BR112012009857A8 - Composições farmacêuticas sólidas contendo um inibidor de integrase - Google Patents

Composições farmacêuticas sólidas contendo um inibidor de integrase

Info

Publication number
BR112012009857A8
BR112012009857A8 BR112012009857A BR112012009857A BR112012009857A8 BR 112012009857 A8 BR112012009857 A8 BR 112012009857A8 BR 112012009857 A BR112012009857 A BR 112012009857A BR 112012009857 A BR112012009857 A BR 112012009857A BR 112012009857 A8 BR112012009857 A8 BR 112012009857A8
Authority
BR
Brazil
Prior art keywords
pharmaceutical compositions
compositions containing
solid pharmaceutical
integrase inhibitor
tablets
Prior art date
Application number
BR112012009857A
Other languages
English (en)
Other versions
BR112012009857A2 (pt
Inventor
Mahjour Majid
Li Feng
Ma Decheng
Sotthivirat Sutthilug
Original Assignee
Merck Sharp & Dohme
Merck Sharp & Dohme Llc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43922462&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012009857(A8) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme, Merck Sharp & Dohme Llc filed Critical Merck Sharp & Dohme
Publication of BR112012009857A2 publication Critical patent/BR112012009857A2/pt
Publication of BR112012009857A8 publication Critical patent/BR112012009857A8/pt

Links

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
    • A61K31/41Heterocyclic 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
    • A61K31/4245Oxadiazoles
    • 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
    • A61JCONTAINERS SPECIALLY ADAPTED FOR MEDICAL OR PHARMACEUTICAL PURPOSES; DEVICES OR METHODS SPECIALLY ADAPTED FOR BRINGING PHARMACEUTICAL PRODUCTS INTO PARTICULAR PHYSICAL OR ADMINISTERING FORMS; DEVICES FOR ADMINISTERING FOOD OR MEDICINES ORALLY; BABY COMFORTERS; DEVICES FOR RECEIVING SPITTLE
    • A61J3/00Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
    • A61J3/10Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of compressed tablets
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61K2121/00Preparations for use in therapy
    • 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

Landscapes

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

Abstract

COMPOSIÇÕES FARMACÊUTICAS SÓLIDAS CONTENDO UM INIBIDOR DE INTEGRASE Os tabletes comprimidos para administração oral contendo raltegravir na forma de um sal farmaceuticamente aceitável são descritos. A tabela compreende: (A) um componente intragranular que compreende (i) uma quantidade eficaz de um sal de metal alcalino de raltegravir, (ii) opcionalmente um primeiro superdesintegrante e (iii) um aglutinante e (B) um componente extragranular que compreende (i) um segundo superdesinegrante, (ii) uma carga e (iii) um lubrificante. Os métodos para a preparação de tabletes e para o uso de tabletes, opcionalmente em combinações com outras agentes anti-HIV, para a inibição de HIV integrasse, para o tratamento ou profilaxia de Infecção de HIV ou para o tratamento, atraso no início ou profilaxia da AIDS também são descritos.
BR112012009857A 2009-10-26 2010-10-21 Composições farmacêuticas sólidas contendo um inibidor de integrase BR112012009857A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25486909P 2009-10-26 2009-10-26
PCT/US2010/053507 WO2011053504A1 (en) 2009-10-26 2010-10-21 Solid pharmaceutical compositions containing an integrase inhibitor

Publications (2)

Publication Number Publication Date
BR112012009857A2 BR112012009857A2 (pt) 2015-09-29
BR112012009857A8 true BR112012009857A8 (pt) 2023-04-11

Family

ID=43922462

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012009857A BR112012009857A8 (pt) 2009-10-26 2010-10-21 Composições farmacêuticas sólidas contendo um inibidor de integrase

Country Status (26)

Country Link
US (2) US9649311B2 (pt)
EP (2) EP3970702A1 (pt)
JP (2) JP6122639B2 (pt)
KR (1) KR101835893B1 (pt)
CN (2) CN106074411A (pt)
AU (1) AU2010313571B2 (pt)
BR (1) BR112012009857A8 (pt)
CA (1) CA2777937C (pt)
CO (1) CO6531485A2 (pt)
CY (1) CY1124914T1 (pt)
DK (1) DK2493312T3 (pt)
ES (1) ES2898348T3 (pt)
HR (1) HRP20211826T1 (pt)
HU (1) HUE057248T2 (pt)
IL (1) IL219369A (pt)
IN (1) IN2012DN03377A (pt)
LT (1) LT2493312T (pt)
MX (1) MX345227B (pt)
MY (1) MY162494A (pt)
PL (1) PL2493312T3 (pt)
PT (1) PT2493312T (pt)
RS (1) RS62600B1 (pt)
RU (1) RU2602865C2 (pt)
SI (1) SI2493312T1 (pt)
WO (1) WO2011053504A1 (pt)
ZA (1) ZA201203012B (pt)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2493312T (pt) 2009-10-26 2021-11-25 Merck Sharp & Dohme Composições farmacêuticas sólidas contendo um inibidor de integrase
JP2014512386A (ja) * 2011-04-22 2014-05-22 メルク・シャープ・アンド・ドーム・コーポレーション 味がマスクされたラルテグラビル製剤
WO2014014933A1 (en) * 2012-07-20 2014-01-23 Merck Sharp & Dohme Corp. Hiv treatment with amido-substituted pyrimidinone derivatives
WO2014064711A2 (en) * 2012-10-22 2014-05-01 Hetero Research Foundation Methods of administering raltegravir and raltegravir compositions
MX364901B (es) * 2012-10-23 2019-05-10 Cipla Ltd Composicion farmaceutica antirretroviral.
EP3019468A4 (en) * 2013-07-11 2017-01-11 Merck Sharp & Dohme Corp. Formulations for cathepsin k inhibitors with vitamin d
CN105237526B (zh) * 2014-06-20 2018-01-23 朱靖华 一种抗艾滋病毒药物及其制备方法
JP7023054B2 (ja) * 2017-04-05 2022-02-21 東和薬品株式会社 レベチラセタム含有医薬組成物及びその製造方法
EP3740209A1 (en) * 2018-01-19 2020-11-25 Gilead Sciences, Inc. Metabolites of bictegravir
US20210290548A1 (en) * 2018-06-06 2021-09-23 Merck Sharp & Dohme Corp. Formulations of raltegravir
RU2688235C1 (ru) * 2018-06-19 2019-05-21 Федеральное государственное бюджетное образовательное учреждение высшего образования "Пермский государственный национальный исследовательский университет" Фармацевтическая противодиабетическая композиция на основе замещенного тиофенкарбоксилата и способ её получения

