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31. 发明授权

US09205097B2 Anti-infective hydroxy-phenyl-benzoates and methods of use 有权
标题翻译：抗感染性羟基苯基苯甲酸酯及其使用方法
公开(公告)号：US09205097B2
公开(公告)日：2015-12-08
申请号：US14229667
申请日：2014-03-28
申请人： Los Angeles Biomedical Research Institute at Harbor-UCLA Medical Center
发明人： Michael R. Yeaman , Arnold S. Bayer
IPC分类号： A61K31/60 , A61K38/14 , A61K31/603
CPC分类号： A61K31/60 , A61K31/5377 , A61K31/603 , A61K38/14 , Y02A50/402 , Y02A50/47 , Y02A50/473 , Y02A50/481 , Y02A50/483
摘要： The invention provides a method for preventing or treating a disease caused by an extracellular microorganism, said method comprising systemically administering to a subject in need thereof a prophylactically or therapeutically effective amount of a salicylic acid (SAL) or a SAL analog. The extracellular microorganism can be of the bacterial genus Staphylococcus, for example, Staphylococcus aureus. The extracellular microorganism can be a strain that is resistant to at least one antibiotic. The strain can be selected from the group consisting of methycillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate Staphylococcus aureus (VISA) and vancomycin-resistant Staphylococcus aureus (VRSA). The invention also provides a method for preventing or treating an infectious disease caused by of methycillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate Staphylococcus aureus (VISA) or vancomycin-resistant Staphylococcus aureus (VRSA), comprising systemically co-administering in a synergistic combination to a subject in need thereof prophylactically or therapeutically effective amounts, individually or collectively, of a salicylic acid (SAL) or a SAL analog and at least one additional antimicrobial agent, for example, vancomycin and/or linezolid.
摘要翻译：本发明提供了一种预防或治疗由细胞外微生物引起的疾病的方法，所述方法包括向有需要的受试者全身施用预防或治疗有效量的水杨酸（SAL）或SAL类似物。细胞外微生物可以是细菌属葡萄球菌，例如金黄色葡萄球菌。细胞外微生物可以是对至少一种抗生素具有抗性的菌株。该菌株可以选自耐甲氧西林金黄色葡萄球菌（MRSA），万古霉素 - 中间体金黄色葡萄球菌（VISA）和耐万古霉素金黄色葡萄球菌（VRSA）。本发明还提供一种预防或治疗由耐甲氧西林金黄色葡萄球菌（MRSA），万古霉素中间体金黄色葡萄球菌（VISA）或万古霉素耐药金黄色葡萄球菌（VRSA）引起的感染性疾病的方法，其包括全身共同施用于对需要其的预防或治疗有效量的水杨酸（SAL）或SAL类似物和至少一种另外的抗微生物剂例如万古霉素和/或利奈唑胺的预防或治疗有效量的协同组合。

32. 发明申请

US20150344522A1 AURISTATIN TYRAMINE PHOSPHATE SALTS AND AURISTATIN AMINOQUINOLINE DERIVATIVES AND PRODRUGS THEREOF 有权
标题翻译： AURISTATIN TYRAMINE PHOSPHATE SALTS AND AURISTATIN AMINOQUINOLINE DERIVATIVES AND PRODRUGS WITHEROFOF
公开(公告)号：US20150344522A1
公开(公告)日：2015-12-03
申请号：US14705651
申请日：2015-05-06
申请人： George R. Pettit , Fiona Hogan , Steven Toms
发明人： George R. Pettit , Fiona Hogan , Steven Toms
IPC分类号： C07K7/02 , A61K47/48 , A61K38/08 , A61K45/06
CPC分类号： A61K47/48415 , A61K31/4709 , A61K31/472 , A61K38/00 , A61K38/07 , A61K38/08 , A61K45/06 , A61K47/6851 , A61K47/6889 , C07D207/12 , C07D401/12 , C07K5/0205 , C07K5/101 , C07K7/02 , C07K16/3076 , G01N33/5014 , Y02A50/401 , Y02A50/475 , Y02A50/483 , Y02A50/57 , A61K2300/00
摘要： The present invention relates to new auristatin compounds and prodrugs thereof, compositions comprising them and uses thereof.
摘要翻译：本发明涉及新的auristatin化合物及其前药，包含它们的组合物及其用途。

