HRP20171093T1 - 5-supstituirani derivati kinazolina i sastavi koji ih sadrže i metode u kojima se koriste - Google Patents
5-supstituirani derivati kinazolina i sastavi koji ih sadrže i metode u kojima se koriste Download PDFInfo
- Publication number
- HRP20171093T1 HRP20171093T1 HRP20171093TT HRP20171093T HRP20171093T1 HR P20171093 T1 HRP20171093 T1 HR P20171093T1 HR P20171093T T HRP20171093T T HR P20171093TT HR P20171093 T HRP20171093 T HR P20171093T HR P20171093 T1 HRP20171093 T1 HR P20171093T1
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- Prior art keywords
- alkyl
- optionally substituted
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- -1 5-substituted quinazolinone Chemical class 0.000 title 1
- 239000002246 antineoplastic agent Substances 0.000 title 1
- 125000001475 halogen functional group Chemical group 0.000 claims 18
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 17
- 239000000126 substance Substances 0.000 claims 14
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 5
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 208000003174 Brain Neoplasms Diseases 0.000 claims 3
- 206010033128 Ovarian cancer Diseases 0.000 claims 3
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 3
- 206010039491 Sarcoma Diseases 0.000 claims 3
- 210000000941 bile Anatomy 0.000 claims 3
- 210000000988 bone and bone Anatomy 0.000 claims 3
- 210000004556 brain Anatomy 0.000 claims 3
- 210000001072 colon Anatomy 0.000 claims 3
- 208000029742 colonic neoplasm Diseases 0.000 claims 3
- 201000010536 head and neck cancer Diseases 0.000 claims 3
- 208000014829 head and neck neoplasm Diseases 0.000 claims 3
- 210000000867 larynx Anatomy 0.000 claims 3
- 210000004185 liver Anatomy 0.000 claims 3
- 210000004072 lung Anatomy 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 210000001672 ovary Anatomy 0.000 claims 3
- 210000000496 pancreas Anatomy 0.000 claims 3
- 210000002307 prostate Anatomy 0.000 claims 3
- 201000001514 prostate carcinoma Diseases 0.000 claims 3
- 210000000664 rectum Anatomy 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000004463 Follicular Adenocarcinoma Diseases 0.000 claims 1
- 208000007766 Kaposi sarcoma Diseases 0.000 claims 1
- 208000018142 Leiomyosarcoma Diseases 0.000 claims 1
- 206010061269 Malignant peritoneal neoplasm Diseases 0.000 claims 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 claims 1
- 206010033701 Papillary thyroid cancer Diseases 0.000 claims 1
- 206010038019 Rectal adenocarcinoma Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 201000010989 colorectal carcinoma Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims 1
- 230000001394 metastastic effect Effects 0.000 claims 1
- 208000021039 metastatic melanoma Diseases 0.000 claims 1
- 206010061289 metastatic neoplasm Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 230000001254 nonsecretory effect Effects 0.000 claims 1
- 201000005163 papillary serous adenocarcinoma Diseases 0.000 claims 1
- 201000002524 peritoneal carcinoma Diseases 0.000 claims 1
- 201000001281 rectum adenocarcinoma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 claims 1
- 208000030045 thyroid gland papillary carcinoma Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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Claims (14)
1. Tvar formule (II)
[image]
Ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer za uporabu u metodi za liječenje, zbrinjavanje ili sprječavanje raka kože, pluća, jajnika, prostate, debelog crijeva, rektuma, mozga, glave i vrata, grkljana, gušterače, kostiju, jetre ili žuči, pri čemu:
R4 je: vodik; halo; -(CH2)nOH; (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo; ili (C1-C6)alkoksi, opcionalno supstituiran s jednim ili više halo;
R5 je: vodik; -(CH2)nOH; fenil; -O-(C1-C6)alkil; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo;
R6 je: vodik; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo; i
n je 0, 1 ili 2.
2. Tvar za uporabu u skladu s patentnim zahtjevom 1, ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer,
gdje je R4 metil ili metoksi; ili
gdje je R4 F ili Cl; ili
gdje je R4 –CF3.
[image]
3. Tvar za uporabu iz patentnog zahtjeva 1, koja je:
[image]
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer.
4. Tvar formule (III):
[image]
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer za uporabu u metodi za liječenje, zbrinjavanje ili sprječavanje raka kože, pluća, jajnika, prostate, debelog crijeva, rektuma, mozga, glave i vrata, grkljana, gušterače, kostiju, jetre ili žuči, pri čemu:
Rd je:
vodik;
(C1-C6)alkil, opcionalno supstituiran s jednim ili više halo;
-C(O)-(C1-C8)alkil, pri čemu je alkil opcionalno supstituiran s jednim ili više halo;
-C(O)-(CH2)n-(C3-C10-cikloalkil);
-C(O)-(CH2)n-NReRf, pri čemu su Re i Rf svaki nezavisno:
vodik;
(C1-C6)alkil, opcionalno supstituiran s jednim ili više halo; ili
(C1-C6)alkoksi, opcionalno supstituiran s jednim ili više halo; ili
-C(O)-(CH2)n-O-(C1-C6)alkil.
