KR102158992B1 - 소-분자 ｇｌｐ1ｒ 아고니스트의 트리스(하이드록시메틸)아미노메탄 염과 그것의 제약 조성물 및 사용 - Google Patents

소-분자 ｇｌｐ1ｒ 아고니스트의 트리스(하이드록시메틸)아미노메탄 염과 그것의 제약 조성물 및 사용 Download PDF

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KR102158992B1
KR102158992B1 KR1020147026362A KR20147026362A KR102158992B1 KR 102158992 B1 KR102158992 B1 KR 102158992B1 KR 1020147026362 A KR1020147026362 A KR 1020147026362A KR 20147026362 A KR20147026362 A KR 20147026362A KR 102158992 B1 KR102158992 B1 KR 102158992B1
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다닐로 알마리에고
다마 라오 폴리세티
에릭 벤자민
압델라위 하산 엘
숨야 피. 사후
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브이티브이 테라퓨틱스 엘엘씨
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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • 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
    • A61P3/08—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
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2/00—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic
    • B01J2/02—Processes or devices for granulating materials, e.g. fertilisers in general; Rendering particulate materials free flowing in general, e.g. making them hydrophobic by dividing the liquid material into drops, e.g. by spraying, and solidifying the drops
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Inorganic Chemistry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020147026362A 2012-03-22 2013-03-20 소-분자 ｇｌｐ1ｒ 아고니스트의 트리스(하이드록시메틸)아미노메탄 염과 그것의 제약 조성물 및 사용 Active KR102158992B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261614265P 2012-03-22 2012-03-22
US61/614,265 2012-03-22
PCT/US2013/033091 WO2013142569A1 (en) 2012-03-22 2013-03-20 Tris(hydroxymethyl)aminomethane salts of a small-molecule glp1r agonist and pharmaceutical compositions and uses thereof

Publications (2)

Publication Number Publication Date
KR20140138758A KR20140138758A (ko) 2014-12-04
KR102158992B1 true KR102158992B1 (ko) 2020-09-23

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KR1020147026362A Active KR102158992B1 (ko) 2012-03-22 2013-03-20 소-분자 ｇｌｐ1ｒ 아고니스트의 트리스(하이드록시메틸)아미노메탄 염과 그것의 제약 조성물 및 사용

Country Status (16)

Country Link
US (1) US9198901B2 (OSRAM)
EP (1) EP2854526B1 (OSRAM)
JP (1) JP2015510947A (OSRAM)
KR (1) KR102158992B1 (OSRAM)
CN (1) CN104202977A (OSRAM)
AU (1) AU2013235167B2 (OSRAM)
CA (1) CA2868033A1 (OSRAM)
EA (1) EA201491749A1 (OSRAM)
ES (1) ES2674951T3 (OSRAM)
HK (1) HK1199371A1 (OSRAM)
IL (1) IL234615B (OSRAM)
IN (1) IN2014DN07867A (OSRAM)
MX (1) MX352804B (OSRAM)
NZ (1) NZ629203A (OSRAM)
SG (1) SG11201405353VA (OSRAM)
WO (1) WO2013142569A1 (OSRAM)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20260036616A (ko) * 2018-05-08 2026-03-17 브이티브이 테라퓨틱스 엘엘씨 Glp1r 작용제의 치료적 용도
EP4141008A4 (en) 2020-04-01 2024-04-17 Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd. PHARMACEUTICALLY ACCEPTABLE ACID SALT OF GLP-1 RECEPTOR AGONIST FREE BASE, AND PREPARATION METHOD THEREFOR
JP2023528565A (ja) 2020-04-01 2023-07-05 ハンジョウ ジョンメイ フアドン ファーマシューティカル シーオー．，エルティーディー． Ｇｌｐ－１受容体アゴニストの結晶形ａおよびその調製法
AU2024340407A1 (en) 2023-09-14 2026-04-23 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025109387A1 (en) 2023-11-24 2025-05-30 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
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

Citations (3)

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Publication number Priority date Publication date Assignee Title
US20100022601A1 (en) * 2008-06-05 2010-01-28 Asahi Kasei Pharma Corporation Sulfonamide compounds and the use
US20100324033A1 (en) * 2008-03-07 2010-12-23 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
US20110064806A1 (en) * 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

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DE69733752T2 (de) * 1996-05-20 2006-06-01 G.D. Searle Llc, Chicago Arzneimittel enthaltend oxaprozin-natriumsalz,-kaliumsalz, oder-tris(hydroxymethyl)aminomethansalz
AR024076A1 (es) * 1999-05-25 2002-09-04 Smithkline Beecham Corp Sales de cis-[4-ciano-4-(3-ciclopentiloxi-4-metoxifenil) ciclohexan-1-carboxilato]
CA2436738A1 (en) * 2001-02-05 2002-08-15 Dr. Reddy's Laboratories Ltd. Salts of pyrimidine derivatives for use against coronary heart disease and atherosclerose
CA2463615C (en) * 2001-10-30 2011-07-26 Applied Research Systems Ars Holding N.V. Oxindole hydrazide modulators of protein tyrosine phosphatases (ptps)
ZA200509355B (en) * 2003-04-18 2007-03-28 Incyte San Diego Inc Substituted isochroman compounds for the treatment of metabolic disorders, cancer and other diseases
JP5627453B2 (ja) * 2008-03-31 2014-11-19 株式会社レナサイエンス プラスミノーゲンアクチベーターインヒビター−１阻害剤
RS53777B1 (sr) * 2008-12-08 2015-06-30 Glaxosmithkline Llc Anhidrid 8-hlor-3-pentil-3,7-dihidro-1h-purin-2,6-dion 2-amino-2-(hidroksimetil)-1,3-propandiola za lečenje bolesti

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
US20100324033A1 (en) * 2008-03-07 2010-12-23 Transtech Pharma, Inc. Oxadiazoanthracene compounds for the treatment of diabetes
US20100022601A1 (en) * 2008-06-05 2010-01-28 Asahi Kasei Pharma Corporation Sulfonamide compounds and the use
US20110064806A1 (en) * 2009-09-11 2011-03-17 Transtech Pharma, Inc. Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

Also Published As

Publication number Publication date
WO2013142569A1 (en) 2013-09-26
EA201491749A1 (ru) 2015-01-30
AU2013235167B2 (en) 2017-03-30
ES2674951T8 (es) 2018-08-23
AU2013235167A1 (en) 2014-09-18
HK1199371A1 (en) 2015-07-03
IN2014DN07867A (OSRAM) 2015-04-24
US20150005339A1 (en) 2015-01-01
KR20140138758A (ko) 2014-12-04
IL234615B (en) 2018-02-28
MX352804B (es) 2017-12-08
US9198901B2 (en) 2015-12-01
CA2868033A1 (en) 2013-09-26
MX2014010366A (es) 2015-05-15
EP2854526B1 (en) 2018-04-25
SG11201405353VA (en) 2014-09-26
ES2674951T3 (es) 2018-07-05
EP2854526A4 (en) 2016-02-24
JP2015510947A (ja) 2015-04-13
EP2854526A1 (en) 2015-04-08
CN104202977A (zh) 2014-12-10
NZ629203A (en) 2015-12-24

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