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    Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors
    1.
    发明申请
    Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors 失效
    包含作为hdac抑制剂的酯或酮键的氨基甲酸化合物

    公开(公告)号：US20060058282A1

    公开(公告)日：2006-03-16

    申请号：US10542281

    申请日：2004-01-19

    申请人： Paul Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Aleksandrs Gutcaits ,  Irena Olutnika ,  Ludmila Serpionova ,  Vija Gailite ,  Rasma Bokaldere

    发明人： Paul Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Aleksandrs Gutcaits ,  Irena Olutnika ,  Ludmila Serpionova ,  Vija Gailite ,  Rasma Bokaldere

    IPC分类号： A61K31/55 ,  A61K31/445 ,  A61K31/40 ,  A61K31/397

    CPC分类号： C07C251/48 ,  C07C259/10 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/32

    摘要： This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently: —O—C(═O)— or —C(═O)—O— or —C(═O)—; Cy is a cyclyl group and is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q2 is an acid leader group, and is independently: C1-8alkylene; and is optionally substituted; or: Q2 is an acid leader group, and is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or C1-7alkylene-C5-20arylene-C1-7alkylene; and is optionally substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

    摘要翻译： 本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些式（I）氨基甲酸化合物：其中：J为连接官能团，独立地为-OC（-O） - 或-C（-O） -O-或-C（-O） - ; Cy是环基，并且独立地为：C 3-20碳环基，C 3-20杂环基或C 5-20芳基; 并且任选被取代; Q 1是环状前导基团，独立地是通过从具有4至7个环原子的饱和单环烃的环碳原子除去两个氢原子而获得的二价二齿基团，或者通过除去两个 具有4至7个环原子的饱和单环杂环化合物的环碳原子包括1个氮环原子或1个氧环原子的氢原子; 并且任选被取代; Q 2是酸前导基团，独立地是：C 1-8烷基; 并且任选被取代; 或：Q 2是酸前导基团，并且独立地为：C 5〜20亚芳基; C 5〜20亚芳基-C 1-7亚烷基; C 1-7亚烷基-C 5-20亚芳基; 或C 1-7亚烷基-C 5 - 亚芳基-C 1-7亚烷基; 并且任选被取代; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症 。

    Carbamic acid compounds comprising an ester or ketone linkage as HDAC inhibitors
    2.
    发明授权
    Carbamic acid compounds comprising an ester or ketone linkage as HDAC inhibitors 失效
    包含酯或酮键的氨基甲酸化合物作为HDAC抑制剂

    公开(公告)号：US07465719B2

    公开(公告)日：2008-12-16

    申请号：US10542281

    申请日：2004-01-19

    申请人： Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Aleksandrs Gutcaits ,  Irena Olutnika ,  Ludmila Serpionova ,  Vija Gailite ,  Rasma Bokaldere

    发明人： Paul W. Finn ,  Ivars Kalvinsh ,  Einars Loza ,  Aleksandrs Gutcaits ,  Irena Olutnika ,  Ludmila Serpionova ,  Vija Gailite ,  Rasma Bokaldere

    IPC分类号： A61K31/55 ,  A61K31/445

    CPC分类号： C07C251/48 ,  C07C259/10 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/32

    摘要： This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently:—O —C(═O)— or —C(═O)—O — or —C(═O)—; Cy is a cyclyl group and is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q2 is an acid leader group, and is independently: C1-8alkylene; and is optionally substituted; or: Q2 is an acid leader group, and is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or C1-7alkylene-C5-20aryleneC1-7alkylene; and is optionally substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC,and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.

    摘要翻译： 本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些式（I）的氨基甲酸化合物：其中：J为连接官能团，独立地为：-O-C（-O） - 或-C（ - O - ） - 或-C（ - O） - ; Cy是环状基团，独立地为：C 3-20碳环基，C 3-20杂环基或C 5-20芳基; 并且任选被取代; Q1是环状前导基团，并且独立地是通过从具有4至7个环原子的饱和单环烃的环碳原子中除去两个氢原子或通过从环碳原子中除去两个氢原子而获得的二价二齿基团 具有4至7个环原子的饱和单环杂环化合物，包括1个氮环原子或1个氧环原子; 并且任选被取代; Q2是酸性引导基团，独立地为：C1-8亚烷基; 并且任选被取代; 或：Q2是酸性引导基团，独立地为：C5-20亚芳基; C 5-20芳基-C 1-7亚烷基; C 1-7亚烷基-C 5 - 亚芳基; 或C 1-7亚烷基-C 5-20亚芳基C 1-7亚烷基; 并且任选被取代; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。 本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症 。