R7 je: vodik; -(CH2)nOH; fenil; -O-(C1-C6)alkil; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo;
R8 je: vodik; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo; i
n je 0, 1 ili 2.
5. Tvar za uporabu u skladu s patentnim zahtjevom 4, ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer,
gdje je R7 metil; ili
gdje je Rd -C(O)-(C1-C6)alkil; ili
gdje je Rd -C(O)-CH2-O-(C1-C6)alkil.
6. Tvar za uporabu u skladu s patentnim zahtjevom 4, koja je:
[image]
[image]
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer.
[image]
7. Tvar za uporabu u skladu s patentnim zahtjevom 6, koja je:
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer.
8. Tvar formule (IV):
[image]
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer za uporabu u metodi za liječenje, zbrinjavanje ili sprječavanje raka kože, pluća, jajnika, prostate, debelog crijeva, rektuma, mozga, glave i vrata, grkljana, gušterače, kostiju, jetre ili žuči, pri čemu:
Rg je:
-(CH2)n-(6 do 10 člani aril);
-C(O)-(CH2)n-(6 do 10 člani aril) ili -C(O)-(CH2)n-(6 do 10 člani heteroaril), pri čemu su aril i heteroaril opcionalno supstituirani s jednim ili više od: halo; -SCF3; (C1-C6)alkilom, koji je sam opcionalno supstituiran s jednim ili više halo; ili (C1-C6)alkoksi, koji je sam opcionalno supstituiran s jednim ili više halo;
-C(O)-(CH2)n-NHRh, pri čemu je Rh:
6 do 10 člani aril, opcionalno supstituirani s jednim ili više od: halo; (C1-C6)alkilom, koji je sam opcionalno supstituiran s jednim ili više halo; ili (C1-C6)alkoksi, koji je sam opcionalno supstituiran s jednim ili više halo; ili
-C(O)-(CH2)n-O-(CH2)n-(6 do 10 člani aril);
R9 je: vodik; -(CH2)nOH; fenil; -O-(C1-C6)alkil; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo;
R10 je: vodik; ili (C1-C6)alkil, opcionalno supstituiran s jednim ili više halo; i
n je 0, 1 ili 2.
9. Tvar za uporabu u skladu s patentnim zahtjevom 8,
gdje je R9 metil; ili
gdje je Rg -C(O)-fenil, -C(O)-CH2-fenil, ili -C(O)-NH-fenil; gdje je fenil opcionalno supstituiran s jednim ili više od metila, -CF3, ili halogena.
10. Tvar za uporabu u skladu s patentnim zahtjevom 8, koja je:
[image]
[image]
ili njena farmaceutski prihvatljiva sol, solvat ili njen stereoizomer.
11. Tvar za uporabu iz bilo kojeg od patentnih zahtjeva 1-10, pri čemu je rak kože melanom.
12. Tvar za uporabu iz bilo kojeg od patentnih zahtjeva 1-10, pri čemu je rak rektalni adenokarcinom, neoperabilni kolorektalni karcinom, metastatski hepatocelularni karcinom, peritonealni karcinom, papilarni serozni karcinom, nesekretabilni hepatocelularni karcinom, papilarni tiroidni karcinom, folikularni tiroidni karcinom ili medularni tiroidni karcinom.
13. Tvar za uporabu iz patentnog zahtjeva 11, pri čemu je melanom metastatski melanom.
14. Tvar za uporabu iz bilo kojeg od patentnih zahtjeva 1-10, pri čemu je rak Kaposijev sarkom, ginekološki sarkom, sarkom mekog tkiva, operirani visokorizični sarkom mekog tkiva ili lejomiosarkom.
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HRP20171093TT HRP20171093T1 (hr) | 2006-09-26 | 2017-07-17 | 5-supstituirani derivati kinazolina i sastavi koji ih sadrže i metode u kojima se koriste |
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- 2017-04-19 JP JP2017082496A patent/JP2017165744A/ja not_active Ceased
- 2017-07-07 US US15/644,119 patent/US20170369471A1/en not_active Abandoned
- 2017-07-17 HR HRP20171093TT patent/HRP20171093T1/hr unknown
- 2017-07-18 HR HRP20171106TT patent/HRP20171106T1/hr unknown
- 2017-07-20 CY CY20171100778T patent/CY1119248T1/el unknown
- 2017-08-02 CY CY20171100831T patent/CY1119176T1/el unknown
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