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1. 发明公开

EP4397755A2 DELIVERY OF THERAPEUTIC AGENTS BY A COLLAGEN BINDING PROTEIN 审中-实审
公开(公告)号：EP4397755A2
公开(公告)日：2024-07-10
申请号：EP24153256.3
申请日：2012-12-14
申请人： The Board of Trustees of the University of Arkansas , The Kitasato Institute , Montefiore Medical Center , National University Corporation Kagawa University
发明人： SAKON, Joshua , PHILOMINATHAN SAGAYA, Theresa, Leena , KATIKANENI, Ranjitha , MATSUSHITA, Osama , PONNAPAKKAM, Tulasi , KOIDE, Takaki , GENSURE, Robert, C. , NISHI, Nozomu
IPC分类号： C12N9/52
CPC分类号： A61K38/29 , A61K8/4913 , A61K8/65 , A61Q7/00 , A61K47/64 , A61K38/179 , A61K38/18 , A61K38/1825 , A61K38/1841 , A61K38/1858 , A61K38/1866 , A61K38/193 , A61K38/30 , A61K38/00 , A61K38/1808 , A61K38/1875 , A61K38/27 , C12N9/52 , C12Y304/24003 , A61P17/00 , A61P17/14 , A61P19/00 , A61P19/04 , A61P19/10 , A61P5/18 , A61P5/20 , Y02A50/30
摘要： Methods of delivering therapeutic agents by administering compositions including a bacterial collagen-binding polypeptide segment linked to the therapeutic agent to subjects in need of treatment with the therapeutic agent are provided. In these methods, the therapeutic agent is not a PTH/PTHrP receptor agonist or antagonist, basic fibroblast growth factor (bFGF) or epidermal growth factor (EGF). The bacterial collagen-binding polypeptide segment delivers the agent to sites of partially untwisted or under-twisted collagen. Methods of treating collagenopathies using a composition including a collagen-binding polypeptide and a PTH/PTHrP receptor agonist are also provided. In addition, methods of treating hyperparathyroidism, and hair loss using compositions comprising a collagen binding polypeptide and a PTH/PTHrP receptor agonist are provided. Finally, methods of reducing hair regrowth by administering a composition including a collagen binding polypeptide and a PTH/PTHrP receptor antagonist are provided.

2. 发明公开

EP4378926A1 UNNATURAL AMINO ACID, AND USE THEREOF, RECOMBINANT PROTEIN CONTAINING SAME, AND RECOMBINANT PROTEIN CONJUGATE 审中-实审
公开(公告)号：EP4378926A1
公开(公告)日：2024-06-05
申请号：EP21951293.6
申请日：2021-07-29
申请人： Novocodex Biopharmaceuticals Co., Ltd.
发明人： YANG, Jinwei , YE, Chenghao , XIA, Gang , HUO, Pengchao , DING, Wen , CHEN, Longfei , JIAO, Lin , HUANG, Hao , HENG, Xin , ZHU, Jingjing , YING, Yuebin , LIANG, Xuejun
IPC分类号： C07C271/22 , C07C235/78 , C07C237/12 , C07C235/20 , C07K14/61 , A61K47/54 , A61K47/60 , A61K38/27 , A61P5/06
CPC分类号： A61K38/27 , A61K47/54 , A61K47/60 , A61P5/06 , C07C235/20 , C07C235/78 , C07C237/12 , C07C271/22 , C07K14/61
摘要： The invention provides an unnatural amino acid, which is a compound with a structure as shown in formula (I) or an enantiomer thereof. The invention further provides use of the unnatural amino acid. Furthermore, the invention further provides a recombinant protein containing the unnatural amino acid and a protein conjugate prepared from the recombinant protein. The unnatural amino acid provided by the invention is simple and convenient to prepare, safe in nature, not easy to be inactivated when being inserted into a protein, and has a high binding rate with a coupling moiety, and the obtained conjugate is higher in stability. The unnatural amino acid provided by the invention is applicable to numerous fields, especially in preparation of a recombinant protein or a recombinant protein conjugate,

