HRP20160011T1 - Imidazopiridazini kao inhibitori akt kinaze - Google Patents
Imidazopiridazini kao inhibitori akt kinaze Download PDFInfo
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- HRP20160011T1 HRP20160011T1 HRP20160011TT HRP20160011T HRP20160011T1 HR P20160011 T1 HRP20160011 T1 HR P20160011T1 HR P20160011T T HRP20160011T T HR P20160011TT HR P20160011 T HRP20160011 T HR P20160011T HR P20160011 T1 HRP20160011 T1 HR P20160011T1
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- 150000005233 imidazopyridazines Chemical class 0.000 title 1
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 28
- 239000001257 hydrogen Substances 0.000 claims 28
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 15
- 150000002367 halogens Chemical class 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 14
- 101100240517 Caenorhabditis elegans nhr-11 gene Proteins 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 12
- 150000001204 N-oxides Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- -1 amino, methoxy, ethoxy, butoxy, pyridin-3-yl Chemical group 0.000 claims 5
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 239000013543 active substance Substances 0.000 claims 2
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 230000009826 neoplastic cell growth Effects 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- 239000000460 chlorine Substances 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 1
- 230000003211 malignant effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 125000004289 pyrazol-3-yl group Chemical group [H]N1N=C(*)C([H])=C1[H] 0.000 claims 1
- 230000009466 transformation Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Reproductive Health (AREA)
- Endocrinology (AREA)
- Pregnancy & Childbirth (AREA)
- Gynecology & Obstetrics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Cosmetics (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Claims (14)
1. Spoj s formulom (I)
[image]
naznačen time da
R1 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-6C-alkil), NHC(O)(1-6C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-6C-alkil, -S(O)2NR5R6 ili skupina odabrana od 1-6C-alkila, 1-6C-alkoksi, 3-7C-cikloalkila, arila, heteroarila, -(1-6C-alkil)-arila, -(1-6C-alkil)-heteroarila, -O-(3-7C-cikloalkil), -O-arila, -O-(3-7C-heterociklil), -O-heteroarila, -O-(1-6C-alkil)-heteroarila, -O-(1-6C-alkil)-(3-7C-heterociklil), -O-(1-6C-alkil)-arila, 2-6C-alkenila, 2-6C-alkinila,
pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži: hidroksi, halogen, 1-6C-alkil, 1-4C-haloalkil, 1-6C-alkoksi, -NR8R9, cijano, - C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-7C-cikloalkil, 3-7C-heterociklil, aril,
R2 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-6C-alkil), NHC(O)(1-6C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-6C-alkil, -S(O)2NR5R6 ili skupina odabrana iz skupa koji sadrži 1-6C-alkil, 1-6C-alkoksi, 3-7C-cikloalkil, aril, heteroaril, -(1-6C-alkil)-aril, -(1-6C-alkil)-heteroaril, -O-(3-7C-cikloalkil), -O-aril, -O-(3-7C-heterociklil), -O-heteroaril, -O-(1-6C-alkil)-heteroaril, -O-(1-6C-alkil)-(3-7C-heterociklil), -O-(1-6C-alkil)-aril, 2-6C-alkenil, 2-6C-alkinil,
pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži:
hidroksi, halogen, 1-6C-alkil, 1-4C-haloalkil, 1-6C-alkoksi, -NR8R9, cijano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-7C-heterociklil, aril,
R3 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-6C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-6C-alkil, -S(O)2NR5R6 ili skupina odabrana iz skupa koji sadrži 1-6C-alkil, 1-6C-alkoksi, 3-7C-cikloalkil, aril, heteroaril, -(1-6C-alkil)-aril, -(1-6C-alkil)-heteroaril, -O-(3-7C-cikloalkil), -O-aril, -O-(3-7C-heterociklil), -O-heteroaril, -O-(1-6C-alkil)-heteroaril, -O-(1-6C-alkil)-(3-7C-heterociklil), -O-(1-6C-alkil)-aril, NHC(O)(1-6C-alkil), 2-6C-alkenil, 2-6C-alkinil, pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži: hidroksi, halogen, 1-6C-alkil, 1-4C-haloalkil, 1-6C-alkoksi, -NR8R9, cijano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-7C-heterociklil, aril,
R4 je fenil koji je proizvoljno supstituiran jedan, dva ili tri puta, istovjetno ili različito, s atomom halogena;
R5 je vodik, 1-6C-alkil,
R6 je vodik, 1-6C-alkil,
R8 je vodik, 1-6C-alkil koji je proizvoljno supstituiran s hidroksi,
R9 je vodik, 1-6C-alkil,
R10 je vodik, 1-6C-alkil,
R11 je vodik, 1-6C-alkil,
X, Y je CH2;
n je 0, 1, 2;
ili N-oksid, sol, tautomer ili stereoizomer navedenog spoja, ili sol navedenog N-oksida, tautomera ili stereoizomera.
