CN102300580A - 二肽连接的药剂 - Google Patents

二肽连接的药剂 Download PDF

Info

Publication number
CN102300580A
CN102300580A CN2009801518123A CN200980151812A CN102300580A CN 102300580 A CN102300580 A CN 102300580A CN 2009801518123 A CN2009801518123 A CN 2009801518123A CN 200980151812 A CN200980151812 A CN 200980151812A CN 102300580 A CN102300580 A CN 102300580A
Authority
CN
China
Prior art keywords
alkyl
hydrogen
aryl
perhaps
atom
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
CN2009801518123A
Other languages
English (en)
Chinese (zh)
Inventor
R·D·迪马基
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.)
Indiana University Research and Technology Corp
Original Assignee
Indiana University Research and Technology Corp
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 Indiana University Research and Technology Corp filed Critical Indiana University Research and Technology Corp
Publication of CN102300580A publication Critical patent/CN102300580A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K38/22—Hormones
    • A61K38/28—Insulins
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
CN2009801518123A 2008-12-19 2009-12-18 二肽连接的药剂 Pending CN102300580A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13922708P 2008-12-19 2008-12-19
US61/139,227 2008-12-19
PCT/US2009/068711 WO2010080605A1 (en) 2008-12-19 2009-12-18 Dipeptide linked medicinal agents

Publications (1)

Publication Number Publication Date
CN102300580A true CN102300580A (zh) 2011-12-28

Family

ID=42316744

Family Applications (1)

Application Number Title Priority Date Filing Date
CN2009801518123A Pending CN102300580A (zh) 2008-12-19 2009-12-18 二肽连接的药剂

Country Status (13)

Country Link
US (1) US20110237493A1 (enExample)
EP (1) EP2376098A4 (enExample)
JP (2) JP2012512898A (enExample)
KR (1) KR20110114568A (enExample)
CN (1) CN102300580A (enExample)
AU (1) AU2009335711A1 (enExample)
CA (1) CA2747195A1 (enExample)
IL (1) IL213341A0 (enExample)
MX (1) MX2011006527A (enExample)
PE (1) PE20120331A1 (enExample)
RU (1) RU2578591C2 (enExample)
SG (1) SG172290A1 (enExample)
WO (1) WO2010080605A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103172726A (zh) * 2011-12-22 2013-06-26 杭州淳泰科技有限公司 胰泌素类似物及其制备方法和用途

