HRP20191202T1 - Pteridini kao inhibitori fgfr - Google Patents
Pteridini kao inhibitori fgfr Download PDFInfo
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- HRP20191202T1 HRP20191202T1 HRP20191202TT HRP20191202T HRP20191202T1 HR P20191202 T1 HRP20191202 T1 HR P20191202T1 HR P20191202T T HRP20191202T T HR P20191202TT HR P20191202 T HRP20191202 T HR P20191202T HR P20191202 T1 HRP20191202 T1 HR P20191202T1
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- Prior art keywords
- 6alkyl
- substituted
- cancer
- alkyl
- nr14r15
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- 239000003112 inhibitor Substances 0.000 title 1
- 150000003195 pteridines Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 43
- 125000000217 alkyl group Chemical group 0.000 claims 32
- 206010028980 Neoplasm Diseases 0.000 claims 30
- 201000011510 cancer Diseases 0.000 claims 27
- 150000001875 compounds Chemical class 0.000 claims 15
- 238000011282 treatment Methods 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 206010005003 Bladder cancer Diseases 0.000 claims 5
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 5
- 239000002246 antineoplastic agent Substances 0.000 claims 5
- 125000004093 cyano group Chemical group *C#N 0.000 claims 5
- 201000005112 urinary bladder cancer Diseases 0.000 claims 5
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 4
- -1 -NR4R5 Chemical group 0.000 claims 4
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 4
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 125000005843 halogen group Chemical group 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 238000011321 prophylaxis Methods 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 1
- 208000034951 Genetic Translocation Diseases 0.000 claims 1
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 229910007161 Si(CH3)3 Inorganic materials 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 208000017572 squamous cell neoplasm Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/02—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4
- C07D475/04—Heterocyclic compounds containing pteridine ring systems with an oxygen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
- C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
- C07D475/08—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Claims (13)
1. Spoj s formulom (I):
uključujući bilo koji njegov tautomerni ili stereokemijski izomerni oblik, naznačen time što
W je -N(R3)-;
svaki R2 je neovisno odabran od halogena ili C1-4alkoksi;
D predstavlja fenil ili aromatski 5-člani ili 6-člani prstenski monociklički heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S, pri čemu navedeni fenil ili heterociklil može biti svaki po izboru supstituiran s jednom ili više (npr. 1, 2 ili 3) skupina R1;
R1 predstavlja vodik, halo, cijano, C1-6alkil, C1-6alkoksi, -C(=O)-O- C1-6alkil, C2-4alkenil, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil, cijanoC1-4alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može po izboru biti supstituiran s jednom ili dvije hidroksilne skupine, -NR4R5, C1-6alkil supstituiran s -O-C(=O)- C1-6alkil, C1-6alkil supstituiran s -NR4R5, -C(=O)-NR4R5, -C(=O)-C1-6alkil-NR4R5, C1-6alkil supstituiran s -C(=O)-NR4R5, -S(=O)2-C1-6alkil, -S(=O)2haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkil, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkil, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -NR12-S(=O)2-NR14R15, R6, C1-6alkil supstituiran s R6, -C(=O)-R6, C1-6alkil supstituiran s -C(=O)-R6, hidroksiC1-6alkil supstituiran s R6, C1-6alkil supstituiran s -Si(CH3)3, C1-6alkil supstituiran s -P(=O)(OH)2 ili C1-6alkil supstituiran s -P(=O)(OC1-6alkil)2;
R3 predstavlja hidroksiC1-6alkil, hidroksihaloC1-6alkil, haloC1-6alkil, C1-6alkil supstituiran s R9, C1-6alkil supstituiran s -NR10R11, C2-6alkinil supstituiran s R9, ili C2-6alkinil;
