HRP20121006T1 - Supstituirani benzimidazoli za lijeäśenje astrocitoma - Google Patents
Supstituirani benzimidazoli za lijeäśenje astrocitoma Download PDFInfo
- Publication number
- HRP20121006T1 HRP20121006T1 HRP20121006AT HRP20121006T HRP20121006T1 HR P20121006 T1 HRP20121006 T1 HR P20121006T1 HR P20121006A T HRP20121006A T HR P20121006AT HR P20121006 T HRP20121006 T HR P20121006T HR P20121006 T1 HRP20121006 T1 HR P20121006T1
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- Croatia
- Prior art keywords
- alkyl
- halo
- formula
- alkoxy
- grade
- Prior art date
Links
- 206010003571 Astrocytoma Diseases 0.000 title claims 18
- 150000001556 benzimidazoles Chemical class 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 125000001475 halogen functional group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003785 benzimidazolyl group Chemical class N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
- 208000005017 glioblastoma Diseases 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- LELOWRISYMNNSU-UHFFFAOYSA-N Hydrocyanic acid Natural products N#C LELOWRISYMNNSU-UHFFFAOYSA-N 0.000 claims 2
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 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
- A61K31/4439—Non 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (9)
1. Derivat benzimidazola, naznačen time, da ima formulu (I):
[image]
gdje
svaki R’ je neovisno odabran od sljedećih: hidroksi, halo, C1-6 alkil, C1-6 alkoksi,
(C1-6 alkil)sulfanil, (C1-6 alkil)sulfonil, cikloalkil, heterocikloalkil, fenil i heteroaril;
R2 je C1-6 alkil ili halo(C1-6 alkil);
svaki R3 je neovisno odabran od halo, C1-6 alkil i C1-6 alkoksi;
svaki R4 je neovisno odabran od sljedećih: hidroksi, C1-6 alkil, C1-6 alkoksi, halo, karboksil, (C1-6 alkoksi)karbonil, aminokarbonil, C1-6 alkilaminokarbonil, karbonitril, cikloalkil, heterocikloalkil, heterocikloalkilkarbonil, fenil i heteroaril;
pri čemu R1, R2, R3 i R4 mogu biti opcijski supstituirani s jednim ili više supstituenata neovisno odabranih od sljedećih: hidroksi, halo, C1-6 alkil, halo(C1-6 alkil), C1-6 alkoksi i halo(C1-6 alkoksi);
a je 1, 2, 3, 4 ili 5;
b je 0, 1, 2 ili 3; i
c je 1 ili 2;
ili njegov tautomer ili stereoizomer ili farmaceutski prihvatljiva sol spoja,
tautomera ili stereoizomera,
te da je za uporabu u postupku liječenja astrocitoma.
2. Derivat benzimidazola prema zahtjevu 1, naznačen time, da su astrocitomi odabrani od astrocitoma stupnja I, stupnja II, stupnja III ili stupnja IV.
3. Derivat benzimidazola prema zahtjevu 1, naznačen time, da spoj formule (I) je
4-metil-3-[[4-(3-piridinil)-2-pirimidinil]amino]-N-[5-(4-metil-1H-imidazol-1-il)-3-(trifluorometil)fenil]benzamid formule (II):
[image]
ili tautomer spoja formule (II) ili farmaceutski prihvatljiva sol tautomera koja ima formulu (III):
[image]
4. Uporaba spoja formule (I):
[image]
naznačena time, da
svaki R’ je neovisno odabran od sljedećih: hidroksi, halo, C1-6 alkil, C1-6 alkoksi, (C1-6 alkil)sulfanil, (C1-6 alkil)sulfonil, cikloalkil, heterocikloalkil, fenil i heteroaril;
R2 je C1-6 alkil ili halo(C1-6 alkil);
svaki R3 je neovisno odabran od halo, C1-6 alkil i C1-6 alkoksi;
svaki R4 je neovisno odabran od sljedećih: hidroksi, C1-6 alkil, C1-6 alkoksi, halo, karboksil, (C1-6 alkoksi)karbonil, aminokarbonil, C1-6 alkilaminokarbonil, karbonitril, cikloalkil, heterocikloalkil, heterocikloalkilkarbonil, fenil i heteroaril;
gdje R1, R2, R3 i R4 mogu biti opcijski supstituirani s jednim ili više supstituenata neovisno odabranih od sljedećih: hidroksi, halo, C1-6 alkil, halo(C1-6 alkil), C1-6 alkoksi i halo(C1-6 alkoksi);
a je 1, 2, 3, 4 ili 5;
b je 0, 1, 2 ili 3; i
c je 1 ili 2;
ili njegov tautomer ili stereoizomer ili farmaceutski prihvatljiva sol spoja, tautomera ili stereoizomera, koja je za proizvodnju farmaceutskog sastava za liječenje astrocitoma.
