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HRP20210732T1 - Supstituirani spojevi 8-oksetan-3-il-3,8-diazabiciklo[3.2.1]oktan-3-ila kao inhibitori hiv-a - Google Patents

Supstituirani spojevi 8-oksetan-3-il-3,8-diazabiciklo[3.2.1]oktan-3-ila kao inhibitori hiv-a Download PDF

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Publication number
HRP20210732T1
HRP20210732T1 HRP20210732TT HRP20210732T HRP20210732T1 HR P20210732 T1 HRP20210732 T1 HR P20210732T1 HR P20210732T T HRP20210732T T HR P20210732TT HR P20210732 T HRP20210732 T HR P20210732T HR P20210732 T1 HRP20210732 T1 HR P20210732T1
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HR
Croatia
Prior art keywords
hiv
compound
inhibitors
inhibitor
tenofovir
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Application number
HRP20210732TT
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English (en)
Inventor
Elizabeth M. Bacon
Elbert Chin
Jeromy J. Cottell
Ashley Anne Katana
Darryl Kato
John O. Link
Nathan Shapiro
Teresa Alejandra Trejo Martin
Zheng-Yu Yang
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Gilead Sciences, Inc.
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=61244746&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20210732(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences, Inc. filed Critical Gilead Sciences, Inc.
Publication of HRP20210732T1 publication Critical patent/HRP20210732T1/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
    • A61K31/495—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
    • A61K31/52—Purines, e.g. adenine
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    • 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
    • C07D487/08—Bridged systems
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring systems
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/685—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • A61K31/688—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols both hydroxy compounds having nitrogen atoms, e.g. sphingomyelins
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C243/00—Compounds containing chains of nitrogen atoms singly-bound to each other, e.g. hydrazines, triazanes
    • C07C243/24—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids
    • C07C243/26—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C243/28—Hydrazines having nitrogen atoms of hydrazine groups acylated by carboxylic acids with acylating carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C275/00—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups
    • C07C275/04—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms
    • C07C275/06—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton
    • C07C275/16—Derivatives of urea, i.e. compounds containing any of the groups, the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to acyclic carbon atoms of an acyclic and saturated carbon skeleton being further substituted by carboxyl groups
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D471/08—Bridged systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • 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
    • C07D487/10—Spiro-condensed systems
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    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D498/02—Heterocyclic 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Liquid Crystal Substances (AREA)
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  • Pyridine Compounds (AREA)

Claims (15)

