专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20080009507A1 Inhibitors of Akt Activity 失效
标题翻译： Akt活性抑制剂
公开(公告)号：US20080009507A1
公开(公告)日：2008-01-10
申请号：US11795156
申请日：2006-02-10
申请人： Nicholas Cosford , Mark Layton , Jun Liang , Craig Lindsley , Philip Sanderson , Zhijian Zhao
发明人： Nicholas Cosford , Mark Layton , Jun Liang , Craig Lindsley , Philip Sanderson , Zhijian Zhao
IPC分类号： A61K31/495 , A61P35/00 , C07D241/36
CPC分类号： C07D471/04
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译：本发明提供抑制Akt活性的化合物。特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。

2. 发明申请

US20050026963A1 Heteroaryl substituted pyrazole modulators of metabotropic glutamate receptor-5 有权
标题翻译：代谢型谷氨酸受体-5的杂芳基取代的吡唑调节剂
公开(公告)号：US20050026963A1
公开(公告)日：2005-02-03
申请号：US10497122
申请日：2002-12-13
申请人： Nicholas Cosford , Chixu Chen , Brian Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas Smith
发明人： Nicholas Cosford , Chixu Chen , Brian Eastman , Dehua Huang , Benito Munoz , Petpiboon Prasit , Nicholas Smith
IPC分类号： A61K31/4155 , A61K31/424 , A61K31/427 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/497 , A61K31/498 , A61K31/506 , A61K45/00 , A61P3/04 , A61P17/06 , A61P21/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/34 , A61P29/00 , A61P43/00 , C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
CPC分类号： C07D231/38 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D417/04
摘要： Pyrazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.
摘要翻译：直接或通过桥连与杂芳基相连接的杂芳基部分的吡唑化合物是可用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症）的mGluR5调节剂，双相情感障碍和恐慌，以及治疗疼痛，昼夜节律紊乱和其他疾病。

3. 发明申请

US20050085514A1 Heteroaryl substituted pyrrole modulators of metabotropic glutamate receptor-5 失效
标题翻译：代谢型谷氨酸受体-5的杂芳基取代吡咯调节剂
公开(公告)号：US20050085514A1
公开(公告)日：2005-04-21
申请号：US10499393
申请日：2002-12-17
申请人： Nicholas Cosford , Dehua Huang , Nicholas Smith
发明人： Nicholas Cosford , Dehua Huang , Nicholas Smith
IPC分类号： A61K31/427 , A61K31/4439 , A61K31/444 , A61P1/14 , A61P3/04 , A61P21/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , A61K31/4025 , C07D43/02
CPC分类号： C07D401/14 , C07D401/04 , C07D417/04
摘要： Pyrrole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, circadian rhythm disorders, and other diseases.
摘要翻译：直接或桥接的杂芳基部分与杂芳基连接点相邻的杂芳基部分取代的吡咯化合物是可用于治疗精神病和情绪障碍的mGluR5调节剂，例如精神分裂症，焦虑症，抑郁症，双相情感障碍和恐慌，以及治疗疼痛，昼夜节律紊乱和其他疾病。

4. 发明申请

US20050043307A1 Pyridazine, pyrimidine and pyrazine ethyne compounds 失效
标题翻译：哒嗪，嘧啶和吡嗪乙炔化合物
公开(公告)号：US20050043307A1
公开(公告)日：2005-02-24
申请号：US10874835
申请日：2004-06-23
申请人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Nicholas Smith , Brian Stearns , Dehua Huang , Bowei Wang
发明人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Nicholas Smith , Brian Stearns , Dehua Huang , Bowei Wang
IPC分类号： A61K31/506 , C07D213/16 , C07D213/30 , C07D233/54 , C07D233/61 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/00 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14 , A61K31/50 , A61K31/497 , A61K31/505
CPC分类号： C07D239/26 , C07D213/16 , C07D213/30 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.
摘要翻译：根据本发明，提供了一类新的杂环化合物。本发明的化合物含有包含至少一个氮原子和至少一个碳原子的取代的，不饱和的五，六或七元杂环。该环另外包括独立地选自碳，氮，硫和氧原子的三个，四个或五个原子。该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。该环的强制取代基包括通过碳 - 碳双键，碳 - 碳三键或偶氮基与杂环连接的部分（B）。强制性取代基位于环氮原子附近。本发明化合物能够具有多种用途。例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。本发明的化合物也可以作为杀虫剂和杀真菌剂。含有本发明化合物的药物组合物也具有广泛用途

