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1. 发明授权

US10752618B2 Process for the preparation of pure and stable crystalline Raltegravir potassium form 3 有权
公开(公告)号：US10752618B2
公开(公告)日：2020-08-25
申请号：US16333613
申请日：2017-09-13
申请人： Lupin Limited
发明人： Purna Chandra Ray , Samir Shanteshwar Shabade , Surinder Kumar Arora , D. Rajput Lalitkumar , B. Shivdavkar Radhakrishna , G. Varade Shantanu , D. Ausekar Govind , Girij Pal Singh , Shreyas Pandurang Deshmukh , Gaurav Amrut Patil
IPC分类号： C07D413/12 , C07D498/12 , A61K31/513
摘要： The present invention provides improved, commercially viable and consistently reproducible processes for the preparation of pure and stable crystalline Raltegravir potassium Form 3 and pharmaceutical composition thereof.

2. 发明授权

US08969339B2 Compositions and methods for bone formation and modeling 有权
标题翻译：骨形成和建模的组成和方法
公开(公告)号：US08969339B2
公开(公告)日：2015-03-03
申请号：US13676630
申请日：2012-11-14
申请人： Enzo Biochem, Inc.
发明人： Dianqing (Dan) Wu , Dakai Liu , James J. Donegan
IPC分类号： A61K31/535 , C07D265/34 , C07D498/02 , C07D498/12 , C07D265/38 , A61K31/538 , C09B19/00
CPC分类号： A61K31/538 , C07D265/38 , C09B19/005
摘要： The present disclosure is directed to methods of identifying a compound that binds to or interacts with a protein receptor involved in bone formation. Specifically, the disclosure is directed to methods of identifying a compound that regulates a Wnt pathway in a cell by binding to or interacting with cavities in proteins such as LRP5, LRP 6 and/or frizzled receptor and interfering with receptor binding to other proteins in a Wnt pathway. The present disclosure is further directed to methods and compositions that comprise an identified compound for treating or preventing a disease in a mammal in which Wnt pathway suppression plays a role.
摘要翻译：本公开涉及鉴定与涉及骨形成的蛋白质受体结合或与之相互作用的化合物的方法。具体地，本公开涉及鉴定通过与蛋白质如LRP5，LRP6和/或卷曲受体中的空腔结合或与其相互作用来调节细胞中Wnt途径的化合物的方法，并干扰受体与其中的其它蛋白质的结合 Wnt途径。本公开进一步涉及包含用于治疗或预防Wnt途径抑制起作用的哺乳动物疾病的鉴定化合物的方法和组合物。

3. 发明授权

US08729065B2 Crystalline forms of a pharmaceutical compound 有权
标题翻译：药物化合物的结晶形式
公开(公告)号：US08729065B2
公开(公告)日：2014-05-20
申请号：US12983558
申请日：2011-01-03
申请人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
发明人： Michael Harold Rock , Heidi Lopez De Diego , Kim Lasse Christensen , Ole Nielsen , Anders Buur , Mark Howells
IPC分类号： A61P25/16 , A61K31/553 , C07D498/12
CPC分类号： C07H19/23 , C07D491/22
摘要： Described are crystalline forms of the pharmaceutical compound “[9S-(9α,10β,12α)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
摘要翻译：描述了药物化合物“[9S-（9α，10α，12α）] -5,16-双[（乙硫基）甲基] -2,3,9,10,11,12-六氢-10- 羟基-9-甲基-1-氧代-9,12-环氧基-1H-二吲哚并[1,2,3-fg：3'，2'，1'-k]吡咯并[3,4-i] 6]苯并二氮辛-10-羧酸甲酯“，以及它们的使用和制备方法。

4. 发明申请

US20100279364A1 CCI-779 derivatives and methods of making same 审中-公开
标题翻译： CCI-779衍生物及其制作方法
公开(公告)号：US20100279364A1
公开(公告)日：2010-11-04
申请号：US12001367
申请日：2007-12-11
申请人： Ping Cai , Mark Ruppen , Russ Tsao
发明人： Ping Cai , Mark Ruppen , Russ Tsao
IPC分类号： C12P17/18 , C07D498/12 , C07K16/00 , C07D405/06 , G01N33/00 , C12P17/16
CPC分类号： C07D405/06
摘要： A method of generating synthetic metabolites of CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples.
摘要翻译：提供了一种产生CCI-779合成代谢产物的方法。描述了五种新型CCI-779衍生物，以及使用这些衍生物检测样品中的CCI-779代谢物的方法。

5. 发明申请

US20100174064A1 FORMS OF RIFAXIMIN AND USES THEREOF 有权
标题翻译：形式的变体及其用途
公开(公告)号：US20100174064A1
公开(公告)日：2010-07-08
申请号：US12708836
申请日：2010-02-19
申请人： Karen S. Gushurst , Donglai Yang , Petinka Vlahova , Jeffrey S. Stults
发明人： Karen S. Gushurst , Donglai Yang , Petinka Vlahova , Jeffrey S. Stults
IPC分类号： C07D498/12
CPC分类号： C07D498/22 , C07D498/12
摘要： The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.
摘要翻译：本发明涉及利福昔明多晶型物，其用于药物制剂和使用它们的治疗方法。

