HRP20120490T1 - Spojevi za inhibiciju napredovanja mitoze - Google Patents

Spojevi za inhibiciju napredovanja mitoze Download PDF

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Publication number
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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HR
Croatia
Prior art keywords
aliphatic
group
fluoroaliphatic
compound according
fluoro
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HRP20120490TT
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English (en)
Inventor
Christopher@F@@Claiborne
Todd@B@@Sells
Stephen@G@@Stroud
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Millennium@Pharmaceuticals
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39315133&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20120490(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Millennium@Pharmaceuticals filed Critical Millennium@Pharmaceuticals
Publication of HRP20120490T1 publication Critical patent/HRP20120490T1/hr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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.
HRP20120490TT 2006-11-16 2012-06-12 Spojevi za inhibiciju napredovanja mitoze HRP20120490T1 (hr)

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

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HRP20120490T1 true HRP20120490T1 (hr) 2012-07-31

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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

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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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CA2669680C (en) 2012-04-10
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ZA200903279B (en) 2010-07-28
NZ597252A (en) 2013-06-28
CR20140544A (es) 2015-01-12
US20110312942A1 (en) 2011-12-22
US9765076B2 (en) 2017-09-19
US20110312943A1 (en) 2011-12-22
SG176443A1 (en) 2011-12-29
DK2086981T3 (da) 2012-08-06
MY153243A (en) 2015-01-29
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KR20110113210A (ko) 2011-10-14
ATE556076T1 (de) 2012-05-15
HK1134672A1 (en) 2010-05-07
EP2497773B1 (en) 2015-02-25
AU2007322046B2 (en) 2012-04-05
EP2944639B1 (en) 2017-01-04
US20150166545A1 (en) 2015-06-18
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NZ611898A (en) 2015-01-30
ES2528793T3 (es) 2015-02-12
NO343338B1 (no) 2019-02-04
WO2008063525A1 (en) 2008-05-29
PH12012502057B1 (en) 2015-09-14
ES2384123T3 (es) 2012-06-29
IL198690A0 (en) 2010-02-17
AU2007322046A1 (en) 2008-05-29
KR101342014B1 (ko) 2013-12-19
EP2497772A1 (en) 2012-09-12
ES2537451T3 (es) 2015-06-08
US10836766B2 (en) 2020-11-17
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US11958855B2 (en) 2024-04-16
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BRPI0718803A2 (pt) 2013-12-03
US20190031662A1 (en) 2019-01-31
CN103483343A (zh) 2014-01-01
CR10782A (es) 2009-06-24
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PH12012502057A1 (en) 2015-09-14
CN103483343B (zh) 2016-06-01
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BRPI0718803B1 (pt) 2020-11-17
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SI2086981T1 (sl) 2012-12-31
MX343391B (es) 2016-11-04
CN101547924B (zh) 2013-09-25
EA200970486A1 (ru) 2009-10-30
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US20210214361A1 (en) 2021-07-15
HK1175778A1 (en) 2013-07-12
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JP2014055166A (ja) 2014-03-27
MX2009004670A (es) 2009-05-15
PT2086981E (pt) 2012-06-20
JP2010510215A (ja) 2010-04-02
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CY1112828T1 (el) 2016-02-10
BRPI0718803B8 (pt) 2021-05-25

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