HRP20221074T1 - Premošteni triciklički spojevi karbamoilpiridona i njihove farmaceutske uporabe - Google Patents

Premošteni triciklički spojevi karbamoilpiridona i njihove farmaceutske uporabe Download PDF

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HRP20221074T1
HRP20221074T1 HRP20221074TT HRP20221074T HRP20221074T1 HR P20221074 T1 HRP20221074 T1 HR P20221074T1 HR P20221074T T HRP20221074T T HR P20221074TT HR P20221074 T HRP20221074 T HR P20221074T HR P20221074 T1 HRP20221074 T1 HR P20221074T1
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Croatia
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pharmaceutically acceptable
acceptable salt
inhibitors
additional therapeutic
therapeutic agents
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HRP20221074TT
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English (en)
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Hang CHU
Ana Z. GONZALEZ BUENROSTRO
Hongyan Guo
Xiaochun Han
Lan Jiang
Jiayao Li
Michael L. Mitchell
Hyung-Jung Pyun
Scott D. Schroeder
Gregg M. SCHWARZWALDER
Nathan D. Shapiro
Devleena M. SHIVAKUMAR
Qiaoyin Wu
Hong Yang
Jennifer R. Zhang
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Gilead Sciences, Inc.
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Publication of HRP20221074T1 publication Critical patent/HRP20221074T1/hr

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4995Pyrazines or piperazines forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/06Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/22Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • AIDS & HIV (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (16)