5. 发明申请

US20070082067A1 Di-aryl substituted triazole modulators of metabotropic glutamate receptor-5 失效
标题翻译：代谢型谷氨酸受体-5的二芳基取代三唑调节剂
公开(公告)号：US20070082067A1
公开(公告)日：2007-04-12
申请号：US10552362
申请日：2004-03-31
申请人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Bowei Wang
发明人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Bowei Wang
IPC分类号： A61K31/444 , C07D403/14 , A61K31/551 , A61K31/485 , A61K31/506
CPC分类号： A61K31/41 , A61K31/4192 , C07D401/10 , C07D401/14
摘要： Novel triazole compounds represented by Formula (1): (where A, A1, A2, A3, A4, A5, B, R11, W, X, Y and Z are as defined herein) in which the triazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases.
摘要翻译：由式（1）表示的新型三唑化合物：其中A，A 1，A 2，A 3，A 4， A，B，R 11，W，X，Y和Z如本文所定义），其中三唑直接被取代，或通过桥，其中i）包含与杂芳基的连接点相邻的N的杂芳基部分和ii）另外的杂芳基或芳基环，其中至少一个环进一步被另一个环取代，是用于治疗精神病学的mGluR5调节剂以及情绪障碍，例如精神分裂症，焦虑症，抑郁症，恐慌症和双相性精神障碍，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，药物戒断，肥胖等疾病。

6. 发明申请

US20050245542A1 Pyridazine, pyrimidine and pyrazine ethyne compounds 失效
标题翻译：哒嗪，嘧啶和吡嗪乙炔化合物
公开(公告)号：US20050245542A1
公开(公告)日：2005-11-03
申请号：US11097047
申请日：2005-04-01
申请人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Nicholas Smith , Brian Stearns , Dehua Huang , Bowei Wang , Thomas Seiders
发明人： Nicholas Cosford , Jeffrey Roppe , Lida Tehrani , Nicholas Smith , Brian Stearns , Dehua Huang , Bowei Wang , Thomas Seiders
IPC分类号： A61K31/506 , C07D213/16 , C07D213/30 , C07D233/54 , C07D233/61 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/00 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D43/02 , C07D43/14
CPC分类号： C07D213/16 , C07D213/30 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/01 , C07D333/08 , C07D401/06 , C07D401/12 , C07D401/14
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.
摘要翻译：根据本发明，提供了一类新的杂环化合物。本发明化合物含有至少两个氮原子的取代或未取代的六元杂环。该环另外包括四个碳原子。该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。该环的强制取代基包括通过碳 - 碳三键与杂环连接的部分（B）。强制性取代基位于环氮原子附近。本发明化合物能够具有多种用途。例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。本发明的化合物也可以作为杀虫剂和杀真菌剂。含有本发明化合物的药物组合物也具有广泛用途

7. 发明申请

US20050085523A1 Imidazolyl and pyrazolyl ethyne compounds 审中-公开
标题翻译：咪唑基和吡唑基乙炔化合物
公开(公告)号：US20050085523A1
公开(公告)日：2005-04-21
申请号：US10874991
申请日：2004-06-23
申请人： Nicholas Cosford , Theodore Kamenecka , Jeffrey Roppe
发明人： Nicholas Cosford , Theodore Kamenecka , Jeffrey Roppe
IPC分类号： C07D213/16 , C07D213/30 , C07D233/54 , C07D233/61 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/00 , C07D285/01 , C07D333/08 , A61K31/445 , A61K31/416 , A61K31/4172 , A61K31/4178
CPC分类号： C07D213/16 , C07D213/30 , C07D239/26 , C07D241/12 , C07D249/08 , C07D263/32 , C07D271/06 , C07D277/22 , C07D277/24 , C07D277/40 , C07D285/01 , C07D333/08
摘要： In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted, unsaturated five, six or seven membered heterocyclic ring that includes at least one nitrogen atom and at least one carbon atom. The ring additionally includes three, four or five atoms independently selected from carbon, nitrogen, sulfur and oxygen atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon double bond, a carbon-carbon triple bond or an azo group. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.
摘要翻译：根据本发明，提供了一类新的杂环化合物。本发明的化合物含有包含至少一个氮原子和至少一个碳原子的取代的，不饱和的五，六或七元杂环。该环另外包括独立地选自碳，氮，硫和氧原子的三个，四个或五个原子。该杂环具有至少一个位于与环氮原子相邻的环位置的取代基。该环的强制取代基包括通过碳 - 碳双键，碳 - 碳三键或偶氮基与杂环连接的部分（B）。强制性取代基位于环氮原子附近。本发明化合物能够具有多种用途。例如，杂环化合物可以通过在神经系统中作为受体的激动剂和拮抗剂起作用来调节生理过程。本发明的化合物也可以作为杀虫剂和杀真菌剂。含有本发明化合物的药物组合物也具有广泛的用途。

