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HRP20201194T2 - Laktami kondenzirani s arilom i heteroarilom - Google Patents

Laktami kondenzirani s arilom i heteroarilom Download PDF

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Publication number
HRP20201194T2
HRP20201194T2 HRP20201194TT HRP20201194T HRP20201194T2 HR P20201194 T2 HRP20201194 T2 HR P20201194T2 HR P20201194T T HRP20201194T T HR P20201194TT HR P20201194 T HRP20201194 T HR P20201194T HR P20201194 T2 HRP20201194 T2 HR P20201194T2
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alkyl
halogen
group
membered heteroaryl
aryl
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HRP20201194TT
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Martin Paul Edwards
Robert Arnold Kumpf
Pei-Pei Kung
Indrawan James Mcalpine
Sacha Ninkovic
Eugene Yuanjin Rui
Scott Channing Sutton
John Howard Tatlock
Martin James Wythes
Luke Raymond Zehnder
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Pfizer Inc.
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Publication of HRP20201194T1 publication Critical patent/HRP20201194T1/hr
Publication of HRP20201194T2 publication Critical patent/HRP20201194T2/hr

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    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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

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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)
  • General Chemical & Material Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Claims (12)

1. Spoj formule (II-A): [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što: R1 je C1-C8 alkil, C1-C8 alkoksi, halogen, -OH, -CN ili -NR7R8, gdje svaki navedeni C1-C8 alkil ili C1-C8 alkoksi može biti supstituiran s jednim ili više R21; R2 je C1-C8 alkil, koji može biti supstituiran s 1 do 3 R22; R3 je H, C1-C8 alkil, C1-C8 alkoksi, halogen, -OH, -CN ili -NR7R8, gdje svaki navedeni C1-C8 alkil ili C1-C8 alkoksi može biti supstituiran s jednim ili više R23; R4 se bira iz skupine koju čine H, halogen, C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, 5-12-eročlani heteroaril, -(C1-C4 alkil)Rz, -ORx, -CN, -C(O)Rx, -CO2Rx, -C(O)NRxRy, -SRx, -SORx, -SO2Rx, -SO2NRxRy, -NO2, -NRxRy, -NRxC(O)Ry, -NRxC(O)NRxRy, -NRxC(O)ORy, -NRxSO2Ry, -NRxSO2NRxRy, -OC(O)Rx i -OC(O)NRxRy; svakog Rx i Ry se neovisno bira iz skupine koju čine H, C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; ili se Rx i Ry može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklilni ili 5-12-eročlani heteroarilni prsten, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S; svakog Rz se neovisno bira iz skupine koju čine C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; i gdje svaki navedeni C1-C8 alkil u R4, Rx ili Ry i svaki navedeni C1-C4 alkil u (C1-C4 alkil)Rz može biti supstituiran s jednim ili više R24, a svaki navedeni C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, ili 5-12-eročlani heteroaril u R4, Rx, Ry, Rz, ili Rx i Ry uzet zajedno može biti supstituiran s jednim ili više R34; svakog R5 se neovisno bira iz skupine koju čine halogen, -OH, =O, C1-C4 alkil, C1-C4 alkoksi, -CN, -NR9R10 i -C(O)NR9R10, gdje svaki navedeni C1-C4 alkil ili C1-C4 alkoksi može biti supstituiran s 1 do 3 supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, C1-C4 alkoksi, -CN, -NR9R10 i -C(O)NR9R10; svakog R7 i R8 se neovisno bira iz skupine koju čine H, C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, te 5-12-eročlani heteroaril; ili R7 i R8 se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklil ili 5-12-eročlani heteroaril, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S; gdje svaki navedeni C1-C8 alkil u R7 ili R8 može biti supstituiran s jednim ili više R27, a svaki navedeni C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, ili 5-12-eročlani heteroaril u R7, R8, ili R7 i R8 uzet zajedno može biti supstituiran s jednim ili više R37; svaki R9 i R10 je neovisno H ili C1-C4 alkil; ili R9 i R10 se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklil ili 5-12-eročlani heteroaril, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S; gdje svaki navedeni C1-C4 alkil u R9 ili R10, te svaki navedeni 3-12-eročlani heterociklil ili 5-12-eročlani heteroaril u R9 i R10 uzet zajedno može biti supstituiran s 1 do 3 supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, =O, C1-C4 alkil, C1-C4 alkoksi, -CN, -NH2, -NH(C1-C4 alkil) i -N(C1-C4 alkil)2; m je 0 do 4; svakog R21, R22, R23 i R24 se neovisno bira iz skupine koju čine halogen, C1-C8 alkil, -CN, =O, -C(O)Re, -CO2Re, -C(O)NReRf, -ORe, -SRe, -SORe, -SO2Re, -SO2NReRf, -NO2, -NReRf, -NReC(O)Rf, -NReC(O)NReRf, -NReC(O)ORf -NReSO2Rf, -NReSO2NReRf, -OC(O)Re, -OC(O)NReRf, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; svakog Re i Rf se neovisno bira iz skupine koju čine H, C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; ili Re i Rf se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklilni ili 5-12-eročlani heteroarilni prsten, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S; gdje svaki navedeni C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril ili 5-12-eročlani heteroaril u R24, Re, Rf, ili Re i Rf uzet zajedno može biti supstituiran s 1 do 3 supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, = O, C1-C4 alkil, C1-C4 alkoksi, C1-C6 haloalkil, C1-C6 hidroksialkil, C1-C4 alkoksi-C1-C6 alkil, -CN, -NH2, -NH(C1-C4 alkil) i -N(C1-C4 alkil)2; svakog R27 se neovisno bira iz skupine koju čine halogen, -OH, C1-C4 alkoksi, -CN, -NR9R10, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril, gdje svaki navedeni C1-C4 alkoksi, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril ili 5-12-eročlani heteroaril može biti supstituiran s 1 do 3 supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, =O, C1-C4 alkil, C1-C4 alkoksi, C1-C6 haloalkil, C1-C6 hidroksialkil, C1-C4 alkoksi-C1-Ca alkil, -CN, -NH2, -NH(C1-C4 alkil) i -N(C1-C4 alkil)2; svakog R34 i R37 se neovisno bira iz skupine koju čine halogen, C1-C8 alkil, -CN, =O, -C(O)Rc, -CO2Rc, -C(O)NRcRd, -ORc, -SRc, -SORc, -SO2Rc, -SO2NRcRd, -NO2, -NRcRd, -NRcC(O)Rd, -NRcC(O)NRcRd, -NRcC(O)ORd, -NRcSO2Rd, -NRcSO2NRcRd, -OC(O)Rc, -OC(O)NRcRd, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; svakog Rc i Rd se neovisno bira iz skupine koju čine H, C1-C6 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril; ili Rc i Rd se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklilni ili 5-12-eročlani heteroarilni prsten, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S; gdje svaki navedeni C1-C8 alkil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril ili 5-12-eročlani heteroaril u R34, R37, Rc, Rd, ili Rc i Rd uzet zajedno može biti supstituiran s 1 do 3 supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, =O, C1-C4 alkil, C1-C4 alkoksi, C1-C6 haloalkil, C1-C6 hidroksialkil, C1-C4 alkoksi-C1-C6 alkil, -CN, -NH2, -NH(C1-C4 alkil) i -N(C1-C4 alkil)2; X i Z se neovisno bira iz skupine koju čine H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, 5-12-eročlani