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GB9109862D0 (en) 1991-05-08 1991-07-03 Beecham Lab Sa Pharmaceutical formulations
US6087383A (en) 1998-01-20 2000-07-11 Bristol-Myers Squibb Company Bisulfate salt of HIV protease inhibitor
GB9922963D0 (en) 1999-09-28 1999-12-01 Pfizer Ltd Polymorphic salt
FR2795962B1 (fr) * 1999-07-08 2003-05-09 Prographarm Laboratoires Procede de fabrication de granules enrobes a gout masque et liberation immediate du principe actif
DE60036961T2 (de) 1999-11-24 2008-08-28 Merck & Co., Inc. Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer
CZ20031028A3 (cs) 2000-10-12 2003-08-13 Merck & Co., Inc. Aza- a polyazanaftalenylkarboxamidy
GEP20063848B (en) 2001-10-26 2006-06-12 Inst Di Richerche Di Biolog Moltcolare P Angeletti Spa N-substituted hydroxypyrimi-dinone carboxamide inhibitors of hiv integrase
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EP1499391A2 (en) 2002-04-10 2005-01-26 Merck & Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant
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NZ555120A (en) * 2004-12-03 2009-11-27 Merck & Co Inc Pharmaceutical formulation of carboxamide HIV integrase inhibitors containing a release rate controlling composition
TR201907729T4 (tr) * 2004-12-03 2019-06-21 Merck Sharp & Dohme Bir anti-çekirdekleştirici ajan içeren farmasötik bileşim.
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US8372431B2 (en) * 2007-10-26 2013-02-12 Bial-Portela & C.A., S.A. Pharmaceutical composition comprising licarbazepine acetate
PT2493312T (pt) 2009-10-26 2021-11-25 Merck Sharp & Dohme Composições farmacêuticas sólidas contendo um inibidor de integrase

Also Published As

Publication number Publication date
KR20120102063A (ko) 2012-09-17
RU2012121857A (ru) 2013-12-10
US9649311B2 (en) 2017-05-16
RS62600B1 (sr) 2021-12-31
IL219369A0 (en) 2012-06-28
LT2493312T (lt) 2022-01-10
CN102655752A (zh) 2012-09-05
EP3970702A1 (en) 2022-03-23
CN106074411A (zh) 2016-11-09
HRP20211826T1 (hr) 2022-03-04
ZA201203012B (en) 2012-12-27
HUE057248T2 (hu) 2022-04-28
RU2602865C2 (ru) 2016-11-20
EP2493312A1 (en) 2012-09-05
PT2493312T (pt) 2021-11-25
US20120213851A1 (en) 2012-08-23
DK2493312T3 (da) 2021-12-13
PL2493312T3 (pl) 2022-01-03
CY1124914T1 (el) 2023-01-05
WO2011053504A1 (en) 2011-05-05
US10772888B2 (en) 2020-09-15
KR101835893B1 (ko) 2018-04-19
MY162494A (en) 2017-06-15
AU2010313571B2 (en) 2014-07-31
US20170231993A1 (en) 2017-08-17
AU2010313571A1 (en) 2012-06-07
MX345227B (es) 2017-01-20
MX2012004903A (es) 2012-06-14
CO6531485A2 (es) 2012-09-28
IL219369A (en) 2017-06-29
JP6122639B2 (ja) 2017-04-26
BR112012009857A2 (pt) 2015-09-29
CA2777937C (en) 2017-08-29
IN2012DN03377A (pt) 2015-10-23
CA2777937A1 (en) 2011-05-05
EP2493312A4 (en) 2013-07-10
SI2493312T1 (sl) 2021-12-31
JP2016034962A (ja) 2016-03-17
ES2898348T3 (es) 2022-03-07
EP2493312B1 (en) 2021-10-20
JP2013508395A (ja) 2013-03-07

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Legal Events

Date Code Title Description
B25A Requested transfer of rights approved

Owner name: SCHERING CORPORATION (US)

B25D Requested change of name of applicant approved

Owner name: MERCK SHARP AND DOHME CORP (US)

B25G Requested change of headquarter approved

Owner name: MERCK SHARP AND DOHME CORP (US)

B15K Others concerning applications: alteration of classification

Ipc: A61K 31/425 (2006.01), A01N 43/78 (2006.01)

B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]
B12B Appeal against refusal [chapter 12.2 patent gazette]
B25A Requested transfer of rights approved

Owner name: MERCK SHARP AND DOHME LLC (US)