33. 发明授权

US09144587B2 Treating pancreatic carcinoma with a whole, leech saliva extract 有权
标题翻译：用整体治疗胰腺癌，水蛭唾液提取物
公开(公告)号：US09144587B2
公开(公告)日：2015-09-29
申请号：US14670262
申请日：2015-03-26
申请人： Biopep Solutions, Inc.
发明人： Abbas Mohammad Ghawi , Ahmed Merzouk , Abdualrahman Abdualkader , Mohamed Alaama
IPC分类号： A61K35/37 , A61K38/00 , A61K35/62 , A61K45/06 , A61K31/4745 , A61K31/282
CPC分类号： A61K35/62 , A01K67/033 , A01N63/00 , A61K9/0014 , A61K31/282 , A61K31/4745 , A61K31/555 , A61K38/21 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/393 , Y02A50/40 , Y02A50/401 , Y02A50/402 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/419 , Y02A50/422 , Y02A50/423 , Y02A50/463 , Y02A50/465 , Y02A50/467 , Y02A50/469 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/479 , Y02A50/481 , Y02A50/483 , Y02A50/491 , A61K2300/00
摘要： Methods are also provided for isolating and using a whole-saliva leech extract in the treatment of pancreatic carcinoma. The methods can include feeding a phagostimulatory agent to a leech; inducing a regurgitation in the leech, the inducing including placing the leech in an environment having a temperature of less than about 0° C.; and, collecting an unrefined, whole saliva in the regurgitation of the cooled leech. The methods can include revitalizing the leech by warming it at a temperature ranging from about 5° C. to about 40° C. Stable, lyophilized, whole-saliva extracts of a leech are also provided, the extract having a stable activity when stored for use at a temperature below about −20° C., the extract maintaining at least 70% of the activity for at least 6 months. The extracts can be used to treat solid tumors, treat liquid tumors, treat diabetes, treat a viral disease, treat a parasitic disease, treat an antibacterial disease, or serve as an anti-oxidant.
摘要翻译：还提供了用于分离和使用全唾液水蛭提取物治疗胰腺癌的方法。所述方法可以包括向水蛭喂养吞噬剂; 诱导水蛭反流，诱导包括将水蛭放置在温度低于约0℃的环境中; 并在冷水蛭的反流中收集未精制的全唾液。所述方法可以包括通过在约5℃至约40℃的温度范围内升温来振兴水蛭。还提供了稳定的，冻干的全唾液提取物，所述提取物在储存时具有稳定的活性在低于约-20℃的温度下使用，提取物保持至少6个月的活性的至少70％。提取物可用于治疗实体瘤，治疗液体肿瘤，治疗糖尿病，治疗病毒性疾病，治疗寄生虫病，治疗抗菌疾病或用作抗氧化剂。

34. 发明申请

US20150224125A1 BETA-LACTAMASE INHIBITORS 有权
标题翻译： BETA-LACTAMASE抑制剂
公开(公告)号：US20150224125A1
公开(公告)日：2015-08-13
申请号：US14693318
申请日：2015-04-22
申请人： VenatoRx Pharmaceuticals, Inc.
发明人： Christopher J. BURNS , Denis DAIGLE , Bin LIU , Daniel McGARRY , Daniel C. PEVEAR , Robert E. Lee TROUT , Randy W. JACKSON
IPC分类号： A61K31/69 , A61K45/06 , C07F5/02
CPC分类号： C07F5/025 , A61K31/407 , A61K31/496 , A61K31/546 , A61K31/69 , A61K45/06 , Y02A50/47 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
摘要翻译：本文描述了调节β-内酰胺酶活性的化合物和组合物。在一些实施方案中，本文所述的化合物抑制β-内酰胺酶。在某些实施方案中，本文所述的化合物可用于治疗细菌感染。