2. Spoj prema zahtjevu 1 naznačen time da
R1 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-3C-alkil), NHC(O)(1-6C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-3C-alkil, -S(O)2NR5R6 ili skupina odabrana iz skupa koji sadrži 1-3C-alkil, 1-3C-alkoksi, 3-6C-cikloalkil, aril, heteroaril, -(1-3C-alkil)-aril, -(1-3C-alkil)-heteroaril, -O-(3-6C-cikloalkil), -O-aril, -O-(3-6C-heterociklil), -O-heteroaril, -O-(1-3C-alkil)-heteroaril, -O-(1-3C-alkil)-(3-6C-heterociklil), -O-(1-3C-alkil)-aril, 2-3C-alkenil, 2-3C-alkinil,
pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži: hidroksi, halogen, 1-3C-alkil, 1-3C-haloalkil, 1-3C-alkoksi, -NR8R9, cijano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-6C-cikloalkil, 3-6C-heterociklil, aril,
R2 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-3C-alkil), NHC(O)(1-3C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-3C-alkil, -S(O)2NR5R6 ili skupina odabrana iz skupa koji sadrži 1-3C-alkil, 1-3C-alkoksi, 3-6C-cikloalkil, aril, heteroaril, -(1-3C-alkil)-aril, -(1-3C-alkil)-heteroaril, -O-(3-6C-cikloalkil), -O-aril, -O-(3-6C-heterociklil), -O-heteroaril, -O-(1-3C-alkil)-heteroaril, -O-(1-3C-alkil)-(3-6C-heterociklil), -O-(1-3C-alkil)-aril, 2-3C-alkenil, 2-3C-alkinil,
pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži: hidroksi, halogen, 1-3C-alkil, 1-3C-haloalkil, 1-3C-alkoksi, -NR8R9, cijano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-6C-heterociklil, aril,
R3 je vodik, hidroksi, NR5R6, halogen, cijano, CO(NR8R9), C(O)OR8, C(O)(1-3C-alkil), NHS(O)2R11, NHC(O)NHR11, -S(O)n-1-3C-alkil, -S(O)2NR5R6 ili skupina odabrana iz skupa koji sadrži 1-3C-alkil, 1-3C-alkoksi, 3-6C-cikloalkil, aril, heteroaril, -(1-3C-alkil)-aril, -(1-3C-alkil)-heteroaril, -O-(3-6C-cikloalkil), -O-aril, -O-(3-6C-heterociklil), -O-heteroaril, -O-(1-3C-alkil)-heteroaril, -O-(1-3C-alkil)-(3-6C-heterociklil), -O-(1-3C-alkil)-aril, NHC(O)(1-3C-alkil), 2-3C-alkenil, 2-3C-alkinil, pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži:
hidroksi, halogen, 1-3C-alkil, 1-3C-haloalkil, 1-3C-alkoksi, -NR8R9, cijano, -C(O)NR8R9, -C(O)OR10, -NHC(O)R11, -NHC(O)NHR11, -NHS(O)2R11, 3-6C-heterociklil, aril,
R4 je fenil koji je proizvoljno supstituiran jedan, dva ili tri puta, istovjetno ili različito, s atomom halogena;
R5 je vodik, 1-3C-alkil,
R6 je vodik, 1-3C-alkil,
R8 je vodik, 1-3C-alkil koji je proizvoljno supstituiran s hidroksi,
R9 je vodik, 1-3C-alkil,
R10 je vodik, 1-3C-alkil,
R11 je vodik, 1-3C-alkil,
X, Y je CH2;
n je 0, 1, 2;
ili N-oksid, sol, tautomer ili stereoizomer navedenog spoja, ili sol navedenog N-oksida, tautomera ili stereoizomera.
