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1. WO2011053504 - SOLID PHARMACEUTICAL COMPOSITIONS CONTAINING AN INTEGRASE INHIBITOR

Publication Number WO/2011/053504
Publication Date 05.05.2011
International Application No. PCT/US2010/053507
International Filing Date 21.10.2010
IPC
A01N 43/78 2006.1
AHUMAN NECESSITIES
01AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
NPRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
43Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds
72having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms
74five-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
781,3-Thiazoles; Hydrogenated 1,3-thiazoles
A61K 31/425 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
425Thiazoles
CPC
A61J 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
JCONTAINERS 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
3Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
10into the form of compressed tablets
A61K 2121/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2121Preparations for use in therapy
A61K 31/4245
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
4245Oxadiazoles
A61K 31/506
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing further heterocyclic rings
A61K 31/513
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
513having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Applicants
  • MERCK SHARP & DOHME CORP. [US]/[US] (AllExceptUS)
  • MAHJOUR, Majid [US]/[US] (UsOnly)
  • LI, Feng [US]/[US] (UsOnly)
  • MA, Decheng [US]/[US] (UsOnly)
  • SOTTHIVIRAT, Sutthilug [TH]/[US] (UsOnly)
Inventors
  • MAHJOUR, Majid
  • LI, Feng
  • MA, Decheng
  • SOTTHIVIRAT, Sutthilug
Common Representative
  • MERCK SHARP & DOHME CORP.
Priority Data
61/254,86926.10.2009US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) SOLID PHARMACEUTICAL COMPOSITIONS CONTAINING AN INTEGRASE INHIBITOR
(FR) COMPOSITIONS PHARMACEUTIQUES SOLIDES CONTENANT UN INHIBITEUR D'INTÉGRASE
Abstract
(EN) Compressed tablets for oral administration containing raltegravir in the form of a pharmaceutically acceptable salt are described. The tablets comprise: (A) an intragranular component comprising (i) an effective amount of an alkali metal salt of raltegravir, (ii) optionally a first superdisintegrant, and (iii) a binder; and (B) an extragranular component comprising (i) a second superdisintegrant, (ii) a filler, and (iii) a lubricant. Methods for preparing the tablets and the use of the tablets, optionally in combination with other anti-HIV agents, for the inhibition of HIV integrase, for the treatment or prophylaxis of HIV infection, or for the treatment, delay in the onset, or prophylaxis of AIDS are also described.
(FR) L'invention porte sur des comprimés pour administration orale qui contiennent du raltégravir sous la forme d'un sel de qualité pharmaceutique. Les comprimés comportent : (A) un composant intragranulaire comportant (i) une quantité efficace d'un sel de métal alcalin du raltégravir, (ii) facultativement un premier super délitant et (iii) un liant ; et (B) un composant extragranulaire comportant (i) un second super délitant, (ii) une charge et (iii) un lubrifiant. L'invention porte également sur des procédés qui permettent de préparer les comprimés et sur l'utilisation des comprimés, facultativement en association avec d'autres agents anti-VIH, pour l'inhibition de l'intégrase du VIH, pour le traitement ou la prophylaxie d'une infection à VIH ou pour le traitement, le retardement de l'apparition ou la prophylaxie du SIDA.
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