CA2847871C - Methods for improving the pharmacokinetics of hiv integrase inhibitors - Google Patents

Methods for improving the pharmacokinetics of hiv integrase inhibitors Download PDF

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Publication number
CA2847871C
CA2847871C CA2847871A CA2847871A CA2847871C CA 2847871 C CA2847871 C CA 2847871C CA 2847871 A CA2847871 A CA 2847871A CA 2847871 A CA2847871 A CA 2847871A CA 2847871 C CA2847871 C CA 2847871C
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Canada
Prior art keywords
compound
administration
patient
food
pharmaceutically acceptable
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Active
Application number
CA2847871A
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English (en)
French (fr)
Other versions
CA2847871A1 (en
Inventor
Brian P. Kearney
Atsuyuki Kakee
Isao Kawaguchi
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Japan Tobacco Inc
Gilead Sciences Inc
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Japan Tobacco Inc
Gilead Sciences Inc
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Publication of CA2847871A1 publication Critical patent/CA2847871A1/en
Application granted granted Critical
Publication of CA2847871C publication Critical patent/CA2847871C/en
Active legal-status Critical Current
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Classifications

    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425Thiazoles
    • A61K31/4261,3-Thiazoles
    • 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
    • A61K31/47042-Quinolinones, e.g. carbostyril
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CA2847871A 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors Active CA2847871C (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US75503905P 2005-12-30 2005-12-30
US60/755,039 2005-12-30
US75663106P 2006-01-06 2006-01-06
US60/756,631 2006-01-06
US76390106P 2006-02-01 2006-02-01
US60/763,901 2006-02-01
CA2635468A CA2635468C (en) 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CA2635468A Division CA2635468C (en) 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
CA2847871A1 CA2847871A1 (en) 2007-07-12
CA2847871C true CA2847871C (en) 2016-07-26

Family

ID=38016698

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2635468A Active CA2635468C (en) 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors
CA2847871A Active CA2847871C (en) 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CA2635468A Active CA2635468C (en) 2005-12-30 2006-12-29 Methods for improving the pharmacokinetics of hiv integrase inhibitors

Country Status (16)

Country Link
US (1) US20070219243A1 (enExample)
EP (2) EP1976517A1 (enExample)
JP (1) JP4676536B2 (enExample)
KR (3) KR20160074018A (enExample)
CN (1) CN104069108A (enExample)
AP (1) AP2702A (enExample)
AU (1) AU2006332664B2 (enExample)
BR (1) BRPI0620865A2 (enExample)
CA (2) CA2635468C (enExample)
EA (2) EA018544B1 (enExample)
HR (1) HRP20080313A2 (enExample)
IL (1) IL192208A (enExample)
NO (1) NO20083333L (enExample)
NZ (1) NZ569576A (enExample)
SG (2) SG170796A1 (enExample)
WO (1) WO2007079260A1 (enExample)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
EP2118082B1 (en) 2007-02-23 2014-10-01 Gilead Sciences, Inc. Modulators of pharmacokinetic properties of therapeutics
CA2692101A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Combination of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and a compound that inhibits a ugt pathway or ugt metabolism
AU2008270634B2 (en) * 2007-06-29 2014-01-16 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
GB2470494B (en) * 2008-01-17 2012-08-08 Univ Holy Ghost Duquesne Antiretroviral drug formulations for treatment of children exposed to HIV/AIDS
EA032868B1 (ru) * 2010-01-27 2019-07-31 Вайв Хелткер Компани Комбинация для лечения вич-инфекции
US8703786B2 (en) * 2011-12-07 2014-04-22 Texas Southern University Etravirine formulations and uses thereof
MX344879B (es) 2012-12-21 2017-01-11 Gilead Sciences Inc Compuestos de carbamoilpiridona policiclicos y su uso farmaceutico.
LT3019503T (lt) 2013-07-12 2017-11-27 Gilead Sciences, Inc. Policikliniai karbamoilpiridono junginiai ir jų panaudojimas živ infekcijų gydymui
NO2865735T3 (enExample) 2013-07-12 2018-07-21
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
LT3236972T (lt) 2014-12-26 2021-11-10 Emory University Antivirusiniai n4-hidroksicitidino dariniai
CA2980362C (en) 2015-04-02 2020-02-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
KR102606625B1 (ko) 2015-11-09 2023-11-27 길리애드 사이언시즈, 인코포레이티드 인간 면역결핍 바이러스의 치료를 위한 치료 조성물
LT3706762T (lt) 2017-12-07 2024-12-27 Emory University N4-hidroksicitidinas ir jo dariniai bei susiję naudojimo prieš virusus būdai