1. Spoj, naznačen time, da on jest: [image] ili njegova farmaceutski prihvatljiva sol.
2. Spoj, naznačen time, da on jest: [image] ili njegova farmaceutski prihvatljiva sol.
3. Farmaceutski pripravak, naznačen time, da sadrži terapijski učinkovitu količinu spoja iz patentnog zahtjeva 1 ili 2, ili njegove farmaceutski prihvatljive soli, i farmaceutski prihvatljivu pomoćnu tvar.
4. Farmaceutski pripravak prema patentnom zahtjevu 3, naznačen time, da nadalje sadrži jednu, dvije, tri ili četiri dodatne terapijske tvari.
5. Spoj prema patentnim zahtjevima 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u liječenju.
6. Spoj prema patentnim zahtjevima 1 ili 2, ili njegova farmaceutski prihvatljiva sol, naznačen time, da je za uporabu u postupku liječenja ili prevencije infekcije virusom humane imunodeficijencije (HIV), koji obuhvaća davanje pojedincu kojemu je to potrebno, terapijski učinkovite količine navedenog spoja.
7. Spoj za uporabu prema patentnom zahtjevu 6, naznačen time, da spomenuti postupak obuhvaća davanje jedne, dvije, tri ili četiri dodatne terapijske tvari.
8. Spoj za uporabu prema patentnom zahtjevu 7, naznačen time, da se dodatne terapijske tvari primjenjuju istovremeno sa spojem prema patentnim zahtjevima 1 ili 2, ili s njegovom farmaceutski prihvatljivom soli.
9. Spoj za uporabu prema patentnom zahtjevu 7, naznačen time, da se spoj prema patentnim zahtjevima 1 ili 2, kombinira s dodatnim terapijskim tvarima u jedinstvenom obliku za doziranje za istovremenu primjenu.
10. Spoj za uporabu prema patentnom zahtjevu 7, naznačen time, da se primjenjuje spoj prema patentnim zahtjevima 1 ili 2, i dodatne terapijske tvari se primjenjuju uzastopno.
11. Spoj za uporabu prema patentnom zahtjevu 7, ili farmaceutski pripravak prema patentnom zahtjevu 4, naznačen time, da se dodatne terapijske tvari biraju iz skupine koja se sastoji od kombiniranih lijekova za HIV, ostalih lijekova za liječenje HIV-a, inhibitora HIV proteaze, nenukleozidnih ili nenukleotidnih inhibitora HIV reverzne transkriptaze, nukleozidnih ili nukleotidnih inhibitora HIV reverzne transkriptaze, inhibitora HIV integraze, inhibitora HIV integraze nekatalitičkog mjesta (ili alosteričnih inhibitora), inhibitora ulaska HIV, inhibitora HIV maturacije, agensa za ukidanje latentnosti, spojeva koji ciljaju na HIV kapsidu, terapija na temelju imunosti, inhibitora fosfofatidilinozitol-3-kinaze (PI3K), HIV protutijela, bispecifičnih protutijela i terapijskih proteina „nalik na protutijelo“, inhibitora HIV p17 matričnog proteina, IL-13 antagonista, modulatora peptid-prolil cis-trans izomeraze A, inhibitora proteinske disulfidne izomeraze, antagonista receptora komplementa C5a, inhibitora DNA metiltransferaze, modulatora vif gena HIV-a, antagonista dimerizacije Vif-a, inhibitora faktora HIV-1 virusne infektivnosti, inhibitora TAT proteina, modulatora HIV-1 Nef, modulatora Hck tirozinske kinaze, inhibitora kinaze-3 (MLK-3) miješanog podrijetla, inhibitora izrezivanja introna kod HIV-1, inhibitora Rev proteina, integrinskih antagonista, inhibitora nukleoproteina, modulatora faktora izrezivanja introna, modulatora proteina 1 koji sadrže COMM domenu, inhibitora HIV ribonukleaze H, retrociklinskih modulatora, inhibitora CDK-9, inhibitora neintegrina 1 koji zahvaćaju dendritički ICAM-3, inhibitora HIV GAG proteina, inhibitora HIV POL proteina, modulatora komplementnog faktora H, inhibitora ubikvitinske ligaze, inhibitora deoksicitidinske kinaze, inhibitora ciklinski ovisne kinaze, stimulatora proproteinske konvertaze PC9, inhibitora RNA helikaze DDX3X ovisne o ATP-u, inhibitora reverzne transkriptaze primarnog kompleksa, inhibitora G6PD i NADH oksidaze, farmakokinetičkih pojačivača, genske terapije HIV-a, HIV cjepiva, ili bilo koje njihove kombinacije.
12. Spoj za uporabu prema patentnom zahtjevu 7, ili farmaceutski pripravak prema patentnom zahtjevu 4, naznačen time, da se navedeni spoj kombinira s abakavir sulfatom, biktegravirom, tenofovirom, tenofovir disoproksilom, tenofovir disoproksil fumaratom, tenofovir disoproksil hemifumaratom, tenofovir alafenamidom, ili tenofovir alafenamid hemifumaratom.
13. Spoj za uporabu prema patentnom zahtjevu 7, naznačen time, da se navedeni spoj kombinira s prvom dodatnom terapijskom tvari odabranom iz skupine koja se sastoji od abakavir sulfata, biktegravira, tenofovira, tenofovir disoproksila, tenofovir disoproksil fumarata, tenofovir alafenamida i tenofovir alafenamid hemifumarata, i s drugom dodatnom terapijskom tvari odabranom iz skupine koja se sastoji od emtricitabina i lamivudina.
14. Farmaceutski pripravak prema bilo kojem od patentnih zahtjeva 4 ili 5, ili spoj za uporabu prema bilo kojem od patentnih zahtjeva 7 do 11, naznačen time, da se dodatne terapijske tvari biraju iz skupine koja se sastoji od: [image] i [image] ili njihove farmaceutski prihvatljive soli.
15. Farmaceutski pripravak prema patentnim zahtjevima 4 ili 5, ili spoj za uporabu prema bilo kojem od patentnih zahtjeva 7 do 11, naznačen time, da se dodatne terapijske tvari biraju iz skupine koja se sastoji od abakavir sulfata, biktegravira, tenofovira, tenofovir disoproksila, tenofovir disoproksil fumarata, tenofovir disoproksil hemifumarata, tenofovir alafenamida, tenofovir alafenamid hemifumarata, emtricitabina, lamivudina, GS-9131, dolutegravira i kabotegravira.
HRP20210732TT 2017-02-06 2021-05-11 Supstituirani spojevi 8-oksetan-3-il-3,8-diazabiciklo[3.2.1]oktan-3-ila kao inhibitori hiv-a HRP20210732T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762455348P 2017-02-06 2017-02-06
PCT/US2018/016893 WO2018145021A1 (en) 2017-02-06 2018-02-05 Atazanavir (atv) analogues for treating hiv infections
EP18706072.8A EP3577110B1 (en) 2017-02-06 2018-02-05 8-oxetan-3-yl-3,8-diazabicyclo[3.2.1]octan-3-yl substituted compounds as hiv inhibitors

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HRP20210732T1 true HRP20210732T1 (hr) 2021-09-17

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US (4) US10294234B2 (hr)
EP (2) EP3909949A1 (hr)
JP (4) JP6814304B2 (hr)
KR (3) KR20230097222A (hr)
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AU (3) AU2018215546B2 (hr)
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HR (1) HRP20210732T1 (hr)
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