HRP20231467T1 - Spojevi - Google Patents

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Publication number
HRP20231467T1
HRP20231467T1 HRP20231467TT HRP20231467T HRP20231467T1 HR P20231467 T1 HRP20231467 T1 HR P20231467T1 HR P20231467T T HRP20231467T T HR P20231467TT HR P20231467 T HRP20231467 T HR P20231467T HR P20231467 T1 HRP20231467 T1 HR P20231467T1
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HR
Croatia
Prior art keywords
substituted
compound
salt
hydroxy
phenyl
Prior art date
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HRP20231467TT
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English (en)
Inventor
Paul Anthony Stupple
Helen Rachel LAGIAKOS
Benjamin Joseph MORROW
Richard Charles FOITZIK
Catherine Fae HEMLEY
Michelle Ang CAMERINO
Ylva Elisabet Bergman BOZIKIS
Scott Raymond WALKER
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Ctxt Pty Ltd
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Publication of HRP20231467T1 publication Critical patent/HRP20231467T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D261/00Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/20Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
    • 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
    • A61K31/42Oxazoles
    • A61K31/423Oxazoles condensed with carbocyclic 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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61K31/425Thiazoles
    • A61K31/428Thiazoles condensed with carbocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Claims (14)

1. Spoj formule (I): [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što: R1, R2, R3 i R4 se neovisno bira između: (i) H; (ii) C1-3 alkila, koji može biti supstituiran s: hidroksi, C1-2 alkoksi, NH2, fenilom, C5-6 heteroarilom, C1-4 alkil-karbamoilom, ili acilamido; (iii) C1-3 alkoksi, koji može biti supstituiran s C3-6 cikloalkilom, ili s jednom ili više fluornih skupina; (iv) C3-6 cikloalkil; (v) halogena; (vi) CORC, gdje se RC bira između NRN1RN2, gdje se RN1 i RN2 neovisno bira između H i metila; (vii) cijano, NH2, ili NO2; i (viii) fenila ili C5-6 heteroarila, koji može biti supstituiran s metilom, hidroksi ili metoksi; Ar je fenil, koji može biti supstituiran s jednom ili više skupina koje se bira između: (i) C1-4 alkila, koji može biti supstituiran s hidroksi, C1-2 alkoksi, NH2, C1-4 alkil-karbamoilom, ili s jednom ili više fluornih skupina; (ii) C3-6 cikloalkila; (iii) hidroksi; cijano; NRN3RN4, gdje se RN3 i RN4 neovisno bira između H i metila; ili acilamido; (iv) halogena; (v) C1-3 alkoksi, koji može biti supstituiran s hidroksi, C(O)NH2, C3-6 cikloalkilom, fenilom, C5-6 heteroarilom, ili s jednom ili više fluornih skupina; (vi) fenoksi, koji može biti supstituiran s fluorom; (vii) fenila ili C5-6 heteroarila; ili (viii) SF5 ili SO2CH3; i gdje najmanje jedan od R1, R2, R3 i R4 nije H.
2. Spoj, ili sol, u skladu s patentnim zahtjevom 1, naznačen time što je najmanje jedan od R1, R2, R3 i R4 C1-3 alkil, koji može biti supstituiran s: hidroksi, C1-2 alkoksi, NH2, fenilom, C5-6 heteroarilom, C1-4 alkil-karbamoilom, ili acilamido.
3. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 2, naznačen time što je najmanje jedan od R1, R2, R3 i R4 C1-3 alkoksi, koji može biti supstituiran s C3-6 cikloalkilom, ili jednom ili više fluornih skupina.
4. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što je najmanje jedan od R1, R2, R3 i R4: (a) C3-6 cikloalkil; (b) CORC, gdje se RC bira između NRN1RN2, gdje se RN1 i RN2 neovisno bira između H i metila; (c) cijano, NH2 ili NO2; ili (d) fenil ili C5-6 heteroaril, koji može biti supstituiran s metilom, hidroksi ili metoksi.
5. Spoj, ili sol, u skladu s patentnim zahtjevom 1, naznačen time što: (a) R4 je metoksi, R2 je CH2OCH3 ili CH2OCH2CH3, a R1 i R3 su H; (b) R4 je metoksi, R2 je fenil, koji može biti supstituiran s metilom ili metoksi, a R1 i R3 su H; (c) R4 je metoksi, R2 je C5-6 heteroaril, koji može biti supstituiran s metilom; (d) R4 je metoksi, a R1, R2 i R3 su H; (e) R4 je klor, R2 je C1-3 alkil ili brom, a R1 i R3 su H; ili (f) R3 je C1-3 alkil, a R1, R2 i R4 su H.
6. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je Ar supstituiran s C1-4 alkilom, koji može biti supstituiran s hidroksi, C1-2 alkoksi, NH2, C1-4 alkil-karbamoilom, ili jednom ili više fluornih skupina.
7. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je Ar supstituiran s C1-3 alkoksi, koji može biti supstituiran s hidroksi, C(O)NH2, C3-6 cikloalkilom, fenilom, C5-6 heteroarilom, ili jednom ili više fluornih skupina.
8. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je Ar supstituiran s: (a) C3-6 cikloalkilom; (b) hidroksi; (c) cijano; (d) NRN3RN4, gdje se RN3 i RN4 neovisno bira između H i metila; ili acilamido; (e) fenoksi, koji može biti supstituiran s fluorom; (f) fenilom ili C5-6 heteroarilom; ili (g) SF5 ili SO2CH3.
9. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je Ar: (a) 5-etil-2-metoksifenil; (b) 5-CF3-2-metoksifenil; ili (c) 2,6-dimetoksifenil.
10. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 9, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivo pomoćno sredstvo.
11. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je namijenjen upotrebi u postupku terapije.
12. Spoj, ili sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 9, naznačen time što je namijenjen upotrebi u liječenju raka.
13. Spoj, ili sol, namijenjen upotrebi u skladu s patentnim zahtjevom 12, naznačen time što se rak bira između leukemije, akutne limfocitne leukemije, akutne mijeloidne leukemije, kronične limfocitne leukemije, kronične mijeloidne leukemije, nehodgkinovske leukemije, Hodgkinove bolesti, raka prostate, raka pluća, melanoma, raka dojke, raka debelog crijeva i rektuma, raka debelog crijeva, karcinoma pločastih stanica i raka želuca.
14. Spoj, ili sol, namijenjen upotrebi u skladu s patentnim zahtjevom 12, naznačen time što se spoj primijenjuje istodobno ili uzastopno u odnosu na radioterapiju i/ili kemoterapiju.
HRP20231467TT 2018-06-20 2019-06-20 Spojevi HRP20231467T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1810092.5A GB201810092D0 (en) 2018-06-20 2018-06-20 Compounds
EP19734722.2A EP3810602B1 (en) 2018-06-20 2019-06-20 Compounds
PCT/EP2019/066337 WO2019243491A1 (en) 2018-06-20 2019-06-20 Compounds

Publications (1)

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HRP20231467T1 true HRP20231467T1 (hr) 2024-03-01

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US (2) US20200039945A1 (hr)
EP (2) EP3810602B1 (hr)
JP (1) JP2021529738A (hr)
KR (1) KR20210022655A (hr)
CN (1) CN112334466A (hr)
AR (1) AR114972A1 (hr)
AU (1) AU2019289888A1 (hr)
BR (1) BR112020025869A2 (hr)
CA (1) CA3101238A1 (hr)
CL (1) CL2020003219A1 (hr)
CO (1) CO2020014586A2 (hr)
CR (1) CR20210032A (hr)
CU (1) CU20200096A7 (hr)
DK (1) DK3810602T3 (hr)
DO (1) DOP2020000249A (hr)
EA (1) EA202092451A1 (hr)
EC (1) ECSP20075270A (hr)
FI (1) FI3810602T3 (hr)
GB (1) GB201810092D0 (hr)
GE (1) GEP20227403B (hr)
HR (1) HRP20231467T1 (hr)
IL (1) IL279554A (hr)
LT (1) LT3810602T (hr)
MA (1) MA52948B1 (hr)
MD (1) MD3810602T2 (hr)
MX (1) MX2020012723A (hr)
NI (1) NI202000092A (hr)
PE (1) PE20210181A1 (hr)
PH (1) PH12020500673A1 (hr)
PL (1) PL3810602T3 (hr)
PT (1) PT3810602T (hr)
RS (1) RS64932B1 (hr)
SG (1) SG11202010450VA (hr)
SI (1) SI3810602T1 (hr)
TW (1) TWI826471B (hr)
UY (1) UY38270A (hr)
WO (1) WO2019243491A1 (hr)

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BR112023000687A2 (pt) 2020-07-15 2023-02-07 Pfizer Métodos e combinações de inibidores de kat6 para o tratamento de câncer
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KR20240046530A (ko) 2021-08-10 2024-04-09 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 설폰아미드 유도체, 이의 제조 방법 및 이의 의학적 용도
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PL3810602T3 (pl) 2024-03-04
PT3810602T (pt) 2024-01-03
EP3810602A1 (en) 2021-04-28
MD3810602T2 (ro) 2024-03-31
PE20210181A1 (es) 2021-01-29
US20200039945A1 (en) 2020-02-06
GEP20227403B (en) 2022-08-10
MX2020012723A (es) 2021-05-14
KR20210022655A (ko) 2021-03-03
SI3810602T1 (sl) 2024-02-29
SG11202010450VA (en) 2021-01-28
FI3810602T3 (fi) 2023-12-21
IL279554A (en) 2021-01-31
PH12020500673A1 (en) 2021-05-31
AR114972A1 (es) 2020-11-11
MA52948B1 (fr) 2024-02-29
NI202000092A (es) 2021-03-23
EP3810602B1 (en) 2023-11-01
TW202016103A (zh) 2020-05-01
LT3810602T (lt) 2024-01-25
GB201810092D0 (en) 2018-08-08
BR112020025869A2 (pt) 2021-03-23
CL2020003219A1 (es) 2021-06-11
DK3810602T3 (da) 2023-12-11
EA202092451A1 (ru) 2021-03-16
DOP2020000249A (es) 2021-02-28
TWI826471B (zh) 2023-12-21
CA3101238A1 (en) 2019-12-26
US20220153710A1 (en) 2022-05-19
CR20210032A (es) 2021-02-11
CU20200096A7 (es) 2021-08-06
MA52948A (fr) 2021-04-28
UY38270A (es) 2020-01-31
ECSP20075270A (es) 2021-02-26
EP4335439A2 (en) 2024-03-13
CN112334466A (zh) 2021-02-05
CO2020014586A2 (es) 2021-03-08
RS64932B1 (sr) 2023-12-29
WO2019243491A1 (en) 2019-12-26
AU2019289888A1 (en) 2020-11-12
JP2021529738A (ja) 2021-11-04

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