AR123783A2 - Dispersión sólida amorfa que comprende un derivado de tetrazol y composición farmacéutica que comprende dicha dispersión - Google Patents
Dispersión sólida amorfa que comprende un derivado de tetrazol y composición farmacéutica que comprende dicha dispersiónInfo
- Publication number
- AR123783A2 AR123783A2 ARP210102833A ARP210102833A AR123783A2 AR 123783 A2 AR123783 A2 AR 123783A2 AR P210102833 A ARP210102833 A AR P210102833A AR P210102833 A ARP210102833 A AR P210102833A AR 123783 A2 AR123783 A2 AR 123783A2
- Authority
- AR
- Argentina
- Prior art keywords
- solid dispersion
- dispersion
- tetrazole derivative
- formula
- nitro
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/475—Quinolines; Isoquinolines having an indole ring, e.g. yohimbine, reserpine, strychnine, vinblastine
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- 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
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
- C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
- C07D257/04—Five-membered rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
La presente invención se refiere a una dispersión sólida amorfa que comprende un derivado de tetrazol de la fórmula (1) o una sal farmacéuticamente aceptable del mismo como ingrediente activo. La dispersión sólida de la presente invención comprende un polímero hidrosoluble o un ácido con el fin de mejorar la solubilidad de su ingrediente activo, es decir, el derivado de tetrazol de la fórmula (1), mejorando de este modo su tasa de absorción y, por lo tanto, puede ser utilizado de manera eficaz para reducir la resistencia a múltiples fármacos (MDR) en las células cancerígenas. Reivindicación 1: Una dispersión sólida amorfa caracterizada porque comprende un derivado de tetrazol de la fórmula (1) o una sal farmacéuticamente aceptable del mismo como ingrediente activo: donde, R¹ es quinolina, isoquinolina, quinoxalina, piridina, pirazina, naftaleno, fenilo, tiofeno, furano, 4-oxo-4H-cromeno o cinolina, que está insustituido o sustituido por alquilo C₁₋₅, hidroxilo, alcoxi C₁₋₅, halógeno, trifluorometilo, nitro o amino; R² a R⁵ y R⁸ a R¹¹ son -cada uno en forma independiente- H, hidroxilo, halógeno, nitro, alquilo C₁₋₅ o alcoxi C₁₋₅; R⁶ y R⁷ son -cada uno en forma independiente- H, hidroxilo, halógeno, nitro, alquileno C₁₋₅ o alcoxi C₁₋₅; y R⁶ y R⁷ pueden estar conectados para formar un anillo de 4 a 8 miembros; m y n son -cada uno en forma independiente- enteros en el rango de 0 a 4; y X es CH₂, O ó S. Reivindicación 2: La dispersión sólida amorfa de la reivindicación 1, caracterizada porque el derivado de tetrazol es el compuesto de fórmula (2) o (3). Reivindicación 3: La dispersión sólida amorfa de la reivindicación 1, caracterizada porque la dispersión sólida también comprende un polímero hidrosoluble. Reivindicación 4: La dispersión sólida amorfa de la reivindicación 3, caracterizada porque el polímero hidrosoluble se selecciona entre el grupo que consta de hipromelosa, hidroxipropil celulosa, polivinilpirrolidona, polivinil acetal, aminoacetato de dietilo, polietilenglicol y una mezcla de ellos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020120145603A KR101986683B1 (ko) | 2012-12-13 | 2012-12-13 | 테트라졸 유도체를 활성 성분으로 포함하는 용해도가 개선된 고체 분산체 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR123783A2 true AR123783A2 (es) | 2023-01-11 |
Family
ID=50934681
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104460A AR093706A1 (es) | 2012-12-13 | 2013-12-03 | Dispersion solida que comprende un derivado de tetrazol como ingrediente activo |
