HRP20211449T1 - Derivati supstituiranih karbonukleozida korisni kao sredstva protiv raka - Google Patents

Derivati supstituiranih karbonukleozida korisni kao sredstva protiv raka Download PDF

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HRP20211449T1
HRP20211449T1 HRP20211449TT HRP20211449T HRP20211449T1 HR P20211449 T1 HRP20211449 T1 HR P20211449T1 HR P20211449T T HRP20211449T T HR P20211449TT HR P20211449 T HRP20211449 T HR P20211449T HR P20211449 T1 HRP20211449 T1 HR P20211449T1
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image
cancer
pharmaceutically acceptable
compound
acceptable salt
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HRP20211449TT
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Robert Arnold Kumpf
Indrawan James Mcalpine
Michele Ann Mctigue
Ryan Patman
Eugene Yuanjin Rui
John Howard Tatlock
Michelle Bich Tran-Dube
Martin James Wythes
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Pfizer Inc.
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Publication of HRP20211449T1 publication Critical patent/HRP20211449T1/hr

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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/02—Halogenated hydrocarbons
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
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    • A—HUMAN NECESSITIES
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    • 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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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C255/01—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms
    • C07C255/32—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
    • C07C255/34—Carboxylic acid nitriles having cyano groups bound to acyclic carbon atoms having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring with cyano groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by unsaturated carbon chains
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/22—Nitrogen and oxygen atoms
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
    • 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
    • C07D471/06—Peri-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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    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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    • C07—ORGANIC CHEMISTRY
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Claims (21)

