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11.发明申请公开(公告)号：US20190290632A1
公开(公告)日：2019-09-26
申请号：US16276144
申请日：2019-02-14
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： A61K31/454 , C07D405/14 , C07D403/10 , A61K31/4192 , A61K31/4178 , A61K31/4025 , C07D403/12 , C07D403/14 , C07D207/273 , C07D205/04 , C07D401/12 , C07D233/42 , A61K31/397
摘要： The present invention relates to aminotetraline and aminoindane derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminotetraline and aminoindane derivatives, and the use of such aminotetraline and aminoindane derivatives for therapeutic purposes. The aminotetraline and aminoindane derivatives are GlyT1 inhibitors.
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公开(公告)号：US10280159B2
公开(公告)日：2019-05-07
申请号：US15388516
申请日：2016-12-22
发明人： Wilhelm Amberg , Udo Lange , Herve Geneste , Michael Ochse , Ralf Biesinger , Frank Oellien
IPC分类号： C07D413/12 , C07D205/04 , C07C229/48 , C07C229/46 , C07D211/62 , C07D261/12 , C07D209/52 , C07D207/16 , C07D207/08 , C07D265/36 , C07C59/72 , C07D405/04 , C07D311/04 , C07D405/14 , C07D311/58 , C07C229/30 , C07C229/36 , C07C229/50 , C07D207/06 , C07D265/38 , C07D209/94 , C07D211/32
摘要： The invention relates to (hetero)cyclic 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：US20170173009A1
公开(公告)日：2017-06-22
申请号：US15449565
申请日：2017-03-03
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： A61K31/501 , A61K31/4433 , A61K31/4155 , A61K31/4192 , A61K31/4178 , A61K31/397
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
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14.发明申请GUANIDINE COMPOUNDS AND USE THEREOF AS BINDING PARTNERS FOR 5-HT5 RECEPTORS 审中-公开胍基化合物及其作为5-HT5受体的结合合作伙伴使用公开(公告)号：US20170037016A1
公开(公告)日：2017-02-09
申请号：US15332744
申请日：2016-10-24
发明人： Astrid Netz , Wilhelm Amberg , Udo Lange , Michael Ochse , Charles W. Hutchins , Francisco-Xavier Garcia-Ladona , Wolfgang Wernet , Andreas Kling
IPC分类号： C07D277/48 , C07D277/82 , C07D333/36 , C07D417/04 , C07D235/30 , C07D513/04 , C07D263/48 , C07D417/12 , C07D277/60
CPC分类号： C07D277/48 , C07D231/56 , C07D235/30 , C07D237/22 , C07D249/14 , C07D261/14 , C07D263/28 , C07D263/48 , C07D277/60 , C07D277/82 , C07D285/08 , C07D285/135 , C07D333/36 , C07D417/04 , C07D417/12 , C07D513/04
摘要： The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.
摘要翻译： 相应的对映异构体，非对映异构体和/或互变异构形式以及其药学上可接受的盐。 本发明化合物还涉及胍化合物作为5-HT 5受体的结合伴侣的用途，用于治疗由5-HT 5受体活性调节的疾病，特别是用于治疗神经变性和神经精神障碍以及相关的 体征，症状和功能障碍。
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15.发明授权4,5-dihydropyrazole derivatives, pharmaceutical compositions containing them, and their use in therapy 有权4,5-二氢吡唑衍生物，含有它们的药物组合物及其在治疗中的用途公开(公告)号：US09550754B2
公开(公告)日：2017-01-24
申请号：US14849470
申请日：2015-09-09
发明人： Wilhelm Amberg , Jason Brewer , Charles Hutchins , Udo Lange , Yanbin Lao , Huan-Qiu Li , Frauke Pohlki , Anil Vasudevan , Ying Wang , Hongyu Zhao
IPC分类号： C07D403/12 , C07D401/14
CPC分类号： C07D403/12 , C07D401/14
摘要： The present invention relates to 4,5-dihydropyrazole derivatives of the formula (I) and physiologically tolerated salts thereof which are GlyT1 inhibitors. The invention further relates to pharmaceutical compositions comprising such 4,5-dihydropyrazole derivatives, and the use of such 4,5-dihydropyrazole derivatives for therapeutic purposes.
