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![Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[e]azulene and crytalline forms thereof](/abs-image/US/2021/06/22/US11040977B2/abs.jpg.150x150.jpg)
公开(公告)号：US11040977B2
公开(公告)日：2021-06-22
申请号：US16291887
申请日：2019-03-04
发明人： Benno Rothenhaeusler , Rene Trussardi , Fabienne Hoffmann-Emery , Urs Schwitter , Jean-Michel Adam , Olaf Grassmann , Thomas Hartung , Frederic Ran , Ralph Diodone , Christophe Pfleger , Bjorn Bartels
IPC分类号： C07D487/04 , C07D243/14
摘要： The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
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![SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF](/abs-image/US/2019/06/27/US20190194210A1/abs.jpg.150x150.jpg)
公开(公告)号：US20190194210A1
公开(公告)日：2019-06-27
申请号：US16291887
申请日：2019-03-04
发明人： Benno Rothenhaeusler , Rene Trussardi , Fabienne Hoffmann-Emery , Urs Schwitter , Jean-Michel Adam , Olaf Grassmann , Thomas Hartung , Frederic Ran , Ralph Diodone , Christophe Pfleger , Bjorn Bartels
IPC分类号： C07D487/04 , C07D243/14
CPC分类号： C07D487/04 , C07B2200/13 , C07D243/14
摘要： The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
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公开(公告)号：US20160289718A1
公开(公告)日：2016-10-06
申请号：US15175779
申请日：2016-06-07
发明人： Rene Trussardi , Hans Iding
IPC分类号： C12P17/14 , C12P13/00 , C07D265/30 , C12P7/02
CPC分类号： C12P17/14 , C07D265/30 , C12P7/02 , C12P7/22 , C12P13/008 , Y02P20/55
摘要： The invention relates to a novel process for the preparation of chiral 2-(4-aminophenyl) morpholines of the formula wherein R1 is hydrogen an amino protecting group. The chiral 2-(4-aminophenyl) morpholines of the formula I are key intermediates for the preparation of compounds that have a good affinity to the trace amine associated receptors (TAARs).
摘要翻译： 式I的手性2-（4-氨基苯基）吗啉是制备与微量胺相关受体（TAAR）具有良好亲和力的化合物的关键中间体。
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公开(公告)号：US10597417B2
公开(公告)日：2020-03-24
申请号：US15890181
申请日：2018-02-06
发明人： Joerg Lill , Rene Trussardi
IPC分类号： C07H15/08 , C07H1/00 , C07H21/02 , A61K47/54 , C07C269/06 , C07C271/22 , C07C245/20 , C07C67/11 , C07C51/41 , C07C229/26
摘要： The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.
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![Synthesis of trans-8-chloro-5-methyl-1-[4-(pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10B-tetraaza-benzo[E]azulene and crytalline forms thereof](/abs-image/US/2019/04/02/US10246460B2/abs.jpg.150x150.jpg)
公开(公告)号：US10246460B2
公开(公告)日：2019-04-02
申请号：US15172542
申请日：2016-06-03
发明人： Benno Rothenhaeusler , Rene Trussardi , Fabienne Hoffmann-Emery , Urs Schwitter , Jean-Michel Adam , Olaf Grassmann , Thomas Hartung , Frederic Ran , Ralph Diodone , Christophe Pfleger , Bjorn Bartels
IPC分类号： C07D487/04 , C07D243/14
摘要： The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
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![SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF](/abs-image/US/2016/09/29/US20160280712A1/abs.jpg.150x150.jpg)
6.发明申请SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF 审中-公开反式-8-氯代-5-甲基-1- [4-（吡啶-2-基） - 苄氧基] -5,6-二氢-4H-2,3,5,10B-四氮杂 - 苯并[E] 其结构和结构形式公开(公告)号：US20160280712A1
公开(公告)日：2016-09-29
申请号：US15172542
申请日：2016-06-03
发明人： Benno Rothenhaeusler , Rene Trussardi , Fabienne Hoffmann-Emery , Urs Schwitter , Jean-Michel Adam , Olaf Grassmann , Thomas Hartung , Frederic Ran , Ralph Diodone , Christophe Pfleger , Bjorn Bartels
IPC分类号： C07D487/04 , C07D243/14
CPC分类号： C07D487/04 , C07B2200/13 , C07D243/14
摘要： The present invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
摘要翻译： 本发明提供了制备取代的1- [4-（吡啶-2-基氧基） - 环己基] -5,6-二氢-4H-2,3,5,10b-四氮杂 - 苯并[e]薁的方法。 还公开了可用作本发明方法中的中间体的化合物。
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公开(公告)号：US20230120311A1
公开(公告)日：2023-04-20
申请号：US17946743
申请日：2022-09-16
发明人： Kirsten Andrea Graeser , Urs Schwitter , Frank Stowasser , Florence Nicole Antoinette Tixeront , Rene Trussardi
IPC分类号： C07D413/12
摘要： Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the TAAR1 agonist 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the TAAR1 agonist, and methods of using the TAAR1 agonist, alone and in combination with other compounds, for treating diseases or conditions that are associated with TAAR1 activity.
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公开(公告)号：US20220127236A1
公开(公告)日：2022-04-28
申请号：US17571182
申请日：2022-01-07
发明人： Paul Spurr , Rene Trussardi
IPC分类号： C07D231/14
摘要： The invention provides a process for manufacturing 5-ethyl-4-methyl-N-[4-[(2S) morpholin-2-yl]phenyl]-1H-pyrazole-3-carboxamide (Formula I), or a pharmaceutically acceptable salt thereof, on an industrial scale, comprising a one-pot process for manufacturing 5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid (1).
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![SYNTHESIS OF TRANS-8-CHLORO-5-METHYL-1 -[4-(PYRIDIN-2-YLOXY)-CYCLOHEXYL]-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENE AND CRYTALLINE FORMS THEREOF](/abs-image/US/2021/09/16/US20210284648A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210284648A1
公开(公告)日：2021-09-16
申请号：US17337547
申请日：2021-06-03
发明人： Benno Rothenhaeusler , Rene Trussardi , Fabienne Hoffmann-Emery , Urs Schwitter , Jean-Michel Adam , Olaf Grassmann , Thomas Hartung , Frederic Ran , Ralph Diodone , Christophe Pfleger , Bjorn Bartels
IPC分类号： C07D487/04 , C07D243/14
摘要： The invention provides processes to manufacture substituted 1-[4-(Pyridin-2-yloxy)-cyclohexyl]-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes. Also disclosed are compounds useful as intermediates in the methods of the invention.
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公开(公告)号：US10337039B2
公开(公告)日：2019-07-02
申请号：US15175779
申请日：2016-06-07
发明人： Rene Trussardi , Hans Iding
IPC分类号： C12P7/02 , C12P7/22 , C12P13/00 , C12P17/14 , C07D265/30
摘要： The invention relates to a novel process for the preparation of chiral 2-(4-aminophenyl) morpholines of the formula wherein R1 is hydrogen an amino protecting group. The chiral 2-(4-aminophenyl) morpholines of the formula I are key intermediates for the preparation of compounds that have a good affinity to the trace amine associated receptors (TAARs).
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