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1. 发明申请

WO2008145616A1 HETEROCYCLIC COMPOUNDS AS POSITIVE MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2 (MGLU2 RECEPTOR) 审中-公开
标题翻译：作为代谢性谷氨酸受体2（MGLU2受体）的阳性调节剂的杂环化合物
公开(公告)号：WO2008145616A1
公开(公告)日：2008-12-04
申请号：PCT/EP2008/056378
申请日：2008-05-23
申请人： ABBOTT GMBH & CO. KG , GENESTE, Hervé , SAUER, Daryl , BRAJE, Wilfried , AMBERG, Wilhelm , MEZLER, Mario , BAKKER, Margaretha Henrica Maria
发明人： GENESTE, Hervé , SAUER, Daryl , BRAJE, Wilfried , AMBERG, Wilhelm , MEZLER, Mario , BAKKER, Margaretha Henrica Maria
IPC分类号： C07D209/26 , C07D231/12 , C07D333/58 , C07D239/26 , C07D277/28 , C07D233/58 , C07D409/04 , C07D409/06 , C07D333/20 , C07D307/14 , C07D213/36 , C07D213/38
CPC分类号： C07D209/14 , C07D207/335 , C07D209/26 , C07D213/36 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04 , C07D409/06
摘要： The present invention relates to heterocyclic compounds which are positive modulatorsof metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的阳性调节剂的杂环化合物。本发明还涉及这些化合物用于制备药物组合物和治疗选自与谷氨酸功能障碍相关的神经和精神障碍的医学病症的方法的用途。

2. 发明申请

WO2005082871A2 GUANIDINVERBINDUNGEN UND IHRE VERWENDUNG ALS BINDUNGSPARTNER FÜR 5-HT5-REZEPTOREN 审中-公开
标题翻译：胍和它们作为结合伴侣5-HT5受体
公开(公告)号：WO2005082871A2
公开(公告)日：2005-09-09
申请号：PCT/EP2005/001521
申请日：2005-02-15
申请人： ABBOTT GMBH & CO. KG , NETZ, Astrid , AMBERG, Wilhelm , LANGE, Udo , OCHSE, Michael , HUTCHINS, Charles, W. , GARCIA-LADONA, Francisco-Xavier , WERNET, Wolfgang , MEZLER, Mario , SAUER, Daryl , BURNS, David , KLING, Andreas
发明人： NETZ, Astrid , AMBERG, Wilhelm , LANGE, Udo , OCHSE, Michael , HUTCHINS, Charles, W. , GARCIA-LADONA, Francisco-Xavier , WERNET, Wolfgang , MEZLER, Mario , SAUER, Daryl , BURNS, David , KLING, Andreas
IPC分类号： C07D277/00
CPC分类号： C07D277/48 , C07D231/56 , C07D235/30 , C07D237/22 , C07D249/14 , C07D261/14 , C07D263/28 , C07D263/48 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/135 , C07D333/36 , C07D417/04 , C07D417/12 , C07D513/04
摘要： Die vorliegende Erfindung betrifft Guanidinverbindungen der allgemeinen Formel (I) entsprechende enantiomere, diastereomere und/oder tautomere Formen davon sowie pharmazeutisch annehmbare Salze davon. Weiterhin betrifft die vorliegende Verbincaung die Verwendung von Guanidinverbindungen als Bindungspartner für 5-HT5-Rezeptoren zur Behandlung von Krankheiten, die durch eine 5-HT5-Rezeptoraktivität moduliert werden, insbesondere zur Behandlung von neurodegenerativen und neuropsychiatrischen Störungen sowie den damit zusammenhängenden Anzeichen, Symptomen und Fehlfunktionen.
摘要翻译：本发明涉及到其通式（I）对映异构体相应的胍化合物，非对映体和/或其互变异构形式，以及药学上可接受的盐。此外，本Verbincaung涉及使用胍作为用于5-HT5受体，它们由5 HT5受体活性调节的疾病的治疗的结合伴侣，尤其是用于治疗神经变性和神经精神病症的，以及相关的征兆，症状和故障，