摘要翻译： 本发明涉及式（I）的4,5-二氢吡唑衍生物及其生理学上耐受的盐，它们是GlyT1抑制剂。 本发明还涉及包含这种4,5-二氢吡唑衍生物的药物组合物，以及这些用于治疗目的的这种4,5-二氢吡唑衍生物的用途。
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16.发明授权Isoindoline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权异二氢吲哚衍生物，含有它们的药物组合物及其在治疗中的应用公开(公告)号：US09365512B2
公开(公告)日：2016-06-14
申请号：US13764454
申请日：2013-02-11
发明人： Wilhelm Amberg , Udo Lange , Michael Ochse , Frauke Pohlki , Charles W. Hutchins , Irini Zanze , Hongyu H. Zhao , Huan-Qiu Li , Ying X. Wang
IPC分类号： C07D403/12 , C07D209/46 , C07D405/14 , C07D209/44
CPC分类号： C07D209/46 , C07D209/44 , C07D403/12 , C07D405/14
摘要： The present invention relates to isoindoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such isoindoline derivatives, and the use of such isoindoline derivatives for therapeutic purposes.
摘要翻译： 本发明涉及式（I）的异二氢吲哚衍生物或其生理上耐受的盐。 本发明还涉及包含这种异二氢吲哚衍生物的药物组合物，以及用于治疗目的的这种异吲哚啉衍生物的用途。
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17.发明申请BENZENESULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 审中-公开适用于治疗多巴胺D3受体调节障碍的苯并呋喃半导体化合物公开(公告)号：US20150175570A1
公开(公告)日：2015-06-25
申请号：US14553923
申请日：2014-11-25
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： C07D401/04
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。
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18.发明申请Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权氨基荧光素，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物，含有它们的药物组合物及其在治疗中的用途公开(公告)号：US20150111867A1
公开(公告)日：2015-04-23
申请号：US14517034
申请日：2014-10-17
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： C07D405/14 , C07D405/04
CPC分类号： A61K31/501 , A61K31/397 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4433 , C07D311/58 , C07D405/04 , C07D405/14
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereofThe invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquin oline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
摘要翻译： 本发明涉及式（I）的氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2,3,4-四氢喹啉衍生物或其生理上可耐受的盐。本发明涉及包含这种氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2 ，3,4-四氢喹啉衍生物，以及用于治疗目的的这种氨基苯并二氢吡喃，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物的用途。 氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2,3,4-四氢喹啉衍生物是GlyT1抑制剂。
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公开(公告)号：US20190290645A1
公开(公告)日：2019-09-26
申请号：US16275938
申请日：2019-02-14
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： A61K31/501 , A61K31/4433 , A61K31/4192 , A61K31/4178 , C07D405/04 , A61K31/397 , C07D311/58 , C07D405/14 , A61K31/4155
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof.The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
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20.发明授权Aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, pharmaceutical compositions containing them, and their use in therapy 有权氨基荧光素，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物，含有它们的药物组合物及其在治疗中的用途公开(公告)号：US09586945B2
公开(公告)日：2017-03-07
申请号：US14517034
申请日：2014-10-17
发明人： Wilhelm Amberg , Frauke Pohlki , Udo Lange , Ying Wang , Jason Brewer , Anil Vasudevan , Yanbin Lao , Charles Hutchins , Hongyu Zhao , Huan-Qiu Li
IPC分类号： C07D405/04 , C07D405/14 , C07D311/58 , A61K31/352
CPC分类号： A61K31/501 , A61K31/397 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4433 , C07D311/58 , C07D405/04 , C07D405/14
摘要： The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.
摘要翻译： 本发明涉及包含这种氨基苯并二氢吡喃，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物的药物组合物，以及用于治疗目的的这种氨基苯并二氢吡喃，氨基硫辛烷和氨基-1,2,3,4-四氢喹啉衍生物的用途。 氨基苯并二氢吡喃，氨基硫色烷和氨基-1,2,3,4-四氢喹啉衍生物是GlyT1抑制剂。
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