DK2393485T3 - Tolagstabletter, der omfatter elvitegravir, cobicistat, emtricitabin og tenofovir - Google Patents

Tolagstabletter, der omfatter elvitegravir, cobicistat, emtricitabin og tenofovir Download PDF

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Publication number
DK2393485T3
DK2393485T3 DK10703766.5T DK10703766T DK2393485T3 DK 2393485 T3 DK2393485 T3 DK 2393485T3 DK 10703766 T DK10703766 T DK 10703766T DK 2393485 T3 DK2393485 T3 DK 2393485T3
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formula
compound
tablet
layer
iii
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DK10703766.5T
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Reza Oliyai
Mark M Menning
Joanna M Koziara
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Gilead Sciences Inc
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (20)

  1. TOLAGSTABLETTER, DER OMFATTER ELVITEGRAVIR, COBICISTAT, EMTRICIT AB IN OG TENOFOVIR
    1. Tablet, der omfatter et første lag og et andet lag, hvor; a) det første lag omfatter: en forbindelse med formlen I:
    og en forbindelse med formlen II:
    og eventuelt en farmaceutisk acceptabel bærer; og b) det andet lag omfatter: en forbindelse med formlen III: og
    et salt med formlen IV:
    IV > og eventuelt en farmaceutisk acceptabel bærer.
  2. 2. Tablet ifølge krav 1, hvor det første lag er i kontakt med det andet lag.
  3. 3. Tablet ifølge et hvilket som helst af kravene 1-2, hvor vægtforholdet mellem forbindelsen med formlen I og forbindelsen med formlen II er 1,0 ± 0,5.
  4. 4. Tablet ifølge et hvilket som helst af kravene 1-3, hvor det første lag endvidere omfatter et antal af siliciumdioxidpartikler.
  5. 5. Tablet ifølge et hvilket som helst af kravene 1-3, hvor forbindelsen med formlen II er forbundet med siliciumdioxidpartikler.
  6. 6. Tablet ifølge et hvilket som helst af kravene 1-5, der omfatter 150 mg ± 10 % af forbindelsen med formlen I; 150 mg ± 10 % af forbindelsen med formlen II; 200 mg ± 10 % af forbindelsen med formlen III; og 300 mg ± 10 % af forbindelsen med formlen IV.
  7. 7. Tablet ifølge krav 6, der omfatter 150 mg ± 5 % af forbindelsen med formlen I.
  8. 8. Tablet ifølge krav 6, der omfatter 150 mg ± 2 % af forbindelsen med formlen I.
  9. 9. Tablet ifølge et hvilket som helst af kravene 6-8, der omfatter 150 mg ± 5 % af forbindelsen med formlen II.
  10. 10. Tablet ifølge et hvilket som helst af kravene 6-8, der omfatter 150 mg ± 2 % af forbindelsen med formlen II.
  11. 11. Tablet ifølge et hvilket som helst af kravene 6-10, der omfatter 200 mg ± 5 % af forbindelsen med formlen III.
  12. 12. Tablet ifølge et hvilket som helst af kravene 6-10, der omfatter 200 mg ± 2 % af forbindelsen med formlen III.
  13. 13. Tablet ifølge et hvilket som helst af kravene 6-12, der omfatter 300 mg ± 5 % af saltet med formlen IV.
  14. 14. Tablet ifølge et hvilket som helst af kravene 6-12, der omfatter 300 mg ± 2 % af saltet med formlen IV.
  15. 15. Tablet ifølge et hvilket som helst af kravene 1-14, der endvidere omfatter en farmaceutisk acceptabel bærer.
  16. 16. Tablet ifølge et hvilket som helst af kravene 1-15, der er formuleret i en doseringsenhedsform.
  17. 17. Tabiet ifølge et hvilket som helst af kravene 1-16, der er formuleret til dosering én gang dagligt.
  18. 18. Fremgangsmåde til fremstilling af en tablet som beskrevet i krav 1, der omfatter: komprimering af en sammensætning, der omfatter forbindelsen med formlen I, og forbindelsen med formlen II til tilvejebringelse af et første komprimeret lag; tilføjelse af forbindelsen med formlen III og saltet med formlen IV til det første pressede lag; og komprimering for tilvejebringelse af tabletten.
  19. 19. Tablet som beskrevet i krav 1, der består af følgende:
  20. 20. Tablet fremstillet som beskrevet i krav 18.
DK10703766.5T 2009-02-06 2010-02-04 Tolagstabletter, der omfatter elvitegravir, cobicistat, emtricitabin og tenofovir DK2393485T3 (da)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US15065509P 2009-02-06 2009-02-06
US15065209P 2009-02-06 2009-02-06
PCT/US2010/023226 WO2010091197A2 (en) 2009-02-06 2010-02-04 Tablets for combination therapy

Publications (1)

Publication Number Publication Date
DK2393485T3 true DK2393485T3 (da) 2015-10-26

Family

ID=41722740

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Application Number Title Priority Date Filing Date
DK10703766.5T DK2393485T3 (da) 2009-02-06 2010-02-04 Tolagstabletter, der omfatter elvitegravir, cobicistat, emtricitabin og tenofovir