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2913805A1 (en) 2005-11-07 2007-05-18 Indiana University Research And Technology Corporation Glucagon analogs exhibiting physiological solubility and stability
CN101578102B (zh) 2007-01-05 2013-07-17 印第安纳大学研究及科技有限公司 在生理性pH缓冲液中显示增强的溶解性的胰高血糖素类似物
NZ578948A (en) 2007-02-15 2012-03-30 Univ Indiana Res & Tech Corp Glucagon/glp-1 receptor co-agonists
WO2009058734A1 (en) 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Compounds exhibiting glucagon antagonist and glp-1 agonist activity
CA2707861A1 (en) 2007-10-30 2009-05-07 Indiana University Research And Technology Corporation Glucagon antagonists
US20110065633A1 (en) 2008-01-30 2011-03-17 Indiana University Research And Technology Corporation Ester-based peptide prodrugs
CA2728284C (en) 2008-06-17 2019-09-10 Richard D. Dimarchi Glucagon/glp-1 receptor co-agonists
TWI541023B (zh) 2008-06-17 2016-07-11 印第安納大學科技研究公司 在生理ph緩衝液中呈現增強之溶解度及穩定性之升糖激素類似物
ES2558842T3 (es) 2008-06-17 2016-02-09 Indiana University Research And Technology Corporation Agonistas mixtos a base de GIP para el tratamiento de trastornos metabólicos y obesidad
EP2376097A4 (en) 2008-12-19 2012-10-03 Univ Indiana Res & Tech Corp PEPTIDE PRODRUGS OF AMIDE-BASED GLUCAGON SUPERFAMILY
US8697632B2 (en) 2008-12-19 2014-04-15 Indiana University Research And Technology Corporation Amide based insulin prodrugs
JP5789515B2 (ja) 2008-12-19 2015-10-07 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation インスリン類似体
WO2010148089A1 (en) 2009-06-16 2010-12-23 Indiana University Research And Technology Corporation Gip receptor-active glucagon compounds
WO2011075393A2 (en) 2009-12-18 2011-06-23 Indiana University Research And Technology Corporation Glucagon/glp-1 receptor co-agonists
KR20120123443A (ko) 2010-01-27 2012-11-08 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 대사 장애 및 비만 치료용 글루카곤 길항제-gip 항진제 콘쥬게이트
ES2661228T3 (es) 2010-05-13 2018-03-28 Indiana University Research And Technology Corporation Péptidos de la superfamilia de glucagón que muestran actividad de receptor nuclear de hormona
RU2012153753A (ru) 2010-05-13 2014-06-20 Индиана Юниверсити Рисерч Энд Текнолоджи Корпорейшн Пептиды глюкагонового суперсемейства, обладающие активностью в отношении сопряженных с g-белком рецепторов
JP5969469B2 (ja) 2010-06-16 2016-08-17 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation インスリン受容体に対して高い活性を示す単鎖インスリンアゴニスト
CA2803164C (en) 2010-06-24 2018-08-21 Indiana University Research And Technology Corporation Amide-based insulin prodrugs
KR20130083843A (ko) * 2010-06-24 2013-07-23 인디애나 유니버시티 리서치 앤드 테크놀로지 코퍼레이션 디펩티드 연결된 약제
US8778872B2 (en) 2010-06-24 2014-07-15 Indiana University Research And Technology Corporation Amide based glucagon superfamily peptide prodrugs
NZ612297A (en) 2010-12-22 2015-10-30 Univ Indiana Res & Tech Corp Glucagon analogs exhibiting gip receptor activity
CN103857408B (zh) 2011-06-22 2017-04-12 印第安那大学科技研究公司 胰高血糖素/glp‑1受体协同激动剂
JP6184404B2 (ja) 2011-06-22 2017-08-23 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 グルカゴン/glp−1レセプターコアゴニスト
BR112014007124A2 (pt) * 2011-11-17 2017-06-13 Univ Indiana Res & Tech Corp superfamília de peptídeos gluxagon que exibem atividade no receptor glicocorticóide
CN104114183A (zh) 2011-12-20 2014-10-22 印第安纳大学研究及科技有限公司 用于治疗糖尿病的基于ctp的胰岛素类似物
ES2810153T3 (es) 2012-03-01 2021-03-08 Novo Nordisk As Profármacos de GLP-1
ES2602486T3 (es) 2012-06-21 2017-02-21 Indiana University Research And Technology Corporation Análogos de glucagón que muestran actividad de receptor de GIP
CN108383902A (zh) 2012-09-26 2018-08-10 印第安纳大学研究及科技有限公司 胰岛素类似物二聚体
JP6538645B2 (ja) 2013-03-14 2019-07-03 インディアナ ユニバーシティー リサーチ アンド テクノロジー コーポレーションIndiana University Research And Technology Corporation インスリン‐インクレチン複合物
WO2015081891A1 (en) 2013-12-06 2015-06-11 Baikang (Suzhou) Co., Ltd Bioreversable promoieties for nitrogen-containing and hydroxyl-containing drugs
CN108271356A (zh) 2014-09-24 2018-07-10 印第安纳大学研究及科技有限公司 肠降血糖素-胰岛素缀合物
EP3197912B1 (en) 2014-09-24 2023-01-04 Indiana University Research & Technology Corporation Lipidated amide-based insulin prodrugs
SI3464336T1 (sl) 2016-06-01 2022-06-30 Athira Pharma, Inc. Spojine
CA3183120A1 (en) * 2020-05-26 2021-12-02 Indiana University Research And Technology Corporation Pth analogs for the treatment of hypoparathyroidism
AU2021312323A1 (en) 2020-07-22 2023-02-02 Novo Nordisk A/S Co-agonists at GLP-1 and GIP receptors suitable for oral delivery
JP7484018B2 (ja) 2020-11-06 2024-05-15 ノヴォ ノルディスク アー/エス Glp-1プロドラッグおよびその使用
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
US20250304645A1 (en) 2022-05-10 2025-10-02 Novo Nordisk A/S Prodrugs of GLP-1 Polypeptide and Uses Thereof
TW202421645A (zh) 2022-11-25 2024-06-01 丹麥商諾佛 儂迪克股份有限公司 如glp—1之肽治療劑的口服投與

