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1. 发明申请

US20070287749A1 BROMFENAC OPHTHALMIC FORMULATIONS AND METHODS OF USE 审中-公开
标题翻译： BROMFENAC OPHTHALMIC制剂和使用方法
公开(公告)号：US20070287749A1
公开(公告)日：2007-12-13
申请号：US11755662
申请日：2007-05-30
申请人： Shirou Sawa , Shuhei Fujita , Lisa Grillone
发明人： Shirou Sawa , Shuhei Fujita , Lisa Grillone
IPC分类号： A61K31/195 , A61P27/02
CPC分类号： A61K47/10 , A61K9/0043 , A61K9/0048 , A61K31/196 , A61K47/02 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/32 , A61K47/34
摘要： The present invention discloses a stability enhanced aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate. The present invention further discloses new bromfenac ophthalmic compositions which can potentially treat a broader patient population, and have greater stability properties, and may require a lower concentration or less doses of bromfenac then previously known bromfenac compositions. The present invention further comprises a method for treating inflammation and/or pain of the eye in a patient which method comprises topical application to the eye of a patient in need thereof of a therapeutically effective amount of a topical ophthalmic composition comprising bromfenac at a concentration of about 0.05% w/v to about 0.24% w/v.
摘要翻译：本发明公开了含有2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物，烷基芳基聚醚醇型聚合物如泰洛沙泊或聚乙二醇脂肪酸的稳定性增强的含水液体制剂酸酯如聚乙二醇单硬脂酸酯。本发明还公开了新的溴芬酸眼用组合物，其可以潜在地治疗更广泛的患者群体并且具有更大的稳定性，并且可能需要较低浓度或较少剂量的溴芬酸，然后是先前已知的溴芬酸组合物。本发明还包括用于治疗患者眼睛的炎症和/或疼痛的方法，该方法包括向有需要的患者的眼睛局部施用治疗有效量的局部眼用组合物，其包含浓度为约0.05％w / v至约0.24％w / v。

2. 发明申请

US20050239895A1 Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid 有权
标题翻译：含有2-氨基-3-（4-溴苯甲酰基）苯乙酸的含水液体制剂
公开(公告)号：US20050239895A1
公开(公告)日：2005-10-27
申请号：US10525006
申请日：2004-01-16
申请人： Shirou Sawa , Shuhei Fujita
发明人： Shirou Sawa , Shuhei Fujita
IPC分类号： A61K9/00 , A61K31/196 , A61K47/14 , A61P27/02 , A61P29/00 , A61K31/195 , A61K9/14
CPC分类号： A61K47/10 , A61K9/0043 , A61K9/0048 , A61K31/196 , A61K47/02 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/32 , A61K47/34
摘要： An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
摘要翻译：含有2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物的本发明的含水液体制剂，烷基芳基聚醚醇型聚合物如泰洛沙夫或聚乙二醇脂肪酸酯如聚乙二醇单硬脂酸酯是稳定的。由于即使在将防腐剂并入所述水性液体制剂的情况下，防腐剂长期存在足够的防腐效果，所以滴眼剂形式的水性液体制剂可用于治疗睑炎，结膜炎，巩膜炎，术后炎症。此外，本发明的鼻滴形式的水性液体制剂可用于治疗过敏性鼻炎和炎症性鼻炎（例如慢性鼻炎，肥大性鼻炎，鼻息肉等）。

3. 发明申请

US20120115957A1 AQUEOUS LIQUID PREPARATION CONTAINING 2-AMINO-3-(4-BROMOBENZOYL)PHENYLACETIC ACID 有权
标题翻译：包含2-氨基-3-（4-溴苯甲酰基）苯甲酸的水性液体制剂
公开(公告)号：US20120115957A1
公开(公告)日：2012-05-10
申请号：US13353653
申请日：2012-01-19
申请人： Shirou Sawa , Shuhei Fujita
发明人： Shirou Sawa , Shuhei Fujita
IPC分类号： A61K31/195 , A61P29/00 , A61P27/02
CPC分类号： A61K47/10 , A61K9/0043 , A61K9/0048 , A61K31/196 , A61K47/02 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/32 , A61K47/34
摘要： An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
摘要翻译：含有2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物的本发明的含水液体制剂，烷基芳基聚醚醇型聚合物如泰洛沙夫或聚乙二醇脂肪酸酯如聚乙二醇单硬脂酸酯是稳定的。由于即使在将防腐剂并入所述水性液体制剂的情况下，防腐剂长期存在足够的防腐效果，所以滴眼剂形式的水性液体制剂可用于治疗睑炎，结膜炎，巩膜炎，术后炎症。此外，本发明的鼻滴形式的水性液体制剂可用于治疗过敏性鼻炎和炎症性鼻炎（例如慢性鼻炎，肥大性鼻炎，鼻息肉等）。

4. 发明授权

US08497304B2 Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid 有权
公开(公告)号：US08497304B2
公开(公告)日：2013-07-30
申请号：US13353653
申请日：2012-01-19
申请人： Shirou Sawa , Shuhei Fujita
发明人： Shirou Sawa , Shuhei Fujita
IPC分类号： A01N37/18 , A01N37/44 , A01N37/10 , A61K31/165 , A61K31/24 , A61K31/19
CPC分类号： A61K47/10 , A61K9/0043 , A61K9/0048 , A61K31/196 , A61K47/02 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/32 , A61K47/34
摘要： An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).

