公开(公告)号：US08383641B2

公开(公告)日：2013-02-26

申请号：US12296739

申请日：2007-04-13

申请人： Roland Grandel ,  Wilfried Martin Braje ,  Andreas Haupt ,  Sean Colm Turner ,  Udo Lange ,  Karla Drescher ,  Liliane Unger

发明人： Roland Grandel ,  Wilfried Martin Braje ,  Andreas Haupt ,  Sean Colm Turner ,  Udo Lange ,  Karla Drescher ,  Liliane Unger

IPC分类号： A61K31/44 ,  A61K31/4965 ,  C07D213/62 ,  C07D239/34

CPC分类号： C07D213/76 ,  C07D239/69

摘要： The present invention relates to aryloxyethylamine compounds of the formula I and the physiologically tolerated acid addition salts thereof. The variables have the meanings given in the claims and the description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

摘要翻译： 本发明涉及式I的芳氧基乙胺化合物及其生理上耐受的酸加成盐。 变量具有权利要求书和说明书中给出的含义。 本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

公开(公告)号：US08232426B2

公开(公告)日：2012-07-31

申请号：US11665288

申请日：2005-10-14

申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

IPC分类号： C07C303/00 ,  A61K31/18

CPC分类号： C07D213/76 ,  C07C311/21 ,  C07C311/29 ,  C07C2601/02 ,  C07D207/09

摘要： The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, or R1a and R2 together are (CH2)n with n being 2, 3 or 4, or R1a and R2a together are (CH2)n with n being 2, 3 or 4; R2 and R2a are are independently of each other H, C1-C4-alkyl or fluorinated C1-C4-alkyl or R2a and R2 together are (CH2)m with m being 1, 2, 3, 4 or 5; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, fluorine, C1-C4-alkyl and fluorinated C1-C4-alkyl or together form a moiety (CH2)p with p being 2, 3, 4 or 5; and the physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

摘要翻译： 本发明涉及式I的芳族化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以带有1个基团R a，并且其中Ar也可以带有1个或2个基团Rb; X为N或CH; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R 1a是H，C 1 -C 4 - 烷基，C 3 -C 4 - 环烷基，C 3 -C 4 - 环烷基甲基，C 3 -C 4 - 烯基，氟化C 1 -C 4 - 烷基，氟化C 3 -C 4 - 环烷基，氟化的C 3 -C 4环烷基甲基， C 3 -C 4 - 烯基或R 1a和R 2一起为（CH 2）n，其中n为2,3或4，或者R 1a和R 2a一起为（CH 2）n，n为2,3或4; R2和R2a彼此独立地为H，C1-C4-烷基或氟化C1-C4-烷基或R2a和R2一起为（CH2）m，其中m为1,2,3,4或5; R3是H或C1-C4-烷基; R 6，R 7彼此独立地选自H，氟，C 1 -C 4 - 烷基和氟化的C 1 -C 4 - 烷基或一起形成部分（CH 2）p，其中p为2,3,4或5; 及其生理上耐受的酸加成盐。 本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

公开(公告)号：US08101754B2

公开(公告)日：2012-01-24

申请号：US11792596

申请日：2005-12-01

申请人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

发明人： Liliane Unger ,  Andreas Haupt ,  Armin Beyerbach ,  Karla Drescher ,  Wilfried Braje ,  John Darbyshire ,  Sean C. Turner ,  Gisela Backfisch

IPC分类号： C07D403/14 ,  C07D403/12 ,  A61K31/506 ,  A61P25/18

CPC分类号： C07D403/12

摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionially substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole 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 triazole 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I化合物：其中n为1或2，Ar为在其余碳原子上携带基团R 1的C结合的1,2,4-三唑基团，其中一个氮气上具有基团R 1a 原子 R 1是氢，C 1 -C 6烷基，C 3 -C 6环烷基，C 1 -C 4烷氧基甲基，氟化C 1 -C 6烷基，氟化C 3 -C 6环烷基，氟化C 1 -C 4烷氧基甲基或选择性取代的苯基或5或6元杂芳基; R 1a是氢或C 1 -C 4烷基; 和R2是C1-C6烷基，C3-C6环烷基，氟化C1-C6烷基或氟化C3-C6环烷基; 以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺的病症的方法 D3激动剂，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III的三唑化合物或生理耐受的酸加成盐。

公开(公告)号：US20110319421A1

公开(公告)日：2011-12-29

申请号：US13187885

申请日：2011-07-21

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

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

IPC分类号： A61K31/496 ,  A61P3/10 ,  A61P25/18 ,  A61P25/30 ,  C07D401/04 ,  A61P25/00

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：US20110144146A1

公开(公告)日：2011-06-16

申请号：US11665287

申请日：2005-10-14

申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

IPC分类号： A61K31/437 ,  C07D209/04 ,  A61K31/405 ,  A61K31/16 ,  C07C331/00 ,  C07D235/00 ,  A61K31/415 ,  C07D471/02 ,  A61K31/40 ,  A61P25/00

CPC分类号： C07D471/04 ,  C07D209/14 ,  C07D209/62 ,  C07D235/14

摘要： The present invention relates to an aminomethyl substituted bicyclic aromatic compound of the formula I wherein Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered C-bound heteroaromatic radical comprising as ring member 1, 2 or 3 heteroatoms which are, independently of each other, selected from O, S and N, and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, 0 and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4-alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; X is a covalent bond or N—R2, CHR2, CHR2CH2, N or C—R2; Y is N—R2a, CHR2a, CHR2aCH2 or CHR2aCH2CH2; is a single bond or a double bond; E is CH2 or NR3; R1 is H, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C1C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-alkenyl, R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3 or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2 or 3; R3 is H or C1C4-alkyl; R4 and R5 independently of each other are H, C1-C4-alkyl, fluorinated C1-C4-alkyl or C1-C4-alkoxy or may form, together with N, a 4-, 5- or 6-membered saturated or unsaturated ring; R6 and R7 independently of each other are H or halogen; and the physiologically tolerated acid addition salts thereof.