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4741897A (en) * 1986-07-08 1988-05-03 Baxter Travenol Thyroxine analogs and reagents for thyroid hormone assays
US20020038026A1 (en) * 2000-08-04 2002-03-28 Rao Nagaraja K.R. Method of synthesizing diketopiperazines
CN1635900A (zh) * 2001-08-28 2005-07-06 伊莱利利公司 Glp-1和基础胰岛素的预混合物

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3740385A (en) * 1970-05-07 1973-06-19 M Ondetti N-terminal derivatives of secretin
DK119785D0 (da) * 1985-03-15 1985-03-15 Nordisk Gentofte Insulinpraeparat
US5545618A (en) * 1990-01-24 1996-08-13 Buckley; Douglas I. GLP-1 analogs useful for diabetes treatment
DE19828113A1 (de) * 1998-06-24 2000-01-05 Probiodrug Ges Fuer Arzneim Prodrugs von Inhibitoren der Dipeptidyl Peptidase IV
US20030236190A1 (en) * 1998-09-02 2003-12-25 Renuka Pillutla Isulin and IGF-1 receptor agonists and antagonists
ATE272650T1 (de) * 1999-03-29 2004-08-15 Uutech Ltd Analoge des magensaft inhibierenden peptides und ihre verwendung für die behandlung von diabetes
AUPQ661800A0 (en) * 2000-03-31 2000-05-04 Metabolic Pharmaceuticals Limited Insulin-potentiating compounds
US7052686B2 (en) * 2000-09-29 2006-05-30 Schering Corporation Pegylated interleukin-10
EP1243276A1 (en) * 2001-03-23 2002-09-25 Franciscus Marinus Hendrikus De Groot Elongated and multiple spacers containing activatible prodrugs
ES2464532T3 (es) * 2001-04-19 2014-06-03 The Scripps Research Institute Métodos y composiciones para la producción de pares ortogonales de ARNt-aminoacil-ARNt sintetasa
US7238656B2 (en) * 2001-08-29 2007-07-03 Yissum Research Development Company Of The Hebrew University Of Jerusalem Protective factors against inflammation, burns and noxious stimuli
AU2002346490A1 (en) * 2001-12-20 2003-07-09 Eli Lilly And Company Insulin molecule having protracted time action
FR2842209B1 (fr) * 2002-07-09 2007-11-23 Nouvelle protease aspartique dite saspase et son utilisation dans le domaine cosmetique et therapeutique
US7557183B2 (en) * 2003-03-19 2009-07-07 Eli Lilly And Company Polyethylene glycol linked GLP-1 compounds
WO2004089280A2 (en) * 2003-04-08 2004-10-21 Yeda Research And Development Co. Ltd. Reversible pegylated drugs
GB0310593D0 (en) * 2003-05-08 2003-06-11 Leuven K U Res & Dev Peptidic prodrugs
EP1670515A2 (en) * 2003-09-19 2006-06-21 Novo Nordisk A/S Albumin-binding derivatives of therapeutic peptides
US20050187147A1 (en) * 2003-09-22 2005-08-25 Newman Michael J. Compositions and methods for increasing drug efficiency
US8263545B2 (en) * 2005-02-11 2012-09-11 Amylin Pharmaceuticals, Inc. GIP analog and hybrid polypeptides with selectable properties
EP1929030A2 (en) * 2005-09-08 2008-06-11 Shire LLC Prodrugs of t3 and t4 with enhanced bioavailability
AU2007227202B2 (en) * 2006-03-21 2013-08-22 Amylin Pharmaceuticals, Llc Peptide-peptidase inhibitor conjugates and methods of using same
KR20090060294A (ko) * 2006-09-08 2009-06-11 암브룩스, 인코포레이티드 변형된 인간 혈장 폴리펩티드 또는 Fc 스캐폴드 및 그의 용도
DE102006052755A1 (de) * 2006-11-08 2008-05-15 N-Zyme Biotec Gmbh Michaelsysteme als Transglutaminaseinhibitoren
NZ578948A (en) * 2007-02-15 2012-03-30 Univ Indiana Res & Tech Corp Glucagon/glp-1 receptor co-agonists
US20110065633A1 (en) * 2008-01-30 2011-03-17 Indiana University Research And Technology Corporation Ester-based peptide prodrugs
EP2376097A4 (en) * 2008-12-19 2012-10-03 Univ Indiana Res & Tech Corp PEPTIDE PRODRUGS OF AMIDE-BASED GLUCAGON SUPERFAMILY