5. 发明授权

US08129431B2 Aqueous liquid preparation containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid 有权
标题翻译：含有2-氨基-3-（4-溴苯甲酰基）苯乙酸的含水液体制剂
公开(公告)号：US08129431B2
公开(公告)日：2012-03-06
申请号：US10525006
申请日：2004-01-16
申请人： Shirou Sawa , Shuhei Fujita
发明人： Shirou Sawa , Shuhei Fujita
IPC分类号： A01N37/18 , A01N37/44 , A01N37/10 , A61K31/165 , A61K31/24 , A61K31/19
CPC分类号： A61K47/10 , A61K9/0043 , A61K9/0048 , A61K31/196 , A61K47/02 , A61K47/14 , A61K47/183 , A61K47/186 , A61K47/32 , A61K47/34
摘要： An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).
摘要翻译：含有2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物的本发明的含水液体制剂，烷基芳基聚醚醇型聚合物如泰洛沙夫或聚乙二醇脂肪酸酯如聚乙二醇单硬脂酸酯是稳定的。由于即使在将防腐剂并入所述水性液体制剂的情况下，防腐剂长期存在足够的防腐效果，所以滴眼剂形式的水性液体制剂可用于治疗睑炎，结膜炎，巩膜炎，术后炎症。此外，本发明的鼻滴形式的水性液体制剂可用于治疗过敏性鼻炎和炎症性鼻炎（例如慢性鼻炎，肥大性鼻炎，鼻息肉等）。

6. 发明申请

US20070021507A1 Aqueous eye drops with accelerated intraocular migration 审中-公开
标题翻译：水性眼药水与眼内移动加速
公开(公告)号：US20070021507A1
公开(公告)日：2007-01-25
申请号：US10568418
申请日：2005-11-04
申请人： Shirou Sawa , Tomoko Fujimoto
发明人： Shirou Sawa , Tomoko Fujimoto
IPC分类号： A61K31/198
CPC分类号： A61K31/133 , A61K31/185 , A61K31/196
摘要： An aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof and an organic amine (for example, aminoethylsulfonic acid or trometamol) or a salt thereof is useful as an eye drop for once a day administration for treating inflammatory diseases of the external segment or the anterior segment of the eyes, since such aqueous eye drop can maintain a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid in anterior aqueous humor for at least 24 hours by once a day administration.
摘要翻译：包含2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物和有机胺（例如氨基乙基磺酸或氨丁三醇）或其盐的水性滴眼剂可用作滴眼剂一天一次的治疗用于治疗外部部分或眼前段的炎性疾病，因为这种水性滴眼剂可以维持前房水中2-氨基-3-（4-溴苯甲酰基）苯乙酸的治疗有效浓度至少24小时，每天一次。

7. 发明授权

US07829544B2 Aqueous solution preparation containing aminoglycoside antibiotic and bromfenac 有权
标题翻译：含有氨基糖苷类抗生素和溴芬酸的水溶液制剂
公开(公告)号：US07829544B2
公开(公告)日：2010-11-09
申请号：US10578359
申请日：2004-11-12
申请人： Shirou Sawa
发明人： Shirou Sawa
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K31/7036 , A61K9/0095 , A61K31/196
摘要： Stable and clear aqueous solution preparations comprising an aminoglycoside antibiotic or a pharmacologically acceptable salt thereof and bromfenac being a nonsteroidal antiinflammatory agent or a pharmacologically acceptable salt thereof.
摘要翻译：稳定且透明的水溶液制剂，其包含氨基糖苷类抗生素或其药理学上可接受的盐和作为非甾体抗炎剂的溴芬酸或其药理学上可接受的盐。

