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1. 发明授权

US08518935B2 Amorphous besifloxacin solid 失效
标题翻译：无定形塞米沙星固体
公开(公告)号：US08518935B2
公开(公告)日：2013-08-27
申请号：US12956009
申请日：2010-11-30
申请人： Mohannad Shawer , Eric Phillips , Harry M. King, Jr.
发明人： Mohannad Shawer , Eric Phillips , Harry M. King, Jr.
IPC分类号： A61K31/55 , A61P31/04 , C07D401/04
CPC分类号： C07D401/04 , C07D223/12
摘要： Amorphous solid-state form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid is characterized by at least one of: (a) an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 6.9-7.1, 9.4, 10.6-10.7, and 13.4-13.7°±0.2°, and a diffuse halo pattern at 11-30°; and (b) a DSC (differential scanning calorimetry) melting peak at about 267-272° C. The amorphous solid is prepared by rapid precipitation from a saturated or supersaturated solution of besifloxacin free base in a solvent comprising at least benzyl alcohol.
摘要翻译：（R） - （+） - 7-（3-氨基-2,3,4,5,6,7-六氢-1H-吖庚因-1-基）-1,4-二氢 - 4-氧代喹啉-3-羧酸的特征在于以下至少一个：（a）X射线粉末衍射（“XRPD”）谱，其包括在2θ角为6.9-7.1,9.4,10.6-10.7和13.4的峰 -13.7°±0.2°，扩散晕图案在11-30°; 在约267-272℃下的DSC（差示扫描量热法）熔融峰。（b）在约267-272℃下的DSC（差示扫描量热法）熔融峰。通过在至少含有苄醇的溶剂中从饱和或过饱和的贝沙沙星游离碱溶液快速沉淀制备无定形固体。

2. 发明申请

US20110144329A1 Amorphous Besifloxacin Solid 失效
标题翻译：无定形贝西沙星固体
公开(公告)号：US20110144329A1
公开(公告)日：2011-06-16
申请号：US12956009
申请日：2010-11-30
申请人： Mohannad Shawer , Eric Phillips , Harry M. King, JR.
发明人： Mohannad Shawer , Eric Phillips , Harry M. King, JR.
IPC分类号： C07D223/12
CPC分类号： C07D401/04 , C07D223/12
摘要： Amorphous solid-state form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid is characterized by at least one of: (a) an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 6.9-7.1, 9.4, 10.6-10.7, and 13.4-13.7°±0.2°, and a diffuse halo pattern at 11-30°; and (b) a DSC (differential scanning calorimetry) melting peak at about 267-272° C. The amorphous solid is prepared by rapid precipitation from a saturated or supersaturated solution of besifloxacin free base in a solvent comprising at least benzyl alcohol.
摘要翻译：（R） - （+） - 7-（3-氨基-2,3,4,5,6,7-六氢-1H-吖庚因-1-基）-1,4-二氢 - 4-氧代喹啉-3-羧酸的特征在于以下中的至少一种：（a）包含在2θ处的峰的X射线粉末衍射（“XRPD”）光谱; 角度为6.9-7.1,9.4,10.6-10.7和13.4-13.7°±0.2°，扩散晕图案为11-30°; 在约267-272℃下的DSC（差示扫描量热法）熔融峰。（b）在约267-272℃下的DSC（差示扫描量热法）熔融峰。通过在至少含有苄醇的溶剂中从饱和或过饱和的贝沙沙星游离碱溶液快速沉淀制备无定形固体。

