CU20150179A7 - Letermovir amorfo y formulaciones farmacéuticas sólidas del mismo para administración por via oral - Google Patents

Letermovir amorfo y formulaciones farmacéuticas sólidas del mismo para administración por via oral

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Publication number
CU20150179A7
CU20150179A7 CUP2015000179A CU20150179A CU20150179A7 CU 20150179 A7 CU20150179 A7 CU 20150179A7 CU P2015000179 A CUP2015000179 A CU P2015000179A CU 20150179 A CU20150179 A CU 20150179A CU 20150179 A7 CU20150179 A7 CU 20150179A7
Authority
CU
Cuba
Prior art keywords
letermovir
amorphous letermovir
solid pharmaceutical
pharmaceutical formulations
amorfo
Prior art date
Application number
CUP2015000179A
Other languages
English (en)
Other versions
CU24619B1 (es
Inventor
Wilfried Schwab
Dirk Jung
Christian Schickaneder
Welljanne Märtens
Michael Limmert
Clemens Bothe
Mathias Berwe
Nicole Rinder-Mann
Original Assignee
Aicuris Anti Infective Cures Gmbh
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Aicuris Anti Infective Cures Gmbh filed Critical Aicuris Anti Infective Cures Gmbh
Publication of CU20150179A7 publication Critical patent/CU20150179A7/es
Publication of CU24619B1 publication Critical patent/CU24619B1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/02Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals 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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Biotechnology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Nutrition Science (AREA)
  • Physiology (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)

Abstract

La presente invención proporciona letermovir amorfo y formulaciones farmacéuticas sólidas administrables por vía oral del mismo (formulación de liberación inmediata). Dicho letermovir amorfo es adecuado para formulaciones de liberación inmediata cuando se aísla de una disolución orgánica por cualquiera de secado con rodillos de dicha disolución orgánica en un disolvente orgánico volátil, en particular acetona, a una temperatura de 30°C a 60°C, y posteriormente secado del letermovir amorfo obtenido, o aislamiento de dicho letermovir amorfo mediante precipitación en disolventes miscibles con agua seleccionados de acetona o acetonitrilo en exceso de agua como antidisolvente, y posteriormente filtración o centrifugación del letermovir amorfo obtenido. Las formulaciones de liberación inmediata de letermovir amorfo están previstas para su uso en métodos de profilaxis o métodos de tratamiento de enfermedades asociadas al grupo de Herpes viridae, preferentemente asociadas a citomegalovirus (CMV), incluso más preferentemente asociadas a citomegalovirus humano (CMVH).
CU2015000179A 2013-06-19 2014-06-19 Letermovir amorfo y formulaciones farmacéuticas sólidas del mismo para administración por via oral CU24619B1 (es)

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
CU20150179A7 true CU20150179A7 (es) 2016-07-29
CU24619B1 CU24619B1 (es) 2022-08-09

Family

ID=50982905

Family Applications (1)

Application Number Title Priority Date Filing Date
CU2015000179A CU24619B1 (es) 2013-06-19 2014-06-19 Letermovir amorfo y formulaciones farmacéuticas sólidas del mismo para administración por via oral

Country Status (34)

Country Link
US (1) US10442773B2 (es)
EP (1) EP3010891B1 (es)
JP (2) JP6445546B2 (es)
KR (1) KR101953270B1 (es)
CN (2) CN105555771B (es)
AU (1) AU2014283231B2 (es)
BR (1) BR112015031979B1 (es)
CA (1) CA2916143C (es)
CU (1) CU24619B1 (es)
CY (1) CY1121732T1 (es)
DK (1) DK3010891T3 (es)
DO (1) DOP2015000303A (es)
EA (1) EA036131B1 (es)
ES (1) ES2730958T3 (es)
HR (1) HRP20190936T1 (es)
HU (1) HUE043721T2 (es)
IL (2) IL243228B (es)
LT (1) LT3010891T (es)
MD (1) MD4673C1 (es)
ME (1) ME03483B (es)
MX (1) MX373764B (es)
MY (1) MY179502A (es)
NZ (1) NZ715387A (es)
PE (1) PE20160659A1 (es)
PH (1) PH12015502821B1 (es)
PL (1) PL3010891T3 (es)
PT (1) PT3010891T (es)
RS (1) RS58882B1 (es)
SG (1) SG11201510426PA (es)
SI (1) SI3010891T1 (es)
SM (1) SMT201900327T1 (es)
UA (1) UA117755C2 (es)
WO (1) WO2014202737A1 (es)
ZA (1) ZA201509239B (es)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
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
US10442773B2 (en) * 2013-06-19 2019-10-15 Aicuris Anti-Infective Cures Gmbh Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration
CN109152787A (zh) 2016-03-31 2019-01-04 英特塞普特医药品公司 具有优越的溶出性的口服制剂
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
CN116338119B (zh) * 2023-02-24 2026-03-13 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
CN120927867B (zh) * 2025-10-11 2026-01-06 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)

