HRP20120490T1 - Spojevi za inhibiciju napredovanja mitoze - Google Patents
Spojevi za inhibiciju napredovanja mitoze Download PDFInfo
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- HRP20120490T1 HRP20120490T1 HRP20120490TT HRP20120490T HRP20120490T1 HR P20120490 T1 HRP20120490 T1 HR P20120490T1 HR P20120490T T HRP20120490T T HR P20120490TT HR P20120490 T HRP20120490 T HR P20120490T HR P20120490 T1 HRP20120490 T1 HR P20120490T1
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- Croatia
- Prior art keywords
- aliphatic
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- fluoroaliphatic
- compound according
- fluoro
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- 150000001875 compounds Chemical class 0.000 title claims abstract 19
- 230000002401 inhibitory effect Effects 0.000 title claims 2
- 230000008600 mitotic progression Effects 0.000 title 1
- 125000001931 aliphatic group Chemical group 0.000 claims abstract 14
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 10
- 125000005843 halogen group Chemical group 0.000 claims abstract 6
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 6
- 239000001257 hydrogen Substances 0.000 claims abstract 6
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 5
- 125000004433 nitrogen atom Chemical group N* 0.000 claims abstract 5
- 150000003839 salts Chemical class 0.000 claims abstract 5
- 125000001153 fluoro group Chemical group F* 0.000 claims abstract 4
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 3
- 125000001424 substituent group Chemical group 0.000 claims abstract 3
- 125000002947 alkylene group Chemical group 0.000 claims abstract 2
- -1 -OH Chemical group 0.000 claims 6
- 102000003989 Aurora kinases Human genes 0.000 claims 5
- 108090000433 Aurora kinases Proteins 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000002541 furyl group Chemical group 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- SRFVRJILPIASPG-UHFFFAOYSA-N 4-[[7-(2-fluoro-6-methoxyphenyl)-9-(1-methylpyrrol-2-yl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C=2N(C=CC=2)C)=C1 SRFVRJILPIASPG-UHFFFAOYSA-N 0.000 claims 1
- ZLHFILGSQDJULK-UHFFFAOYSA-N 4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5H-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 ZLHFILGSQDJULK-UHFFFAOYSA-N 0.000 claims 1
- NRJOLMQQQLDIPP-UHFFFAOYSA-N 4-[[9-ethynyl-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoic acid Chemical compound C1=C(C(O)=O)C(OC)=CC(NC=2N=C3C4=CC=C(C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)C#C)=C1 NRJOLMQQQLDIPP-UHFFFAOYSA-N 0.000 claims 1
- 102000004000 Aurora Kinase A Human genes 0.000 claims 1
- 108090000461 Aurora Kinase A Proteins 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000006519 CCH3 Chemical group 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 125000000219 ethylidene group Chemical group [H]C(=[*])C([H])([H])[H] 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- AIUYVPGHBMKGAC-UHFFFAOYSA-M sodium;4-[[9-chloro-7-(2-fluoro-6-methoxyphenyl)-5h-pyrimido[5,4-d][2]benzazepin-2-yl]amino]-2-methoxybenzoate Chemical compound [Na+].C1=C(C([O-])=O)C(OC)=CC(NC=2N=C3C4=CC=C(Cl)C=C4C(=NCC3=CN=2)C=2C(=CC=CC=2F)OC)=C1 AIUYVPGHBMKGAC-UHFFFAOYSA-M 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 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