3. Spoj prema zahtjevu 1 naznačen time da
R1 je vodik, hidroksi, NR5R6, CO(NR8R9), C(O)OR8, NHC(O)(1-6C-alkil), ili skupina odabrana iz skupa koji sadrži 1-6C-alkil, 3-7C-cikloalkil, aril, heteroaril, 1-4C-alkoksi, pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim iz skupa koji sadrži: halogen, 1-6C-alkil, 1-6C-alkoksi, -C(O)OR10, 3-7-cikloalkil, aril,
R2 je vodik, 1-6C-alkil,
R3 je vodik, hidroksi, NR5R6, halogen ,CO(NR8R9), C(O)OR8, C(O)(1-6C-alkil), NHS(O)2R11, S(O)n-1-6C-alkil, ili skupina odabrana iz skupa koji sadrži 1-6C-alkil, 1-6C-alkoksi aril, NHC(O)(1-6C-alkil), 2-6C-alkenil, pri čemu je navedena skupina proizvoljno supstituirana, jednom ili više puta, istovjetno ili različito, sa supstituentom odabranim od: halogena, -C(O)OR10,
R4 je fenil,
R5 je vodik,
R6 je vodik,
R8 je vodik, 1-4C-alkil, koji je proizvoljno supstituiran s hidroksi,
R9 je vodik, 1-4C-alkil,
R10 je 1-4C-alkil,
R11 je 1-4C-alkil,
X, Y je CH2
n je 0, 1, 2;
ili N-oksid, sol, tautomer ili stereoizomer navedenog spoja, ili sol navedenog N-oksida, tautomera ili stereoizomera.
4. Spoj prema zahtjevu 1 naznačen time da
R1 je vodik, hidroksil, amino, metoksi, etoksi, butoksi, piridin-3-il, piridin-4-il, pirazol-3-il, 1-metil-pirazol-3-il, imidazol-2-il, metil, propil, -O-(CH2)-O-CH3, -O-CH2-fenil, -O-CH2-ciklopropil, -C(O)OCH3, -C(O)-NHCH3, -C(O)-NH2, 4-fluoro-fenil, -(CH2)2-C(O)OCH3, ciklopropil, -NH-C(O)CH3,
R2 je vodik, metil,
R3 je vodik, hidroksi, amino, metil, etil, metoksi, etoksi, -O-CH2-C(O)OCH3, -S-CH3, -SO2-CH3, brom, klor, trifluorometil, C(O)NH2, COOH,C(O)OCH3, C(O)OCH2CH3, C(O)NH2, C(O)NHCH3, C(O)N(CH3)2, C(O)NH(CH2)2-OH, -CH=CH2, 4-fluoro-fenil, NHC(O)CH3, NHC(O)CF3, NH-SO2-CH3, C(O)CH3,
R4 je fenil
X, Y je CH2
ili N-oksid, sol, tautomer ili stereoizomer navedenog spoja, ili sol navedenog N-oksida, tautomera ili stereoizomera.
5. Spoj prema zahtjevu 1 naznačen time da je spoj izabran iz skupa koji čine
[image]
[image]
6. Spoj prema zahtjevu 5 naznačen time da je spoj odabran iz skupa koji čine
[image]
[image]
7. Spoj prema zahtjevu 5 naznačen time da je odabran iz skupa koji čine
[image]
8. Postupak za proizvodnju spojeva opće formule (I) prema zahtjevu 1 reakcijom spoja opće formule (II)
[image]
naznačen time da
R1-R4 imaju značenje kao što je navedeno u zahtjevu 1 i
Rx, Ry su R6, ili zaštitna skupina,
pri čemu se transformacija u spoj s općom formulom (I) postiže uporabom prikladne reakcije deprotekcije.
9. Spoj prema zahtjevu 1 naznačen time da je za uporabu za liječenje bolesti.
10. Spoj za uporabu prema zahtjevu 9 naznačen time da bolest je benigna neoplazija ili maligna neoplazija.
11. Spoj prema zahtjevu 1-7 naznačen time da je za uporabu za liječenje raka dojke.
12. Farmaceutski pripravak naznačen time da sadrži barem jedan spoj s općom formulom (I) prema bilo kojem od zahtjeva 1 do 7, zajedno s barem jednim farmaceutski prihvatljivim dodatkom.