3. 发明申请

US20110237605A1 Molecular Crystal of (4-(1,8-Naphthyridin-2-YL)Piperidin-1-YL)Pyrimidine Derivative 审中-公开
标题翻译：（4-（1,8-萘啶-2-基）哌啶-1-基）嘧啶衍生物的分子结晶
公开(公告)号：US20110237605A1
公开(公告)日：2011-09-29
申请号：US13018896
申请日：2011-02-01
申请人： Eric Phillips , Mohannad Shawer
发明人： Eric Phillips , Mohannad Shawer
IPC分类号： A61K31/506 , C07D471/04 , A61P27/02 , A61P35/00
CPC分类号： C07D471/04
摘要： A molecular crystal form of (S)-3-(2,5-dimethyl-6-(4-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)piperidin-1-yl)pyrimidin-4-ylamino)-2-(4-methoxyphenylsulfonamido)propanoic acid is characterized by an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 7.44, 14.80, 16.64, and 23.04±0.2°. The molecular crystal can be formulated into pharmaceutical composition for treating or controlling diseases resulting from pathological angiogenesis.
摘要翻译：分子晶形式的（S）-3-（2,5-二甲基-6-（4-（5,6,7,8-四氢-1,8-二氮杂萘-2-基）哌啶-1-基）嘧啶-4-基氨基）-2-（4-甲氧基苯基磺酰氨基）丙酸的特征在于包含在2θ处的峰的X射线粉末衍射（“XRPD”）光谱; 角度为7.44,14.80,16.64和23.04±0.2°。分子晶体可以配制成药物组合物，用于治疗或控制由病理性血管生成引起的疾病。

4. 发明授权

US08173169B2 Formulation and process for the preparation of modafinil 有权
标题翻译：莫达非尼的制备和制备方法
公开(公告)号：US08173169B2
公开(公告)日：2012-05-08
申请号：US11776012
申请日：2007-07-11
申请人： Mohannad Shawer , AlSayed AlArabi Sallam , Dalia Jawhari
发明人： Mohannad Shawer , AlSayed AlArabi Sallam , Dalia Jawhari
IPC分类号： A61K9/16 , A61K9/20 , A61K9/48
CPC分类号： A61K9/2077 , A61K9/2018 , A61K9/2027 , A61K9/2059 , A61K31/165
摘要： The present invention provides pharmaceutical tablets comprising modafinil particles, processes for preparing such pharmaceutical tablets, and methods of treating a disease or disorder using the pharmaceutical tablet of the invention. In particular, the pharmaceutical tablet of the invention comprises modafinil particles and one or more pharmaceutically acceptable excipients, wherein the modafinil particles have a size distribution such that at least about 65% of the modafinil particles have a diameter greater than 220 microns and the tablet is bioequivalent to PROVIGIL®. The pharmaceutical tablet of the invention is prepared by a dry granulation method.
摘要翻译：本发明提供了包含莫替非尼颗粒的药物片剂，制备该药物片剂的方法，以及使用本发明的药物片剂治疗疾病或病症的方法。特别地，本发明的药物片剂包含莫替非尼颗粒和一种或多种药学上可接受的赋形剂，其中莫达非尼颗粒的尺寸分布使得至少约65％的莫达非尼颗粒的直径大于220微米，与PROVIGIL®具有生物等效性。本发明的药片通过干法制粒法制备。

5. 发明申请

US20120252756A1 Pharmaceutical Compositions and Methods for Treating, Controlling, Ameliorating, or Reversing Conditions of the Eye 审中-公开
标题翻译：用于治疗，控制，改善或逆转眼睛条件的药物组合物和方法
公开(公告)号：US20120252756A1
公开(公告)日：2012-10-04
申请号：US13469853
申请日：2012-05-11
申请人： Martin J. Coffey , Reza Haque , Ngumah Quintus , Mohannad Shawer , Jinzhong Zhang
发明人： Martin J. Coffey , Reza Haque , Ngumah Quintus , Mohannad Shawer , Jinzhong Zhang
IPC分类号： A61K31/717 , A61P27/04 , A61P27/02
CPC分类号： A61K9/0048 , A61K31/4709 , A61K31/4725 , A61K31/55 , A61K31/56 , A61K45/06 , A61K47/10 , A61K47/38 , A61K2300/00
摘要： A pharmaceutical composition comprises a polyethylene glycol having a molecular weight in the range from about 1,000 to about 10,000, and a water-soluble cellulose derivative having a molecular weight in the range from about 50,000 to 120,000. The composition can further comprise boric acid and/or phosphate, a non-ionic surfactant, and/or an ophthalmic therapeutic agent. The composition is effective in treating, controlling, ameliorating, or reversing one or more conditions or symptoms of dry eye.
摘要翻译：药物组合物包含分子量在约1,000至约10,000范围内的聚乙二醇和分子量在约50,000至120,000范围内的水溶性纤维素衍生物。组合物还可以包含硼酸和/或磷酸盐，非离子表面活性剂和/或眼科治疗剂。该组合物在治疗，控制，改善或逆转干眼症的一种或多种病症或症状方面是有效的。

