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1. 发明申请

WO2018137627A1 阿立哌唑及其衍生物的缓释组合物与该缓释组合物的制备方法审中-公开
公开(公告)号：WO2018137627A1
公开(公告)日：2018-08-02
申请号：PCT/CN2018/073897
申请日：2018-01-24
申请人：广州帝奇医药技术有限公司
发明人：刘锋 , 赖树挺 , 曹付春 , 郑阳 , 连远发
IPC分类号： A61K9/16 , A61K9/54 , A61K31/496 , A61K47/34 , A61P25/18
CPC分类号： A61K9/0002 , A61K9/1641 , A61K31/496
摘要：一种阿立哌唑及其衍生物的缓释组合物及其制备方法，所述缓释组合物的非溶剂型制备原料包含阿立哌唑和水难溶性聚合物。所述缓释组合物具有良好的释放性能，无明显释放延迟期或突释现象，并能在数周或以上的时间内维持稳定的血药浓度，且具有较好的稳定性。

2. 发明申请

WO2017180590A1 BIODEGRADABLE IN SITU FORMING MICROPARTICLES AND METHODS FOR PRODUCING THE SAME 审中-公开
标题翻译：可生物降解的原位形成微粒及其制备方法
公开(公告)号：WO2017180590A1
公开(公告)日：2017-10-19
申请号：PCT/US2017/026954
申请日：2017-04-11
申请人： SOUTHERN RESEARCH INSTITUTE
发明人： HUDSON, Michael, E.
IPC分类号： A61K31/095 , A61L27/52
CPC分类号： A61K9/1075 , A61K9/0024 , A61K9/1641 , A61K9/1647 , A61K9/1694
摘要： In accordance with the present invention, disclosed herein is a kit comprising a first mixture comprising a pharmaceutically acceptable polar liquid and a fully or nearly fully dissolved biodegradable polymer; a second mixture comprising a pharmaceutically acceptable non-polar liquid; and a mixing device configured to mix the first mixture and second mixture, thereby forming a droplet comprising the biodegradable polymer. Also disclosed herein are methods of producing a microparticle in vivo in a subject.
摘要翻译：根据本发明，本文公开了包含第一混合物和第二混合物的试剂盒，所述第一混合物包含药学上可接受的极性液体和完全或几乎完全溶解的生物可降解聚合物; 包含药学上可接受的非极性液体的第二混合物; 以及配置为混合第一混合物和第二混合物，从而形成包含生物可降解聚合物的液滴的混合装置。本文还公开了在受试者体内产生微粒的方法。

3. 发明申请

WO2017106214A1 AMORPHOUS ONAPRISTONE COMPOSITIONS AND METHODS OF MAKING THE SAME 审中-公开
标题翻译：非晶蛋白组合物及其制备方法
公开(公告)号：WO2017106214A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/066420
申请日：2016-12-13
申请人： ARNO THERAPEUTICS, INC.
发明人： BRITTAIN, Harry G. , PRONIUK, Stefan
IPC分类号： A61K9/127 , A61K31/565 , A61K31/569 , A61K31/575 , A61K38/00 , A61K45/06 , C07J41/00
CPC分类号： A61K31/575 , A61K9/146 , A61K9/1635 , A61K9/1641 , A61K9/1682 , A61K9/1694 , C07B2200/13 , C07J41/0055 , C07J41/0083
摘要： Amorphous forms of onapristone and methods of making such amorphous forms are provided. Amorphous forms can be characterized by their X-ray powder diffraction patterns and other properties.
摘要翻译：提供了非培养形式的奥那司酮和制备这种无定形形式的方法。无定形形式可以通过其X-射线粉末衍射图案和其他性质来表征。

4. 发明申请

WO2017105990A1 PH-RESPONSIVE MUCOADHESIVE POLYMERIC ENCAPSULATED MICROORGANISMS 审中-公开
标题翻译： PH响应性粘附聚合物包裹的微生物
公开(公告)号：WO2017105990A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/065535
申请日：2016-12-08
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY
发明人： ANSELMO, Aaron, C. , LANGER, Robert, S. , JAKLENEC, Ana
IPC分类号： A61K9/50 , A23L33/135 , A61K35/741 , A61K36/36 , A61K35/76 , A61K39/00
CPC分类号： A61K9/1652 , A23L33/135 , A61K9/1641 , A61K9/5026 , A61K9/5036 , A61K9/5073 , A61K9/5089 , A61K35/741 , A61K35/742 , A61K35/745 , A61K35/747 , A61K35/76 , A61K36/064 , A61K39/07 , A61K39/12 , A61K2039/52 , A61K2039/525 , A61K2039/542
摘要： Methods of encapsulating microorganisms, or components thereof, for targeted enteric delivery to an animal host have been developed. In particular, the encapsulation provides a prolonged survival, extended retention and a pH-sensitive release of the encapsulated microorganisms or antigenic components thereof at targeted sites within the gastrointestinal tract. The formulations are useful for diagnostic, therapeutic and prophylactic purposes and can alter a host's microbial composition associated with a condition or a disease state.
摘要翻译：已经开发了包封微生物或其组分用于靶向肠递送至动物宿主的方法。具体而言，包封提供了胃肠道内靶向部位的包封的微生物或其抗原性组分的延长的存活期，延长的滞留期和pH敏感性释放。该制剂可用于诊断，治疗和预防目的，并可改变宿主与病症或疾病状态相关的微生物组成。

