CN105612173A - 用于治疗心力衰竭的环状apelin衍生物 - Google Patents

用于治疗心力衰竭的环状apelin衍生物 Download PDF

Info

Publication number
CN105612173A
CN105612173A CN201480052673.XA CN201480052673A CN105612173A CN 105612173 A CN105612173 A CN 105612173A CN 201480052673 A CN201480052673 A CN 201480052673A CN 105612173 A CN105612173 A CN 105612173A
Authority
CN
China
Prior art keywords
polypeptide
salt
side chain
peptide
ester
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201480052673.XA
Other languages
English (en)
Chinese (zh)
Inventor
F·泽克里
P·格罗舍
八十岛华杨
H·赵
J·袁
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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 CN105612173A publication Critical patent/CN105612173A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • 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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/1703—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • A61K38/1709—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • 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
    • A61K47/62—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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Marine Sciences & Fisheries (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
CN201480052673.XA 2013-07-25 2014-07-21 用于治疗心力衰竭的环状apelin衍生物 Pending CN105612173A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361858280P 2013-07-25 2013-07-25
US61/858,280 2013-07-25
PCT/US2014/047372 WO2015013165A1 (en) 2013-07-25 2014-07-21 Cyclic apelin derivatives for the treatment of heart failure

Publications (1)

Publication Number Publication Date
CN105612173A true CN105612173A (zh) 2016-05-25

Family

ID=51301346

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480052673.XA Pending CN105612173A (zh) 2013-07-25 2014-07-21 用于治疗心力衰竭的环状apelin衍生物

Country Status (5)

Country Link
US (1) US9908919B2 (https=)
EP (1) EP3024846A1 (https=)
JP (1) JP6505691B2 (https=)
CN (1) CN105612173A (https=)
WO (1) WO2015013165A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112007027A (zh) * 2020-09-14 2020-12-01 宁波熙健医药科技有限公司 含酯基芳香丙酰胺类化合物及其代谢产物在制备治疗心衰药物中的应用
WO2026007693A1 (zh) * 2024-07-05 2026-01-08 浙江大学 Apelin-13多肽突变体

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8673848B2 (en) 2012-01-27 2014-03-18 Novartis Ag Synthetic apelin mimetics for the treatment of heart failure
UY35144A (es) * 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
JP6505691B2 (ja) 2013-07-25 2019-04-24 ノバルティス アーゲー 心不全治療用の環状アペリン誘導体
MX2016001020A (es) 2013-07-25 2016-08-03 Novartis Ag Polipeptidos ciclicos para el tratamiento de insuficiencia cardiaca.
CN105705167A (zh) 2013-07-25 2016-06-22 诺华股份有限公司 合成的apelin多肽的生物缀合物
US9683018B2 (en) 2013-07-25 2017-06-20 Novartis Ag Disulfide cyclic polypeptides for the treatment of heart failure
EP3157942B1 (en) 2014-06-23 2020-06-17 Novartis AG Site specific protein modifications
US10588980B2 (en) 2014-06-23 2020-03-17 Novartis Ag Fatty acids and their use in conjugation to biomolecules
US10849992B1 (en) * 2015-04-07 2020-12-01 Alector Llc Methods of screening for sortilin binding antagonists
ES2930077T3 (es) * 2016-02-15 2022-12-07 Inst Nat Sante Rech Med Apelina para su uso en el tratamiento de la disfunción cognitiva posoperatoria
JOP20190245A1 (ar) 2017-04-20 2019-10-15 Novartis Ag أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102203117A (zh) * 2008-11-04 2011-09-28 安科治疗公司 Apj受体化合物
CN102428368A (zh) * 2009-05-05 2012-04-25 B.R.A.H.M.S有限公司 患有内皮功能/功能障碍相关疾病的患者的基于血管活性激素的分层
WO2012126441A2 (es) * 2011-03-21 2012-09-27 Centro De Ingenieria Genetica Y Biotecnologia Péptidos cíclicos con actividad antineoplásica y antiangiogénica.

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8673848B2 (en) * 2012-01-27 2014-03-18 Novartis Ag Synthetic apelin mimetics for the treatment of heart failure
EP1929073A4 (en) * 2005-09-27 2010-03-10 Amunix Inc PROTEIN MEDICAMENT AND ITS USE
BRPI0915718A2 (pt) * 2008-06-20 2017-06-20 Univ Texas peptídeos de direção crkl
AU2012229336B2 (en) * 2011-03-11 2017-02-02 Genzyme Corporation Pegylated Apelin and uses thereof
JP2014529293A (ja) * 2011-07-08 2014-11-06 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ レラキシンを放出する融合タンパク質およびその使用
UY35144A (es) 2012-11-20 2014-06-30 Novartis Ag Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca
ES2732574T3 (es) * 2012-11-30 2019-11-25 Novartis Ag Métodos para preparar conjugados a partir de proteínas que contienen disulfuro
MX2016001020A (es) 2013-07-25 2016-08-03 Novartis Ag Polipeptidos ciclicos para el tratamiento de insuficiencia cardiaca.
JP6505691B2 (ja) 2013-07-25 2019-04-24 ノバルティス アーゲー 心不全治療用の環状アペリン誘導体
CN105705167A (zh) * 2013-07-25 2016-06-22 诺华股份有限公司 合成的apelin多肽的生物缀合物
US9683018B2 (en) 2013-07-25 2017-06-20 Novartis Ag Disulfide cyclic polypeptides for the treatment of heart failure

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102203117A (zh) * 2008-11-04 2011-09-28 安科治疗公司 Apj受体化合物
CN102428368A (zh) * 2009-05-05 2012-04-25 B.R.A.H.M.S有限公司 患有内皮功能/功能障碍相关疾病的患者的基于血管活性激素的分层
WO2012126441A2 (es) * 2011-03-21 2012-09-27 Centro De Ingenieria Genetica Y Biotecnologia Péptidos cíclicos con actividad antineoplásica y antiangiogénica.

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
JURI HAMADA等: "Evaluation of novel cyclic analogues of apelin", 《INTERNATIONAL JOURNAL OF MOLECULAR MEDICINE》 *
M. V. SIDOROVA1等: "Synthesis and Cardioprotective Properties of Apelin-12 and its Structural Analogues", 《RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112007027A (zh) * 2020-09-14 2020-12-01 宁波熙健医药科技有限公司 含酯基芳香丙酰胺类化合物及其代谢产物在制备治疗心衰药物中的应用
WO2026007693A1 (zh) * 2024-07-05 2026-01-08 浙江大学 Apelin-13多肽突变体

Also Published As

Publication number Publication date
US9908919B2 (en) 2018-03-06
JP2016527248A (ja) 2016-09-08
JP6505691B2 (ja) 2019-04-24
US20160159871A1 (en) 2016-06-09
WO2015013165A1 (en) 2015-01-29
EP3024846A1 (en) 2016-06-01

Similar Documents

Publication Publication Date Title
CN104220452B (zh) 用于治疗心力衰竭的合成的apelin模拟物
AU2014293387B2 (en) Bioconjugates of synthetic apelin polypeptides
US9683018B2 (en) Disulfide cyclic polypeptides for the treatment of heart failure
AU2014293386B2 (en) Cyclic polypeptides for the treatment of heart failure
US9908919B2 (en) Cyclic apelin derivatives for the treatment of heart failure
CN105007928B (zh) 用于治疗心力衰竭的合成线性apelin模拟物
US8921307B2 (en) Synthetic linear apelin mimetics for the treatment of heart failure

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20160525

WD01 Invention patent application deemed withdrawn after publication