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1. WO2020194223 - DOXOPHYLLINE DERIVATIVES

Publication Number WO/2020/194223
Publication Date 01.10.2020
International Application No. PCT/IB2020/052846
International Filing Date 26.03.2020
IPC
C07D 473/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
02with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6
04two oxygen atoms
A61P 11/08 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
08Bronchodilators
A61P 29/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A61K 31/522 2006.01
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
519ortho- or peri-condensed with heterocyclic rings
52Purines, e.g. adenine
522having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
CPC
A61P 11/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
08Bronchodilators
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
C07D 473/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
473Heterocyclic compounds containing purine ring systems
02with oxygen, sulfur or nitrogen atoms directly attached in positions 2 and 6
04two oxygen atoms
Applicants
  • ABC FARMACEUTICI S.P.A. [IT]/[IT]
Inventors
  • GIRAUDI, Alberto
  • GIRAUDI, Giovanni
  • CUZZOCREA, Salvatore
  • DI PAOLA, Rosanna
  • GENAZZANI, Armando
  • PIRALI, Tracey
  • SERAFINI, Marta
Agents
  • RAMBELLI, Paolo
  • JACOBACCI, Guido
  • QUINTERNO, Giuseppe
  • GERBINO, Angelo
  • FIORAVANTI, Corrado
  • DEAMBROGI, Edgardo
  • COMOGLIO, Elena
  • VANZINI, Christian
  • RIMINI, Rebecca
  • SAVOCA, Agatino
Priority Data
10201900000434126.03.2019IT
Publication Language English (EN)
Filing Language Italian (IT)
Designated States
Title
(EN) DOXOPHYLLINE DERIVATIVES
(FR) DÉRIVÉS DE DOXOPHYLLINE
Abstract
(EN)
Deuterated doxophylline compounds having the following formula (I), with an improved pharmacokinetic profile and improved activity, are described: Formula (I) wherein: R1 is protium (H) or deuterium (D), independently of each other, provided that at least one of R1 is deuterium (D), and a process for the preparation thereof. The preferred compounds comprise: 7-((1,3-dioxolan-2-yl) methyl-d3)-1,3 -dimethyl-1H-purine-2, 6 (3H,7H)-dione, 7-((1,3 -dioxolan-2-il) methyl-d4)-1,3-dimethyl-1H-purine-2, 6 (3H,7H)-dione, and 7-((1,3 -dioxolan-2-il) methyl-d7)-1,3-dimethyl-1H-purine-2, 6 (3H,7H)-dione.
(FR)
L'invention concerne des composés de doxophylline deutérés de formule suivante (I), ayant un profil pharmacocinétique amélioré et une activité améliorée : Formule (I) : dans laquelle, R1 représente le protium (H) ou le deutérium (D), indépendamment l'un de l'autre, à condition qu'au moins l'un de R1 soit du deutérium (D). L'invention concerne également un procédé de préparation associé. Les composés préférés comprennent : 7-((1,3-dioxolan-2-yl) méthyl-d3)-1,3 -diméthyl-1H-purine-2, 6 (3H,7H)-dione, 7-((1,3 -dioxolan-2-il) méthyl-d4)-1,3-diméthyl-1H-purine-2, 6 (3H,7H)-dione et 7-((1,3 -dioxolan-2-il) méthyl-d7)-1,3-diméthyl-1H-purine-2, 6 (3H,7H)-dione.
Latest bibliographic data on file with the International Bureau