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1. 发明授权

US09242933B2 Heterocyclic compounds as positive modulators of metabotropic glutamate receptor 2 (mGlu2 receptor) 有权
标题翻译：杂环化合物作为代谢型谷氨酸受体2（mGlu2受体）的阳性调节剂
公开(公告)号：US09242933B2
公开(公告)日：2016-01-26
申请号：US12126174
申请日：2008-05-23
申请人： Herve Geneste , Daryl Sauer , Wilfried Braje , Wilhelm Amberg , Mario Mezler , Margaretha Henrica Maria Bakker
发明人： Herve Geneste , Daryl Sauer , Wilfried Braje , Wilhelm Amberg , Mario Mezler , Margaretha Henrica Maria Bakker
IPC分类号： C07D207/335 , C07D409/06 , C07D215/12 , C07D231/12 , A61K31/44 , C07D209/14 , C07D209/26 , C07D213/36 , C07D213/38 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04
CPC分类号： C07D209/14 , C07D207/335 , C07D209/26 , C07D213/36 , C07D213/38 , C07D215/12 , C07D231/12 , C07D233/58 , C07D239/26 , C07D261/08 , C07D277/28 , C07D307/14 , C07D307/54 , C07D333/20 , C07D333/58 , C07D407/04 , C07D409/04 , C07D409/06
摘要： The present invention relates to heterocyclic compounds which are positive modulators of metabotropic glutamate receptor. The present invention also relates to the use of these compounds for preparing a pharmaceutical composition and to a method of treating a medical disorder, selected from neurological and psychiatric disorders associated with glutamate dysfunction.
摘要翻译：本发明涉及作为代谢型谷氨酸受体的阳性调节剂的杂环化合物。本发明还涉及这些化合物用于制备药物组合物和治疗选自与谷氨酸功能障碍相关的神经和精神障碍的医学病症的方法的用途。

2. 发明授权

US08653100B2 Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：四氢异喹啉，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US08653100B2
公开(公告)日：2014-02-18
申请号：US12933326
申请日：2009-03-31
申请人： Michael Ochse , Udo Lange , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Wilhelm Amberg , Charles W. Hutchins
发明人： Michael Ochse , Udo Lange , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Wilhelm Amberg , Charles W. Hutchins
IPC分类号： C07D217/00 , A61K31/472
CPC分类号： C07D217/18 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07D513/04
摘要： The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）的四氢异喹啉或其生理上耐受的盐。本发明涉及包含这种四氢异喹啉的药物组合物以及用于治疗目的的这种四氢异喹啉的用途。四氢异喹啉是GlyT1抑制剂。

3. 发明授权

US08642587B2 Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：杂环化合物，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US08642587B2
公开(公告)日：2014-02-04
申请号：US12706321
申请日：2010-02-16
申请人： Udo Lange , Andreas Heutling , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler
发明人： Udo Lange , Andreas Heutling , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler
IPC分类号： A61K35/55 , A61K35/44 , C07D421/00 , C07D471/00 , C07D223/16
CPC分类号： C07D471/04 , C07D471/14 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for therapeutic purposes.
摘要翻译：本发明涉及式（I）的杂环化合物或其生理上耐受的盐。本发明还涉及包含这种杂环化合物的药物组合物，以及这些杂环化合物用于治疗目的的用途。

4. 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。

5. 发明申请

US20130203749A1 Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy 有权
公开(公告)号：US20130203749A1
公开(公告)日：2013-08-08
申请号：US13792105
申请日：2013-03-10
申请人： Wilhelm Amberg , Michael Ochse , Udo Lange , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles Hutchins
发明人： Wilhelm Amberg , Michael Ochse , Udo Lange , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles Hutchins
IPC分类号： C07D217/18 , C07D409/12 , C07D401/04 , C07D401/08 , C07D513/04 , C07D498/04 , C07D401/12 , C07D413/14
CPC分类号： C07D217/18 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07D513/04
摘要： The present invention relates to tetrahydroisoquinoline of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such tetrahydroisoquinolines, and the use of such tetrahydroisoquinolines for therapeutic purposes. The tetrahydroisoquinolines are GlyT1 inhibitors.

6. 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。

7. 发明授权

US08420670B2 4-benzylaminoquinolines, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译： 4-苄基氨基喹啉，含有它们的药物组合物及其在治疗中的用途
公开(公告)号：US08420670B2
公开(公告)日：2013-04-16
申请号：US12666629
申请日：2008-08-22
申请人： Wilhelm Amberg , Michael Ochse , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins
发明人： Wilhelm Amberg , Michael Ochse , Wilfried Braje , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D215/42 , C07D215/46 , C07D401/12 , C07D401/14
摘要： The present invention relates to 4-benzylaminoquinolines of the formula (I) or physiologically tolerated salts thereof. The invention relates to pharmaceutical compositions comprising such quinolines, and the use of such quinolines for therapeutic purposes. The quinolines are GIyTI inhibitors.
摘要翻译：本发明涉及式（I）的4-苄基氨基喹啉或其生理上耐受的盐。本发明涉及包含这种喹啉的药物组合物，以及这些喹啉用于治疗目的的用途。喹啉是GlyTI抑制剂。