- A61K31/505—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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Enzymes And Modification Thereof (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Spoj formule I ili njegova farmaceutski prihvatljiva sol u kojem Ra je izabran iz grupe koju čine C alifatik C fluoroalifatik R T R R i T R T je C alkilen lanac izborno supstituiran sa fluoro R je ili člani aril heteroaril ili heterociklil prsten izborno supstituiran sa jednim ili dva supstituenta nezavisno izabrana iz grupe koju čine halo C alifatik i C fluoroalifatik R je izabran iz grupe koju čine halo C C R CH CH R N R i OR R je vodikC alifatik C fluoroalifatik ili CH OCH ili aril heteroaril ili heterociklil grupa svakoR nezavisno je vodik ili alifatična aril heteroaril ili heterociklil grupa ili dva R na istom atomu dušika zajedno sa atomom dušika formiraju do člani heteroaril ili do člani heterociklil prsten koji ima pored atoma dušika heteroatoma u prstenu izabrana od N O i S R je vodik C alifatična C fluoroalifatična ili aril heteroaril ili heterociklil grupa iRb je izabran iz grupe koju čine fluoro kloro CH CF OH OCH OCF OCH CH i OCH CF Patent sadržijoš patentnih zahtjeva
Claims (15)
1. Spoj formule (I):
[image]
ili njegova farmaceutski prihvatljiva sol u kojem:
Ra je izabran iz grupe koju čine C1-3 alifatik, C1-3 fluoroalifatik, -R1, -T-R1, -R2 i -T-R2;
T je C1-3 alkilen lanac izborno supstituiran sa fluoro;
R1 je 5- ili 6-člani aril, heteroaril ili heterociklil prsten izborno supstituiran sa jednim ili dva supstituenta nezavisno izabrana iz grupe koju čine halo, C1-3 alifatik i C1-3 fluoroalifatik;
R2 je izabran iz grupe koju čine halo, -C≡C-R3, -CH=CH-R3, -N(R4)2 i -OR5;
R3 je vodik, C1-3 alifatik, C1-3 fluoroalifatik ili -CH2OCH3 ili aril, heteroaril, ili heterociklil grupa;
svako R4 nezavisno je vodik ili alifatična, aril, heteroaril ili heterociklil grupa; ili dva R4 na istom atomu dušika, zajedno sa atomom dušika formiraju 5- do 6-člani heteroaril ili 4- do 8-člani heterociklil prsten koji ima, pored atoma dušika, 0-2 heteroatoma u prstenu izabrana od N, O i S;
R5 je vodik, C1-3 alifatična, C1-3 fluoroalifatična ili aril, heteroaril ili heterociklil grupa; i
Rb je izabran iz grupe koju čine fluoro, kloro, -CH3, -CF3, -OH, -OCH3, -OCF3, -OCH2CH3 i -OCH2CF3.
2. Spoj prema patentnom zahtjevu 1, u kojem, Ra je halo, C1-3 alifatik, C1-3 fluoroalifatik, -OH, -O(C1-3 alifatik), -O(C1-3 fluoroalifatik) ili -C≡C-R3, -CH=CH-R3, pri čemu, R3 je vodik, C1-3 alifatik, C1-3 fluoroalifatik ili -CH2-OCH3;
ili Ra je fenil, furil, pirolidinil ili tienil prsten izborno supstituiran sa jednim ili dva supstituenta nezavisno izabrana iz grupe koju čine halo, C1-3 alifatik i C1-3 fluoroalifatik.
3. Spoj prema patentnom zahtjevu 2, u kojem je Ra izabran iz grupe koju čine kloro, fluoro, C1-3 alifatik, C1-3 fluoroalifatik, -OCH3, -OCF3, -C≡C-H, -C≡C-CH3, -C≡C-CH2OCH3, -CH=CH2, -CH=CHCH3, N-metilpirolidinil, tienil, metiltienil, furil, metilfuril, fenil, fluorofenil i tolil.
4. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je 4-{[9-etinil-7-(2-fluoro-6-metoksifenil)-5H-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoksibenzoeva kiselina ili njena farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je 4-{[7-(2-fluoro-6-metoksifenil)-9-(1-metil-1H-pirol-2-il)-5H-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoksibenzoeva kiselina ili njena farmaceutski prihvatljiva sol.
6. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je 4-{[9-kloro-7-(2-fluoro-6-metoksifenil)-5H-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoksibenzoeva kiselina ili njena farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time što, spoj je natrijev 4-{[9-kloro-7-(2-fluoro-6-metoksifenil)-5H-pirimido[5,4-d][2]benzazepin-2-il]amino}-2-metoksibenzoat.
8. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1-7.
9. Farmaceutska kompozicija prema patentnom zahtjevu 8, koja sadrži farmaceutski prihvatljiv nosač i koja izborno dodatno sadrži drugo terapeutsko sredstvo.
