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1. 发明授权

US07868008B2 Substituted isoindolones and their use as metabotropic glutamate receptor potentiators 失效
标题翻译：取代的异吲哚酮及其作为代谢型谷氨酸受体增强剂的用途
公开(公告)号：US07868008B2
公开(公告)日：2011-01-11
申请号：US12063018
申请日：2006-02-15
申请人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
发明人： Bradford Van Wagenen , Radhakrishnan Ukkiramapandian , Joshua Clayton , Ian Egle , James Empfield , Methvin Isaac , Fupeng Ma , Abdelmalik Slassi , Gary Steelman , Rebecca Urbanek , Sally Walsh
IPC分类号： C07D209/46 , C07D401/06 , C07D401/14 , A61K31/4035 , A61K31/454
CPC分类号： C07D209/46 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/04 , C07D413/14
摘要： The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和n如说明书中对式I所定义。本发明还涉及制备化合物的方法和用于制备中的新中间体，含有该化合物的药物组合物，以及该化合物在治疗中的用途。

2. 发明授权

US07585881B2 Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：额外的杂多环化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US07585881B2
公开(公告)日：2009-09-08
申请号：US11053752
申请日：2005-02-09
申请人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tau Xin , Jalaj Arora
发明人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tau Xin , Jalaj Arora
IPC分类号： A61K31/4439 , C07D401/14 , C07D413/04
CPC分类号： C07D487/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention relates to new compounds of formula I, to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：本发明涉及新的式I化合物，含有该化合物的药物制剂，以及该化合物在预防和/或治疗mGluR5受体介导的病症中的用途。

3. 发明申请

US20090131454A1 New compounds 067 失效
标题翻译：新化合物067
公开(公告)号：US20090131454A1
公开(公告)日：2009-05-21
申请号：US12285988
申请日：2008-10-17
申请人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
发明人： Erwan Arzel , Louise Edwards , Methvin Isaac , Donald A. McLeod , Abdelmalik Slassi , Tao Xin
IPC分类号： A61K31/497 , C07D401/14 , C07D403/14 , A61K31/506 , A61K31/4439
CPC分类号： C07D401/14 , C07D403/14
摘要： The present invention is directed to novel compounds, their use in therapy and pharmaceutical compositions comprising said novel compounds.
摘要翻译：本发明涉及新化合物，它们在治疗中的用途和包含所述新化合物的药物组合物。

4. 发明申请

US20080125436A1 MgluR5 modulators 失效
标题翻译： MgluR5调节剂
公开(公告)号：US20080125436A1
公开(公告)日：2008-05-29
申请号：US11902784
申请日：2007-09-25
申请人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Peter Dove , Tao Xin , Tomislav Stefanac
发明人： Methvin Isaac , Abdelmalik Slassi , Louise Edwards , Peter Dove , Tao Xin , Tomislav Stefanac
IPC分类号： A61K31/513 , A61K31/501 , A61K31/497 , A61K31/4439 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D413/14 , C07D401/14
摘要： The present invention is directed to compounds of formula I: Wherein R1 to R5, X and Z are further defined in the description. The invention also relates to processes for the preparation of the compounds and to intermediates used in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中R 1至R 5，X和Z在说明书中进一步定义。本发明还涉及制备化合物和制备中使用的方法，含有该化合物的药物组合物以及该化合物在治疗中的用途。

5. 发明申请

US20080045571A1 ADDITIONAL HETEROPOLYCYCLIC COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS 审中-公开
标题翻译：其他杂环化合物及其作为代谢谷氨酸受体拮抗剂的使用
公开(公告)号：US20080045571A1
公开(公告)日：2008-02-21
申请号：US11840953
申请日：2007-08-18
申请人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Jalaj Arora
发明人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald McLeod , Alexander Mindis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Jalaj Arora
IPC分类号： A61K31/4439 , A61K31/4196 , A61K31/4245 , A61P19/06 , A61P25/18 , A61P25/30 , A61P29/00 , A61P9/00 , C07D413/14 , C12N5/00 , C07D271/06 , A61P35/00 , A61P27/02 , A61P25/28 , A61P25/08 , A61P19/02 , A61K31/443
CPC分类号： C07D487/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention relates to new compounds of formula I, to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：本发明涉及新的式I化合物，含有该化合物的药物制剂，以及该化合物在预防和/或治疗mGluR5受体介导的病症中的用途。

