AU2014207748B2 - Combinations of a GLP1R agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders - Google Patents

Combinations of a GLP1R agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders Download PDF

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Publication number
AU2014207748B2
AU2014207748B2 AU2014207748A AU2014207748A AU2014207748B2 AU 2014207748 B2 AU2014207748 B2 AU 2014207748B2 AU 2014207748 A AU2014207748 A AU 2014207748A AU 2014207748 A AU2014207748 A AU 2014207748A AU 2014207748 B2 AU2014207748 B2 AU 2014207748B2
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Prior art keywords
metformin
phenyl
glp1r agonist
agonist
day
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AU2014207748A
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AU2014207748A1 (en
Inventor
Robert Carl Andrews
Bradley Alan CLARK
Stephen Thomas Davis
Adnan M. M. Mjalli
Dharma Rao Polisetti
James C. Quada Jr.
Maria Carmen Valcarce Lopez
Thomas Scott Yokum
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vTv Therapeutics LLC
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vTv Therapeutics LLC
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • 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
    • 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
    • C07C279/00—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups
    • C07C279/20—Derivatives of guanidine, i.e. compounds containing the group, the singly-bound nitrogen atoms not being part of nitro or nitroso groups containing any of the groups, X being a hetero atom, Y being any atom, e.g. acylguanidines
    • C07C279/24—Y being a hetero atom
    • C07C279/26—X and Y being nitrogen atoms, i.e. biguanides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2014207748A 2013-01-17 2014-01-14 Combinations of a GLP1R agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders Active AU2014207748B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361753567P 2013-01-17 2013-01-17
US61/753,567 2013-01-17
PCT/US2014/011394 WO2014113357A1 (en) 2013-01-17 2014-01-14 Combinations of a glp1r agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders

Publications (2)

Publication Number Publication Date
AU2014207748A1 AU2014207748A1 (en) 2015-07-09
AU2014207748B2 true AU2014207748B2 (en) 2018-10-11

Family

ID=50030537

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2014207748A Active AU2014207748B2 (en) 2013-01-17 2014-01-14 Combinations of a GLP1R agonist and metformin and use thereof for the treatment of type 2 diabetes and other disorders

Country Status (13)

Country Link
US (1) US20150313908A1 (enExample)
EP (1) EP2945618B1 (enExample)
JP (1) JP6445459B2 (enExample)
KR (1) KR102165434B1 (enExample)
CN (1) CN104968341B (enExample)
AU (1) AU2014207748B2 (enExample)
CA (1) CA2896308C (enExample)
EA (1) EA201591123A1 (enExample)
ES (1) ES2687083T3 (enExample)
IL (1) IL239714A0 (enExample)
MX (1) MX366685B (enExample)
SG (2) SG10201704716XA (enExample)
WO (1) WO2014113357A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3684793A1 (en) 2017-09-22 2020-07-29 Regeneron Pharmaceuticals, Inc. Glucagon-like peptide 1 receptor agonists and uses thereof
WO2019217165A1 (en) * 2018-05-08 2019-11-14 Vtv Therapeutics Llc Therapeutic uses of glp1r agonists
EP4130005A4 (en) * 2020-04-01 2024-04-24 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. CRYSTALLINE FORM A OF A GLP-1 RECEPTOR AGONIST AND METHOD OF MANUFACTURING THEREOF
CN115315426B (zh) * 2020-04-01 2023-12-12 杭州中美华东制药有限公司 Glp-1受体激动剂游离碱的药学上可接受的酸式盐及其制备方法
US12582651B2 (en) * 2020-12-31 2026-03-24 Dong Kook Pharm. Co., Ltd. Pharmaceutical composition comprising tadalafil or pharmaceutically acceptable salt thereof and dutasteride or pharmaceutically acceptable salt thereof exhibiting novel dissolution rate
JP2025532651A (ja) 2022-09-21 2025-10-01 リジェネロン・ファーマシューティカルズ・インコーポレイテッド 肥満、糖尿病および肝機能障害を処置する方法
WO2025158275A1 (en) 2024-01-24 2025-07-31 Pfizer Inc. Combination therapy using glucose-dependent insulinotropic polypeptide receptor antagonist compounds and glp-1 receptor agonist compounds
US20260199503A1 (en) 2025-01-10 2026-07-16 Regeneron Pharmaceuticals, Inc. Glp1r agonist-tethered gdf8 antibody conjugates and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009111700A2 (en) * 2008-03-07 2009-09-11 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
US20110118180A1 (en) * 2009-11-13 2011-05-19 Sanofi-Aventis Deutschland Gmbh Method of treatment of diabetes type 2 comprising add-on therapy to metformin
US20120295846A1 (en) * 2009-11-13 2012-11-22 Sanofi-Aventis Deutschland Gmbh Pharmaceutical composition comprising a glp-1 agonist, an insulin and methionine
WO2012156312A1 (en) * 2011-05-13 2012-11-22 Sanofi-Aventis Deutschland Gmbh Pharmaceutical combination for use in the treatment of diabetes type 2

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4080472A (en) 1974-03-22 1978-03-21 Societe D'etudes Et D'exploitation De Marques Et Brevets S.E.M.S. Metformin 2-(p-chlorophenoxy)-2-methylpropionate
AU2006311601A1 (en) * 2005-11-07 2007-05-18 Elixir Pharmaceuticals, Inc. Combinations of metformin and meglitinide
MX2011010347A (es) * 2009-03-30 2011-11-29 Transtech Pharma Inc Derivados sustituidos de azoantraceno, composiciones farmaceuticas y metodos de uso de los mismos.
WO2011031620A1 (en) 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009111700A2 (en) * 2008-03-07 2009-09-11 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
US20110118180A1 (en) * 2009-11-13 2011-05-19 Sanofi-Aventis Deutschland Gmbh Method of treatment of diabetes type 2 comprising add-on therapy to metformin
US20120295846A1 (en) * 2009-11-13 2012-11-22 Sanofi-Aventis Deutschland Gmbh Pharmaceutical composition comprising a glp-1 agonist, an insulin and methionine
WO2012156312A1 (en) * 2011-05-13 2012-11-22 Sanofi-Aventis Deutschland Gmbh Pharmaceutical combination for use in the treatment of diabetes type 2

Also Published As

Publication number Publication date
AU2014207748A1 (en) 2015-07-09
MX2015008555A (es) 2016-01-22
ES2687083T3 (es) 2018-10-23
EP2945618B1 (en) 2018-06-13
SG11201504778UA (en) 2015-07-30
EP2945618A1 (en) 2015-11-25
IL239714A0 (en) 2015-08-31
KR102165434B1 (ko) 2020-10-14
MX366685B (es) 2019-07-19
WO2014113357A1 (en) 2014-07-24
JP6445459B2 (ja) 2018-12-26
EA201591123A1 (ru) 2015-11-30
KR20150104572A (ko) 2015-09-15
HK1210424A1 (en) 2016-04-22
CA2896308A1 (en) 2014-07-24
SG10201704716XA (en) 2017-07-28
US20150313908A1 (en) 2015-11-05
CN104968341B (zh) 2020-06-09
JP2016505039A (ja) 2016-02-18
CA2896308C (en) 2021-11-09
CN104968341A (zh) 2015-10-07

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