JP7581385B2 - 経口送達に好適なglp-1受容体およびgip受容体共作動薬 - Google Patents

経口送達に好適なglp-1受容体およびgip受容体共作動薬 Download PDF

Info

Publication number
JP7581385B2
JP7581385B2 JP2022577750A JP2022577750A JP7581385B2 JP 7581385 B2 JP7581385 B2 JP 7581385B2 JP 2022577750 A JP2022577750 A JP 2022577750A JP 2022577750 A JP2022577750 A JP 2022577750A JP 7581385 B2 JP7581385 B2 JP 7581385B2
Authority
JP
Japan
Prior art keywords
amino
peptide
compound
substituent
absent
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.)
Active
Application number
JP2022577750A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2022018186A5 (enExample
JP2023534131A (ja
Inventor
クナー、パトリック、ジェイ.
フィナン、ブライアン
ディマルキ、リチャード
リンデロート、ラース
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.)
Novo Nordisk AS
Original Assignee
Novo Nordisk AS
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 Novo Nordisk AS filed Critical Novo Nordisk AS
Publication of JP2023534131A publication Critical patent/JP2023534131A/ja
Publication of JPWO2022018186A5 publication Critical patent/JPWO2022018186A5/ja
Priority to JP2024187587A priority Critical patent/JP2025020197A/ja
Application granted granted Critical
Publication of JP7581385B2 publication Critical patent/JP7581385B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K14/00Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/001Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof by chemical synthesis
    • 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
    • A61K47/64Drug-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
    • 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Toxicology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
JP2022577750A 2020-07-22 2021-07-22 経口送達に好適なglp-1受容体およびgip受容体共作動薬 Active JP7581385B2 (ja)

Priority Applications (1)

Application Number Priority Date Filing Date Title
JP2024187587A JP2025020197A (ja) 2020-07-22 2024-10-24 経口送達に好適なglp-1受容体およびgip受容体共作動薬

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202063055026P 2020-07-22 2020-07-22
US63/055,026 2020-07-22
EP20192414 2020-08-24
EP20192414.9 2020-08-24
US202163156988P 2021-03-05 2021-03-05
US63/156,988 2021-03-05
PCT/EP2021/070485 WO2022018186A1 (en) 2020-07-22 2021-07-22 Co-agonists at glp-1 and gip receptors suitable for oral delivery

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2024187587A Division JP2025020197A (ja) 2020-07-22 2024-10-24 経口送達に好適なglp-1受容体およびgip受容体共作動薬

Publications (3)

Publication Number Publication Date
JP2023534131A JP2023534131A (ja) 2023-08-08
JPWO2022018186A5 JPWO2022018186A5 (enExample) 2024-07-24
JP7581385B2 true JP7581385B2 (ja) 2024-11-12

Family

ID=77179985

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2022577750A Active JP7581385B2 (ja) 2020-07-22 2021-07-22 経口送達に好適なglp-1受容体およびgip受容体共作動薬
JP2024187587A Pending JP2025020197A (ja) 2020-07-22 2024-10-24 経口送達に好適なglp-1受容体およびgip受容体共作動薬

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2024187587A Pending JP2025020197A (ja) 2020-07-22 2024-10-24 経口送達に好適なglp-1受容体およびgip受容体共作動薬

Country Status (15)

Country Link
US (4) US20220177538A1 (enExample)
EP (1) EP4185607A1 (enExample)
JP (2) JP7581385B2 (enExample)
KR (2) KR102446310B1 (enExample)
CN (1) CN116157143A (enExample)
AU (1) AU2021312323A1 (enExample)
BR (1) BR112023000270A2 (enExample)
CA (1) CA3184717A1 (enExample)
CL (1) CL2023000087A1 (enExample)
CO (1) CO2023000097A2 (enExample)
IL (1) IL299701A (enExample)
MX (1) MX2023000303A (enExample)
PE (1) PE20231841A1 (enExample)
TW (2) TW202315883A (enExample)
WO (1) WO2022018186A1 (enExample)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112023000270A2 (pt) 2020-07-22 2023-01-31 Novo Nordisk As Composto, composição farmacêutica, e, peptídeo
WO2023012263A1 (en) 2021-08-04 2023-02-09 Novo Nordisk A/S Solid oral peptide formulations
TW202330584A (zh) * 2022-01-20 2023-08-01 丹麥商諾佛 儂迪克股份有限公司 前藥及其用途
JP2025523681A (ja) * 2022-07-13 2025-07-23 杭州中美華東製薬有限公司 Glp-1/gip二重アゴニスト、その調製方法および使用
WO2024110614A1 (en) 2022-11-25 2024-05-30 Novo Nordisk A/S Oral administration of peptide therapeutics, such as glp-1
CN117646017A (zh) * 2023-11-02 2024-03-05 中国人民解放军海军军医大学 Gip/glp-1双激动剂多肽编码基因、及其重组乳酸菌和应用
TW202529796A (zh) * 2023-11-22 2025-08-01 大陸商杭州中美華東製藥有限公司 Glp-1r/gipr雙標靶激動劑在製備動物藥的用途
JP7755031B2 (ja) 2023-11-30 2025-10-15 ノヴォ ノルディスク アー/エス Glp-1、gip、およびアミリン受容体の三重作動薬
WO2025133045A1 (en) 2023-12-22 2025-06-26 Novo Nordisk A/S Fermentation process
WO2025149039A1 (zh) * 2024-01-12 2025-07-17 杭州中美华东制药有限公司 长效glp-1/gip双激动剂的药物组合物
WO2025176999A2 (en) * 2024-02-23 2025-08-28 Ip2Ipo Innovations Limited Novel compounds