5. 发明申请

WO2017103677A1 COMPLEXES OF CELECOXIB AND ITS SALTS AND DERIVATIVES PROCESS FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：塞来昔布及其盐和衍生物的配制物及其制备方法和含有它们的药物组合物
公开(公告)号：WO2017103677A1
公开(公告)日：2017-06-22
申请号：PCT/IB2016/001893
申请日：2016-12-15
申请人： DRUGGABILITY TECHNOLOGIES IP HOLDCO LIMITED
发明人： ANGI, Erzsébet Réka , JORDÁN, Tamás , KÁRPATI, Richard Balázs , PATYI, Gergö , BASA-DÉNES, Orsolya , SOLYMOSI, Tamás , ÖTVÖS, Zsolt , MOLNÁR, Lázló , GLAVINAS, Hristos , FILIPCSEI, Genovéva
IPC分类号： A61K31/415 , A61K31/635 , A61K45/06 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/51
CPC分类号： A61K31/635 , A61K9/0056 , A61K9/006 , A61K9/0095 , A61K9/10 , A61K9/146 , A61K9/1635 , A61K9/1641 , A61K9/5138 , A61K9/5146 , A61K31/415 , A61K45/06 , A61K47/20 , A61K2300/00 , B01F3/00 , C07B2200/13 , C07D231/10
摘要： Disclosed herein are stable complexes with controlled particle size, increased apparent solubility and increased dissolution rate comprising as active compound Celecoxib, its salts, or derivatives thereof, which is useful in the treatment of osteoarthritis, rheumatoid arthritis, juvenile rheumatoid arthritis, ankylosing spondylitis, acute pain especially in cancer related acute pain, primary dysmenorrhea. More specifically, the complexes possess instantaneous redispersibility, increased apparent solubility and permeability that provide faster onset of action for acute pain relief and lower GI related side effects. Further disclosed are methods of formulating and manufacturing the complexes described herein, pharmaceutical compositions, and uses and methods of treatment.
摘要翻译：本文公开了稳定的复合物，其具有可控的粒度，增加的表观溶解度和增加的溶解速率，其包含作为活性化合物塞来考昔，其盐或其衍生物，其可用于治疗骨关节炎，类风湿性关节炎，幼年型类风湿关节炎，强直性脊柱炎，急性疼痛特别是与癌症相关的急性疼痛，原发性痛经。更具体地说，该配合物具有瞬时再分散性，增加的表观溶解度和渗透性，为急性疼痛缓解和较低GI相关副作用提供更快的起效作用。还公开了配制和制造本文所述复合物的方法，药物组合物，以及治疗方法和用途。

6. 发明申请

WO2017049245A3 COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于治疗药物的细胞内递送的化合物和组合物
公开(公告)号：WO2017049245A3
公开(公告)日：2017-05-18
申请号：PCT/US2016052352
申请日：2016-09-16
申请人： MODERNATX INC
发明人： BENENATO KERRY E , KUMARASINGHE ELLALAHEWAGE SATHYAJITH , CORNEBISE MARK
IPC分类号： C07C229/12 , A61K9/127 , C07C237/04 , C07C237/06 , C07C271/20 , C07C279/12 , C07C279/28 , C07C279/32 , C07C311/07 , C07C311/49 , C07C321/14 , C07D207/27 , C07D233/72 , C07D249/04 , C07D263/20 , C07D265/33 , C07D271/06 , C07D271/10 , C07D277/38
CPC分类号： A61K48/0033 , A61K9/0019 , A61K9/0043 , A61K9/0073 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/1617 , A61K9/1641 , A61K9/5123 , A61K9/5146 , A61K31/7105 , A61K38/1725 , A61K38/1816 , A61K47/543 , A61K47/6911 , A61K48/00 , A61K48/005 , C07C227/16 , C07C227/18 , C07C229/12 , C07C229/16 , C07C233/36 , C07C235/10 , C07C255/24 , C07C271/20 , C07C275/14 , C07C279/12 , C07C279/24 , C07C279/28 , C07C279/32 , C07C311/05 , C07C335/08 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D207/27 , C07D233/72 , C07D249/04 , C07D263/20 , C07D265/33 , C07D271/06 , C07D271/10 , C07D277/38 , C07F9/091 , C07K14/505
摘要： The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
摘要翻译：本公开的特征在于新颖的脂质和涉及其的组合物。纳米颗粒组合物包含新型脂质以及其他脂质，例如磷脂，结构脂质和PEG脂质。纳米颗粒组合物还包含治疗剂和/或预防剂如RNA，可用于将治疗剂和/或预防剂递送至哺乳动物细胞或器官以例如调节多肽，蛋白质或基因表达。