R4 i R5 svaki neovisno predstavljaju vodik, C1-6alkil, C1-6alkil supstituiran s -NR14R15, hidroksiC1-6alkil, haloC1-6alkil, hidroksihaloC1-6alkil, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može po izboru biti supstituiran s jednom ili dvije hidroksilne skupine, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, -C(=O)-NR14R15, -C(=O)-O- C1-6alkil, -C(=O)-R13, C1-6alkil supstituiran s -S(=O)2-C1-6alkil, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkil, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -NH- S(=O)2-NR14R15, R13 ili C1-6alkil supstituiran s R13;
R6 predstavlja C3-8cikloalkil, C3-8cikloalkenil, fenil, 4-člani do 7-člani monociklički heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S; navedeni C3-8cikloalkil, C3-8cikloalkenil, fenil, 4-člani do 7-člani monociklički heterociklil, po izboru je svaki neovisno supstituiran s 1, 2, 3, 4 ili 5 supstituenata, svaki supstituent je neovisno odabran iz niza koji čine cijano, C1-6alkil, cijanoC1-6alkil, hidroksil, karboksil, hidroksiC1-6alkil, halogen, haloC1-6alkil, hidroksihaloC1-6alkil, C1-6alkoksi, C1-6alkoksiC1-6alkil, C1-6alkil-O-C(=O)-, -NR14R15, -C(=O)-NR14R15, C1-6alkil supstituiran s -NR14R15, C1-6alkil supstituiran s -C(=O)-NR14R15, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkil, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkil, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkil ili C1-6alkil supstituiran s -NH-S(=O)2-NR14R15;
R9 predstavlja C3-6cikloalkil, 3-člani zasićeni heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S, ili 5-člani ili 6-člani zasićeni ili aromatski heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S, navedeni 5-člani ili 6-člani zasićeni ili aromatski heterociklil svaki po izboru i svaki je neovisno supstituiran s 1, 2, 3, 4 ili 5 supstituenata, svaki supstituent je neovisno odabran iz niza koji čine =O, C1-4alkil, hidroksil, karboksil, hidroksiC1-4alkil, cijano, cijanoC1-4alkil, C1-4alkil-O-C(=O)-, C1-4alkil supstituiran s C1-4alkil-O-C(=O)-, C1-4alkil-C(=O)-, C1-4alkoksiC1-4alkil pri čemu svaki C1-4alkil može po izboru biti supstituiran s jednom ili dvije hidroksilne skupine, halogenom, haloC1-4alkil, hidroksihaloC1-4alkil, -NR14R15, -C(=O)-NR14R15, C1-4alkil supstituiran s -NR14R15, C1-4alkil supstituiran s -C(=O)-NR14R15, C1-4alkoksi, -S(=O)2-C1-4alkil, -S(=O)2-haloC1-4alkil, -S(=O)2-NR14R15, C1-4alkil supstituiran s -S(=O)2-NR14R15, C1-4alkil supstituiran s -NH-S(=O)2-C1-4alkil, C1-4alkil supstituiran s -NH-S(=O)2-haloC1-4alkil, C1-4alkil supstituiran s -NH-S(=O)2-NR14R15, R13, -C(=O)-R13, C1-4alkil supstituiran s R13, fenil po izboru supstituiran s R16, fenilC1-6alkil pri čemu je fenil po izboru supstituiran s R16, 5-člani ili 6-člani aromatski monociklički heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S pri čemu je navedeni heterociklil po izboru supstituiran s R16;
R10 i R11 svaki neovisno predstavljaju vodik, karboksil, C1-6alkil, cijanoC1-6alkil, C1-6alkil supstituiran s -NR14R15, C1-6alkil supstituiran s -C(=O)-NR14R15, haloC1-6alkil, hidroksiC1-6alkil, hidroksihaloC1-6alkil, C1-6alkoksi, C1-6alkoksiC1-6alkil pri čemu svaki C1-6alkil može po izboru biti supstituiran s jednom ili dvije hidroksilne skupine, R6, C1-6alkil supstituiran s R6, -C(=O)-R6, -C(=O)-C1-6alkil, -C(=O)-hidroksiC1-6alkil, -C(=O)-haloC1-6alkil,-C(=O)-hidroksihaloC1-6alkil, C1-6alkil supstituiran s -Si(CH3)3, -S(=O)2-C1-6alkil, -S(=O)2-haloC1-6alkil, -S(=O)2-NR14R15, C1-6alkil supstituiran s -S(=O)2-C1-6alkil, C1-6alkil supstituiran s -S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s -S(=O)2-NR14R15, C1-6alkil supstituiran s -NH-S(=O)2-C1-6alkil, C1-6alkil supstituiran s -NH-S(=O)2-haloC1-6alkil, C1-6alkil supstituiran s karboksilom, ili C1-6alkil supstituiran s -NH-S(=O)2-NR14R15;
R12 predstavlja vodik ili C1-4alkil po izboru supstituiran s C1-4alkoksi;