Family Cites Families (44)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI0915282A2 (pt) 2008-06-17 2017-02-07 Univ Indiana Res & Tech Corp agonistas mistos baseados no gip para o tratamento de distúrbios metabólicos e obesidade
RU2578591C2 (ru) 2008-12-19 2016-03-27 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Лекарственные средства, связанные с дипептидами
AR074811A1 (es) 2008-12-19 2011-02-16 Univ Indiana Res & Tech Corp Profarmaco de peptido de la superfamilia de glucagon basados en amida
US9150632B2 (en) 2009-06-16 2015-10-06 Indiana University Research And Technology Corporation GIP receptor-active glucagon compounds
HUE027229T2 (en) 2009-12-16 2016-08-29 Novo Nordisk As Double acylated glp-1 derivatives
CA2796894A1 (en) 2010-06-24 2011-12-29 Indiana University Research And Technology Corporation Amide based glucagon superfamily peptide prodrugs
EP2588127A4 (en) 2010-06-24 2014-06-11 Univ Indiana Res & Tech Corp DIPEPTIDE-NETWORKED MEDICAL ACTIVE SUBSTANCES
HRP20180425T1 (hr) 2010-12-16 2018-04-20 Novo Nordisk A/S Čvrste kompozicije koje sadrže agonist glp-1 i sol n-(8-(2-hidroksibenzoil)amino)kaprilne kiseline
US8975223B2 (en) * 2010-12-22 2015-03-10 Marcadia Biotech, Inc. Methods for treating metabolic disorders and obesity with a peptide comprising the amino acid sequence of SEQ ID No. 146
WO2012088116A2 (en) 2010-12-22 2012-06-28 Indiana University Research And Technology Corporation Glucagon analogs exhibiting gip receptor activity
JP5914641B2 (ja) 2011-06-10 2016-05-11 ベイジン・ハンミ・ファーマシューティカル・カンパニー・リミテッドBeijing Hanmi Pharmaceutical Co., Ltd. グルコース依存性インスリン分泌刺激ポリペプチドのアナログ、医薬組成物及びその使用
WO2013139695A1 (en) * 2012-03-22 2013-09-26 Novo Nordisk A/S Compositions comprising a delivery agent and preparation thereof
IN2014MN02304A (enExample) 2012-05-03 2015-08-07 Zealand Pharma As
JP6517690B2 (ja) 2012-06-20 2019-05-22 ノヴォ ノルディスク アー/エス ペプチド及び送達剤を含む錠剤製剤
PL2864350T3 (pl) 2012-06-21 2019-01-31 Indiana University Research And Technology Corporation Analogi glukagonu wykazujące aktywność wobec receptora GIP
SG10201705097PA (en) 2012-12-21 2017-07-28 Sanofi Sa Functionalized exendin-4 derivatives
US20160058881A1 (en) 2013-03-15 2016-03-03 Indiana University Research And Technology Corporation Prodrugs with prolonged action
ES2688462T3 (es) * 2013-05-02 2018-11-02 Novo Nordisk A/S Dosificación oral de compuestos de GLP-1
WO2014192284A1 (en) 2013-05-28 2014-12-04 Takeda Pharmaceutical Company Limited Peptide compound
WO2015022420A1 (en) 2013-08-16 2015-02-19 Medimmune Limited Gip and glp-1 receptor dual-agonists for the treatment of diabetes
WO2015035419A1 (en) 2013-09-09 2015-03-12 Hoffmann-La Roche Inc. Dosages of gip/glp-1 co-agonist peptides for human administration
CN105849122B (zh) * 2013-11-06 2021-04-30 西兰制药公司 Gip-glp-1双重激动剂化合物及方法
WO2015086728A1 (en) 2013-12-13 2015-06-18 Sanofi Exendin-4 peptide analogues as dual glp-1/gip receptor agonists
EP3080154B1 (en) 2013-12-13 2018-02-07 Sanofi Dual glp-1/gip receptor agonists
TW201625670A (zh) * 2014-04-07 2016-07-16 賽諾菲公司 衍生自exendin-4之雙重glp-1/升糖素受體促效劑
GB2528436A (en) 2014-07-15 2016-01-27 Lancaster Univ Business Entpr Ltd Treatment of neurological diseases
JP6701208B2 (ja) 2014-09-24 2020-05-27 インディアナ ユニヴァーシティ リサーチ アンド テクノロジー コーポレイション 脂質化アミド系インスリンプロドラッグ
WO2016077220A1 (en) 2014-11-10 2016-05-19 Mb2 Llc Gip/glp-1 co-agonist peptides for human administration
JP2018012644A (ja) 2014-11-26 2018-01-25 武田薬品工業株式会社 ペプチド化合物
JOP20200119A1 (ar) 2015-01-09 2017-06-16 Lilly Co Eli مركبات مساعد مشترك من gip وglp-1
WO2016131893A1 (en) 2015-02-18 2016-08-25 Medimmune Limited Incretin fusion polypeptides
US20170112897A1 (en) 2015-10-23 2017-04-27 Cedars-Sinai Medical Center Methods for treating brain insulin resistance
US10501516B2 (en) 2016-05-24 2019-12-10 Takeda Pharmaceutical Company Limited Peptide compound
GB201620611D0 (en) 2016-12-05 2017-01-18 Univ Of Lancaster Treatment of neurological diseases
JOP20180028A1 (ar) 2017-03-31 2019-01-30 Takeda Pharmaceuticals Co مركب ببتيد
EP3746111B1 (en) 2018-02-02 2023-07-19 Novo Nordisk A/S Solid compositions comprising a glp-1 agonist, a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant
AU2019263674B2 (en) 2018-05-04 2023-03-02 Novo Nordisk A/S GIP derivatives and uses thereof
CN112469431A (zh) 2018-07-23 2021-03-09 伊莱利利公司 使用gip/glp1共激动剂用于糖尿病的方法
UA128697C2 (uk) 2018-07-23 2024-10-02 Елі Ліллі Енд Компані Способи застосування коагоніста gip/glp-1 для терапії
TW202523681A (zh) 2018-07-23 2025-06-16 美商美國禮來大藥廠 Gip/glp1共促效劑化合物
CN112351994B (zh) * 2019-04-11 2024-06-07 江苏豪森药业集团有限公司 一种多受体激动剂及其医药用途
CN110642935A (zh) 2019-09-25 2020-01-03 成都奥达生物科技有限公司 一种替瑞帕肽类似物
CN110684082B (zh) 2019-10-08 2021-12-10 江苏诺泰澳赛诺生物制药股份有限公司 Gip和glp-1双激动多肽化合物及药学上可接受的盐与用途
BR112023000270A2 (pt) 2020-07-22 2023-01-31 Novo Nordisk As Composto, composição farmacêutica, e, peptídeo