| ARP210102833A AR123783A2 (es) | 2012-12-13 | 2021-10-13 | Dispersión sólida amorfa que comprende un derivado de tetrazol y composición farmacéutica que comprende dicha dispersión |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP130104460A AR093706A1 (es) | 2012-12-13 | 2013-12-03 | Dispersion solida que comprende un derivado de tetrazol como ingrediente activo |
Country Status (38)
| Country | Link |
|---|---|
| US (1) | US9283218B2 (es) |
| EP (1) | EP2931720B1 (es) |
| JP (1) | JP6355645B2 (es) |
| KR (1) | KR101986683B1 (es) |
| CN (1) | CN104870443B (es) |
| AR (2) | AR093706A1 (es) |
| AU (1) | AU2013360544B2 (es) |
| BR (1) | BR112015013905A2 (es) |
| CA (1) | CA2892376C (es) |
| CL (1) | CL2015001551A1 (es) |
| CR (1) | CR20150361A (es) |
| DK (1) | DK2931720T3 (es) |
| DO (1) | DOP2015000128A (es) |
| EC (1) | ECSP15029808A (es) |
| ES (1) | ES2731806T3 (es) |
| GT (1) | GT201500123A (es) |
| HU (1) | HUE044659T2 (es) |
| IL (1) | IL239327A (es) |
| JO (1) | JO3534B1 (es) |
| LT (1) | LT2931720T (es) |
| MX (1) | MX363644B (es) |
| MY (1) | MY174746A (es) |
| NI (1) | NI201500073A (es) |
| NZ (1) | NZ709071A (es) |
| PE (1) | PE20151066A1 (es) |
| PH (1) | PH12015501312A1 (es) |
| PL (1) | PL2931720T3 (es) |
| PT (1) | PT2931720T (es) |
| PY (1) | PY1358434A (es) |
| RU (1) | RU2662819C2 (es) |
| SA (1) | SA515360535B1 (es) |
| SG (1) | SG11201504067SA (es) |
| SI (1) | SI2931720T1 (es) |
| TR (1) | TR201908746T4 (es) |
| TW (1) | TWI652073B (es) |
| UY (1) | UY35186A (es) |
| WO (1) | WO2014092489A1 (es) |
| ZA (1) | ZA201503795B (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102044223B1 (ko) * | 2016-09-12 | 2019-11-13 | 성균관대학교산학협력단 | 텔미사르탄을 포함하는 고체 분산체 및 이의 제조방법 |
| WO2019173526A1 (en) * | 2018-03-07 | 2019-09-12 | Andrew Xian Chen | Aqueous formulations for insoluble drugs |
| CZ2018188A3 (cs) * | 2018-04-18 | 2019-10-30 | Zentiva, K.S. | Částice s obsahem amorfního empagliflozinu, způsob jejich přípravy a farmaceutický přípravek |
| AU2019395284B2 (en) * | 2018-12-14 | 2025-07-17 | Health Hope Pharma Hk Limited | Therapeutic combinations of orally administered irinotecan and a P-gp inhibitor for the treatment of cancer |
| WO2020124069A1 (en) * | 2018-12-14 | 2020-06-18 | Athenex HK Innovative Limited | Therapeutic combinations of orally administered docetaxel and a p-gp inhibitor for the treatment of cancer |
| US12404267B2 (en) * | 2019-02-14 | 2025-09-02 | Assia Chemical Industries Ltd. | Solid state forms of n-[2-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-2(1H)-isoquinolinyl)ethyl]phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxyphenyl]-4-oxo-4H-chromene-2-carboxamide and of its mesylate salt |
| WO2022011221A1 (en) | 2020-07-10 | 2022-01-13 | Teva Czech Industries S.R.O | Solid state forms of n-[2-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-2(1h)-isoquinolinyl)ethyl]phenyl}-2h-tetrazol-5-yl)-4,5-dimethoxyphenyl]-4-oxo-4h-chromene-2-carboxamide mesylate salt |
| TWI900672B (zh) * | 2020-10-07 | 2025-10-11 | 香港商希華醫藥有限公司 | 乙醯胺基－苯基四唑衍生物及其使用方法 |
| JP2023548384A (ja) | 2020-10-30 | 2023-11-16 | アテネックス アールアンドディ エルエルシー | Ｈｍ３０１８１メシル酸塩の多形 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW487582B (en) * | 1995-08-11 | 2002-05-21 | Nissan Chemical Ind Ltd | Method for converting sparingly water-soluble medical substance to amorphous state |
| JP2000309588A (ja) * | 1999-04-28 | 2000-11-07 | Taisho Pharmaceut Co Ltd | 固体分散体 |
| CL2004001884A1 (es) * | 2003-08-04 | 2005-06-03 | Pfizer Prod Inc | Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros. |
| KR20060033033A (ko) * | 2003-08-04 | 2006-04-18 | 화이자 프로덕츠 인크. | 콜레스테릴 에스테르 전달 단백질 억제제의 제어 방출 및ｈｍｇ-ｃｏａ 리덕타제 억제제의 순간 방출을 제공하는제형 |
| KR100557093B1 (ko) * | 2003-10-07 | 2006-03-03 | 한미약품 주식회사 | 다약제 내성 저해 활성을 갖는 테트라졸 유도체 및 그의제조방법 |