5. Uporaba prema zahtjevu 4, naznačena time, da su astrocitomi odabrani od astrocitoma stupnja I, stupnja II, stupnja III ili stupnja IV.
6. Uporaba spoja formule (II):
[image]
ili tautomera spoja formule (II) ili farmaceutski prihvatljive soli tautomera koja ima formulu (III):
[image]
ili njegove farmaceutski prihvatljive soli, naznačena time, da je za proizvodnju farmaceutskog sastava za liječenje astrocitoma.
7. Uporaba prema zahtjevu 6, naznačena time, da su spomenuti astrocitomi odabrani od astrocitoma stupnja I, stupnja II, stupnja III ili stupnja IV.
8. Spoj formule (II):
[image]
ili tautomer spoja formule (II) ili farmaceutski prihvatljiva sol tautomera koja ima formulu (III):
[image]
naznačen time, da se upotrebljava u postupku liječenja sisavaca, uključujući ljude, koji boluju od astrocitoma.
9. Farmaceutski preparat, naznačen time, da je za liječenje astrocitoma, a sadrži spoj formule (II):
[image]
ili tautomer spoja formule (II) ili farmaceutski prihvatljivu sol tautomera koja ima formulu (III):
[image]
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14811709P | 2009-01-29 | 2009-01-29 | |
PCT/US2010/022332 WO2010088335A1 (en) | 2009-01-29 | 2010-01-28 | Substituted benzimidazoles for the treatment of astrocytomas |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20121006T1 true HRP20121006T1 (hr) | 2013-01-31 |
Family
ID=42008468
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20121006AT HRP20121006T1 (hr) | 2009-01-29 | 2012-12-06 | Supstituirani benzimidazoli za lijeäśenje astrocitoma |
Country Status (11)
Country | Link |
---|---|
US (1) | US20110281917A1 (hr) |
EP (1) | EP2391366B1 (hr) |
JP (1) | JP2012516345A (hr) |
DK (1) | DK2391366T3 (hr) |
ES (1) | ES2396023T3 (hr) |
HR (1) | HRP20121006T1 (hr) |
PL (1) | PL2391366T3 (hr) |
PT (1) | PT2391366E (hr) |
SI (1) | SI2391366T1 (hr) |
TW (1) | TW201031406A (hr) |
WO (1) | WO2010088335A1 (hr) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SG11202107080VA (en) | 2019-01-11 | 2021-07-29 | Naegis Pharmaceuticals Inc | Leukotriene synthesis inhibitors |
KR102085692B1 (ko) * | 2019-08-13 | 2020-03-06 | 한양대학교 에리카산학협력단 | Flt3 저해 활성을 갖는 신규한 이미다졸 유도체 및 이의 용도 |
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-
2010
- 2010-01-28 WO PCT/US2010/022332 patent/WO2010088335A1/en active Application Filing
- 2010-01-28 EP EP10703564A patent/EP2391366B1/en not_active Not-in-force
- 2010-01-28 JP JP2011548278A patent/JP2012516345A/ja not_active Withdrawn
- 2010-01-28 DK DK10703564.4T patent/DK2391366T3/da active
- 2010-01-28 TW TW099102430A patent/TW201031406A/zh unknown
- 2010-01-28 SI SI201030103T patent/SI2391366T1/sl unknown
- 2010-01-28 ES ES10703564T patent/ES2396023T3/es active Active
- 2010-01-28 PL PL10703564T patent/PL2391366T3/pl unknown
- 2010-01-28 US US13/146,675 patent/US20110281917A1/en not_active Abandoned
- 2010-01-28 PT PT107035644T patent/PT2391366E/pt unknown
-
2012
- 2012-12-06 HR HRP20121006AT patent/HRP20121006T1/hr unknown
Also Published As
Publication number | Publication date |
---|---|
WO2010088335A1 (en) | 2010-08-05 |
JP2012516345A (ja) | 2012-07-19 |
DK2391366T3 (da) | 2013-01-07 |
EP2391366A1 (en) | 2011-12-07 |
TW201031406A (en) | 2010-09-01 |
EP2391366B1 (en) | 2012-11-28 |
SI2391366T1 (sl) | 2013-01-31 |
PL2391366T3 (pl) | 2013-04-30 |
ES2396023T3 (es) | 2013-02-18 |
PT2391366E (pt) | 2013-02-05 |
US20110281917A1 (en) | 2011-11-17 |
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