6. 发明申请

US20070179188A1 Additional heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：额外的杂多环化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US20070179188A1
公开(公告)日：2007-08-02
申请号：US10588702
申请日：2005-02-15
申请人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald Mcleod , Alexander Minidis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Jalaj Arora
发明人： Louise Edwards , Methvin Isaac , Martin Johansson , Annika Kers , Johan Malmberg , Donald Mcleod , Alexander Minidis , Karin Staaf , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Jalaj Arora
IPC分类号： A61K31/4439 , A61K31/4245 , C07D413/14 , C07D413/02
CPC分类号： C07D487/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention relates to new compounds of formula (I), to pharmaceutical formulations containing the compounds, and to the use of the compounds in the prevention and/or treatment of mGluR5 receptor-mediated disorders.
摘要翻译：本发明涉及新的式（I）化合物，含有该化合物的药物制剂，以及该化合物在预防和/或治疗mGluR5受体介导的病症中的用途。

7. 发明申请

US20060235024A1 Acetylinic piperazine compounds and their use as metabotropic glutamate receptor antagonists 审中-公开
标题翻译：乙酰哌嗪化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US20060235024A1
公开(公告)日：2006-10-19
申请号：US11060470
申请日：2005-08-17
申请人： Chris Bryan , Methvin Isaac , Tomislav Stefanac , Abdelmalik Slassi , Louise Edwards
发明人： Chris Bryan , Methvin Isaac , Tomislav Stefanac , Abdelmalik Slassi , Louise Edwards
IPC分类号： A61K31/496 , A61K31/495 , C07D409/02 , C07D241/04
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61 , C07D295/073 , C07D295/205 , C07D307/52 , C07D333/20
摘要： The present invention relates to new acetylinic piperazine compounds of formula I, their pharmaceutically acceptable salts, and hydrates: wherein R1, R2, R3, R4, M, and n are as defined in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I的新的乙炔哌嗪化合物，其药学上可接受的盐和水合物：其中R 1，R 2，R 3， >，R 4，M和n如说明书中所定义。本发明还涉及制备化合物的方法和用于制备中的新中间体，含有该化合物的药物组合物，以及该化合物在治疗中的用途。

8. 发明申请

US20060122397A1 Compounds 失效
标题翻译：化合物
公开(公告)号：US20060122397A1
公开(公告)日：2006-06-08
申请号：US11274611
申请日：2005-11-14
申请人： Jalaj Arora , Louise Edwards , Methvin Isaac , Donald McLeod , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Helena Gyback , Martin Johansson , Annika Kers , John Malmberg , Alexander Minidis , Karin Oscarsson , Mangus Waldman , Ulrika Yngve , Christoffer Osterwall
发明人： Jalaj Arora , Louise Edwards , Methvin Isaac , Donald McLeod , Abdelmalik Slassi , Tomislav Stefanac , Thomas Stormann , David Wensbo , Tao Xin , Helena Gyback , Martin Johansson , Annika Kers , John Malmberg , Alexander Minidis , Karin Oscarsson , Mangus Waldman , Ulrika Yngve , Christoffer Osterwall
IPC分类号： A61K31/4439 , A61K31/4245 , C07D417/14 , C07D413/14 , C07D409/14
CPC分类号： C07D413/14 , C07D413/12 , C07D417/14
摘要： The present invention relates to new compounds of formula I, a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
摘要翻译：本发明涉及新的式I化合物，其制备方法和其中制备的新中间体，含有所述化合物的药物制剂和所述化合物在治疗中的用途。

