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1. 发明申请

US20050165048A1 Imidazo-pyridine derivatives as ligands for gaba receptors 失效
标题翻译：咪唑并吡啶衍生物作为gaba受体的配体
公开(公告)号：US20050165048A1
公开(公告)日：2005-07-28
申请号：US10512984
申请日：2003-05-23
申请人： Simon Goodacre , Hallett David James , Humphries Charles , Jones Philip , Kelly Margaret , Merchant John , Moore William , Reader Michael
发明人： Simon Goodacre , Hallett David James , Humphries Charles , Jones Philip , Kelly Margaret , Merchant John , Moore William , Reader Michael
IPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61P25/00 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/28 , A61P25/30 , C07D471/04 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： A class of 8-fluoro-3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a —NH— or —OCH2— linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类在苯环的间位被任选取代的芳基或杂芳基取代的8-氟-3-苯基咪唑并[1,2-a]吡啶衍生物，或直接连接或桥接的吡咯烷基由氧原子或-NH-或-OCH 2 - 键组成，是GABA A A受体的选择性配体，特别是对α2和/或 α3和/或α5亚基因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

2. 发明授权

US08501765B2 Diazacarbazoles and methods of use 有权
标题翻译： Diazacarbazoles和使用方法
公开(公告)号：US08501765B2
公开(公告)日：2013-08-06
申请号：US12997066
申请日：2009-06-10
申请人： Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum MacLeod , Karen Williams
发明人： Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum MacLeod , Karen Williams
IPC分类号： A61K31/437 , C07D471/14
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D491/107 , C07D495/04 , C07D513/04 , C07D519/00
摘要： The invention relates to 1,7-diazacarbazole compounds of Formula (I), which are useful as kinase inhibitors, more specifically useful as checkpoint kinase I (chk1) inhibitors, thus useful as cancer therapeutics.
摘要翻译：本发明涉及式（I）的1,7-二氮杂咔唑化合物，其可用作激酶抑制剂，更具体地用作检查点激酶I（chk1）抑制剂，因此可用作癌症治疗剂。

3. 发明申请

US20060041125A1 Substituted pyrido-pyridazine derivatives which enhance cognition via the gaba-a receptors 失效
标题翻译：取代的吡啶并哒嗪衍生物，其通过gaba-α受体增强认知
公开(公告)号：US20060041125A1
公开(公告)日：2006-02-23
申请号：US10531517
申请日：2003-10-29
申请人： Simon Goodacre , David Hallett
发明人： Simon Goodacre , David Hallett
IPC分类号： C07D487/02 , A61K31/503
CPC分类号： C07D471/04
摘要： The present invention discloses a compound of formula 1, or a pharmaceutically acceptable salt thereof: wherein X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, —ORa, —SRa, —SORa, —SO2Ra, —SO2NRaRb, NRaRb, —NRaCORb, —NRaCO2Rb, —CORa, —CO2Ra, —CONRaRb or —CRa&=NORb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; a pharmaceutical composition comprising it; its use in a method of treatment; use of it to manufacture a medicament; and a method of using it to prevent or treat anxiety, convulsions or cognitive disorders.
摘要翻译：本发明公开了式1化合物或其药学上可接受的盐：其中X 1表示氢，卤素，C 1-6烷基，三氟甲基或C _{1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-键; Z表示任选取代的芳基或杂芳基; R 1表示氢，烃，杂环基，卤素，氰基，三氟甲基，硝基，-OR a，-SR a，-SOR 一个或两个以上的一个或多个，其中，R 1，R 2，R 2，其中，R a，R b，R b，R b，R b， CO 2，CO 2 CO 2 SO 2，-SO 2 R 2，或者 - a 并且R a和R b独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来预防或治疗焦虑，抽搐或认知障碍的方法。}

