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1. WO2015073476 - INHIBITORS OF INFLUENZA VIRUSES REPLICATION

Publication Number WO/2015/073476
Publication Date 21.05.2015
International Application No. PCT/US2014/065114
International Filing Date 12.11.2014
IPC
C07D 403/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 471/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/506 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
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
506not condensed and containing 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
  • NTI-ADDAE, Kwame, W.
  • WALDO, Michael
  • O'NEIL, Simon, Adam
  • VAN ALSTEN, John, Gregg
  • MACIKENAS, Dainius
  • MUDUNURI, Praveen
  • SHI, Yi
  • LEDEBOER, Mark, Willem
  • JURKAUSKAS, Valdas
  • MEDEK, Ales
  • JONES, Steven
  • BYRN, Randal
  • ASMAL, Mohammed
  • ROBERTSON, Sarah, Marie
  • TSAI, Wanjung
Agents
  • WEBER, Andrew, N.
Priority Data
61/903,57213.11.2013US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) INHIBITORS OF INFLUENZA VIRUSES REPLICATION
(FR) INHIBITEURS DE LA RÉPLICATION DES VIRUS DE LA GRIPPE
Abstract
(EN) Polymorphic forms of Compound (1) or a pharmaceutically acceptable salt thereof, wherein Compound (1) is represented by the following structural formula: are Form A of HCl salt of Compound (1)·1/2Η20, Form F of HCl salt of Compound (1)·3Η20, Form D of HCl salt of Compound (1), Form A of Compound (1), and Form A of tosylate salt of Compound (1). Such polymorphic forms are employed for treating influenza, inhibiting the replication of influenza viruses, or reducing the amount of influenza viruses in a biological sample or in a subject.
(FR) L'invention porte sur des formes polymorphes de composé (1) ou d'un sel pharmaceutiquement acceptable de ce dernier, le composé (1) étant représenté par la formule développée suivante : qui sont la forme A du sel HCl de composé (1) ·1/2Η20, la forme F du sel HCl de composé (1) ·3Η20, la forme D du sel HCl de composé (1), la forme A du composé (1) et la forme A du sel tosylate de composé (1). Ces formes polymorphes sont utilisées pour traiter la grippe, inhiber la réplication des virus de la grippe ou réduire la quantité de virus de la grippe dans un échantillon biologique ou chez un sujet.
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