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1. 发明授权

US06753015B2 Microparticle compositions and methods for the manufacture thereof 有权
公开(公告)号：US06753015B2
公开(公告)日：2004-06-22
申请号：US09967462
申请日：2001-09-28
申请人： Jia-Hwa Fang , Mammohan Singh , Derek O'Hagan , Maninder Hora
发明人： Jia-Hwa Fang , Mammohan Singh , Derek O'Hagan , Maninder Hora
IPC分类号： A61K914
CPC分类号： A61K9/1676 , A61K9/1647
摘要： Microparticles with adsorbed complexes of macromolecule and detergent, methods of making such microparticles, and uses thereof, are disclosed. The microparticles comprise a polymer, such as a poly(&agr;-hydroxy acid), a polyhydroxy butyric acid, a polycaprolactone, a polyorthoester, a polyanhydride, and the like, and are formed using cationic, anionic, or nonionic detergents. The surfaces of the microparticles have adsorbed thereon a complex of biologically active macromolecules, such as nucleic acids, polypeptides, antigens, and adjuvants, and a detergent. Preferred polymers are poly(D,L-lactide-co-glycolides), more preferably those having a lactide/glycolide molar ratio ranging from 40:60 to 60:40 and having a molecular weight ranging from 30,000 Daltons to 70,000 Daltons. Preferred macromolecules are bacterial and viral antigens (such as HIV antigens, meningitis B antigens, streptococcus B antigens, and Influenza A hemagglutinin antigens) as well as polynucleotides that encode for such antigens.

2. 发明授权

US07846479B2 Microparticle compositions and methods for the manufacture thereof 有权
标题翻译：微粒组合物及其制造方法
公开(公告)号：US07846479B2
公开(公告)日：2010-12-07
申请号：US10775964
申请日：2004-02-10
申请人： Jia-Hwa Fang , Manmohan Singh , Derek O'Hagan , Maninder Hora
发明人： Jia-Hwa Fang , Manmohan Singh , Derek O'Hagan , Maninder Hora
IPC分类号： A61K9/14
CPC分类号： A61K9/1676 , A61K9/1647
摘要： Microparticles with adsorbed complexes of macromolecule and detergent, methods of making such microparticles, and uses thereof, are disclosed. The microparticles comprise a polymer, such as a poly(α-hydroxy acid), a polyhydroxy butyric acid, a polycaprolactone, a polyorthoester, a polyanhydride, and the like, and are formed using cationic, anionic, or nonionic detergents. The surfaces of the microparticles have adsorbed thereon a complex of biologically active macromolecules, such as nucleic acids, polypeptides, antigens, and adjuvants, and a detergent. Preferred polymers are poly(D,L-lactide-co-glycolides), more preferably those having a lactide/glycolide molar ratio ranging from 40:60 to 60:40 and having a molecular weight ranging from 30,000 Daltons to 70,000 Daltons. Preferred macromolecules are bacterial and viral antigens (such as HIV antigens, meningitis B antigens, streptococcus B antigens, and Influenza A hemagglutinin antigens) as well as polynucleotides that encode for such antigens.
摘要翻译：公开了具有大分子和洗涤剂的吸附复合物的微粒，制备这种微粒的方法及其用途。微粒包含聚（α-羟基酸），多羟基丁酸，聚己内酯，聚原酸酯，聚酐等聚合物，并使用阳离子，阴离子或非离子型洗涤剂形成。微粒表面上吸附有生物活性大分子如核酸，多肽，抗原和佐剂以及洗涤剂的复合物。优选的聚合物是聚（D，L-丙交酯 - 共 - 乙交酯），更优选丙交酯/乙交酯摩尔比范围为40:60至60:40且分子量范围为30,000道尔顿至70,000道尔顿的聚合物。优选的大分子是细菌和病毒抗原（例如HIV抗原，脑膜炎B抗原，B链球菌抗原和甲型流感血凝素抗原）以及编码这些抗原的多核苷酸。

