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HRP20221389T1 - Inhibitori bromodomena - Google Patents

Inhibitori bromodomena Download PDF

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Publication number
HRP20221389T1
HRP20221389T1 HRP20221389TT HRP20221389T HRP20221389T1 HR P20221389 T1 HRP20221389 T1 HR P20221389T1 HR P20221389T T HRP20221389T T HR P20221389TT HR P20221389 T HRP20221389 T HR P20221389T HR P20221389 T1 HRP20221389 T1 HR P20221389T1
Authority
HR
Croatia
Prior art keywords
pharmaceutically acceptable
compound
acceptable salt
alkyl
hydrogen
Prior art date
Application number
HRP20221389TT
Other languages
English (en)
Inventor
Michael John Bennett
Juan Manuel BETTANCORT
Amogh BLOOR
Stephen W. Kaldor
Jeffrey Alan Stafford
James Marvin Veal
Original Assignee
Celgene Quanticel Research, Inc.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Celgene Quanticel Research, Inc. filed Critical Celgene Quanticel Research, Inc.
Publication of HRP20221389T1 publication Critical patent/HRP20221389T1/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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/495—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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/92—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with a hetero atom directly attached to the ring nitrogen atom
    • C07D211/94—Oxygen atom, e.g. piperidine N-oxide
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/73—Unsubstituted amino or imino radicals
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
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    • C07D213/72—Nitrogen atoms
    • C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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    • 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
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    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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    • 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
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Claims (14)

1. Spoj, ili farmaceutski prihvatljiva sol istog, sa formulom (XXIV) [image] pri čemu, R13 je -I-Z; pri čemu I je odabrano od veze ili -CH2-; i Z je odabrano od -SO2R21, -N(R22)SO2R21, ili -N(R22)2; i pri čemu svako R21 je nezavisno odabrano od alkila, cikloalkila, cikloalkilalkila, arila, aralkila, heterociklila, heterociklilalkila, heteroarila, ili heteroarilalkila; i svako R22 je nezavisno odabrano od hidrogena, alkila, cikloalkila, cikloalkilalkila, arila, aralkila, heterociklila, heterociklilalkila, heteroarila, ili heteroarilalkila; R14 je vodik, halogen, C1-C3 alkil, ili C1-C3 alkoksi; R15 je halogen ili U-V, pri čemu U je veza, -O-, ili -CH2-; i V je -CN, alkil, alkinil, aril, aralkil, cikloalkil, cikloalkilalkil, heterociklil, heterociklilalkil, heteroaril, ili heteroarilalkil; i RB je [image] pri čemu X6 je C-R7, pri čemu R7 je vodik ili halogen; X7 je C-R8, pri čemu R8 je vodik ili halogen; ili RB je [image] pri čemu X5 je C-R5, pri čemu R5 je vodik ili halogen; i R6 je vodik, alkil, alkoksi, ili halogen; ili RB je [image] pri čemu prsten B je po izboru supstituirani 5-člani heterociklil prsten koji sadrži najmanje jedan atom kisika ili sumpora.
2. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu I je -CH2-.
3. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu I je veza.
4. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu: (i) R21 je alkil, cikloalkil, cikloalkilalkil, heterociklil ili heterociklilalkil; ili (ii) R21 je alkil, i alkil je C1-C4 alkil.
5. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu: (i) R22 je alkil, cikloalkil, ili aralkil; ili (ii) R22 je vodik ili metil.
6. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu R14 je vodik.
7. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu U je veza.
8. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu U je -O-.
9. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu U je -CH2-.
10. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu V je alkil, aril, aralkil, cikloalkilalkil, heterociklilalkil, heteroaril, heteroarilalkil, ili alkinil.
11. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu: (i) I je veza, Z je -N(R22)SO2R21, U je -O-, i V je aril, aralkil ili cikloalkilalkil; ili (ii) I je veza, Z je -SO2R21, U je -O-, i V je aril, aralkil ili cikloalkilalkil.
12. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu RB je [image]
13. Spoj iz patentnog zahtjeva 1, ili farmaceutski prihvatljiva sol istog, pri čemu: (i) R7 je halogen i R8 je vodik; (ii) R7 je halogen i R8 je vodik; ili (iii) R7 i R8 su vodik.
14. Farmaceutska kompozicija koja sadrži spoj iz bilo kojeg od patentnih zahtjeva 1-13, ili farmaceutski prihvatljiva sol istog, i najmanje jedan farmaceutski prihvatljiv ekscipijens.
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