HRP20210999T1 - Derivati tirozina i pripravci koji ih sadrže - Google Patents

Derivati tirozina i pripravci koji ih sadrže Download PDF

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Publication number
HRP20210999T1
HRP20210999T1 HRP20210999TT HRP20210999T HRP20210999T1 HR P20210999 T1 HRP20210999 T1 HR P20210999T1 HR P20210999T T HRP20210999T T HR P20210999TT HR P20210999 T HRP20210999 T HR P20210999T HR P20210999 T1 HRP20210999 T1 HR P20210999T1
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Croatia
Prior art keywords
tyrosine
methyl
amino
propanoate
chloro
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HRP20210999TT
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English (en)
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Steven Hoffman
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Tyme, Inc.
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Publication of HRP20210999T1 publication Critical patent/HRP20210999T1/hr

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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
    • A61K31/13—Amines
    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
    • A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic 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, pantothenic acid
    • A61K31/198—Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/40—Peroxides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • 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
    • 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
    • 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
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
    • 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
    • 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
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/02—Radiation therapy using microwaves
    • A61N5/022—Apparatus adapted for a specific treatment
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/06—Radiation therapy using light
    • A61N5/0613—Apparatus adapted for a specific treatment
    • A61N5/062—Photodynamic therapy, i.e. excitation of an agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/06—Radiation therapy using light
    • A61N2005/0658—Radiation therapy using light characterised by the wavelength of light used
    • A61N2005/0659—Radiation therapy using light characterised by the wavelength of light used infrared
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/06—Radiation therapy using light
    • A61N2005/0658—Radiation therapy using light characterised by the wavelength of light used
    • A61N2005/0661—Radiation therapy using light characterised by the wavelength of light used ultraviolet
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/06—Radiation therapy using light
    • A61N2005/0658—Radiation therapy using light characterised by the wavelength of light used
    • A61N2005/0662—Visible light
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A61N2005/1092—Details
    • A61N2005/1098—Enhancing the effect of the particle by an injected agent or implanted device

Claims (13)

