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1. 发明授权

US08748600B2 Cyclic triazo sodium channel blockers 有权
标题翻译：环状三唑钠通道阻滞剂
公开(公告)号：US08748600B2
公开(公告)日：2014-06-10
申请号：US13382741
申请日：2010-07-08
申请人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
发明人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
IPC分类号： C07D253/07 , A61K31/53 , A61P25/08 , A61P25/28 , A61P25/04
CPC分类号： C07D253/07 , C07D409/06
摘要： The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ═NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.
摘要翻译：本发明涉及具有钠通道阻断性质的三嗪化合物，以及该化合物用于制备用于治疗相关病症的药物的用途。三嗪化合物具有式（I），其中：R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; R 3和R 4均为碳环，杂环或烷基，可以相同或不同; 并且R 5为氢，烷基或环状芳基，条件是：当R 3和R 4均为烷基时，它们连接形成环烷基，R 5为环状芳基; 当R 3和R 4均为碳环或杂环基时，R 5为氢或烷基; 或其盐。

2. 发明申请

US20120135993A1 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 有权
公开(公告)号：US20120135993A1
公开(公告)日：2012-05-31
申请号：US13382741
申请日：2010-07-08
申请人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
发明人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
IPC分类号： A61K31/53 , C07D409/06 , C07D409/14 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/06 , A61P25/28 , A61P25/16 , C07D253/075 , A61P29/00
CPC分类号： C07D253/07 , C07D409/06
摘要： The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ═NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.
摘要翻译：本发明涉及具有钠通道阻断性质的三嗪化合物，以及该化合物用于制备用于治疗相关病症的药物的用途。三嗪化合物具有式（I），其中：R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; R 3和R 4均为碳环，杂环或烷基，可以相同或不同; 并且R 5为氢，烷基或环状芳基，条件是：当R 3和R 4均为烷基时，它们连接形成环烷基，R 5为环状芳基; 当R 3和R 4均为碳环或杂环基时，R 5为氢或烷基; 或其盐。

3. 发明申请

US20120135992A1 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 有权
公开(公告)号：US20120135992A1
公开(公告)日：2012-05-31
申请号：US13382720
申请日：2010-07-08
申请人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
发明人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
IPC分类号： A61K31/53 , C07D409/04 , C07D405/04 , C07D403/04 , C07D401/04 , A61P9/10 , A61P25/00 , A61P29/00 , A61P25/22 , A61P25/18 , A61P25/06 , A61P35/00 , A61P27/02 , A61P25/08 , A61P27/06 , A61P33/06 , C07D253/075
CPC分类号： C07D253/075 , C07C309/04 , C07C309/06 , C07C309/08 , C07D253/07 , C07D309/04 , C07D309/06 , C07D309/08 , C07D409/04
摘要： The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.
摘要翻译：本发明涉及具有钠通道阻断性质的三嗪化合物，以及该化合物用于制备用于治疗相关病症的药物的用途。化合物具有式（I）：其中z是单键或任选取代的连接基团，R 1是卤代烷基; 和A是任选取代的芳族杂环或碳环系; 或其盐。

4. 发明授权

US08748599B2 Cyclic triazo sodium channel blockers 有权
标题翻译：环状三唑钠通道阻滞剂
公开(公告)号：US08748599B2
公开(公告)日：2014-06-10
申请号：US13382720
申请日：2010-07-08
申请人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
发明人： Michael Leach , Karl Franzmann , Dieter Riddall , Laurence Harbige
IPC分类号： C07D253/07 , A61K31/53 , A61P25/08 , A61P25/28 , A61P25/04
CPC分类号： C07D253/075 , C07C309/04 , C07C309/06 , C07C309/08 , C07D253/07 , C07D309/04 , C07D309/06 , C07D309/08 , C07D409/04
摘要： The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.
摘要翻译：本发明涉及具有钠通道阻断性质的三嗪化合物，以及该化合物用于制备用于治疗相关病症的药物的用途。化合物具有式（I）：其中z是单键或任选取代的连接基团，R 1是卤代烷基; 和A是任选取代的芳族杂环或碳环系; 或其盐。

5. 发明授权

US08691818B2 Cyclic triazo and diazo sodium channel blockers 有权
标题翻译：环状三唑和重氮钠通道阻滞剂
公开(公告)号：US08691818B2
公开(公告)日：2014-04-08
申请号：US12811884
申请日：2009-01-16
申请人： Michael Leach , Laurence Harbige , Dieter Riddall , Karl Franzmann
发明人： Michael Leach , Laurence Harbige , Dieter Riddall , Karl Franzmann
IPC分类号： A61K31/53 , C07D253/06 , C07D253/08
CPC分类号： C07D253/075 , C07D253/06 , C07D253/07 , C07D253/10 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12
摘要： Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria.
摘要翻译： X和Y各自为N或C，X和Y中的至少一个为N的一般结构化合物; Z是单键或任选取代的连接基团R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; 或N *为NRaRb基团，其中Ra和Rb独立地为H或烷基; 或N *是任选取代的哌嗪基环; 并且A是任选取代的杂环或碳环系，其可以通过R 2与三偶氮/重氮环连接以形成稠合多环; 适用于治疗对钠通道阻滞剂和抗叶酸剂敏感的哺乳动物的疾病，特别是诸如癫痫，多发性硬化，青光眼和uev病，脑创伤和脑缺血性脑卒中，脑损伤，脊髓损伤，手术创伤神经退行性疾病，运动神经元疾病，阿尔茨海默病，帕金森病，慢性炎性疼痛，神经性疼痛，偏头痛，双相情感障碍，情绪，焦虑和认知障碍，精神分裂症和三叉神经性自主性头痛。用于治疗哺乳动物癌症; 并用于治疗疟疾。

