AU2018216738B2 - Crystalline forms of tenofovir alafenamide - Google Patents

Crystalline forms of tenofovir alafenamide Download PDF

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Publication number
AU2018216738B2
AU2018216738B2 AU2018216738A AU2018216738A AU2018216738B2 AU 2018216738 B2 AU2018216738 B2 AU 2018216738B2 AU 2018216738 A AU2018216738 A AU 2018216738A AU 2018216738 A AU2018216738 A AU 2018216738A AU 2018216738 B2 AU2018216738 B2 AU 2018216738B2
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Prior art keywords
tenofovir alafenamide
inhibitors
crystalline
reflections
degrees
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AU2018216738A1 (en
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Chiajen Lai
Bing Shi
Robert G. Strickley
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Gilead Sciences Inc
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Gilead Sciences Inc
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Priority to AU2022283687A priority patent/AU2022283687B2/en
Priority to AU2024267064A priority patent/AU2024267064A1/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/20—Sebacic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C65/00—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C65/01—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups
    • C07C65/105—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic
    • C07C65/11—Compounds having carboxyl groups bound to carbon atoms of six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups containing hydroxy or O-metal groups polycyclic with carboxyl groups on a condensed ring system containing two rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Hydrogenated Pyridines (AREA)
AU2018216738A 2017-01-31 2018-01-29 Crystalline forms of tenofovir alafenamide Active AU2018216738B2 (en)

Priority Applications (3)

Application Number Priority Date Filing Date Title
AU2021200857A AU2021200857B2 (en) 2017-01-31 2021-02-10 Crystalline forms of tenofovir alafenamide
AU2022283687A AU2022283687B2 (en) 2017-01-31 2022-12-07 Crystalline forms of tenofovir alafenamide
AU2024267064A AU2024267064A1 (en) 2017-01-31 2024-11-29 Crystalline forms of tenofovir alafenamide

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762452428P 2017-01-31 2017-01-31
US62/452,428 2017-01-31
PCT/US2018/015770 WO2018144390A1 (en) 2017-01-31 2018-01-29 Crystalline forms of tenofovir alafenamide

Related Child Applications (1)

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AU2021200857A Division AU2021200857B2 (en) 2017-01-31 2021-02-10 Crystalline forms of tenofovir alafenamide

Publications (2)

Publication Number Publication Date
AU2018216738A1 AU2018216738A1 (en) 2019-07-11
AU2018216738B2 true AU2018216738B2 (en) 2021-03-04

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AU2018216738A Active AU2018216738B2 (en) 2017-01-31 2018-01-29 Crystalline forms of tenofovir alafenamide
AU2021200857A Active AU2021200857B2 (en) 2017-01-31 2021-02-10 Crystalline forms of tenofovir alafenamide
AU2022283687A Active AU2022283687B2 (en) 2017-01-31 2022-12-07 Crystalline forms of tenofovir alafenamide
AU2024267064A Pending AU2024267064A1 (en) 2017-01-31 2024-11-29 Crystalline forms of tenofovir alafenamide

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AU2021200857A Active AU2021200857B2 (en) 2017-01-31 2021-02-10 Crystalline forms of tenofovir alafenamide
AU2022283687A Active AU2022283687B2 (en) 2017-01-31 2022-12-07 Crystalline forms of tenofovir alafenamide
AU2024267064A Pending AU2024267064A1 (en) 2017-01-31 2024-11-29 Crystalline forms of tenofovir alafenamide

Country Status (14)

Country Link
US (4) US10287307B2 (https=)
EP (2) EP3577125B1 (https=)
JP (3) JP2020505411A (https=)
KR (3) KR20210047978A (https=)
CN (2) CN115925747A (https=)
AR (1) AR110768A1 (https=)
AU (4) AU2018216738B2 (https=)
CA (2) CA3049028C (https=)
ES (1) ES2981241T3 (https=)
PL (1) PL3577125T3 (https=)
PT (1) PT3577125T (https=)
SI (1) SI3577125T1 (https=)
TW (5) TWI820984B (https=)
WO (1) WO2018144390A1 (https=)

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TWI820984B (zh) 2017-01-31 2023-11-01 美商基利科學股份有限公司 替諾福韋埃拉酚胺(tenofovir alafenamide)之晶型
SI3661937T1 (sl) 2017-08-01 2021-11-30 Gilead Sciences, Inc. Kristalinične oblike etil((S)-((((2R,5R)-5-(6-amino-9H-purin-9-IL)-4- fluoro-2,5-dihidrofuran-2-IL)oksi)metil)(fenoksi)fosforil)-L-alaninata (GS-9131) za zdravljenje virusnih okužb
CN108997428B (zh) * 2018-06-13 2021-04-13 中山大学 一种替诺福韦艾拉酚胺与香草酸的共晶及其制备方法
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WO2021011891A1 (en) 2019-07-18 2021-01-21 Gilead Sciences, Inc. Long-acting formulations of tenofovir alafenamide
WO2021016543A1 (en) * 2019-07-25 2021-01-28 Romark Laboratories L.C. Antiviral combinations of thiazolide compounds
WO2021034804A1 (en) 2019-08-19 2021-02-25 Gilead Sciences, Inc. Pharmaceutical formulations of tenofovir alafenamide
US20220370447A1 (en) * 2019-09-20 2022-11-24 Hoffmann-La Roche Inc. Method of treating hbv infection using a core protein allosteric modulator
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SI4204421T1 (sl) * 2020-08-27 2024-07-31 Gilead Sciences, Inc., Spojine in postopki za zdravljenje virusnih okužb

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