公开(公告)号：US07851463B2

公开(公告)日：2010-12-14

申请号：US11665399

申请日：2005-10-14

申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel ,  Christophe Henry ,  Gisela Backfisch ,  Armin Beyerbach ,  Wilfried Lubisch

发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel ,  Christophe Henry ,  Gisela Backfisch ,  Armin Beyerbach ,  Wilfried Lubisch

IPC分类号： A61K31/397 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/40 ,  C07D239/42 ,  C07D401/04 ,  C07D207/04

CPC分类号： C07D413/14 ,  C07D205/04 ,  C07D207/09 ,  C07D211/28 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/10 ,  C07D413/12

摘要： The invention relates to compounds of the formula (I). The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.

摘要翻译： 本发明涉及式（I）化合物。 本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。 本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

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：US07759397B2

公开(公告)日：2010-07-20

申请号：US11665420

申请日：2005-10-14

申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

IPC分类号： A61K31/135 ,  C07C211/00

CPC分类号： C07D239/38 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07D221/06 ,  C07D333/34 ,  C07D401/12 ,  C07D409/12

摘要： The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及式（I）的6-氨基（氮杂）二氢化茚化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基，其中Ar可以带有1个基团Ra，其中Ar也可以 携带I或2个基团Rb; X为N或CH; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R1a是H或R1a，R2或R1a和R2a同时为（CH2）n，n为1,2,3或4; R2和R2a各自独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C，-C4-烷基; 和这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式（I）化合物或其药学上可接受的盐的药物组合物和治疗易受多巴胺D3受体配体治疗的医学疾病的方法，所述方法包括施用有效量 的至少一种式（I）化合物或其药学上可接受的盐。

公开(公告)号：US20090264437A1

公开(公告)日：2009-10-22

申请号：US11659063

申请日：2005-08-08

申请人： Andreas Haupt ,  Liliane Unger ,  Karla Drescher ,  Ana Lucia Jongen-Relo ,  Roland Grandel ,  Wilfried Braje ,  Herve Geneste

发明人： Andreas Haupt ,  Liliane Unger ,  Karla Drescher ,  Ana Lucia Jongen-Relo ,  Roland Grandel ,  Wilfried Braje ,  Herve Geneste

IPC分类号： A61K31/506 ,  A61P25/00 ,  C07D417/14 ,  C07D403/14 ,  C07D401/14 ,  C07D403/04

CPC分类号： C07D239/42 ,  C07D239/52 ,  C07D239/56 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12

摘要： 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 D3 receptor. The 4-piperzinylpyrimidine compounds have the general formula I wherein Ar, X, A, R1 and R1a are as defined in the claims.

摘要翻译： 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特性，特别适用于治疗对多巴胺D3受体调节作出反应的疾病。 4-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。

公开(公告)号：US20080318996A1

公开(公告)日：2008-12-25

申请号：US11665420

申请日：2005-10-14

申请人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

发明人： Karla Drescher ,  Andreas Haupt ,  Liliane Unger ,  Sean C. Turner ,  Wilfried Braje ,  Roland Grandel

IPC分类号： A61K31/435 ,  C07C311/15 ,  A61K31/18 ,  A61P25/00 ,  C07D221/06

CPC分类号： C07D239/38 ,  C07C311/21 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2602/08 ,  C07D221/06 ,  C07D333/34 ,  C07D401/12 ,  C07D409/12

摘要： The present invention relates to 6-amino(aza)indane compound of the formula (I) Wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical R6 and wherein Ar may also carry I or 2 radicals Rb; X is N or CH; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H or R1a and R2 or R1a and R2a together are (CH2)n with n being 1, 2, 3 or 4; R2 and R2a each independently are H, CH3, CH2F, CHF2 or CF3; R3 is H or C,-C4-alkyl; and the physiologically tolerated acid addition salts of these compounds. The invention also relates to pharmaceutical compositions comprising at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof and to a method for treating a medical disorder susceptible to treatment with a dopamine D3 receptor ligand, said method comprising administering an effective amount of at least one compound of the formula (I) or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明涉及式（I）的6-氨基（氮杂）二氢化茚化合物，其中Ar是苯基或芳族5-或6-元C-结合的杂芳族基团，其中Ar可以携带1个基团R6，并且其中Ar也可以 携带I或2个基团Rb; X为N或CH; E为CR6R7或NR3; R 1是C 1 -C 4烷基，C 3 -C 4环烷基，C 3 -C 4环烷基甲基，C 3 -C 4链烯基，氟化C 1 -C 4烷基，氟化C 3 -C 4环烷基，氟化C 3 -C 4环烷基甲基， C4-烯基，甲酰基或C1-C3-烷基羰基; R1a是H或R1a，R2或R1a和R2a同时为（CH2）n，n为1,2,3或4; R2和R2a各自独立地为H，CH3，CH2F，CHF2或CF3; R3是H或C，-C4-烷基; 和这些化合物的生理上耐受的酸加成盐。 本发明还涉及包含至少一种式（I）化合物或其药学上可接受的盐的药物组合物和治疗易受多巴胺D3受体配体治疗的医学疾病的方法，所述方法包括施用有效量 的至少一种式（I）化合物或其药学上可接受的盐。