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1. 发明公开

EP2424844A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译： BENZOLSULFONANILIDVERBINDUNGEN参与疾病治疗的适合ON血清素5-HT6受体应答的调节
公开(公告)号：EP2424844A1
公开(公告)日：2012-03-07
申请号：EP10718564.7
申请日：2010-04-29
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： HAUPT, Andreas , POHLKI, Frauke , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , RELO, Ana-Lucia , BESPALOV, Anton , VOGG, Barbara , BACKFISCH, Gisela , DELZER, Juergen , ZHANG, Min
IPC分类号： C07D243/08 , C07D405/12 , C07D295/135 , A61P3/04 , A61P25/00 , A61K31/495 , A61K31/496
CPC分类号： C07D295/135 , C07D243/08 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT
6 receptor. Formula (I) (I') wherein n is 1 or 2; R
1 is hydrogen or methyl and is positioned vicinal to the radical R
1 ; R
2 is hydrogen or methyl; R
3 is C
1 -C
3 alkyl; R
4 is hydrogen, C
1 -C
4 alkyl, cyclopropyl, C
3 -C
4 cycloalkylmethyl or fluorinated C
1 -C
4 alkyl; R
5 is hydrogen, fluorine, chlorine, C
1 -C
4 alkyl, fluorinated C
1 -C
4 alkyl, C
1 -C
4 alkoxy or fluorinated C
1 -C
4 alkoxy; and R
6 is hydrogen, fluorine or chlorine.

2. 发明授权

EP0877744B1 SUBSTITUIERTE AZA- UND DIAZACYCLOHEPTAN- UND -CYCLOOCTANVERBINDUNGEN UND DEREN VERWENDUNG 失效
标题翻译：取代的氮杂和DIAZACYCLOHEPTAN-和-CYCLOOCTANVERBINDUNGEN及其用途
公开(公告)号：EP0877744B1
公开(公告)日：2004-08-11
申请号：EP97901000.6
申请日：1997-01-10
申请人： Abbott GmbH & Co. KG
发明人： TREIBER, Hans-Jörg , BLANK, Stefan , STARCK, Dorothea , UNGER, Liliane , TESCHENDORF, Hans-Jürgen , WICKE, Karsten
IPC分类号： C07D403/12 , C07D403/04 , C07D243/08 , C07D409/12 , C07D213/73 , C07D403/14 , C07D401/14 , A61K31/505
CPC分类号： C07D403/04 , C07D403/12 , C07D403/14 , C07D417/14

3. 发明公开

EP2155724A1 AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译： FOR疾病对血清素5-HT 6受体反应APPROPRIATE AZETIDINVERBINDUNGEN的调制于治疗
公开(公告)号：EP2155724A1
公开(公告)日：2010-02-24
申请号：EP08735448.6
申请日：2008-03-20
申请人： Abbott GmbH & Co. KG
发明人： SCHULTZ, Thomas , BRAJE, Wilfried , TURNER, Sean Colm , HAUPT, Andreas , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , MAYRER, Matthias
IPC分类号： C07D403/04 , C07D471/04 , A61K31/404 , A61P25/28
CPC分类号： C07D471/04 , C07D403/04
摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; --- is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro- annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six- membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.

4. 发明公开

EP2139880A1 QUINOLINE COMPOUNDS SUITABLE FOR TREATING DIDORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译： FOR疾病对血清素5-HT 6受体反应APPROPRIATE喹啉的调制于治疗
公开(公告)号：EP2139880A1
公开(公告)日：2010-01-06
申请号：EP08735447.8
申请日：2008-03-20
申请人： Abbott GmbH & Co. KG
发明人： TURNER, Sean Colm , HAUPT, Andreas , BRAJE, Wilfried , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , WERNET, Wolfgang , MAYRER, Matthias
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P25/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. formula (I) wherein R is a moiety of the formula (R) wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2-Ar3 or Ar2-O-Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

