公开(公告)号：US20080045493A1

公开(公告)日：2008-02-21

申请号：US11665399

申请日：2005-10-14

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

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

IPC分类号： A61K31/397 ,  A61K31/4025 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/433 ,  A61K31/445 ,  A61K31/4523 ,  A61K31/496 ,  A61K31/4965 ,  A61K31/501 ,  A61K31/502 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5375 ,  A61K31/538 ,  A61K31/541 ,  A61P25/16 ,  C07D205/04 ,  C07D207/08 ,  C07D211/28 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D411/12 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

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) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C1-C6-alkyl, C1-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S 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, O 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; and 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.

公开(公告)号：US20110160176A1

公开(公告)日：2011-06-30

申请号：US12868480

申请日：2010-08-25

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 ,  C07D207/08 ,  A61K31/40 ,  C07D401/02 ,  C07D205/02 ,  C07D403/02 ,  A61K31/506 ,  C07D417/02 ,  A61K31/433 ,  C07D413/14 ,  A61K31/422 ,  C07D211/08 ,  A61K31/445 ,  A61P25/28

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) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S 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, O 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-C4alkylcarbonyl 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; and 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）化合物，其中n为0,1或2; G是CH 2或CHR 3; R 1是被C 3 -C 6 - 环烷基取代的C 1 -C 6 - 烷基，C 1 -C 6 - 烷基，C 1 -C 6羟基烷基，氟化C 1 -C 6 - 烷基，C 3 -C 6环烷基，氟化C 3 -C 6 - 环烷基，C3-C6烯基，氟化C3-C6-烯基，甲酰基，乙酰基或丙酰基; R2，R3和R4彼此独立地为H，甲基，氟甲基，二氟甲基或三氟甲基; A是可以被一个或多个选自卤素，甲基，甲氧基和CF 3的取代基取代的亚苯基，亚吡啶基，亚嘧啶基，吡嗪基，哒嗪基或噻吩基; E是NR5或CH2，其中R5是H或C1-C3-烷基; Ar是选自苯基，5或6元杂芳族基团的环状基团，其包含选自N，O和S的环成员1,2或3个杂原子和与饱和或不饱和5 - 或6-元碳环或杂环，其中杂环包含作为环成员1,2或3个选自N，O和S的杂原子和/或1,2或3个各自独立地选自NR8的含杂原子的基团，其中 R8是H，C1-C4-烷基，氟化C1-C4-烷基，C1-C4烷基羰基或氟化C1-C4-烷基羰基，其中环状基团Ar可以带有1,2或3个取代基Ra，其中变量Ra具有 在权利要求和说明书中给出的含义; 和其生理学耐受的酸加成盐。 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：US08470810B2

公开(公告)日：2013-06-25

申请号：US12868480

申请日：2010-08-25

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 ,  C07D413/02

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) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S 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, O 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-C4alkylcarbonyl 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; and 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）化合物，其中n为0,1或2; G是CH 2或CHR 3; R 1是被C 3 -C 6 - 环烷基取代的C 1 -C 6 - 烷基，C 1 -C 6 - 烷基，C 1 -C 6羟基烷基，氟化C 1 -C 6 - 烷基，C 3 -C 6环烷基，氟化C 3 -C 6 - 环烷基，C3-C6烯基，氟化C3-C6-烯基，甲酰基，乙酰基或丙酰基; R2，R3和R4彼此独立地为H，甲基，氟甲基，二氟甲基或三氟甲基; A是可以被一个或多个选自卤素，甲基，甲氧基和CF 3的取代基取代的亚苯基，亚吡啶基，亚嘧啶基，吡嗪基，哒嗪基或噻吩基; E是NR5或CH2，其中R5是H或C1-C3-烷基; Ar是选自苯基，5或6元杂芳族基团的环状基团，其包含选自N，O和S的环成员1,2或3个杂原子和与饱和或不饱和5 - 或6-元碳环或杂环，其中杂环包含作为环成员1,2或3个选自N，O和S的杂原子和/或1,2或3个各自独立地选自NR8的含杂原子的基团，其中 R8是H，C1-C4-烷基，氟化C1-C4-烷基，C1-C4烷基羰基或氟化C1-C4-烷基羰基，其中环状基团Ar可以带有1,2或3个取代基Ra，其中变量Ra具有 在权利要求和说明书中给出的含义; 和其生理学耐受的酸加成盐。 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：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：US20060160809A1

公开(公告)日：2006-07-20

申请号：US10823317

申请日：2004-04-13

申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl Sauer ,  Sean Turner

发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl Sauer ,  Sean Turner

IPC分类号： A61K31/53 ,  A61K31/506 ,  A61K31/501

CPC分类号： C07D213/76 ,  C07D213/74 ,  C07D239/69 ,  C07D401/04 ,  C07D487/08

摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

公开(公告)号：US20070054918A1

公开(公告)日：2007-03-08

申请号：US10552842

申请日：2004-04-13

申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl Sauer ,  Sean Turner

发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl Sauer ,  Sean Turner

IPC分类号： A61K31/506 ,  A61K31/501 ,  A61K31/496 ,  C07D403/14 ,  C07D403/02

CPC分类号： C07D213/74 ,  C07D213/76 ,  C07D239/48 ,  C07D239/50 ,  C07D403/04 ,  C07D403/14 ,  C07D487/08

摘要： The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1—C4-alkyl and C1—C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1—C6-alkyl, C2—C6-alkenyl, C2—C6-alkynyl, C3—C6-cycloalkyl, C3—C6-cycloalkyl-C1—C4-alkyl and C1—C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3—C4-alkylene; R1 is hydrogen, C1—C4-alkyl, C1—C4-haloalkyl, C3—C6-cycloalkyl, C3—C6-cycloalkyl-C1—C4-alkyl, C1—C4-hydroxyalkyl, C1—C4-alkoxy-C1—C4-alkyl, C3—C4-alkenyl or C3—C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.

公开(公告)号：US20080171751A1

公开(公告)日：2008-07-17

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： A61K31/496 ,  C07D403/14 ,  A61P25/00

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 optionally 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是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基，和 其中一个氮原子上的基团R 1a， R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基， 杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基， 氟化C 1 -C 6烷基或氟化C 3 -C 6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D 3的病症的方法 受体拮抗剂或多巴胺D 3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：US20120095015A1

公开(公告)日：2012-04-19

申请号：US13333702

申请日：2011-12-21

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： A61K31/506 ,  A61P25/00 ,  A61P25/18 ,  C07D403/14

CPC分类号： C07D403/12

摘要： The invention relates to compounds of 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 optionally 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 there compounds. The invention also relates to a pharmaceutically 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R1的C结合的1,2,4-三唑基团， 氮原子; 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烷氧基甲基或任选取代的苯基或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; 以及该化合物的生理耐受酸加成盐。 本发明还涉及包含至少一种式（I）的三唑化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂的病症的方法 或多巴胺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（I）的三唑化合物或生理上耐受的酸加成盐。

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：US08207160B2

公开(公告)日：2012-06-26

申请号：US10583590

申请日：2004-12-17

申请人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

发明人： Wilfried Braje ,  Andreas Haupt ,  Wilfried Lubisch ,  Roland Grandel ,  Karla Drescher ,  Herve Geneste ,  Liliane Unger ,  Daryl R. Sauer

IPC分类号： A61P25/00 ,  A61K31/55 ,  C07D223/16 ,  C07D409/12

CPC分类号： C07D223/16 ,  C07D409/12

摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.

摘要翻译： 本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐 的这些化合物和N-氧化物的生理上耐受的酸加成盐。 本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。 根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。