8. 发明申请

US20050020585A1 Heteroaryl substituted triazole modulators of metabotropic glutamate receptor-5 失效
标题翻译：代谢型谷氨酸受体-5的杂芳基取代三唑调节剂
公开(公告)号：US20050020585A1
公开(公告)日：2005-01-27
申请号：US10499391
申请日：2002-12-13
申请人： Nicholas Cosford , Petpiboon Prasit , Jeffrey Roppe , Nicholas Smith , Lida Tehrani
发明人： Nicholas Cosford , Petpiboon Prasit , Jeffrey Roppe , Nicholas Smith , Lida Tehrani
IPC分类号： A61K31/135 , A61K31/145 , A61K31/185 , A61K31/19 , A61K31/195 , A61K31/4439 , A61K31/485 , A61K31/506 , A61K31/5513 , A61K45/00 , A61K45/06 , A61P3/04 , A61P3/12 , A61P3/14 , A61P21/00 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P29/00 , C07D401/04 , C07D401/14 , A61K31/54 , A61K31/4178 , A61K31/4196 , A61K31/454 , A61K31/496 , A61K31/5377
CPC分类号： C07D401/04 , C07D401/14
摘要： Triazole compounds substituted directly, or by a bridge, with a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl which are metabotropic glutamate receptor—subtype 5 (“mGluR5”) modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorder and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal and other diseases.
摘要翻译：直接或桥接的三唑化合物与杂芳基部分相邻的杂芳基部分，杂芳基部分与杂芳基的连接点相邻，杂芳基是代谢型谷氨酸受体 - 亚型5（“mGluR5”）调节剂，可用于治疗精神病和情绪障碍，例如例如精神分裂症，焦虑症，抑郁症，双相情感障碍和恐慌，以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律紊乱，药物成瘾，药物滥用，戒毒等疾病。

9. 发明申请

US20060217420A1 4-Ring imidazole derivatives as modulators of metabotropic glutamate receptor-5 审中-公开
标题翻译： 4-环咪唑衍生物作为代谢型谷氨酸受体-5的调节剂
公开(公告)号：US20060217420A1
公开(公告)日：2006-09-28
申请号：US10552107
申请日：2004-03-30
申请人： Nicholas Cosford , Dehua Huang , Nicholas Smith , Essa Hsinyi Hu
发明人： Nicholas Cosford , Dehua Huang , Nicholas Smith , Essa Hsinyi Hu
IPC分类号： A61K31/444 , C07D403/14
CPC分类号： C07D233/64 , C07D401/04 , C07D401/14 , C07D471/04
摘要： Imidazole compounds of Formula (I): (where A, B, R11, R12, W, X, Y and Z are as defined herein) wherein the imidazole is substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, which are MgluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, bipolar disorders, and panic, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm and sleep disorders—such as shift-work induced sleep disorder and jet-lag, drug addiction, drug abuse, drug withdrawal, obesity and other diseases, and pharmaceutical compositions and methods of treating these diseases.
摘要翻译：式（I）的咪唑化合物（其中A，B，R 11，R 12，W，X，Y和Z如本文所定义），其中咪唑是直接或桥接，其中i）杂芳基部分，其含有与杂芳基的连接点相邻的N，和ii）另一杂芳基或芳基环，其中至少一个环进一步被另一个环取代，用于治疗精神病和情绪障碍（例如精神分裂症，焦虑症，抑郁症，双相性精神障碍和恐慌）以及治疗疼痛，帕金森病，认知功能障碍，癫痫，昼夜节律和睡眠的MgluR5调节剂疾病 - 如转移工作诱导的睡眠障碍和时滞，药物成瘾，药物滥用，药物戒断，肥胖症等疾病，以及治疗这些疾病的药物组合物和方法。

10. 发明申请

US20070287716A1 Pyrimidine and Quinoline Potentiators of Metabotropic Glutamate Receptors 审中-公开
标题翻译：代谢型谷氨酸受体的嘧啶和喹啉电位
公开(公告)号：US20070287716A1
公开(公告)日：2007-12-13
申请号：US11665422
申请日：2005-10-24
申请人： Essa Hu , Jean-Michel Vernier , Peter Chua , John Hutchinson , Nicholas Cosford
发明人： Essa Hu , Jean-Michel Vernier , Peter Chua , John Hutchinson , Nicholas Cosford
IPC分类号： A61K31/47 , A61P25/00 , C07D215/12 , C07D239/28
CPC分类号： C07D239/26 , C07D215/06
摘要： The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的增强剂（包括mGluR2受体）的化合物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。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预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式