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4741897A (en) * 1986-07-08 1988-05-03 Baxter Travenol Thyroxine analogs and reagents for thyroid hormone assays
US20020038026A1 (en) * 2000-08-04 2002-03-28 Rao Nagaraja K.R. Method of synthesizing diketopiperazines
CN1635900A (zh) * 2001-08-28 2005-07-06 伊莱利利公司 Glp-1和基础胰岛素的预混合物

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DE ARNAB: "Design of Peptide-Based Prodrug Chemistry and Its Application to Glucagon-like Peptide I", 《INDIANA UNIVERSITY》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103172726A (zh) * 2011-12-22 2013-06-26 杭州淳泰科技有限公司 胰泌素类似物及其制备方法和用途
CN103172726B (zh) * 2011-12-22 2017-06-13 杭州淳泰科技有限公司 胰泌素类似物及其制备方法和用途

Also Published As

Publication number Publication date
JP2012512898A (ja) 2012-06-07
EP2376098A4 (en) 2014-06-11
IL213341A0 (en) 2011-07-31
MX2011006527A (es) 2011-08-17
CA2747195A1 (en) 2010-07-15
PE20120331A1 (es) 2012-04-14
RU2011129764A (ru) 2013-01-27
RU2578591C2 (ru) 2016-03-27
KR20110114568A (ko) 2011-10-19
WO2010080605A1 (en) 2010-07-15
SG172290A1 (en) 2011-07-28
AU2009335711A1 (en) 2010-07-15
US20110237493A1 (en) 2011-09-29
JP2016028082A (ja) 2016-02-25
EP2376098A1 (en) 2011-10-19

Similar Documents

Publication Publication Date Title
RU2578591C2 (ru) Лекарственные средства, связанные с дипептидами
CN102958533B (zh) 二肽连接的药剂
TWI489992B (zh) 醯胺系胰高血糖素超級家族之胜肽前驅藥物
CN103649115B (zh) 多肽
CA2802485C (en) Single chain insulin agonists exhibiting high activity at the insulin receptor
JP6387008B2 (ja) インスリンアナローグダイマー
TWI362392B (en) Acylated glp-1 compounds
TW201209062A (en) Amide based glucagon superfamily peptide prodrugs
CN103119057B (zh) 基于酰胺的胰岛素前药
EP4736944A2 (en) Polypeptides and uses thereof
CN105324125A (zh) 具有长效的前体药物
CN104395338A (zh) 人胰岛淀粉样多肽类似物
JPH06228199A (ja) 血液脳関門通過可能なペプチド結合体
CA3200526A1 (en) Pharmaceutical composition of glp-1/glp-2 dual agonists
HK1165310A (en) Dipeptide linked medicinal agents
US20170313755A1 (en) Insulin receptor partial agonists
HK1183824A (en) Amide based glucagon superfamily peptide prodrugs
HK1165711A (en) Amide based glucagon superfamily peptide prodrugs

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1165310

Country of ref document: HK

RJ01 Rejection of invention patent application after publication

Application publication date: 20111228

RJ01 Rejection of invention patent application after publication
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1165310

Country of ref document: HK