6. 发明申请

US20110009413A1 CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS 有权
标题翻译：环状三唑和二氧化硅通道阻塞剂
公开(公告)号：US20110009413A1
公开(公告)日：2011-01-13
申请号：US12811884
申请日：2009-01-16
申请人： Michael Leach , Laurence Harbige , Dieter Riddall , Karl Franzmann
发明人： Michael Leach , Laurence Harbige , Dieter Riddall , Karl Franzmann
IPC分类号： A61K31/53 , C07D253/075 , C07D405/04 , C07D403/12 , C07D409/04 , C07D253/07 , C07D405/14 , C07D401/04 , A61P25/08 , A61P25/00 , A61P27/06 , A61P25/28 , A61P25/16 , A61P25/06 , A61P25/18 , A61P25/22 , A61P29/00
CPC分类号： C07D253/075 , C07D253/06 , C07D253/07 , C07D253/10 , C07D401/04 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12
摘要： Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ═NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia and trigeminal autonomic cephalalgias; for treatment of mammalian cancers; and for treatment of malaria.
摘要翻译： X和Y各自为N或C，X和Y中的至少一个为N的一般结构化合物; Z是单键或任选取代的连接基团R 1是氢或取代基; R2是氨基或取代基; 当R 1为氢时，N *为氨基，或当R 1为取代基时为= NH; 或N *为NRaRb基团，其中Ra和Rb独立地为H或烷基; 或N *是任选取代的哌嗪基环; 并且A是任选取代的杂环或碳环系，其可以通过R 2与三偶氮/重氮环连接以形成稠合多环; 适用于治疗对钠通道阻滞剂和抗叶酸剂敏感的哺乳动物的疾病，特别是诸如癫痫，多发性硬化，青光眼和uev病，脑创伤和脑缺血性脑卒中，脑损伤，脊髓损伤，手术创伤神经退行性疾病，运动神经元疾病，阿尔茨海默病，帕金森病，慢性炎性疼痛，神经性疼痛，偏头痛，双相情感障碍，情绪，焦虑和认知障碍，精神分裂症和三叉神经性自主性头痛。用于治疗哺乳动物癌症; 并用于治疗疟疾。

7. 发明授权

US08268823B2 Medical use of triazine derivatives 有权
标题翻译：医药用途三嗪衍生物
公开(公告)号：US08268823B2
公开(公告)日：2012-09-18
申请号：US12373561
申请日：2007-07-13
申请人： Michael Leach , Laurence Harbige , Dieter Riddall , Paul Barraclough
发明人： Michael Leach , Laurence Harbige , Dieter Riddall , Paul Barraclough
IPC分类号： A61K31/53
CPC分类号： A61K31/53 , Y02A50/411
摘要： Compounds of formula (I) especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or heterocyclyl-alkyl are disclosed.
摘要翻译：式（I）化合物，特别是其中R 1为任选取代的烷基，芳烷基或杂环基 - 烷基的化合物显示具有钠通道阻断剂或抗叶酸剂的活性。公开了一些其中R 1是芳烷基或杂环基 - 烷基的新化合物。

8. 发明申请

US20090291954A1 Medical Use of Triazine Derivatives 有权
标题翻译：三嗪衍生物的医疗用途
公开(公告)号：US20090291954A1
公开(公告)日：2009-11-26
申请号：US12373561
申请日：2007-07-13
申请人： Michael Leach , Laurence Harbige , Dieter Riddall , Paul Barraclough
发明人： Michael Leach , Laurence Harbige , Dieter Riddall , Paul Barraclough
IPC分类号： A61K31/53 , C07D253/06 , A61P25/00
CPC分类号： A61K31/53 , Y02A50/411
摘要： Compounds of formula (I) especially where R1 is an optionally substituted alkyl, aralkyl or heterocyclyl-alkyl group, are shown to have activity as sodium channel blockers or as antifolates. Some novel compounds where R1 is an aralkyl or hetero-cyclyl-alkyl are disclosed.
摘要翻译：式（I）化合物，特别是其中R 1为任选取代的烷基，芳烷基或杂环基 - 烷基的化合物显示具有钠通道阻断剂或抗叶酸剂的活性。公开了一些其中R 1是芳烷基或杂环烷基 - 烷基的新化合物。

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