3. 发明授权

EP2776066B1 RANK/RANKL ANTAGONISTS FOR USE IN TREATING NEUROMUSCULAR DISORDERS, GENETIC MYOPATHIES AND/OR NON GENETIC MYOPATHIES 有权
公开(公告)号：EP2776066B1
公开(公告)日：2018-09-19
申请号：EP12847546.4
申请日：2012-11-06
申请人： Université Laval
发明人： FRENETTE, Jérôme , PENNINGER, Josef
IPC分类号： A61K31/137 , A61K31/167 , A61K31/401 , A61K31/403 , A61K31/405 , A61K31/417 , A61K31/472 , A61K31/55 , A61K31/568 , A61K31/573 , A61K31/675 , A61K31/7105 , A61K38/17 , A61K38/27 , A61K38/30 , A61K45/06 , G01N33/68 , A61P21/00
CPC分类号： A61K39/3955 , A61K31/137 , A61K31/167 , A61K31/401 , A61K31/403 , A61K31/405 , A61K31/417 , A61K31/472 , A61K31/55 , A61K31/568 , A61K31/573 , A61K31/675 , A61K31/7105 , A61K38/1793 , A61K38/27 , A61K38/30 , A61K45/06 , C07K16/2875 , C12N15/1136 , G01N33/6863 , G01N2333/7151 , G01N2800/2878 , A61K2300/00
摘要： The present invention relates to uses and methods comprising one or more RANK/RANKL antagonists or of a pharmaceutical composition comprising one or more RANK/RANKL antagonists and a pharmaceutically acceptable carrier for treating neuromuscular disorders, non-genetic myopathies, or genetic myopathies; maintaining and/or preserving the excitation:contraction:relaxation coupling; reducing loss of muscle strength associated with neuromuscular disorders, non-genetic myopathies or genetic myopathies; reducing the loss of muscular strength associated with skeletal or cardiac muscle disuse, diseases and aging; or regulating skeletal or cardiac muscle disuse, diseases and/or aging in a patient in need thereof. The present invention also relates to combinations and compositions comprising one or more RANK/RANKL antagonists and to methods for identifying candidate compounds.

4. 发明公开

EP3302450A1 AMINE PEGYLATION METHODS FOR THE PREPARATION OF SITE-SPECIFIC PROTEIN CONJUGATES 审中-公开
标题翻译：用于制备特定于位点的蛋白质缀合物的胺PEG化方法
公开(公告)号：EP3302450A1
公开(公告)日：2018-04-11
申请号：EP16803982.4
申请日：2016-05-19
申请人： Antriabio, Inc.
发明人： ROSENDAHL, Mary S. , MANTRIPRAGADA, Sankaram B.
IPC分类号： A61K31/00 , C07K14/62 , C07K14/00
CPC分类号： A61K38/26 , A61K9/5031 , A61K38/27 , A61K38/28 , A61K38/29 , A61K47/60
摘要： Examples include a method of making a protein-PEG conjugate. The method may include providing an aqueous protein solution. The aqueous protein solution may include a protein, a pH buffer, and a chelating agent. The chelating agent may be chosen from the group consisting of an aminopolycarboxylic acid, a hydroxyaminocarboxylic acid, an N-substituted glycine, 2-(2-amino-2-oxocthyl) aminoethane sulfonic acid (BES), and deferoxamine (DEF). The method may also include introducing sodium cyanoborohydride and a methoxy polyethylene glycol aldehyde to the aqueous protein solution. The sodium cyanoborohydride in the methoxy polyethylene glycol aldehyde may have a molar ratio ranging from about 5:1 to about 1.5:1. The method may further include reacting the methoxy polyethylene glycol aldehyde with the protein to form the protein-PEG conjugate. The pH buffer may maintain a pH of the aqueous protein solution ranging from 4.0 to 4.4 during the reaction.

5. 发明授权

EP2512450B1 DRY GROWTH HORMONE COMPOSITION TRANSIENTLY LINKED TO A POLYMER CARRIER 有权转让
标题翻译：暂时与聚合物载体连接的干生长激素组合物
公开(公告)号：EP2512450B1
公开(公告)日：2018-02-07
申请号：EP10790843.6
申请日：2010-12-15
申请人： ASCENDIS PHARMA ENDOCRINOLOGY DIVISION A/S
发明人： RASMUSSEN, Grethe, Nørskov , KINDERMANN, Susanne , RAU, Harald , WEGGE, Thomas
IPC分类号： A61K9/14 , A61K9/19 , A61K38/27 , A61K47/26 , A61K47/60
CPC分类号： A61K38/27 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/18 , A61K47/26 , A61K47/60 , A61M5/19
摘要： The present invention relates to dry compositions of rhGH polymer prodrug containing a lyoprotectant and, optionally, one or more than one excipient. Such compositions are stable for at least 1 year, when stored at 2-8° C. The invention further relates to methods of manufacturing said compositions, containers comprising such composition as well as a kit of parts.

