HRP20200395T1 - Derivat izoksazola kao inhibitor mutirane izocitratne dehidrogenaze 1 - Google Patents

Derivat izoksazola kao inhibitor mutirane izocitratne dehidrogenaze 1 Download PDF

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HRP20200395T1
HRP20200395T1 HRP20200395TT HRP20200395T HRP20200395T1 HR P20200395 T1 HRP20200395 T1 HR P20200395T1 HR P20200395T T HRP20200395T T HR P20200395TT HR P20200395 T HRP20200395 T HR P20200395T HR P20200395 T1 HRP20200395 T1 HR P20200395T1
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hydrogen atom
pharmaceutically acceptable
acceptable salt
compound according
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Shoichi Saito
Masao Itoh
Tetsunori Fujisawa
Hironao Saito
Yohei Kiyotsuka
Hideaki Watanabe
Hironori Matsunaga
Yoshiko Kagoshima
Tetsuya Suzuki
Yoko Ogawara
Kazuo Kitabayashi
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Daiichi Sankyo Company, Limited
National Cancer Center
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Publication of HRP20200395T1 publication Critical patent/HRP20200395T1/hr

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    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/495—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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
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    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
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    • 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

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
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Claims (18)

1. Spoj predstavljen općom formulom (I) ili njegova farmaceutski prihvatljiva sol: [image] gdje Z-Y predstavlja N-O ili O-N; R1 predstavlja fenil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe A, ili piridil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe A; R2 predstavlja -NR21R22, C1 do C6 alkil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe B, C3 do C6 cikloalkil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe C, ili 4- do 6-očlanu heterocikličnu grupu koja ima 1 ili 2 heteroatoma nezavisno odabrana iz grupe koja se sastoji od atoma dušika i atoma kisika u prstenu, gdje 4- do 6-očlana heterociklična grupa opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe C, i premošćena struktura je opcionalno vezana unutar heterocikličnog prstena, ili je jedan C3 do C6 cikloalkil prsten opcionalno vezan na heterociklični prsten preko spiro veze; R21 i R22 svako nezavisno predstavlja atom vodika, C1 do C6 alkil grupu, ili -C(=O)R23; R23 predstavlja C2 do C6 alkenil grupu ili C2 do C6 alkinil grupu; R3 predstavlja bilo koju od narednih formula (II) do (IV): [image] gdje R31 predstavlja atom vodika, atom halogena, C1 do C6 alkil grupu opcionalno supstituiranu sa 1 do 3 atoma halogena, C3 do C6 cikloalkil grupu, ili C1 do C6 alkilkarbonil grupu, R32 predstavlja atom vodika ili C1 do C6 alkil grupu, ili R31 i R32 opcionalno zajedno formiraju cikloheksanski prsten, R33 predstavlja atom vodika ili C1 do C6 alkil grupu, ili R32 i R33 opcionalno zajedno formiraju ciklopropanski prsten, R34 predstavlja atom vodika ili C1 do C6 alkil grupu, R35 predstavlja C1 do C6 alkil grupu, R36 predstavlja atom vodika ili C1 do C6 alkil grupu, R37 predstavlja atom vodika ili C1 do C6 alkil grupu, ili R36 i R37 opcionalno zajedno formiraju benzenov prsten, R38 predstavlja atom vodika ili atom halogena, X predstavlja atom dušika ili CH, W predstavlja atom dušika ili CH, i isprekidana linija predstavlja jednostruku vezu ili dvostruku