CA2903433A1 - Stable glucokinase activator compositions - Google Patents
Stable glucokinase activator compositions Download PDFInfo
- Publication number
- CA2903433A1 CA2903433A1 CA2903433A CA2903433A CA2903433A1 CA 2903433 A1 CA2903433 A1 CA 2903433A1 CA 2903433 A CA2903433 A CA 2903433A CA 2903433 A CA2903433 A CA 2903433A CA 2903433 A1 CA2903433 A1 CA 2903433A1
- Authority
- CA
- Canada
- Prior art keywords
- cyclohexyl
- propoxy
- acetic acid
- trans
- ureido
- Prior art date
- Legal status (The legal status 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 status listed.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims description 79
- 229940124828 glucokinase activator Drugs 0.000 title description 2
- 238000000034 method Methods 0.000 claims abstract description 64
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 63
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 145
- 239000002105 nanoparticle Substances 0.000 claims description 105
- 239000003795 chemical substances by application Substances 0.000 claims description 69
- 239000000725 suspension Substances 0.000 claims description 61
- 150000003839 salts Chemical class 0.000 claims description 51
- 239000003381 stabilizer Substances 0.000 claims description 43
- 239000011230 binding agent Substances 0.000 claims description 34
- 229940079593 drug Drugs 0.000 claims description 31
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- 239000000594 mannitol Substances 0.000 claims description 22
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- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 15
- 239000002904 solvent Substances 0.000 claims description 14
- HPGJSAAUJGAMLV-UHFFFAOYSA-N 2-[[2-[[cyclohexyl-(4-propoxycyclohexyl)carbamoyl]amino]-1,3-thiazol-5-yl]sulfanyl]acetic acid Chemical compound C1CC(OCCC)CCC1N(C(=O)NC=1SC(SCC(O)=O)=CN=1)C1CCCCC1 HPGJSAAUJGAMLV-UHFFFAOYSA-N 0.000 claims description 10
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Classifications
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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
- A61K9/141—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
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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
- A61K31/41—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
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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
- A61K31/41—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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- 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
- A61K9/146—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 macromolecular compounds
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- 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
Landscapes
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- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Bioinformatics & Cheminformatics (AREA)
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- Chemical Kinetics & Catalysis (AREA)
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- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US201361772022P | 2013-03-04 | 2013-03-04 | |
| US61/772,022 | 2013-03-04 | ||
| PCT/US2014/019349 WO2014137797A2 (en) | 2013-03-04 | 2014-02-28 | Stable glucokinase activator compositions |
Publications (1)
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| CA2903433A1 true CA2903433A1 (en) | 2014-09-12 |
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| CA2903433A Abandoned CA2903433A1 (en) | 2013-03-04 | 2014-02-28 | Stable glucokinase activator compositions |