    CARRIER FOR TARGETING NERVE CELLS
    8.
    发明申请
    CARRIER FOR TARGETING NERVE CELLS 有权

    公开(公告)号：US20130315888A1

    公开(公告)日：2013-11-28

    申请号：US13867740

    申请日：2013-04-22

    申请人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    发明人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    IPC分类号： C12N9/52

    CPC分类号： C12N9/52 ,  A61K38/00 ,  C07K14/33 ,  C12Y304/24069 ,  Y02A50/469 ,  Y02A50/473

    摘要： The present invention relates to a transport protein which can be obtained by modifying the heavy chain of the neurotoxin formed by Clostridium botulinum wherein (i) the protein binds specifically to nerve cells with a higher or lower affinity as the native neurotoxin; (ii) the protein has an increased or reduced neurotoxicity compared to the native neurotoxin, the neurotoxicity being preferably determined in the hemidiaphragm assay; and/or (iii) the protein comprises a lower affinity against neutralizing antibodies compared to the native neurotoxin. The invention also relates to methods for producing the same and the use thereof in cosmetic and pharmaceutical compositions.

    Carrier for targeting nerve cells
    9.
    发明授权
    Carrier for targeting nerve cells 有权

    公开(公告)号：US08481040B2

    公开(公告)日：2013-07-09

    申请号：US11919302

    申请日：2006-04-26

    申请人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    发明人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    IPC分类号： C07K14/33

    CPC分类号： C12N9/52 ,  A61K38/00 ,  C07K14/33 ,  C12Y304/24069 ,  Y02A50/469 ,  Y02A50/473

    摘要： The present invention relates to a transport protein which can be obtained by modifying the heavy chain of the neurotoxin formed by Clostridium botulinum wherein (i) the protein binds specifically to nerve cells with a higher or lower affinity as the native neurotoxin; (ii) the protein has an increased or reduced neurotoxicity compared to the native neurotoxin, the neurotoxicity being preferably determined in the hemidiaphragma assay; and/or (iii) the protein comprises a lower affinity against neutralizing antibodies compared to the native neurotoxin. The invention also relates to methods for producing the same and the use thereof in cosmetic and pharmaceutical compositions.

    Carrier for targeting nerve cells
    10.
    发明申请
    Carrier for targeting nerve cells 有权
    用于靶向神经细胞的载体

    公开(公告)号：US20090311275A1

    公开(公告)日：2009-12-17

    申请号：US11919302

    申请日：2006-04-26

    申请人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    发明人： Andreas Rummel ,  Tanja Weil ,  Aleksandrs Gutcaits

    IPC分类号： A61K39/44 ,  C07K14/33 ,  C12P21/02 ,  C12N1/21 ,  C12N15/70 ,  C12N1/19 ,  C12N15/75 ,  C12N15/81 ,  A61K38/48

    CPC分类号： C12N9/52 ,  A61K38/00 ,  C07K14/33 ,  C12Y304/24069 ,  Y02A50/469 ,  Y02A50/473

    摘要： The present invention relates to a transport protein which can be obtained by modifying the heavy chain of the neurotoxin formed by Clostridium botulinum wherein (i) the protein binds specifically to nerve cells with a higher or lower affinity as the native neurotoxin; (ii) the protein has an increased or reduced neurotoxicity compared to the native neurotoxin, the neurotoxicity being preferably determined in the hemidiaphragma assay; and/or (iii) the protein comprises a lower affinity against neutralizing antibodies compared to the native neurotoxin. The invention also relates to methods for producing the same and the use thereof in cosmetic and pharmaceutical compositions.

    摘要翻译： 本发明涉及通过改变由肉毒梭菌形成的神经毒素的重链而获得的转运蛋白，其中（i）所述蛋白质以与天然神经毒素更高或更低的亲和力的神经细胞特异性结合; （ii）与天然神经毒素相比，蛋白质具有增加或减少的神经毒性，神经毒性优选在膈肌测定中确定; 和/或（iii）与天然神经毒素相比，蛋白质包含对中和抗体的较低亲和力。 本发明还涉及其制备方法及其在化妆品和药物组合物中的用途。