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1. 发明授权

US08003672B2 CB-1 receptor modulator formulations 失效
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US08003672B2
公开(公告)日：2011-08-23
申请号：US12386402
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/44
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/2027 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文所述是大麻逆反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

2. 发明申请

US20090264436A1 CB-1 receptor modulator formulations 失效
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US20090264436A1
公开(公告)日：2009-10-22
申请号：US12386402
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/4985 , A61K31/44
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/2027 , A61K31/4985 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文所述是大麻逆反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

3. 发明申请

US20090264476A1 CB-1 receptor modulator formulations 审中-公开
标题翻译： CB-1受体调节剂制剂
公开(公告)号：US20090264476A1
公开(公告)日：2009-10-22
申请号：US12386403
申请日：2009-04-17
申请人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
发明人： Craig McKelvey , Sarah Geers , Justin Moser , Bhagwant Rege , Dina Zhang , Sutthilug Sotthivirat
IPC分类号： A61K31/44 , A61K31/4985 , A61P3/04
CPC分类号： A61K31/44 , A61K9/1635 , A61K9/1652 , A61K9/1694 , A61K9/2077 , A61K9/2095 , A61K31/4412 , A61K45/06 , A61K2300/00
摘要： Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabinoid inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
摘要翻译：本文描述的是大麻素受体反向激动剂如塔拉班班特的固体，稳定的药物制剂，以及制备这些制剂的方法。另外，本文描述的是大麻素反向激动剂如塔拉班班特和另外的治疗剂的固体稳定药物制剂，以及制备这种药物制剂的方法。

4. 发明申请

US20120059011A1 PHARMACEUTICAL COMPOSITIONS OF COMBINATIONS OF DIPEPTIDYL PEPTIDASE-4 INHIBITORS WITH PIOGLITAZONE 审中-公开
标题翻译： DIPEPTIDYL PEPTIDASE-4抑制剂与PIOGLITAZONE的组合药物组合物
公开(公告)号：US20120059011A1
公开(公告)日：2012-03-08
申请号：US13319718
申请日：2010-06-04
申请人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
发明人： Nicholas Birringer , Christopher T. John , Adam Procopio , Bhagwant Rege , Lawrence A. Rosen , Sutthilug Sotthivirat , Wei Xu
IPC分类号： A61K31/4439 , A61K31/513 , A61P3/10 , A61K31/4985
CPC分类号： A61K45/06 , A61K31/44 , A61K31/4439 , A61K2300/00
摘要： This invention relates to pharmaceutical compositions comprising fixed-dose combinations of a dipeptidyl peptidase-4 inhibitor and pioglitazone, methods of preparing such pharmaceutical compositions, and methods of treating Type 2 diabetes with such pharmaceutical compositions.
摘要翻译：本发明涉及包含二肽基肽酶-4抑制剂和吡格列酮的固定剂量组合的药物组合物，制备这种药物组合物的方法，以及用这种药物组合物治疗2型糖尿病的方法。

5. 发明申请

US20120213851A1 SOLID PHARMACEUTICAL COMPOSITIONS CONTAINING AN INTEGRASE INHIBITOR 有权
标题翻译：含有集成抑制剂的固体药物组合物
公开(公告)号：US20120213851A1
公开(公告)日：2012-08-23
申请号：US13503939
申请日：2010-10-21
申请人： Majid Mahjour , Feng Li , Decheng Ma , Sutthilug Sotthivirat
发明人： Majid Mahjour , Feng Li , Decheng Ma , Sutthilug Sotthivirat
IPC分类号： A61K9/20 , A61P31/18 , A61K31/506
CPC分类号： A61K31/513 , A61K9/2009 , A61K9/2013 , A61K9/2054 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.
摘要翻译：描述了含有药学上可接受的盐形式的raltegravir的口服给药片剂。片剂包括：（A）颗粒内组分，其包含（i）有效量的拉尔维那韦的碱金属盐，（ii）任选的第一超级崩解剂，和（iii）粘合剂; 和（B）颗粒外组分，其包含（i）第二超级崩解剂，（ii）填料和（iii）润滑剂。制备片剂的方法和片剂的使用，任选地与其它抗HIV剂组合用于抑制HIV整合酶，用于治疗或预防HIV感染或治疗，延缓发作或预防的艾滋病也被描述。