9. 发明申请

US20060009443A1 Fused heterocyclic compounds and their use as metabotropic glutamate receptor antagonists 失效
标题翻译：稠合杂环化合物及其作为代谢型谷氨酸受体拮抗剂的用途
公开(公告)号：US20060009443A1
公开(公告)日：2006-01-12
申请号：US11060560
申请日：2005-02-18
申请人： David Wensbo , Martin Johansson , Alexander Minidis , Karin Staaf , Annika Kers , Louise Edwards , Methvin Isaac , Tom Stefanac , Abdelmalik Slassi , Don McLeod , Tao Xin
发明人： David Wensbo , Martin Johansson , Alexander Minidis , Karin Staaf , Annika Kers , Louise Edwards , Methvin Isaac , Tom Stefanac , Abdelmalik Slassi , Don McLeod , Tao Xin
IPC分类号： A61K31/407
CPC分类号： C07D211/22 , C07D223/08 , C07D241/18 , C07D273/02 , C07D403/12 , C07D409/12 , C07D413/12 , C07D471/04
摘要： The present invention is directed to compounds of formula I: wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, R1, R2, R3, R4, and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.
摘要翻译：本发明涉及式I化合物：其中X 1，X 2，X 3，X 4， >，X 5，X 6，X 7，X 8，X 9， >，X <10>，R 1，R 2，R 3，R 4， >，n如在说明书中对式I所定义。本发明还涉及制备化合物的方法和用于制备中的新中间体，含有该化合物的药物组合物，以及该化合物在治疗中的用途。

10. 发明授权

US06916818B2 Azaindoles having serotonin receptor affinity 失效
标题翻译：阿魏醇具有5-羟色胺受体亲和力
公开(公告)号：US06916818B2
公开(公告)日：2005-07-12
申请号：US10739302
申请日：2003-12-19
申请人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
发明人： Louise Edwards , Abdelmalik Slassi , Ashok Tehim , Tao Xin
IPC分类号： A61K31/498 , A61P25/18 , A61P25/24 , C07D471/04 , C07D487/04 , C07D519/00 , C07D401/04 , A61K31/496
CPC分类号： C07D471/04 , C07D519/00
摘要： Described herein are compounds with affinity for the 5-HT6 receptor, which have the general formula I: wherein: R represents a group of Formula II or Formula III; one of A, B D or E is a N atom, the remainder being CH groups; R1 is selected from the group consisting of SO2Ar, C(O)Ar, CH2Ar and Ar; R2, R3 and R4 are independently selected from the group consisting of H and alkyl; — represents a single or double bond, with the proviso that there is only one double bond in the ring at a time; n is an integer of from 1-3; Z is selected from the group consisting of C, CH and N, provided that when —is a double bond, Z is C and when — is a single bond, Z is selected from CH and N; Ar is an optionally substituted aryl group; with the proviso that when R is a group of Formula II, R1 is SO2Ar. Also described is the use of these compounds as pharmaceuticals to treat indications where inhibition of the 5-HT6 receptor is implicated, such as schizophrenia.
摘要翻译：本文描述的是具有对具有通式I的5-HT 6受体具有亲和性的化合物：其中：R代表式II或式III的基团; A，B D或E之一为N原子，其余为CH基团; R 1选自SO 2 Ar，C（O）Ar，CH 2 Ar和Ar; R 2，R 3和R 4独立地选自H和烷基; - 表示单键或双键，条件是每次只有一个双键; n为1-3的整数; Z选自C，CH和N，条件是当 - 双键，Z为C且当 - 为单键时，Z选自CH和N; Ar是任选取代的芳基; 条件是当R是式II的基团时，R 1是SO 2 Ar。还描述了这些化合物作为药物用于治疗其中涉及5-HT 6受体的抑制的适应症的用途，例如精神分裂症。

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