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1. 发明申请

WO2019136269A1 COMPOSITIONS COMPRISING CO-SELECTED MICROBIOTA AND METHODS FOR USE THEREOF 审中-公开
公开(公告)号：WO2019136269A1
公开(公告)日：2019-07-11
申请号：PCT/US2019/012376
申请日：2019-01-04
申请人： NUBIYOTA LLC
发明人： ALLEN-VERCOE, Emma
IPC分类号： A61K9/00 , A61K9/14 , A61K35/74
CPC分类号： A61K9/4858 , A61K9/4891 , A61K35/74
摘要： Anhydrous compositions comprising a co-selected microbiota and methods for using same to treat disorders associated with dysbiosis (an imbalance of the microbial community inhabiting a subject or inhabiting a particular tissue in a subject) are described herein. In particular, anhydrous compositions comprising a co-selected microbiota and methods for treating gastrointestinal disorders associated with dysbiosis are envisioned. The use of such anhydrous compositions comprising a co-selected microbiota for treating disorders associated with dysbiosis (e.g., gastrointestinal disorders associated with dysbiosis) and the use of such anhydrous compositions comprising a co-selected microbiota in the preparation of a medicament for treating disorders associated with dysbiosis (e.g., gastrointestinal disorders associated with dysbiosis) are also embodied herein.

2. 发明申请

WO2019014668A1 FORMULATIONS, METHODS, KIT, AND DOSAGE FORMS FOR IMPROVED STABILITY OF AN ACTIVE PHARMACEUTICAL INGREDIENT 审中-公开
公开(公告)号：WO2019014668A1
公开(公告)日：2019-01-17
申请号：PCT/US2018/042264
申请日：2018-07-16
申请人： ASANA BIOSCIENCES, LLC
发明人： SHAH, Navnit , SANDHU, Harpreet , CHATTERJI, Ashish , USANSKY, Helen , DENIS, Louis , RAO, Niranjan , TOKER, Sarper
IPC分类号： A61K31/505 , A61K31/517 , A61K31/519 , C07D239/94 , C07D403/02 , C07D403/14
CPC分类号： A61K9/1652 , A61K9/0053 , A61K9/0056 , A61K9/1611 , A61K9/1617 , A61K9/1623 , A61K9/1694 , A61K9/2013 , A61K9/2018 , A61K9/2054 , A61K9/28 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K9/50 , A61K9/5015 , A61K9/5026 , A61K9/5042 , C07B2200/13 , C07D471/04
摘要： Embodiments of the disclosure relate generally to formulations, methods, kits, and dosage forms for improved stability of an active pharmaceutical ingredient, wherein the active ingredient comprises a compound of the formula:(I) wherein X is N, Y is H or optionally substituted C 1 -C 6 alkyl; R 4 is morpholine optionally substituted with by C 1 -C 6 alkyl; R 7 is C 1 -C 6 alkyl optionally substituted by one or more F; R 8' is halogen; and R 6 is (II),, wherein R 10 is H, C 1 ,-C 6 alkyl, halogen, CN or CF 3 ; R 12 is H or halogen; R 13 is H, halogen or C1-C 6 alkyl; and R 17 is H, C 1 -C 6 alkyl, (C 1 -C 6 alkyl)-NH 2 ; and, pharmaceutically acceptable salts and free bases thereof, wherein the active ingredient remains in substantially amorphous form after storage of the pharmaceutical formulation for a predetermined time and conditions. In one embodiment the formulations, methods, kits and dosage forms comprising the active pharmaceutical ingredient with improved stability can be used in the treatment of a condition characterized by the dysregulation of one of both of the RAS/RAF/MEK/ERK and PI3 K/AKT/PTEN/mTOR pathways.

