HRP20231241T1 - Upotreba sastava braf inhibitora za lokalnu primjenu za liječenje radijacijskog dermatitisa - Google Patents

Upotreba sastava braf inhibitora za lokalnu primjenu za liječenje radijacijskog dermatitisa Download PDF

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HRP20231241T1
HRP20231241T1 HRP20231241TT HRP20231241T HRP20231241T1 HR P20231241 T1 HRP20231241 T1 HR P20231241T1 HR P20231241T T HRP20231241T T HR P20231241TT HR P20231241 T HRP20231241 T HR P20231241T HR P20231241 T1 HRP20231241 T1 HR P20231241T1
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Noa Shelach
Noa LOWENTON-SPIER
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Lutris Pharma Ltd.
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    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/16Emollients or protectives, e.g. against radiation
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Toxicology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (12)

1. Sastav za lokalnu primjenu koji sadrži terapeutski i/ili profilaktički učinkovitu dozu najmanje jednog BRaf inhibitora ili njihove kombinacije i farmaceutski prihvatljivog nosača ili pomoćne tvari za upotrebu u liječenju, prevenciji ili ublažavanju radijacijskog dermatitisa lokalnom primjenom subjektu kojem je to potrebno, pri čemu je navedeni najmanje jedan BRaf inhibitor odabran između BAY43-9006 (Sorafenib), LGX818 (enkorafenib), PLX4032 (vemurafenib), GSK2118436 (dabrafenib), ARQ736, ARQ680, AZ628, C-I, C-15, C-19, C-A, CEP-32496, GDC-0879, NMS-P186, NMS-P349, NMS-P383, NMS-P396, NMS-P730, PLX3603 (RO5212054), PLX4720 (difluorofenil-sulfonamin), PF-04880594, PLX4734, RAF265, R04987655, SB590885, ZM336372, BMS908662, WYE-130600, TAK632, MLN 2480, XL281, spoj formule (I): [image] pri čemu je R odabran iz skupine koju čine p-klorofenil, 3-etinilfenil, 3-kloro-4-fluorofenil, 2-fluoro-4-jodofenil, 4-kloro-3-(trifluorometil)fenil, 3-(1, 1-dimetiletil)-1-metil-1H-pirazol-5-il, 3-(trifluorometoksi)fenil, 3,5-dihidroksifenil, fenil-3-sulfonamid ili 3-(trifluorometil)fenil, ili farmaceutski prihvatljiva sol ili njegov solvat; spoj formule (II): [image] pri čemu R je NHR1, pri čemu je R1 2-fluoro-4-jodofenil, ili njegova farmaceutski prihvatljiva sol ili solvat; spoj formule (III): [image] pri čemu je R NHR1, pri čemu je R1 3-etinilfenil, 3-kloro-4-fluorofenil, 2-fluoro-4-jodofenil ili 4-kloro 3-(trifluorometil) fenil, ili njegova farmaceutski prihvatljiva sol ili solvat; ili njihovu kombinaciju; i farmaceutski prihvatljiv nosač ili pomoćna tvar.
2. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 1, pri čemu je BRaf inhibitor spoj formule (I) i pri čemu je R 3-(trifluorometoksi)fenil.
3. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 2, pri čemu je sastav u obliku gela, hidrogela, masti, kreme, paste, pjene, spreja, losiona, tekućine ili dermalnog flastera.
4. Sastav za lokalnu primjenu za upotrebu prema bilo kojem patentnom zahtjevu 1-3, pri čemu je BRaf inhibitor prisutan u sastavu u koncentraciji od 1% masenog udjela do 5% masenog udjela od ukupne mase sastava.
5. Sastav za lokalnu primjenu za upotrebu prema bilo kojem patentnom zahtjevu 1-3, pri čemu je BRaf inhibitor prisutan u sastavu u koncentraciji od 0.1% masenog udjela do 10% masenog udjela od ukupne mase sastava.
6. Sastav za lokalnu primjenu za upotrebu prema bilo kojem patentnom zahtjevu 1-5, pri čemu upotreba smanjuje ozbiljnost ili sprječava eskalaciju radijacijskog dermatitisa.
7. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba smanjuje ozbiljnost kožne nuspojave sa stupnja 4 na stupanj 3, 2, 1 ili 0 kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili prema ljestvici ocjenjivanja Onkološke grupe za radijacijsku terapiju (RTOG).
8. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba smanjuje ozbiljnost kožne nuspojave sa stupnja 3 na stupanj 2, 1 ili 0, kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili odgovarajućom RTOG ocjenom.
9. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba smanjuje ozbiljnost kožne nuspojave sa stupnja 2 na stupanj 1 ili 0, kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili odgovarajućom RTOG ocjenom.
10. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba smanjuje ozbiljnost kožne nuspojave sa stupnja 1 na stupanj 0, kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili odgovarajućom RTOG ocjenom.
11. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba sprječava eskalaciju kožne nuspojave sa stupnja 0 na stupanj 1, 2, 3 ili 4, kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili odgovarajućom RTOG ocjenom.
12. Sastav za lokalnu primjenu za upotrebu prema patentnom zahtjevu 6, pri čemu upotreba sprječava eskalaciju kožne nuspojave sa stupnja 1 na stupanj 2, 3 ili 4, kako je definirano Zajedničkim terminološkim kriterijima za nuspojave Nacionalnog instituta za rak (NCI-CTCAE) verzije 5.0 ili odgovarajućom RTOG ocjenom.
HRP20231241TT 2019-02-12 2020-02-11 Upotreba sastava braf inhibitora za lokalnu primjenu za liječenje radijacijskog dermatitisa HRP20231241T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962804235P 2019-02-12 2019-02-12
EP20756229.9A EP3923911B1 (en) 2019-02-12 2020-02-11 Use of topical braf inhibitor compositions for treatment of radiation dermatitis
PCT/IB2020/051073 WO2020165755A1 (en) 2019-02-12 2020-02-11 Use of topical braf inhibitor compositions for treatment of radiation dermatitis