1. Spoj formule (IV): [image] , ili njegova farmaceutski prihvatljiva sol, naznačen time što: svakog R1 se neovisno bira iz skupine koju čine (C1-C8)alkil, (C1-C8)halogenalkil, hidroksi, (C1-C8)alkoksi, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil, 3-12-eročlani heterociklil, OR4, SR4 i N(R4)2; R2 je vodik, halogen, (C1-C8)alkil, hidroksi, (C1-C8)alkoksi ili N(R5)2, gdje je svaki R5 neovisno vodik ili (C1-C8)alkil, ili se dva R5 spaja kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S; svaki R3 je neovisno vodik, hidroksi ili NH2; ili kada D je C(R3)2, gdje se R3 dodatno bira između fluora; svaki R9 je neovisno vodik ili fluor; D je C(R3)2, O, ili S(O)1-2; B je N ili C; E je NR1, CH2, C(R1)2, O ili -S(O)2; svaki R8 je odsutan ili ga se neovisno bira iz skupine koju čine (C1-C8)alkil, (C1-C8)halogenalkil, hidroksi, (C1-C8)alkoksi, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil, 3-12-eročlani heterociklil, OR4, SR4, N(R4)2, CN, halogen i CON(R4)2, gdje se dva R8 mogu spojiti kako bi tvorili 4-6-eročlani spiro-cikloalkilni prsten, cikloalkilni kondenzirani prsten, ili alkilenski most, te gdje se dva R8 mogu spojiti kako bi tvorili karbonil; svaki R4 je neovisno A-R14, gdje A je odsutan, (C1-C3)alkil, -C(O)- ili -SO2-, a R14 je vodik, (C1-C8)alkil, (C5-C12)aril, 5-12-eročlani heteroaril, (C3-C10)cikloalkil ili 3-12-eročlani heterociklil, ili se dva R4 spoje kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S; Q je odsutan ili je dvovalentni ostatak kojeg se bira između O, S, NH i (C1-C8)alkilena; V je N ili C, gdje ako V tvori dvostruku vezu V je ugljik; W je N ili C, gdje ako W tvori dvostruku vezu W je ugljik; X je N ili C, gdje ako X tvori dvostruku vezu X je ugljik; Y je CR10, N, NR10, O ili S, gdje se svakog R10 neovisno bira između vodika, (C1-C8)alkila, hidroksi, (C1-C8)alkoksi, halogena, SH, S-(C1-C8)alkila i N(R11)2 ako je Y CR10, gdje Y tvori dvostruku vezu sa susjednim članom prstena kada je Y CR10 ili N, te gdje je svaki R11 neovisno vodik, (C1-C8)alkil, (C5-C12)aril ili 5-12-eročlani heteroaril ili se dva R11 spajaju kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S, ili Y je C(R10)2, a dva R10 i ugljik na kojeg su vezani tvore karbonil ili tiokarbonil; Z je CR12, N, NR12, O ili S, gdje se svakog R12 neovisno bira između vodika, (C1-C8)alkila, hidroksi, (C1-C8)alkoksi, fluora, klora, broma, SH, S-(C1-C8)alkil i N(R13)2, gdje Z tvori dvostruku vezu sa susjednim članom prstena ako je CR12 ili N, gdje je svaki R13 neovisno vodik, (C1-C8)alkil, (C5-C12)aril ili 5-12-eročlani heteroaril, ili se dva R13 spoje kako bi tvorili 4-6-eročlani heterociklički prsten koji sadrži 1-3 heteroatoma koje se bira između N, O i S, te gdje Z nije NR12 ako je X N, V je C, W je C, a Y je CR10, ili je Z C(R12)2, a dva R12 i ugljik na kojeg su vezani tvore karbonil ili tiokarbonil; i svaki ----- je izborna veza, gdje može biti prisutno najviše dva nesusjedna -----.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima formulu (III): [image] , ili njegova farmaceutski prihvatljiva sol.
3. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-2, naznačen time što: [image] se bira između: [image] [image] [image] [image] , [image] , [image] , [image] [image] [image]
4. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 3, naznačen time što: [image] se bira između: [image]
5. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 4, naznačen time što: [image] je: [image] .
6. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 2, naznačen time što: [image] se bira između: [image] [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] , [image] , [image] , [image] , [image] [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] , [image] , [image] , [image] [image] [image] [image] [image] [image]
7. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 6, naznačen time što: [image] je: [image] ili [image] .
8. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 7, naznačen time što: [image] je: [image] .
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ga se bira između: [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , [image] , te [image] , ili njihovih farmaceutski prihvatljivih soli.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (1S,2S,3S,5R)-3-((6-(difluormetil)-5-fluor-1,2,3,4-tetrahidroizokinolin-8-il)oksi)-5-(4-metil-7H-pirolo[2,3-d]pirimidin-7-il)ciklopentan-1,2-diol, ili njegova farmaceutski prihvatljiva sol.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima strukturu: [image] .
14. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1-13, naznačen time što se navedenu sol bira između acetatne, aspartatne, benzoatne, besilatne, bikarbonatne/karbonatne, bisulfatne/sulfatne, boratne, kamsilatne, citratne, edisilatne, esilatne, formijatne, fumaratne, gluceptatne, glukonatne, glukuronatne, heksafluorofosfatne, hibenzatne, hidroklorid/klorid, hidrobromid/bromid, hidrojodid/jodid, izetionatne, laktatne, malatne, maleatne, malonatne, mesilatne, metil-sulfatne, naftilatne, 2-napsilatne, nikotinatne, nitratne, orotatne, oksalatne, palmitatne, pamoatne, fosfatne/vodikfosfatne/divodikfosfatne, saharatne, stearatne, sukcinatne, tartaratne, tosilatne, trifluoracetatne, aluminijeve, arginin, benzatin, kalcijeve, kolinove, dietilaminske, diolaminske, glicinske, lizinske, magnezijeve, megluminske, olaminske, kalijeve, natrijeve, trometaminske i cinkove soli.
15. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s patentnim zahtjevom 14, naznačen time što se navedenu sol bira između hidrokloridne, tosilatne i mesilatne soli.
16. Farmaceutski pripravak, naznačen time što sadrži spoj, ili njegovu farmaceutski prihvatljivu sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 15, kao i farmaceutski prihvatljivi nosač.
17. Spoj, ili njegova farmaceutski prihvatljiva sol, u skladu s bilo kojim od patentnih zahtjeva 1 do 15, naznačen time što je namijenjen upotrebi u liječenju abnormalnog staničnog rasta kod sisavca.
18. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 17, naznačen time što je abnormalni stanični rast rak.
19. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 18, naznačen time što je rak rak pluća, rak kostiju, rak gušterače, rak kože, rak glave ili vrata, kutani ili intraokularni melanom, rak maternice, rak jajnika, rak rektuma, rak analnog područja, rak želuca, rak debelog crijeva, rak dojke, rak maternice, karcinom jajovoda, karcinom endometrija, karcinom vrata maternice, karcinom vagine, karcinom vulve, Hodgkinova bolest, rak jednjaka, rak tankog crijeva, rak endokrinog sustava, rak štitnjače, rak nusštitnjače, rak nadbubrežne žlijezde, sarkom mekog tkiva, rak mokraćne cijevi, rak penisa, rak prostate, kronična ili akutna leukemija, limfocitni limfomi, rak mokraćnog mjehura, rak bubrega ili mokraćovoda, karcinom bubrežnih stanica, karcinom nakapnice, novotvor središnjeg živčanog sustava (CNS), primarni limfom CNS-a, tumori leđne moždine, gliom moždanog debla ili adenom hipofize.
20. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 19, naznačen time što je rak rak pluća, rak glave ili vrata, rak dojke, karcinom endometrija, karcinom vrata maternice, rak jednjaka ili rak mokraćnog mjehura.
21. Spoj, ili njegova farmaceutski prihvatljiva sol, namijenjen upotrebi u skladu s patentnim zahtjevom 20, naznačen time što je rak rak pluća.
HRP20211449TT 2016-06-06 2017-06-03 Derivati supstituiranih karbonukleozida korisni kao sredstva protiv raka HRP20211449T1 (hr)

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