3. 发明申请

WO2019011415A1 SOLUBILISAT MIT CURCUMIN, XANTHOHUMOL UND SÜßHOLZWURZELEXTRAKT 审中-公开
公开(公告)号：WO2019011415A1
公开(公告)日：2019-01-17
申请号：PCT/EP2017/067382
申请日：2017-07-11
申请人： AQUANOVA AG
发明人： BEHNAM, Dariush
IPC分类号： A61K36/9066 , A61K31/12 , A61K36/185 , A61K36/484 , A61K47/26 , A61K9/107
CPC分类号： A61K31/12 , A23L2/00 , A61K9/1075 , A61K9/4858 , A61K31/353 , A61K36/185 , A61K36/484 , A61K36/9066 , A61K47/10 , A61K47/26 , A61K2300/00
摘要： Um eine Formulierung bereitzustellen, welche die gesundheitsfördernden bis heilenden Eigenschaften von Curcumin, Xanthohumol und Süßholzwurzelextrakt, insbesondere Glavonoid, dem menschlichen oder tierischen Organismus zugänglich macht, stellt die Erfindung ein Solubilisat zur Verfügung enthaltend Xanthohumol mit einem Anteil von kleiner oder gleich 10 Gew.-%, bevorzugt kleiner oder gleich 6 Gew.-%, besonders bevorzugt 2,7 Gew.-% bis 4,8 Gew.-% und Curcumin mit einem Anteil von kleiner oder gleich 10 Gew.- %, bevorzugt kleiner oder gleich 6 Gew.-%, besonders bevorzugt 2,3 Gew.-% bis 4,8 Gew.-% und Fluid enthaltend Süßholzwurzelextrakt, insbesondere einer hydrophobe Lösung eines Süßholzwurzelextraktes, bevorzugt Glavonoid und/oder Glabridin mit einem Anteil von kleiner oder gleich 10 Gew.-%, bevorzugt kleiner oder gleich 8 Gew.-%, besonders bevorzugt 3,3 Gew.-% bis 5 Gew.-% zumindest einem Emulgator mit einem HLB-Wert im Bereich zwischen 13 und 18, insbesondere Polysorbat 80 oder Polysorbat 20 oder einer Mischung aus Polysorbat 20 und Polysorbat 80.

4. 发明申请

WO2017137468A1 STABLE SOLID PHARMACEUTICAL FORMULATIONS CONTAINING 2-(2-NITRO-4-TRIFLUOROMETHYLBENZOYL)-1,3-CYCLOHEXANEDIONE 审中-公开
标题翻译：含有2-（2-硝基-4-三氟甲基苯甲酰基）-1,3-环己二酮的稳定的固体药物制剂
公开(公告)号：WO2017137468A1
公开(公告)日：2017-08-17
申请号：PCT/EP2017/052805
申请日：2017-02-09
申请人： DIPHARMA S.A.
发明人： CONTI, Chiara , GIAMMILLARI, Salvatore Agostino , MACCARI, Giuseppe
IPC分类号： A61K9/48 , A61K31/122
CPC分类号： A61K9/4866 , A61K9/4858 , A61K31/122
摘要： The present invention relates to highly stable drug dosage forms comprising. The invention also contemplates said highly stable drug dosage forms for the treatment of diseases where inhibition of 4-hydroxyphenylpyruvate dioxygenase 5 will result at improving the health of the patient.
摘要翻译：本发明涉及高度稳定的药物剂型，其包含。本发明还考虑到所述高度稳定的药物剂型用于治疗疾病，其中抑制4-羟基苯基丙酮酸双加氧酶5将导致患者健康的改善。

5. 发明申请

WO2017116190A1 PHARMACEUTICAL COMPOSITION COMPRISING DUTASTERIDE AND PROPYLENE GLYCOL MONOLAURATE AND PREPARATION METHOD OF THE SAME 审中-公开
标题翻译：包含DUTASTERIDE和丙二醇单月桂酸酯的药物组合物及其制备方法
公开(公告)号：WO2017116190A1
公开(公告)日：2017-07-06
申请号：PCT/KR2016/015533
申请日：2016-12-29
申请人： YUYU PHARMA, INC. , AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
发明人： BAIK, Taegon , KIM, Seyeon , AHN, Kyeongjin , KIM, Ju-hee , PARK, Young-joon
IPC分类号： A61K9/48 , A61K47/10 , A61K47/14 , A61K31/568
CPC分类号： A61K9/4866 , A61K9/4858 , A61K31/568
摘要： The present invention relates to a pharmaceutical composition comprising dutasteride and propylene glycol monolaurate, which improves the stability of dutasteride, which is a poorly soluble drug as a 5-alpha reductase inhibitor, and a process for its preparation. More particularly, the present invention also relates to a capsule formulation which is smaller in size than a commercial dutasteride capsule formulation (AVODART ® ), but has the equivalent dissolution rate by preparing a pharmaceutical composition comprising propylene glycol monolaurate and dutasteride, which can improve the stability of the dutasteride. A dutasteride formulation having enhanced patient's compliance and improved stability and a method for producing the same are provided.
摘要翻译：本发明涉及包含度他雄胺和丙二醇单月桂酸酯的药物组合物，其提高作为5-α还原酶抑制剂的难溶药物度他定（dutasteride）的稳定性，及其制备方法。更具体地说，本发明还涉及胶囊制剂，其尺寸比市售度他雄胺胶囊制剂（AVODART TM）小，但具有相同的溶解速率，通过制备包含丙二醇单月桂酸酯和度他雄胺，这可以提高度他雄胺的稳定性。提供了具有增强的患者依从性和改善的稳定性的度他雄胺制剂及其制备方法。

