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1. 发明授权

US07465719B2 Carbamic acid compounds comprising an ester or ketone linkage as HDAC inhibitors 失效
标题翻译：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。

2. 发明申请

US20060058282A1 Carbamic acid compounds comprising an ester or ketone linkage as hdac inhibitors 失效
标题翻译：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。

3. 发明授权

US07985753B2 Substituted pyrazolo[1,5-A]pyrimidines as metabotropic glutamate receptor modulators 失效
标题翻译：取代的吡唑并[1,5-A]嘧啶作为代谢型谷氨酸受体调节剂
公开(公告)号：US07985753B2
公开(公告)日：2011-07-26
申请号：US11890199
申请日：2007-08-03
申请人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
发明人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P25/02 , A61P35/00 , A61P25/22
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：取代的式（I）的吡唑并嘧啶衍生物，其中Y 1，Y 2，Y 3，Y 4表示N或C-，其中Y 1至Y 4中的至少两个表示碳原子，R 1表示氯或溴，R 2至R 7表示例如。氢，甲基或乙基; 并且R 10和R 11独立地表示例如。氢或C1-C6烷基是有效的mGluR5调节剂，可用于预防急性和慢性神经障碍。

4. 发明申请

US20080032998A1 Pyrazolopyrimidines, a process for their preparation and their use as medicine 审中-公开
标题翻译：吡唑并嘧啶，其制备方法及其用作药物
公开(公告)号：US20080032998A1
公开(公告)日：2008-02-07
申请号：US11890230
申请日：2007-08-03
申请人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
发明人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
IPC分类号： A61K31/519 , A61P1/00 , A61P25/00 , A61P3/00 , A61P35/00 , A61P9/00 , C07D239/70
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 independently represent e.g. hydrogen or C1-6-alkyl; R8 represents a radical R9 or a radical R10, whereby one of the two radicals R8 represents R9 and the other radical R8 represents Ret; R9 represents e.g. a phenyl or thiophene group, and R10 represents e.g. hydrogen or methyl; are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：式（I）的取代的吡唑并嘧啶衍生物其中R 1表示氯或溴; R 2，R 3，R 4，R 5，R 6和R 6，和 R＆lt; 7＆gt;独立地代表例如氢或C 1-6 - 烷基; R 8表示基团R 9或基团R 10，其中两个基团R 8中的一个表示 R 9和另一个基团R 8表示Ret; R 9表示例如，苯基或噻吩基团，R 10代表例如。氢或甲基; 是有效的mGluR5调节剂，可用于预防急性和慢性神经障碍。

5. 发明授权

US07947689B2 Substituted pyrazolo[1,5-a]pyrimidines as metabotropic glutamate receptor modulators 失效
标题翻译：取代的吡唑并[1,5-a]嘧啶作为代谢型谷氨酸受体调节剂
公开(公告)号：US07947689B2
公开(公告)日：2011-05-24
申请号：US11890211
申请日：2007-08-03
申请人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
发明人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
IPC分类号： C07D487/04 , A61K31/519 , A61P25/28 , A61P25/02 , A61P35/00 , A61P25/22
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2 and Y3 independently are e.g. CR10, NH, S or O, whereby at least one of Y1, Y2 and Y3 represents CR10; R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 represent e.g. hydrogen or C1-C6-alkyl, and R10 represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.
摘要翻译：本发明涉及式（I）的吡唑并嘧啶衍生物，其中Y 1，Y 2和Y 3独立地为例如。 CR10，NH，S或O，其中Y1，Y2和Y3中的至少一个表示CR10; R1代表氯或溴; R2，R3，R4，R5，R6和R7表示例如。氢或C 1 -C 6烷基，R 10代表例如。氢，卤素或苯基; 它们是有效的mGluR5调节剂，可用于治疗各种神经障碍。

6. 发明申请

US20080039458A1 Substituted pyrazolopyrimidines, a process for their preparation and their use as medicine 失效
标题翻译：取代的吡唑并嘧啶，其制备方法和用作药物
公开(公告)号：US20080039458A1
公开(公告)日：2008-02-14
申请号：US11890199
申请日：2007-08-03
申请人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
发明人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
IPC分类号： A61K31/5377 , A61K31/519 , A61P1/00 , A61P25/00 , A61P3/00 , A61P43/00 , A61P9/00 , C07D239/70 , C07D295/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2, Y3, Y4 represent N or C—, whereby at least two of the groups Y1 to Y4 represent a carbon atom, R1 represents chloro or bromo, R2 to R7 represent e.g. hydrogen, methyl or ethyl; and R10 and R11 independently represent e.g. hydrogen or C1-C6alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：其中Y 1，Y 2，Y 3，Y 4的取代的吡唑并嘧啶衍生物代表N 或C-，其中基团Y 1至Y 4中的至少两个表示碳原子，R 1表示氯或溴，R R＆lt; 2＆gt;〜＆lt; 7＆gt;表示例如氢，甲基或乙基; R 10和R 11独立地表示例如，氢或C 1 -C 6烷基是有效的mGluR5调节剂，并且可用于预防急性和慢性神经障碍。

7. 发明申请

US20080039476A1 Pyrazolopyrimidines, a process for their preparation and their use as medicine 失效
标题翻译：吡唑并嘧啶，其制备方法及其用作药物
公开(公告)号：US20080039476A1
公开(公告)日：2008-02-14
申请号：US11890211
申请日：2007-08-03
申请人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
发明人： Wojciech Danysz , Andrzej Dekundy , Mirko Hechenberger , Markus Henrich , Claudia Jatzke , Jens Nagel , Christopher Graham Raphael Parsons , Tanja Weil , Juris Fotins , Aleksandrs Gutcaits , Ivars Kalvinsh , Ronalds Zemribo , Valerjans Kauss
IPC分类号： A61K31/519 , A61P25/00 , C07D487/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The invention relates to pyrazolopyrimidine derivatives of formula (I) wherein Y1, Y2 and Y3 independently are e.g. CR10, NH, S or O, whereby at least one of Y1, Y2 and Y3 represents CR10; R1 represents chloro or bromo; R2, R3, R4, R5, R6 and R7 represent e.g. hydrogen or C1-C6-alkyl, and R10 represents e.g. hydrogen, halogen or phenyl; which are potent mGluR5 modulators and are e.g. useful for the treatment of various neurological disorders.
摘要翻译：本发明涉及式（I）的吡唑并嘧啶衍生物，其中Y 1，Y 2和Y 3独立地为例如。 CR 10，NH，S或O，由此Y 1，Y 2和Y 3中的至少一个，表示CR <10; R 1表示氯或溴; R 2，R 3，R 4，R 5，R 6和R 6，和 R＆lt; 7＆gt;代表例如氢或C 1 -C 6 - 烷基，R 10表示例如C 1 -C 6烷基。氢，卤素或苯基; 它们是有效的mGluR5调节剂，可用于治疗各种神经障碍。

8. 发明申请

US20130315888A1 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.

9. 发明授权

US08481040B2 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.

10. 发明申请

US20090311275A1 Carrier for targeting nerve cells 有权
标题翻译：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。

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