6. 发明授权

EP2616045B1 SYSTEMS AND METHODS OF DELIVERY OF BIOACTIVE AGENTS USING BACTERIAL TOXIN-DERIVED TRANSPORT SEQUENCES 有权
标题翻译：使用细菌毒素衍生输送序列递送生物活性剂的系统和方法
公开(公告)号：EP2616045B1
公开(公告)日：2017-10-25
申请号：EP11825567.8
申请日：2011-09-15
申请人： Mrsny, Randall J. , Mahmood, Tahir
发明人： Mrsny, Randall J. , Mahmood, Tahir
IPC分类号： A61K9/00 , A61K31/554 , A61K38/21 , A61K38/27 , A61K38/28 , A61K47/64 , C07K14/28
CPC分类号： A61K47/48261 , A61K9/5184 , A61K31/7088 , A61K31/7105 , A61K31/711 , A61K31/713 , A61K38/212 , A61K38/27 , A61K38/28 , A61K47/6415 , A61K47/65 , C07K14/28 , C07K19/00 , C07K2319/50 , C12Y204/02 , Y02A50/471
摘要： The field of the present invention relates, in part, to a strategy for novel pharmaceutical applications. More specifically, the present invention relates to a genetically detoxified form of Vibrio cholera exotoxin (cholix) and the use of cholix-derived polypeptide sequences to enhance intestinal delivery of biologically-active therapeutics. Importantly, the systems and methods described herein provide for the following: the ability to deliver macromolecule doses without injections; the ability to deliver cargo, such as (but not limited to) siRNA or antisense molecules into intracellular compartments where their activity is required; and the delivery of nanoparticles and dendrimer-based carriers across biological membranes, which otherwise would have been impeded due to the barrier properties of most such membranes.

7. 发明公开

EP3218395A1 TREATMENT OF HORMONAL DISORDERS OF GROWTH 有权转让
标题翻译：治疗生长激素失衡
公开(公告)号：EP3218395A1
公开(公告)日：2017-09-20
申请号：EP15798305.7
申请日：2015-11-12
申请人： The United States of America, as represented by The Secretary, Department of Health and Human Services , Université de Liège , Centre Hospitalier Universitaire de Liège
发明人： BECKERS, Albert , DALY, Adrian Francis , FAUCZ, Fabio Rueda , STRATAKIS, Constantine A. , TRIVELLIN, Giampaolo
IPC分类号： C07K14/705 , A61P5/06
CPC分类号： A61K38/31 , A61K31/352 , A61K31/437 , A61K31/473 , A61K31/48 , A61K31/713 , A61K38/12 , A61K38/1709 , A61K38/27 , A61K47/60 , C07K14/705 , C07K16/28 , C12N15/1138 , C12N2310/11 , C12N2310/14
摘要： The present invention refers to a GPR101 inhibitor, antagonist or inverse agonist or inverse agonist for use in preventive and/or therapeutic treatment of diseases selected from the group consisting of acromegaly and gigantism and to methods for preventive and/or therapeutic treatment of diseases selected from the group consisting of acromegaly and gigantism wherein to a subject GPR101 inhibitor, antagonist or inverse agonist is administered. Further, the present invention provides a GPR101 agonist for use in preventive and/or therapeutic treatment of disorders selected from the group consisting of dwarfism, short stature, hypopituitarism and a disease of low levels of pituitary hormone secretion and to methods for preventive and/or therapeutic treatment of diseases selected from the group consisting of dwarfism, short stature, hypopituitarism and a disease of low levels of pituitary hormone secretion wherein to a subject GPR101 agonist is administered. The present invention also provides GHRH inhibitors, antagonists or inverse agonists and GH antagonists for use in the therapeutic treatment of X-linked acrogigantism (X-LAG syndrome). In addition, the present invention refers to a method of increasing body mass and/or body size of livestock comprising administering to livestock an effective amount of GPR101 agonist. Further, the present invention is directed to a non-human transgenic animal, comprising as expressed transgene a gene encoding GPR101 or overexpressing endogenous GPR101 gene.
摘要翻译：本发明涉及用于预防和/或治疗选自肢端肥大症和巨人症的疾病的GPR101抑制剂，拮抗剂或反向激动剂或反向激动剂，以及涉及预防和/或治疗性治疗选自由肢端肥大症和巨人症组成的组，其中给予受试者GPR101抑制剂，拮抗剂或反向激动剂。此外，本发明提供了用于预防和/或治疗选自侏儒症，身材矮小症，垂体机能减低和垂体激素分泌水平低的疾病的疾病的GPR101激动剂，以及用于预防和/或治疗治疗性治疗选自由侏儒症，身材矮小症，垂体机能减退症和垂体激素分泌水平低的疾病组成的组的疾病，其中给予受试者GPR101激动剂。本发明还提供了用于治疗性治疗X连接的助孕作用（X-LAG综合症）的GHRH抑制剂，拮抗剂或反向激动剂和GH拮抗剂。另外，本发明涉及一种增加生命体的体重和/或身体大小的方法，包括给家畜施用有效量的GPR101激动剂。此外，本发明涉及非人转基因动物，其包含编码GPR101或过表达内源GPR101gen的基因的表达转基因。