35. 发明授权

US09089586B2 Levocarrimycin, pharmaceutical compositions, preparation methods and uses thereof 有权
标题翻译：洛伐他汀，药物组合物，制备方法和用途
公开(公告)号：US09089586B2
公开(公告)日：2015-07-28
申请号：US13699358
申请日：2011-05-25
申请人： Yang Jiang , Yuyou Hao
发明人： Yang Jiang , Yuyou Hao
IPC分类号： A61K31/7048 , A61P31/00 , A61P31/04 , C12P19/62 , C07H17/08
CPC分类号： A61K31/7048 , C07H17/08 , C12P19/62 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/483 , A61K2300/00
摘要： The present invention relates to levocarrimycin, its pharmaceutical compositions, preparation methods and application. Levocarrimycin is a mixture of isovalerylspiramycin III, II and I as main components and contains some isobutyrylspiramycin III and II, butyrylspiramycin III and II, propionylspiramycin III and II, as well as acetylspiramycin III and II, among which, the content of isovalerylspiramycin III is no less than 30 wt %, the total content of isovalerylspiramycin III, II and I is no less than 60 wt %, and the content of acylspiramycin is 80-98 wt %. Specific optical rotation of said levocarrimycin is [α]D=−52°˜−57° in the solution of 0.02 g/ml chloroform at temperature of 25° C. The present invention also relates to the crystalline compound of isovalerylspiramycin III, II or I in levocarrimycin, and pharmaceutical compositions containing the said levocarrimycin. In present invention, the active components in levocarrimycin or its pharmaceutical compositions have optical activity and excellent anti-infective effect.
摘要翻译：本发明涉及左卡霉素，其药物组合物，制备方法和用途。莱卡霉素是异戊酰基螺旋霉素III，II和I作为主要成分的混合物，含有一些异丁酰基ir霉素Ⅲ和Ⅱ，丁酰yl霉素Ⅲ和Ⅳ，丙酰基ir霉素Ⅲ和Ⅳ以及乙酰基ir霉素Ⅲ和Ⅳ，其中异戊酰ir霉素Ⅲ的含量为小于30重量％，异戊酰螺杆霉素III，II和I的总含量不小于60重量％，酰基丝氨酸的含量为80-98重量％。在0.02g / ml氯仿的溶液中，所述左卡马瑞霉素的比旋光度在25℃的温度下为[α] D = -52°〜57°。本发明还涉及异戊酰螺旋霉素III，II或我在左卡波霉素中的药物组合物，以及含有所述的左卡罗明珠霉素的药物组合物。在本发明中，左卡霉素或其药物组合物中的活性成分具有光学活性和优异的抗感染作用。

36. 发明授权

US09072759B2 Biodefenses using triazole-containing macrolides 有权
标题翻译：使用含三唑的大环内酯类生物鉴定
公开(公告)号：US09072759B2
公开(公告)日：2015-07-07
申请号：US13125550
申请日：2009-10-24
申请人： Prabhavathi B. Fernandes
发明人： Prabhavathi B. Fernandes
IPC分类号： A61K31/70 , A61K31/7048 , A61K31/7052
CPC分类号： A61K31/7048 , A61K31/424 , A61K31/70 , A61K31/7052 , A61K31/7056 , C07D498/04 , C07H17/08 , Y02A50/406 , Y02A50/47 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481 , Y02A50/483
摘要： Use of macrolide and ketolide antibiotics for the treatment of acute exposure and diseases caused by biodefense pathogens is described.
摘要翻译：描述了使用大环内酯和酮内酯抗生素治疗由生物防治病原体引起的急性暴露和疾病。