6. 发明申请

WO2017112894A1 METHODS FOR TREATING IMMUNODEFICIENCY DISEASE 审中-公开
标题翻译：治疗免疫缺陷病的方法
公开(公告)号：WO2017112894A1
公开(公告)日：2017-06-29
申请号：PCT/US2016/068394
申请日：2016-12-22
申请人： X4 PHARMACEUTICALS, INC.
发明人： ARBEIT, Robert M. , RAGAN, Paula Marie
IPC分类号： A61K31/395 , A61K31/47 , A61K31/4709 , A61K31/4725 , C07D235/14 , C07D401/04
CPC分类号： A61K31/4709 , A61K9/0053 , A61K9/485 , A61K9/4858 , A61K9/4866 , C07D235/14 , C07D401/04 , C07D401/12
摘要： The present invention relates to methods of treating patients with WHIM syndrome or related disorders, such as myelokathexis, in which X4P-001 is administered in order to reduce the activity of CXCR4. The methods demonstrate surprising effectiveness, with comparatively little toxicity.
摘要翻译：本发明涉及治疗患有WHIM综合征或相关病症（例如骨髓移植）的患者的方法，其中施用X4P-001以降低CXCR4的活性。这些方法表现出惊人的有效性，毒性相对较小。

7. 发明申请

WO2017106859A1 COVALENT HETEROBIVALENT ANTIBODY INHIBITORS AND LIGANDS 审中-公开
标题翻译：共价多分子抗体抑制剂和配体
公开(公告)号：WO2017106859A1
公开(公告)日：2017-06-22
申请号：PCT/US2016/067588
申请日：2016-12-19
申请人： UNIVERSITY OF NOTRE DAME DU LAC
发明人： BILGICER, Zihni Basar , DEAK, Peter Edward , KIZILTEPE BILGICER, Tanyel , HANDLOGTEN, Michael William , ASHLEY, Jonathan Darryl
IPC分类号： A61K9/127 , A61K38/05 , A61K38/07 , C07K16/46
CPC分类号： A61K9/4866 , A61K9/0014 , A61K9/0019 , A61K9/0073 , A61K9/2018 , A61K9/2027 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K47/02 , A61K47/10 , A61K47/54 , A61K47/62
摘要： The invention provides a strategy for site specific covalent modification of antibodies using a specialized targeting covalent heterobivalent ligand (cHBL), and corresponding design for a covalent heterobivalent inhibitor (cHBI) that can be used to prevent Immunoglobulin E (IgE) mediated allergic reactions triggered by drug molecules, according to one embodiment. These molecules contain four important components: (1) an IgE antigen binding site (ABS) ligand that can be a mimotope for the allergen protein, a small molecule, or a peptidomimetic, (2) an appropriate linker, which can be any flexible or rigid chemical linker, providing spacing between the ABS binder and the other moieties, (3) a nucleotide binding site (NBS) ligand, and (4) a reactive moiety to form a covalent link with an amino acid side chain of target IgE antibodies.
摘要翻译：本发明提供了使用专门的靶向共价异二价配体（cHBL）对抗体进行位点特异性共价修饰的策略，以及可用于预防免疫球蛋白E的共价异二价抑制剂（cHBI）的相应设计（IgE）介导的由药物分子触发的变态反应。这些分子含有四个重要组分：（1）可以是变应原蛋白，小分子或肽模拟物的模拟表位的IgE抗原结合位点（ABS）配体，（2）适当的接头，其可以是任何柔性的或（3）核苷酸结合位点（NBS）配体，以及（4）与靶IgE抗体的氨基酸侧链形成共价连接的反应性部分，提供ABS粘合剂与其他部分之间的间隔。