R13 predstavlja C3-8cikloalkil ili zasićeni 4-člani do 6-člani monociklički heterociklil koji sadržava barem jedan heteroatom koji je odabran od N, O ili S, pri čemu je navedeni C3-8cikloalkil ili monociklički heterociklil po izboru supstituiran s 1, 2 ili 3 supstituenata koji su svaki neovisno odabrani iz niza koji čine halogen, hidroksil, C1-6alkil, haloC1-6alkil, =O, cijano, -C(=O)-C1-6alkil, C1-6alkoksi, ili -NR14R15;
R14 i R15 svaki neovisno predstavljaju vodik, ili haloC1-4alkil, ili C1-4alkil po izboru supstituiran sa supstituentom odabranim iz niza koji čine hidroksil, C1-4alkoksi, amino ili mono-ili di(C1-4alkil)amino;
R16 predstavlja hidroksil, halogen, cijano, C1-4alkil, C1-4alkoksi, -NR14R15 ili -C(=O)NR14R15;
n neovisno predstavlja cijeli broj jednak 2, 3 ili 4;
njegov N-oksid, njegova farmaceutski prihvatljiva sol ili njegov solvat.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je D po izboru supstituiran pirazolil.
3. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time što R1 predstavlja C1-6alkil.
4. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time što R3 predstavlja hidroksiC1-6alkil, haloC1-6alkil ili C1-6alkil supstituiran s R9.
5. Spoj prema bilo kojem od prethodnih patentnih zahtjeva, naznačen time što n je 2 ili 4.
6. Spoj prema patentnom zahtjevu 1, naznačen time što W je -N(R3)-, D je fenil ili aromatski 5-člani ili 6-člani monociklički heterociklil, pri čemu navedeni fenil ili heterociklil može po izboru biti supstituiran s jednom ili više (npr. 1, 2 ili 3) skupina R1; n je 2, 3 ili 4; R2 je C1-4alkoksi ili halo; R3 je hidroksiC1-6alkil, haloC1-6alkil, C1-6alkil supstituiran s - NR10R11, ili C1-6alkil supstituiran s R9; R10 i R11 svaki neovisno predstavljaju vodik ili C1-6alkil.
7. Spoj prema patentnom zahtjevu 6, naznačen time što je D fenil ili po izboru supstituiran pirazolil.
8. Spoj prema bilo kojem od patentnih zahtjeva 1 do 7 ili njegova farmaceutski prihvatljiva sol ili solvat.
9. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8, naznačen time što je za uporabu u terapiji.
10. Spoj prema bilo kojem od patentnih zahtjeva 1 do 8 za:
(i) uporabu za profilaksu ili liječenje raka posredovanog s FGFR kinazom; ili
(ii) uporabu za profilaksu ili liječenje raka; ili
(iii) uporabu za liječenje raka pri čemu rak je odabran od raka prostate, raka mokraćnog mjehura, raka pluća kao što je NSCLC, raka dojke, raka želuca, i raka jetre; ili.
(iv) uporabu za liječenje raka pri čemu rak je odabran od multiplog mijeloma, mijeloproliferativnih poremećaja, raka endometrija, raka prostate, raka mokraćnog mjehura, raka pluća, raka jajnika, raka dojke, raka želuca, kolorektalnog karcinoma, i oralnog karcinoma skvamoznih stanica; ili
(v) uporabu za liječenje raka pri čemu rak je odabran od raka pluća, naročito od NSCLC, karcinoma skvamoznih stanica, karcinoma jetre, raka bubrega, raka dojke, raka debelog crijeva, kolorektalnog karcinoma, raka prostate; ili
(vi) uporabu za liječenje raka pri čemu je rak multipli mijelom; ili
(vii) uporabu za liječenje raka pri čemu je rak multipli mijelom pozitivan na translokaciju t(4;14); ili
(viii) uporabu za liječenje raka pri čemu rak je rak mokraćnog mjehura; ili
(ix) uporabu za liječenje raka pri čemu rak je rak mokraćnog mjehura s FGFR3 kromosomskom translokacijom; ili
(x) uporabu za liječenje raka pri čemu rak je rak mokraćnog mjehura s FGFR3 točkastom mutacijom; ili
(xi) uporabu za liječenje raka pri čemu rak je tumor s mutantom FGFR1, FGFR2, FGFR3 ili FGFR4; ili
(xii) uporabu za liječenje raka pri čemu rak je tumor s pojačanom funkcijom mutanta FGFR2 ili FGFR3; ili
(xiii) uporabu za liječenje raka pri čemu rak je tumor s prekomjernom ekspresijom FGFR1; ili
(xiv) uporabu za liječenje raka pri čemu se navedeni spoj koristi u kombinaciji s jednim ili više sredstava protiv raka; ili
(xv) uporabu za liječenje raka pri čemu se navedeni spoj koristi u kombinaciji s jednim ili više sredstava protiv raka i pri čemu jedno ili više sredstava protiv raka sadrži inhibitor kinaze.
