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1. 发明公开

EP2451806A2 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 失效
标题翻译： CYCLIC三偶氮钠通道阻断剂
公开(公告)号：EP2451806A2
公开(公告)日：2012-05-16
申请号：EP10732407.1
申请日：2010-07-08
申请人： University of Greenwich
发明人： LEACH, Michael , FRANZMANN, Karl , RIDDALL, Dieter , HARBIGE, Laurence
IPC分类号： C07D409/04
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.

2. 发明授权

EP2043656B1 NEW MEDICAL USE OF TRIAZINE DERIVATIVES 失效
标题翻译：导数的三嗪新的医疗用途
公开(公告)号：EP2043656B1
公开(公告)日：2014-02-12
申请号：EP07766446.4
申请日：2007-07-13
申请人： University of Greenwich
发明人： LEACH, Michael , HARBIGE, Laurence , RIDDALL, Dieter , BARRACLOUGH, Paul
IPC分类号： A61K31/53 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/06 , A61P33/06 , A61P35/00 , A61P43/00
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 heterocyclyl-alkyl are disclosed.

3. 发明公开

EP2229371A1 CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS 无效
标题翻译：循环和氮唑重氮钠通道阻滞剂
公开(公告)号：EP2229371A1
公开(公告)日：2010-09-22
申请号：EP09701748.7
申请日：2009-01-16
申请人： University of Greenwich
发明人： LEACH, Michael , HARBIGE, Laurence , RIDDALL, Dieter , FRANZMANN, Karl
IPC分类号： C07D253/06 , A61K31/53 , A61P25/00
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： The invention relates to compounds of general formula (I), or a salt or solvate thereof; in which: X and Y are each N; A is an optionally substituted phenyl group or an optionally substituted sulphur containing heterocycle; Z is a single bond or a linking group which is a carbon atom carrying substituents R4 and R5, wherein R4 and R5 are independently selected from hydrogen, optionally substituted C 1-6 alkyl and another group A, provided that no more than one of R4 or R5 are hydrogen; R1 is hydrogen, or a substituent group selected from C 1-10 alkyl, C 2-10 alkenyl, benzyl, piperidine-methyl, thienyl-methyl, furyl-methyl or C 3-10 cycloalkyl, any of which is optionally substituted by hydroxy, halogen, carboxamide, halo C 1-4 alkyl, C 1-6 alkyl or C 1-6 alkoxy; or the Y nitrogen is unsubstituted; R2 is amino or a substituent group selected from optionally substituted alkyl or phenyl groups; and N* is =NH when R1 is hydrogen or 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. The compounds can be used to treat disorders in mammals that are susceptible to sodium channel blockers and antifolates, particularly disorders such as epilepsy, multiple sclerosis, glaucoma and uveitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motor neurone 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.

4. 发明公开

EP3307273A1 TRIAZINE DERIVATIVES AS INTERFERON-GAMMA INHIBITORS 有权
标题翻译：三嗪衍生物作为干扰素γ-咔啉抑制剂
公开(公告)号：EP3307273A1
公开(公告)日：2018-04-18
申请号：EP16729340.6
申请日：2016-06-10
申请人： University of Greenwich
发明人： HARBIGE, Laurence , LEACH, Michael
IPC分类号： A61K31/53 , A61P25/00
CPC分类号： A61K31/53
摘要： The present invention relates to interferon-gamma (IFN-γ) inhibitors, and their utility in treating or controlling diseases that can be treated or controlled through inhibition of IFN-γ production, such as Alzheimer's disease, prion diseases, multiple sclerosis, epilepsy, rheumatoid arthritis, inflammatory bowel disease, uveitis, autoimmune skin diseases, psoriasis, Sjögren's syndrome, Crohn's disease, and type 1 diabetes mellitus. The compounds are of Formula 1, 2 3, or are solvates, tautomers, or pharmaceutically acceptable salts thereof; (I), (II), (III) in which: A is an aromatic ring selected from; i. a phenyl ring substituted with up to five substituents, each independently selected from halogen atoms, haloalkyl groups having from 1 to 4 carbon atoms, alkoxy groups having from 1 to 4 carbon atoms, and haloalkoxy groups having from 1 to 4 carbon atoms; ii. a thiophene ring optionally substituted with up to three substituents each selected independently from halogen atoms, alkyl groups having from 1 to 4 carbon atoms, haloalkyl groups having from 1 to 4 carbon atoms, alkoxy groups having from 1 to 4 carbon atoms and haloalkoxy groups having from 1 to 4 carbon atoms; and iii. a C(Rd)3 group, wherein each Rd is independently selected from hydrogen, alkyl groups having from 1 to 4 carbon atoms, haloalkyl groups having from 1 to 4 carbon atoms, alkoxy groups having from 1 to 4 carbon atoms, haloalkoxy groups having from 1 to 4 carbon atoms, and phenyl rings optionally substituted with up to five substituents, each independently selected from halogen atoms, alkyl groups having from 1 to 4 carbon atoms, haloalkyl groups having from 1 to 4 carbon atoms, alkoxy groups having from 1 to 4 carbon atoms, and haloalkoxy groups having from 1 to 4 carbon atoms, cycloalkyl groups having from 3 to 8 carbon atoms, halocycloalkyl groups having from 3 to 8 carbon atoms, and wherein at least one Rd is an optionally substituted phenyl ring; Ra is selected from hydrogen, haloalkyl groups having from 1 to 4 carbon atoms, and alkyl-alkoxy groups having from 1 to 6 carbon atoms that are optionally substituted with one or more halogen atoms, with the proviso that when A is a phenyl ring comprising one or more directly bound halogen substituents, the compound is of Formula 2 or Formula 3, and Ra is not hydrogen; and each Rb is independently selected from hydrogen, and alkyl groups having from 1 to 4 carbon atoms, and haloalkyl groups having from 1 to 4 carbon atoms.