13. Farmaceutski pripravak naznačen time da sadrži prvu aktivnu tvar, koja je barem jedan spoj s općom formulom (I) prema bilo kojem od zahtjeva 1 do 7, te drugu aktivnu tvar, koja je barem jedno dodatno antikancerogeno sredstvo.
14. Pripravak prema zahtjevu 12 ili 13 naznačen time da je za uporabu za liječenje raka dojke.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161472732P | 2011-04-07 | 2011-04-07 | |
| PCT/EP2012/056300 WO2012136776A1 (en) | 2011-04-07 | 2012-04-05 | Imidazopyridazines as akt kinase inhibitors |
| EP12713963.2A EP2694510B1 (en) | 2011-04-07 | 2012-04-05 | Imidazopyridazines as akt kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20160011T1 true HRP20160011T1 (hr) | 2016-02-12 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20160011TT HRP20160011T1 (hr) | 2011-04-07 | 2016-01-05 | Imidazopiridazini kao inhibitori akt kinaze |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9029408B2 (en) | 2008-06-16 | 2015-05-12 | Gtx, Inc. | Compounds for treatment of cancer |
| KR20160079934A (ko) | 2008-06-16 | 2016-07-06 | 유니버시티 오브 테네시 리서치 파운데이션 | 암 치료용 화합물 |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
| WO2011109059A1 (en) | 2010-03-01 | 2011-09-09 | Gtx, Inc. | Compounds for treatment of cancer |
| CA2832374A1 (en) * | 2011-04-07 | 2012-10-11 | Bayer Intellectual Property Gmbh | Imidazopyridazines as akt kinase inhibitors |
| CA2860724A1 (en) * | 2012-01-10 | 2013-07-18 | Bayer Intellectual Property Gmbh | Substituted pyrazolopyrimidines as akt kinase inhibitors |
| CA2860723A1 (en) * | 2012-01-10 | 2013-07-18 | Bayer Intellectual Property Gmbh | Substituted imidazopyrazines as akt kinase inhibitors |
| PT2925299T (pt) * | 2012-11-30 | 2018-10-16 | Novartis Ag | Composição farmacêutica inovadora |
| KR102246652B1 (ko) * | 2013-03-05 | 2021-04-29 | 유니버시티 오브 테네시 리서치 파운데이션 | 암 치료용 화합물 |
| US20150352121A1 (en) * | 2013-03-12 | 2015-12-10 | Glaxosmithkline Llc | Combination |
| US20160045531A1 (en) * | 2013-03-14 | 2016-02-18 | Epizyme, Inc. | Combination therapy for treating cancer |
| JP2017503809A (ja) * | 2014-01-09 | 2017-02-02 | バイエル・ファルマ・アクティエンゲゼルシャフト | アミド置換イミダゾピリダジン |
| ES2896938T3 (es) | 2016-11-28 | 2022-02-28 | Bristol Myers Squibb Co | Inhibidores de GSK-3 |
| EP3453706A1 (en) | 2017-09-08 | 2019-03-13 | Basf Se | Pesticidal imidazole compounds |
Family Cites Families (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR0017037A (pt) | 1999-12-23 | 2003-06-10 | Nitromed Inc | Inibidores de ciclooxigenase-2 nitrosados e nitrosilados, composições e métodos de uso |
| US6908929B2 (en) | 2000-03-31 | 2005-06-21 | Ortho-Mcneil Pharmaceutical, Inc. | Phenyl-substituted imidazopyridines |
| WO2001083481A1 (fr) | 2000-04-27 | 2001-11-08 | Yamanouchi Pharmaceutical Co., Ltd. | Derives d'imidazopyridine |
| JP2006520796A (ja) | 2003-03-17 | 2006-09-14 | タケダ サン ディエゴ インコーポレイテッド | ヒストンデアセチラーゼインヒビター |
| US7579355B2 (en) | 2003-04-24 | 2009-08-25 | Merck & Co., Inc. | Inhibitors of Akt activity |
| EP1660500B1 (en) | 2003-07-30 | 2007-12-12 | Laboratorios S.A.L.V.A.T., S.A. | Substituted imidazopyrimidines for the prevention and treatment of cancer |