3. 发明申请

WO2009027392A1 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 审中-公开
标题翻译： 4-（4-吡啶基） - 苯甲酸酯及其作为岩石活性调节剂的用途
公开(公告)号：WO2009027392A1
公开(公告)日：2009-03-05
申请号：PCT/EP2008/061135
申请日：2008-08-26
申请人： ABBOTT GMBH & CO. KG , MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl
发明人： MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl
IPC分类号： C07D213/56 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P35/00 , A61P29/00
CPC分类号： C07D401/12 , C07D213/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R 1 and R 2 are, independently of each other, hydrogen, hydroxy, cyano, C 1 -C 8 -alkyl, C 1 - C 8 -haloalkyl, C 1 -C 8 -alkoxy or C 1 -C 8 -haloalkoxy; R 3 , R 4 , R 5 and R 6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, C 1 -C 8 -alkoxy, C 1 -C 8 -haloalkoxy, amino, C 1 -C 8 -alkylamino or di-(C 1 -C 8 -alkyl)-amino; R 7 is hydrogen, C 1 -C 8 -alkyl, C 1 -C 8 -haloalkyl, aryl or aryl-C 1 -C 8 -alkyl; R 8 is a group of the formula -X-W, where X is a single bond, C 1 -C 4 -alkylene or C 1 -C 4 -alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R 9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR 11 , NR 12 R 13 , S(O) m -R 14 , phenyl which may carry 1, 2, 3 or 4 substituents R 15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C 1 C 4 -alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.
摘要翻译：本发明涉及式（I）的新型4-（4-吡啶基） - 苯甲酰胺。化合物I具有有价值的治疗特性，特别适用于治疗对Rho激酶（ROCK）的调节作用的疾病。 R 1和R 2彼此独立地为氢，羟基，氰基，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，C 1 -C 8 - 烷氧基或C 1 -C 8 - 卤代烷氧基; R3，R4，R5和R6彼此独立地为氢，羟基，卤素，氰基，C1-C8-烷基，C1-C8-卤代烷基，C1-C8-烷氧基，C1-C8-卤代烷氧基，氨基，C1- C 8 - 烷基氨基或二 - （C 1 -C 8 - 烷基） - 氨基; R 7是氢，C 1 -C 8 - 烷基，C 1 -C 8 - 卤代烷基，芳基或芳基-C 1 -C 8 - 烷基; R8是式-XW的基团，其中X是单键，C1-C4-亚烷基或C1-C4-亚烷基-O-，其中三个最后提及的基团中的亚烷基可以是直链或支链的，并且可以部分或完全卤化和/或可以被羟基取代和/或可被氧原子中断; 并且W是选自苯基和5-或6-元饱和，部分不饱和或芳族杂环的环状基团，其含有作为环成员1,2或3的选自O，S和N的杂原子和任选的1或2个羰基 ; R9是式-YZ的基团，其中Z是氢，卤素，OR11，NR12R13，S（O）m -R14，可以携带1,2,3或4个取代基R15或5-或6-元的苯基饱和，部分不饱和或芳族杂环; Y是可部分或完全卤化和/或可被羟基和/或苯环取代的直链或支链C 1 -C 4亚烷基; 或者Z为苯基或上述5-或6-元杂环的情况下，Y也可以是单键。

4. 发明公开

EP2167464A1 HETEROCYCLIC COMPOUNDS AS POSITIVE MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR 2 (MGLU2 RECEPTOR) 有权
标题翻译：杂环化合物代谢型谷氨酸受体2（的mGlu2 PRS）作为正调节剂
公开(公告)号：EP2167464A1
公开(公告)日：2010-03-31
申请号：EP08759978.3
申请日：2008-05-23
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： GENESTE, Hervé , SAUER, Daryl , BRAJE, Wilfried , AMBERG, Wilhelm , MEZLER, Mario , BAKKER, Margaretha Henrica Maria
IPC分类号： C07D209/26 , C07D231/12 , C07D333/58 , C07D239/26 , C07D277/28 , C07D233/58 , C07D409/04 , C07D409/06 , C07D333/20 , C07D307/14 , C07D213/36 , C07D213/38
CPC分类号： C07D209/14 , C07D207/335 , C07D209/26 , C07D213/36 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04 , C07D409/06
摘要： The present invention relates to heterocyclic compounds which are positive modulatorsof metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.

5. 发明公开

EP2193119A1 4-(4-PYRIDINYL)-BENZAMIDES AND THEIR USE AS ROCK ACTIVITY MODULATORS 有权
标题翻译： 4-（4-吡啶基）苯甲酰胺及其作为ROCK活性的调节剂
公开(公告)号：EP2193119A1
公开(公告)日：2010-06-09
申请号：EP08787483.0
申请日：2008-08-26
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： MACK, Helmut , TEUSCH, Nicole , MÜLLER, Bernhard K. , HORNBERGER, Wilfried , JARVIS, Michael F. , SAUER, Daryl , SWANN, Steve Jr , HOBSON, Adrian Donald , KEDDY, Ryan , BONAFOUX, Dominique , VASUDEVAN, Anil
IPC分类号： C07D213/56 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/4427 , A61P9/00 , A61P25/00 , A61P35/00 , A61P29/00
CPC分类号： C07D401/12 , C07D213/56 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs). R1 and R2 are, independently of each other, hydrogen, hydroxy, cyano, C1-C8-alkyl, C1- C8-haloalkyl, C1-C8-alkoxy or C1-C8-haloalkoxy; R3, R4, R5 and R6 are, independently of each other, hydrogen, hydroxy, halogen, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, amino, C1-C8-alkylamino or di-(C1-C8-alkyl)-amino; R7 is hydrogen, C1-C8-alkyl, C1-C8-haloalkyl, aryl or aryl-C1-C8-alkyl; R8 is a group of the formula -X-W, where X is a single bond, C1-C4-alkylene or C1-C4-alkylene-O-, where the alkylene group in the three last-mentioned radicals may be linear or branched and may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or may be interrupted by an oxygen atom; and W is a cyclic radical selected from phenyl and a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring which contains as ring members 1, 2 or 3 heteroatoms selected from O, S and N and optionally 1 or 2 carbonyl groups; R9 is a group of the formula -Y-Z, where Z is hydrogen, halogen, OR11, NR12R13, S(O)m-R14, phenyl which may carry 1, 2, 3 or 4 substituents R15 or a 5- or 6-membered saturated, partly unsaturated or aromatic heterocyclic ring; and Y is linear or branched C1C4-alkylene which may be partly or fully halogenated and/or may be substituted by a hydroxyl group and/or a phenyl ring; or, in case Z is phenyl or the 5- or 6-membered heterocyclic ring as defined above, Y can also be a single bond.

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