8. 发明申请

US20120088790A1 PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 有权
标题翻译： PHENALKYLAMINE衍生物，含有它们的药物组合物及其在治疗中的使用
公开(公告)号：US20120088790A1
公开(公告)日：2012-04-12
申请号：US13206750
申请日：2011-08-10
申请人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Charles W. Hutchins , Wilfried Hornberger , Mario Mezler
发明人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Charles W. Hutchins , Wilfried Hornberger , Mario Mezler
IPC分类号： A61K31/4725 , A61K31/4035 , C07D401/12 , A61P25/00 , C07D217/18 , C07D209/44 , C07D217/22 , A61P25/18 , A61K31/472 , C07D217/26
CPC分类号： C07D401/12 , A61K31/357 , A61K31/472 , A61K31/4725 , A61K31/538 , C07D217/02 , C07D217/08 , C07D217/22 , C07D217/26
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) or (II) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such phenalkylamine derivatives, and the use of such phenalkylamine derivatives for therapeutic purposes. The phenalkylamine derivatives are GlyT1 inhibitors.
摘要翻译：本发明涉及式（I）或（II）的苯烷基胺衍生物或其生理上耐受的盐。本发明涉及包含这种苯烷基胺衍生物的药物组合物，以及这种苯烷基胺衍生物用于治疗目的的用途。酚烷基胺衍生物是GlyT1抑制剂。

9. 发明申请

US20110245247A1 NOVEL SMALL MOLECULE POTENTIATORS OF METABOTROPIC GLUTAMATE RECEPTORS 有权
公开(公告)号：US20110245247A1
公开(公告)日：2011-10-06
申请号：US13073087
申请日：2011-03-28
申请人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
发明人： Wilfried Braje , Katja Jantos , Hervé Geneste , Mario Mezler , Margaretha Henrica Maria Bakker
IPC分类号： A61K31/5377 , C07D401/12 , C07D401/14 , C07D413/14 , C07D403/12 , A61K31/4439 , A61K31/496 , A61K31/4725 , A61K31/497 , A61K31/4709 , A61K31/498 , A61P25/00 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/08 , A61P25/06
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要： The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I wherein X1 is N or C—R1, X2 is N or C—R2, X3 is N or C—R3, X4 is N or C—R4 provided that none or one of X1, X2, X3 or X4 is N; Y1 is N, C or C—R5, Y2 is N, C or C—R6, Y3 is Y1, Y2, N, C or C—R7, Y4 is N, C or C—R8 provided that only the moiety Y1, Y2, Y3 or Y4 to which Z is bound is C and further provided at most one of Y1, Y2, Y3 or Y4 is N; Z is O, S, S(O), S(O)2 or NRZ; Q is CH2 or CH2CH2, where one or two of the hydrogen atoms in CH2 or CH2CH2 may be replaced by halogen, C1-C4-alkyl or C1-C4-haloalkyl; R1 is inter alia hydrogen, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C4-haloalkoxy, C3-C8-cycloalkyl, a radical NR1aR1b, C-bound 3- to 7-membered, saturated heterocyclyl having 1 or 2 nitrogen atoms and 0 or 1 heteroatoms, selected from O and S, as ring members, aryl, aryl-CH2, aryloxy, hetaryl, hetaryloxy or hetaryl-CH2, wherein the heterocyclyl, aryl and hetaryl rings ring in the last six radicals themselves are unsubstituted or carry 1, 2, 3, 4 or 5 identical or different radicals R1c; R2 has one of the meanings given for R1; R3 and R4 are, inter alia, selected from hydrogen, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkyl, phenyl, C1-C4-haloalkoxy, a radical (CH2)nNR′R″; R5, R6, R7, R8 are, independently of each other, selected from hydrogen, halogen, etc.; Ra is C3-C6-cycloalkyl, C1-C6-haloalkyl or C1-C6-alkyl, which is unsubstituted or carries one radical selected from C1-C4-alkoxy, C1-C4-haloalkoxy and a radical NRa1Ra2; and the N-oxides and the pharmaceutically acceptable salts thereof.

10. 发明申请

US20110009378A1 Heterocyclic compounds, pharmaceutical compositions containing them, and their use in therapy 有权
标题翻译：杂环化合物，含有它们的药物组合物及其在治疗中的应用
公开(公告)号：US20110009378A1
公开(公告)日：2011-01-13
申请号：US12706321
申请日：2010-02-16
申请人： Udo Lange , Andreas Heutling , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler
发明人： Udo Lange , Andreas Heutling , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler
IPC分类号： A61K31/437 , C07D471/04 , A61K31/519 , C07D513/04 , A61P25/00
CPC分类号： C07D471/04 , C07D471/14 , C07D491/04 , C07D495/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to heterocyclic compounds of the formula (I) or a physiologically tolerated salt thereof.The present invention also relates to pharmaceutical compositions comprising such heterocyclic compounds, and the use of such heterocyclic compounds for therapeutic purposes.
摘要翻译：本发明涉及式（I）的杂环化合物或其生理上耐受的盐。本发明还涉及包含这种杂环化合物的药物组合物，以及这些杂环化合物用于治疗目的的用途。

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