3. 发明授权

US06573238B2 Method for producing sustained-release formulations 失效
标题翻译：缓释制剂的制备方法
公开(公告)号：US06573238B2
公开(公告)日：2003-06-03
申请号：US09187780
申请日：1998-11-06
申请人： Bret Shirley , Maninder Hora , Derek O'Hagan , Manmohan Singh
发明人： Bret Shirley , Maninder Hora , Derek O'Hagan , Manmohan Singh
IPC分类号： A61K3800
CPC分类号： A61K9/0019 , A61K9/0024 , A61K9/1647 , A61K9/1694 , A61K38/30 , A61K47/183
摘要： Methods for preparing biodegradable microparticles are provided. Also provided are microparticles prepared by the method which include IGF-1 entrapped therein. The microparticles allow for controlled release of IGF-1 and other polypeptides over prolonged periods of time.
摘要翻译：提供了制备可生物降解的微粒的方法。还提供了通过包含IGF-1的方法制备的微粒。微粒允许在长时间内控制释放IGF-1和其他多肽。

4. 发明授权

US09517263B2 Benzonaphthyridine-containing vaccines 有权
标题翻译：含有苯并萘啶的疫苗
公开(公告)号：US09517263B2
公开(公告)日：2016-12-13
申请号：US13377511
申请日：2010-06-10
申请人： Derek O'Hagan , Manmohan Singh , Siddhartha Jain , Sushma Kommareddy
发明人： Derek O'Hagan , Manmohan Singh , Siddhartha Jain , Sushma Kommareddy
IPC分类号： A61K39/02 , C07D471/00 , A61K39/39 , A61K39/00 , A61K39/12
CPC分类号： A61K39/39 , A61K2039/55511 , A61K2039/6093
摘要： The invention provides, inter alia, immunogenic compositions that comprise (a) a first antigen, (b) polymeric particles and (c) a benzonaphthyridine compound, which compositions elicits an immune response when administered to a vertebrate subject. The invention also provides, inter alia, methods of producing immunogenic compositions and methods for using immunogenic compositions (e.g., for treatment), among other benefits.
摘要翻译：本发明尤其提供了免疫原性组合物，其包含（a）第一抗原，（b）聚合物颗粒和（c）苯并萘啶化合物，该组合物在施用于脊椎动物受试者时引起免疫应答。本发明尤其提供产生免疫原性组合物的方法和使用免疫原性组合物（例如用于治疗）的方法以及其它益处。

5. 再颁专利

USRE45137E1 Adjuvanted meningococcus compositions 有权
标题翻译：佐剂脑膜炎球菌组成
公开(公告)号：USRE45137E1
公开(公告)日：2014-09-16
申请号：US13587840
申请日：2012-08-16
申请人： Derek O'Hagan , Nicholas Valiante
发明人： Derek O'Hagan , Nicholas Valiante
IPC分类号： A61K39/02 , A61K39/00 , A61K39/116 , A61K39/095 , A61K38/00 , C07K14/00
摘要： A combination of CpG oligonucleotides and polymer microparticles is an extremely effective adjuvant for Neisserial antigens. The invention therefore provides a composition comprising: (a) a Neisserial antigen; (b) a CpG oligonucleotide; and (c) a biodegradable polymer microparticle.
摘要翻译： CpG寡核苷酸和聚合物微粒的组合是奈瑟氏球菌抗原非常有效的佐剂。因此，本发明提供一种组合物，其包含：（a）奈维菌素抗原; （b）CpG寡核苷酸; 和（c）可生物降解的聚合物微粒。