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| EP (1) | EP2964198A2 (cg-RX-API-DMAC7.html) |
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| WO (1) | WO2014137797A2 (cg-RX-API-DMAC7.html) |
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| KR101878252B1 (ko) | 2010-05-26 | 2018-07-13 | 브이티브이 테라퓨틱스 엘엘씨 | 글루코키나아제 활성화제와 병용되는 메트포르민의 용도, 및 메트포르민과 글루코키나아제 활성화제를 포함하는 조성물 |
| HK1202458A1 (en) | 2012-05-17 | 2015-10-02 | Vtv治疗有限责任公司 | Glucokinase activator compositions for the treatment of diabetes |
| CN109674752B (zh) * | 2016-12-15 | 2022-10-11 | 华领医药技术（上海）有限公司 | 葡萄糖激酶激活剂的口服制剂及其制备方法 |
| MX2020008905A (es) | 2018-06-12 | 2020-12-03 | Vtv Therapeutics Llc | Usos terapeuticos de activadores de glucoquinasa en combinacion con insulina o analogos de insulinas. |
| US12391658B2 (en) | 2020-02-18 | 2025-08-19 | Vtv Therapeutics Llc | Sulfoxide and sulfone glucokinase activators and methods of use thereof |
| US11857536B2 (en) | 2020-06-04 | 2024-01-02 | Hua Medicine (Shanghai) Ltd. | Glucokinase activator for treating diabetes with renal impairment |
| AU2020451588A1 (en) * | 2020-06-04 | 2023-01-19 | Hua Medicine (Shanghai) Ltd. | Glucokinase activator for treating diabetes with renal impairment |
| WO2021252311A1 (en) * | 2020-06-08 | 2021-12-16 | 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 |
| CN116056760A (zh) * | 2020-06-08 | 2023-05-02 | 维特卫治疗有限责任公司 | {2-[3-环己基-3-(反式-4-丙氧基-环己基)-脲基]-噻唑-5-基硫烷基}-乙酸的结晶形式及其用途 |
| KR20240084229A (ko) * | 2022-12-06 | 2024-06-13 | 유노비아 주식회사 | 안정성이 향상된 gpr40 효현제를 유효성분으로 포함하는 약제학적 조성물 |
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| US5552160A (en) * | 1991-01-25 | 1996-09-03 | Nanosystems L.L.C. | Surface modified NSAID nanoparticles |
| US6375986B1 (en) * | 2000-09-21 | 2002-04-23 | Elan Pharma International Ltd. | Solid dose nanoparticulate compositions comprising a synergistic combination of a polymeric surface stabilizer and dioctyl sodium sulfosuccinate |
| US6316029B1 (en) * | 2000-05-18 | 2001-11-13 | Flak Pharma International, Ltd. | Rapidly disintegrating solid oral dosage form |
| EP1429731B1 (en) * | 2001-09-19 | 2007-01-03 | Elan Pharma International Limited | Nanoparticulate insulin formulations |
| WO2003094894A1 (en) * | 2002-05-06 | 2003-11-20 | Elan Pharma International Ltd. | Nanoparticulate nystatin formulations |
| JP2005531606A (ja) * | 2002-06-10 | 2005-10-20 | エラン ファーマ インターナショナル，リミティド | ナノ粒子ステロール製剤およびステロールの組合せ |
| AU2003241477A1 (en) * | 2002-06-10 | 2003-12-22 | Elan Pharma International, Ltd. | Nanoparticulate polycosanol formulations and novel polycosanol combinations |
| MXPA06007667A (es) * | 2004-01-06 | 2006-09-01 | Novo Nordisk As | Heteroaril-ureas y su uso como activadores de glucocinasa. |
| CA2587710C (en) * | 2004-11-16 | 2014-10-21 | Elan Pharma International Ltd. | Injectable nanoparticulate olanzapine formulations |
| UA89513C2 (uk) * | 2004-12-03 | 2010-02-10 | Элан Фарма Интернешнл Лтд. | Стабільна композиція з наночастинок ралоксифену гідрохлориду |
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| WO2006069098A1 (en) * | 2004-12-22 | 2006-06-29 | Elan Pharma International Ltd. | Nanoparticulate bicalutamide formulations |
| KR20070118224A (ko) * | 2005-01-06 | 2007-12-14 | 엘란 파마 인터내셔널 리미티드 | 나노입자형 칸데사르탄 제제 |
| BRPI0608173A2 (pt) * | 2005-02-24 | 2010-11-09 | Elan Pharma Int Ltd | composição, uso da mesma, e, método de produzir uma composição de docetaxel nanoparticulada ou análogo do mesmo |
| CA2601312A1 (en) * | 2005-03-17 | 2006-09-28 | Elan Pharma International Limited | Injectable compositions of nanoparticulate immunosuppressive compounds |
| CA2601363A1 (en) * | 2005-03-17 | 2006-09-28 | Elan Pharma International Limited | Nanoparticulate biphosphonate compositions |
