公开(公告)号：WO2010124042A2

公开(公告)日：2010-10-28

申请号：PCT/US2010/031974

申请日：2010-04-22

Applicant: ABBOTT LABORATORIES ,  ABBOTT GMBH & CO. KG ,  WANG, Ying ,  BREWER, Jason, T. ,  AKRITOPOULOU-ZANZE, Irini ,  DJURIC, Stevan, W. ,  POHLKI, Frauke ,  BRAJE, Wilfried ,  RELO, Ana-Lucia

Inventor： WANG, Ying ,  BREWER, Jason, T. ,  AKRITOPOULOU-ZANZE, Irini ,  DJURIC, Stevan, W. ,  POHLKI, Frauke ,  BRAJE, Wilfried ,  RELO, Ana-Lucia

IPC: C07D498/04

CPC classification number: C07D498/04 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2- a ][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2- a ][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1 H -pyrido[3,4- d ][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2- a ][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7 H -pyrazino[1,2- a ][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1 H -pyrazino[2,1- d ][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2- d ]pyrido[3,2- b ][1,4]diazepine derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , and Y 3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及1,2,3,4,4a，5,6,7-八氢吡嗪并[1,2-a] [1,4]苯并二氮杂，1,2,3,4,4a， 7-八氢吡嗪并[1,2-a] [1,5]苯并二氮杂，2,3,4,4a，5,6,7,11b-八氢-1H-吡啶并[3,4-d] [2]苯并氮杂， 1,2,3,4,4a，5,6,7-八氢吡嗪并[1,2-a] [1]苯并氮杂，1,2,3,4,4a，5-六氢-7H-吡嗪并[1,2 -a] [4,1]苯并氧氮杂和2,3,4,4a，5,6-六氢-1H-吡嗪并[2,1-d] [1,5]苯并氧氮杂和5,6,7,7a ，其中R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 5，R 6， X1，X2，X3，X4，Y1，Y2和Y3如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：WO2012059432A1

公开(公告)日：2012-05-10

申请号：PCT/EP2011/069009

申请日：2011-10-28

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  HAUPT, Andreas ,  POHLKI, Frauke ,  UNGER, Liliane ,  RELO, Ana Lucia ,  WICKE, Karsten ,  ZHANG, Min

Inventor： HAUPT, Andreas ,  POHLKI, Frauke ,  UNGER, Liliane ,  RELO, Ana Lucia ,  WICKE, Karsten ,  ZHANG, Min

IPC: C07D295/096 ,  A61K31/495 ,  A61K31/551 ,  A61P25/00 ,  A61P3/04 ,  C07D243/08

CPC classification number: C07D295/096 ,  C07D243/08

Abstract: The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, 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.

Abstract translation: 本发明涉及式I的N-苯基 - （同）哌嗪基 - 苯磺酰基或苯磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

公开(公告)号：WO2010124042A3

公开(公告)日：2011-02-03

申请号：PCT/US2010031974

申请日：2010-04-22

Applicant: ABBOTT LAB ,  ABBOTT GMBH & CO KG ,  WANG YING ,  BREWER JASON T ,  AKRITOPOULOU-ZANZE IRINI ,  DJURIC STEVAN W ,  POHLKI FRAUKE ,  BRAJE WILFRIED ,  RELO ANA-LUCIA

Inventor： WANG YING ,  BREWER JASON T ,  AKRITOPOULOU-ZANZE IRINI ,  DJURIC STEVAN W ,  POHLKI FRAUKE ,  BRAJE WILFRIED ,  RELO ANA-LUCIA

IPC: C07D498/04 ,  A61K31/4985 ,  A61K31/551 ,  A61K31/553 ,  A61P25/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

CPC classification number: C07D498/04 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/04