11. Farmaceutski pripravak, naznačen time što sadrži spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 8.
12. Kombinacija spoja s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 8 s jednim ili više sredstava protiv raka.
13. Proizvod, naznačen time što kao prvi aktivni sastojak sadrži spoj s formulom (I) prema bilo kojem od patentnih zahtjeva 1 do 8 i kao daljnji aktivni sastojak jedno ili više sredstava protiv raka, kao kombinirani pripravak za istovremenu, odvojenu ili uzastopnu upotrebu za liječenje oboljelih od raka.
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PCT/GB2013/051427 WO2013179033A1 (en) | 2012-05-30 | 2013-05-30 | Pteridines as fgfr inhibitors |
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2012
- 2012-05-30 GB GBGB1209613.7A patent/GB201209613D0/en not_active Ceased
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2013
- 2013-05-30 HU HUE13731850A patent/HUE045663T2/hu unknown
- 2013-05-30 RU RU2014153050A patent/RU2702906C2/ru active
- 2013-05-30 EP EP13731850.7A patent/EP2855480B1/en active Active
- 2013-05-30 JP JP2015514587A patent/JP6363068B2/ja active Active
- 2013-05-30 DK DK13731850.7T patent/DK2855480T3/da active
- 2013-05-30 ES ES13731850T patent/ES2739348T3/es active Active
- 2013-05-30 SI SI201331519T patent/SI2855480T1/sl unknown
- 2013-05-30 BR BR112014029709-6A patent/BR112014029709B1/pt active IP Right Grant
- 2013-05-30 CA CA2874967A patent/CA2874967C/en active Active
- 2013-05-30 AU AU2013269316A patent/AU2013269316C1/en active Active
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- 2013-05-30 LT LTEP13731850.7T patent/LT2855480T/lt unknown
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JP6363068B2 (ja) | 2018-07-25 |
BR112014029709A2 (pt) | 2017-06-27 |
JP2015518039A (ja) | 2015-06-25 |
GB201209613D0 (en) | 2012-07-11 |
US9447098B2 (en) | 2016-09-20 |
HUE045663T2 (hu) | 2020-01-28 |
MX359418B (es) | 2018-09-27 |
US20170000796A1 (en) | 2017-01-05 |
CA2874967A1 (en) | 2013-12-05 |
AU2013269316B2 (en) | 2017-10-19 |
CN104507944A (zh) | 2015-04-08 |
EP2855480B1 (en) | 2019-06-26 |
EP2855480A1 (en) | 2015-04-08 |
KR20150016595A (ko) | 2015-02-12 |
AU2013269316C1 (en) | 2018-04-12 |
RU2702906C2 (ru) | 2019-10-14 |
AU2013269316A1 (en) | 2014-10-30 |
MX2014014110A (es) | 2015-06-17 |
US10272087B2 (en) | 2019-04-30 |
DK2855480T3 (da) | 2019-07-22 |
IN2014MN02069A (hr) | 2015-08-21 |
BR112014029709B1 (pt) | 2022-03-22 |
RU2014153050A (ru) | 2016-07-20 |
CN104507944B (zh) | 2017-04-12 |
ES2739348T3 (es) | 2020-01-30 |
SI2855480T1 (sl) | 2019-09-30 |
WO2013179033A1 (en) | 2013-12-05 |
CA2874967C (en) | 2021-11-09 |
US20150291589A1 (en) | 2015-10-15 |
LT2855480T (lt) | 2019-08-12 |
KR102149759B1 (ko) | 2020-08-31 |
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