CN104202977A - 小分子glp1r激动剂的三(羟甲基)氨基甲烷盐及其药物组合物和用途 - Google Patents

小分子glp1r激动剂的三(羟甲基)氨基甲烷盐及其药物组合物和用途 Download PDF

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Publication number
CN104202977A
CN104202977A CN201380015508.2A CN201380015508A CN104202977A CN 104202977 A CN104202977 A CN 104202977A CN 201380015508 A CN201380015508 A CN 201380015508A CN 104202977 A CN104202977 A CN 104202977A
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solid composite
salt
tris
odaad1
patient
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Chinese (zh)
Inventor
D·阿尔玛里戈
D·R·珀里斯蒂
E·本杰明
H·艾尔阿博德劳伊
S·P·萨霍
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vTv Therapeutics LLC
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Trans Tech Pharma Inc
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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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  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Inorganic Chemistry (AREA)
  • Nutrition Science (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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)
CN201380015508.2A 2012-03-22 2013-03-20 小分子glp1r激动剂的三(羟甲基)氨基甲烷盐及其药物组合物和用途 Pending CN104202977A (zh)

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 (1)

Publication Number Publication Date
CN104202977A true CN104202977A (zh) 2014-12-10

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CN201380015508.2A Pending CN104202977A (zh) 2012-03-22 2013-03-20 小分子glp1r激动剂的三(羟甲基)氨基甲烷盐及其药物组合物和用途

Country Status (16)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021196951A1 (zh) * 2020-04-01 2021-10-07 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
WO2021196949A1 (zh) * 2020-04-01 2021-10-07 杭州中美华东制药有限公司 一种glp-1受体激动剂的晶型a及其制备方法

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3790549A1 (en) * 2018-05-08 2021-03-17 vTv Therapeutics LLC Therapeutic uses of glp1r agonists
TW202521533A (zh) 2023-09-14 2025-06-01 香港商歌禮製藥(中國)有限公司 Glp-1r 激動劑及其治療方法
US12291530B1 (en) 2023-11-24 2025-05-06 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 (6)

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CN1225580A (zh) * 1996-05-20 1999-08-11 G·D·瑟尔公司 钾、钠和三羟甲基氨基甲烷噁丙秦盐药物配方
CN1351491A (zh) * 1999-05-25 2002-05-29 史密丝克莱恩比彻姆公司 顺－[4－氰基－4－(3－环戊氧基－4－甲氧苯基)环己烷－1－羧酸]的盐类
CN101959405A (zh) * 2008-03-07 2011-01-26 转化技术制药公司 治疗糖尿病的氧杂二氮杂蒽化合物
TW201114422A (en) * 2009-09-11 2011-05-01 Transtech Pharma Inc Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same
CN102056897A (zh) * 2008-06-05 2011-05-11 旭化成制药株式会社 磺酰胺化合物及其用途
CN102245606A (zh) * 2008-12-08 2011-11-16 葛兰素史密斯克莱有限责任公司 新化合物

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JP2004520393A (ja) * 2001-02-05 2004-07-08 ドクター・レディーズ・ラボラトリーズ・リミテッド ヘテロ環化号物の薬学的に許容可能な塩
US7696231B2 (en) * 2001-10-30 2010-04-13 Laboratoires Serono Sa Oxindole hydrazide modulators of protein tyrosine phosphatases (PTPs)
CN1774246A (zh) * 2003-04-18 2006-05-17 因齐特圣迭戈公司 用于治疗代谢失调、癌症和其它疾病的取代异色满化合物
WO2009123241A1 (ja) * 2008-03-31 2009-10-08 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

Patent Citations (6)

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CN1225580A (zh) * 1996-05-20 1999-08-11 G·D·瑟尔公司 钾、钠和三羟甲基氨基甲烷噁丙秦盐药物配方
CN1351491A (zh) * 1999-05-25 2002-05-29 史密丝克莱恩比彻姆公司 顺－[4－氰基－4－(3－环戊氧基－4－甲氧苯基)环己烷－1－羧酸]的盐类
CN101959405A (zh) * 2008-03-07 2011-01-26 转化技术制药公司 治疗糖尿病的氧杂二氮杂蒽化合物
CN102056897A (zh) * 2008-06-05 2011-05-11 旭化成制药株式会社 磺酰胺化合物及其用途
CN102245606A (zh) * 2008-12-08 2011-11-16 葛兰素史密斯克莱有限责任公司 新化合物
TW201114422A (en) * 2009-09-11 2011-05-01 Transtech Pharma Inc Solid compositions comprising an oxadiazoanthracene compound and methods of making and using the same

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021196951A1 (zh) * 2020-04-01 2021-10-07 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
WO2021196949A1 (zh) * 2020-04-01 2021-10-07 杭州中美华东制药有限公司 一种glp-1受体激动剂的晶型a及其制备方法
CN115315426A (zh) * 2020-04-01 2022-11-08 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
CN115461344A (zh) * 2020-04-01 2022-12-09 杭州中美华东制药有限公司 一种glp-1受体激动剂的晶型a及其制备方法
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
CN115461344B (zh) * 2020-04-01 2024-01-12 杭州中美华东制药有限公司 一种glp-1受体激动剂的晶型a及其制备方法
US12421245B2 (en) 2020-04-01 2025-09-23 Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd. Pharmaceutically acceptable acid salt of free base of GLP1 receptor agonist, and preparation method therefor
US12459954B2 (en) 2020-04-01 2025-11-04 Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd. Crystalline form a of GLP-1 receptor agonist and preparation method therefor

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Publication number Publication date
AU2013235167B2 (en) 2017-03-30
JP2015510947A (ja) 2015-04-13
EP2854526A1 (en) 2015-04-08
CA2868033A1 (en) 2013-09-26
KR102158992B1 (ko) 2020-09-23
MX352804B (es) 2017-12-08
EP2854526B1 (en) 2018-04-25
NZ629203A (en) 2015-12-24
AU2013235167A1 (en) 2014-09-18
ES2674951T8 (es) 2018-08-23
KR20140138758A (ko) 2014-12-04
US20150005339A1 (en) 2015-01-01
US9198901B2 (en) 2015-12-01
EA201491749A1 (ru) 2015-01-30
SG11201405353VA (en) 2014-09-26
MX2014010366A (es) 2015-05-15
IN2014DN07867A (https=) 2015-04-24
IL234615B (en) 2018-02-28
EP2854526A4 (en) 2016-02-24
WO2013142569A1 (en) 2013-09-26
ES2674951T3 (es) 2018-07-05
HK1199371A1 (en) 2015-07-03

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