JP7017248B2 - エキセナチド類似体の持続放出コンジュゲート - Google Patents

エキセナチド類似体の持続放出コンジュゲート Download PDF

Info

Publication number
JP7017248B2
JP7017248B2 JP2018548652A JP2018548652A JP7017248B2 JP 7017248 B2 JP7017248 B2 JP 7017248B2 JP 2018548652 A JP2018548652 A JP 2018548652A JP 2018548652 A JP2018548652 A JP 2018548652A JP 7017248 B2 JP7017248 B2 JP 7017248B2
Authority
JP
Japan
Prior art keywords
substituted
alkyl
heteroaryl
aryl
arylalkyl
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
JP2018548652A
Other languages
English (en)
Japanese (ja)
Other versions
JP2019511497A5 (OSRAM
JP2019511497A (ja
Inventor
シュナイダー,エリック,エル.
ハーン,ブライアン
ヘニーズ,ジェフリー,シー.
アシュリー,ゲーリー,ダブリュー.
サンティ,ダニエル,ブイ.
Original Assignee
プロリンクス エルエルシー
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 プロリンクス エルエルシー filed Critical プロリンクス エルエルシー
Publication of JP2019511497A publication Critical patent/JP2019511497A/ja
Publication of JP2019511497A5 publication Critical patent/JP2019511497A5/ja
Application granted granted Critical
Publication of JP7017248B2 publication Critical patent/JP7017248B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/62Medicinal 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
    • A61K47/65Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/56Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60Medicinal 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/26Glucagons
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/69Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6903Medicinal 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being semi-solid, e.g. an ointment, a gel, a hydrogel or a solidifying gel
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0002Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0004Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575Hormones
    • C07K14/605Glucagons

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Zoology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Toxicology (AREA)
  • Immunology (AREA)
  • Emergency Medicine (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
JP2018548652A 2016-03-16 2017-03-16 エキセナチド類似体の持続放出コンジュゲート Expired - Fee Related JP7017248B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201662309330P 2016-03-16 2016-03-16
US62/309,330 2016-03-16
US201662416058P 2016-11-01 2016-11-01
US62/416,058 2016-11-01
PCT/US2017/022791 WO2017161174A1 (en) 2016-03-16 2017-03-16 Extended release conjugates of exenatide analogs

Publications (3)

Publication Number Publication Date
JP2019511497A JP2019511497A (ja) 2019-04-25
JP2019511497A5 JP2019511497A5 (OSRAM) 2020-04-30
JP7017248B2 true JP7017248B2 (ja) 2022-02-08

Family

ID=59852218

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018548652A Expired - Fee Related JP7017248B2 (ja) 2016-03-16 2017-03-16 エキセナチド類似体の持続放出コンジュゲート

Country Status (13)

Country Link
US (1) US20200164083A1 (OSRAM)
EP (2) EP3922269A1 (OSRAM)
JP (1) JP7017248B2 (OSRAM)
KR (1) KR20180129825A (OSRAM)
CN (1) CN109414469A (OSRAM)
AU (2) AU2017234680A1 (OSRAM)
BR (1) BR112018068639A2 (OSRAM)
CA (1) CA3016814A1 (OSRAM)
MX (1) MX2018011149A (OSRAM)
RU (1) RU2764547C2 (OSRAM)
SG (1) SG11201807832VA (OSRAM)
WO (1) WO2017161174A1 (OSRAM)
ZA (2) ZA201805953B (OSRAM)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016243922A1 (en) * 2015-04-01 2017-11-02 The Scripps Research Institute Methods and compositions related to GPCR agonist polypeptides
JOP20190245A1 (ar) 2017-04-20 2019-10-15 Novartis Ag أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط
TW202027794A (zh) 2018-10-03 2020-08-01 瑞士商諾華公司 血管生成素樣3多肽之持續遞送
AU2020253560A1 (en) 2019-04-05 2021-11-25 Prolynx Llc Improved conjugation linkers
WO2021026494A1 (en) * 2019-08-07 2021-02-11 Prolynx Llc Steam sterilization of hydrogels crosslinked by beta-eliminative linkers
JP2023550784A (ja) * 2020-11-25 2023-12-05 プロリンクス エルエルシー C-ナトリウム利尿ペプチドの徐放性ヒドロゲルコンジュゲート
WO2025128916A1 (en) * 2023-12-13 2025-06-19 Cellanome, Inc. Devices and methods for analyzing biological samples
KR102716759B1 (ko) 2023-12-20 2024-10-15 (주)인벤티지랩 엑세나타이드를 포함하는 서방형 주사제 조성물 및 이의 제조 방법

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526899A (ja) 2005-01-14 2008-07-24 ウクスィ・グランドチャンプ・ファーマシューティカル・テクノロジー・カンパニー・リミテッド 修飾されたエキセンディン(Exendins)及びその使用
WO2013059323A1 (en) 2011-10-18 2013-04-25 Prolynx Llc Peg conjugates of exenatide
JP2014531433A (ja) 2011-09-07 2014-11-27 プロリンクス エルエルシー 生分解性架橋を有するヒドロゲル
JP2015172078A (ja) 2008-06-26 2015-10-01 プロリンクス エルエルシー 制御された薬剤放出速度を有するプロドラッグ及び薬剤−高分子のコンジュゲート