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US (1) US11439648B2 (hr)
EP (1) EP3923911B1 (hr)
JP (1) JP2022519675A (hr)
KR (1) KR102534457B1 (hr)
CN (1) CN113382717A (hr)
AU (1) AU2020220895B9 (hr)
BR (1) BR112021015137A2 (hr)
CA (1) CA3127175C (hr)
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HR (1) HRP20231241T1 (hr)
HU (1) HUE063091T2 (hr)
IL (1) IL285560B2 (hr)
MX (1) MX2021009535A (hr)
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RS (1) RS64618B1 (hr)
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WO2022136912A1 (en) * 2020-12-24 2022-06-30 Lutris Pharma Ltd. Topical braf inhibitor compositions for treatment of egfr downstream effectors - induced reactions
WO2023275620A2 (en) * 2021-07-02 2023-01-05 Lutris Pharma Ltd. Use of isoquinoline-1,5-diamines for wound healing
CN118139621A (zh) * 2021-09-30 2024-06-04 北京大学 一种对红系前体细胞或成红细胞进行扩增的方法及其应用

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AU2020220895A1 (en) 2021-08-12
EP3923911A4 (en) 2022-11-09
CN113382717A (zh) 2021-09-10
BR112021015137A2 (pt) 2021-09-28
WO2020165755A1 (en) 2020-08-20
US20210346389A1 (en) 2021-11-11
IL285560B2 (en) 2024-04-01
MX2021009535A (es) 2022-10-10
CA3127175C (en) 2023-06-27
RS64618B1 (sr) 2023-10-31
AU2020220895B2 (en) 2022-11-17
KR20210126665A (ko) 2021-10-20
JP2022519675A (ja) 2022-03-24
EP3923911A1 (en) 2021-12-22
ZA202106581B (en) 2022-09-28
IL285560B1 (en) 2023-12-01
CA3127175A1 (en) 2020-08-20
EP3923911C0 (en) 2023-07-12
ES2952251T3 (es) 2023-10-30
KR102534457B1 (ko) 2023-05-18
PL3923911T3 (pl) 2023-12-27
US11439648B2 (en) 2022-09-13
EP3923911B1 (en) 2023-07-12
AU2020220895B9 (en) 2023-02-02

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