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1. 发明申请

WO2022269008A1 CRYSTALLINE FORM OF SOTORASIB 审中-公开
公开(公告)号：WO2022269008A1
公开(公告)日：2022-12-29
申请号：PCT/EP2022/067276
申请日：2022-06-23
申请人： SANDOZ AG
发明人： ADAMER, Verena , MARGREITER, Renate , PICHLER, Arthur
IPC分类号： C07D471/04 , A61P35/00 , A61K31/519
摘要： The present invention relates to a crystalline form of sotorasib and to a process for its preparation. Furthermore, the invention relates to a pharmaceutical composition comprising the crystalline form of sotorasib of the present invention and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment of a cancer with a KRAS mutation.

2. 发明申请

WO2017025526A1 FORM C OF AVIBACTAM SODIUM 审中-公开
标题翻译：甲基磺酸钠
公开(公告)号：WO2017025526A1
公开(公告)日：2017-02-16
申请号：PCT/EP2016/068925
申请日：2016-08-09
申请人： SANDOZ AG
发明人： HOTTER, Andreas , ADAMER, Verena , LENGAUER, Hannes
IPC分类号： C07D471/04 , A01N43/90
CPC分类号： A61K31/551 , A61P31/04 , B01D9/0054 , C07D471/04
摘要： The present invention relates to crystalline form C of avibactam sodium and to a process for its preparation. The invention also concerns a pharmaceutical composition comprising form C and one or more antibacterial agents, wherein at least one antibacterial agent is a beta-lactam antibiotic. The pharmaceutical composition of the present invention can be used as medicament, in particular for treatment and/or prevention of bacterial infections.
摘要翻译：本发明涉及阿维菌素钠的结晶形式C及其制备方法。本发明还涉及包含C型和一种或多种抗菌剂的药物组合物，其中至少一种抗菌剂是β-内酰胺抗生素。本发明的药物组合物可以用作药物，特别是用于治疗和/或预防细菌感染。

3. 发明申请

WO2013153162A1 POLYMORPH OF RILPIVIRINE HYDROCHLORIDE 审中-公开
标题翻译：吡咯烷酮氢氯化物的聚合物
公开(公告)号：WO2013153162A1
公开(公告)日：2013-10-17
申请号：PCT/EP2013/057597
申请日：2013-04-11
申请人： SANDOZ AG
发明人： HOTTER, Andreas , PICHLER, Arthur , ADAMER, Verena , GRIESSER, Ulrich
IPC分类号： C07D239/48 , A61K31/505 , A61P31/18
CPC分类号： C07D239/48
摘要： The present invention relates to a novel polymorph and to a novel methanol solvate of rilpivirine hydrochloride, as well as to their preparation. The novel methanol solvate is a valuable intermediate for the preparation of the novel polymorph of rilpivirine hydrochloride of the present invention. Moreover the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and additional therapeutic agents.
摘要翻译：本发明涉及一种新型多晶型物和一种新型盐酸雷非司他甲醇溶剂化物及其制备方法。新型甲醇溶剂化物是制备本发明盐酸利乐结济新型多晶型物的有价值的中间体。此外，本发明涉及新型多晶型物在制备药物中的用途。此外，本发明涉及包含有效量的盐酸利乐普林新型多晶型物的药物组合物及其制备方法。最后，本发明涉及药物组合，其包含有效量的盐酸利乐瑞林的新型多晶型物和另外的治疗剂。