10. In vitro postupak za inhibiciju aktivnosti Aurora kinaze u stanici, koji sadrži dovođenje u kontakt stanice u kojoj je poželjna inhibicija Aurora kinaze sa spojem prema bilo kojem od patentnih zahtjeva 1-7.
11. Postupak prema patentnom zahtjevu 8, naznačen time što, Aurora kinaza je Aurora A kinaza.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-7 za upotrebu u liječenju poremećaja posredovanog preko Aurora kinaze.
13. Spoj prema patentnom zahtjevu 12, naznačen time što, poremećaj posredovan preko Aurora kinaze, je kancer.
14. Spoj prema patentnom zahtjevu 13, naznačen time što je kancer izabran iz grupe koju čine kolorektalni kancer, kancer jajnika, kancer dojke, kancer želudca, kancer prostate i kancer pankreasa.
15. Upotreba spoja prema bilo kojem od patentnih zahtjeva 1 do 7 u proizvodnji lijeka za liječenje kancera.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US85934006P | 2006-11-16 | 2006-11-16 | |
PCT/US2007/023948 WO2008063525A1 (en) | 2006-11-16 | 2007-11-14 | Compounds for inhibiting mitotic progression |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20120490T1 true HRP20120490T1 (hr) | 2012-07-31 |
Family
ID=39315133
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20120490TT HRP20120490T1 (hr) | 2006-11-16 | 2012-06-12 | Spojevi za inhibiciju napredovanja mitoze |
HRP20150047TT HRP20150047T1 (en) | 2006-11-16 | 2015-01-13 | Compound for inhibiting mitotic progression |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20150047TT HRP20150047T1 (en) | 2006-11-16 | 2015-01-13 | Compound for inhibiting mitotic progression |
Country Status (35)
Country | Link |
---|---|
US (6) | US8026246B2 (hr) |
EP (4) | EP2497773B1 (hr) |
JP (3) | JP5102839B2 (hr) |
KR (2) | KR101110458B1 (hr) |
CN (2) | CN103483343B (hr) |
AR (1) | AR064246A1 (hr) |
AT (1) | ATE556076T1 (hr) |
AU (1) | AU2007322046B2 (hr) |
BR (1) | BRPI0718803B8 (hr) |
CA (1) | CA2669680C (hr) |
CL (1) | CL2007003244A1 (hr) |
CR (3) | CR10782A (hr) |
CY (1) | CY1112828T1 (hr) |
DK (2) | DK2086981T3 (hr) |
EA (1) | EA015779B1 (hr) |
ES (3) | ES2384123T3 (hr) |
GE (1) | GEP20125459B (hr) |
HK (4) | HK1134672A1 (hr) |
HR (2) | HRP20120490T1 (hr) |
IL (1) | IL198690A0 (hr) |
MA (1) | MA30988B1 (hr) |
MX (3) | MX343391B (hr) |
MY (1) | MY153243A (hr) |
NO (1) | NO343338B1 (hr) |
NZ (3) | NZ577042A (hr) |
PH (1) | PH12012502057A1 (hr) |
PL (2) | PL2497772T3 (hr) |
PT (2) | PT2086981E (hr) |
RS (2) | RS53788B1 (hr) |
SG (2) | SG176443A1 (hr) |
SI (2) | SI2086981T1 (hr) |
TW (1) | TWI401255B (hr) |
UA (1) | UA94129C2 (hr) |
WO (1) | WO2008063525A1 (hr) |
ZA (1) | ZA200903279B (hr) |
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JP4467616B2 (ja) | 2004-05-14 | 2010-05-26 | ミレニアム・ファーマシューティカルズ・インコーポレイテッド | Auroraキナーゼの阻害により有糸分裂の進行を阻止するための化合物および方法 |
CL2007003244A1 (es) | 2006-11-16 | 2008-04-04 | Millennium Pharm Inc | Compuestos derivados de pirimido[5,4-d][2]benzazepina; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto para el tratamiento del cancer. |
AR074487A1 (es) * | 2008-12-05 | 2011-01-19 | Millennium Pharm Inc | Tiolactamas inhibidoras de proteinquinasas plk, composiciones farmaceuticas que las contienen y usos de las mismas para el tratamiento de trastornos proliferativos e inflamatorios, en particular cancer. |
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