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Country Link
US (2) US20100285122A1 (da)
EP (1) EP2393485B1 (da)
JP (2) JP5611242B2 (da)
KR (2) KR101645759B1 (da)
CN (1) CN102307573B (da)
AP (1) AP3250A (da)
AR (1) AR075369A1 (da)
AU (1) AU2010210598B2 (da)
BR (1) BRPI1008664A2 (da)
CA (1) CA2750521A1 (da)
CL (1) CL2011001885A1 (da)
CY (1) CY1116852T1 (da)
DK (1) DK2393485T3 (da)
EA (2) EA030123B1 (da)
EC (1) ECSP11011307A (da)
ES (1) ES2548886T3 (da)
HK (1) HK1164737A1 (da)
HR (1) HRP20151009T1 (da)
HU (1) HUE025822T2 (da)
IL (1) IL214227A (da)
MX (1) MX2011008289A (da)
NZ (1) NZ594214A (da)
PE (1) PE20110994A1 (da)
PL (1) PL2393485T3 (da)
PT (1) PT2393485E (da)
SG (3) SG173544A1 (da)
SI (1) SI2393485T1 (da)
SM (1) SMT201500266B (da)
TW (1) TWI444367B (da)
UY (1) UY32424A (da)
WO (1) WO2010091197A2 (da)

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EA020489B1 (ru) 2006-07-07 2014-11-28 Джилид Сайэнс, Инк. Модуляторы фармакокинетических свойств лекарственных средств
SG183059A1 (en) * 2007-02-23 2012-08-30 Gilead Sciences Inc Modulators of pharmacokinetic properties of therapeutics
PL2296633T3 (pl) 2008-05-02 2016-03-31 Gilead Sciences Inc Zastosowanie cząsteczek stałych nośników dla udoskonalenia przetwarzalności środka farmaceutycznego
TWI556840B (zh) 2010-11-19 2016-11-11 吉李德科學股份有限公司 治療用組成物
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DK3067358T3 (da) 2012-12-21 2019-11-04 Gilead Sciences Inc Polycykliske carbamoylpyridon-forbindelser og deres farmaceutiske anvendelse
PT3607939T (pt) 2015-06-30 2022-09-12 Gilead Sciences Inc Formulações farmacêuticas compreendendo tenofovir e emtricitabina
CN113546052A (zh) 2015-11-09 2021-10-26 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物
ES2806604T3 (es) 2016-02-02 2021-02-18 Sandoz Ag Formas cristalinas de monofumarato de tenofovir alafenamida

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Publication number Publication date
CY1116852T1 (el) 2017-04-05
SMT201500266B (it) 2016-01-08
US20100285122A1 (en) 2010-11-11
AP3250A (en) 2015-05-31
JP2012517432A (ja) 2012-08-02
CL2011001885A1 (es) 2012-05-25
EA030123B1 (ru) 2018-06-29
KR20160093100A (ko) 2016-08-05
EA201190125A1 (ru) 2012-01-30
JP5911927B2 (ja) 2016-04-27
NZ594214A (en) 2013-05-31
US20150150810A1 (en) 2015-06-04
MX2011008289A (es) 2011-09-15
HUE025822T2 (en) 2016-04-28
SI2393485T1 (sl) 2015-10-30
EP2393485B1 (en) 2015-07-29
WO2010091197A3 (en) 2011-06-03
HRP20151009T1 (hr) 2015-10-23
KR101738325B1 (ko) 2017-05-19
IL214227A0 (en) 2011-09-27
IL214227A (en) 2017-01-31
CN102307573A (zh) 2012-01-04
EA021313B1 (ru) 2015-05-29
CN102307573B (zh) 2013-09-11
ECSP11011307A (es) 2011-10-31
KR20110122729A (ko) 2011-11-10
AP2011005857A0 (en) 2011-10-31
JP2014221845A (ja) 2014-11-27
TW201040142A (en) 2010-11-16
AR075369A1 (es) 2011-03-30
SG10201706215UA (en) 2017-08-30
WO2010091197A2 (en) 2010-08-12
PT2393485E (pt) 2015-10-23
PL2393485T3 (pl) 2015-12-31
UY32424A (es) 2010-09-30
ES2548886T3 (es) 2015-10-21
SG173544A1 (en) 2011-09-29
EA201491658A1 (ru) 2015-05-29
HK1164737A1 (en) 2012-09-28
KR101645759B1 (ko) 2016-08-04
SG2014007744A (en) 2014-05-29
AU2010210598A1 (en) 2011-08-25
AU2010210598B2 (en) 2015-03-05
JP5611242B2 (ja) 2014-10-22
EP2393485A2 (en) 2011-12-14
TWI444367B (zh) 2014-07-11
PE20110994A1 (es) 2012-01-24
BRPI1008664A2 (pt) 2016-03-08
CA2750521A1 (en) 2010-08-12

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