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1. 发明申请

WO2023039063A1 SOLID FORM OF 5-(3,4-DICHLOROPHENYL)-N-((1R,2R)-2-HYDROXYCYCLOHEXYL)-6-(2,2,2-TRIFLUOROETHOXY)NICOTINAMIDE FOR USE IN TREATING KIDNEY DISEASES 审中-公开
公开(公告)号：WO2023039063A1
公开(公告)日：2023-03-16
申请号：PCT/US2022/042905
申请日：2022-09-08
申请人： RIVER 3 RENAL CORP. , F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： HONGYAN, He , SIYI, Jiang , SCHWITTER, Urs , DOTT, Pascal , DIODONE, Ralph , WHTTENBACH, Nicole , GRASSMANN, Olaf
IPC分类号： C07D213/82 , A61P13/12 , A61K31/465
摘要： The disclosure is in part directed to crystalline forms of 5-(3,4-dichlorophenyl)-N-((1R,2R)-2-hydroxycyclohexyl)-6-(2,2,2-trifluoroethoxy)nicotinamide and pharmaceutical compositions thereof.

3. 发明申请

WO2021185878A1 SALTS AND CRYSTALLINE FORMS OF A TAAR1 AGONIST 审中-公开
公开(公告)号：WO2021185878A1
公开(公告)日：2021-09-23
申请号：PCT/EP2021/056749
申请日：2021-03-17
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GRAESER, Kirsten Andrea , SCHWITTER, Urs , STOWASSER, Frank , TIXERONT, Florence Nicole Antoinette
IPC分类号： C07D413/12 , A61P25/24 , A61K31/5355
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.

4. 发明申请

WO2015082370A1 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
标题翻译：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：WO2015082370A1
公开(公告)日：2015-06-11
申请号：PCT/EP2014/076041
申请日：2014-12-01
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： ROTHENHAEUSLER, Benno , TRUSSARDI, René , HOFFMANN-EMERY, Fabienne , SCHWITTER, Urs , ADAM, Jean-Michel , GRASSMANN, Olaf , HARTUNG, Thomas , RAN, Frederic , DIODONE, Ralph , PFLEGER, Christophe , BARTELS, Bjoern
IPC分类号： C07D487/04 , A61K31/5517 , A61P25/00
CPC分类号： C07D487/04 , C07B2200/13 , C07D243/14
摘要： The present invention provides processes to manufacture substituted l-[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。

5. 发明申请

WO2014040936A1 SOLID FORMS OF (S)-2-METHOXY-3-{4-[2-(5-METHYL-2-PHENYL-OXAZOL-4-YL)-ETHOXY]-BENZO[B]THIOPHEN-7-YL}-PROPIONIC ACID AND OF SALTS THEREOF 审中-公开
标题翻译：（S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 氧杂-4-基） - 乙氧基] - 苯并[b]噻吩-7-基}}丙酸的固体形式酸及其盐
公开(公告)号：WO2014040936A1
公开(公告)日：2014-03-20
申请号：PCT/EP2013/068561
申请日：2013-09-09
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： DREIER, Lukas , EGLI, André , FAEHNRICH, Karsten , GRASSMANN, Olaf , MOHR, Peter , SCHWITTER, Urs , STAHR, Helmut , WYTTENBACH, Nicole
IPC分类号： C07D263/22 , A61K31/421
CPC分类号： A61K31/422 , C07D263/22
摘要： The present invention relates to solid forms of (S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl- oxazol-4-yl)-ethoxy]-benzo[b]thiophen-7-yl}-propionic acid, and of salts of (S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-oxazol-4-yl)-ethoxy]-benzo[b]thiophen-7-yl}- propionic acid.
摘要翻译：本发明涉及（S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 恶唑-4-基） - 乙氧基] - 苯并[b]噻吩-7 （S）-2-甲氧基-3- {4- [2-（5-甲基-2-苯基 - 恶唑-4-基） - 乙氧基] - 苯并[b] 噻吩-7-基} - 丙酸。

6. 发明申请

WO2020079203A1 NEW FORMS OF PYRIDO[1,2-A]PYRIMIDIN-4-ONE DERIVATIVES, ITS FORMULATION AND ITS PROCESS OF MAKING 审中-公开
公开(公告)号：WO2020079203A1
公开(公告)日：2020-04-23
申请号：PCT/EP2019/078313
申请日：2019-10-18
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： MEIER, Roland , SCHWITTER, Urs , DE PAEPE, Anne , KUEHL, Peter , THUN, Juergen , STOWASSER, Frank
IPC分类号： C07D519/00 , A61P21/00 , A61K31/519
摘要： The present invention relates to a process for the preparation of 7-(4,7-diazaspiro[2.5]octan-7-yl)-2-(2,8-dimethylimidazo[1,2-b]pyridazin-6-yl)pyrido[1,2-a]pyrimidin-4-one useful as pharmaceutically active compounds.

