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ME03793B - Laktami kondezirani s arilom i heteroarilom - Google Patents

Laktami kondezirani s arilom i heteroarilom

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Publication number
ME03793B
ME03793B MEP-2020-147A MEP2020147A ME03793B ME 03793 B ME03793 B ME 03793B ME P2020147 A MEP2020147 A ME P2020147A ME 03793 B ME03793 B ME 03793B
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Montenegro
Prior art keywords
alkyl
membered heteroaryl
cycloalkyl
halogen
group
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MEP-2020-147A
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German (de)
English (en)
French (fr)
Inventor
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
Original Assignee
Pfizer
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Publication of ME03793B publication Critical patent/ME03793B/me

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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)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • 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): , 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 Rx i Ry se može uzeti zajedno s N atomom na kojeg su vezani kako bi tvorili 3-12-eročlani heterociklil ili 5-12-eročlani heteroaril 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, a 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 to 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 R8 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 heterociklil ili 5-12-eročlani heteroaril 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 heterociklil ili 5-12-eročlani heteroaril 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, C1-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-C8alkil, 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 supstituenti, 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 supstituenti, koje se neovisno bira iz skupine koju čine halogen, C1-C4 alkil, -OR14, -NR142, -CO2R14, -C(O)NR142, -SO2R14 i -SO2NR142, gdje svaki R14 je 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, naznačen time što navedeni heterociklil ili heteroaril može biti supstituiran s jednim ili više supstituenti, 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 R2 C1-C4 alkil 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-C6 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.
MEP-2020-147A 2012-12-21 2013-12-05 Laktami kondezirani s arilom i heteroarilom ME03793B (me)

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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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