vezu; grupa A se sastoji od atoma halogena, C1 do C6 alkil grupe i C1 do C6 alkoksi grupe; grupa B se sastoji od atoma halogena, hidroksi grupe, C1 do C6 alkoksi grupe, C1 do C6 alkilamino grupe, i di-C1 do C6 alkilamino grupe, grupa C se sastoji od C2 do C6 alkenil grupe, atoma halogena, hidroksi grupe, cijano grupe, C1 do C6 alkil grupe koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz naredne grupe D, C1 do C6 alkoksi grupe, -NR211R212, -C(=O)R213, i -SO2R213; R211 i R212 svako nezavisno predstavlja atom vodika ili C1 do C6 alkil grupu; R213 predstavlja C2 do C6 alkenil grupu ili C2 do C6 alkinil grupu; i grupa D se sastoji od amino grupe, C1 do C6 alkoksi grupe, di-C1 do C6 alkilamino grupe, okso grupe, i C3 do C6 cikloalkil grupe.
2. Spoj prema patentnom zahtjevu 1 ili njegova farmaceutski prihvatljiva sol, gdje u formuli (I), R1 predstavlja fenil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz grupe A.
3. Spoj prema patentnom zahtjevu 1 ili 2 ili njegova farmaceutski prihvatljiva sol, gdje u formuli (I), R2 predstavlja C1 do C6 alkil grupu koja opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz grupe B, ili 4- do 6-očlanu alifatičnu heterocikličnu grupu koja ima 1 ili 2 heteroatoma nezavisno odabrana iz grupe koja se sastoji od atoma dušika i atoma kisika u prstenu, gdje 4- do 6-očlana alifatična heterociklična grupa opcionalno ima 1 do 3 supstituenta nezavisno odabrana iz grupe C.
4. Spoj prema bilo kojem od patentnih zahtjeva 1 do 3 ili njegova farmaceutski prihvatljiva sol, gdje u formuli (I), R2 predstavlja bilo koju od narednih formula: [image]
5. Spoj prema bilo kojem od patentnih zahtjeva 1 do 4 ili njegova farmaceutski prihvatljiva sol, gdje u formuli(I), R3 predstavlja narednu formulu (IV') ili (V): [image] gdje R3a predstavlja atom vodika ili C1 do C6 alkil grupu opcionalno supstituiranu sa 1 do 3 atoma halogena, R3b predstavlja atom vodika ili C1 do C6 alkil grupu, R3c predstavlja atom vodika ili C1 do C6 alkil grupu, R3d predstavlja atom vodika ili C1 do C6 alkil grupu, R3e predstavlja atom vodika ili atom halogena, i isprekidana linija predstavlja jednostruku vezu ili dvostruku vezu.
6. Spoj prema bilo kojem od patentnih zahtjeva 1 do 5 ili njegova farmaceutski prihvatljiva sol, gdje u formuli (I), R3 predstavlja bilo koju od narednih formula: [image]
7. Spoj prema patentnom zahtjevu 1 predstavljeno općom formulom VI ili njegova farmaceutski prihvatljiva sol: [image] gdje R4, R5, i R6 svako nezavisno predstavlja atom vodika ili atom halogena, R7 predstavlja bilo koju od narednih formula: [image] i R8 i R9 svako nezavisno predstavlja atom vodika ili C1 do C6 alkil grupu.
8. Spoj prema patentnom zahtjevu 1 predstavljeno općom formulom VII ili njegova farmaceutski prihvatljiva sol: [image] gdje R10, R11, i R12 svako nezavisno predstavlja atom vodika ili atom halogena, R13 predstavlja bilo koju od narednih formula: [image] i R14 predstavlja atom vodika ili C1 do C6 alkil grupu.
9. Spoj prema patentnom zahtjevu 1 odabrano iz naredne grupe ili njegova farmaceutski prihvatljiva sol: (2E)-3-(1-{[5-(3-metiloksetan-3-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-1H-indol-4-il)prop-2-enska kiselina (2E)-3-(1-{[5-(2-fluoropropan-2-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enska kiselina (2E)-3-(1-{[5-(terc-butil)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-1H-indol-4-il)prop-2-enska kiselina (2E)-3-(1-{[3-(2,4-dikloro-6-fluorofenil)-5-(2-fluoropropan-2-il)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enska kiselina (2E)-3-(1-{[3-(2,4-diklorofenil)-5-(2-fluoropropan-2-il)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enska