公开(公告)号：US20090131452A1

公开(公告)日：2009-05-21

申请号：US12262455

申请日：2008-10-31

申请人： Wilfried Martin Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Wolfgang Wernet ,  Matthias Mayrer ,  Ana Jongen-Relo ,  Anton Bespalov ,  Min Zhang

发明人： Wilfried Martin Braje ,  Sean Colm Turner ,  Andreas Haupt ,  Udo Lange ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Mario Mezler ,  Wolfgang Wernet ,  Matthias Mayrer ,  Ana Jongen-Relo ,  Anton Bespalov ,  Min Zhang

IPC分类号： A61K31/496 ,  C07D295/182 ,  C07D405/12 ,  A61P25/00 ,  A61K31/495

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.

摘要翻译： 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：US20120040969A1

公开(公告)日：2012-02-16

申请号：US13284204

申请日：2011-10-28

申请人： Andreas Haupt ,  Frauke Pohlki ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Ana-Lucia Relo ,  Anton Bespalov ,  Barbara Vogg ,  Gisela Backfisch ,  Juergen Delzer ,  Min Zhang ,  Yanbin Lao

发明人： Andreas Haupt ,  Frauke Pohlki ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Ana-Lucia Relo ,  Anton Bespalov ,  Barbara Vogg ,  Gisela Backfisch ,  Juergen Delzer ,  Min Zhang ,  Yanbin Lao

IPC分类号： A61K31/551 ,  C07D241/04 ,  A61P25/28 ,  A61P25/00 ,  A61P25/18 ,  C07D243/08 ,  A61K31/4965

CPC分类号： C07D241/04 ,  C07D243/08 ,  C07D295/096 ,  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-HT6 receptor.

摘要翻译： 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。

公开(公告)号：US20100292220A1

公开(公告)日：2010-11-18

申请号：US12769878

申请日：2010-04-29

申请人： Andreas Haupt ,  Frauke Pohlki ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Ana-Lucia Relo ,  Anton Bespalov ,  Barbara Vogg ,  Gisela Backfisch ,  Juergen Delzer ,  Min Zhang

发明人： Andreas Haupt ,  Frauke Pohlki ,  Karla Drescher ,  Karsten Wicke ,  Liliane Unger ,  Ana-Lucia Relo ,  Anton Bespalov ,  Barbara Vogg ,  Gisela Backfisch ,  Juergen Delzer ,  Min Zhang

IPC分类号： A61K31/551 ,  C07D243/08 ,  A61P25/28 ,  A61P25/18 ,  A61P25/30 ,  A61P3/04

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-HT6 receptor. wherein R1 is hydrogen or methyl; R2 is hydrogen or methyl and is positioned vicinal to the radical R1; R3 hydrogen, C1-C3 alkyl, halogen, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R4 is hydrogen, C1-C4 alkyl, C3-C4 cycloalkyl, C3-C4 cycloalkylmethyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, chlorine, C1-C4 alkyl, fluorinated C1-C4 alkyl, C1-C4 alkoxy or fluorinated C1-C4 alkoxy; and R6 is hydrogen, fluorine or chlorine.

摘要翻译： 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，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：US20100210664A1

公开(公告)日：2010-08-19

申请号：US12666627

申请日：2008-10-30

申请人： Sean Colm Turner ,  Andreas Haupt ,  Wilfred Braje ,  Udo Lange ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Bespalov Anton

发明人： Sean Colm Turner ,  Andreas Haupt ,  Wilfred Braje ,  Udo Lange ,  Karla Drescher ,  Liliane Unger ,  Ana Lucia Jongen-Relo ,  Bespalov Anton

IPC分类号： A61K31/496 ,  C07D401/04 ,  A61P25/00 ,  A61P25/30 ,  A61P25/18

CPC分类号： C07D401/04 ,  C07D213/76

摘要： The invention relates to compounds of the formula R1 is selected from the group consisting of hydrogen, linear C1-C3 alkyl and fluorinated linear C1-C3 alkyl; R2 is hydrogen or methyl; R3 is selected from the group consisting of hydrogen, halogen, C1-C2-alkyl, fluorinated C1-C2-alkyl, C1-C2-alkoxy and fluorinated C1-C2-alkoxy, R4 is C1-C2-alkyl or fluorinated C1-C2-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 D3 receptor antagonists or dopamine D3 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.

摘要翻译： 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：US08268815B2

公开(公告)日：2012-09-18

申请号：US12842776

申请日：2010-07-23

申请人： Hervè Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

发明人： Hervè Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

IPC分类号： C07D401/12 ,  C07D413/12 ,  C07D417/12 ,  A61K31/506 ,  A61P25/36

CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D413/12

摘要： The invention relates to compounds of formula (I) and the use of these compounds.