| CA2561311A1 (en) | 2004-04-09 | 2005-10-27 | Merck & Co., Inc. | Inhibitors of akt activity |
| US7544677B2 (en) | 2004-08-23 | 2009-06-09 | Merck & Co., Inc. | Inhibitors of Akt activity |
| JP2008510741A (ja) | 2004-08-24 | 2008-04-10 | ビーエーエスエフ ソシエタス・ヨーロピア | イオン液体を製造するための出発化合物としてのイミダゾリウム−メチルスルファイト |
| JP2008524339A (ja) | 2004-12-15 | 2008-07-10 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性のインヒビター |
| CA2609299A1 (en) | 2005-05-20 | 2006-11-23 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
| EP1898903B8 (en) | 2005-06-10 | 2013-05-15 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| PE20070978A1 (es) | 2006-02-14 | 2007-11-15 | Novartis Ag | COMPUESTOS HETEROCICLICOS COMO INHIBIDORES DE FOSFATIDILINOSITOL 3-QUINASAS (PI3Ks) |
| US7530313B2 (en) | 2006-05-12 | 2009-05-12 | Day & Zimmerman, Inc. | Self-destruct fuze delay mechanism |
| AR064010A1 (es) | 2006-12-06 | 2009-03-04 | Merck & Co Inc | Inhibidores de la actividad de la akt |
| BRPI0811065A2 (pt) * | 2007-06-08 | 2014-12-02 | Abbott Lab | Indazóis 5-heteroaril substituídos como inibidores de quinase |
| BRPI0815207A2 (pt) | 2007-08-14 | 2017-03-28 | Bayer Schering Pharma Ag | pirimidinas bicíclicas fundidas |
| EP2176259B1 (en) | 2007-08-14 | 2011-03-30 | Bayer Schering Pharma Aktiengesellschaft | Fused imidazoles for cancer treatment |
| WO2009086130A1 (en) | 2007-12-21 | 2009-07-09 | Wyeth | Imidazo [1,2-b] pyridazine compounds as modulators of liver x receptors |
| CA2726358A1 (en) | 2008-06-03 | 2009-12-10 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| CA2726317A1 (en) | 2008-06-03 | 2009-12-10 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| AR074072A1 (es) | 2008-11-11 | 2010-12-22 | Lilly Co Eli | Compuesto de imidazol -piperidin -pirrol-pirimidin-6-ona, composicion farmaceutica que lo comprende y su uso para preparar un medicamento util para tratar el glioblastoma multiforme |
| PA8854101A1 (es) | 2008-12-18 | 2010-07-27 | Ortho Mcneil Janssen Pharm | Derivados de imidazol bicíclicos sustituidos como moduladores de gamma secretasa |
| JP2012516847A (ja) | 2009-02-02 | 2012-07-26 | メルク・シャープ・エンド・ドーム・コーポレイション | Ａｋｔ活性の阻害剤 |
| KR20110114663A (ko) * | 2009-02-13 | 2011-10-19 | 바이엘 파마 악티엔게젤샤프트 | 융합된 피리미딘 |
| WO2010104933A1 (en) | 2009-03-11 | 2010-09-16 | Merck Sharp & Dohme Corp. | Inhibitors of akt activity |
| EP2413932A4 (en) | 2009-04-01 | 2012-09-19 | Merck Sharp & Dohme | INHIBITORS OF AKT ACTIVITY |
| AR076936A1 (es) | 2009-06-02 | 2011-07-20 | Vitae Pharmaceuticals Inc | Inhibidores de carbamato y urea de la 11 beta hidroxiesteroide deshidrogenasa 1 |
| WO2011033265A1 (en) * | 2009-09-18 | 2011-03-24 | Almac Discovery Limited | Pharmaceutical compounds |
| CA2804845A1 (en) | 2010-07-12 | 2012-01-19 | Stuart Ince | Substituted imidazo[1,2-a]pyrimidines and -pyridines |
| JP5926727B2 (ja) | 2010-07-28 | 2016-05-25 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾ［１，２−ｂ］ピリダジン |
| CA2832374A1 (en) * | 2011-04-07 | 2012-10-11 | Bayer Intellectual Property Gmbh | Imidazopyridazines as akt kinase inhibitors |
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