HRP20221355T1 - Liofilizirani pripravak citotoksičnih dipeptida - Google Patents

Liofilizirani pripravak citotoksičnih dipeptida Download PDF

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Publication number
HRP20221355T1
HRP20221355T1 HRP20221355TT HRP20221355T HRP20221355T1 HR P20221355 T1 HRP20221355 T1 HR P20221355T1 HR P20221355T T HRP20221355T T HR P20221355TT HR P20221355 T HRP20221355 T HR P20221355T HR P20221355 T1 HRP20221355 T1 HR P20221355T1
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Croatia
Prior art keywords
cancer
pharmaceutical preparation
melphalan flufenamide
lyophilized pharmaceutical
solution
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HRP20221355TT
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English (en)
Inventor
Jack Spira
Fredrik Lehmann
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Oncopeptides Ab
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Publication of HRP20221355T1 publication Critical patent/HRP20221355T1/hr

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    • 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
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/05Dipeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/10Peptides having 12 to 20 amino acids
    • A61K38/105Bombesin; Related peptides
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/40Cyclodextrins; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • FMECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
    • F26DRYING
    • F26BDRYING SOLID MATERIALS OR OBJECTS BY REMOVING LIQUID THEREFROM
    • F26B5/00Drying solid materials or objects by processes not involving the application of heat
    • F26B5/04Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum
    • F26B5/06Drying solid materials or objects by processes not involving the application of heat by evaporation or sublimation of moisture under reduced pressure, e.g. in a vacuum the process involving freezing

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Mechanical Engineering (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Claims (12)

1. Liofilizirani farmaceutski pripravak, naznačen time, da sadržava: (i) melfalan flufenamid, ili njegovu farmaceutski prihvatljivu sol; i (ii) saharozu.
2. Liofilizirani farmaceutski pripravak u skladu s patentnim zahtjevom 1, naznačen time, da je količina pomoćne tvari od 10 do 100 % težinskog udjela navedenog melfalan flufenamida.
3. Liofilizirani farmaceutski pripravak u skladu s patentnim zahtjevom 1 ili 2, naznačen time, što nadalje sadržava fiziološki prihvatljivu otopinu.
4. Liofilizirani farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 1-3, naznačen time, što je nema ili je znatno oslobođen od organskih otapala.
5. Pribor, naznačen time, da se sastoji od (i) liofiliziranog farmaceutskog pripravka sukladno bilo kojem od patentnih zahtjeva 1-4; i (ii) fiziološki prihvatljive otopine.
6. Liofilizirani farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time, da se koristi kao lijek.
7. Liofilizirani farmaceutski pripravak u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time, da se koristi u liječenju i/ili prevenciji raka.
8. Liofilizirani farmaceutski pripravak u skladu s patentnim zahtjevom 7, naznačen time, što je rečeni rak bilo koji od raka jajnika, raka pluća, raka mokraćnog mjehura, mezotelioma, višestrukog mijeloma, raka dojke ili hematoloških oblika raka.
9. Komplet dijelova u skladu s patentnim zahtjevom 5, naznačeno time, da je za upotrebu u liječenju raka, na primjer gdje je navedeni rak bilo koji od raka jajnika, raka pluća, raka mokraćnog mjehura, mezotelioma, višestrukog mijeloma, raka dojke ili hematoloških oblika raka.
10. Postupak priprave liofiliziranog farmaceutskog pripravka u skladu s bilo kojim od patentnih zahtjeva 1-4, naznačen time, da: a. melfalan flufenamid ili njegova farmaceutski prihvatljiva sol je rastopljen u organskom otapalu kako bi se dobila otopina melfalan flufenamida; b. voda se dodaje u otopinu melfalan flufenamida kako bi se dobila vodena otopina melfalan flufenamida, u koncentraciji od 0,2-3,0 mg / ml; c. saharoza se dodaje otopini melfalan flufenamida; i d. vodena otopina melfalan flufenamida koja sadrži pomoćnu tvar/tvari podvrgava se liofilizaciji.
11. Postupak u skladu s patentnim zahtjevom 10, naznačen time, da: a. melfalan flufenamid ili njegova farmaceutski prihvatljiva sol je rastopljena u organskom otapalu; b. voda se dodaje otopini dobivenoj u koraku a) kako bi se dobila otopina rečenog melfalan flufenamida ili njegova farmaceutski prihvatljiva sol, u koncentraciji od 0,2-3,0 mg / ml; c. saharoza se dodaje otopini dobivenoj u koraku b); i d. otopina dobivena u koraku c) podvrgava se liofilizaciji.
12. Postupak u skladu s patentnim zahtjevom 10 ili 11, naznačeno time, što je organsko otapalo odabrano između bilo kojeg od etanola, kiseline koja sadrži etanol, glicerina, propilen glikola, benzil alkohola, dimetilacetamida (DMA), N-metil-2- pirolidona, izopropanola, n-butanola, terc-butanola, metil terc-butil etera, propilen glikola, dimetilsulfoksida, tetrahidrofurana, 2-metil tetrahidrofurana, acetona, dimetilformamida, acetonitrila, dioksana, octene kiseline, mliječne kiseline, propionske kiseline, n-butanola, izopropanola, n-propanola, terc-butanola, sek-butanola, metanola i smjese etanola i vode.
HRP20221355TT 2011-04-28 2012-04-25 Liofilizirani pripravak citotoksičnih dipeptida HRP20221355T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
SE1150371 2011-04-28
US201161535126P 2011-09-15 2011-09-15
EP19215699.0A EP3656393B1 (en) 2011-04-28 2012-04-25 Lyophilized preparation of cytotoxic dipeptides