8. 发明公开

EP3217963A1 METHODS FOR TREATING SUBJECTS WITH PRADER-WILLI SYNDROME OR SMITH-MAGENIS SYNDROME 有权转让
标题翻译：用PRADER-WILLI综合症或史密斯 - 麦氏综合征治疗对象的方法
公开(公告)号：EP3217963A1
公开(公告)日：2017-09-20
申请号：EP15859169.3
申请日：2015-11-12
申请人： Essentialis, Inc.
发明人： COWEN, Neil M.
IPC分类号： A61K9/22 , A61K31/54 , A61K31/549 , C07D285/22
CPC分类号： A61K31/549 , A61K9/00 , A61K9/0004 , A61K9/2054 , A61K9/5026 , A61K9/5042 , A61K9/5047 , A61K31/137 , A61K31/155 , A61K31/551 , A61K38/27 , A61K45/06 , A61K2300/00 , C07D285/18 , C07D285/22
摘要： Provided are immediate or prolonged administration of certain potassium ATP (KATP) channel openers, optionally in combination with growth hormone, to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of KATP channel openers that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are methods of co-administering KATP channel openers with other drugs (e.g., in combination with growth hormone) to treat diseases of humans and animals (e.g., Prader-Willi Syndrome (PWS), Smith-Magenis syndrome (SMS), and the like.
摘要翻译：提供立即或延长给予受试者的任何钾ATP（KATP）通道开放剂，任选地与生长激素组合以在治疗涉及KATP的疾病或病症中实现新的药效学，药代动力学，治疗学，生理学，代谢和组成结果通道。还提供了实现这些结果的药物制剂，KATP通道开放剂的施用和给药方法，并降低了治疗个体的不良反应发生率。进一步提供了将KATP通道开放剂与其他药物（例如与生长激素组合）共同给药以治疗人和动物疾病（例如Prader-Willi综合征（PWS），Smith-Magenis综合征（SMS）和类似。

9. 发明授权

EP2251006B1 MICROPARTICLES AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权
标题翻译：微粒及其制药组合物
公开(公告)号：EP2251006B1
公开(公告)日：2017-07-19
申请号：EP09713553.7
申请日：2009-02-20
申请人： Toray Industries, Inc.
发明人： KAKIZAWA, Yoshinori , NISHIO, Reiji , MICHIZOE, Junji , KOIWA, Masakazu , IDA, Nobuo , HIRANO, Taisuke , KOSHI, Yoichiro
IPC分类号： A61K9/52 , A61K38/27 , A61K38/28 , A61K47/34 , A61K47/36 , A61P3/10 , A61P5/00
CPC分类号： A61K9/1647 , A61K9/1652 , A61K9/1694 , A61K9/19 , A61K38/2278 , A61K38/27 , A61K38/28

10. 发明公开

EP3141257A1 SUSTAINED RELEASE FORMULATIONS COMPRISING VERY LOW MOLECULAR WEIGHT POLYMERS 审中-公开
标题翻译：与聚合物的缓释制剂具有非常低分子量
公开(公告)号：EP3141257A1
公开(公告)日：2017-03-15
申请号：EP16187114.0
申请日：2007-10-26
申请人： IPSEN PHARMA S.A.S.
发明人： CHERIF-CHEIKH, Roland , DELGADO, Anne-Paula , LACOMBE, Frédéric , LACHAMP, Laurence , BOURISSOU, Didier
IPC分类号： A61K38/09 , A61K38/30 , A61K38/31 , A61K47/34 , A61K47/36 , A61K9/00
CPC分类号： A61K38/30 , A61K9/0024 , A61K38/09 , A61K38/25 , A61K38/26 , A61K38/27 , A61K47/34 , A61K47/36
摘要： The present invention relates to a parenteral sustained and controlled release semisolid formulation comprising an oligomer end-capped and an active substance without any supplementary viscosity reducing agent or excipient.
摘要翻译：本发明涉及肠胃外缓控释的半固体制剂，没有任何补充粘度降低剂或赋形剂，其包括低聚物封端的和活性物质。

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