WO2007082264A3 - Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions - Google Patents

Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions Download PDF

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Publication number
WO2007082264A3
WO2007082264A3 PCT/US2007/060383 US2007060383W WO2007082264A3 WO 2007082264 A3 WO2007082264 A3 WO 2007082264A3 US 2007060383 W US2007060383 W US 2007060383W WO 2007082264 A3 WO2007082264 A3 WO 2007082264A3
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WO
WIPO (PCT)
Prior art keywords
peptide
glp
diabetes
treatment
human glucagon
Prior art date
Application number
PCT/US2007/060383
Other languages
French (fr)
Other versions
WO2007082264A2 (en
Inventor
Tasir Shamsul Haque
William R Ewing
Claudio Mapelli
Ving G Lee
Richard B Sulsky
Douglas James Riexinger
Rogelio L Martinez
Yeheng Zhu
Zheming Ruan
Original Assignee
Bristol Myers Squibb Co
Tasir Shamsul Haque
William R Ewing
Claudio Mapelli
Ving G Lee
Richard B Sulsky
Douglas James Riexinger
Rogelio L Martinez
Yeheng Zhu
Zheming Ruan
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 Bristol Myers Squibb Co, Tasir Shamsul Haque, William R Ewing, Claudio Mapelli, Ving G Lee, Richard B Sulsky, Douglas James Riexinger, Rogelio L Martinez, Yeheng Zhu, Zheming Ruan filed Critical Bristol Myers Squibb Co
Priority to EP07717953A priority Critical patent/EP1976873A2/en
Priority to JP2008550516A priority patent/JP2009523177A/en
Publication of WO2007082264A2 publication Critical patent/WO2007082264A2/en
Publication of WO2007082264A3 publication Critical patent/WO2007082264A3/en
Priority to NO20082958A priority patent/NO20082958L/en

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    • 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
    • C07K14/575—Hormones
    • C07K14/605—Glucagons
    • 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
    • A61K38/26—Glucagons
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P25/00—Drugs for disorders of the nervous 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • 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
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/16—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/18—Fluorenes; Hydrogenated fluorenes

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Biophysics (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Urology & Nephrology (AREA)
  • Toxicology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Peptides Or Proteins (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Vascular Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified compounds that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The compounds of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.
PCT/US2007/060383 2006-01-11 2007-01-11 Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions WO2007082264A2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
EP07717953A EP1976873A2 (en) 2006-01-11 2007-01-11 Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions
JP2008550516A JP2009523177A (en) 2006-01-11 2007-01-11 Human glucagon-like peptide-1 modulator and its use in the treatment of diabetes and related conditions
NO20082958A NO20082958L (en) 2006-01-11 2008-07-03 Human glucagon-like peptide-1 modulators and their use in the treatment of diabetes and related conditions

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US75810706P 2006-01-11 2006-01-11
US75809606P 2006-01-11 2006-01-11
US75816406P 2006-01-11 2006-01-11
US75816506P 2006-01-11 2006-01-11
US60/758,165 2006-01-11
US60/758,107 2006-01-11
US60/758,164 2006-01-11
US60/758,096 2006-01-11

Publications (2)

Publication Number Publication Date
WO2007082264A2 WO2007082264A2 (en) 2007-07-19
WO2007082264A3 true WO2007082264A3 (en) 2007-12-21

Family

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Family Applications (1)

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PCT/US2007/060383 WO2007082264A2 (en) 2006-01-11 2007-01-11 Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions

Country Status (5)

Country Link
US (1) US20070238669A1 (en)
EP (1) EP1976873A2 (en)
JP (1) JP2009523177A (en)
NO (1) NO20082958L (en)
WO (1) WO2007082264A2 (en)

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MX2010006287A (en) 2007-12-11 2010-10-26 Cadila Healthcare Ltd Peptidomimetics with glucagon antagonistic and glp-1 agonistic activities.
US20120264685A1 (en) 2009-10-22 2012-10-18 Rajesh Bahekar Short chain peptidomimetics based orally active glp 1 agonist and glucagon receptor antagonist
US20140066370A1 (en) 2009-11-23 2014-03-06 Amylin Pharmaceuticals, Llc Polypeptide Conjugate
KR20130101005A (en) * 2010-07-28 2013-09-12 아밀린 파마슈티칼스, 엘엘씨. Glp-1 receptor agonist compounds having stabilized regions
CN103370083B (en) 2010-09-28 2016-11-16 艾米琳制药有限责任公司 There is the engineered polypeptide of the acting duration of enhancing
BR122021020041B1 (en) 2010-09-28 2023-03-07 Amylin Pharmaceuticals, Llc CHIMERIC POLYPEPTIDE, ITS USE AND COMPOSITION INCLUDING IT
US20140221282A1 (en) 2011-05-25 2014-08-07 Astrazeneca Pharmaceuticals Lp Long duration dual hormone conjugates
JP6040464B2 (en) 2011-07-08 2016-12-07 アエゲリオン・ファーマシューティカルズ・インコーポレイテッドＡｅｇｅｒｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． Engineered polypeptides with increased duration of action and reduced immunogenicity
EP2729481B1 (en) 2011-07-08 2018-10-17 Amylin Pharmaceuticals, LLC Engineered polypeptides having enhanced duration of action with reduced immunogenicity
CN102363633B (en) * 2011-11-16 2013-11-20 天津拓飞生物科技有限公司 Glucagon like peptide-1 mutant polypeptide and preparation method, medicinal composition and use thereof
US20220024901A1 (en) 2018-11-22 2022-01-27 Qilu Regor Therapeutics Inc. Glp-1r agonists and uses thereof
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
EP3842449A1 (en) * 2019-12-23 2021-06-30 Merck Sharp & Dohme Corp. Stapled olefin co-agonists of the glucagon and glp-1 receptors
WO2022266467A2 (en) 2021-06-17 2022-12-22 Dana-Farber Cancer Institute, Inc. Recombinant histone polypeptide and uses thereof
CN114196317B (en) * 2021-12-16 2022-11-25 新沂肽科生物科技有限公司 Modified gamma-polyglutamic acid anti-fog coating material and preparation method and application thereof

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