Family Cites Families (23)

* Cited by examiner, † Cited by third party
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US5696270A (en) 1989-05-23 1997-12-09 Abbott Laboratories Intermediate for making retroviral protease inhibiting compounds
US5354866A (en) 1989-05-23 1994-10-11 Abbott Laboratories Retroviral protease inhibiting compounds
EP1090914B1 (en) * 1992-12-29 2003-01-02 Abbott Laboratories Retroviral protease inhibiting compounds
US5567823A (en) 1995-06-06 1996-10-22 Abbott Laboratories Process for the preparation of an HIV protease inhibiting compound
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
CA2371109C (en) * 1999-06-04 2011-04-26 Laman A. Alani Improved pharmaceutical formulations
US6541515B2 (en) * 2000-08-09 2003-04-01 Merck & Co., Inc. HIV integrase inhibitors
US6407128B1 (en) * 2001-12-03 2002-06-18 Elan Pharmaceuticals, Inc. Method for increasing the bioavailability of metaxalone
AR037797A1 (es) * 2001-12-12 2004-12-01 Tibotec Pharm Ltd Combinacion de inhibidores de proteasa dependientes del citocromo p450
AU2003301439A1 (en) 2002-10-16 2004-05-04 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
JP3567162B1 (ja) * 2002-11-20 2004-09-22 日本たばこ産業株式会社 4−オキソキノリン化合物及びそのhivインテグラーゼ阻害剤としての利用
SI1564210T1 (sl) * 2002-11-20 2010-01-29 Japan Tobacco Inc 4-oksokinolinske spojine in njihova uporaba kot inhibitorji HIV integraze
CA2513141A1 (en) * 2003-01-27 2004-08-12 Pfizer Inc. Hiv-integrase inhibitors, pharmaceutical compositions, and methods for their use
JP2006528694A (ja) 2003-05-13 2006-12-21 スミスクライン ビーチャム コーポレーション ナフチリジンインテグラーゼインヒビター
WO2005113509A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
MY134672A (en) * 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
EP1891089B1 (en) * 2005-06-02 2014-11-05 Merck Sharp & Dohme Corp. HCV protease inhibitors in combination with food
US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
CN105503721A (zh) * 2006-09-12 2016-04-20 吉里德科学公司 制备整合酶抑制剂的方法和中间体
CA2692101A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Combination of 6-(3-chloro-2-fluorobenzyl)-1-[(2s)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and a compound that inhibits a ugt pathway or ugt metabolism
AU2008270634B2 (en) * 2007-06-29 2014-01-16 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
AR068403A1 (es) * 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa

Also Published As

Publication number Publication date
AP2008004522A0 (en) 2008-06-30
CA2635468A1 (en) 2007-07-12
KR20140082858A (ko) 2014-07-02
JP4676536B2 (ja) 2011-04-27
WO2007079260A9 (en) 2007-08-30
JP2009525265A (ja) 2009-07-09
EA200801619A1 (ru) 2008-10-30
SG170795A1 (en) 2011-05-30
KR20160074018A (ko) 2016-06-27
CA2847871A1 (en) 2007-07-12
EA201201496A1 (ru) 2013-07-30
HRP20080313A2 (en) 2008-11-30
AU2006332664B2 (en) 2013-03-14
EA018544B1 (ru) 2013-08-30
EP1976517A1 (en) 2008-10-08
SG170796A1 (en) 2011-05-30
CA2635468C (en) 2016-08-09
NZ569576A (en) 2011-09-30
IL192208A0 (en) 2009-02-11
EP2308490A1 (en) 2011-04-13
AU2006332664A1 (en) 2007-07-12
AP2702A (en) 2013-07-23
WO2007079260A1 (en) 2007-07-12
US20070219243A1 (en) 2007-09-20
IL192208A (en) 2013-10-31
BRPI0620865A2 (pt) 2011-11-29
CN104069108A (zh) 2014-10-01
NO20083333L (no) 2008-09-29
KR20080081358A (ko) 2008-09-09
KR101524165B1 (ko) 2015-06-01

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Effective date: 20140328