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：WO2010125135A1

公开(公告)日：2010-11-04

申请号：PCT/EP2010/055790

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 ,  C07D295/135 ,  A61P3/04 ,  A61P25/00 ,  A61K31/495 ,  A61K31/496

CPC classification number: C07D295/135 ,  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. 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.

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。 式（I）（I'）其中n为1或2; R1是氢或甲基，并且位于基团R1的邻近位置; R2是氢或甲基; R3是C1-C3烷基; R4是氢，C1-C4烷基，环丙基，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：WO2009056625A1

公开(公告)日：2009-05-07

申请号：PCT/EP2008/064795

申请日：2008-10-31

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

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

IPC: C07D403/12 ,  A61K31/53 ,  A61P25/00 ,  A61P25/18 ,  A61P25/30

CPC classification number: C07D403/12

Abstract: The invention relates to compounds of the formula (I), wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R 1 is selected from the group consisting of hydrogen, C 1 -C 3 alkyl and fluorinated C 1 -C 3 alkyl; R 2 is hydrogen, halogen, cyano, C 1 -C 3 alkyl, C 1 -C 3 alkoxy, fluorinated C 1 -C 3 alkyl or fluorinated C 1 -C 3 alkoxy; R 3 is selected from the group consisting of branched C 4 -C 6 alkyl and C 3 -C 6 cycloalkyl, and R 4 is C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, fluorinated C 1 -C 3 alkyl and fluorinated C 3 -C 6 cycloalkyl. 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 furtherto amethod 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（I）化合物，其中A是链长为4-6个碳原子的饱和或不饱和烃链，该烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C 4 -C 6烷基和C 3 -C 6环烷基，且R 4为C 1 -C 6烷基，C 3 -C 6环烷基，氟化C 1 -C 3烷基和氟化C 3 -C 6环烷基。 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，还涉及用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3拮抗剂的病症的方法， 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）的化合物或生理学上耐受的酸加成盐。

公开(公告)号：WO2010142739A1

公开(公告)日：2010-12-16

申请号：PCT/EP2010/058107

申请日：2010-06-09

Applicant: ABBOTT GMBH & CO. KG ,  ABBOTT LABORATORIES ,  BRAJE, Wilfried ,  VAN GAALEN, Marcel ,  BESPALOV, Anton ,  MILLS, Charles David

Inventor： BRAJE, Wilfried ,  VAN GAALEN, Marcel ,  BESPALOV, Anton ,  MILLS, Charles David

IPC: A61K31/404 ,  C07B59/00 ,  A61P25/00

CPC classification number: A61K31/404

Abstract: The present invention relates to the use of substituted oxindole derivatives of formula I as defined in the claims and description for the treatment or prophylaxis of pain.

Abstract translation: 本发明涉及如权利要求和说明书所定义的式I的取代羟吲哚衍生物在治疗或预防疼痛中的应用。

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。