4. 发明申请

WO2016097314A1 AMORPHOUS AND CRYSTALLINE FORMS OF IDELALISIB AND PROCESS FOR FORMING THE SAME 审中-公开
标题翻译：非晶形态和晶体形态及其形成过程
公开(公告)号：WO2016097314A1
公开(公告)日：2016-06-23
申请号：PCT/EP2015/080537
申请日：2015-12-18
申请人： SANDOZ AG
发明人： RICHTER, Frank , ADAMER, Verena
IPC分类号： C07D473/34 , A61K31/52
CPC分类号： C07D473/34
摘要： The present invention concerns pure and stable amorphous idelalisib, crystalline solvates of idelalisib and a process for the formation of pure and stable amorphous idelalisib using the crystalline solvates of idelalisib.
摘要翻译：本发明涉及纯的和稳定的无定形无底物，伊曲利氏菌素的结晶溶剂合物以及使用伊曲利布的结晶溶剂合物形成纯的和稳定的无定形伊曲利布的方法。

5. 发明申请

WO2015158910A2 SOLID DISPERSION COMPRISING AN OREXIN RECEPTOR ANTAGONIST 审中-公开
标题翻译：包含OREXIN受体拮抗剂的固体分散体
公开(公告)号：WO2015158910A2
公开(公告)日：2015-10-22
申请号：PCT/EP2015/058426
申请日：2015-04-17
申请人： SANDOZ AG
发明人： ADAMER, Verena , KREKELER, Andreas , SEDLMAYR, Michael
IPC分类号： C07D413/14
CPC分类号： A61K9/2022 , A61K9/2009 , A61K31/551 , C07D413/14
摘要： A solid dispersion comprising suvorexant or a salt thereof in amorphous form and at least one pharmaceutically acceptable matrix compound, wherein the matrix compound is (i) a polymer and wherein the solid dispersion contains the suvorexant or salt thereof in an 5 amount of at least 50 weight-% based on the combined weight of the suvorexant or salt thereof and the at least one matrix compound, or (ii) a silicon-based inorganic adsorbent.
摘要翻译：一种固体分散体，其包含无定形形式的磺维生素或其盐和至少一种药学上可接受的基质化合物，其中所述基质化合物是（i）聚合物，并且其中所述固体分散体含有5重量至少为50 基于所述suvorex或其盐和所述至少一种基质化合物的组合重量的重量％，或（ii）硅类无机吸附剂。

6. 发明申请

WO2013153161A2 NOVEL POLYMORPH OF RILPIVIRINE HYDROCHLORIDE 审中-公开
标题翻译：吡咯烷酮氯化氢的新型聚合物
公开(公告)号：WO2013153161A2
公开(公告)日：2013-10-17
申请号：PCT/EP2013/057596
申请日：2013-04-11
申请人： SANDOZ AG
发明人： HOTTER, Andreas , PICHLER, Arthur , ADAMER, Verena , GRIESSER, Ulrich
IPC分类号： C07D239/48
CPC分类号： C07D239/48
摘要： The present invention relates to a novel polymorph and to novel solvates of rilpivirine hydrochloride, as well as to their preparation. The novel solvates are valuable intermediates for the preparation of the novel polymorph of rilpivirine hydrochloride of the present invention. Moreover the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel polymorph of rilpivirine hydrochloride and additional therapeutic agents.
摘要翻译：本发明涉及一种新型多晶型物和盐酸利乐普林的新型溶剂合物及其制备方法。新型溶剂合物是制备本发明的盐酸利乐结济新型多晶型物的有价值的中间体。此外，本发明涉及新型多晶型物在制备药物中的用途。此外，本发明涉及包含有效量的盐酸利乐普林新型多晶型物的药物组合物及其制备方法。最后，本发明涉及药物组合，其包含有效量的盐酸利乐瑞林的新型多晶型物和另外的治疗剂。