8. 发明授权

US5942508A Method for solubilizing pyridonecarboxylic acid solubilizer thereof and aqueous solution containing solubilized pyridonecarboxylic acid 失效
标题翻译：溶解吡啶酮羧酸增溶剂的方法和含有溶解的吡啶酮羧酸的水溶液
公开(公告)号：US5942508A
公开(公告)日：1999-08-24
申请号：US17499
申请日：1998-02-02
申请人： Shirou Sawa
发明人： Shirou Sawa
IPC分类号： A61K9/00 , A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/5025 , A61K31/535 , A61K31/5383 , A61K47/12 , A61K31/19 , A61K31/445
CPC分类号： A61K47/12 , A61K31/435 , A61K31/4375 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/5025 , A61K31/535 , A61K31/5383 , A61K9/0043 , A61K9/0048
摘要： A method for solubilizing a pyridonecarboxylic acid or a pharmacologically acceptable salt thereof, which comprises adding an arylcarboxylic acid of the formula (I):L.sup.1 --R.sup.1 COOH (I)wherein L.sup.1 is an optionally substituted heterocyclic group or aryl group having not more than 14 carbon atoms, and R.sup.1 is an optionally substituted alkyl group having not more than 4 carbon atoms or a single bond, to the pyridonecarboxylic acid or the pharmacologically acceptable salt thereof, a solubilizer thereof and an aqueous solution containing a solubilized pyridonecarboxylic acid. According to the solubilization method of the present invention, the solubility of pyridonecarboxylic acid compounds and salts thereof at near physiological pH can be increased, thereby making the production of an aqueous solution to be used as an eye drop, nasal drop, ear drop and the like possible.
摘要翻译：一种溶解吡啶酮羧酸或其药理学上可接受的盐的方法，其包括加入式（I）的芳基羧酸：其中L 1为任选取代的杂环基或不多于14个碳的芳基的L1-R1COOH（Ⅰ）原子，R 1为不大于4个碳原子或单键的任选取代的烷基，与吡啶酮羧酸或其药理学上可接受的盐，其增溶剂和含有溶解的吡啶酮羧酸的水溶液。根据本发明的溶解方法，可以提高吡啶酮羧酸化合物及其盐在接近生理pH下的溶解度，从而使水溶液的制备用作滴眼剂，滴鼻剂，滴耳剂和像可能的

9. 发明授权

US08658703B2 Aqueous suspension preparations 失效
标题翻译：水性悬浮液制剂
公开(公告)号：US08658703B2
公开(公告)日：2014-02-25
申请号：US12484636
申请日：2009-06-15
申请人： Shirou Sawa
发明人： Shirou Sawa
IPC分类号： A61K47/32
CPC分类号： A61K9/0046 , A61K9/0014 , A61K9/0019 , A61K9/0043 , A61K9/0048 , A61K31/198 , A61K31/496 , A61K31/573 , A61K47/32 , A61K47/36 , A61K47/38
摘要： Addition of polyvinylpyrrolidone and a water-soluble anionic macromolecular compound to an aqueous suspension of a hardly soluble drug allows to provide an aqueous suspension in which aggregation of drug particles, formation of macro crystals from suspended particles and formation of secondary particles from deposited particles are prevented, and adhesion and adsorption to containers made of plastics, e.g., polypropylene or polyethylene, are avoided. As it has a good redispersibility, the aqueous suspension is useful as eye drops, nasal drops, ear drops, injections, oral preparations, liniments and lotions.
摘要翻译：将聚乙烯吡咯烷酮和水溶性阴离子高分子化合物加入到几乎不溶性药物的水性悬浮液中，可以提供一种水性悬浮液，其中可以防止药物颗粒的聚集，悬浮颗粒的宏观晶体的形成和沉积颗粒的二次颗粒的形成，并且避免了由塑料例如聚丙烯或聚乙烯制成的容器的粘附和吸附。由于其具有良好的再分散性，所述水悬浮液可用作滴眼剂，滴鼻剂，滴耳剂，注射剂，口服制剂，搽剂和洗剂。

10. 发明授权

US08299124B2 Aqueous intraocular penetration-promoting eye drop 有权
标题翻译：水中眼内渗透促进性眼药水
公开(公告)号：US08299124B2
公开(公告)日：2012-10-30
申请号：US13332827
申请日：2011-12-21
申请人： Shirou Sawa , Tomoko Fujimoto
发明人： Shirou Sawa , Tomoko Fujimoto
IPC分类号： A61K31/19 , A61K31/04
CPC分类号： A61K31/133 , A61K31/185 , A61K31/196
摘要： An aqueous eye drop comprising 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof and an organic amine (for example, aminoethylsulfonic acid or trometamol) or a salt thereof is useful as an eye drop for once a day administration for treating inflammatory diseases of the external segment or the anterior segment of the eyes, since such aqueous eye drop can maintain a therapeutically effective concentration of 2-amino-3-(4-bromobenzoyl)phenylacetic acid in anterior aqueous humor for at least 24 hours by once a day administration.
摘要翻译：包含2-氨基-3-（4-溴苯甲酰基）苯乙酸或其药理学上可接受的盐或其水合物和有机胺（例如氨基乙基磺酸或氨丁三醇）或其盐的水性滴眼剂可用作滴眼剂一天一次的治疗用于治疗外部部分或眼前段的炎性疾病，因为这种水性滴眼剂可以维持前房水中2-氨基-3-（4-溴苯甲酰基）苯乙酸的治疗有效浓度至少24小时，每天一次。

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