8. 发明申请

WO2017095736A1 ASPIRIN SOFT GELATIN CAPSULE AS A SINGLE ACTIVE OR IN COMBINATION WITH OTHER ACTIVES 审中-公开
标题翻译：阿司匹林软明胶胶囊作为单一主动或与其他活动组合使用
公开(公告)号：WO2017095736A1
公开(公告)日：2017-06-08
申请号：PCT/US2016/063845
申请日：2016-11-28
申请人： R.P. SCHERER TECHNOLOGIES, LLC
发明人： AHMAD, Humera , LIN, Jing , GULLAPALLI, Ram
IPC分类号： A61K9/48 , A61K9/50 , A61K47/40 , A61K31/616 , A23L33/10 , A23L33/135 , A23L33/15 , A23P10/35
CPC分类号： A61K31/616 , A61K9/4858
摘要： A soft gelatin capsule is provided that has a shell and a liquid fill encapsulated therein. The liquid fill comprises at least one oil, at least one surfactant, and a moisture sensitive pharmaceutical and/or a moisture sensitive dietary supplement dispersed in the oil. A moisture barrier may be included between the shell and the liquid fill.
摘要翻译：提供了一种软明胶胶囊，其具有包封在其中的壳和液体填充物。液体填充物包含至少一种油，至少一种表面活性剂和分散在油中的湿度敏感药物和/或湿度敏感膳食补充剂。壳体和液体填充物之间可能包含防潮层。

9. 发明申请

WO2017054754A1 ORAL TAXANE COMPOSITIONS AND METHODS 审中-公开
标题翻译：口服紫杉醇组合物和方法
公开(公告)号：WO2017054754A1
公开(公告)日：2017-04-06
申请号：PCT/CN2016/100807
申请日：2016-09-29
申请人： ATHENEX HK INNOVATIVE LIMITED
发明人： CHAN, Denise S.B. , LEE, Ming Tsung , YOON, Weng Li , LAU, Johnson Yiu-Nam
IPC分类号： A61K31/337 , A61K9/10 , A61P35/00
CPC分类号： A61K31/337 , A61K9/0053 , A61K9/4858 , A61K31/4725 , A61K45/06 , A61K47/12 , A61K47/26 , A61K47/44 , A61K2300/00
摘要： A pharmaceutical composition comprises a taxane (e.g., paclitaxel, docetaxel, cabazitaxel, larotaxel, ortataxel, and/or tesetaxel) in a mixture of first and second surfactants. The absorption of the taxane is increased from the pharmaceutical composition is greater than the sum of the absorption of docetaxel from either the first or the second surfactant. The increase in absorption is especially enhanced when the ratio of the first surfactant to the second surfactant in the pharmaceutical composition is between 60:40 and 85:15 by weight, and the total surfactant weight does not exceed 98％of the total weight. Polysorbate 80, polysorbate 20, and caprylocaproyl polyoxylglycerides serve as suitable first surfactants, and polysorbate 80 or polyethyoxylated castor oil serve as suitable second surfactants. The stability of the pharmaceutical composition may be enhanced by further including a stabilizer (e.g., citric acid and/or ascorbic acid).
摘要翻译：药物组合物包含在第一和第二表面活性剂的混合物中的紫杉烷（例如紫杉醇，多西紫杉醇，卡巴他赛，拉罗哌赛，奥他他和/或替西他赛）。紫杉烷的吸收从药物组合物的增加大于多西他赛从第一或第二表面活性剂的吸收的总和。当药物组合物中第一表面活性剂与第二表面活性剂的重量比在60:40至85:15之间时，吸收的增加尤其增加，总表面活性剂重量不超过总重量的98％。聚山梨醇酯80，聚山梨醇酯20和辛酰己酰基聚氧乙烯甘油酯用作适合的第一表面活性剂，聚山梨醇酯80或聚乙氧基化蓖麻油用作合适的第二表面活性剂。通过进一步包括稳定剂（例如柠檬酸和/或抗坏血酸）可以增强药物组合物的稳定性。

10. 发明申请

WO2017048702A1 SOLID FORMS OF ISOQUINOLINONE DERIVATIVES, PROCESS OF MAKING, COMPOSITIONS COMPRISING, AND METHODS OF USING THE SAME 审中-公开
标题翻译：异喹啉酮衍生物的固体形式，制备方法，包含的组合物及其使用方法
公开(公告)号：WO2017048702A1
公开(公告)日：2017-03-23
申请号：PCT/US2016/051490
申请日：2016-09-13
申请人： INFINITY PHARMACEUTICALS, INC.
发明人： CRENIER, Louis , LESCARBEAU, Andre , SHARMA, Praveen , GENOV, Daniel G.
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K9/485 , A61K9/4858 , A61K9/4866 , A61K31/519 , C07B2200/13 , C07D231/12 , C07D231/38 , C07D401/06
摘要： Solid forms of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphic forms, cocrystals, and amorphous forms thereof, and pharmaceutical compositions thereof.
摘要翻译：本文描述了调节激酶活性（包括PI3激酶活性）的化合物的固体形式，以及化合物，药物组合物和治疗与激酶活性（包括PI3激酶活性）相关的疾病和病症的方法。本文还提供了制备化合物，多晶型物，共晶体和其无定形形式的方法及其药物组合物。

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