heteroaril, halogen, CN, -C(O)Ra, -CO2Ra, -C(O)NRaRb, -SRa, -SORa, -SO2Ra, -SO2NRaRb, -NO2, -NRaRb, -NRaC(O)Rb, -NRaC(O)NRaRb, -NRaC(O)ORa, -NRaSO2Rb, -NRaSO2NRaRb, -ORa, -OC(O)Ra ili -OC(O)NRaRb; gdje svaki navedeni C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, ili 5-12-eročlana heteroarilna skupina mogu biti supstituirani s jednim ili više supstituenta, koje se neovisno bira iz skupine koju čine halogen, -CN, -C(O)Ra, -CO2Ra, -C(O)NRaRb, -SRa, -SORa, -SO2Ra, -SO2NRaRb, -NO2, -NRaRb, -NRaC(O)Rb, -NRaC(O)NRaRb, -NRaC(O)ORa -NRaSO2Rb, -NRaSO2NRaRb, -ORa, -OC(O)Ra, -OC(O)NRaRb, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril, te 5-12-eročlani heteroaril; svaki Ra i Rb je neovisno H, C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril ili 5-12-eročlani heteroaril, gdje svaki navedeni C1-C8 alkil, C2-C8 alkenil, C2-C8 alkinil, C3-C8 cikloalkil, 3-12-eročlani heterociklil, C6-C12 aril i 5-12-eročlani heteroaril može biti supstituiran s jednim ili više supstituenta, koje se neovisno bira iz skupine koju čine halogen, C1-C4 alkil, -OR14, -NR142, -CO2R14, -C(O)NR142, -SO2R14 i -SO2NR142, gdje je svaki R14 neovisno H ili C1-C4 alkil; ili Ra i Rb se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklil ili 5-12-eročlani heteroaril, od kojih svaki može sadržavati 1, 2 ili 3 dodatna heteroatoma, koje se bira između O, N i S, gdje navedeni heterociklil ili heteroaril mogu biti supstituirani s jednim ili više supstituenta, koje se neovisno bira iz skupine koju čine halogen, -OH, =O, C1-C4 alkil, C1-C4 alkoksi, C1-C6 haloalkil, C1-C6 hidroksialkil, C1-C4 alkoksi-C1-C6 alkil, -CN, -NH2, -NH(C1-C4 alkil) i -N(C1-C4 alkil)2; i Y je H, halogen, -OH ili C1-C4 alkoksi.
2. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što je R1 C1-C6 alkil ili halogen.
3. Spoj ili sol u skladu s patentnim zahtjevom 1 ili 2, naznačen time što je R2 C1-C4 alkil, koji može biti supstituiran s 1 do 3 R22.
4. Spoj ili sol u skladu s patentnim zahtjevom 3, naznačen time što se svakog R22 neovisno bira između halogena, -C(O)NReRf, -ORe, -NReRf, -NReC(O)Rf i -NReSO2Rf.
5. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time što se R4 bira iz skupine koju čine H, halogen, -CN i C1-C8 alkil, gdje navedeni C1-C8 alkil može biti supstituiran s 1 do 3 R24.
6. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 5, naznačen time što je R3 H, a R4 je H ili halogen.
7. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 6, naznačen time što se X i Z neovisno bira iz skupine koju čine H, C1-C8 alkil i C3-C8 cikloalkil, a Y je H.
8. Spoj ili sol u skladu s bilo kojim od patentnih zahtjeva 1 do 7, naznačen time što je m 0.
9. Farmaceutski pripravak, naznačen time što sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegovu farmaceutski prihvatljivu sol, kao i farmaceutski prihvatljivi nosač ili pomoćnu tvar.
10. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegova farmaceutski prihvatljiva sol, naznačen time što je namijenjen upotrebi u liječenju abnormalnog staničnog rasta kod subjekta.
11. Spoj namijenjen upotrebi u skladu s patentnim zahtjevom 10, naznačen time što je abnormalan stanični rast rak.
12. Kombinacija, naznačena time što je kombinacija spoja u skladu s bilo kojim od patentnih zahtjeva 1 do 8, ili njegove farmaceutski prihvatljive soli, sa sredstvom protiv raka.
HRP20201194TT 2012-12-21 2020-07-30 Laktami kondenzirani s arilom i heteroarilom HRP20201194T2 (hr)

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US201261740596P 2012-12-21 2012-12-21
EP17206218.4A EP3339303B9 (en) 2012-12-21 2013-12-05 Aryl and heteroaryl fused lactams

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