* Cited by examiner, † Cited by third party
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
BRPI0607537A2 (pt) * 2005-04-12 2009-09-15 Elan Pharma Int Ltd formulações de derivado de quinazolina nanoparticulado
DE102005027517A1 (de) 2005-06-15 2006-12-21 Bayer Healthcare Ag Verfahren zur Herstellung von Dihydrochinazolinen
US20140044759A1 (en) * 2011-05-04 2014-02-13 Dimitrios Zarkadas Drug substances, pharmaceutical compositions and methods for preparing the same
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
DE102012101673A1 (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
US10442773B2 (en) * 2013-06-19 2019-10-15 Aicuris Anti-Infective Cures Gmbh Amorphous letermovir and solid pharmaceutical formulations thereof for oral administration

Also Published As

Publication number Publication date
LT3010891T (lt) 2019-08-26
RS58882B1 (sr) 2019-08-30
EA036131B1 (ru) 2020-10-01
BR112015031979B1 (pt) 2022-05-24
HK1223935A1 (en) 2017-08-11
HUE043721T2 (hu) 2019-09-30
PE20160659A1 (es) 2016-07-24
IL243228A0 (en) 2016-02-29
JP6770035B2 (ja) 2020-10-14
PL3010891T3 (pl) 2019-11-29
WO2014202737A1 (en) 2014-12-24
IL243228B (en) 2020-04-30
JP6445546B2 (ja) 2018-12-26
CA2916143C (en) 2019-01-29
CN120097924A (zh) 2025-06-06
US10442773B2 (en) 2019-10-15
IL263978A (en) 2019-01-31
KR20160029075A (ko) 2016-03-14
CN105555771A (zh) 2016-05-04
UA117755C2 (uk) 2018-09-25
SG11201510426PA (en) 2016-01-28
SI3010891T1 (sl) 2019-09-30
AU2014283231A1 (en) 2016-01-21
MX2015017758A (es) 2016-06-21
MD20150126A2 (ro) 2016-06-30
EP3010891A1 (en) 2016-04-27
EA201600024A1 (ru) 2016-12-30
IL263978B (en) 2020-07-30
ES2730958T3 (es) 2019-11-13
US20160145216A1 (en) 2016-05-26
MD4673B1 (ro) 2020-02-29
CU24619B1 (es) 2022-08-09
PH12015502821B1 (en) 2019-09-25
CY1121732T1 (el) 2020-07-31
MD4673C1 (ro) 2020-11-30
SMT201900327T1 (it) 2019-07-11
CN105555771B (zh) 2025-02-21
AU2014283231B2 (en) 2017-12-07
CA2916143A1 (en) 2014-12-24
ME03483B (me) 2020-01-20
PH12015502821A1 (en) 2016-03-21
JP2016522238A (ja) 2016-07-28
NZ715387A (en) 2018-02-23
JP2018193401A (ja) 2018-12-06
EP3010891B1 (en) 2019-04-10
DOP2015000303A (es) 2016-01-15
DK3010891T3 (da) 2019-06-24
MX373764B (es) 2020-03-24
KR101953270B1 (ko) 2019-02-28
MY179502A (en) 2020-11-09
BR112015031979A8 (pt) 2018-01-23
PT3010891T (pt) 2019-06-21
HRP20190936T1 (hr) 2019-10-04
BR112015031979A2 (pt) 2017-07-25
ZA201509239B (en) 2022-03-30

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