5. 发明公开

EP2043656A2 NEW MEDICAL USE OF TRIAZINE DERIVATIVES 失效
标题翻译：导数的三嗪新的医疗用途
公开(公告)号：EP2043656A2
公开(公告)日：2009-04-08
申请号：EP07766446.4
申请日：2007-07-13
申请人： University of Greenwich
发明人： LEACH, Michael , HARBIGE, Laurence , RIDDALL, Dieter , BARRACLOUGH, Paul
IPC分类号： A61K31/53 , A61P25/00 , A61P25/06 , A61P25/08 , A61P25/16 , A61P25/18 , A61P25/28 , A61P27/06 , A61P33/06 , A61P35/00 , A61P43/00
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 heterocyclyl-alkyl are disclosed.

6. 发明授权

EP2451806B1 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 失效
标题翻译： CYCLIC三偶氮钠通道阻断剂
公开(公告)号：EP2451806B1
公开(公告)日：2016-03-09
申请号：EP10732407.1
申请日：2010-07-08
申请人： University of Greenwich
发明人： LEACH, Michael , FRANZMANN, Karl , RIDDALL, Dieter , HARBIGE, Laurence
IPC分类号： C07D409/04
CPC分类号： C07D253/075 , C07C309/04 , C07C309/06 , C07C309/08 , C07D253/07 , C07D309/04 , C07D309/06 , C07D309/08 , C07D409/04

7. 发明授权

EP2229371B1 CYCLIC TRIAZO AND DIAZO SODIUM CHANNEL BLOCKERS 无效
标题翻译：循环和氮唑重氮钠通道阻滞剂
公开(公告)号：EP2229371B1
公开(公告)日：2015-12-23
申请号：EP09701748.7
申请日：2009-01-16
申请人： University of Greenwich
发明人： LEACH, Michael , HARBIGE, Laurence , RIDDALL, Dieter , FRANZMANN, Karl
IPC分类号： C07D253/06 , A61K31/53 , A61P25/00
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： The invention relates to compounds of general formula (I), or a salt or solvate thereof; in which: X and Y are each N; A is an optionally substituted phenyl group or an optionally substituted sulphur containing heterocycle; Z is a single bond or a linking group which is a carbon atom carrying substituents R4 and R5, wherein R4 and R5 are independently selected from hydrogen, optionally substituted C 1-6 alkyl and another group A, provided that no more than one of R4 or R5 are hydrogen; R1 is hydrogen, or a substituent group selected from C 1-10 alkyl, C 2-10 alkenyl, benzyl, piperidine-methyl, thienyl-methyl, furyl-methyl or C 3-10 cycloalkyl, any of which is optionally substituted by hydroxy, halogen, carboxamide, halo C 1-4 alkyl, C 1-6 alkyl or C 1-6 alkoxy; or the Y nitrogen is unsubstituted; R2 is amino or a substituent group selected from optionally substituted alkyl or phenyl groups; and N* is =NH when R1 is hydrogen or 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. The compounds can be used to treat disorders in mammals that are susceptible to sodium channel blockers and antifolates, particularly disorders such as epilepsy, multiple sclerosis, glaucoma and uveitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motor neurone 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.

8. 发明授权

EP2451807B1 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 失效
标题翻译： CYCLIC三偶氮钠通道阻断剂
公开(公告)号：EP2451807B1
公开(公告)日：2015-09-02
申请号：EP10732408.9
申请日：2010-07-08
申请人： University of Greenwich
发明人： LEACH, Michael , FRANZMANN, Karl , RIDDALL, Dieter , HARBIGE, Laurence
IPC分类号： C07D409/06 , C07D253/07 , A61K31/53 , A61P25/00 , A61P35/00 , A61P33/06
CPC分类号： C07D253/07 , C07D409/06

9. 发明公开

EP2451807A1 CYCLIC TRIAZO SODIUM CHANNEL BLOCKERS 失效
标题翻译：循环TRIAZO钠通道阻塞剂
公开(公告)号：EP2451807A1
公开(公告)日：2012-05-16
申请号：EP10732408.9
申请日：2010-07-08
申请人： University of Greenwich
发明人： LEACH, Michael , FRANZMANN, Karl , RIDDALL, Dieter , HARBIGE, Laurence
IPC分类号： C07D409/06 , C07D253/07 , A61K31/53 , A61P25/00 , A61P35/00 , A61P33/06
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，以及该化合物在制备用于治疗相关病症的药物中的用途。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R1是氢时N *是氨基或当R1是取代基时是= NH; R3和R4均为碳环，杂环或烷基，并且可以相同或不同; 且R5为氢，烷基或环状芳基，条件是：当R3和R4均为烷基时，它们连接形成环烷基，并且R5为环状芳族基团; 当R3和R4都是碳环或杂环基时，R5是氢或烷基; 或其盐。

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