7. 发明申请

WO2017066626A1 INJECTABLE NEUROSTEROID FORMULATIONS CONTAINING NANOPARTICLES 审中-公开
标题翻译：含纳米颗粒的注射用神经调节制剂
公开(公告)号：WO2017066626A1
公开(公告)日：2017-04-20
申请号：PCT/US2016/057120
申请日：2016-10-14
申请人： MARINUS PHARMACEUTICALS, INC.
发明人： ZHANG, Mingbao , GLOWAKY, Raymond C. , CZEKAI, David
IPC分类号： A61K9/00 , A61K47/24 , A61K47/32 , A61K47/36 , A61K9/10 , A61K9/19 , A61K9/51 , A61K31/57 , A61P25/08
CPC分类号： A61K31/573 , A61K9/0019 , A61K9/10 , A61K9/146 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K9/1652 , A61K9/19 , A61K9/5138 , A61K9/5161 , A61K31/57 , A61K45/06 , A61K47/24 , A61K47/32 , A61K47/36 , A61K2300/00
摘要： The disclosure provides an injectable neurosteroid nanoparticle formulation comprising nanoparticles having a D50 of less than 2000 nm the nanoparticles comprising a neurosteroid of Formula I, where the variables R 1 -R 9 and X are defined herein and at least one surface stabilizer. The surface stabilizer can be a polymeric surface stabilizer such as hydroxyethyl starch, dextran, or povidone. The injectable neurosteroid nanoparticle formulation can be an intravenous formulation. The disclosure also provides a lyophilized powder of the injectable neurosteroid nanoparticle formulation that can be reconstituted in an aqueous solution prior to administration. The disclosure provides injectable neurosteroid nanoparticle formulations and dry powders of such formulations that have been sterilized by ebeam irradiation. The disclosure provides a method of treating a patient having a seizure disorder, stroke, or traumatic brain injury, comprising administering an effective amount of the injectable neurosteroid nanoparticle formulation. The disclosure also provides combination methods in which the injectable neurosteroid nanoparticle formulation is a first active agent that is administered in combination with at least one additional active agent.
摘要翻译：本公开提供了包含D50小于2000nm的纳米颗粒的可注射的神经甾体纳米颗粒制剂，所述纳米颗粒包含式I的神经甾体，其中变量R 1 -R 4，本文定义了X和X以及至少一个表面稳定剂。表面稳定剂可以是聚合物表面稳定剂，例如羟乙基淀粉，葡聚糖或聚维酮。可注射的神经类固醇纳米颗粒制剂可以是静脉内制剂。本公开还提供了可在施用前在水溶液中重构的可注射的神经甾体纳米颗粒制剂的冻干粉末。本公开提供了可注射的神经甾体纳米粒子制剂和已经通过电子束照射灭菌的这种制剂的干粉。本公开提供了治疗患有癫痫，中风或创伤性脑损伤的患者的方法，其包括施用有效量的可注射的神经类固醇纳米颗粒制剂。本公开内容还提供了组合方法，其中可注射的神经甾体纳米粒子制剂是与至少一种另外的活性剂组合施用的第一活性剂。

8. 发明申请

WO2017062871A1 CROSSLINKED PARTICLES 审中-公开
标题翻译：交联颗粒
公开(公告)号：WO2017062871A1
公开(公告)日：2017-04-13
申请号：PCT/US2016/056135
申请日：2016-10-07
申请人： LE DÉVÉDEC, Frantz , ALLEN, Christine Jane , STEVENS, David Michael , RAGER-AGUIAR, Dean James , RUCKH, Timothy Tordella , ELMQUIST, Carl Eric
发明人： LE DÉVÉDEC, Frantz , ALLEN, Christine Jane , STEVENS, David Michael , RAGER-AGUIAR, Dean James , RUCKH, Timothy Tordella , ELMQUIST, Carl Eric
IPC分类号： C08J9/16 , C08J9/22
CPC分类号： A61K9/5123 , A61K9/1641 , A61K9/5146 , A61K31/122 , A61K31/337 , A61K31/573 , A61K31/58
摘要： Disclosed are crosslinked particles (e.g., microparticles) that are capable of storing and releasing drugs. The particles can be macroparticles, microparticles, or nanoparticles and can be composed of polyester backbones. The particles can be loaded with a drug. The particles can degrade in vivo to release the drug. The particles can be prepared by crosslinking functionalized polyester backbones and loaded with a given drug. The particles of the present disclosure can be injected with a syringe. In some embodiments, the particles of the present disclosure are administered in connection with a surgery and release the drug after the site of the surgery for a period of 1-6 months.
摘要翻译：公开了能够储存和释放药物的交联颗粒（例如微粒）。颗粒可以是大颗粒，微粒或纳米颗粒，并且可以由聚酯主链组成。颗粒可以装载药物。颗粒可在体内降解以释放药物。颗粒可以通过交联官能化的聚酯主链并加载给定的药物来制备。本公开的颗粒可以用注射器注射。在一些实施方案中，本公开的颗粒与手术相关联地施用并在手术部位后释放药物1-6个月。