Also Published As

Publication number Publication date
AU2021312323A1 (en) 2023-02-02
CA3184717A1 (en) 2022-01-27
US11779648B2 (en) 2023-10-10
US20230272029A1 (en) 2023-08-31
TWI801942B (zh) 2023-05-11
MX2023000303A (es) 2023-02-09
CL2023000087A1 (es) 2023-07-07
BR112023000270A2 (pt) 2023-01-31
JP2025020197A (ja) 2025-02-12
TW202208411A (zh) 2022-03-01
TW202315883A (zh) 2023-04-16
CO2023000097A2 (es) 2023-03-27
US20230120597A1 (en) 2023-04-20
US20220177538A1 (en) 2022-06-09
EP4185607A1 (en) 2023-05-31
KR102446310B1 (ko) 2022-09-23
US20220125940A1 (en) 2022-04-28
CN116157143A (zh) 2023-05-23
JP2023534131A (ja) 2023-08-08
IL299701A (en) 2023-03-01
KR20230029480A (ko) 2023-03-03
KR20220012840A (ko) 2022-02-04
PE20231841A1 (es) 2023-11-21
WO2022018186A1 (en) 2022-01-27

Similar Documents

Publication Publication Date Title
JP7581385B2 (ja) 経口送達に好適なglp-1受容体およびgip受容体共作動薬
TWI707865B (zh) Gip衍生物及其用途
US20230391845A1 (en) Glp-1, gip and glucagon receptor triple agonists
US20230346961A1 (en) Glp-1 and gip receptor co-agonists
JP7434616B2 (ja) プロドラッグおよびその使用
EA049130B1 (ru) Коагонисты рецепторов glp-1 и gip, подходящие для пероральной доставки
CN118632867A (zh) Glp-1/gip受体共激动剂前药及其用途

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20230220

RD03 Notification of appointment of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7423

Effective date: 20230227

RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20230417

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20240712

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20240712

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20240712

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: 20240930

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20241030

R150 Certificate of patent or registration of utility model

Ref document number: 7581385

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150