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    Decladinosyl-macrolides with anti-inflammatory activity
    3.
    发明授权
    Decladinosyl-macrolides with anti-inflammatory activity 失效
    具有抗炎活性的宣称大肠杆菌素

    公开(公告)号：US07910559B2

    公开(公告)日：2011-03-22

    申请号：US11813876

    申请日：2006-01-13

    申请人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    发明人： Ognjen Culic ,  Martina Bosnar ,  Sulejman Alihodzic ,  Gorjana Lazarevski ,  Zorica Marusic Istuk ,  Antun Hutinec ,  Vanja Vela ,  Goran Kragol

    IPC分类号： A61K31/70 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-α, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.

    摘要翻译： 本发明涉及具有抗炎活性的新型半合成大环内酯类。 更具体地说，本发明涉及在C-3位上缺少被克拉替糖糖化的14-和15-元大环内酯，其药学上可接受的衍生物，其制备方法和中间体，含有它们的药物组合物及其活性和用途 特别是与过量分泌TNF-α，IL-1，IL-6，IL-8，IL-2或IL-5相关的那些疾病的治疗中， 和/或过度淋巴细胞增殖的抑制剂; 和/或过量粒细胞脱粒。

    Substituted 9A-N-[N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl] and 9A-N-[N'(B-Cyanoethyl)-N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl]Derivatives of 9-Deoxo-9-Dihydro-9A-Aza-9A-Homoerithomycin A
    4.
    发明申请
    Substituted 9A-N-[N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl] and 9A-N-[N'(B-Cyanoethyl)-N'-(Benzenesulfonyl)Carbamoyl-Y-Aminopropyl]Derivatives of 9-Deoxo-9-Dihydro-9A-Aza-9A-Homoerithomycin A 审中-公开
    9-Deoxo-取代的9A-N- [N' - （苯磺酰基）氨基甲酰基-N-氨基丙基]和9A-N- [N'（B-氰基乙基）-N' - （苯磺酰基）氨基甲酰基-Y-氨基丙基] 9-二氢-9A-Aza-9A-同源霉素A

    公开(公告)号：US20070270356A1

    公开(公告)日：2007-11-22

    申请号：US10534261

    申请日：2003-11-10

    申请人： Nedjeljko Kujundzic ,  Mirjana Krajacic ,  Karmen Brajsa

    发明人： Nedjeljko Kujundzic ,  Mirjana Krajacic ,  Karmen Brajsa

    IPC分类号： A61K31/7048 ,  A61P31/04 ,  C07H17/08

    CPC分类号： C07H17/08 ,  C07H17/00

    摘要： The invention relates to substituted 9a-N—[N′-(benzenesulfonyl)carbamoyl-γ-aminopropyl] and 9a-N—[N′-(β-cyanoethyl)-N′-(benzenesulfonyl)carbamoyl-γ-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-( )-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the formula (I) wherein R represents H or cladinosyl moiety, R1 represents H or β-cyanoethyl group an R2 represents II or fluoro, chloro and methyl group, and pharmaceutically acceptable salts thereof with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions as well as to the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings.

    摘要翻译： 本发明涉及取代的9a-N- [N' - （苯磺酰基）氨基甲酰基-γ-氨基丙基]和9a-N- [N' - （β-氰乙基）-N' - （苯磺酰基）氨基甲酰基-γ-氨基丙基]衍生物 的9-脱氧-9-二氢-9a-氮杂-9a-高雪霉素A和5-（（S） - 氨基甲酰基-9-脱氧-9-二氢-9a-氮杂-9a-高丝氨酸内酯A），这种新的半合成大环内酯类抗生素 ，其中R表示H或克拉糖苷基部分的式（I），R 1表示H或β-氰基乙基，R 2表示II或氟，氯和甲基 及其与无机或有机酸的药学上可接受的盐，用于制备药物组合物的方法以及将其组合物用于灭菌室和医疗仪器以及用于保护墙壁和木器漆。

    1-Aza-dibenzo[e,h]azulenes for the treatment of central nervous system diseases and disorders
    6.
    发明申请
    1-Aza-dibenzo[e,h]azulenes for the treatment of central nervous system diseases and disorders 审中-公开
    1-氮杂 - 二苯并[e，h]薁用于治疗中枢神经系统疾病和病症

    公开(公告)号：US20070111968A1

    公开(公告)日：2007-05-17

    申请号：US10595932

    申请日：2004-11-19

    申请人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic

    发明人： Mladen Mercep ,  Milan Mesic ,  Dijana Pesic

    IPC分类号： A61K31/695 ,  A61K31/55 ,  A61K31/407

    CPC分类号： A61K31/403 ,  A61K31/407 ,  A61K31/55

    摘要： The present invention relates to the use of compounds from the group of 1-aza-dibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates in a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.

    摘要翻译： 本发明涉及使用来自1-氮杂 - 二苯并[e，h]薁的化合物及其药理学上可接受的盐和溶剂合物在药物制剂中用于治疗和预防中枢的疾病，损害和障碍 神经系统（CNS）由生物胺或其他神经递质的神经化学平衡紊乱引起。

    3-Decladinosyl 9a-n-carbamoyl and 9a-n-thiocarbamoyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a
    8.
    发明申请
    3-Decladinosyl 9a-n-carbamoyl and 9a-n-thiocarbamoyl derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin a 审中-公开
    9-去氧-9-二氢-9a-氮杂-9a-高红霉素a的3-突变二糖基-9a-正 - 氨基甲酰基和9a-正 - 硫代氨基甲酰基衍生物

    公开(公告)号：US20070066544A1

    公开(公告)日：2007-03-22

    申请号：US10557025

    申请日：2004-05-11

    申请人： Zorica Marusic-Istuk ,  Nedjeljko Kujundzic ,  Stjepan Mutak

    发明人： Zorica Marusic-Istuk ,  Nedjeljko Kujundzic ,  Stjepan Mutak

    IPC分类号： A61K31/7052 ,  C07H17/08

    CPC分类号： C07H17/08

    摘要： The present invention relates to the new 3-decladinosyl derivatives of 9a-N-carbamoyl- and 9a-N-thiocarbamoyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.

    摘要翻译： 本发明涉及通式（I）的9a-N-氨基甲酰基 - 和9a-N-硫代氨基甲酰基-9-脱氧-9-二氢-9a-氮杂-9a-高红霉素A的新的3-降乳糖苷衍生物，它们的 与无机或有机酸及其水合物的药学上可接受的加成盐，用于合成具有抗菌活性的其它大环内酯类化合物的中间体，其制备方法，其与无机或有机酸及其水合物的药学上可接受的加成盐与该方法 用于制备药物组合物，以及用于治疗细菌感染的药物组合物。