HRP20120785T1 - Spojevi i postupci za inhibiciju napredovanja mitoze putem inhibicije aurora kinaze - Google Patents

Spojevi i postupci za inhibiciju napredovanja mitoze putem inhibicije aurora kinaze Download PDF

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Publication number
HRP20120785T1
HRP20120785T1 HRP20120785TT HRP20120785T HRP20120785T1 HR P20120785 T1 HRP20120785 T1 HR P20120785T1 HR P20120785T T HRP20120785T T HR P20120785TT HR P20120785 T HRP20120785 T HR P20120785T HR P20120785 T1 HRP20120785 T1 HR P20120785T1
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Croatia
Prior art keywords
cancer
hydrogen
group
aliphatic
compound according
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HRP20120785TT
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English (en)
Inventor
Christopher F. Claiborne
Lloyd J. Payne
Richard J. Boyce
Todd B. Sells
Stephen G. Stroud
Stuart Travers
Tricia J. Vos
Gabriel S. Weatherhead
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Millennium Pharmaceuticals, Inc.
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Application filed by Millennium Pharmaceuticals, Inc. filed Critical Millennium Pharmaceuticals, Inc.
Publication of HRP20120785T1 publication Critical patent/HRP20120785T1/hr

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    • 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
    • A61K31/55—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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings

Claims (9)

1. Spoj formule (Va): [image] ili njegova farmaceutski prihvatljiva sol u kojem: Re je vodik; svako od Rb2 i Rb3 nezavisno je izabrano iz grupe koju čine vodik, -halo, C1-3 alifatik, C1-3 fluoroalifatik i -OR5’, gde je R5’ vodik ili C1-3 alifatik; i svako od Rc1 i Rc5 nezavisno je izabrano iz grupe koju čine vodik, -halo, C1-3 alifatik, C1-3 fluoroalifatik i -OR5’, gde je R5’ vodik ili C1-3 alifatik; Rg je vodik; svako od Rh i Rk nezavisno je vodik ili Rd, i najmanje jedan od Rh i Rk je izabran iz grupe koju čine -CO2R5, -C(O)N(R4)2, -C(=NR4)-N(R4)2, -C(O)N(R4)C(=NR4)-N(R4)2, -N(R4)C(=NR4)-N(R4)-C(O)R5 ili -NR4C(O)R5; svako Rd nezavisno je R2d, izborno supstituirani alifatik, ili izborno supstituirani aril, heteroaril ili heterociklil grupa; R2d je -halo, -NO2, -CN, -C(R5)=C(R5)2, -C≡C-R5, -OR5, -SR6, -S(O)R6, -SO2R6, -SO2N(R4)2, -N(R4)2, -NR4C(O)R5, -NR4C(O)N(R4)2, -NR4CO2R6, -O-CO2R5, -OC(O)N(R4)2, -O-C(O)R5, -CO2R5, -C(O)-C(O)R5, -C(O)R5, -C(O)N(R4)2, -C(=NR4)-N(R4)2, -C(=NR4)-OR5, -N(R4)-N(R4)2, -N(R4)C(=NR4)-N(R4)2, -N(R4)SO2R6, -N(R4)SO2N(R4)2, -P(O)(R5)2 ili -P(O)(OR5)2; svako R4 nezavisno je vodik ili izborno supstituirani alifatik, aril, heteroaril ili heterociklil grupa; ili dva R4 na istom atomu dušika, uzeti zajedno sa atomom dušika, formiraju izborno supstituirani 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. svako R5 nezavisno je vodik ili izborno supstituirani alifatik, aril, heteroaril ili heterociklil grupa; i svako R6 nezavisno je izborno supstituirana alifatična ili aril grupa; pri čemu „alifatik/alifatična grupa“ označava ravnolančane, razgranate ili ciklične C1-12 ugljikovodike koji su potpuno zasićeni ili koji sadrže jednu ili više jedinica nezasićenja, ali koji nisu aromatični.
2. Spoj prema patentnom zahtjevu 1, u kojem: svako od Rb2 i Rb3 nezavisno je izabrano iz grupe koju čine vodik, kloro, fluoro, bromo, metil, trifluorometil i metoksi; svako od Rc1 i Rc5 nezavisno je izabrano iz grupe koju čine vodik, kloro, fluoro, bromo, metil, trifluorometil i metoksi; i najmanje jedan od Rh i Rk je -CO2R5, gde je R5 vodik ili C1-6 alifatik.
3. Farmaceutska kompozicija koja sadrži spoj prema patentnom zahtjevu 1 ili 2 i farmaceutski prihvatljiv nosač.
4. Farmaceutska kompozicija prema patentnom zahtjevu 3, koja dalje sadrži drugo terapeutsko sredstvo.
5. Spoj prema patentnom zahtjevu 1 ili 2 za uporabu u inhibiciji aktivnosti Aurora kinaze u stanici.
6. Spoj prema patentnom zahtjevu 1 ili 2 za uporabu u liječenju poremećaja posredovanog preko Aurora kinaze.
7. Spoj prema patentnom zahtjevu 6 za uporabu u liječenju poremećaja posredovanog preko Aurora kinaze, pri čemu je poremećaj posredovan preko Aurora kinaze kancer.
8. Spoj prema patentnom zahtjevu 7 za uporabu u liječenju kancera, pri čemu je kancer izabran iz grupe koju čine kolorektalni kancer, kancer jajnika, kancer dojke, kancer želuca, kancer prostate i kancer pankreasa.
9. Uporaba spoja prema patentnom zahtjevu 1 ili patentnom zahtjevu 2 u proizvodnji lijeka za liječenje poremećaja posredovanog preko Aurora kinaze koji je izabran iz grupe koju čine kancer, kolorektalni kancer, kancer jajnika, kancer dojke, kancer želuca, kancer prostate i kancer pankreasa.
HRP20120785TT 2004-05-14 2012-10-02 Spojevi i postupci za inhibiciju napredovanja mitoze putem inhibicije aurora kinaze HRP20120785T1 (hr)

Applications Claiming Priority (2)

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US57165304P 2004-05-14 2004-05-14
US61722104P 2004-10-08 2004-10-08

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HRP20080120TT HRP20080120T5 (hr) 2004-05-14 2008-03-19 Spojevi i postupci za inhibiciju napredovanja mitoze s pomoću inhibicije aurora kinaze
HRP20120785TT HRP20120785T1 (hr) 2004-05-14 2012-10-02 Spojevi i postupci za inhibiciju napredovanja mitoze putem inhibicije aurora kinaze

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US (9) US7572784B2 (hr)
EP (4) EP2719698B1 (hr)
JP (4) JP4467616B2 (hr)
KR (3) KR101748290B1 (hr)
CN (1) CN104193750B (hr)
AR (1) AR049277A1 (hr)
AT (1) ATE381566T1 (hr)
AU (1) AU2005243175B2 (hr)
BR (1) BRPI0511139B8 (hr)
CA (1) CA2565411C (hr)
CY (2) CY1108092T1 (hr)
DE (1) DE602005003951T4 (hr)
DK (1) DK1771450T5 (hr)
EA (1) EA012112B1 (hr)
ES (3) ES2391577T3 (hr)
HK (4) HK1102500A1 (hr)
HR (2) HRP20080120T5 (hr)
IL (1) IL179063A (hr)
MX (1) MXPA06013042A (hr)
MY (1) MY139355A (hr)
NZ (1) NZ551370A (hr)
PL (1) PL1771450T3 (hr)
PT (2) PT1771450E (hr)
RS (2) RS52436B (hr)
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WO (1) WO2005111039A2 (hr)

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