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1. 发明授权

US08318793B2 Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors 有权
标题翻译：杂环化合物及其作为糖原合酶激酶-3抑制剂的用途
公开(公告)号：US08318793B2
公开(公告)日：2012-11-27
申请号：US12748875
申请日：2010-03-29
申请人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Wilfried Hornberger , Falko Ernst Wolter
发明人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Wilfried Hornberger , Falko Ernst Wolter
IPC分类号： A61K31/40 , C07D209/34 , C07D295/00
CPC分类号： C07D401/04 , C07D491/04
摘要： The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：本发明涉及可用于抑制糖原合酶激酶3（GSK-3），制备该化合物的方法，含该化合物的组合物和使用该化合物的治疗方法的新型杂环化合物。

2. 发明授权

US09266855B2 Heterocyclic compounds and their use as glycogen synthase kinase-3 inhibitors 有权
标题翻译：杂环化合物及其作为糖原合酶激酶-3抑制剂的用途
公开(公告)号：US09266855B2
公开(公告)日：2016-02-23
申请号：US13245123
申请日：2011-09-26
申请人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Marcel Van Gaalen , Falko Ernst Wolter , Wilfried Hornberger , Marjoleen Nijsen
发明人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Marcel Van Gaalen , Falko Ernst Wolter , Wilfried Hornberger , Marjoleen Nijsen
IPC分类号： C07D215/20 , A61K31/4709 , C07D401/04 , C07D471/04
CPC分类号： C07D471/04 , C07D401/04
摘要： The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：本发明涉及可用于抑制糖原合酶激酶3（GSK-3），制备该化合物的方法，含该化合物的组合物和使用该化合物的治疗方法的新型杂环化合物。

3. 发明授权

US08497273B2 Heterocyclic compounds suitable for treating disorders that respond to modulation of the serotonin 5HT6 receptor 有权
标题翻译：适用于治疗对血清素5HT6受体的调节作用的病症的杂环化合物
公开(公告)号：US08497273B2
公开(公告)日：2013-07-30
申请号：US12297328
申请日：2007-04-18
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： A61K31/496 , C07D401/04 , C07D401/14 , A61K31/4439 , A61K31/4545 , C07D413/14 , C07D417/14
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The invention relates to compounds of the formula (I) wherein the variables have 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 medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
摘要翻译：本发明涉及式（I）化合物，其中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5HT6受体配体治疗的医学病症的药物中的用途。

4. 发明申请

US20110086863A1 BENZENESULFONANILIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：US20110086863A1
公开(公告)日：2011-04-14
申请号：US12851466
申请日：2010-08-05
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 , C07D241/04 , A61K31/495 , C07D405/12 , A61P25/00 , A61P3/04
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 and 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，氟和氯。

5. 发明申请

US20100048582A1 HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5HT6 RECEPTOR 有权
标题翻译：用于治疗响应调节SEROTONIN 5HT6受体的疾病的异种化合物
公开(公告)号：US20100048582A1
公开(公告)日：2010-02-25
申请号：US12297328
申请日：2007-04-18
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： A61K31/496 , C07D401/02 , A61P25/00 , A61P25/28 , A61P25/18
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The invention relates to compounds of the formula (I) wherein the variables have 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 medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
摘要翻译：本发明涉及式（I）化合物，其中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5HT6受体配体治疗的医学病症的药物中的用途。

6. 发明授权

US08642642B2 Heterocyclic arylsulphones suitable for treating disorders that respond to modulation of the serotonin 5HT6 receptor 有权
标题翻译：适用于治疗对血清素5HT6受体调节作出反应的病症的杂环芳香砜
公开(公告)号：US08642642B2
公开(公告)日：2014-02-04
申请号：US12297350
申请日：2007-04-18
申请人： Roland Grandel , Wilfried Martin Braje , Andreas Haupt , Sean Colm Turner , Udo Lange , Karla Drescher , Liliane Unger , Dan Plata
发明人： Roland Grandel , Wilfried Martin Braje , Andreas Haupt , Sean Colm Turner , Udo Lange , Karla Drescher , Liliane Unger , Dan Plata
IPC分类号： C07D417/10 , C07D413/10 , C07D409/10 , C07D401/10 , C07D403/10 , C07D207/09 , A61K31/5377 , A61K31/454 , A61K31/427 , A61K31/422 , A61K31/433 , A61K31/4245 , A61K31/4155 , A61K31/4025 , A61K31/40
CPC分类号： C07D207/09 , C07D205/04 , C07D211/28 , C07D401/12 , C07D403/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to compounds of the formula (I) wherein the variables have 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 medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
摘要翻译：本发明涉及式（I）化合物，其中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5HT6受体配体治疗的医学疾病的药物中的用途。

