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MX2016001021A - Bioconjugados de polipeptidos de apelina sinteticos. - Google Patents

Bioconjugados de polipeptidos de apelina sinteticos.

Info

Publication number
MX2016001021A
MX2016001021A MX2016001021A MX2016001021A MX2016001021A MX 2016001021 A MX2016001021 A MX 2016001021A MX 2016001021 A MX2016001021 A MX 2016001021A MX 2016001021 A MX2016001021 A MX 2016001021A MX 2016001021 A MX2016001021 A MX 2016001021A
Authority
MX
Mexico
Prior art keywords
bioconjugates
heart failure
life extending
extending moiety
diabetes
Prior art date
Application number
MX2016001021A
Other languages
English (en)
Inventor
Yuan Jun
L Caplan Shari
Golosov Andrei
Thomas Parker David
Zecri Frederic
Zhao Hongjuan
Grosche Philipp
Guimaraes Carla
Kanter Aaron
Lou Changgang
Richardson Usera Aimee
Yasoshima Kayo
C Peters Eric
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of MX2016001021A publication Critical patent/MX2016001021A/es

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10—Peptides having 12 to 20 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542—Carboxylic acids, e.g. a fatty acid or an amino acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/68—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P21/02—Muscle relaxants, e.g. for tetanus or cramps
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/06—Antiarrhythmics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/76—Albumins
    • C07K14/765—Serum albumin, e.g. HSA
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/30—Non-immunoglobulin-derived peptide or protein having an immunoglobulin constant or Fc region, or a fragment thereof, attached thereto
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K2319/00—Fusion polypeptide
    • C07K2319/31—Fusion polypeptide fusions, other than Fc, for prolonged plasma life, e.g. albumin

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Toxicology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)

Abstract

La invención proporciona bioconjugados que comprenden un polipéptido sintético de la fórmula I': X1-X2-X3-X4-X5-X6-X7-X8-X9 -X10-X11-X12-X13 (I') o una amida, un éster, o una sal del mismo, en donde X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 y X13 se definen en la presente, y una fracción prolongadora de la vida media, en donde el péptido y la fracción prolongadora de la vida media se enlazan o se funden de una manera covalente, opcionalmente por medio de un enlazador. Los polipéptidos son agonistas del receptor de APJ. La invención también se refiere a un método para la elaboración de los bioconjugados de la invención, y a sus usos terapéuticos, tales como el tratamiento o la prevención de insuficiencia cardíaca descompensada aguda (ADHF), insuficiencia cardíaca crónica, hipertensión pulmonar, fibrilación auricular, síndrome de Brugada, taquicardia ventricular, ateroesclerosis, hipertensión, restenosis, enfermedades cardiovasculares isquémicas, cardiomiopatía, fibrosis cardíaca, arritmia, retención de agua, diabetes (incluyendo diabetes gestacional), obesidad, arteriopatía periférica, accidentes cerebrovasculares, ataques isquémicos transitorios, lesiones cerebrales traumáticas, esclerosis lateral amiotrófica, lesiones por quemaduras (incluyendo quemadura de sol) y preeclampsia. La presente invención proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica.
MX2016001021A 2013-07-25 2014-07-21 Bioconjugados de polipeptidos de apelina sinteticos. MX2016001021A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361858303P 2013-07-25 2013-07-25
US201462015848P 2014-06-23 2014-06-23
PCT/US2014/047378 WO2015013169A2 (en) 2013-07-25 2014-07-21 Bioconjugates of synthetic apelin polypeptides

Publications (1)

Publication Number Publication Date
MX2016001021A true MX2016001021A (es) 2016-08-03

Family

ID=51265872

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016001021A MX2016001021A (es) 2013-07-25 2014-07-21 Bioconjugados de polipeptidos de apelina sinteticos.