4. 发明申请

US20110118230A1 DIAZACARBAZOLES AND METHODS OF USE 有权
标题翻译： DIAZACARBAZOLES和使用方法
公开(公告)号：US20110118230A1
公开(公告)日：2011-05-19
申请号：US12997066
申请日：2009-06-10
申请人： Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum Macleod , Karen Williams
发明人： Huifen Chen , Hazel Joan Dyke , Charles Ellwood , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Samuel Kintz , Joseph Lyssikatos , Calum Macleod , Karen Williams
IPC分类号： A61K31/4375 , C07D471/14 , C07D513/04 , C07D495/04 , C07D491/107 , C07D487/04 , A61K31/496 , A61K31/4545 , A61K31/5377 , A61K31/553 , A61K31/55 , A61K31/541 , A61K31/438 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61P35/00 , A61P35/02
CPC分类号： C07D471/14 , A61K31/4375 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , C07D491/107 , C07D495/04 , C07D513/04 , C07D519/00
摘要： The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及可用作激酶抑制剂的式（I），（I-a）和（I-b）的1,7-二氮杂咔唑化合物，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况。

5. 发明申请

US20060058303A1 Imidazo-triazine derivatives as ligands for gaba receptors 失效
标题翻译：咪唑并三嗪衍生物作为gaba受体的配体
公开(公告)号：US20060058303A1
公开(公告)日：2006-03-16
申请号：US10512608
申请日：2003-05-01
申请人： Mark Chambers , Simon Goodacre , David Hallett , Robert Maxey , Michael Russell , Leslie Street
发明人： Mark Chambers , Simon Goodacre , David Hallett , Robert Maxey , Michael Russell , Leslie Street
IPC分类号： A61K31/53 , C07D487/04
CPC分类号： C07D487/04
摘要： A class of imidazo[1,2b][1,2,4]triazine derivatives, substituted at the 7-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在7-位取代的咪唑并[1,2b] [1,2,4]三嗪衍生物，是GABA A，特别是具有对α2和/或α3和/或α5亚基具有良好亲和力的受体，因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，惊厥和认知障碍）方面是有益的。

6. 发明申请

US20060052385A1 8-Fluoroimidazo 1,2-a pyridine derivatives as ligands for gaba receptors 失效
标题翻译： 8-氟咪唑并[1,2-a]吡啶衍生物作为gaba受体的配体
公开(公告)号：US20060052385A1
公开(公告)日：2006-03-09
申请号：US10515165
申请日：2003-05-25
申请人： Wesley Blackaby , Jose Castro Pineiro , Simon Goodacre , David Hallett , Alexander Humphries , Philip Jones , Kevin Merchant , Michael Reader
发明人： Wesley Blackaby , Jose Castro Pineiro , Simon Goodacre , David Hallett , Alexander Humphries , Philip Jones , Kevin Merchant , Michael Reader
IPC分类号： A61K31/506 , A61K31/502 , A61K31/497 , C07D471/02
CPC分类号： C07D471/04
摘要： A class of 8-fluoroimidazo[1,2-α]pyridine derivatives, substituted at the 3-position by an optionally substituted five-membered or six-membered heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类由任选取代的五元或六元杂芳环在3-位被取代的8-氟咪唑并[1,2-α]吡啶衍生物，是GABA A A受体的选择性配体特别是对α2和/或α3和/或α5亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

