PH12015502821B1 - Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration - Google Patents
Amorphous letermovir and solid pharmaceutical formulations thereof for oral administrationInfo
- Publication number
- PH12015502821B1 PH12015502821B1 PH12015502821A PH12015502821A PH12015502821B1 PH 12015502821 B1 PH12015502821 B1 PH 12015502821B1 PH 12015502821 A PH12015502821 A PH 12015502821A PH 12015502821 A PH12015502821 A PH 12015502821A PH 12015502821 B1 PH12015502821 B1 PH 12015502821B1
- Authority
- PH
- Philippines
- Prior art keywords
- amorphous letermovir
- amorphous
- solid pharmaceutical
- immediate release
- pharmaceutical formulations
- Prior art date
Links
- FWYSMLBETOMXAG-QHCPKHFHSA-N letermovir Chemical compound COC1=CC=CC(N2CCN(CC2)C=2N([C@@H](CC(O)=O)C3=CC=CC(F)=C3N=2)C=2C(=CC=C(C=2)C(F)(F)F)OC)=C1 FWYSMLBETOMXAG-QHCPKHFHSA-N 0.000 title abstract 7
- 229950010668 letermovir Drugs 0.000 title abstract 7
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 239000007787 solid Substances 0.000 title abstract 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 abstract 4
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 abstract 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract 3
- 241000701022 Cytomegalovirus Species 0.000 abstract 2
- 241000701024 Human betaherpesvirus 5 Species 0.000 abstract 2
- 238000001035 drying Methods 0.000 abstract 2
- 238000009472 formulation Methods 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 2
- 241000700586 Herpesviridae Species 0.000 abstract 1
- 239000012296 anti-solvent Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003960 organic solvent Substances 0.000 abstract 1
- 238000001556 precipitation Methods 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 239000002904 solvent Substances 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K47/02—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
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- 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
- A61K47/30—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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Organic Chemistry (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Molecular Biology (AREA)
- Inorganic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Biotechnology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP13003120 | 2013-06-19 | ||
| EP14165027 | 2014-04-16 | ||
| PCT/EP2014/062974 WO2014202737A1 (en) | 2013-06-19 | 2014-06-19 | Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PH12015502821A1 PH12015502821A1 (en) | 2016-03-21 |
| PH12015502821B1 true PH12015502821B1 (en) | 2019-09-25 |
Family
ID=50982905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12015502821A PH12015502821B1 (en) | 2013-06-19 | 2015-12-18 | Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration |
Country Status (34)
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10319612A1 (de) * | 2003-05-02 | 2004-11-18 | Bayer Healthcare Ag | Substituierte Dihydrochinazoline |
| DE102012101673A1 (de) | 2012-02-29 | 2013-08-29 | Aicuris Gmbh & Co. Kg | Salze eines Dihydrochinazolinderivats |
| PL3010891T3 (pl) * | 2013-06-19 | 2019-11-29 | Aicuris Anti Infective Cures Gmbh | Amorficzny letermowir i jego stałe preparaty farmaceutyczne do podawania doustnego |
| US11413295B2 (en) | 2016-03-31 | 2022-08-16 | Intercept Pharmaceuticals, Inc. | Oral preparation of obeticholic acid |
| AU2020237505B2 (en) * | 2019-03-12 | 2023-02-02 | Microbiotix, Inc. | Combination drug treatment for human cytomegalovirus |
| CN111024861A (zh) * | 2019-12-31 | 2020-04-17 | 山东省药学科学院 | 一种莱特莫韦及含莱特莫韦的制剂中有关物质的检测方法 |
| EP3906929A1 (en) | 2020-05-08 | 2021-11-10 | AiCuris GmbH & Co. KG | Letermovir for use in the prevention and the treatment of coronavirus infections |