7. 发明申请

WO2018078129A1 PREPARING AND ANALYZING SOLID FORM PROPERTIES OF A SUBSTANCE 审中-公开
标题翻译：一种物质的固体形态的制备和分析
公开(公告)号：WO2018078129A1
公开(公告)日：2018-05-03
申请号：PCT/EP2017/077665
申请日：2017-10-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： SCHWITTER, Urs , RAN, Frédéric , ALKER, André , KISSLING, Tom , ZUMSTEIN, Thomas
IPC分类号： B01L3/00 , B01L3/06
摘要： In a method of analyzing solid form properties of a substance, which comprising the step of solidifying the substance, the solidified substance is obtained in one of a plurality of wells (1, 46) of a multi-well plate (4). In the multi-well plate (4) the at least one of the plurality of wells (1, 46) has a bottom (22) made of a thermoplastic polyimide. The method further comprises analyzing the solidified substance in the well (1, 46) of the multi-well plate (4) by X-ray diffraction. Thereby, said analysis comprises providing X-ray through the solidified substance and a bottom (22) of the well (1, 46) and evaluating the X-ray which passed the solidified substance and the bottom (22) of the well (1, 46). Such method and multi-well plate (4) provide a durable and cost efficient system allowing a high quality analysis of solid form properties of the substance and an efficient and safe processing of the substance.
摘要翻译：在分析包括固化物质的步骤的物质的固体形态性质的方法中，固化的物质在多级多孔体（1,46）中的一个中获得，（4）。在多孔板（4）中，多个井（1,46）中的至少一个具有由热塑性聚酰亚胺制成的底部（22）。该方法还包括通过X射线衍射分析多孔板（4）的孔（1,46）中的固化物质。因此，所述分析包括提供穿过固化物质和井（1,46）的底部（22）的X射线并且评估穿过固化物质和井（1，46）的底部（22）的X射线， 46）。这种方法和多孔板（4）提供了耐用且成本有效的系统，允许高质量地分析该物质的固体形式特性以及该物质的有效且安全的处理。

8. 发明申请

WO2015063001A1 CRYSTALLINE FORMS OF A PYRROLIDONE DERIVATIVE USEFUL IN THE TREATMENT OF ALZHEIMER'S DISEASE AND PREPARATION THEREOF 审中-公开
标题翻译：用于治疗阿尔茨海默病的吡咯烷酮衍生物的晶体形式及其制备
公开(公告)号：WO2015063001A1
公开(公告)日：2015-05-07
申请号：PCT/EP2014/072934
申请日：2014-10-27
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GRASSMANN, Olaf , HILDBRAND, Stefan , MEIER, Roland , SCALONE, Michelangelo , SCHWITTER, Urs , WIRZ, Beat , ZUTTER, Ulrich
IPC分类号： C07D207/273
CPC分类号： C07D207/273 , C07B2200/13 , C07C237/22
摘要： The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are polymorphic forms of said compound as well as compounds useful as intermediates in the methods of the invention.
摘要翻译：本发明提供了制备N - [（3S）-1- [4 - [（3-氟苯基）甲氧基]苯基] -5-氧代 - 吡咯烷-3-基]乙酰胺结晶的方法。还公开了所述化合物的多晶形式以及用作本发明方法中的中间体的化合物。

9. 发明申请

WO2018127526A3 SOLID FORMS OF [(1 S)-1 -[(2S,4R,5R)-5-(5-AMINO-2-OXO-THIAZOLO[4,5-D]PYRIMIDIN-3-YL)-4-HYDROXY-TE TRAHYDROFURAN-2-YL]PROPYL] ACETATE 审中-公开
公开(公告)号：WO2018127526A3
公开(公告)日：2018-07-12
申请号：PCT/EP2018/050160
申请日：2018-01-04
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GROSSE-SENDER, Katja , SCHWITTER, Urs , STOWASSER, Frank , WANG, Xuemei , XIONG, Jing
IPC分类号： C07D513/04 , A61K31/519 , A61P31/12
摘要： The present invention relates to novel solid forms of compound (I) [(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

10. 发明申请

WO2018127526A2 NEW SOLID FORMS OF [(1S)-1-[(2S,4R,5R)-5-(5-AMINO-2-OXO-THIAZOLO[4,5-D]PYRIMIDIN-3-YL)-4-HYDROXY-TETRAHYDROFURAN-2-YL]PROPYL] ACETATE 审中-公开
公开(公告)号：WO2018127526A2
公开(公告)日：2018-07-12
申请号：PCT/EP2018/050160
申请日：2018-01-04
申请人： F. HOFFMANN-LA ROCHE AG , HOFFMANN-LA ROCHE INC.
发明人： GROSSE-SENDER, Katja , SCHWITTER, Urs , STOWASSER, Frank , WANG, Xuemei , XIONG, Jing
IPC分类号： C07D513/04 , A61K31/519 , A61P31/12
摘要： The present invention relates to novel solid forms of compound (I) [(1S)-1-[(2S,4R,5R)-5-(5-amino-2-oxo-thiazolo[4,5-d]pyrimidin-3-yl)-4-hydroxy-tetrahydrofuran-2-yl]propyl] acetate and pharmaceutical compositions comprising the solid forms thereof disclosed herein, which may be used as a TLR7 agonist, or for the treatment or prophylaxis of a viral disease in a patient relating to HBV infection or a disease caused by HBV infection.

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