7. 发明申请

US20060014744A1 Midazopyrazinones and imidazotriazinones derivates as gaba-a receptor anxiolytic 失效
标题翻译：咪唑并吡嗪酮和咪唑并三嗪酮衍生为gaba-a受体抗焦虑药
公开(公告)号：US20060014744A1
公开(公告)日：2006-01-19
申请号：US10533152
申请日：2003-10-29
申请人： William Carling , Jose Castro Pineiro , Simon Goodacre , David Hallett , Leslie Street
发明人： William Carling , Jose Castro Pineiro , Simon Goodacre , David Hallett , Leslie Street
IPC分类号： A61K31/53 , A61K31/519 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention discloses a compound of formula I, or a pharmaceutically acceptable salt thereof: (I) wherein —U—V— represents —CH═CH—, or —CH2—CH2—, —N═CH— or —CH═N—; X1 represents hydrogen, halogen, C1-6 alkyl, trifluoromethyl or C1-6 alkoxy; X2 represents hydrogen or halogen; Y represents a chemical bond, an oxygen atom, or a —NH— or —OCH2— linkage; Z represents an optionally substituted aryl or heteroaryl group; R1 represents hydrocarbon, a heterocyclic group, trifluoromethyl, —SO2Ra, —SO2NRaRb, —CORa, —CO2Ra or —CONRaRb; and Ra and Rb independently represent hydrogen, hydrocarbon or a heterocyclic group; pharmaceutical compositions comprising it; its use in methods of treatment; use of it in the manufacture of a medicament for treating and/or preventing anxiety; convulsions or a cognitive disorder; and methods of treatment using it.
摘要翻译：本发明公开了式I化合物或其药学上可接受的盐：（I）其中-UV-表示-CH-CH-或-CH 2 -CH 2， -N - ， - CH-或-CH-N-; X 1表示氢，卤素，C 1-6烷基，三氟甲基或C 1-6烷氧基; X 2表示氢或卤素; Y表示化学键，氧原子或-NH-或-OCH 2 - 键; Z表示任选取代的芳基或杂芳基; R 1表示烃，杂环基，三氟甲基，-SO 2 R 2，-SO 2 NR 2， - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - ^{a B ; R a和R b各自独立地表示氢，烃或杂环基; 包含它的药物组合物; 其用于治疗方法; 在制备用于治疗和/或预防焦虑的药物中的用途; 惊厥或认知障碍; 和使用它的治疗方法。}

8. 发明申请

US20110124654A1 DIAZACARBAZOLES AND METHODS OF USE 审中-公开
标题翻译： DIAZACARBAZOLES和使用方法
公开(公告)号：US20110124654A1
公开(公告)日：2011-05-26
申请号：US12997069
申请日：2009-06-10
申请人： Huifen Chen , Hazel Joan Dyke , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Joseph Lyssikatos , Calum Macleod , Karen Williams
发明人： Huifen Chen , Hazel Joan Dyke , Emanuela Gancia , Lewis J. Gazzard , Simon Goodacre , Joseph Lyssikatos , Calum Macleod , Karen Williams
IPC分类号： A61K31/519 , C07D403/14 , A61P35/00 , A61P35/02
CPC分类号： C07D471/14
摘要： The invention relates to 1,5-diazacarbazole compounds of Formula (I), (I-a), (I-b), (I-c), (I-d), (I-e), (I-f), (I-g) and (I-h) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
摘要翻译：本发明涉及有用的式（I），（Ia），（Ib），（Ic），（Id），（Ie），（If），（Ig）和（Ih）的1,5-二氮杂咔唑化合物作为激酶抑制剂，更具体地用作检查点激酶1（chk1）抑制剂，因此可用作癌症治疗剂。本发明还涉及包含这些化合物的组合物，更具体地是包含这些化合物的药物组合物以及使用该组合物治疗各种形式的癌症和过度增殖性疾病的方法，以及将该化合物用于体外，原位和体内诊断或治疗哺乳动物细胞或相关病理状况。

9. 发明申请

US20050165023A1 Imidazo-triazine derivatives as ligands for gaba receptors 失效
标题翻译：咪唑并三嗪衍生物作为gaba受体的配体
公开(公告)号：US20050165023A1
公开(公告)日：2005-07-28
申请号：US10512655
申请日：2003-05-01
申请人： Michela Bettati , Mark Chambers , Simon Goodacre , David Hallett , Michael Neil , Leslie Street
发明人： Michela Bettati , Mark Chambers , Simon Goodacre , David Hallett , Michael Neil , Leslie Street
IPC分类号： A61K31/53 , A61P1/08 , A61P1/14 , A61P13/10 , A61P15/00 , A61P21/02 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P27/16 , C07D487/04
CPC分类号： C07D487/04
摘要： A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a —NH— linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类7-苯基咪唑并[1,2-b] [1,2,4]三嗪衍生物，其在苯环的间位被任选取代的被氧原子连接或桥连的芳基或杂芳基取代或-NH-键，并且在苯环上被一个或两个如本文所定义的其它取代基取代，是GABA A A受体的选择性配体，特别是对α2和/或α3具有良好的亲和力和/或其α5亚基因此在治疗和/或预防中枢神经系统的不良状况（包括焦虑，惊厥和认知障碍）方面是有益的。

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