6. 发明申请

US20210330660A1 FORMULATIONS FOR CGRP RECEPTOR ANTAGONISTS 有权
公开(公告)号：US20210330660A1
公开(公告)日：2021-10-28
申请号：US17114169
申请日：2020-12-07
申请人： Majid Mahjour , Leonardo R. Allain , Sutthilug Sotthivirat , Russell G. Maus , Rebecca Nofsinger , Lisa Lupton , Wei Xu , Francis Flanagan
发明人： Majid Mahjour , Leonardo R. Allain , Sutthilug Sotthivirat , Russell G. Maus , Rebecca Nofsinger , Lisa Lupton , Wei Xu , Francis Flanagan
IPC分类号： A61K31/4545 , A61K47/10 , A61K9/08
摘要： The instant invention relates to liquid pharmaceutical compositions containing CGRP receptor antagonists. The CGRP receptor antagonist liquid pharmaceutical compositions of the instant invention are alcohol-free, low volume liquid pharmaceutical compositions that can be taken without water for the treatment of migraine headache.

7. 发明申请

US20210361663A1 Formulations of Antiviral Compounds 有权
公开(公告)号：US20210361663A1
公开(公告)日：2021-11-25
申请号：US17286620
申请日：2019-10-21
申请人： Sutthilug SOTTHIVIRAT , Joyce STELLABOTT , Walter R. WASYLASCHUK , Merck Sharp & Dohme Corp.
发明人： Sutthilug Sotthivirat , Joyce Stellabott , Walter R. Wasylaschuk
IPC分类号： A61K31/5365 , A61K9/20
摘要： The present disclosure is directed to pharmaceutical formulations comprising an amorphous inhibitor of hepatitis C vims NS5A. These pharmaceutical formulations may be prepared by roller-compaction or wet-granulation methods. The present disclosure is also directed to oral dosage forms, such as tablets, comprising such pharmaceutical formulations.

8. 发明授权

US09649311B2 Solid pharmaceutical compositions containing an integrase inhibitor 有权
公开(公告)号：US09649311B2
公开(公告)日：2017-05-16
申请号：US13503939
申请日：2010-10-21
申请人： Majid Mahjour , Feng Li , Decheng Ma , Sutthilug Sotthivirat
发明人： Majid Mahjour , Feng Li , Decheng Ma , Sutthilug Sotthivirat
IPC分类号： A61K9/20 , A61K31/506 , A61P31/18 , A61K31/513 , A61K45/06 , A61K9/24
CPC分类号： A61K31/513 , A61K9/2009 , A61K9/2013 , A61K9/2054 , A61K9/2077 , A61K9/209 , A61K9/2095 , A61K31/506 , A61K45/06 , A61K2300/00
摘要： Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.

9. 发明申请

US20130023462A1 LYOPHILIZED ANTI-FUNGAL COMPOSITIONS 有权
标题翻译： LYOPHILISO抗真菌组合物
公开(公告)号：US20130023462A1
公开(公告)日：2013-01-24
申请号：US13628592
申请日：2012-09-27
申请人： Sachin Mittal , Hossain Jahansouz , Sutthilug Sotthivirat
发明人： Sachin Mittal , Hossain Jahansouz , Sutthilug Sotthivirat
IPC分类号： A61K38/12 , A61P31/10
CPC分类号： A61K38/12 , A61K9/0019 , A61K9/19 , A61K47/12 , A61K47/26
摘要： A lyophilized anti-fungal composition comprises (A) caspofungin, or a pharmaceutically acceptable salt thereof, in an effective amount; (B) one or more non-reducing sugars having a glass transition temperature Tg(s) of at least about 90° C.; and (C) an acetate buffer in an amount effective to provide a pH in a range of from about 5 to about 7; wherein the weight ratio of the one or more non-reducing sugars to caspofungin is in a range of from about 1.1:1 to about 10:1; the composition has a moisture content of about 0.8 wt. % or less; and the composition has a glass transition temperature Tg(c) of at least about 55° C. The lyophilized composition has good storage stability at temperatures up to and including room temperature. The composition can be reconstituted for use in preventing or treating fungal infections.
摘要翻译：冻干的抗真菌组合物包含有效量的（A）卡泊芬净或其药学上可接受的盐; （B）玻璃化转变温度Tg（s）至少约90℃的一种或多种非还原糖; 和（C）有效提供约5至约7范围内的pH的乙酸盐缓冲液; 其中所述一种或多种非还原性糖与卡泊芬净的重量比在约1.1:1至约10:1的范围内; 该组合物的水分含量为约0.8wt。％或更少; 并且所述组合物的玻璃化转变温度Tg（c）为至少约55℃。所述冻干组合物在高达并且包括室温的温度下具有良好的储存稳定性。该组合物可以重构用于预防或治疗真菌感染。

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