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    Selective caspase inhibitors and uses thereof
    2.
    发明授权
    Selective caspase inhibitors and uses thereof 有权
    选择性胱天蛋白酶抑制剂及其用途

    公开(公告)号：US09045524B2

    公开(公告)日：2015-06-02

    申请号：US13321681

    申请日：2010-05-21

    申请人： Jan-Eric Ahlfors ,  Khalid Mekouar

    发明人： Jan-Eric Ahlfors ,  Khalid Mekouar

    IPC分类号： C07K5/08 ,  C07K5/10 ,  A61K38/00 ,  C07K5/02 ,  C07K5/093 ,  C07K14/81

    CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0819 ,  C07K14/8139

    摘要： The present invention relates to compounds of Formula I, II, IVC, VIIIC, IXC, or XC and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, II, IVC, VIIIC, IXC, or XC are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases). Processes for synthesizing tripeptides are provided.

    摘要翻译： 本发明涉及式I，II，IVC，VIIIC，IXC或XC的化合物及其药物用途。 本发明的特定方面涉及这些化合物用于选择性抑制一种或多种半胱天冬酶的用途。 还描述了将式I，II，IVC，VIIIC，IXC或XC的化合物用于预防和/或治疗受试者中的各种疾病和病症的方法，包括半胱天冬酶介导的疾病如败血症，心肌梗死， 缺血性中风，脊髓损伤（SCI），创伤性脑损伤（TBI）和神经变性疾病（例如多发性硬化症（MS）和阿尔茨海默氏症，帕金森病和亨廷顿疾病）。 提供了合成三肽的方法。

    SELECTIVE CASPASE INHIBITORS AND USES THEREOF
    3.
    发明申请
    SELECTIVE CASPASE INHIBITORS AND USES THEREOF 有权
    选择性CASPASE抑制剂及其用途

    公开(公告)号：US20120157394A1

    公开(公告)日：2012-06-21

    申请号：US13321681

    申请日：2010-05-21

    申请人： Jan-Eric Ahlfors ,  Khalid Mekouar

    发明人： Jan-Eric Ahlfors ,  Khalid Mekouar

    IPC分类号： A61K38/07 ,  C07K5/08 ,  A61K38/06 ,  C07K5/10

    CPC分类号： C07K5/0202 ,  A61K38/00 ,  C07K5/0819 ,  C07K14/8139

    摘要： The present invention relates to compounds of Formula I, II, IVC, VIIIC, IXC, or XC and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more caspases. Also described are methods where the compounds of Formula I, II, IVC, VIIIC, IXC, or XC are used in the prevention and/or treatment of various diseases and conditions in subjects, including caspase-mediated diseases such as sepsis, myocardial infarction, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative disease (e.g. multiple sclerosis (MS) and Alzheimer's, Parkinson's, and Huntington's diseases). Processes for synthesizing tripeptides are provided.

    摘要翻译： 本发明涉及式I，II，IVC，VIIIC，IXC或XC的化合物及其药物用途。 本发明的特定方面涉及这些化合物用于选择性抑制一种或多种半胱天冬酶的用途。 还描述了将式I，II，IVC，VIIIC，IXC或XC的化合物用于预防和/或治疗受试者中的各种疾病和病症的方法，包括半胱天冬酶介导的疾病如败血症，心肌梗死， 缺血性中风，脊髓损伤（SCI），创伤性脑损伤（TBI）和神经变性疾病（例如多发性硬化症（MS）和阿尔茨海默氏症，帕金森病和亨廷顿疾病）。 提供了合成三肽的方法。

    Anti-viral 7-deaza D-nucleosides and uses thereof
    4.
    发明申请
    Anti-viral 7-deaza D-nucleosides and uses thereof 审中-公开
    抗病毒7-脱氮D-核苷及其用途

    公开(公告)号：US20050026853A1

    公开(公告)日：2005-02-03

    申请号：US10627586

    申请日：2003-07-25

    申请人： Khalid Mekouar ,  Robert Deziel

    发明人： Khalid Mekouar ,  Robert Deziel

    IPC分类号： C07H19/14 ,  A61K31/7064 ,  A61P31/12 ,  A61P31/20 ,  C07H19/00 ,  C07H19/22 ,  A61K31/7076

    CPC分类号： C07H19/00 ,  C07H19/22

    摘要： The present invention relates generally to anti-viral compounds, particularly anti-viral 7-deaza D-nucleosides and analogues, or derivatives thereof. The invention also relates to the use of such compounds to treat or prevent hepatitis B virus (HBV) infections, and to the use of such compounds to examine the biological mechanisms of HBV infection.