| KR100572411B1 (ko) * | 2003-10-23 | 2006-04-18 | 한미약품 주식회사 | 열역학적으로 안정한 무정형 토라세미드 고체분산체와이를 포함하는 약학 조성물 및 이의 제조 방법 |
| BRPI0516772A (pt) * | 2004-10-25 | 2008-09-23 | Japan Tobacco Inc | formulação sólida com solubilidade e estabilidade melhoradas e método para produção da referida formulação |
| KR100678824B1 (ko) * | 2005-02-04 | 2007-02-05 | 한미약품 주식회사 | 용해성이 증가된 무정형 타크로리무스 고체분산체 및 이를포함하는 약제학적 조성물 |
| WO2007027494A2 (en) * | 2005-08-29 | 2007-03-08 | Sanofi-Aventis U.S. Llc | Morphous solid dispersions of 7-chloro-n,n, 5-trimethyl-4-oxo-3-phenyl-3, 5,-dihydro-4h-pyridazino [4, 5-b] indole-1-acetamide |
| KR101466245B1 (ko) * | 2010-01-15 | 2014-12-01 | 한미사이언스 주식회사 | 테트라졸 메탄설폰산 염의 제조방법 및 이에 사용되는 신규 화합물 |
| KR20110132116A (ko) * | 2010-06-01 | 2011-12-07 | (주)국전약품 | 라록시펜 염산염을 포함하는 고체분산체, 이의 제조방법, 및 이를 포함하는 경구용 제제 |
| KR20130109092A (ko) * | 2010-06-09 | 2013-10-07 | 아보트 러보러터리즈 | 키나제 억제제를 함유하는 고체 분산물 |
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2012
- 2012-12-13 KR KR1020120145603A patent/KR101986683B1/ko active Active
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2013
- 2013-12-03 AR ARP130104460A patent/AR093706A1/es not_active Application Discontinuation
- 2013-12-06 PY PY201301358434A patent/PY1358434A/es unknown
- 2013-12-11 JO JOP/2013/0361A patent/JO3534B1/ar active
- 2013-12-12 DK DK13863463.9T patent/DK2931720T3/da active
- 2013-12-12 SI SI201331462T patent/SI2931720T1/sl unknown
- 2013-12-12 MX MX2015006416A patent/MX363644B/es unknown
- 2013-12-12 NZ NZ709071A patent/NZ709071A/en unknown
- 2013-12-12 TR TR2019/08746T patent/TR201908746T4/tr unknown
- 2013-12-12 US US14/439,735 patent/US9283218B2/en active Active
- 2013-12-12 CA CA2892376A patent/CA2892376C/en active Active
- 2013-12-12 SG SG11201504067SA patent/SG11201504067SA/en unknown
- 2013-12-12 JP JP2015547856A patent/JP6355645B2/ja active Active
- 2013-12-12 CN CN201380064980.5A patent/CN104870443B/zh active Active
- 2013-12-12 BR BR112015013905A patent/BR112015013905A2/pt not_active Application Discontinuation
- 2013-12-12 HU HUE13863463 patent/HUE044659T2/hu unknown
- 2013-12-12 PL PL13863463T patent/PL2931720T3/pl unknown
- 2013-12-12 PE PE2015000908A patent/PE20151066A1/es unknown
- 2013-12-12 UY UY0001035186A patent/UY35186A/es active IP Right Grant
- 2013-12-12 RU RU2015128002A patent/RU2662819C2/ru active
- 2013-12-12 EP EP13863463.9A patent/EP2931720B1/en active Active
- 2013-12-12 TW TW102145931A patent/TWI652073B/zh active
- 2013-12-12 AU AU2013360544A patent/AU2013360544B2/en active Active
- 2013-12-12 MY MYPI2015701648A patent/MY174746A/en unknown
- 2013-12-12 ES ES13863463T patent/ES2731806T3/es active Active
- 2013-12-12 WO PCT/KR2013/011545 patent/WO2014092489A1/en not_active Ceased
- 2013-12-12 LT LTEP13863463.9T patent/LT2931720T/lt unknown
- 2013-12-12 PT PT13863463T patent/PT2931720T/pt unknown
-
2015
- 2015-05-25 GT GT201500123A patent/GT201500123A/es unknown
- 2015-05-26 NI NI201500073A patent/NI201500073A/es unknown
- 2015-05-27 ZA ZA2015/03795A patent/ZA201503795B/en unknown
- 2015-05-29 DO DO2015000128A patent/DOP2015000128A/es unknown
- 2015-06-05 CL CL2015001551A patent/CL2015001551A1/es unknown
- 2015-06-06 SA SA515360535A patent/SA515360535B1/ar unknown
- 2015-06-09 PH PH12015501312A patent/PH12015501312A1/en unknown
- 2015-06-10 IL IL239327A patent/IL239327A/en active IP Right Grant
- 2015-07-09 CR CR20150361A patent/CR20150361A/es unknown
- 2015-07-11 EC ECIEPI201529808A patent/ECSP15029808A/es unknown
-
2021
- 2021-10-13 AR ARP210102833A patent/AR123783A2/es not_active Application Discontinuation
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