JP6505691B2 - 心不全治療用の環状アペリン誘導体 - Google Patents

心不全治療用の環状アペリン誘導体 Download PDF

Info

Publication number
JP6505691B2
JP6505691B2 JP2016529805A JP2016529805A JP6505691B2 JP 6505691 B2 JP6505691 B2 JP 6505691B2 JP 2016529805 A JP2016529805 A JP 2016529805A JP 2016529805 A JP2016529805 A JP 2016529805A JP 6505691 B2 JP6505691 B2 JP 6505691B2
Authority
JP
Japan
Prior art keywords
polypeptide
side chain
peptide
ester
salt
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.)
Expired - Fee Related
Application number
JP2016529805A
Other languages
English (en)
Japanese (ja)
Other versions
JP2016527248A (ja
JP2016527248A5 (enExample
Inventor
ゼクリ，フレデリック
グローシュ，フィリップ
佳代 八十島
佳代 八十島
チャオ，ホンジュアン
ユアン，ジュン
Original Assignee
ノバルティス アーゲー
ノバルティス アーゲー
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 ノバルティス アーゲー, ノバルティス アーゲー filed Critical ノバルティス アーゲー
Publication of JP2016527248A publication Critical patent/JP2016527248A/ja
Publication of JP2016527248A5 publication Critical patent/JP2016527248A5/ja
Application granted granted Critical
Publication of JP6505691B2 publication Critical patent/JP6505691B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (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)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Child & Adolescent Psychology (AREA)
JP2016529805A 2013-07-25 2014-07-21 心不全治療用の環状アペリン誘導体 Expired - Fee Related JP6505691B2 (ja)

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 (3)

Publication Number Publication Date
JP2016527248A JP2016527248A (ja) 2016-09-08
JP2016527248A5 JP2016527248A5 (enExample) 2017-08-31
JP6505691B2 true JP6505691B2 (ja) 2019-04-24

Family

ID=51301346

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016529805A Expired - Fee Related JP6505691B2 (ja) 2013-07-25 2014-07-21 心不全治療用の環状アペリン誘導体

Country Status (5)

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

Families Citing this family (12)

* 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
EP3024845A1 (en) 2013-07-25 2016-06-01 Novartis AG Cyclic polypeptides for the treatment of heart failure
EP3024847A1 (en) 2013-07-25 2016-06-01 Novartis AG Disulfide cyclic polypeptides for the treatment of heart failure
WO2015013165A1 (en) 2013-07-25 2015-01-29 Novartis Ag Cyclic apelin derivatives for the treatment of heart failure
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
ES2818109T3 (es) 2014-06-23 2021-04-09 Novartis Ag Modificaciones de proteínas específicas para un sitio
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
CN112007027B (zh) * 2020-09-14 2022-07-15 长春金赛药业有限责任公司 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

Family Cites Families (14)

* 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
US20070191272A1 (en) * 2005-09-27 2007-08-16 Stemmer Willem P Proteinaceous pharmaceuticals and uses thereof
WO2009155556A2 (en) * 2008-06-20 2009-12-23 The Board Of Regents Of The University Of Texas System Crkl targeting peptides
KR20110091702A (ko) * 2008-11-04 2011-08-12 앵커 테라퓨틱스, 인코포레이티드 Ａｐｊ 수용체 화합물
US9229013B2 (en) * 2009-05-05 2016-01-05 B.R.A.H.M.S Gmbh Vasoactive hormone-based stratification of patients suffering from diseases related to endothelial function/dysfunction
HRP20160547T1 (hr) * 2011-03-11 2016-06-17 Genzyme Corporation Pegilirani apelin i njegova upotreba
CU23950B1 (es) * 2011-03-21 2013-10-29 Ct De Ingeniería Genética Y Biotecnología Péptidos cíclicos con actividad antineoplásica y antiangiogénica
BR112014000474A2 (pt) * 2011-07-08 2017-02-21 Bayer Ip Gmbh proteínas de fusão libertadoras de relaxina e suas utilizações
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
WO2015013165A1 (en) 2013-07-25 2015-01-29 Novartis Ag Cyclic apelin derivatives for the treatment of heart failure
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
EP3024845A1 (en) 2013-07-25 2016-06-01 Novartis AG Cyclic polypeptides for the treatment of heart failure
EP3024847A1 (en) 2013-07-25 2016-06-01 Novartis AG Disulfide cyclic polypeptides for the treatment of heart failure

Also Published As

Publication number Publication date
JP2016527248A (ja) 2016-09-08
EP3024846A1 (en) 2016-06-01
WO2015013165A1 (en) 2015-01-29
US9908919B2 (en) 2018-03-06
CN105612173A (zh) 2016-05-25
US20160159871A1 (en) 2016-06-09

Similar Documents

Publication Publication Date Title
JP6505692B2 (ja) 心不全治療のためのジスルフィド環状ポリペプチド
JP6595553B2 (ja) 心不全治療用の合成アペリン模倣物
JP6501775B2 (ja) 心不全治療用の環状ポリペプチド
JP6505691B2 (ja) 心不全治療用の環状アペリン誘導体
AU2014293387B2 (en) Bioconjugates of synthetic apelin polypeptides
JP6444882B2 (ja) 心不全治療用の合成鎖状アペリン模倣物
US8921307B2 (en) Synthetic linear apelin mimetics for the treatment of heart failure
HK1200470B (en) Synthetic apelin mimetics for the treatment of heart failure

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160419

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170721

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20170721

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20180619

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180911

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181116

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20190305

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190327

R150 Certificate of patent or registration of utility model

Ref document number: 6505691

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees