及其应用

    公开(公告)号：WO2009109156A3

    公开(公告)日：2010-04-29

    申请号：PCT/CZ2009000034

    申请日：2009-03-03

    Applicant: USTAV ORGANICKE CHEMIE A BIOCH ,  CEROVSKY VACLAV ,  SLANINOVA JIRINA ,  HOVORKA OLDRICH ,  CVACKA JOSEF ,  VOBURKA ZDENEK ,  FUCIK VLADIMIR ,  BEDNAROVA LUCIE ,  VOTRUBA IVAN ,  BOROVICKOVA LENKA ,  TURANEK JAROSLAV

    Inventor： CEROVSKY VACLAV ,  SLANINOVA JIRINA ,  HOVORKA OLDRICH ,  CVACKA JOSEF ,  VOBURKA ZDENEK ,  FUCIK VLADIMIR ,  BEDNAROVA LUCIE ,  VOTRUBA IVAN ,  BOROVICKOVA LENKA ,  TURANEK JAROSLAV

    IPC: C07K7/08 ,  A61K38/10

    CPC classification number: C07K14/43572 ,  A61K38/00 ,  C07K7/08

    Abstract: This invention involves four novel peptides of the formulas I, II, III a IV isolated from natural sources and their synthetic analogs of general formula V and VI, where R 1 represents acyl, alkyl or unprotected amino group, R 2 represents amid, substituted amid, unprotected carboxylic group or ester, Xaa represents, independently from each other, proteinogenic amino acid, D-amino acid, non-standard amino acid or amino acid with the side chain modification, n means position of the amino acid replacement and m means the number of the replacements in the peptide chain, and their applications as antimicrobial, antiviral, antifungal, antiparasitic and anticancer compounds. Therefore, they are practical for the production of medication for the treatment of microbial, parasitic and fungal diseases and for the cancer treatment. Formulas for summary: H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH2 (I) H-VaI-Asn-Trp-Lys-Lys-VaI-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH2 (II) H-VaI-Asn-Trp-Lys-Lys-IIe-Leu-GIy-Lys-IIe-IIe-Lys-VaI-AIa-Lys-NH2 (III) H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-NH2 (IV) R1-[Xaan]m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R2 (V) R1-[Xaan]m-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R2 (VI)

    Abstract translation: 本发明涉及从天然来源分离的四种分子式I，II，III和IV的新型肽及其通式V和VI的合成类似物，其中R 1表示酰基，烷基或未被保护的氨基，R 2表示氨基，取代的氨基 ，未被保护的羧基或酯，Xaa彼此独立地表示蛋白质氨基酸，D-氨基酸，非标准氨基酸或具有侧链修饰的氨基酸，n表示氨基酸置换的位置，m表示 肽链中的替代物的数量，以及它们作为抗微生物剂，抗病毒剂，抗真菌剂，抗寄生虫和抗癌化合物的应用。 因此，它们可用于生产用于治疗微生物，寄生虫和真菌疾病和癌症治疗的药物。 总结公式：H-Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-NH2（I） Asn-Trp-Lys-Lys-Val-Leu-Gly-Lys-IIe-IIe-Lys-Val-Ala-Lys-NH2（II）H-Val-Asn-Trp-Lys-Lys-IIe-Leu- Lys-IIe-IIe-Lys-Val-Ala-Lys-NH 2（III）H-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val- NH 2（IV）R 1 - [Xanan] m -Gly-Phe-Leu-Ser-Ile-Leu-Lys-Lys-Val-Leu-Pro-Lys-Val-Met-Ala-His-Met-Lys-R2 ）R1- [Xanan] m-Val-Asn-Trp-Lys-Lys-Ile-Leu-Gly-Lys-Ile-Ile-Lys-Val-Val-Lys-R2（VI）

    NATURAL BRASSINOSTEROIDS FOR USE FOR TREATING HYPERPROLIFERATION, TREATING PROLIFERATIVE DISEASES AND REDUCING ADVERSE EFFECTS OF STEROID DYSFUNCTION IN MAMMALS, PHARMACEUTICAL COMPOSITION AND ITS USE
    8.
    发明申请
    NATURAL BRASSINOSTEROIDS FOR USE FOR TREATING HYPERPROLIFERATION, TREATING PROLIFERATIVE DISEASES AND REDUCING ADVERSE EFFECTS OF STEROID DYSFUNCTION IN MAMMALS, PHARMACEUTICAL COMPOSITION AND ITS USE 审中-公开
    用于治疗高血压，治疗增殖性疾病和减少母体，药物组合物中甾体功能障碍的不良影响的天然铜蓝蛋白

    公开(公告)号：WO2009024103A3

    公开(公告)日：2009-07-16

    申请号：PCT/CZ2008000097

    申请日：2008-08-20

    Applicant: USTAV ORGANICKE CHEMIE A BIOCH ,  UNIVERZITA PALACKEHO V OLOMOUC ,  OKLESTKOVA JANA ,  HOFFMANNOVA LUCIE ,  STEIGEROVA JANA ,  KOHOUT LADISLAV ,  KOLAR ZDENEK ,  STRNAD MIROSLAV

    Inventor： OKLESTKOVA JANA ,  HOFFMANNOVA LUCIE ,  STEIGEROVA JANA ,  KOHOUT LADISLAV ,  KOLAR ZDENEK ,  STRNAD MIROSLAV

    IPC: C07J73/00 ,  A61K31/575 ,  A61K31/58 ,  A61P35/04 ,  C07D313/10 ,  C07J9/00 ,  C07J17/00

    CPC classification number: C07J17/005 ,  C07D313/06 ,  C07D313/10 ,  C07J9/00 ,  C07J73/00

    Abstract: The present invention relates to natural brassinosteroids of general formula (I), wherein R is CH2 or O-CH2 group, R2 is hydrogen or hydroxyl, R3 is hydroxyl, R24 is alkyl or alkenyl, which are selected from the group consisting of methyl, ethyl, propyl, isopropyl, methylen, ethylen and propylen, and R25 is alkyl selected from the group consisting of methyl and ethyl, and a pharmaceutically acceptable salt thereof, for use for treating hyperproliferation, treating proliferative diseases and reducing adverse effects of steroid dysfunction in mammals. The present invention also provides methods capable to arrest of the cell cycle by natural brassinosteroids resulting in apoptotic changes in cancer cells. More specifically, the present invention relates to use for treatment of the adverse effects of hyperproliferation on mammalian cells in vitro and in vivo, especially treatment of hyperproliferative diseases in mammals by administering compositions containing natural brassinosteroids. This invention also describes new use for treating consisting in a new therapeutic way for modifying cell viability of human breast and prostate cancer cells.

    Abstract translation: 本发明涉及通式（I）的天然油菜素类固醇，其中R是CH 2或O-CH 2基，R 2是氢或羟基，R 3是羟基，R 24是烷基或链烯基，其选自甲基， 乙基，丙基，异丙基，亚甲基，亚乙基和丙基，R25为选自甲基和乙基的烷基及其药学上可接受的盐，用于治疗过度增生，治疗增殖性疾病和减少类固醇功能障碍的不良反应 哺乳动物。 本发明还提供能够通过天然的油菜素甾醇阻止细胞周期的方法，导致癌细胞凋亡的变化。 更具体地说，本发明涉及在体外和体内治疗过度增生对哺乳动物细胞的不利影响的用途，特别是通过施用含有天然油菜素内酯的组合物来治疗哺乳动物的过度增殖性疾病。 本发明还描述了用于治疗人类乳腺癌和前列腺癌细胞的细胞活力的新治疗方法的新用途。

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