7. 发明授权

US08507469B2 Azetidin compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor 有权
标题翻译：适用于治疗对5-羟色胺5-HT 6受体的调节作用的疾病的氮杂环丁啶化合物
公开(公告)号：US08507469B2
公开(公告)日：2013-08-13
申请号：US12532406
申请日：2008-03-20
申请人： Thomas Schultz , Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer
发明人： Thomas Schultz , Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer
IPC分类号： A61K31/397 , C07D403/04 , C07D471/04
CPC分类号： C07D471/04 , C07D403/04
摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.
摘要翻译：本发明涉及式（I）化合物，其中A为C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6羟基烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 卤代烯基，C 3 -C 6 - 芳基-C 1 -C 4 - 烷基，芳基-C 2 -C 4 - 烯基，芳基或杂芳基; 是单键或双键; X1和X2是N，CRx1，NRx2或CRx3Rx4; Rx1，Rx3和Rx4是H，卤素，CN，NO2，C1-C6-烷基，C1-C6-烷氧基，C1-C6-烷基羰基等，或两个偕根基Rx3和Rx4与它们所在的碳原子一起结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢，C1-C6-烷基，C1-C6-烷基羰基，C1-C6-卤代烷基等; 或两个连位基Rx1，Rx2，Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1，Y2和Y3为N或CRy; Ry是H，卤素，CN，NO 2，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基羰基，C 1 -C 6 - 卤代烷基等; 其中基团X1，X2，Y1，Y2和Y3中的最多3个选自NRx1和N; R1是氢，C1-C6-烷基，C1-C6-羟基烷基，C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物，包含它们的药物组合物，治疗选自中枢神经系统疾病，成瘾疾病或肥胖症的医学病症的方法，所述方法包括向受试者施用有效量的这些化合物并且使用这种化合物来制备药物组合物。

8. 发明授权

US08455648B2 1-(7-(hexahydropyrrolo [3,4-c] pyrrol-2 (1H)-yl) quinolin-4-yl) -3- (pyrazin-2-yl) urea derivatives and related compounds as glycogen synthase kinase 3 (GSK-3) 有权
标题翻译： 1-（7-（六氢吡咯并[3,4-c]吡咯-2（1H） - 基）喹啉-4-基）-3-（吡嗪-2-基）脲衍生物和相关化合物作为糖原合酶激酶3 GSK-3）
公开(公告)号：US08455648B2
公开(公告)日：2013-06-04
申请号：US12988833
申请日：2009-04-24
申请人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Wilfried Hornberger
发明人： Sean Colm Turner , Margaretha Henrica Maria Bakker , Wilfried Hornberger
IPC分类号： C07D215/38
CPC分类号： C07D487/04 , C07D487/08 , C07D491/048
摘要： The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
摘要翻译：本发明涉及可用于抑制糖原合酶激酶3（GSK-3），制备该化合物的方法，含该化合物的组合物和使用该化合物的治疗方法的新型杂环化合物。

9. 发明授权

US08383641B2 Aryloxyethylamine compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作用的病症的芳氧基乙胺化合物
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。

10. 发明授权

US08293913B2 Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin-5-HT6 receptor 有权
标题翻译：喹啉化合物适用于治疗对血清素-5-HT6受体调节作用的疾病
公开(公告)号：US08293913B2
公开(公告)日：2012-10-23
申请号：US12664394
申请日：2008-08-06
申请人： Sean Colm Turner , Wilfried Braje , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Andrea Hager-Wernet, legal representative , Matthias Mayrer
发明人： Sean Colm Turner , Wilfried Braje , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer
IPC分类号： C07D215/36
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.
摘要翻译：本发明涉及式（I）的新颖喹啉化合物及其盐。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。在式（I）中，R是式（R）的部分，其中*表示与喹啉基的结合位点，其中A，B，X'，Y，Q，R 1，R 2，R 3，R 4，R 5， n，p，q，Ra，Rb，X和Ar如权利要求1所定义。

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