7. 发明申请

WO2021001457A1 CRYSTALLINE (R)-2-AMINO-3-PHENYLPROPYLCARBAMATE ACID ADDITION SALTS 审中-公开
公开(公告)号：WO2021001457A1
公开(公告)日：2021-01-07
申请号：PCT/EP2020/068588
申请日：2020-07-01
申请人： SANDOZ AG
发明人： ADAMER, Verena , THALER, Andrea
IPC分类号： A61P25/00 , C07C271/12 , C07C309/29 , C07C233/82 , C07C53/02 , C07C55/02 , C07C57/145 , A61K31/27 , C07C59/245 , C07C59/255 , C07C233/83 , C07C309/30
摘要： The present invention relates to crystalline salt forms of ( R )-2-amino-3-phenylpropylcarbamate and a process for their preparation. The invention also relates to a pharmaceutical composition comprising one or more of the crystalline salt forms of ( R )-2-amino-3-phenylpropylcarbamate, preferably in a predetermined and/or effective amount and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used for the treatment of various CNS disorders, in particular in the improvement of wakefulness and reduction of excessive sleepiness in patients with narcolepsy or obstructive sleep apnea.

8. 发明申请

WO2020239759A1 AMORPHOUS ENASIDENIB IN A STABILIZED FORM 审中-公开
公开(公告)号：WO2020239759A1
公开(公告)日：2020-12-03
申请号：PCT/EP2020/064563
申请日：2020-05-26
申请人： SANDOZ AG
发明人： ADAMER, Verena , THALER, Andrea , SCHWARZ, Franz , PICHLER, Arthur
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K31/53 , A61P35/02
摘要： The invention relates to an adsorbate comprising amorphous enasidenib mesylate and a solid carrier, wherein the amorphous enasidenib mesylate is preferably present in the carrier in the form of a solid dispersion. The invention also relates to a method of preparing said adsorbate comprising amorphous enasidenib mesylate and a solid carrier. Further, the invention relates to a pharmaceutical formulation and a method for preparing a tablet, wherein both the pharmaceutical formulation and the tablet contain the adsorbate of the present invention.

9. 发明申请

WO2020108941A1 MULTI-COMPONENT CRYSTALS OF AN ORALLY AVAILABLE HIF PROLYL HYDROXYLASE INHIBITOR 审中-公开
公开(公告)号：WO2020108941A1
公开(公告)日：2020-06-04
申请号：PCT/EP2019/080511
申请日：2019-11-07
申请人： SANDOZ AG
发明人： ADAMER, Verena , THALER, Andrea , SCHREINER, Erwin
IPC分类号： C07D213/81 , C07D207/16 , A61P7/06 , A61K31/44
摘要： The present invention relates to crystalline compounds comprising vadadustat and L -proline and processes for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising one or more of the crystalline compounds of the present invention and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment and/or prevention of anemia for example in patients with end-stage renal disease (ESRD) and/or chronic kidney disease (CKD).

10. 发明申请

WO2011161245A2 POLYMORPHS OF AN ACTIVE PHARMACEUTICAL INGREDIENT 审中-公开
标题翻译：活性药物成分的多重性
公开(公告)号：WO2011161245A2
公开(公告)日：2011-12-29
申请号：PCT/EP2011/060630
申请日：2011-06-24
申请人： SANDOZ AG , HOTTER, Andreas , GRIESSER, Ulrich , ADAMER, Verena , LANGES, Christoph
发明人： HOTTER, Andreas , GRIESSER, Ulrich , ADAMER, Verena , LANGES, Christoph
IPC分类号： C07D277/56 , A61K31/425 , A61P19/06
CPC分类号： C07D277/56
摘要： The present invention relates to crystalline form I of Febuxostat as well as to pharmaceutical compositions comprising crystalline form I as an active pharmaceutical ingredient. Furthermore the present invention relates to a further polymorphic form of Febuxostat designated as form II and to a novel solvate of Febuxostat. The present invention also relates to methods of making crystalline form I, form II and the novel solvate of Febuxostat.
摘要翻译：本发明涉及非索非斯坦的结晶形式I以及包含结晶形式I作为活性药物成分的药物组合物。此外，本发明还涉及另一种指定为II型的异丙酚钠的多晶型物，还涉及一种新颖的非索非司他溶剂合物。本发明还涉及制备结晶形式I，形式II和新戊酸钠的新型溶剂合物的方法。

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