1. Spoj, naznačen time, da je predstavljen formulom: [image] ili [image] ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] [image] ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1, naznačen time, da je predstavljen formulom: [image] ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak, naznačen time, da sadrži terapijski učinkovitu količinu spoja prema bilo kojem od patentnih zahtjeva 1 do 10, ili njegove farmaceutski prihvatljive soli, te farmaceutski prihvatljivo pomoćno sredstvo.
12. Farmaceutski pripravak prema patentnom zahtjevu 11, naznačen time, da nadalje sadrži: (i) jedan, dva, tri ili četiri dodatna terapijska sredstva; (ii) jedan, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su anti-HIV sredstva; (iii) jedan, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su inhibitori HIV proteaze, nenukleozidni ili nenukleotidni inhibitori HIV reverzne transkriptaze, nukleozidni ili nukleotidni inhibitori HIV reverzne transkriptaze, inhibitori HIV kapsida, gp41 inhibitori, CXCR4 inhibitori, gp120 inhibitori, CCR5 inhibitori, reverzibilna sredstva latencije, inhibitori kapsidne polimerizacije, HIV nNAbs, TLR7 agonisti, farmakokinetički pojačivači, ostali lijekovi za liječenje HIV-a, ili njihove kombinacije; ili (iv) jedan, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su abakavir, tenofovir alafenamid, tenofovir disoproksil, N-((S)-1-(3-(4-kloro-3-(metilsulfonamido)-1-(2,2,2-trifluoroetil)-1H-indazol-7-il)-6-(3-metil-3-(metilsulfonil)but-1-in-1-il)piridin-2-il)-2-(3,5-difluorofenil)etil)-2-((3bS,4aR)-5,5-difluoro-3-(trifluorometil)-3b,4,4a,5-tetrahidro-1H-ciklopropa[3,4]ciklopenta[1,2-c]pirazol-1-il)acetamid, ili njihova farmaceutski prihvatljiva sol.
13. Farmaceutski pripravak prema patentnom zahtjevu 11 ili 12, naznačen time, da je farmaceutski pripravak za oralnu ili parenteralnu primjenu.
14. Spoj ili njegova farmaceutski prihvatljiva sol prema bilo kojem od patentnih zahtjeva 1 do 10, naznačen time, da je za uporabu u postupku liječenja HIV infekcije kod čovjeka koji ima infekciju ili je pod rizikom da dobije infekciju, pri čemu postupak obuhvaća davanje čovjeku terapijski učinkovite količine spoja ili njegove farmaceutski prihvatljive soli.
15. Spoj ili njegova farmaceutski prihvatljiva sol za uporabu prema patentnom zahtjevu 14, naznačen time, da nadalje sadrži: (i) davanje čovjeku terapijski učinkovite količine jednog, dva, tri ili četiri dodatna terapijska sredstva; (ii) davanje čovjeku terapijski učinkovite količine jednog, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su anti-HIV sredstva; (iii) davanje čovjeku terapijski učinkovite količine jednog, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su inhibitori HIV proteaze, nenukleozidni ili nenukleotidni inhibitori HIV reverzne transkriptaze, nukleozidni ili nukleotidni inhibitori HIV reverzne transkriptaze, inhibitori HIV kapsida, gp41 inhibitori, CXCR4 inhibitori, gp120 inhibitori, CCR5 inhibitori, reverzibilna sredstva latencije, inhibitori kapsidne polimerizacije, HIV nNAbs, TLR7 agonisti, farmakokinetički pojačivači, ostali lijekovi za liječenje HIV-a, ili njihove kombinacije; ili (iv) davanje čovjeku terapijski učinkovite količine jednog, dva, tri ili četiri dodatna terapijska sredstva, pri čemu dodatna terapijska sredstva su abakavir, tenofovir alafenamid, tenofovir disoproksil, N-((S)-1-(3-(4-kloro-3-(metilsulfonamido)-1-(2,2,2-trifluoroetil)-1H-indazol-7-il)-6-(3-metil-3-(metilsulfonil)but-1-in-1-il)piridin-2-il)-2-(3,5-difluorofenil)etil)-2-((3bS,4aR)-5,5-difluoro-3-(trifluorometil)-3b,4,4a,5-tetrahidro-1H-ciklopropa[3,4]ciklopenta[1,2-c]pirazol-1-il)acetamid, ili njihova farmaceutski prihvatljiva sol.
16. Spoj ili njegova farmaceutski prihvatljiva sol za uporabu prema patentnom zahtjevu 14 ili 15, naznačen time, da je primjena oralna, intravenozna, supkutana ili intramuskularna.
HRP20221074TT 2019-03-22 2020-03-20 Premošteni triciklički spojevi karbamoilpiridona i njihove farmaceutske uporabe HRP20221074T1 (hr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201962822703P 2019-03-22 2019-03-22
US201962948697P 2019-12-16 2019-12-16
PCT/US2020/023819 WO2020197991A1 (en) 2019-03-22 2020-03-20 Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
EP20719849.0A EP3938047B1 (en) 2019-03-22 2020-03-20 Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use

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US (3) US11084832B2 (hr)
EP (2) EP4122537A1 (hr)
JP (2) JP7265647B2 (hr)
KR (1) KR20210142711A (hr)
CN (1) CN113874079A (hr)
AU (2) AU2020245350B2 (hr)
BR (1) BR112021018827A2 (hr)
CA (1) CA3128961A1 (hr)
CL (2) CL2021002444A1 (hr)
CO (1) CO2021012319A2 (hr)
CR (1) CR20210486A (hr)
DK (1) DK3938047T3 (hr)
DO (2) DOP2021000195A (hr)
ES (1) ES2927041T3 (hr)
HR (1) HRP20221074T1 (hr)
HU (1) HUE059677T2 (hr)
IL (1) IL286328A (hr)
LT (1) LT3938047T (hr)
MX (1) MX2021011394A (hr)
PE (1) PE20212074A1 (hr)
PL (1) PL3938047T3 (hr)
PT (1) PT3938047T (hr)
SG (1) SG11202109650XA (hr)
SI (1) SI3938047T1 (hr)
TW (2) TWI745900B (hr)
UA (1) UA127822C2 (hr)
WO (1) WO2020197991A1 (hr)
ZA (1) ZA202107015B (hr)

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