37. 发明申请

US20150119363A1 METHODS OF TREATING BACTERIAL INFECTIONS 审中-公开
标题翻译：治疗细菌感染的方法
公开(公告)号：US20150119363A1
公开(公告)日：2015-04-30
申请号：US14377163
申请日：2013-02-11
申请人： Rampex Pharmaceuticals, Inc.
发明人： Michael N. Dudley , Scott Hecker , Olga Rodny
IPC分类号： A61K31/69 , A61K31/427 , A61K31/4196
CPC分类号： A61K31/69 , A61K31/397 , A61K31/407 , A61K31/4196 , A61K31/423 , A61K31/427 , A61K31/43 , A61K31/439 , A61K31/4436 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/5383 , A61K31/545 , A61K31/551 , A61K31/662 , Y02A50/401 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/483
摘要： The present invention relates to compounds, compositions and methods for treating bacterial infections. Embodiments of the present invention include antibiotics and β-lactamase inhibitors to treat resistant infections.
摘要翻译：本发明涉及用于治疗细菌感染的化合物，组合物和方法。本发明的实施方案包括治疗抗性感染的抗生素和β-内酰胺酶抑制剂。

38. 发明申请

US20150099006A1 ANTIBACTERIAL THERAPY WITH A WHOLE, LEECH SALIVA EXTRACT 审中-公开
标题翻译：具有全身，LELLAL SALIVA提取物的抗生素治疗
公开(公告)号：US20150099006A1
公开(公告)日：2015-04-09
申请号：US14563829
申请日：2014-12-08
申请人： Biopep Solutions, Inc.
发明人： Abbas Mohammad GHAWI , Ahmed MERZOUK , Abdualrahman ABDUALKADER , Mohamed ALAAMA
IPC分类号： A61K35/62 , A01N63/00
CPC分类号： A61K35/62 , A01K67/033 , A01N63/00 , A61K9/0014 , A61K31/282 , A61K31/4745 , A61K31/555 , A61K38/21 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/393 , Y02A50/40 , Y02A50/401 , Y02A50/402 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/419 , Y02A50/422 , Y02A50/423 , Y02A50/463 , Y02A50/465 , Y02A50/467 , Y02A50/469 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/479 , Y02A50/481 , Y02A50/483 , Y02A50/491 , A61K2300/00
摘要： Methods are provided for isolating and using a whole-saliva leech extract. The methods can include feeding a phagostimulatory agent to a leech; inducing a regurgitation in the leech, the inducing including placing the leech in an environment having a temperature of less than about 0° C.; and, collecting an unrefined, whole saliva in the regurgitation of the cooled leech. The methods can include revitalizing the leech by warming it at a temperature ranging from about 5° C. to about 40° C. Stable, lyophilized, whole-saliva extracts of a leech are also provided, the extract having a stable activity when stored for use at a temperature below about −20° C., the extract maintaining at least 70% of the activity for at least 6 months. The extracts can be used to treat solid tumors, treat liquid tumors, treat diabetes, treat a viral disease, treat a parasitic disease, treat an antibacterial disease, or serve as an anti-oxidant.
摘要翻译：提供了分离和使用全唾液水蛭提取物的方法。所述方法可以包括向水蛭喂养吞噬剂; 诱导水蛭反流，诱导包括将水蛭放置在温度低于约0℃的环境中; 并在冷水蛭的反流中收集未精制的全唾液。所述方法可以包括通过在约5℃至约40℃的温度范围内升温来振兴水蛭。还提供了稳定的，冻干的全唾液提取物，所述提取物在储存时具有稳定的活性在低于约-20℃的温度下使用，提取物保持至少6个月的活性的至少70％。提取物可用于治疗实体瘤，治疗液体肿瘤，治疗糖尿病，治疗病毒性疾病，治疗寄生虫病，治疗抗菌疾病或用作抗氧化剂。