kiselina (2E)-[1-{[5-(1-akriloilpiperidin-4-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-3,4-dihidrobenzo[cd]indol-5(1H)-iliden]etanska kiselina (2E)-3-(1-{[5-(1-akriloilpiperidin-4-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enska kiselina (2E)-[1-{[5-(1-akriloilpiperidin-4-il)-3-(2,4-dikloro-6-fluorofenil)-1,2-oksazol-4-il]karbonil}-3,4-dihidrobenzo[cd]indol-5(1H)-iliden]etanska kiselina (2E)-[1-{[5-(1-akriloilpiperidin-4-il)-3-(2,4-dikloro-5-fluorofenil)-1,2-oksazol-4-il]karbonil}-3,4-dihidrobenzo[cd]indol-5(1H)-iliden]etanska kiselina (2E)-[1-{[5-(1-akriloilpiperidin-4-il)-3-(2,4-diklorofenil)-1,2-oksazol-4-il]karbonil}-3,4-dihidrobenzo[cd]indol-5(1H)-iliden]etanska kiselina.
10. Spoj prema patentnom zahtjevu 1 koje je (2E)-3-(1-{[5-(2-fluoropropan-2-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enska kiselina ili njegova farmaceutski prihvatljiva sol.
11. Spoj prema patentnom zahtjevu 1 koje je (2E)-3-(1-{[5-(2-fluoropropan-2-il)-3-(2,4,6-triklorofenil)-1,2-oksazol-4-il]karbonil}-3-metil-1H-indol-4-il)prop-2-enske kiseline terc-butilamin sol.
12. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegova farmaceutski prihvatljiva sol za primjenu kao inhibitor mutirane izocitratne dehidrogenaze 1.
13. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegova farmaceutski prihvatljiva sol za primjenu kao inhibitor proizvodnje D-2-hidroksiglutarata.
14. Farmaceutska kompozicija koja sadrži spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegovu farmaceutski prihvatljivu sol kao aktivni sastojak.
15. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegova farmaceutski prihvatljiva sol za primjenu kao antitumorski agens protiv tumora koji ima mutaciju gena izocitratne dehidrogenaze 1.
16. Spoj prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegova farmaceutski prihvatljiva sol za primjenu u metodi za liječenje tumora koji ima mutaciju gena izocitratne dehidrogenaze 1.
17. Primjena spoja prema bilo kojem od patentnih zahtjeva 1 do 11 ili njegove farmaceutski prihvatljive soli za proizvodnju farmaceutske kompozicije za liječenje tumora koji ima mutaciju gena izocitratne dehidrogenaze 1.
18. Spoj ili njegova farmaceutski prihvatljiva sol za primjenu prema patentnom zahtjevu 15 ili patentnom zahtjevu 16, ili primjena prema patentnom zahtjevu 17, gdje tumor je tumor na mozgu (uključujući gliom), akutna mijeloidna leukemija, mijelodisplastični sindrom, mijeloproliferativni tumor, periferni limfom T stanica, hondrosarkom, osteosarkom, rak žučnog kanala, primitivni neuroektodermalni tumor, limfoblastični limfom B stanica, maligni melanom, rak prostate, kolorektalni rak i tiroidni rak.
HRP20200395TT 2014-10-01 2020-03-10 Derivat izoksazola kao inhibitor mutirane izocitratne dehidrogenaze 1 HRP20200395T1 (hr)

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JP2014203475 2014-10-01
JP2015116774 2015-06-09
EP15845549.3A EP3202766B1 (en) 2014-10-01 2015-10-01 Isoxazole derivative as mutated isocitrate dehydrogenase 1 inhibitor
PCT/JP2015/077916 WO2016052697A1 (ja) 2014-10-01 2015-10-01 変異型イソクエン酸デヒドロゲナーゼ１阻害剤としてのイソキサゾール誘導体

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CN109311863B (zh) 2016-06-06 2021-10-29 伊莱利利公司 突变型idh1抑制剂
WO2018010142A1 (en) 2016-07-14 2018-01-18 Shanghai Meton Pharmaceutical Co., Ltd Iso-citrate dehydrogenase (idh) inhibitor
EP3661559A1 (en) * 2017-08-01 2020-06-10 Deutsches Krebsforschungszentrum Stiftung des Öffentlichen Rechts Combination of midh1 inhibitors and dna hypomethylating agents (hma)
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