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1. WO2015073491 - FORMULATIONS OF AZAINDOLE COMPOUNDS

Publication Number WO/2015/073491
Publication Date 21.05.2015
International Application No. PCT/US2014/065144
International Filing Date 12.11.2014
IPC
A61K 45/06 2006.1
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/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/497 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
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
4965Non-condensed pyrazines
497containing further heterocyclic rings
A61P 31/16 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
31Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
12Antivirals
14for RNA viruses
16for influenza or rhinoviruses
CPC
A61K 2300/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
2300Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
A61K 31/16
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
16Amides, e.g. hydroxamic acids
A61K 31/215
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
21Esters, e.g. nitroglycerine, selenocyanates
215of carboxylic acids
A61K 31/351
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
335having oxygen as the only ring hetero atom, e.g. fungichromin
35having six-membered rings with one oxygen as the only ring hetero atom
351not condensed with another ring
A61K 31/437
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
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
437the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4965
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
4965Non-condensed pyrazines
Applicants
  • VERTEX PHARMACEUTICALS INCORPORATED [US]/[US]
Inventors
  • SIMONE, Eric, Arthur
  • SANGHVI, Tapan
  • BANDA, Alamelu
  • STAVROPOULOS, Katherine
Agents
  • WEBER, Andrew, N.
Priority Data
61/903,84013.11.2013US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) FORMULATIONS OF AZAINDOLE COMPOUNDS
(FR) FORMULATIONS DE COMPOSÉS AZA-INDOLE
Abstract
(EN) A pharmaceutical composition comprises: a) 5 wt% to 95 wt% of a HC1 salt of Compound (1)·χΗ20 by the weight of the pharmaceutical composition, wherein x is from 0 to 3; and b) 5 wt% to 95 wt% of a filler by the weight of the pharmaceutical composition. Another pharmaceutical composition comprises: a) 1 mg/mL to 20 mg/mL of Compound (1) in water; and b) 0.01 M to 0.1 M of a pharmaceutically acceptable pH modifier. A method of preparing a pharmaceutical composition, comprising providing a mixture of Compound (1) that includes the HC1 salt of Compound (1)·χΗ20 and the filler. Another method of preparing a pharmaceutical composition comprises mixing the HC1 salt of Compound (1)·χ¾0 and the pH modifier to form 1 mg/mL to 20 mg/mL of Compound (1) in water. Methods of reducing the amount of influenza viruses, inhibiting the replication of influenza viruses, and treating influenza each independently employ such pharmaceutical compositions.
(FR) L'invention concerne une composition pharmaceutique comprenant : a) 5 % en poids à 95 % en poids d'un sel HC1 du composé (1)·χΗ2O par rapport au poids de la composition pharmaceutique, x valant 0 à 3 ; et b) 5 % en poids à 95 % en poids d'une charge par rapport au poids de la composition pharmaceutique. Une autre composition pharmaceutique comprend : a) 1 mg/ml à 20 mg/ml du composé (1) dans l'eau ; et b) 0,01 M à 0,1 M d'un agent pharmaceutiquement acceptable de modification du pH. L'invention concerne également un procédé pour préparer une composition pharmaceutique, comprenant l'utilisation d'un mélange du composé (1) qui comprend le sel HC1 du composé (1)·χΗ20 et la charge. Un autre procédé de préparation d'une composition pharmaceutique comprend le mélange du sel HC1 du composé (1)·χ¾O et de l'agent de modification du pH pour former 1 mg/ml à 20 mg/ml de composé (1) dans l'eau. Des procédés pour réduire la quantité de virus de la grippe, inhiber la réplication des virus de la grippe et traiter la grippe utilisent, chacun indépendamment, ces compositions pharmaceutiques
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