9. 发明申请

WO2017049245A2 COMPOUNDS AND COMPOSITIONS FOR INTRACELLULAR DELIVERY OF THERAPEUTIC AGENTS 审中-公开
标题翻译：用于细胞内递送治疗药物的化合物和组合物
公开(公告)号：WO2017049245A2
公开(公告)日：2017-03-23
申请号：PCT/US2016/052352
申请日：2016-09-16
申请人： MODERNATX, INC.
发明人： BENENATO, Kerry, E. , KUMARASINGHE, Ellalahewage, Sathyajith , CORNEBISE, Mark
IPC分类号： C07C229/12 , C07D233/72 , A61K9/127 , C07C271/20 , C07C279/12 , C07C279/28 , C07C279/32 , C07C311/07 , C07C311/49 , C07C321/14 , C07D249/04 , C07D263/20 , C07C237/04 , C07C237/06 , C07D265/33 , C07D271/06 , C07D271/10 , C07D207/27 , C07D277/38
CPC分类号： C07C229/12 , A61K9/0019 , A61K9/0043 , A61K9/0073 , A61K9/127 , A61K9/1271 , A61K9/1272 , A61K9/1617 , A61K9/1641 , A61K9/5123 , A61K9/5146 , A61K31/7105 , A61K38/1725 , A61K38/1816 , A61K47/543 , A61K47/6911 , A61K48/00 , A61K48/0033 , A61K48/005 , C07C227/16 , C07C227/18 , C07C229/16 , C07C233/36 , C07C235/10 , C07C255/24 , C07C271/20 , C07C275/14 , C07C279/12 , C07C279/24 , C07C279/28 , C07C279/32 , C07C311/05 , C07C335/08 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07C2601/18 , C07D207/27 , C07D233/72 , C07D249/04 , C07D263/20 , C07D265/33 , C07D271/06 , C07D271/10 , C07D277/38 , C07F9/091 , C07K14/505
摘要： The disclosure features novel lipids and compositions involving the same. Nanoparticle compositions include a novel lipid as well as additional lipids such as phospholipids, structural lipids, and PEG lipids. Nanoparticle compositions further including therapeutic and/or prophylactics such as RNA are useful in the delivery of therapeutic and/or prophylactics to mammalian cells or organs to, for example, regulate polypeptide, protein, or gene expression.
摘要翻译：本公开的特征在于新颖的脂质和涉及其的组合物。纳米颗粒组合物包括新型脂质以及其它脂质，例如磷脂，结构脂质和PEG脂质。进一步包括治疗和/或预防因素例如RNA的纳米颗粒组合物可用于向哺乳动物细胞或器官递送治疗和/或预防剂以例如调节多肽，蛋白质或基因表达。

10. 发明申请

WO2017042325A1 PROTECTING ORAL OVERDOSE WITH ABUSE DETERRENT IMMEDIATE RELEASE FORMULATIONS 审中-公开
标题翻译：保护口服过量，免除感染立即释放配方
公开(公告)号：WO2017042325A1
公开(公告)日：2017-03-16
申请号：PCT/EP2016/071287
申请日：2016-09-09
申请人： GRÜNENTHAL GMBH
发明人： WENING, Klaus , SCHWIER, Sebastian , BERTRAM, Ulrike
IPC分类号： A61K9/16 , A61K9/20 , A61K31/167 , A61K31/485 , A61K9/48 , A61K31/137
CPC分类号： A61K9/2022 , A61K9/1641 , A61K9/1694 , A61K9/2054 , A61K9/4808 , A61K31/137 , A61K31/167 , A61K31/485
摘要： The invention relates to a pharmaceutical dosage form which is particularly useful for the prevention of an overdose of the pharmacologically active ingredient contained therein after accidental or intentional simultaneous administration of a plurality of the dosage forms containing an overall supratherapeutic dose of the pharmacologically active ingredient.
摘要翻译：本发明涉及药物剂型，其特别可用于在意外或故意同时施用含有总体超治疗剂量的药理学活性成分的多种剂型之后防止其中所含的药理学活性成分过量。

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