摘要翻译： 本发明涉及式（I）化合物和这些化合物的用途。

公开(公告)号：US08008488B2

公开(公告)日：2011-08-30

申请号：US10548931

申请日：2004-03-12

申请人： Hervé Geneste ,  Andreas Kling ,  Wilfried Braje ,  Andreas Haupt ,  Liliane Unger

发明人： Hervé Geneste ,  Andreas Kling ,  Wilfried Braje ,  Andreas Haupt ,  Liliane Unger

IPC分类号： C07D403/06 ,  C07D403/14 ,  C07D401/06 ,  C07D401/14 ,  A61K31/505 ,  A61K31/506 ,  A61P25/16 ,  A61P25/18 ,  A61P25/24 ,  A61P25/22 ,  A61P25/30

CPC分类号： C07D239/36 ,  C07D239/52 ,  C07D239/54 ,  C07D239/553 ,  C07D239/56 ,  C07D401/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14

摘要： The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.

摘要翻译： 除了（I）的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外，本发明涉及通式（I）的嘧啶-2-酮化合物。 在所述式中，A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O，S， C（O），NR 3，C（O）NR 3，NR 3 C（O），OC（O）和C（O）O; B表示式（II）的基团，其中X表示CH2或N，Y表示CH2或CH2CH2，或X-Y也可共同表示C = CH，C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。 本发明还涉及含有至少一种化合物（I）和所述化合物的互变异构体，衍生物和/或酸加成盐，任选地与生理上可接受的载体和/或辅助剂一起的药剂。 本发明还涉及式（I）化合物及其互变异构体，衍生物和药理学上可接受的酸加成盐的用途，用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。

公开(公告)号：US20110118232A1

公开(公告)日：2011-05-19

申请号：US12842776

申请日：2010-07-23

申请人： Hervè Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

发明人： Hervè Geneste ,  Andreas Haupt ,  Wilfried Braje ,  Wilfried Lubisch ,  Gerd Steiner

IPC分类号： A61K31/554 ,  C07D403/14 ,  A61K31/496 ,  C07D413/14 ,  A61K31/538 ,  C07D417/14 ,  A61K31/5415 ,  A61K31/551 ,  A61K31/55 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D417/12 ,  C07D401/12 ,  C07D413/12

摘要： The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C═W or CRfRg; B represents a chemical bond or a group CRhRi; X represents O, S, a group N—Rk or a group CRmRn; D represents C═O or a chemical bond; E represents a linear or branched 2- to 10-membered alkylene chain that, as members of a chain, can have 1 or 2 non-adjacent heteroatom group(s) K, which is selected among O, S, S(O), S(O)2 and N—Rp and which can comprise a carbonyl group and/or a cycloalkanediyl group and/or a double or triple bond; W represents oxygen or sulfur; Z, together with the carbon atoms, to which it is bound, represents a condensed, optionally substituted 5-, 6- or 7-membered carbocyclic compound or heterocyclic compound that has 1, 2, 3 or 4 heteroatoms, which are selected among N, O and S; J represents CH2, CH2—CH2 or CH2—CH2—CH2; M represents CH or N; Y represents CH2, CH2—CH2 or CH2—CH2—CH2 or M-X, together, represent CH═C or CH2—CH═C; n is 0 or 1, and; Ra, Rb, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rk, Rp, R1, R2, R3, R4, R5 and R6 have the meanings cited in the claims and in the description. The invention also relates to the physiologically compatible acid addition salts of the aforementioned compounds, and to the use of these compounds of general formula (I) and of the physiologically compatible acid addition salts of compounds (I) for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor antagonists or agonists.

摘要翻译： 本发明涉及通式（I）的新型嘧啶化合物，其中：A代表基团C = W或CRfRg; B表示化学键或CRhRi基; X表示O，S，基团N-Rk或基团CRmRn; D表示C = O或化学键; E表示直链或支链的2-至10-元亚烷基链，其作为链的成员可以具有1或2个不相邻的杂原子K，其选自O，S，S（O）， S（O）2和N-Rp，并且其可以包含羰基和/或环烷二基和/或双键或三键; W表示氧或硫; Z与其结合的碳原子一起代表具有1,2,3或4个杂原子的缩合的，任选取代的5-，6-或7-元碳环化合物或杂环化合物，其选自N ，O和S; J表示CH 2，CH 2 -CH 2或CH 2 -CH 2 -CH 2; M表示CH或N; Y表示CH 2，CH 2 -CH 2或CH 2 -CH 2 -CH 2或M-X，一起表示CH = C或CH 2 -CH = C; n为0或1， Ra，Rb，Rc，Rd，Re，Rf，Rg，Rh，Ri，Rk，Rp，R1，R2，R3，R4，R5和R6具有权利要求书和说明书中引用的含义。 本发明还涉及上述化合物的生理上相容的酸加成盐，以及这些化合物（I）的化合物和化合物（I）的生理上相容的酸加成盐在制备用于治疗疾病的药剂中的用途 ，其响应于多巴胺D3受体拮抗剂或激动剂的影响。

公开(公告)号：US20110245266A1

公开(公告)日：2011-10-06

申请号：US13103734

申请日：2011-05-09

申请人： Hervé Geneste ,  Wilfried Braje ,  Andreas Haupt

发明人： Hervé Geneste ,  Wilfried Braje ,  Andreas Haupt

IPC分类号： A61K31/497 ,  C07D403/14 ,  A61P25/18 ,  A61P25/24

CPC分类号： C07D401/12

摘要： The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.