Abstract: The present application relates to 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,4]benzodiazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1,5]benzodiazepine, 2,3,4,4a,5,6,7,11b-octahydro-1H-pyrido[3,4-d][2]benzazepine, 1,2,3,4,4a,5,6,7-octahydropyrazino[1,2-a][1]benzazepine, 1,2,3,4,4a,5-hexahydro-7H-pyrazino[1,2-a][4,1]benzoxazepine, and 2,3,4,4a,5,6-hexahydro-1H-pyrazino[2,1-d][1,5]benzoxazepine, and 5,6,7,7a,8,9,10,11-octahydropyrazino[1,2-d]pyrido[3,2-b][1,4]diazepine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X1, X2, X3, X4, Y1, Y2, and Y3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及1,2,3,4,4a，5,6,7-八氢吡嗪并[1,2-a] [1,4]苯并二氮杂，1,2,3,4,4a， 7-八氢吡嗪并[1,2-a] [1,5]苯并二氮杂，2,3,4,4a，5,6,7,11b-八氢-1H-吡啶并[3,4-d] [2]苯并氮杂， 1,2,3,4,4a，5,6,7-八氢吡嗪并[1,2-a] [1]苯并氮杂，1,2,3,4,4a，5-六氢-7H-吡嗪并[1,2 -a] [4,1]苯并氧氮杂和2,3,4,4a，5,6-六氢-1H-吡嗪并[2,1-d] [1,5]苯并氧氮杂和5,6,7,7a ，其中R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 5，R 6， X1，X2，X3，X4，Y1，Y2和Y3如说明书中所定义。 本申请还涉及包含这些化合物的组合物，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：WO2012059431A1

公开(公告)日：2012-05-10

申请号：PCT/EP2011/069007

申请日：2011-10-28

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  HAUPT, Andreas ,  POHLKI, Frauke ,  UNGER, Liliane ,  RELO, Ana Lucia ,  WICKE, Karsten ,  ZHANG, Min

Inventor： HAUPT, Andreas ,  POHLKI, Frauke ,  UNGER, Liliane ,  RELO, Ana Lucia ,  WICKE, Karsten ,  ZHANG, Min

IPC: C07D209/52 ,  C07D211/24 ,  C07D221/06 ,  A61K31/403 ,  A61P25/00 ,  A61K31/439

CPC classification number: C07D209/52 ,  C07D211/24 ,  C07D221/06

Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae (IA) and (IB) wherein the variables have the meanings given in the claims and the description, 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.

Abstract translation: 本发明涉及式（IA）和（IB）的苯磺酰基或磺酰胺化合物，其中变量具有权利要求书和说明书中给出的含义，含有它们的药物组合物及其在治疗中的用途。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

公开(公告)号：WO2010125134A1

公开(公告)日：2010-11-04

申请号：PCT/EP2010/055789

申请日：2010-04-29

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  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

Inventor： 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: C07D241/04 ,  C07D317/06 ,  C07D295/096 ,  A61K31/495 ,  A61P25/18 ,  A61P25/28 ,  A61P25/30

CPC classification number: C07D295/096 ,  C07D241/04 ,  C07D243/08 ,  C07D317/46

Abstract: 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.

Abstract translation: 本发明涉及N-苯基 - （哌嗪基或高哌嗪基） - 苯磺酰胺或苯磺酰基 - 苯基 - （哌嗪或高哌嗪）化合物，含有它们的药物组合物及其在治疗中的用途。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。 其中X为键或基团N-R4; R1是氢或甲基; R2是氢或甲基; R3是氢，C1-C3烷基，氟，C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基，C3-C4环烷基或C3-C4环烷基-CH2-; R5是氢，氟，氯，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯; 且n为1或2。

公开(公告)号：WO2009056632A1

公开(公告)日：2009-05-07

申请号：PCT/EP2008/064811

申请日：2008-10-31

Applicant: ABBOTT GMBH & CO. KG ,  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

Inventor： 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: C07D295/12 ,  C07D405/12 ,  A61K31/495 ,  A61K31/496 ,  A61P3/04 ,  A61P25/00 ,  A61P25/18 ,  A61P25/28 ,  A61P25/30

CPC classification number: C07D295/12 ,  C07D405/12

Abstract: 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. wherein R 1 is hydrogen or methyl R 2 is hydrogen or methyl R 3 hydrogen, fluorine C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; R 4 is hydrogen, C 1 -C 4 alkyl or fluorinated C 1 -C 4 alkyl; R 5 is hydrogen, fluorine, C 1 -C 2 alkyl, fluorinated C 1 -C 2 alkyl, C 1 -C 2 alkoxy or fluorinated C 1 -C 2 alkoxy; and R 6 is hydrogen, fluorine or chlorine.