6. 发明授权

US08541023B2 Immunogenic compositions containing phospholipid 有权
标题翻译：含有磷脂的免疫原性组合物
公开(公告)号：US08541023B2
公开(公告)日：2013-09-24
申请号：US13270107
申请日：2011-10-10
申请人： Derek O'Hagan
发明人： Derek O'Hagan
IPC分类号： A61K39/00 , A61K39/38 , A61K38/00 , A61K39/02 , A61K45/00 , A61K47/00 , A61K9/48 , A61K9/14 , A61K9/16
CPC分类号： A61K47/26 , A61K9/0019 , A61K9/10 , A61K9/1075 , A61K9/1676 , A61K9/19 , A61K9/5031 , A61K39/095 , A61K39/12 , A61K39/21 , A61K39/39 , A61K47/06 , A61K2039/545 , A61K2039/55555 , A61K2039/55561 , A61K2039/55566 , A61K2039/6093 , A61K2039/622 , C12N2740/16234
摘要： Immunogenic compositions containing phospholipid adjuvants, including microparticle and emulsion compositions. According to one aspect of the invention, an immunogenic microparticle composition is provided comprising: water; a polymer microparticle; an antigen adsorbed to the microparticle; and a phospholipid compound, e.g., a synthetic phospholipid compound comprising: (i) one or more phosphoryl groups independently selected from a phosphato group and a phosphodiester group; (ii) a plurality of linear alkane groups. According to another aspect of the invention an immunogenic emulsion composition is provided that comprises: water; a metabolizable oil; an emulsifying agent; an antigen; and a phospholipid compound, e.g., a synthetic phospholipid compound like that above. The emulsion composition is an oil-in-water emulsion having oil and aqueous phases, in which the oil phase is in the form of oil droplets, substantially all of which are less than 1 micron in diameter.
摘要翻译：含有磷脂佐剂的免疫原性组合物，包括微粒和乳剂组合物。根据本发明的一个方面，提供免疫原性微粒组合物，其包含：水; 聚合物微粒; 吸附在微粒上的抗原; 和磷脂化合物，例如合成磷脂化合物，其包含：（i）一个或多个独立地选自磷酸酯基和磷酸二酯基团的磷酰基; （ii）多个直链烷烃基团。根据本发明的另一方面，提供免疫原性乳剂组合物，其包含：水; 代谢油; 乳化剂; 抗原; 和磷脂化合物，例如如上所述的合成磷脂化合物。乳液组合物是具有油相和水相的水包油乳液，其中油相是油滴形式，其基本上都小于1微米直径。

7. 发明申请

US20120263753A1 BENZONAPHTHYRIDINE-CONTAINING VACCINES 有权
标题翻译：含有苯并噻嗪的疫苗
公开(公告)号：US20120263753A1
公开(公告)日：2012-10-18
申请号：US13377511
申请日：2010-06-10
申请人： Derek O'Hagan , Manmohan Singh , Siddhartha Jain , Sushma Kommareddy
发明人： Derek O'Hagan , Manmohan Singh , Siddhartha Jain , Sushma Kommareddy
IPC分类号： A61K39/39 , A61P37/04 , A61K39/02 , A61K39/00 , A61K39/12
CPC分类号： A61K39/39 , A61K2039/55511 , A61K2039/6093
摘要： The invention provides, inter alia, immunogenic compositions that comprise (a) a first antigen, (b) polymeric particles and (c) a benzonaphthyridine compound, which compositions elicits an immune response when administered to a vertebrate subject. The invention also provides, inter alia, methods of producing immunogenic compositions and methods for using immunogenic compositions (e.g., for treatment), among other benefits.
摘要翻译：本发明尤其提供了免疫原性组合物，其包含（a）第一抗原，（b）聚合物颗粒和（c）苯并萘啶化合物，该组合物在施用于脊椎动物受试者时引起免疫应答。本发明尤其提供产生免疫原性组合物的方法和使用免疫原性组合物（例如用于治疗）的方法以及其它益处。

8. 发明申请

US20120171244A1 MUCOSAL BOOSTING FOLLOWING PARENTERAL PRIMING 审中-公开
标题翻译：在下面的MUCOSAL升级
公开(公告)号：US20120171244A1
公开(公告)日：2012-07-05
申请号：US13366296
申请日：2012-02-04
申请人： Derek O'Hagan
发明人： Derek O'Hagan
IPC分类号： A61K39/00 , A61K39/095 , A61K39/102 , A61K39/09 , A61P31/04 , A61P31/12 , A61K39/21 , A61K39/12 , A61K39/29 , A61K39/155 , A61K39/145 , A61K39/245 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P35/00 , A61P37/04
CPC分类号： A61K39/385 , A61K9/0031 , A61K9/0034 , A61K9/0043 , A61K9/1647 , A61K39/00 , A61K39/0011 , A61K39/092 , A61K39/095 , A61K39/12 , A61K39/21 , A61K2039/53 , A61K2039/54 , A61K2039/541 , A61K2039/545 , A61K2039/55555 , A61K2039/55561 , A61K2039/57 , A61K2039/6093 , C12N2740/16134 , Y02A50/464
摘要： Mucosal immunization using one or more antigens following parenteral administration of the same or different antigens is described.
摘要翻译：描述了肠胃外给予相同或不同抗原后使用一种或多种抗原的粘膜免疫。