5. 发明授权

EP1572698B1 3-SUBSTITUIERTE 3,4-DIHYDRO-THIENO¬2,3-D PYRIMIDIN-4-ONE-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 有权
标题翻译： 3-取代的-3,4-二氢THIENO¬2,3-D嘧啶-4-酮衍生物，其生产和使用
公开(公告)号：EP1572698B1
公开(公告)日：2008-07-02
申请号：EP03813137.1
申请日：2003-12-17
申请人： Abbott GmbH & Co. KG
发明人： BAKKER, Margaretha , HORNBERGER, Wilfried , KLING, Andreas , LANGE, Udo , MACK, Helmut , MOELLER, Achim , MUELLER, Reinhold , SCHELLHAAS, Kurt , SCHMIDT, Martin , STEINER, Gerd , WICKE, Karsten
IPC分类号： C07D495/14 , A61K31/519 , A61P25/00
CPC分类号： C07D495/14
摘要： The invention relates to 3,4-dihydro-thieno[2,3-d]pyrimidinde-4-one-derivatives which are substituted at 3-position with 5-membered heteroaryl which can be condensed with an aryl or heteroaryl radical. The heteroaryl and, optionally, the condensed aryl or heteroaryl radical 1,2 or 3 can independently include selected substitutents from C1-5-alkyl, C1-5-alkoxy, C1-5-alkylthio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2, -NH(R6), aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl, the substituents aryl, aryloxy, aralkyl, aralkyloxy and heteroaryl 1,2 or 3 independently include selected substituents from C1-5-alkythio, halogen, CN, halogen-C1-5-alkyl, halogen-C1-5alkoxy, hydroxy, -NH2, -N(R6)2 and -NH(R6). The invention also relates to the production and use of said derivatives, especially for therapeutical purposes, e.g. in the treatment of depression.

6. 发明授权

EP1023296B1 3-SUBSTITUIERTE PYRIDO 3',4':4,5] THIENO 2,3-d] PYRIMIDIN-DERIVATE, IHRE HERSTELLUNG UND VERWENDUNG 失效
标题翻译： 3-取代的吡啶并3”，4' ：4,5]噻吩并2,3-d]嘧啶衍生物，其生产和使用
公开(公告)号：EP1023296B1
公开(公告)日：2003-12-17
申请号：EP98936299.1
申请日：1998-05-29
申请人： Abbott GmbH & Co. KG
发明人： STEINER, Gerd , DULLWEBER, Uta , STARCK, Dorothea , BACH, Alfred , WICKE, Karsten , TESCHENDORF, Hans-Jürgen , GARCIA-LADONA, Francisco-Javier , EMLING, Franz
IPC分类号： C07D495/14 , A61K31/505
CPC分类号： C07D495/14
摘要： The invention relates to 3-substituted 3,4,5,6,7,8-hexahydro-pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives of formula (I) wherein R1 is a hydrogen atom, a C¿1?-C4 alkyl group, an acetyl group, a phenyl alkyl C1-C4 radical, the aromatic being optionally substituted by halogen, C1-C4 alkyl, trifluoromethyl, hydroxy, C1-C4 alkoxy, amino, cyano or nitro groups, or a phenylalkanon radical in which the phenyl group can be substituted by halogen, R?2¿ means a phenyl, pyridyl, pyrimidinyl or pyrazinyl group which is optionally mono- or disubstituted by halogen atoms, C¿1?-C4 alkyl, trifluoromethyl, trifluoromethoxy, hydroxy, C1-C4 alkoxy, amino, monomethylamino, dimethylamino, cyano or nitro groups and said group can be optionally anellated with a benzene nucleus which can be optionally mono- or disubstituted by halogen atoms, C1-C4 alkyl, hydroxy, trifluoromethyl, C1-C4 alkoxy, amino, cyano or nitro groups and may contain one nitrogen atom, or with a 5 or 6-membered ring which may contain 1-2 oxygen atoms, A represents NH or an oxygen atom, Y is CH2, CH2-CH2, CH2-CH2-CH2 or CH2CH, Z represents a nitrogen atom, carbon atom or CH and the bond between Y and Z can also be a double bond, and n represents the number 2, 3 or 4. The invention also relates to the physiologically compatible salts of the inventive 3-substituted pyrido [3',4':4,5] thieno [2,3-d] pyrimidine derivatives. The inventive compounds show a high level of affinity for the serotonin receptors 5-HT1B, 5-HT1D and 5-HT1A. The affinity for said receptors is approximately equal, at least on the same scale. Some of the inventive compounds also have a good capacity for inhibiting serotonin reuptake, a property used in most antidepressants.