Abstract translation: 本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。 其中R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基，氟化C1-C2烷基，C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

公开(公告)号：WO2011146089A1

公开(公告)日：2011-11-24

申请号：PCT/US2010/057454

申请日：2010-11-19

Applicant: ABBOTT LABORATORIES ,  AKRITOPOULOU-ZANZE, Irini ,  BRAJE, Wilfried ,  DJURIC, Stevan W. ,  WILSON, Noel S. ,  TURNER, Sean C. ,  KRUGER, Albert W. ,  RELO, Ana-Lucia ,  SHEKHAR, Shashank ,  WELCH, Dennie S. ,  ZHAO, Hongyu ,  GANDARILLA, Jorge ,  GASIECKI, Alan F. ,  LI, Huanqiu ,  THOMPSON, Christina M. ,  ZHANG, Min ,  ABBOTT GMBH & CO. KG

Inventor： AKRITOPOULOU-ZANZE, Irini ,  BRAJE, Wilfried ,  DJURIC, Stevan W. ,  WILSON, Noel S. ,  TURNER, Sean C. ,  KRUGER, Albert W. ,  RELO, Ana-Lucia ,  SHEKHAR, Shashank ,  WELCH, Dennie S. ,  ZHAO, Hongyu ,  GANDARILLA, Jorge ,  GASIECKI, Alan F. ,  LI, Huanqiu ,  THOMPSON, Christina M. ,  ZHANG, Min

IPC: A01N43/00 ,  A01N43/46 ,  A61K31/55

CPC classification number: C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D513/04

Abstract: The present application relates to aryl- and heteroaryl-fused decahydropyrroloazepine, octahydrooxepinopyrrole, octahydropyrrolothiazepine dioxide, decahydrocyclohepta[ c ]pyrrole, and octahydrocyclohepta[ c ]pyrrole derivatives of formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , A, Y 1 , Y 2 , and Y 3 are as defined in the specification. The present application also relates to compositions comprising such compounds, processes for making such compounds, and methods of treating disease conditions using such compounds and compositions, and methods for identifying such compounds.

Abstract translation: 本申请涉及式（I）的芳基 - 和杂芳基 - 稠合十氢吡咯并氮平，二氢八氢化吡咯并噻吩，十氢环庚三烯并[c]吡咯和八氢环庚三烯并[c]吡咯衍生物，其中R1，R2，R3，R4，R5，A，Y1 ，Y2和Y3如说明书中所定义。 本申请还涉及包含这些化合物的组合物，制备这些化合物的方法，以及使用这些化合物和组合物治疗疾病状况的方法，以及鉴定这些化合物的方法。

公开(公告)号：WO2010125136A1

公开(公告)日：2010-11-04

申请号：PCT/EP2010/055791

申请日：2010-04-29

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  HAUPT, Andreas ,  POHLKI, Frauke ,  DRESCHER, Karla ,  WICKE, Karsten ,  UNGER, Liliane ,  RELO, Ana-Lucia ,  BESPALOV, Anton ,  VOGG, Barbara ,  BACKFISCH, Gisela ,  DELZER, Juergen ,  ZHANG, Min

Inventor： HAUPT, Andreas ,  POHLKI, Frauke ,  DRESCHER, Karla ,  WICKE, Karsten ,  UNGER, Liliane ,  RELO, Ana-Lucia ,  BESPALOV, Anton ,  VOGG, Barbara ,  BACKFISCH, Gisela ,  DELZER, Juergen ,  ZHANG, Min

IPC: C07D243/08 ,  C07D405/12 ,  A61K31/55 ,  A61P3/00

CPC classification number: C07D243/08 ,  C07D405/12

Abstract: 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.