Country Status (22)

Country Link
US (2) US9340582B2 (es)
EP (1) EP3024492A2 (es)
JP (1) JP2016527249A (es)
KR (1) KR20160031552A (es)
CN (1) CN105705167A (es)
AP (1) AP2016009019A0 (es)
AU (1) AU2014293387B2 (es)
BR (1) BR112016001376A2 (es)
CA (1) CA2918077A1 (es)
CL (1) CL2016000157A1 (es)
CR (1) CR20160049A (es)
CU (1) CU20160012A7 (es)
EA (1) EA201690282A1 (es)
HK (1) HK1218252A1 (es)
IL (1) IL243691A0 (es)
MX (1) MX2016001021A (es)
PE (1) PE20160991A1 (es)
PH (1) PH12016500103A1 (es)
SG (1) SG11201600208RA (es)
TW (1) TW201518323A (es)
UY (1) UY35671A (es)
WO (1) WO2015013169A2 (es)

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EP3024846A1 (en) 2013-07-25 2016-06-01 Novartis AG Cyclic apelin derivatives for the treatment of heart failure
TW201536814A (zh) 2013-07-25 2015-10-01 Novartis Ag 用於治療心臟衰竭之合成環狀多肽
US9683018B2 (en) 2013-07-25 2017-06-20 Novartis Ag Disulfide cyclic polypeptides for the treatment of heart failure
PE20160991A1 (es) * 2013-07-25 2016-10-15 Novartis Ag Bioconjugados de polipeptidos de apelina sintetica
CN105916881A (zh) 2013-11-20 2016-08-31 瑞泽恩制药公司 Aplnr调节剂及其用途
JP6675333B2 (ja) 2014-06-23 2020-04-01 ノバルティス アーゲー 部位特異的タンパク質修飾
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
WO2016014501A1 (en) * 2014-07-21 2016-01-28 Novartis Ag Sortase molecules and uses thereof
WO2016014553A1 (en) 2014-07-21 2016-01-28 Novartis Ag Sortase synthesized chimeric antigen receptors
US11566082B2 (en) 2014-11-17 2023-01-31 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
CA2972871A1 (en) * 2015-01-23 2016-07-28 Novartis Ag Synthetic apelin fatty acid conjugates with improved half-life
TWI614030B (zh) * 2015-05-20 2018-02-11 免疫功坊股份有限公司 具有標的部分及效應部分的分子構建體
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JP2019508419A (ja) * 2016-02-16 2019-03-28 ザ ユニバーシティー オブ クイーンズランド 新規アルファコノトキシンペプチド
JP7031934B2 (ja) 2016-05-11 2022-03-08 サイティバ・バイオプロセス・アールアンドディ・アクチボラグ 分離マトリックス
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CN109071613A (zh) 2016-05-11 2018-12-21 通用电气医疗集团生物工艺研发股份公司 分离基质
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US10889615B2 (en) 2016-05-11 2021-01-12 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
US10703774B2 (en) 2016-09-30 2020-07-07 Ge Healthcare Bioprocess R&D Ab Separation method
US11753438B2 (en) 2016-05-11 2023-09-12 Cytiva Bioprocess R&D Ab Method of cleaning and/or sanitizing a separation matrix
US12448411B2 (en) 2016-09-30 2025-10-21 Cytiva Bioprocess R&D Ab Separation method
US10738338B2 (en) 2016-10-18 2020-08-11 The Research Foundation for the State University Method and composition for biocatalytic protein-oligonucleotide conjugation and protein-oligonucleotide conjugate
CN110072531A (zh) 2016-10-19 2019-07-30 阿维夫公司 用于治疗心血管相关疾病的爱帕琳的新型聚乙二醇化的脂质体制剂
JP7001285B2 (ja) * 2017-03-29 2022-01-19 国立大学法人 宮崎大学 長時間作用型アドレノメデュリン誘導体
US10639382B2 (en) 2017-04-13 2020-05-05 National Guard Health Affairs Method for treating leukemia
EP3649146B1 (en) 2017-07-03 2024-06-26 The Governors of the University of Alberta Apelin peptides and uses thereof
CN113194983B (zh) * 2018-09-06 2025-11-18 奇达拉治疗公司 用于治疗病毒感染的组合物及方法
KR102509217B1 (ko) * 2020-08-28 2023-03-14 기초과학연구원 시스테인 선택적 결합 퀴놀리논 유도체 화합물, 이의 펩티드 결합체 및 이를 포함하는 항체-약물 접합체
CN112546198B (zh) * 2020-12-17 2022-03-25 温州医科大学慈溪生物医药研究院 一种用于治疗脑中风和急性脑梗的药物组合物
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