7. 发明公开

EP2432770A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译： BENZOLSULFONANILIDVERBINDUNGEN用于治疗血清素5-HT 6受体调节有吸引力疾病
公开(公告)号：EP2432770A1
公开(公告)日：2012-03-28
申请号：EP10715854.5
申请日：2010-04-29
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： HAUPT, Andreas , POHLKI, Frauke , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , RELO, Ana-Lucia , BESPALOV, Anton , VOGG, Barbara , BACKFISCH, Gisela , DELZER, Juergen , ZHANG, Min
IPC分类号： C07D243/08 , C07D405/12 , A61K31/55 , A61P3/00
CPC分类号： C07D243/08 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the Formulae (I) and (I') and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT
6 receptor. (I) (I') F wherein R
1 is hydrogen or methyl; R
2 is hydrogen or methyl and is positioned vicinal to the radical R
1 ; R
3 hydrogen, C
1 -C
3 alkyl, halogen, C
1 -C
3 alkoxy, fluorinated C
1 -C
3 alkyl or fluorinated C
1 -C
3 alkoxy; R
4 is hydrogen, C
1 -C
4 alkyl, C
3 -C
4 cycloalkyl, C
3 -C
4 cycloalkylmethyl or fluorinated C
1 -C
4 alkyl; R
5 is hydrogen, fluorine, chlorine, C
1 -C
4 alkyl, fluorinated C
1 -C
4 alkyl, C
1 -C
4 alkoxy or fluorinated C
1 -C
4 alkoxy; and R
6 is hydrogen, fluorine or chlorine.

8. 发明授权

EP2139880B1 QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译： FOR疾病对血清素5-HT 6受体反应APPROPRIATE喹啉的调制于治疗
公开(公告)号：EP2139880B1
公开(公告)日：2011-09-14
申请号：EP08735447.8
申请日：2008-03-20
申请人： Abbott GmbH & Co. KG
发明人： TURNER, Sean Colm , HAUPT, Andreas , BRAJE, Wilfried , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , WERNET, Wolfgang , MAYRER, Matthias
IPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14 , A61K31/4709 , A61P25/00
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. formula (I) wherein R is a moiety of the formula (R) wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2-Ar3 or Ar2-O-Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.

9. 发明公开

EP2432769A1 N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR& xA; 有权
标题翻译： N-苯基（哌嗪基或高哌嗪基）-BENZOLSULFONAMID- OR苯磺酰基苯基 - （哌嗪或高哌嗪）的化合物，用于治疗血清素5-HT6受体调节疾病的吸引力
公开(公告)号：EP2432769A1
公开(公告)日：2012-03-28
申请号：EP10719748.5
申请日：2010-04-29
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： HAUPT, Andreas , POHLKI, Frauke , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , RELO, Ana-Lucia , BESPALOV, Anton , VOGG, Barbara , BACKFISCH, Gisela , DELZER, Juergen , ZHANG, Min , LAO, Yanbin
IPC分类号： C07D241/04 , C07D317/06 , C07D295/096 , A61K31/495 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D295/096 , C07D241/04 , C07D243/08 , C07D317/46
摘要： The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)- benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds,pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT
6 receptor. wherein X is a bond or a group N-R
4 ; R
1 is hydrogen or methyl; R
2 is hydrogen or methyl; R
3 is hydrogen, C
1 -C
3 alkyl, fluorine, C
1 -C
2 alkoxy or fluorinated C1-C
2 alkoxy; R
4 is hydrogen, C
1 -C
4 alkyl, C
3 -C
4 cycloalkyl, or C
3 -C
4 cycloalkyl-CH
2 -; R
5 is hydrogen, fluorine, chlorine, C
1 -C
2 alkyl, fluorinated C1-C2 alkyl, C
1 -C
2 alkoxy or fluorinated C
1 -C
2 alkoxy; R
6 is hydrogen, fluorine or chlorine; and n is 1 or 2.

10. 发明公开

EP2217583A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译： BENZOLSULFONANILIDVERBINDUNGEN参与疾病治疗的适合ON血清素5-HT6受体应答的调节
公开(公告)号：EP2217583A1
公开(公告)日：2010-08-18
申请号：EP08845310.5
申请日：2008-10-31
申请人： Abbott GmbH & Co. KG , Abbott Laboratories
发明人： BRAJE, Wilfried , TURNER, Sean Colm , HAUPT, Andreas , LANGE, Udo , DRESCHER, Karla , WICKE, Karsten , UNGER, Liliane , MEZLER, Mario , WERNET, Wolfgang , MAYRER, Matthias , JONGEN-RELO, Ana Lucia , BESPALOV, Anton , ZHANG, Min
IPC分类号： C07D295/12 , C07D405/12 , A61K31/495 , A61K31/496 , A61P3/04 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl, fluorinated C1-C2 alkyl, C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.

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