    摘要翻译： 本发明一般涉及抗病毒化合物，特别是抗病毒7-脱氮D-核苷及其类似物或其衍生物。 本发明还涉及这种化合物用于治疗或预防乙型肝炎病毒（HBV）感染的用途，以及使用这些化合物来检查HBV感染的生物学机制。

    Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof
    5.
    发明授权
    Quinoline derivatives, having in particular antiviral properties, preparation and biological applications thereof 失效
    喹啉衍生物，具有特别的抗病毒性质，其制备和生物应用

    公开(公告)号：US06670377B1

    公开(公告)日：2003-12-30

    申请号：US09402858

    申请日：2001-01-16

    申请人： Khalid Mekouar ,  Jean D'Angelo ,  Didier Desmaele ,  Jean-Francois Mouscadet ,  Frèdèric Subra ,  Christian Auclair

    发明人： Khalid Mekouar ,  Jean D'Angelo ,  Didier Desmaele ,  Jean-Francois Mouscadet ,  Frèdèric Subra ,  Christian Auclair

    IPC分类号： A61K3147

    CPC分类号： C07D215/26 ,  C07D215/14 ,  C07D215/48

    摘要： The invention concerns quinoline derivatives of formula (I) in which: Ra, Rb and Rc, identical or different represent one or several substituents, themselves identical or different, in any position on the cycles, this or these substituents being selected among a —(CH2)n—Y or —CH═CH—Y group, in which Y is halogen, —OH, —OR, —COH, —COR, —COOH, COOR, —COH, —COR, —CONH2, —CON(Rx, Ry)—CH═NOH, —CO— —CH═NOH, —NH2, —N(Rx, Ry), —NO2, —PO(OR)2—SH2, —SR, —SO2R, —SO2NHR, CN, or Z(Rc) in which R is a C1-C8 alkyl, or aryl or a heterocyclic compound, Rx and Ry, identical or different are C1-C5 alkyl, an aryl or heterocyclic compound and n is nil or a whole number between 1 and 5 Rb can further represent a hydrogen, and when Y is —COOH or —COOR in Rc, Z, if it represents an aryl, comprises at least 3 substituents or the quinoline ring is trisubstituted; X is an ethylene double bond; a —(CH2)n— group in which n is a whole number between 1 and 5: or a —CH(Rd—CH(Re) group, Rd and Re, identical or different, representing a hydrogen, a halogen, hydroxy or epoxy; or a —(CH2)n, —O—C—(CH2)m—, —(CH2)n, —C(O)—O—(CH2)m, —(CH2)n, —O—(CH2)m—, (CH2)n, —N(Q)—(CH2)m—, or (CH2)n, —S(O)—(CH2)m—, group, in which n=1 to 8, m=0 to 8, t=0, 1 or 2, and Q=h, aryl or alkyl. The invention also concerns the pharmaceutically acceptable salts of these derivatives, the diastereoisomeric and the enantiomeric forms thereof. The invention is useful as medicines with HIV anti-integrase inhibiting effect.

    摘要翻译： 本发明涉及式（I）的喹啉衍生物，其中：相同或不同的R a，R b和R c表示一个或几个取代基，它们在循环中的任何位置本身相同或不同，这些或这些取代基选自 - （ CH2）nY或-CH = CH-Y基，其中Y是卤素，-OH，-OR，-COH，-COR，-COOH，COOR，-COH，-COR，-CONH2，-CON（Rx，Ry ）-CH = NOH，-CO--CH = NOH，-NH2，-N（Rx，Ry），-NO2，-PO（OR）2-SH2，-SR，-SO2R，-SO2NHR，CN或Z （Rc）其中R为C1-C8烷基或芳基或杂环化合物，Rx和Ry相同或不同，为C1-C5烷基，芳基或杂环化合物，n为零或整数为1至5 如果R代表芳基，当Y是-COOH或-COOR时，R 3可以进一步代表氢，当代表芳基时，Z包含至少3个取代基或喹啉环是三取代的; X是乙烯双键; 其中n是1至5之间的整数的 - （CH 2）n - 基团或-CH（R d-CH（Re）基团，R d和R e相同或不同，表示氢，卤素，羟基或 环氧基或 - （CH 2）n，-OC-（CH 2）m - ， - （CH 2）n，-C（O）-O-（CH 2）m - ，（CH 2）n，-O- m - ，（CH2）n，-N（Q） - （CH2）m-或（CH2）n，-S（O） - （CH2）m-，其中n = 1至8，m = 0至8，t = 0,1或2，Q = h，芳基或烷基，本发明还涉及这些衍生物的药学上可接受的盐，其非对映异构体和对映体形式。本发明可用作具有HIV抗性的药物 - 内酯酶抑制作用。

    Selective Cysteine Protease Inhibitors and Uses Thereof
    8.
    发明申请
    Selective Cysteine Protease Inhibitors and Uses Thereof 有权
    选择性半胱氨酸蛋白酶抑制剂及其用途

