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公开(公告)号：US10556914B2
公开(公告)日：2020-02-11
申请号：US16409323
申请日：2019-05-10
发明人： Jürgen Dinges , Achim Moeller , Michael Ochse , Martin Schmidt , Michael Schulz , Sean Turner , Elizabeth Louise Van Der Kam , Anil Vasudevan
IPC分类号： C07D498/04 , C07D513/04 , A61K31/4985
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
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公开(公告)号：US10556907B2
公开(公告)日：2020-02-11
申请号：US15248994
申请日：2016-08-26
发明人： Udo Lange , Michael Ochse , Elizabeth van der Kam , Jeroen van Bergeijk , Sean Turner , Frank Oellien , Patrick Walleser , Wilhelm Amberg , Wilfried Hornberger , Herve Geneste , Mario Mezler , Charles Hutchins
IPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.
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公开(公告)号：US09828381B2
公开(公告)日：2017-11-28
申请号：US15133851
申请日：2016-04-20
发明人： Ramin Faghih , Achim Moeller , Michael Ochse , Frauke Pohlki , Martin Schmidt , Kevin Sippy , Sean Turner , Elizabeth Louise Van Der Kam
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , A61K31/519 , C07D519/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
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公开(公告)号：US20170057966A1
公开(公告)日：2017-03-02
申请号：US15248994
申请日：2016-08-26
发明人： Udo Lange , Michael Ochse , Elizabeth van der Kam , Jeroen van Bergeijk , Sean Turner , Frank Oellien , Patrick Walleser , Wilhelm Amberg , Wilfried Hornberger , Herve Geneste , Mario Mezler , Charles Hutchins
IPC分类号： C07D487/04 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to heterocyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.
摘要翻译： 本发明涉及作为S1P调节剂的杂环化合物，包含这些化合物的药物组合物及其用于治疗，缓解或预防由S1P受体介导的疾病或病症的用途。
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5.发明授权Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy 有权苯烷基胺衍生物，含有它们的药物组合物及其在治疗中的用途公开(公告)号：US09238619B2
公开(公告)日：2016-01-19
申请号：US14282712
申请日：2014-05-20
发明人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins , Sean Turner
IPC分类号： A61K31/135 , C07C211/25 , C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D295/135 , C07D401/12 , C07D403/12 , C07D233/84
CPC分类号： C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) 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）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。
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公开(公告)号：US20220169620A1
公开(公告)日：2022-06-02
申请号：US17537600
申请日：2021-11-30
发明人： Willie Amberg , Gisela Backfisch , Karen Bodié , Katja Hempel , Loic Laplanche , Mario Mezler , Michael Ochse , Sean Turner , Jeroen van Bergeijk , Elizabeth van der Kam
IPC分类号： C07D265/34
摘要： The present invention is directed to spiro-cyclic amine derivatives which are modulators of S1P receptors and are useful in the treatment of CNS disorders.
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公开(公告)号：US10155770B2
公开(公告)日：2018-12-18
申请号：US15793711
申请日：2017-10-25
发明人： Ramin Faghih , Achim Moeller , Michael Ochse , Frauke Pohlki , Martin Schmidt , Kevin Sippy , Sean Turner , Elizabeth Louise Van Der Kam
IPC分类号： A61K31/519 , C07D487/04 , C07D519/00
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the γ-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.
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![Substituted furo[3,2-c]pyridines, thieno[3,2-c]pyridines, thieno[2,3-d]pyridazines and pyrido[3,4-d]pyridazines as phosphodiesterase type 10A inhibitors](/abs-image/US/2017/05/23/US09657034B2/abs.jpg.150x150.jpg)
公开(公告)号：US09657034B2
公开(公告)日：2017-05-23
申请号：US14997997
申请日：2016-01-18
发明人： Hervé Geneste , Michael Ochse , Karla Drescher , Sean Turner , Berthold Behl , Loic Laplanche , Jürgen Dinges , Clarissa Jakob , Lawrence Black , Katja Jantos
IPC分类号： A61K31/5025 , A61K31/4355 , A61K31/4365 , C07D487/04 , C07D491/048 , C07D495/04 , C07D519/00 , C07D401/14 , C07D401/06 , C07D471/04 , C07D417/14 , C07D413/14 , C07D405/14
CPC分类号： C07D519/00 , C07D401/06 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04
摘要： The present invention relates to novel compounds of the formula I which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders. wherein Q is O or S, X1 is N or CH, X2 is N or C—R7; X3 is O, S—X4═C(R8)—, where C(R8) is bound to the carbon atom which carries R2, or —X5═C(R9)—, where X5 is bound to the carbon atom which carries R2; X4 is N or C—R9; X5 is N; Het is selected from optionally substituted phenyl, monocyclic hetaryl and fused bicyclic hetaryl; R1 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkylsulfanyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, the moiety Y1-Cyc1; R2 is selected inter alia from hydrogen, halogen, OH, C1-C4-alkyl, trimethylsilyl, C1-C4-alkoxy-C1-C4-alkyl, C1-C4-alkoxy, C1-C4-alkoxy-C1-C4-alkoxy, C2-C4-alkenyloxy, etc; A represents one of the following groups A1, A2, A3, A4 or A5: where * indicates the points of attachment to Het and to the nitrogen atom, respectively; and where R3 to R9, R3e, R3f, A′, Y1 and Cyc1 are defined in the claims.
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9.发明申请PHENALKYLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM, AND THEIR USE IN THERAPY 有权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：US20140256701A1
公开(公告)日：2014-09-11
申请号：US14282712
申请日：2014-05-20
发明人： Frauke Pohlki , Udo Lange , Wilhelm Amberg , Michael Ochse , Berthold Behl , Wilfried Hornberger , Mario Mezler , Charles W. Hutchins , Sean Turner
IPC分类号： C07D403/12 , C07D231/18 , C07D401/12 , C07D295/135 , C07C311/05 , C07C311/06 , C07D233/84 , C07C311/10
CPC分类号： C07C311/06 , C07C311/04 , C07C311/05 , C07C311/10 , C07C2601/02 , C07C2601/04 , C07D205/04 , C07D207/08 , C07D207/267 , C07D231/18 , C07D233/42 , C07D233/84 , C07D295/135 , C07D401/12 , C07D403/12
摘要： The present invention relates to phenalkylamine derivatives of the formula (I) 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）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。
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