Publications (1)

Publication Number Publication Date
HRP20221355T1 true HRP20221355T1 (hr) 2022-12-23

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HRP20171523TT HRP20171523T1 (hr) 2011-04-28 2017-10-10 Liofilizirani pripravak citotoksičnih dipeptida

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US (7) US20140128462A1 (hr)
EP (4) EP3656393B1 (hr)
JP (1) JP6042412B2 (hr)
KR (2) KR102122416B1 (hr)
CN (2) CN103547279A (hr)
AU (1) AU2012247545B2 (hr)
BR (2) BR122019017088B1 (hr)
CA (2) CA3024230C (hr)
CY (2) CY1119453T1 (hr)
DK (3) DK3656393T3 (hr)
ES (2) ES2642676T3 (hr)
FI (1) FIC20230004I1 (hr)
FR (1) FR23C1000I2 (hr)
HR (2) HRP20221355T1 (hr)
HU (3) HUE037863T2 (hr)
IL (3) IL228889A0 (hr)
LT (2) LT3656393T (hr)
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NO (1) NO2023004I1 (hr)
PL (3) PL3656393T3 (hr)
PT (2) PT3656393T (hr)
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IL228889A0 (en) 2013-12-31
IL265457A (en) 2019-05-30
JP2014512402A (ja) 2014-05-22
US11344622B2 (en) 2022-05-31
DK2701720T3 (en) 2017-10-09
PL3656393T3 (pl) 2023-01-16
RS56462B1 (sr) 2018-01-31
CA3024230A1 (en) 2012-11-01
CA3024230C (en) 2022-10-18
NZ617197A (en) 2015-06-26
KR20170140409A (ko) 2017-12-20
HUE060783T2 (hu) 2023-04-28
DK3228319T3 (da) 2020-09-07
RS63747B1 (sr) 2022-12-30
HUE037863T2 (hu) 2018-09-28
US10869928B2 (en) 2020-12-22
KR20140041497A (ko) 2014-04-04
CY1123242T1 (el) 2021-10-29
FR23C1000I1 (fr) 2023-03-10
CA2833500A1 (en) 2012-11-01
LT2701720T (lt) 2017-11-10
US20140128462A1 (en) 2014-05-08
US10543274B2 (en) 2020-01-28
KR102122416B1 (ko) 2020-06-12
EP3228319A1 (en) 2017-10-11
BR122019017088B1 (pt) 2021-11-16
PT2701720T (pt) 2017-10-20
PL3228319T3 (pl) 2021-02-08
KR101808895B1 (ko) 2017-12-13
JP6042412B2 (ja) 2016-12-14
IL272429A (en) 2020-03-31
LT3656393T (lt) 2022-12-12
SI3228319T1 (sl) 2020-10-30
RU2013152751A (ru) 2015-06-10
MX345102B (es) 2017-01-16
CN108096563A (zh) 2018-06-01
MX2013012545A (es) 2014-04-16
US20200345848A1 (en) 2020-11-05
BR112013027584A2 (pt) 2016-09-06
WO2012146625A1 (en) 2012-11-01
DK3656393T3 (da) 2022-11-14
US20170049894A1 (en) 2017-02-23
CN103547279A (zh) 2014-01-29
HRP20171523T1 (hr) 2017-11-17
SI2701720T1 (sl) 2017-11-30
IL272429B (en) 2022-05-01
CY1119453T1 (el) 2018-03-07
US20200121794A1 (en) 2020-04-23
ES2642676T3 (es) 2017-11-17
ES2930140T3 (es) 2022-12-07
US20220323585A1 (en) 2022-10-13
NL301206I2 (nl) 2023-01-24
PT3656393T (pt) 2022-11-03
BR112013027584B1 (pt) 2020-11-03
IL265457B (en) 2021-02-28
AU2012247545A1 (en) 2013-10-31
ZA201308765B (en) 2016-02-24
US20190240332A1 (en) 2019-08-08
EP3656393A1 (en) 2020-05-27
HUS2300005I1 (hu) 2023-02-28
RU2597154C2 (ru) 2016-09-10
EP4122482A1 (en) 2023-01-25
PL2701720T3 (pl) 2017-12-29
CA2833500C (en) 2019-01-08
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AU2012247545B2 (en) 2016-08-11
EP3228319B1 (en) 2020-06-03
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EP3656393B1 (en) 2022-08-24
US10322182B2 (en) 2019-06-18
US11896668B2 (en) 2024-02-13
RS60719B1 (sr) 2020-09-30
FR23C1000I2 (fr) 2024-03-15
EP2701720A1 (en) 2014-03-05
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FIC20230004I1 (fi) 2023-01-19
US20200009252A1 (en) 2020-01-09

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