    公开(公告)号：US20140038903A1

    公开(公告)日：2014-02-06

    申请号：US14111738

    申请日：2012-04-15

    申请人： Jan-Eric Ahlfors ,  Khalid Mekouar

    发明人： Jan-Eric Ahlfors ,  Khalid Mekouar

    IPC分类号： C07K5/103 ,  C07K5/02 ,  C07K5/083 ,  C07K5/062

    CPC分类号： C07K5/1008 ,  A61K38/06 ,  C07K5/02 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06095 ,  C07K5/06104 ,  C07K5/06113 ,  C07K5/0806 ,  C07K5/0808 ,  C07K5/081 ,  C07K5/0812 ,  C07K5/0819 ,  C07K5/0821 ,  C07K14/8139

    摘要： The present invention relates to compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 and their pharmaceutical uses. Particular aspects of the invention relate to the use of those compounds for the selective inhibition of one or more cysteine proteases. Also described are methods where the compounds of Formula I, II, IA-VA, IVA1-IVA5, IIIA1-IIIA5 are used in the prevention and/or treatment of various diseases and conditions in subjects, including cysteine protease-mediated diseases and/or caspase-mediated diseases such as sepsis, myocardial infarction, cancer, tissue atrophy, ischemia, ischemic stroke, spinal cord injury (SCI), traumatic brain injury (TBI) and neurodegenerative diseases such as multiple sclerosis (MS), ALS, Alzheimer's disease, Parkinson's disease, and Huntington's disease).

    摘要翻译： 本发明涉及式I，II，IA-VA，IVA1-IVA5，IIIA1-IIIA5的化合物及其药物用途。 本发明的特定方面涉及这些化合物用于选择性抑制一种或多种半胱氨酸蛋白酶的用途。 还描述了将式I，II，IA-VA，IVA1-IVA5，IIIA1-IIIA5的化合物用于预防和/或治疗受试者中的各种疾病和病症的方法，包括半胱氨酸蛋白酶介导的疾病和/或 胱天蛋白酶介导的疾病如败血症，心肌梗死，癌症，组织萎缩，缺血，缺血性中风，脊髓损伤（SCI），创伤性脑损伤（TBI）和神经变性疾病如多发性硬化（MS），ALS，阿尔茨海默病， 帕金森病和亨廷顿疾病）。

    Preparation of camptothecin and nothapodytine derivatives
    10.
    发明授权
    Preparation of camptothecin and nothapodytine derivatives 失效
    喜树碱和非生物素衍生物的制备

    公开(公告)号：US06500953B1

    公开(公告)日：2002-12-31

    申请号：US09744547

    申请日：2001-01-26

    申请人： Khalid Mekouar ,  Yves Genisson ,  Stefanie Leue ,  Andrew-Elliot Greene

    发明人： Khalid Mekouar ,  Yves Genisson ,  Stefanie Leue ,  Andrew-Elliot Greene

    IPC分类号： C07D49100

    CPC分类号： C07D471/14

    摘要： The invention concerns the preparation of nothapodytine or camptothecin derivatives which consists in causing 4-ethyl 2methyl hepta-2,4-dienoic acid act on a 3-aminomethyl 2-bromo quinoline derivative (III) wherein R1 and R2 are H or R1 is a halogen atom or alkyl, R2 is a O—CO—X radical as defined for the camptothecin derivatives; or R1 and R2 are defined for the known camptothecin derivatives or represent protected radicals or radicals easily convertible into the radicals R1 and R2, to obtain the quinoline derivative (IV); adding to the resulting quinoline derivative (2-methoxy carbonyl vinyl) tributyltin in the presence of a complex of palladium and triphenylarsin to obtain the quinoline derivative (V); cyclizing the resulting quinoline derivative to obtain the tetracyclic derivative (VI); then in subjecting said derivative to an ozonolysis followed by treatment with dimethyl sulphide to obtain the tetracyclic derivative (VII); saponification followed by decarboxylation in oxidising conditions of the resulting tetracyclic derivative to obtain the nothopodytine derivative (VIII); then optionally transforming the resulting derivative into a camptothecin derivative or into a mappicine derivative.

    摘要翻译： 本发明涉及制备异头蛇嘌呤或喜树碱衍生物，其中包括使4-乙基-2-甲基庚-2,4-二烯酸作用于3-氨基甲基2-溴喹啉衍生物（III），其中R 1和R 2为H或R 1为 卤素原子或烷基，R2是对于喜树碱衍生物所定义的O-CO-X基团; 或者R 1和R 2定义为已知的喜树碱衍生物，或表示易于转化成基团R 1和R 2的被保护的基团或基团，以获得喹啉衍生物（Ⅳ）。 在钯和三苯基胂络合物的存在下，向所得的喹啉衍生物（2-甲氧基羰基乙烯基）三丁基锡中加入，得到喹啉衍生物（Ⅴ）; 使得到的喹啉衍生物环化，得到四环衍生物（VI）; 然后使所述衍生物进行臭氧分解，然后用二甲基硫醚处理以获得四环衍生物（VII）; 皂化，随后在所得四环衍生物的氧化条件下脱羧，得到羟基喹啉衍生物（VIII）; 然后任选将得到的衍生物转化为喜树碱衍生物或映射蛋白衍生物。