1. Postupak, naznačen time, da obuhvaća: ⋅ pribavljanje derivata tirozina, čvrstog materijala u česticama, i melanina; i ⋅ primjenu akceleracijske sile na navedeni derivat tirozina, navedeni čvrsti materijal u česticama, i navedeni melanin u vremenskom periodu i pod uvjetima koji su učinkoviti tako, da uzrokuju, da najmanje jedan od navedenog derivata tirozina i navedenog čvrstoga materijala u česticama potpuno opkoljava ili djelomično opkoljava drugi od navedenog derivata tirozina i navedenog čvrstog materijala u česticama.
2. Postupak prema patentnom zahtjevu 1, naznačen time, da se derivat tirozina nalazi u svojem L-obliku, svojem D-obliku, ili u racemičnom obliku.
3. Postupak prema patentnom zahtjevu 1, naznačen time, da je derivat tirozina jedan ili više od: metil (2R)-2-amino-3-(2-kloro-4-hidroksifenil)propanoat, D-tirozin etilester hidroklorid, metil (2R)-2-amino-3-(2,6-dikloro-3,4-dimetoksifenil)propanoat, H-D-Tyr(TBU)-alilester HCl, metil (2R)-2-amino-3-(3-kloro-4,5-dimetoksifenil)propanoat, metil (2R)-2-amino-3-(2-kloro-3-hidroksi-4-metoksi-fenil)propanoat, metil (2R)-2-amino-3-(4-[(2-kloro-6-fluorofenil)metoksi]fenil)propanoat, metil (2R)-2-amino-3-(2-kloro-3,4-dimetoksifenil)propanoat, metil (2R)-2-amino-3-(3-kloro-5-fluoro-4-hidroksifenil)propanoat, dietil 2-(acetilamino)-2-(4-[(2-kloro-6-fluorobenzil)oksi]benzil malonat, metil (2R)-2-amino-3-(3-kloro-4-metoksifenil)propanoat, metil (2R)-2-amino-3-(3-kloro-4-hidroksi-5-metoksifenil)propanoat, metil (2R)-2-amino-3-(2,6-dikloro-3-hidroksi-4-metoksifenil)propanoat, metil (2R)-2-amino-3-(3-kloro-4-hidroksifenil)propanoat, H-DL-Tyr-OMe HCl, H-3,5-dijodo-Tyr-OMe HCl, H-D-3,5-dijodo-Tyr-OMe HCl, H-D-Tyr-OMe HCl, D-tirozin metilester hidroklorid, D-tirozin-OMe HCl, metil D-tirozinat hidroklorid, H-D-Tyr-OMe HCl, D-tirozin metilester HCl, H-D-Tyr-OMe HCl, (2R)-2-amino-3-(4-hidroksifenil)propionska kiselina, (2R)-2-amino-3-(4-hidroksifenil)metilester hidroklorid, metil (2R)-2-amino-3-(4-hidroksifenil)propanoat hidroklorid, metil (2R)-2-azanil-3-(4-hidroksifenil)propanoat hidroklorid, 3-kloro-L-tirozin 3-nitro-L-tirozin, 3-nitro-L-tirozin etilester hidroklorid, DL-m-tirozin, DL-o-tirozin, Boc-Tyr(3,5-I2)-OSu, Fmoc-Tyr(3-NO2)-OH, α-metil-L-tirozin, α-metil-D-tirozin, i α-metil-DL-tirozin.
4. Postupak prema patentnom zahtjevu 3, naznačen time, da derivat tirozina je α-metil-L-tirozin, α-metil-D-tirozin, ili α-metil-DL-tirozin u racemičnom obliku.
5. Postupak prema patentnom zahtjevu 1, naznačen time, da je čvrsti materijal u česticama topiv u vodi ili nije topiv u vodi.
6. Postupak prema bilo kojem od patentnih zahtjeva 1 do 5, naznačen time, da čvrsti materijal u česticama jest farmaceutski aktivni sastojak ili ga sadrži.
7. Postupak prema patentnom zahtjevu 6, naznačen time, da farmaceutski aktivni sastojak posjeduje terapijsko djelovanje u liječenju raka, gdje primjerice, farmaceutski aktivni sastojak sadrži najmanje jedan od selektivnog modulatora estrogenskog receptora, inhibitora aromataze, inhibitora signalne transdukcije, medikamenta koja modificira funkciju proteina koji reguliraju ekspresiju gena i ostale stanične funkcije, medikamenta koja inducira stanice raka da se podvrgnu apoptozi, i medikamenta koja interferira s angiogenezom, te je on poželjno tamoksifen, toremifen, fulvestrant, anastrozol, eksemestan, letrozol, imatinib mesilat, dasatinib, nilotinib, bosutinib, lapatinib, gefitinib, erlotinib, temzirolimus, everolimus, vandetanib, vemurafenib, krizotinib, vorinostat, romidepsin, beksaroten, alitretinoin, tretinoin, bortezomib, karfilzomib, pralatreksat, sorafenib, sunitinib, pazopanib, regorafenib, kabozantinib, denileukin, diftitoks, ziv-aflibercept, cisplatin, cisplatinum, (cis-diamindikloroplatinum(II)), karboplatin, oksaliplatin, benzil izotiocijanat, acetilkolin, i dihidrotestosteron (DHT).
8. Postupak prema bilo kojem od patentnih zahtjeva 1 do 7, naznačen time, da nadalje obuhvaća dodavanje vodikovog peroksida u navedeni derivat tirozina i navedeni čvrsti materijal u česticama nakon primjene spomenute sile na navedeni derivat tirozina i navedeni čvrsti materijal u česticama.
9. Postupak prema patentnom zahtjevu 1, naznačen time, da se spomenuta sila primjenjuje putem doticaja navedenog derivata tirozina i navedenog čvrstog materijala u česticama s najmanje jednim keramičkim elementom.
10. Pripravak, naznačen time, da se proizvodi putem postupka prema bilo kojem od prethodnih patentnih zahtjeva.
11. Pripravak prema definiciji u patentnom zahtjevu 10, naznačen time, da je za uporabu kao lijek.
12. Pripravak prema definiciji u patentnom zahtjevu 10, naznačen time, da je za uporabu kao lijek za liječenje raka.
13. Pripravak za uporabu prema patentnom zahtjevu 11 ili 12, naznačen time, da se pripravak daje oralno, nazalno, supkutano, intravenozno, intramuskularno, transdermalno, vaginalno, rektalno ili u bilo kojoj kombinaciji navedenoga.
HRP20210999TT 2013-10-22 2021-06-24 Derivati tirozina i pripravci koji ih sadrže HRP20210999T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361894279P 2013-10-22 2013-10-22
US14/062,194 US9585841B2 (en) 2013-10-22 2013-10-24 Tyrosine derivatives and compositions comprising them
EP14802529.9A EP3060200B1 (en) 2013-10-22 2014-10-21 Tyrosine derivatives and compositions comprising them
PCT/US2014/061527 WO2015061288A1 (en) 2013-10-22 2014-10-21 Tyrosine derivatives and compositions comprising them

Publications (1)

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HRP20210999T1 true HRP20210999T1 (hr) 2021-11-26

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US (2) US9585841B2 (hr)
EP (1) EP3060200B1 (hr)
JP (1) JP6684210B2 (hr)
KR (1) KR102292206B1 (hr)
CN (1) CN106232105A (hr)
AU (1) AU2014340263B2 (hr)
CA (1) CA2927980C (hr)
CY (1) CY1124386T1 (hr)
DK (1) DK3060200T3 (hr)
ES (1) ES2879947T3 (hr)
HR (1) HRP20210999T1 (hr)
HU (1) HUE055110T2 (hr)
IL (1) IL245173B (hr)
LT (1) LT3060200T (hr)
MX (1) MX2016005166A (hr)
PH (1) PH12016500729A1 (hr)
PL (1) PL3060200T3 (hr)
PT (1) PT3060200T (hr)
RS (1) RS62216B1 (hr)
SI (1) SI3060200T1 (hr)
WO (1) WO2015061288A1 (hr)
ZA (1) ZA201602770B (hr)

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US9585841B2 (en) 2017-03-07
US20150112116A1 (en) 2015-04-23
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US20170172924A1 (en) 2017-06-22
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