CN112263552A - 包括葡糖激酶活化剂的固体组合物及其制备和使用方法 - Google Patents

包括葡糖激酶活化剂的固体组合物及其制备和使用方法 Download PDF

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Publication number
CN112263552A
CN112263552A CN202011088593.3A CN202011088593A CN112263552A CN 112263552 A CN112263552 A CN 112263552A CN 202011088593 A CN202011088593 A CN 202011088593A CN 112263552 A CN112263552 A CN 112263552A
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China
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solid composition
cyclohexyl
grams
ylsulfanyl
ureido
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Pending
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CN202011088593.3A
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English (en)
Chinese (zh)
Inventor
E.本杰明
T.索尔斯坦森
S.K.拉普鲁
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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
    • 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
    • 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
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • A—HUMAN NECESSITIES
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    • 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
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • A61K47/02—Inorganic compounds
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
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    • 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
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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    • 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
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2027—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
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • 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
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K9/1682—Processes
    • A61K9/1694—Processes resulting in granules or microspheres of the matrix type containing more than 5% of excipient

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  • Health & Medical Sciences (AREA)
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  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Biochemistry (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
CN202011088593.3A 2013-03-04 2014-02-28 包括葡糖激酶活化剂的固体组合物及其制备和使用方法 Pending CN112263552A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361771969P 2013-03-04 2013-03-04
US61/771,969 2013-03-04
CN201480011657.6A CN105188676A (zh) 2013-03-04 2014-02-28 包括葡糖激酶活化剂的固体组合物及其制备和使用方法

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CN201480011657.6A Pending CN105188676A (zh) 2013-03-04 2014-02-28 包括葡糖激酶活化剂的固体组合物及其制备和使用方法

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US (4) US20160015816A1 (cg-RX-API-DMAC7.html)
EP (1) EP2964197B1 (cg-RX-API-DMAC7.html)
JP (1) JP6441829B2 (cg-RX-API-DMAC7.html)
KR (2) KR20150126362A (cg-RX-API-DMAC7.html)
CN (2) CN112263552A (cg-RX-API-DMAC7.html)
AU (1) AU2014226292B2 (cg-RX-API-DMAC7.html)
CA (1) CA2903440C (cg-RX-API-DMAC7.html)
ES (1) ES2794018T3 (cg-RX-API-DMAC7.html)
HK (1) HK1213197A1 (cg-RX-API-DMAC7.html)
IL (1) IL240729A0 (cg-RX-API-DMAC7.html)
MX (1) MX2015011110A (cg-RX-API-DMAC7.html)
WO (1) WO2014137799A1 (cg-RX-API-DMAC7.html)

Families Citing this family (12)

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SI2576524T1 (en) 2010-05-26 2018-01-31 Vtv Therapeutics Llc USE OF METFORMIN IN COMBINATION WITH GLUCOIN-ACTIVE ACTIVATORS, ALSO THE COMPOSITION, COMPARING METFORMIN AND GLUCOIN-ACTIVE ACTUATOR
JP6234443B2 (ja) 2012-05-17 2017-11-22 ブイティーブイ・セラピューティクス・エルエルシー 糖尿病治療のためのグルコキナーゼ活性化因子組成物
RU2728824C1 (ru) * 2016-12-15 2020-07-31 Хуа Медсин (Шанхай) Лтд. Препарат активатора глюкокиназы для перорального введения и способ его получения
US11541015B2 (en) 2017-05-17 2023-01-03 Massachusetts Institute Of Technology Self-righting systems, methods, and related components
AU2018269711B2 (en) 2017-05-17 2023-07-27 Massachusetts Institute Of Technology Self-righting systems and related components and methods
AU2019269636A1 (en) 2018-05-17 2020-11-19 Massachusetts Institute Of Technology Systems for electrical stimulation
CN112040945A (zh) 2018-06-12 2020-12-04 Vtv治疗有限责任公司 葡萄糖激酶激活剂与胰岛素或胰岛素类似物组合的治疗用途
EP3917598B1 (en) 2019-02-01 2025-10-29 Massachusetts Institute of Technology Systems for liquid injection
EP3819336A1 (en) * 2019-11-08 2021-05-12 Roquette Freres Use of octenyl-succinate starches as a binder in wet granulation
US12391658B2 (en) 2020-02-18 2025-08-19 Vtv Therapeutics Llc Sulfoxide and sulfone glucokinase activators and methods of use thereof
AU2021289309A1 (en) 2020-06-08 2023-01-19 Vtv Therapeutics Llc Salts or co-crystals of {2-[3-cyclohexyl-3-(trans-4-propoxy-cyclohexyl)-ureido]-thiazol-5-ylsulfanyl}-acetic acid and uses thereof
JP2023530785A (ja) * 2020-06-08 2023-07-19 ブイティーブイ・セラピューティクス・エルエルシー ｛２－［３－シクロヘキシル－３－（ｔｒａｎｓ－４－プロポキシ－シクロヘキシル）－ウレイド］－チアゾール－５－イルスルファニル｝－酢酸の結晶形およびその使用

Citations (1)

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CN102906077A (zh) * 2010-05-26 2013-01-30 转化技术制药公司 二甲双胍与葡萄糖激酶激活剂的联合使用以及包含二甲双胍和葡萄糖激酶激活剂的组合物

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PT1723128E (pt) * 2004-01-06 2013-02-27 Novo Nordisk As Heteroaril-ureias e o seu uso como activadores da glicoquinase
CN1910166B (zh) * 2004-01-06 2012-01-04 诺和诺德公司 杂芳基脲及其作为葡糖激酶活化剂的用途
JP2023530785A (ja) * 2020-06-08 2023-07-19 ブイティーブイ・セラピューティクス・エルエルシー ｛２－［３－シクロヘキシル－３－（ｔｒａｎｓ－４－プロポキシ－シクロヘキシル）－ウレイド］－チアゾール－５－イルスルファニル｝－酢酸の結晶形およびその使用

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102906077A (zh) * 2010-05-26 2013-01-30 转化技术制药公司 二甲双胍与葡萄糖激酶激活剂的联合使用以及包含二甲双胍和葡萄糖激酶激活剂的组合物

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US20190046645A1 (en) 2019-02-14
US20220233701A1 (en) 2022-07-28
JP2016510741A (ja) 2016-04-11
US20250288681A1 (en) 2025-09-18
KR20220009496A (ko) 2022-01-24
KR102694699B1 (ko) 2024-08-12
ES2794018T3 (es) 2020-11-17
CA2903440A1 (en) 2014-09-12
CN105188676A (zh) 2015-12-23
IL240729A0 (en) 2015-10-29
JP6441829B2 (ja) 2018-12-19
CA2903440C (en) 2021-04-13
US20160015816A1 (en) 2016-01-21
MX2015011110A (es) 2015-10-29
HK1213197A1 (zh) 2016-06-30
AU2014226292A1 (en) 2015-10-08
EP2964197B1 (en) 2020-03-25
EP2964197A1 (en) 2016-01-13
KR20150126362A (ko) 2015-11-11
AU2014226292B2 (en) 2018-10-04
WO2014137799A1 (en) 2014-09-12

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