6. 发明申请

US20090076263A1 ELIMINATION OF HETEROGENEOUS OR MIXED CELL POPULATION IN TUMORS 失效
标题翻译：消除肿瘤中异种或混合细胞群体
公开(公告)号：US20090076263A1
公开(公告)日：2009-03-19
申请号：US12186411
申请日：2008-08-05
申请人： Viktor S. Goldmakher , Robert J. Lutz , Ravi V.J. Chari , Yelena V. Kovtun , John M. Lambert , Rita Steeves , Hans K. Erickson
发明人： Viktor S. Goldmakher , Robert J. Lutz , Ravi V.J. Chari , Yelena V. Kovtun , John M. Lambert , Rita Steeves , Hans K. Erickson
IPC分类号： C07D498/12
CPC分类号： C07K16/3046 , A61K31/5383 , A61K31/58 , A61K47/6803 , A61K47/6849 , A61K2039/505 , C07D498/18 , C07K2317/24
摘要： Methods of killing or inhibiting tumors comprising of heterogeneous or mixed cell populations is described. The killing or inhibition of tumors is achieved by selectively targeting a unique ligand suspected of being expressed on a particular cell population to also kill a cell population lacking the unique ligand. These conjugates have therapeutic use as they are delivered to a specific cell population to kill these cells and the cytotoxic drug is released to kill non-targeted cells, thereby eliminating the tumor.
摘要翻译：描述了杀死或抑制包含异源或混合细胞群的肿瘤的方法。通过选择性地靶向疑似在特定细胞群体上表达的独特配体也杀死缺乏独特配体的细胞群体来实现肿瘤的杀伤或抑制。这些缀合物具有治疗用途，因为它们被递送到特定细胞群以杀死这些细胞，并释放细胞毒性药物以杀死非靶向细胞，从而消除肿瘤。

7. 发明申请

US20080287675A1 CASCADE SYSTEM 审中-公开
标题翻译： CASCADE系统
公开(公告)号：US20080287675A1
公开(公告)日：2008-11-20
申请号：US12120868
申请日：2008-05-15
申请人： Yao-En Li
发明人： Yao-En Li
IPC分类号： C07D498/12
CPC分类号： C07D498/18
摘要： A method of purifying an active pharmaceutical ingredient sufficient for administration into a human subject can include: obtaining a reaction product composition having the active pharmaceutical ingredient and impurities, wherein said active pharmaceutical ingredient is rapamycin or a rapamycin analog; introducing the reaction product composition into a first column of a chromatography system; directing a first portion of a first elutant from the first column to waste, said first portion having more impurity than active pharmaceutical ingredient; directing a second portion of the first elutant from the first column into a second column, said second portion having more active pharmaceutical ingredient than impurity; collecting factions of a second elutant from the second column that include the active pharmaceutical ingredient; and concentrating the said collected fractions to obtain a purity of the active pharmaceutical ingredient greater than 98% and with less than or about 0.95% being first and second major impurities.
摘要翻译：纯化足以施用于人受试者的活性药物成分的方法可以包括：获得具有活性药物成分和杂质的反应产物组合物，其中所述活性药物成分是雷帕霉素或雷帕霉素类似物; 将反应产物组合物引入色谱系统的第一列; 将来自第一塔的第一洗脱液的第一部分引导至废物，所述第一部分具有比活性药物成分更多的杂质; 将所述第一洗脱液的第二部分从所述第一塔引导到第二塔中，所述第二部分具有比杂质更多的活性药物成分; 从第二列收集包含活性药物成分的第二洗脱液的派系; 并浓缩所述收集的级分以获得大于98％且小于或约0.95％的活性药物成分的纯度为第一和第二主要杂质。

8. 发明申请

US20080071082A1 Heteroatoms-Containing Tricyclic Compounds 有权
标题翻译：含杂原子的三环化合物
公开(公告)号：US20080071082A1
公开(公告)日：2008-03-20
申请号：US11575757
申请日：2005-10-10
申请人： Maximilian Grassberger , Amarylla Horvath
发明人： Maximilian Grassberger , Amarylla Horvath
IPC分类号： C07D498/12
CPC分类号： C07D498/18 , C07H19/01 , Y02P20/55
摘要： A process for the production of 33-Epi-33-chloro-FR 520 in one step from FR520 wherein protecting groups are avoided.
摘要翻译：从FR520一步制备33-Epi-33-氯-FR 520的方法，其中避免了保护基团。

9. 发明申请

US20060189666A1 Novel gamma-secretase inhibitors 失效
标题翻译：新型γ-分泌酶抑制剂
公开(公告)号：US20060189666A1
公开(公告)日：2006-08-24
申请号：US10566486
申请日：2004-07-29
申请人： Michela Bettati , Amanda Boase , Ian Churcher , Tamara Ladduwahetty , Kevin Merchant , Abdul Quddus
发明人： Michela Bettati , Amanda Boase , Ian Churcher , Tamara Ladduwahetty , Kevin Merchant , Abdul Quddus
IPC分类号： A61K31/433 , C07D498/12
CPC分类号： C07D231/12 , C07D417/06
摘要： Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）的化合物：通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

10. 发明申请

US20040009976A1 Hypoglycemic imidazoline compounds 审中-公开
标题翻译：低血糖咪唑啉化合物
公开(公告)号：US20040009976A1
公开(公告)日：2004-01-15
申请号：US10135963
申请日：2002-04-30
发明人： Kumiko Takeuchi , Michael Robert Jirousek , Michael Paal , Gerd Ruhter , Theo Schotten
IPC分类号： A61K031/541 , A61K031/5377 , A61K031/496 , A61K031/4747 , C07D498/12 , C07D491/12 , C07D487/12
CPC分类号： C07D401/04 , C07D233/06 , C07D233/20 , C07D233/22 , C07D403/04 , C07D403/06 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/04 , C07D409/10 , C07D409/14
摘要： This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.
摘要翻译：本发明涉及某些新的咪唑啉化合物及其类似物，其用于治疗糖尿病，糖尿病并发症，代谢紊乱或其中存在葡萄糖处置受损的相关疾病，其包含它们的药物组合物及其制备方法。

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