6. 发明申请

US20070275057A1 Formulation and Process for the Preparation of Modafinil 有权
标题翻译：莫达非尼的制备和制备方法
公开(公告)号：US20070275057A1
公开(公告)日：2007-11-29
申请号：US11776012
申请日：2007-07-11
申请人： Mohannad Shawer , AlSayed Sallam , Dalia Jawhari
发明人： Mohannad Shawer , AlSayed Sallam , Dalia Jawhari
IPC分类号： A61K31/165 , A61K9/20 , A61K9/14
CPC分类号： A61K9/2077 , A61K9/2018 , A61K9/2027 , A61K9/2059 , A61K31/165
摘要： The present invention provides pharmaceutical tablets comprising modafinil particles, processes for preparing such pharmaceutical tablets, and methods of treating a disease or disorder using the pharmaceutical tablet of the invention. In particular, the pharmaceutical tablet of the invention comprises modafinil particles and one or more pharmaceutically acceptable excipients, wherein the modafinil particles have a size distribution such that at least about 65% of the modafinil particles have a diameter greater than 220 microns and the tablet is bioequivalent to PROVIGIL®. The pharmaceutical tablet of the invention is prepared by a dry granulation method.
摘要翻译：本发明提供了包含莫替非尼颗粒的药物片剂，制备该药物片剂的方法，以及使用本发明的药物片剂治疗疾病或病症的方法。特别地，本发明的药物片剂包含莫替非尼颗粒和一种或多种药学上可接受的赋形剂，其中莫达非尼颗粒的尺寸分布使得至少约65％的莫达非尼颗粒的直径大于220微米，与PROVIGIL（R）的生物等效性。本发明的药片通过干法制粒法制备。

7. 发明申请

US20110319502A1 Compositions and Methods for Enhancing Reduction of Spore-Forming Microorganisms 审中-公开
标题翻译：用于增强孢子形成微生物的减少的组合物和方法
公开(公告)号：US20110319502A1
公开(公告)日：2011-12-29
申请号：US13116100
申请日：2011-05-26
申请人： Martin J. Coffey , Mohannad Shawer
发明人： Martin J. Coffey , Mohannad Shawer
IPC分类号： A61K47/26 , A61K47/18
CPC分类号： A61K9/0048 , A61K31/00 , A61K31/7004 , A61K31/7016 , A61K47/26 , A61K2300/00
摘要： A pharmaceutical formulation comprises a pharmaceutically acceptable preservative and a material selected from the group consisting of D-glucose, sucrose, maltose, D-mannose, trehalose, glutamic acid, mixtures thereof, and combinations thereof, wherein the formulation has enhanced preservative efficacy against spore-forming microorganisms. The formulation can further comprise boric acid and/or phosphate. A method for enhancing the preservative efficacy of a pharmaceutical formulation against spore-forming microorganisms, comprising adding a pharmaceutically acceptable preservative, and a material selected from the group consisting of D-glucose, sucrose, maltose, D-mannose, trehalose, glutamic acid, mixtures thereof, and combinations thereof, to the pharmaceutical formulation. The formulation optionally includes an active agent for treating or controlling a disease or disorder of the eye. The formulation may be used to treat, clean, disinfect, store, wet, or rewet contact lenses.
摘要翻译：药物制剂包含药学上可接受的防腐剂和选自D-葡萄糖，蔗糖，麦芽糖，D-甘露糖，海藻糖，谷氨酸，其混合物及其组合的材料，其中所述制剂对孢子具有增强的防腐功效形成微生物。制剂还可以包含硼酸和/或磷酸盐。一种用于增强药物制剂对孢子形成微生物的防腐功效的方法，包括加入药学上可接受的防腐剂和选自D-葡萄糖，蔗糖，麦芽糖，D-甘露糖，海藻糖，谷氨酸，它们的混合物，及其组合。制剂任选地包括用于治疗或控制眼睛疾病或病症的活性剂。该制剂可用于治疗，清洁，消毒，储存，湿润或再湿润隐形眼镜。

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