39. 发明申请

US20150086645A1 TREATING LEUKEMIA WITH A WHOLE, LEECH SALIVA EXTRACT 审中-公开
标题翻译：用全方位的LALIS SALIVA提取物处理低密度脂蛋白
公开(公告)号：US20150086645A1
公开(公告)日：2015-03-26
申请号：US14552388
申请日：2014-11-24
申请人： Biopep Solutions, Inc.
发明人： ABBAS MOHAMMAD GHAWI , AHMED MERZOUK , ABDUALRAHMAN ABDUALKADER , MOHAMED ALAAMA
IPC分类号： A61K35/62 , A61K31/555 , A61K31/4745
CPC分类号： A61K35/62 , A01K67/033 , A01N63/00 , A61K9/0014 , A61K31/282 , A61K31/4745 , A61K31/555 , A61K38/21 , A61K45/06 , Y02A50/385 , Y02A50/387 , Y02A50/393 , Y02A50/40 , Y02A50/401 , Y02A50/402 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/419 , Y02A50/422 , Y02A50/423 , Y02A50/463 , Y02A50/465 , Y02A50/467 , Y02A50/469 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/479 , Y02A50/481 , Y02A50/483 , Y02A50/491 , A61K2300/00
摘要： Methods are provided for isolating and using a whole-saliva leech extract. The methods can include feeding a phagostimulatory agent to a leech; inducing a regurgitation in the leech, the inducing including placing the leech in an environment having a temperature of less than about 0° C.; and, collecting an unrefined, whole saliva in the regurgitation of the cooled leech. The methods can include revitalizing the leech by warming it at a temperature ranging from about 5° C. to about 40° C. Stable, lyophilized, whole-saliva extracts of a leech are also provided, the extract having a stable activity when stored for use at a temperature below about −20° C., the extract maintaining at least 70% of the activity for at least 6 months. The extracts can be used to treat solid tumors, treat liquid tumors, treat diabetes, treat a viral disease, treat a parasitic disease, treat an antibacterial disease, or serve as an anti-oxidant.
摘要翻译：提供了分离和使用全唾液水蛭提取物的方法。所述方法可以包括向水蛭喂养吞噬剂; 诱导水蛭反流，诱导包括将水蛭放置在温度低于约0℃的环境中; 并在冷水蛭的反流中收集未精制的全唾液。所述方法可以包括通过在约5℃至约40℃的温度范围内升温来振兴水蛭。还提供了稳定的，冻干的全唾液提取物，所述提取物在储存时具有稳定的活性在低于约-20℃的温度下使用，提取物保持至少6个月的活性的至少70％。提取物可用于治疗实体瘤，治疗液体肿瘤，治疗糖尿病，治疗病毒性疾病，治疗寄生虫病，治疗抗菌疾病或用作抗氧化剂。

40. 发明申请

US20150038477A1 ORALLY ADMINISTRABLE GALLIUM COMPOSITIONS AND METHODS OF USE 审中-公开
公开(公告)号：US20150038477A1
公开(公告)日：2015-02-05
申请号：US14457930
申请日：2014-08-12
申请人： Lawrence R. Bernstein
发明人： Lawrence R. Bernstein
IPC分类号： A61K47/38 , A23K1/175 , A61K31/555
CPC分类号： A61K47/38 , A23K20/20 , A23L33/16 , A23V2002/00 , A61K9/0095 , A61K9/2013 , A61K9/2054 , A61K9/4858 , A61K9/4866 , A61K31/28 , A61K31/555 , A61K31/717 , A61K33/24 , A61K45/06 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/483 , A61K2300/00
摘要： Provided are pharmaceutical gallium compositions that are particularly useful for oral administration. The pharmaceutical compositions include solid, liquid, and paste formulations, which have high oral gallium bioavailability and are suitable for human and veterinary applications. The compositions comprise pharmaceutically acceptable gallium compounds, such as gallium maltolate, gallium 8-quinolinolonate, or gallium nitrate, together with certain viscosity-increasing agents, such as water-soluble forms of methylcellulose or carboxymethylcellulose.
摘要翻译：提供特别可用于口服给药的药物镓组合物。药物组合物包括固体，液体和糊剂制剂，其具有高口服镓生物利用度并且适用于人和兽医应用。组合物包括药学上可接受的镓化合物，例如麦芽糖醇镓，8-羟基喹啉镓酸镓或硝酸镓，以及某些增粘剂，例如水溶性形式的甲基纤维素或羧甲基纤维素。

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