| US20230312485A1 (en) | 2020-08-17 | 2023-10-05 | Lupin Limited | A precipitation process for amorphous letermovir |
| US20240041882A1 (en) * | 2020-12-16 | 2024-02-08 | Merck Sharp & Dohme Llc | Mini-tablet dosage form of a viral terminase inhibitor and uses thereof |
| CN115403528B (zh) * | 2021-05-27 | 2025-01-07 | 南京正大天晴制药有限公司 | 无定形3,4-二氢喹唑啉衍生物的制备方法 |
| CN114942278B (zh) * | 2022-04-12 | 2023-09-08 | 山东诚创蓝海医药科技有限公司 | 来特莫韦中间体二d-(+)-二对甲基苯甲酰酒石酸乙酸乙酯络合物有关物质的分析方法 |
| WO2024037485A1 (zh) * | 2022-08-15 | 2024-02-22 | 上海迪赛诺化学制药有限公司 | 一种来特莫韦无定形的制备方法 |
| CN116338119A (zh) * | 2023-02-24 | 2023-06-27 | 重庆希韦医药科技有限公司 | 一种来特莫韦包合物溶液体外释放度的测定方法 |
| WO2025133248A1 (en) | 2023-12-21 | 2025-06-26 | Aic246 Ag & Co. Kg | Diastereomeric aminoalcohol and aminoether salts of 2-[(4r,s)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl]acetic acid and their use for enantiomeric separation |
| JP2025161786A (ja) * | 2024-04-12 | 2025-10-24 | 東和薬品株式会社 | レテルモビル含有医薬組成物ならびにその製造方法および用途 |
| CN119745803A (zh) * | 2024-12-30 | 2025-04-04 | 上海奥科达医药科技股份有限公司 | 一种来特莫韦制剂组合物及其制备方法 |
| CN120927867A (zh) * | 2025-10-11 | 2025-11-11 | 成都诺和晟欣生物医药有限公司 | 一种来特莫韦注射液中对映异构体的hplc检测方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10207026A1 (de) * | 2002-02-20 | 2003-08-28 | Boehringer Ingelheim Kg | Pulverinhalativum, enthaltend den CGRP-Antagonisten BIBN4096 und Verfahren zu dessen Herstellung |
| DE10319612A1 (de) * | 2003-05-02 | 2004-11-18 | Bayer Healthcare Ag | Substituierte Dihydrochinazoline |
| DE10305785A1 (de) * | 2003-02-12 | 2004-08-26 | Bayer Healthcare Ag | Dihydrochinazoline |
| DE10338402A1 (de) * | 2003-08-18 | 2005-03-17 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Sprühgetrocknetes, amorphes BIBN 4096, Verfahren zu dessen Herstellung sowie dessen Verwendung als Inhalativum |
| JP2008535924A (ja) * | 2005-04-12 | 2008-09-04 | エラン ファーマ インターナショナル リミテッド | ナノ粒子キナゾリン誘導体製剤 |
| DE102005027517A1 (de) | 2005-06-15 | 2006-12-21 | Bayer Healthcare Ag | Verfahren zur Herstellung von Dihydrochinazolinen |
| KR20140022855A (ko) * | 2011-05-04 | 2014-02-25 | 머크 샤프 앤드 돔 코포레이션 | C형 간염 바이러스의 억제제의 제조 방법 |
| DE102012101673A1 (de) * | 2012-02-29 | 2013-08-29 | Aicuris Gmbh & Co. Kg | Salze eines Dihydrochinazolinderivats |
| DE102012101680A1 (de) * | 2012-02-29 | 2013-08-29 | Aicuris Gmbh & Co. Kg | Pharmazeutische Zubereitung enthaltend ein antiviral wirksames Dihydrochinazolinderivat |
| DE102012101659A1 (de) * | 2012-02-29 | 2013-08-29 | Aicuris Gmbh & Co. Kg | Salze eines Dihydrochinazolinderivats |
| WO2014047562A2 (en) * | 2012-09-21 | 2014-03-27 | Epiphany Biosciences | Method of treating and/or preventing shingles and method of treating and/or preventing zoster associated pain |
| PL3010891T3 (pl) * | 2013-06-19 | 2019-11-29 | Aicuris Anti Infective Cures Gmbh | Amorficzny letermowir i jego stałe preparaty farmaceutyczne do podawania doustnego |
-
2014
- 2014-06-19 PL PL14732545T patent/PL3010891T3/pl unknown
- 2014-06-19 SM SM20190327T patent/SMT201900327T1/it unknown
- 2014-06-19 CN CN201480040969.XA patent/CN105555771B/zh active Active
- 2014-06-19 ES ES14732545T patent/ES2730958T3/es active Active
- 2014-06-19 SG SG11201510426PA patent/SG11201510426PA/en unknown
- 2014-06-19 WO PCT/EP2014/062974 patent/WO2014202737A1/en not_active Ceased
- 2014-06-19 AU AU2014283231A patent/AU2014283231B2/en active Active
- 2014-06-19 MY MYPI2015002983A patent/MY179502A/en unknown
- 2014-06-19 PT PT14732545T patent/PT3010891T/pt unknown
- 2014-06-19 HR HRP20190936TT patent/HRP20190936T1/hr unknown
- 2014-06-19 DK DK14732545.0T patent/DK3010891T3/da active
- 2014-06-19 RS RS20190686A patent/RS58882B1/sr unknown
- 2014-06-19 NZ NZ715387A patent/NZ715387A/en unknown
- 2014-06-19 HU HUE14732545A patent/HUE043721T2/hu unknown
- 2014-06-19 MD MDA20150126A patent/MD4673C1/ro active IP Right Grant