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE460942T1 (de) * 1999-01-14 2010-04-15 Amylin Pharmaceuticals Inc Exendine zur glucagon suppression
EP1539210A4 (en) * 2002-09-06 2006-06-07 Bayer Pharmaceuticals Corp GLP-1 RECEPTOR MODIFIED AGONISTS AND THEIR PHARMACOLOGICAL METHODS OF USE
KR20050083713A (ko) 2002-10-02 2005-08-26 질랜드 파마 에이/에스 안정화된 엑센딘-4 화합물
GB2427360A (en) 2005-06-22 2006-12-27 Complex Biosystems Gmbh Aliphatic prodrug linker
CN102827284B (zh) * 2006-11-14 2015-07-29 上海仁会生物制药股份有限公司 带有聚乙二醇基团的Exendin或其类似物及其制剂和用途
WO2008116294A1 (en) 2007-03-23 2008-10-02 Matregen Corp. Exendin analogs
US20110268807A1 (en) * 2008-08-04 2011-11-03 James Su Biodegradable Microspheres and Methods of Use Thereof
CN102711804B (zh) * 2009-11-13 2015-09-16 赛诺菲-安万特德国有限公司 包含glp-1激动剂和甲硫氨酸的药物组合物
CN103025164B (zh) * 2010-05-05 2017-03-08 普罗林科斯有限责任公司 从固体支撑物中药物的控制释放
CN103025165B (zh) * 2010-05-05 2016-06-08 普罗林科斯有限责任公司 自大分子共轭物的控释
EP2571496A4 (en) 2010-05-05 2016-03-30 Prolynx Llc CONTROLLED RELEASE OF MEDICINE FROM DENIMERS
WO2011156407A2 (en) * 2010-06-09 2011-12-15 Amylin Pharmaceuticals, Inc. Glp-1 receptor agonists to treat pancre-atitis

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2008526899A (ja) 2005-01-14 2008-07-24 ウクスィ・グランドチャンプ・ファーマシューティカル・テクノロジー・カンパニー・リミテッド 修飾されたエキセンディン(Exendins)及びその使用
JP2015172078A (ja) 2008-06-26 2015-10-01 プロリンクス エルエルシー 制御された薬剤放出速度を有するプロドラッグ及び薬剤−高分子のコンジュゲート
JP2014531433A (ja) 2011-09-07 2014-11-27 プロリンクス エルエルシー 生分解性架橋を有するヒドロゲル
WO2013059323A1 (en) 2011-10-18 2013-04-25 Prolynx Llc Peg conjugates of exenatide

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Bioconjugate Chem,2016年,vol.27, p.1210-1215

Also Published As

Publication number Publication date
AU2021232810A1 (en) 2021-10-14
RU2018136200A3 (OSRAM) 2020-12-25
EP3429608A4 (en) 2019-12-11
RU2018136200A (ru) 2020-04-16
MX2018011149A (es) 2019-05-30
RU2764547C2 (ru) 2022-01-18
BR112018068639A2 (pt) 2019-07-30
AU2017234680A1 (en) 2018-10-11
WO2017161174A1 (en) 2017-09-21
US20200164083A1 (en) 2020-05-28
AU2017234680A2 (en) 2018-12-13
SG11201807832VA (en) 2018-10-30
CA3016814A1 (en) 2017-09-21
KR20180129825A (ko) 2018-12-05
EP3429608A1 (en) 2019-01-23
ZA201905787B (en) 2021-03-31
EP3922269A1 (en) 2021-12-15
CN109414469A (zh) 2019-03-01
JP2019511497A (ja) 2019-04-25
ZA201805953B (en) 2019-11-27

Similar Documents

Publication Publication Date Title
JP7017248B2 (ja) エキセナチド類似体の持続放出コンジュゲート
EP3666792B1 (en) Insulin receptor partial agonists
US10413594B2 (en) Conjugates of somatostatin analogues
US20190177393A1 (en) Insulin receptor partial agonists
HK40064590A (en) Extended release conjugates of exenatide analogs
NZ786229A (en) Extended release conjugates of exenatide analogs
CN117177735A (zh) 药物glp肽组合物及其制备方法
EA041034B1 (ru) Частичные агонисты инсулинового рецептора
BR112017010481B1 (pt) Composto útil como agonista parcial de receptor de insulina, composição, e, uso de uma composição
BR122024000898B1 (pt) Composto, composição, e, uso do composto
BR122024000903B1 (pt) Composto, composição, e, uso do composto

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200313

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200313

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20200313

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20200316

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20210316

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20210317

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A821

Effective date: 20210318

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210519

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20210818

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20211012

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20211215

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: 20220114

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20220120

R150 Certificate of patent or registration of utility model

Ref document number: 7017248

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees