HRP20192209T1 - Derivati benzofurana, postupci njihove pripreme i njihova uporaba u medicini - Google Patents
Derivati benzofurana, postupci njihove pripreme i njihova uporaba u medicini Download PDFInfo
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- HRP20192209T1 HRP20192209T1 HRP20192209TT HRP20192209T HRP20192209T1 HR P20192209 T1 HRP20192209 T1 HR P20192209T1 HR P20192209T T HRP20192209T T HR P20192209TT HR P20192209 T HRP20192209 T HR P20192209T HR P20192209 T1 HRP20192209 T1 HR P20192209T1
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- alkyl
- heterocyclyl
- cycloalkyl
- compound
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- 238000002360 preparation method Methods 0.000 title claims 2
- 150000001907 coumarones Chemical class 0.000 title 1
- 239000003814 drug Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 28
- 125000000753 cycloalkyl group Chemical group 0.000 claims 24
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 23
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 16
- 125000001188 haloalkyl group Chemical group 0.000 claims 16
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 125000003545 alkoxy group Chemical group 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 14
- -1 nitro, hydroxy Chemical group 0.000 claims 12
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000004438 haloalkoxy group Chemical group 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 5
- 208000032839 leukemia Diseases 0.000 claims 4
- 206010025323 Lymphomas Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010027406 Mesothelioma Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 125000004043 oxo group Chemical group O=* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 2
- 206010042863 synovial sarcoma Diseases 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000013452 Fallopian tube neoplasm Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 1
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000003445 Mouth Neoplasms Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 238000009833 condensation Methods 0.000 claims 1
- 230000005494 condensation Effects 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000003444 follicular lymphoma Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000000050 myeloid neoplasm Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Claims (15)
1. Spoj formule (I):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova smjesa, ili njegova farmaceutski prihvatlјiva sol,
gdje:
prsten A je odabran iz skupine sastavljene od heterociklila i cikloalkila;
svaki R1 je jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, halogen, alkil, haloalkil, alkoksi, haloalkoksi, amino, nitro, hidroksi, cijano, cikloalkil, heterociklil, aril, heteroaril, -OR6, -C(O)R6, -C(O)OR6, -S(O)mR6, -S(O)mNR7R8 i -(CH2)xRa, pri čemu je svaka alkil, haloalkil, heterociklil, aril i heteroaril skupinu nezavisno i po izboru supstituisana s jednom ili više skupina odabranih iz skupine koju čine alkil, haloalkil, halogena, amino, nitro, cijano, hidroksi, alkoksi, haloalkoksi, hidroksialkil, cikloalkil, heterociklil, aril i heteroaril skupine;
Ra je odabran iz skupine koju čine halogen, cikloalkil, heterociklil i -NR7R8, pri čemu je svaki cikloalkil i heterociklil nezavisno i po izboru supstituiran s jednom ili više skupina odabran iz skupine koju čine alkil, haloalkil, halogena, amino, nitro, cijano, hidroksi, alkoksi, haloalkoksi, hidroksialkil, cikloalkil, heterociklil, aril i heteroaryl skupina;
R2 je vodik ili alkil, pri čemu je alkil po izboru supstituiran s jednom ili više odabranih iz skupine koju čine halogen, hidroksi, cijano, cikloalkil i heterociklil;
R3 je odabran iz skupine koju čine vodik, alkil, halogena, cijano, alkoksi i haloalkil skupina;
svaki R4 je jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, alkil, haloalkil, hidroksi, amino, alkoksi, haloalkoksi, cikloalkil, heterociklil, aril, heteroaril skupina, -OR6, -C(O)R6, -C(O)OR6, -S(O)mR6, -S(O)mNR7R8 i -NR7R8;
svaki R5 je jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, alkil, okso, halogena, haloalkil, hidroksi, amino, alkoksi, haloalkoksi, cikloalkil, heterociklil, aril, heteroaril skupina, -OR6, -C(O)R6, -C(O)OR6, -S(O)mR6, -S(O)mNR7R8 i -NR7R8;
R6 je odabran iz skupine koju čine vodik, alkil, haloalkil, alkoksi, hidroksialkil, hidroksi, amino, cikloalkil, heterociklil, aril i heteroaril skupina;
R7 i R8 su jednaki ili različiti i svaki je neovisno odabran iz skupine koju čine vodik, alkil, alkoksi, hidroksialkil, hidroksi, amino, alkoksikarbonil, cikloalkil, heterociklil, aril i heteroaril skupina, pri čemu je svaka alkil, amino, cikloalkil, heterociklil, aril i heteroaril skupina neovisno i po izboru supstituirana s jednom ili više skupina odabranih iz skupine koju čine alkil, halogena, hidroksi, amino, alkoksikarbonil, nitro, cijano, alkoksi, hidroksialkil, cikloalkil, heterociklil, aril i heteroaril skupina;
m je 0, 1 ili 2;
n je 0, 1, 2 ili 3;
p je 0, 1, 2, 3, 4 ili 5;
q je 0, 1 ili 2; i
x je 0, 1, 2 ili 3.
2. Spoj formule (I) sukladno patentnom zahtjevu 1, gdje je n 2; i/ili
gdje je svaki od p i q 0, 1 ili 2.
3. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva 1 ili 2, gdje je svaki R1 jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, halogen, alkil, haloalkil, cijano, cikloalkil, heterociklil i -(CH2)xRa, pri čemu je svaki alkil i heterociklil neovisno i po izboru supstituiran s jednom ili s više skupina odabranih iz skupine sastavljene od alkila, hidroksialkila i halogena; i Ra je odabran iz skupine koju čine halogen, cikloalkil, heterociklil i -NR7R8, pri čemu je svaki cikloalkil i heterociklil neovisno i po izboru supstituiran s jednom ili više skupina odabranih iz skupine sastavljene od hidroksialkila, alkila i halogena; a R7, R8 i x su kao što je definirano u patentnom zahtjevu 1; po izboru, gdje je svaki R1 jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, alkil, haloalkil, cijano i -(CH2)xRa, pri čemu je x 0 i Ra je halogen ili cikloalkil.
4. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva od 1 do 3, gdje je R2 alkil, po izboru supstituiran sa cikloalkil skupinom; i/ili
gdje je R3 odabran iz skupine sastavljene od alkila, halogena i haloalkila.
5. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva od 1 do 4, gdje je svaki R4 jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, alkil i alkoksi; i/ili
gdje je svaki R5 jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, halogen, okso, haloalkil, -C(O)R6, -S(O)mR6 i - NR7R8, pri čemu su od R6 do R8 i m kao što je definirano u patentnom zahtjevu 1 i poželjno vodik.
6. Spoj formule (I) sukladno patentnom zahtjevu 1, koje je spoj formule (II):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova smjesa, ili njegova farmaceutski prihvatljiva sol,
gdje:
G je odabran iz skupine koju čine CRbRc, C=O, NRd, S(O)m i kisik;
svaki Rb i Rc je neovisno odabran iz skupine koju čine vodik, alkil, alkoksi, halogena, amino, nitro, hidroksi, cijano, cikloalkil, heterociklil, aril, heteroaril skupina, -OR6, -C(O)R6, -C(O)OR6, -S(O)mR6 i -NR7R8;
Rd je odabran iz skupine koju čine vodik, alkil, cikloalkil, haloalkil, hidroksialkil, heterociklil, aril, heteroaril, -C(O)R6, -C(O)OR6 i S(O)mR6; i
R1 do R4, R6 do R8, n, m i q su kao što je definirano u patentnom zahtjevu 1.
7. Spoj formule (II) sukladno patentnom zahtjevu 6, koje je spoj formule (III):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova smjesa, ili njegova farmaceutski prihvatljiva sol,
gdje:
E je CH ili N atom;
F je odabran iz skupine sastavljene od CRbRc, C=O, NRd i kisika;
svaki Rb i Rc su neovisno odabrani iz skupine koju čine vodik, alkil, alkoksi, halogena, amino, nitro, hidroksi, cijano, cikloalkil, heterociklil, aril, heteroaril skupina, -OR6, -C(O)R6, -C(O)OR6, -S(O)mR6 i -NR7R8;
Rd je odabran iz skupine koju čine vodik, alkil, cikloalkil, haloalkil, hidroksialkil, heterociklil, aril, heteroaril, -C(O)R6, -C(O)OR6 i S(O)mR6;
svaki Re je jednak ili različit i svaki je neovisno odabran iz skupine koju čine vodik, alkil, haloalkil, halogena, amino, nitro, cijano, hidroksi, alkoksi, haloalkoksi, hidroksialkil, cikloalkil, heterociklil, aril i heteroaril skupina;
t je 0, 1, 2, 3, 4 ili 5;
x je 0, 1, 2 ili 3;
y je 0, 1, 2 ili 3; i
R1 do R4, R6 do R8, m i n su kao što je definirano u patentnom zahtjevu 1.
8. Spoj formule (III) sukladno patentnom zahtjevu 7, koji je spoj formule (IV):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova smjesa, ili njegova farmaceutski prihvatljiva sol,
gdje:
svaki Re je jednak ili različit i svaki je odabran iz skupine sastavljene od vodika, alkila i halogena;
t je 0, 1, 2, 3, 4 ili 5; i
R2 do R4 i n su kao što je definirano u patentnom zahtjevu 1.
9. Spoj formule (III) sukladno patentnom zahtjevu 7, koji spoj formule je (V):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova sjmesa, ili njegova farmaceutski prihvatljiva sol,
gdje:
Re je odabran iz skupine koju čine vodik, alkil, haloalkil, halogena, amino, nitro, cijano, hidroksi, alkoksi, haloalkoksi, hidroksialkil, cikloalkil, heterociklil, aril i heteroaril skupina; i
R2 do R4 i n su kao što je definirano u patentnom zahtjevu 1.
10. Spoj sukladno bilo kojem od patentnih zahtjeva od 1 do 9, pri čemu je spoj odabran iz skupine sastavljene od:
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
[image]
11. Spoj formule (VI):
[image]
ili tautomer, mezomer, racemat, enantiomer, dijastereomer ili njihova smjesa, ili njegova farmaceutski prihvatljiva sol,
gdje:
prsten A, R1 do R3, R5, p i q su kao što je opisano u patentnom zahtjevu 1.
12. Postupak za dobivanje spoja formule (I) sukladno patentnom zahtjevu 1, koji sadrži korak:
[image]
kondenzacije spoja formule (VI) sa spojem formule (VII) na sobnoj temperaturi da bi se dobio spoj formule (I);
gdje:
R1 do R5, prstenovi A, p, q i n su kao što je definirano u patentnom zahtjevu 1.
13. Farmaceutski pripravak koji sadrži terapijski učinkovitu količinu spoja formule (I) sukladno bilo kojem od patentnih zahtjeva od 1 do 10 i jedan ili više farmaceutski prihvatljivih nosača, otapala ili ekscipijenasa.
14. Spoj formule (I) sukladno bilo kojem od patentnih zahtjeva od 1 do 14 ili farmaceutski pripravak sukladno patentnom zahtjevu 13, za uporabu u obliku inhibitora EZH2 radi prevencije i/ili liječenja tumora i karcinoma.
15. Spoj ili pripravak radi uporabe sukladno patentnom zahtjevu 14, pri čemu su tumor i karcinom odabrani iz skupine sastavljene od limfoma, leukemije, karcinoma dojke, karcinoma pluća, karcinoma prostate, karcinoma jajnika, karcinoma jetre, melanoma, rabdomiosarkoma, sinovijalnog sarkoma, mezotelioma, karcinoma grlića materice, karcinoma debelog crijeva, rektalnog karcinoma, karcinoma želuca, karcinoma pankreasa, karcinoma mozga, karcinoma kože, oralnog karcinoma, karcinoma kostiju, karcinoma bubrega, karcinoma mokraćnog mjehura, tumora jajovoda, tumora jajnika, peritonealnog tumora, glioma, glioblastoma, karcinoma glave i vrata i mijeloma; poželјno limfoma, leukemije, karcinoma dojke, karcinoma pluća, karcinoma prostate, karcinoma jajnika, karcinoma jetre, melanoma, rabdomiosarkoma, sinovijalnog sarkoma i mezotelioma;
pri čemu je leukemija poželјno kronična mijeloična leukemija, akutna mijeloična leukemija ili leukemija mješovitih linija; i pri čemu je limfom poželjno non-Hodkinov limfom, difuzni krupnostanični B-limfom ili folikularni limfom.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510800975 | 2015-11-19 | ||
| PCT/CN2016/104318 WO2017084494A1 (zh) | 2015-11-19 | 2016-11-02 | 苯并呋喃类衍生物、其制备方法及其在医药上的应用 |
| EP16865671.8A EP3378859B1 (en) | 2015-11-19 | 2016-11-02 | Benzofuran derivative, preparation method thereof and use thereof in medicine |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20192209T1 true HRP20192209T1 (hr) | 2020-07-24 |
Family
ID=58717310
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20192209TT HRP20192209T1 (hr) | 2015-11-19 | 2019-12-09 | Derivati benzofurana, postupci njihove pripreme i njihova uporaba u medicini |
Country Status (22)
| Country | Link |
|---|---|
| US (2) | US10759787B2 (hr) |
| EP (1) | EP3378859B1 (hr) |
| JP (1) | JP6828229B2 (hr) |
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Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| TWI810185B (zh) * | 2017-05-18 | 2023-08-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 一種ｅｚｈ２抑制劑與ｂｔｋ抑制劑聯合在製備治療腫瘤的藥物中的用途 |
| MX2019012967A (es) | 2017-05-18 | 2020-01-20 | Jiangsu Hengrui Medicine Co | Cristal de base libre de derivados benzofurano y metodo de preparacion. |
| EP3708567A4 (en) * | 2017-11-10 | 2021-07-07 | Jiangsu Hengrui Medicine Co., Ltd. | PROCESS FOR THE PREPARATION OF A BENZOFURANE DERIVATIVE |
| CA3089639A1 (en) | 2018-01-31 | 2019-08-08 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidinyl compounds as prc2 inhibitors |
| CN110179796B (zh) * | 2018-02-23 | 2023-01-24 | 江苏恒瑞医药股份有限公司 | 一种苯并呋喃类衍生物的组合物及制备方法 |
| BR112020021194A2 (pt) * | 2018-04-18 | 2021-03-23 | Constallation Pharmaceuticals, Inc. | moduladores de enzimas modificadoras de metila, composições e usos dos mesmos |
| CN110563722A (zh) * | 2018-06-06 | 2019-12-13 | 上海青煜医药科技有限公司 | 吡啶或哒嗪并环化合物及其应用 |
| CN112512580B (zh) * | 2018-09-29 | 2024-04-16 | 江苏恒瑞医药股份有限公司 | Ezh2抑制剂与免疫检查点抑制剂联合在制备治疗肿瘤的药物中的用途 |
| WO2020192652A1 (zh) | 2019-03-25 | 2020-10-01 | 上海华汇拓医药科技有限公司 | 酰胺类化合物制备方法及其在医药领域的应用 |
| CN113302185B (zh) * | 2019-04-29 | 2024-04-09 | 上海和誉生物医药科技有限公司 | 苯并呋喃-6-甲酰胺衍生物、其制备方法和药学上的应用 |
| CN110003187B (zh) * | 2019-05-10 | 2021-11-05 | 南京工业大学 | 一种多氟烷基取代苯并呋喃类化合物及其制备方法 |
| TW202108578A (zh) * | 2019-05-10 | 2021-03-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | 6-取代氨基苯并呋喃化合物的製備方法 |
| CN112007162B (zh) * | 2019-05-30 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | Ezh2抑制剂与免疫检查点抑制剂、vegfr抑制剂联合在制备治疗肿瘤药物中的用途 |
| CN110172448B (zh) * | 2019-05-30 | 2020-07-28 | 中南大学湘雅二医院 | 一种滑膜肉瘤细胞系hSS-005R及其子代细胞系 |
| TW202114663A (zh) * | 2019-09-30 | 2021-04-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | EZH2抑制劑與含有TGF-β受體的融合蛋白聯合在製備治療腫瘤的藥物中的用途 |
| TW202114670A (zh) * | 2019-09-30 | 2021-04-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 一種ezh2抑制劑與cdk4/6抑制劑聯合在製備治療腫瘤藥物中的用途 |
| TW202126302A (zh) * | 2019-09-30 | 2021-07-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | Ｅｚｈ２抑制劑與免疫檢查點抑制劑、酪胺酸激酶抑制劑聯合在製備治療腫瘤藥物中的用途 |
| CN112870365A (zh) * | 2019-11-29 | 2021-06-01 | 江苏恒瑞医药股份有限公司 | Ezh2抑制剂和/或parp抑制剂与化疗药物联合在制备治疗肿瘤药物中的用途 |
| IL311097A (en) | 2021-08-30 | 2024-04-01 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Use of an EZH2 inhibitor in the preparation of drugs for the treatment of T-cell lymphoma |
| TW202330509A (zh) * | 2021-10-15 | 2023-08-01 | 大陸商江蘇恒瑞醫藥股份有限公司 | 苯並呋喃衍生物的製備方法 |
| WO2023244917A1 (en) | 2022-06-13 | 2023-12-21 | Treeline Biosciences, Inc. | 1,8-naphthyridin-2-one heterobifunctional bcl6 degraders |
| WO2023244918A1 (en) | 2022-06-13 | 2023-12-21 | Treeline Biosciences, Inc. | Quinolone bcl6 bifunctional degraders |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20110275630A1 (en) | 2003-06-02 | 2011-11-10 | Abbott Laboratories | Isoindolinone kinase inhibitors |
| WO2009101022A1 (en) * | 2008-02-14 | 2009-08-20 | F. Hoffmann-La Roche Ag | Heterocyclic antiviral compounds |
| WO2011140325A1 (en) | 2010-05-07 | 2011-11-10 | Glaxosmithkline Llc | Indazoles |
| EP2566327B1 (en) * | 2010-05-07 | 2017-03-29 | Glaxosmithkline LLC | Indoles |
| EP2566479B1 (en) | 2010-05-07 | 2014-12-24 | GlaxoSmithKline LLC | Azaindazoles |
| EP2410171A1 (en) | 2010-07-23 | 2012-01-25 | Ewt Ip B.V. | Wind turbine having a rotor with hub |
| SG180031A1 (en) | 2010-10-15 | 2012-05-30 | Agency Science Tech & Res | Combination treatment of cancer |
| EP2681216B1 (en) * | 2011-02-28 | 2017-09-27 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| TW201733984A (zh) * | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| EP2755962B1 (en) * | 2011-09-13 | 2017-03-01 | Glaxosmithkline LLC | Azaindazoles |
| CN103987842A (zh) | 2011-09-30 | 2014-08-13 | 葛兰素史密斯克莱有限责任公司 | 治疗癌症的方法 |
| WO2013067300A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| WO2013173441A2 (en) | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| UA111305C2 (uk) | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| CN105308038B (zh) | 2013-04-30 | 2018-05-29 | 葛兰素史密斯克莱知识产权（第2 号）有限公司 | Zeste增强子同源物2的抑制剂 |
| US9822103B2 (en) * | 2013-11-22 | 2017-11-21 | Bristol-Myers Squibb Company | Inhibitors of lysine methyl transferase |
| SI3121175T1 (sl) | 2014-03-17 | 2020-07-31 | Daiichi Sankyo Company, Limited | Derivati 1,3-benzodioksola kot EZH1 in/ali EZH2 inhibitorji |
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2016
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| SI3378859T1 (sl) | 2020-03-31 |
| PL3378859T3 (pl) | 2020-04-30 |
| AU2016357900B2 (en) | 2020-09-17 |
| HUE047785T2 (hu) | 2020-05-28 |
| CN107428742A (zh) | 2017-12-01 |
| US11059811B2 (en) | 2021-07-13 |
| JP6828229B2 (ja) | 2021-02-10 |
| BR112018007876B1 (pt) | 2023-10-17 |
| LT3378859T (lt) | 2020-01-27 |
| CA3002436A1 (en) | 2017-05-26 |
| US20180327394A1 (en) | 2018-11-15 |
| EP3378859A4 (en) | 2018-09-26 |
| RU2018119173A3 (hr) | 2020-02-13 |
| TW201718561A (zh) | 2017-06-01 |
| EP3378859A1 (en) | 2018-09-26 |
| TWI718207B (zh) | 2021-02-11 |
| MX2018005019A (es) | 2018-06-13 |
| DK3378859T3 (da) | 2020-01-20 |
| RU2727198C2 (ru) | 2020-07-21 |
| KR20180081587A (ko) | 2018-07-16 |
| AU2016357900A1 (en) | 2018-05-24 |
| US20200354349A1 (en) | 2020-11-12 |
| JP2018538257A (ja) | 2018-12-27 |
| PT3378859T (pt) | 2019-12-11 |
| RU2018119173A (ru) | 2019-12-19 |
| WO2017084494A1 (zh) | 2017-05-26 |
| ES2760510T3 (es) | 2020-05-14 |
| BR112018007876A2 (pt) | 2018-10-30 |
| CN107428742B (zh) | 2020-05-08 |
| HK1243414A1 (zh) | 2018-07-13 |
| EP3378859B1 (en) | 2019-10-30 |
| RS59763B1 (sr) | 2020-02-28 |
| US10759787B2 (en) | 2020-09-01 |
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