9. 发明授权

US08206749B1 Microemulsions with adsorbed macromolecules and microparticles 有权
公开(公告)号：US08206749B1
公开(公告)日：2012-06-26
申请号：US09914279
申请日：2000-02-09
申请人： Derek O'Hagan , Gary S. Ott , John Donnelly , Jina Kazzaz , Mildred Ugozzoli , Manmohan Singh , John Barackman
发明人： Derek O'Hagan , Gary S. Ott , John Donnelly , Jina Kazzaz , Mildred Ugozzoli , Manmohan Singh , John Barackman
IPC分类号： A61K9/50
CPC分类号： A61K39/39 , A61K9/1075 , A61K9/167 , A61K39/0208 , A61K39/21 , A61K39/245 , A61K39/29 , Y02A50/411 , Y02A50/471
摘要： Microparticles with adsorbent surfaces, methods of making such microparticles, and uses thereof, are disclosed. The microparticles comprise a polymer, such as a poly(α-hydroxy acid), a polyhydroxy butyric acid, a polycaprolactone, a polyorthoester, a polyanhydride, and the like, and are formed using cationic, anionic, or nonionic detergents. The surface of the microparticles efficiently adsorb biologically active macromolecules, such as DNA, polypeptides, antigens, and adjuvants. Also provided are compositions of an oil droplet emulsion having a metabolizable oil and an emulsifying agent. Immunogenic compositions having an immunostimulating amount of an antigenic substance, and an immunostimulating amount of an adjuvant composition are also provided. Methods of stimulating an immune response, methods of immunizing a host animal against a viral, bacterial, or parasitic infection, and methods of increasing a Th1 immune response in a host animal by administering to the animal an immunogenic composition of the microparticles, and/or microemulsions of the invention, are also provided.

10. 发明申请

US20110150923A1 MUCOSAL MENINGOCOCCAL VACCINES 审中-公开
标题翻译：粘膜肉芽孢杆菌疫苗
公开(公告)号：US20110150923A1
公开(公告)日：2011-06-23
申请号：US13036007
申请日：2011-02-28
申请人： Giuseppe Del Giudice , Barbara Baudner , Derek O'Hagan
发明人： Giuseppe Del Giudice , Barbara Baudner , Derek O'Hagan
IPC分类号： A61K39/095 , A61K39/108 , A61P31/04 , A61K39/295
CPC分类号： A61K39/095 , A61K2039/543 , A61K2039/55544 , A61K2039/55583 , A61K2039/6037
摘要： The invention provides immunogenic compositions for mucosal delivery comprising capsular saccharides from at least two of serogroups A, C, W135 and Y of N. meningitidis. It is preferred that the capsular saccharides in the compositions of the invention are conjugated to carrier protein(s) and/or are oligosaccharides. Conjugated oligosaccharide antigens are particularly preferred. The invention also provides immunogenic compositions comprising (a) a capsular saccharide antigen from serogroup C of N. meningitidis, and (b) a chitosan adjuvant. The composition preferably comprises (c) one or more further antigens and/or (d) one or more further adjuvants. The compositions are particularly suitable for mucosal delivery, including intranasal delivery. The use of chitosan and/or detoxified ADP-ribosylating toxin adjuvants enhances anti-meningococcal mucosal immune responses and can shift the Th1/Th2 bias of the responses.
摘要翻译：本发明提供用于粘膜递送的免疫原性组合物，其包含来自脑膜炎奈瑟菌脑膜炎的血清群A，C，W135和Y的至少两个的荚膜糖。本发明组合物中的荚膜糖优选与载体蛋白结合，和/或是寡糖。共轭寡糖抗原是特别优选的。本发明还提供免疫原性组合物，其包含（a）来自脑膜炎奈瑟氏球菌的血清群C的荚膜糖抗原和（b）壳聚糖佐剂。组合物优选包含（c）一种或多种另外的抗原和/或（d）一种或多种另外的佐剂。组合物特别适用于粘膜递送，包括鼻内递送。使用壳聚糖和/或解毒的ADP-核糖基化毒素佐剂增强了抗脑膜炎球菌粘膜免疫应答，并且可以改变反应的Th1 / Th2偏差。

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