| WO2006110809A2 (en) * | 2005-04-12 | 2006-10-19 | Elan Pharma International, Limited | Nanoparticulate lipase inhibitor formulations |
| EP1888037A2 (en) * | 2005-05-10 | 2008-02-20 | Elan Pharma International Limited | Nanoparticulate clopidogrel formulations |
| US20100028439A1 (en) * | 2005-05-23 | 2010-02-04 | Elan Pharma International Limited | Nanoparticulate stabilized anti-hypertensive compositions |
| EA015336B1 (ru) * | 2005-06-03 | 2011-06-30 | Элан Фарма Интернэшнл Лтд. | Стабильная композиция с наночастицами ацетаминофена |
| EA201100022A1 (ru) * | 2005-06-03 | 2011-06-30 | Элан Фарма Интернэшнл Лтд. | Способ получения композиции наночастиц мезилата иматиниба |
| CA2611475A1 (en) * | 2005-06-09 | 2006-12-21 | Elan Pharma International, Limited | Nanoparticulate ebastine formulations |
| CA2614412A1 (en) * | 2005-07-07 | 2007-01-18 | Elan Pharma International, Limited | Nanoparticulate clarithromycin formulations |
| US8367112B2 (en) * | 2006-02-28 | 2013-02-05 | Alkermes Pharma Ireland Limited | Nanoparticulate carverdilol formulations |
| CN101495096A (zh) * | 2006-05-30 | 2009-07-29 | 伊兰制药国际有限公司 | 纳米微粒泊沙康唑制剂 |
| US20090004262A1 (en) * | 2006-11-28 | 2009-01-01 | Marinus Pharmaceuticals | Nanoparticulate formulations and methods for the making and use therof |
| WO2008079787A2 (en) * | 2006-12-20 | 2008-07-03 | Takeda San Diego, Inc. | Glucokinase activators |
| US20090028680A1 (en) * | 2007-07-27 | 2009-01-29 | Kling Troy L | Intermediate apparatus for towing utility vehicles |
| EA018988B1 (ru) * | 2008-05-16 | 2013-12-30 | Такеда Калифорния, Инк. | Активаторы глюкокиназы |
| US8054567B2 (en) * | 2008-07-23 | 2011-11-08 | Hitachi High-Technologies Corporation | Method for measuring write/read width of a composite magnetic head and a measuring device using the method |
| RU2012101627A (ru) * | 2009-06-18 | 2013-07-27 | Эбботт Лэборетриз | Стабильная суспензия лекарственного средства в виде наночастиц |
| US20120135053A1 (en) * | 2009-06-19 | 2012-05-31 | Filipcsei Genoveva | Nanoparticulate telmisartan compositions and process for the preparation thereof |
| CN101829061A (zh) * | 2010-05-14 | 2010-09-15 | 无锡纳生生物科技有限公司 | 一种紫杉醇纳米颗粒组合物及其制备方法 |
| KR101878252B1 (ko) * | 2010-05-26 | 2018-07-13 | 브이티브이 테라퓨틱스 엘엘씨 | 글루코키나아제 활성화제와 병용되는 메트포르민의 용도, 및 메트포르민과 글루코키나아제 활성화제를 포함하는 조성물 |
-
2014
- 2014-02-28 EP EP14714823.3A patent/EP2964198A2/en not_active Withdrawn
- 2014-02-28 KR KR1020157025036A patent/KR20150123838A/ko not_active Withdrawn
- 2014-02-28 HK HK16101756.4A patent/HK1213780A1/zh unknown
- 2014-02-28 MX MX2015011109A patent/MX2015011109A/es unknown
- 2014-02-28 JP JP2015561468A patent/JP6441828B2/ja not_active Expired - Fee Related
- 2014-02-28 AU AU2014226290A patent/AU2014226290B2/en not_active Expired - Fee Related
- 2014-02-28 CA CA2903433A patent/CA2903433A1/en not_active Abandoned
- 2014-02-28 CN CN201480011647.2A patent/CN105050585A/zh active Pending
- 2014-02-28 WO PCT/US2014/019349 patent/WO2014137797A2/en not_active Ceased
-
2015
- 2015-08-20 IL IL240735A patent/IL240735A0/en unknown
- 2015-08-31 US US14/840,682 patent/US20160015638A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| IL240735A0 (en) | 2015-10-29 |
| MX2015011109A (es) | 2015-11-16 |
| AU2014226290B2 (en) | 2018-11-15 |
| WO2014137797A2 (en) | 2014-09-12 |
| CN105050585A (zh) | 2015-11-11 |
| HK1213780A1 (zh) | 2016-07-15 |
| KR20150123838A (ko) | 2015-11-04 |
| JP6441828B2 (ja) | 2018-12-19 |
| US20160015638A1 (en) | 2016-01-21 |
| WO2014137797A3 (en) | 2014-10-30 |
| AU2014226290A1 (en) | 2015-10-08 |
| EP2964198A2 (en) | 2016-01-13 |
| JP2016513625A (ja) | 2016-05-16 |
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