摘要翻译： 本发明涉及通式（I）的新型吡啶-2-酮化合物，其中A表示可具有1或2个甲基作为取代基的4至6元烃链，其中1或2个碳原子可以是 由氧，羰基或硫取代，烃链可以具有双键或三键; R1，R2，R3和R4具有权利要求书和说明书中引用的含义。 本发明还涉及化合物I的互变异构体，化合物I的生理上可接受的盐，以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式（I）的化合物和 互变异构体，以及化合物I和互变异构体的生理上可接受的盐的用途，用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。

公开(公告)号：US08334289B2

公开(公告)日：2012-12-18

申请号：US13103734

申请日：2011-05-09

申请人： Hervé Geneste ,  Wilfried Braje ,  Andreas Haupt

发明人： Hervé Geneste ,  Wilfried Braje ,  Andreas Haupt

IPC分类号： A61K31/506

CPC分类号： C07D401/12

摘要： The invention relates to novel pyridin-2-one compounds of general formula (I), in which A represents a 4- to 6-membered hydrocarbon chain that can have 1 or 2 methyl groups as substituents, wherein 1 or 2 carbon atoms can be replaced by oxygen, a carbonyl group or sulfur, and the hydrocarbon chain can have a double bond or a triple bond; R1, R2, R3 and R4 have the meanings as cited in the claims and in the description. The invention also relates to the tautomers of compounds I, the physiologically acceptable salts of compounds I, and to the physiologically acceptable salts of the tautomers of compounds I. The invention also relates to the use of compounds of general formula (I) and of the tautomers, and to the use of the physiologically acceptable salts of compounds I and of the tautomers for producing a pharmaceutical agent for treating diseases that respond to the influence of dopamine D3 receptor antagonists or agonists.

摘要翻译： 本发明涉及通式（I）的新型吡啶-2-酮化合物，其中A表示可具有1或2个甲基作为取代基的4至6元烃链，其中1或2个碳原子可以是 由氧，羰基或硫取代，烃链可以具有双键或三键; R1，R2，R3和R4具有权利要求书和说明书中引用的含义。 本发明还涉及化合物I的互变异构体，化合物I的生理上可接受的盐，以及化合物I的互变异构体的生理上可接受的盐。本发明还涉及通式（I）的化合物和 互变异构体，以及化合物I和互变异构体的生理上可接受的盐的用途，用于制备用于治疗对多巴胺D3受体拮抗剂或激动剂的影响作出反应的疾病的药剂。

公开(公告)号：US20070219182A1

公开(公告)日：2007-09-20

申请号：US10582285

申请日：2004-12-10

申请人： Wilfried Lubisch ,  Andreas Haupt

发明人： Wilfried Lubisch ,  Andreas Haupt

IPC分类号： A61K31/55 ,  A61P13/12 ,  A61P25/28 ,  C07D223/16 ,  C07D401/12 ,  C07D403/12

CPC分类号： C07D401/12 ,  C07D223/16 ,  C07D403/12

摘要： The invention relates to novel keto lactam compounds, hydrogenated derivatives and tautomers thereof. These compounds have valuable therapeutic properties and are particularly suited for treating diseases that respond to the modulation of the dopamine D3 receptor. The keto lactams have general formula (I), wherein: (a) represents a group of formulas (b) or (c), wherein D is bound to the nitrogen atom and W, Rp and Rq have the meanings cited in Claim 1; —B— represents a bond or (d), wherein Rm and Rn have the meanings cited in Claim 1; (e) represents a single bond or a double bond; Rv, Rw, Rx and Ry have the meanings cited in Claim 1; D represents a linear or branched 2 to 10-membered alkylene chain that can have, as chain members, a heteroatom group K, which is selected among O, S, S(O), S(O)2, N—R8, CO—O, C(O)NR8 and/or 1 or 2 non-adjacent carbonyl groups and which can have a cycloalkane diyl group and/or a double or triple bond: (f) represents a saturated or monounsaturated monocyclic nitrogen heterocyclic compound having 5 to 8 cyclic members or a bicyclic saturated nitrogens heterocyclic compound having 7 to 12 cyclic members.

摘要翻译： 本发明涉及新型酮内酰胺化合物，氢化衍生物及其互变异构体。 这些化合物具有有价值的治疗特性，特别适用于治疗对多巴胺D 3受体调节作出反应的疾病。 酮内酰胺具有通式（I），其中：（a）表示式（b）或（c）的基团，其中D与氮原子结合，W，R p和R ^{具有权利要求1中引用的含义; -B-表示键或（d），其中R“和”R“具有权利要求1中引用的含义; （e）表示单键或双键; R 0，R x，R x和R y具有权利要求1中引用的含义; D表示可以具有作为链成员的选自O，S，S（O），S（O）2}