Abstract translation: 本发明涉及式（I）和（I'）的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。 该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。 （I）（I'）F其中R1是氢或甲基; R2是氢或甲基，并且位于基团R1的邻近位置; R3氢，C1-C3烷基，卤素，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R4是氢，C1-C4烷基，C3-C4环烷基，C3-C4环烷基甲基或氟化C1-C4烷基; R5是氢，氟，氯，C1-C4烷基，氟化C1-C4烷基，C1-C4烷氧基或氟化C1-C4烷氧基; R6是氢，氟或氯。

公开(公告)号：WO2009056600A1

公开(公告)日：2009-05-07

申请号：PCT/EP2008/064732

申请日：2008-10-30

Applicant: ABBOTT GMBH & CO. KG ,  TURNER, Sean Colm ,  HAUPT, Andreas ,  BRAJE, Wilfried ,  LANGE, Udo ,  DRESCHER, Karla ,  UNGER, Liliane ,  JONGEN-RELO, Ana Lucia ,  BESPALOV, Anton

Inventor： TURNER, Sean Colm ,  HAUPT, Andreas ,  BRAJE, Wilfried ,  LANGE, Udo ,  DRESCHER, Karla ,  UNGER, Liliane ,  JONGEN-RELO, Ana Lucia ,  BESPALOV, Anton

IPC: C07D213/76 ,  C07D401/04 ,  A61P25/00 ,  A61K31/444

CPC classification number: C07D401/04 ,  C07D213/76

Abstract: The invention relates to compounds of the formula R 1 is selected from the group consisting of hydrogen, linear C 1 -C 3 alkyl and fluorinated linear C 1 -C 3 alkyl; R 2 is hydrogen or methyl; R 3 is selected from the group consisting of hydrogen, halogen, C 1 -C 2 -alkyl, fluorinated C 1 -C 2 -alkyl, C 1 -C 2 -alkoxy and fluorinated C 1 -C 2 -alkoxy, R 4 is C 1 -C 2 -alkyl or fluorinated C 1 -C 2 -alkyl; n is 0, 1 or 2, and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D 3 receptor antagonists or dopamine D 3 agonists, said method comprising administering an effective amount of at least one compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.

Abstract translation: 本发明涉及式R1的化合物选自氢，直链C 1 -C 3烷基和氟化线性C 1 -C 3烷基; R2是氢或甲基; R3选自氢，卤素，C1-C2-烷基，氟化C1-C2-烷基，C1-C2-烷氧基和氟化C1-C2-烷氧基，R4是C1-C2-烷基或氟化C1-C2 -烷基; n为0,1或2，以及这些化合物的生理上耐受的盐及其N-氧化物。 本发明还涉及包含至少一种式I化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺D3的病症的方法 所述方法包括向有需要的受试者施用有效量的至少一种式I化合物或生理学上耐受的酸加成盐。

公开(公告)号：WO2006015842A1

公开(公告)日：2006-02-16

申请号：PCT/EP2005/008592

申请日：2005-08-08

Applicant: ABBOTT GMBH & CO. KG ,  HAUPT, Andreas ,  UNGER, Liliane ,  DRESCHER, Karla ,  JONGEN-RELO, Ana, Lucia ,  GRANDEL, Roland ,  BRAJE, Wilfried ,  GENESTE, Hervé

Inventor： HAUPT, Andreas ,  UNGER, Liliane ,  DRESCHER, Karla ,  JONGEN-RELO, Ana, Lucia ,  GRANDEL, Roland ,  BRAJE, Wilfried ,  GENESTE, Hervé

IPC: C07D417/12

CPC classification number: C07D239/42 ,  C07D239/52 ,  C07D239/56 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

Abstract: The present invention relates to novel 4-piperazinylpyrimidine compounds. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D 3 receptor. The 4­ piperzinylpyrimidine compounds have the general formula (I), wherein Ar, X, A, R 1 and R 1a are as defined in the claims.

Abstract translation: 本发明涉及新的4-哌嗪基嘧啶化合物。 该化合物具有有价值的治疗性质，特别适用于治疗对多巴胺D 3受体调节作出反应的疾病。 4个哌嗪基嘧啶化合物具有通式（I），其中Ar，X，A，R 1和R 1a如权利要求中所定义。