- 2014-06-19 CA CA2916143A patent/CA2916143C/en active Active
- 2014-06-19 BR BR112015031979-3A patent/BR112015031979B1/pt active IP Right Grant
- 2014-06-19 US US14/899,178 patent/US10442773B2/en active Active
- 2014-06-19 SI SI201431243T patent/SI3010891T1/sl unknown
- 2014-06-19 LT LTEP14732545.0T patent/LT3010891T/lt unknown
- 2014-06-19 UA UAA201600339A patent/UA117755C2/uk unknown
- 2014-06-19 CU CU2015000179A patent/CU24619B1/es unknown
- 2014-06-19 EP EP14732545.0A patent/EP3010891B1/en active Active
- 2014-06-19 ME MEP-2019-149A patent/ME03483B/me unknown
- 2014-06-19 MX MX2015017758A patent/MX373764B/es active IP Right Grant
- 2014-06-19 KR KR1020167001010A patent/KR101953270B1/ko active Active
- 2014-06-19 EA EA201600024A patent/EA036131B1/ru unknown
- 2014-06-19 PE PE2015002639A patent/PE20160659A1/es unknown
- 2014-06-19 JP JP2016520499A patent/JP6445546B2/ja active Active
- 2014-06-19 CN CN202510264255.7A patent/CN120097924A/zh active Pending
-
2015
- 2015-12-18 ZA ZA2015/09239A patent/ZA201509239B/en unknown
- 2015-12-18 DO DO2015000303A patent/DOP2015000303A/es unknown
- 2015-12-18 PH PH12015502821A patent/PH12015502821B1/en unknown
- 2015-12-20 IL IL243228A patent/IL243228B/en active IP Right Grant
-
2018
- 2018-09-07 JP JP2018168220A patent/JP6770035B2/ja active Active
- 2018-12-26 IL IL263978A patent/IL263978B/en active IP Right Grant
-
2019
- 2019-06-11 CY CY20191100607T patent/CY1121732T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PH12015502821B1 (en) | Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration | |
| HK1243930A1 (zh) | 作爲fxr/tgr5激动剂的胆汁酸类似物和其使用方法 | |
| SG10201909545XA (en) | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof | |
| BR112015020819A2 (pt) | uso de faecalibacterium prausnitzii htf-f (dsm 26943) para supressão de inflamação | |
| WO2017132432A8 (en) | Benzimidazole derivatives as modulators of ror-gamma | |
| WO2015042078A8 (en) | Substituted aminopyrimidine compounds and methods of use | |
| CU20170162A7 (es) | Derivados de fenil-tieno(2,3-d)pirimidina-hidroxiácido útiles en el tratamiento del cáncer y enfermedades autoinmunes, método de preparación de los mismos y composiciones farmacéuticas que los contienen | |
| EA033046B1 (ru) | Состав, содержащий пролекарство гемцитабина | |
| EP3495362A4 (en) | IMIDAZOPYRIDINE-THIOGLYCOLIC ACID DERIVATIVE, PRODUCTION METHOD THEREFOR AND USE THEREOF | |
| EA201692292A1 (ru) | Соединения и композиции для стимулирования хондрогенеза | |
| NZ602109A (en) | Plant protection agent | |
| BR112017009510A2 (pt) | composições compreendendo ciclosporina | |
| WO2016048861A3 (en) | Heterocyclic compounds and use thereof | |
| MX369742B (es) | Formulación de liberación modificada. | |
| PH12015502717B1 (en) | Anti-fibrogenic compounds, methods and uses thereof | |
| EA202091493A1 (ru) | Аморфный летермовир и содержащие его твердые фармацевтические препараты, предназначенные для перорального введения | |
| MX384987B (es) | Derivados del ácido acético azaindol y su uso como moduladores de receptor de prostaglandina d2. | |
| NZ704342A (en) | Compositions comprising spicamycin derivatives and methods of use thereof | |
| WO2015031198A3 (en) | Bendamustine pharmaceutical compositions | |
| HK1216619A1 (zh) | 藥物化合物 | |
| MX2016011900A (es) | Derivados de acido azaindol-acetico y su uso como moduladores del receptor de prostaglandina d2. | |
| TH165370A (th) | อมอร์ฟัสลีเทอร์โมเวียร์และสูตรผสมของแข็งทางเภสัชกรรมของมันสำหรับให้เข้าทางปาก | |
| WO2016016820A3 (en) | Anionically modified n-sulfonic polyallylamine derivative, pharmaceutical composition comprising the n-sulfonic polyallylamine derivative as the active substance and use of said derivate for the production of a medicine | |
| WO2015154883A8 (en) | Neosoraphens | |
| EA201200799A1 (ru) | Гепатопротекторное средство |