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1. WO2011001113 - NOVEL 1,2,3,4-TETRAHYDRO-PYRIMIDO(1,2-A)PYRIMIDIN-6-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF

Publication Number WO/2011/001113
Publication Date 06.01.2011
International Application No. PCT/FR2010/051374
International Filing Date 01.07.2010
IPC
C07D 487/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
487Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/-C07D477/183
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/519 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
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
C07D 239/06 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
06having one double bond between ring members or between a ring member and a non-ring member
C07D 239/42 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
32One oxygen, sulfur or nitrogen atom
42One nitrogen atom
CPC
A61K 31/519
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
519ortho- or peri-condensed with heterocyclic rings
A61K 31/5377
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
535having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
53751,4-Oxazines, e.g. morpholine
5377not condensed and containing further heterocyclic rings, e.g. timolol
A61P 3/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
A61P 33/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
33Antiparasitic agents
A61P 33/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
33Antiparasitic agents
02Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
Applicants
  • SANOFI [FR]/[FR] (AllExceptUS)
  • BACQUE, Eric [FR]/[FR] (UsOnly)
  • BROLLO, Maurice [FR]/[FR] (UsOnly)
  • CLAUSS, Annie [FR]/[FR] (UsOnly)
  • EL AHMAD, Youssef [FR]/[FR] (UsOnly)
  • FILOCHE-ROMMÉ, Bruno [FR]/[FR] (UsOnly)
  • HALLEY, Frank [FR]/[FR] (UsOnly)
  • KARLSSON, Karl Andreas [SE]/[FR] (UsOnly)
  • MARCINIAK, Gilbert [FR]/[FR] (UsOnly)
  • RONAN, Baptiste [FR]/[FR] (UsOnly)
  • SCHIO, Laurent [FR]/[FR] (UsOnly)
  • VIVET, Bertrand [FR]/[FR] (UsOnly)
  • VIVIANI, Fabrice [FR]/[FR] (UsOnly)
  • ZIMMERMANN, André [FR]/[FR] (UsOnly)
Inventors
  • BACQUE, Eric
  • BROLLO, Maurice
  • CLAUSS, Annie
  • EL AHMAD, Youssef
  • FILOCHE-ROMMÉ, Bruno
  • HALLEY, Frank
  • KARLSSON, Karl Andreas
  • MARCINIAK, Gilbert
  • RONAN, Baptiste
  • SCHIO, Laurent
  • VIVET, Bertrand
  • VIVIANI, Fabrice
  • ZIMMERMANN, André
Agents
  • BOURGOUIN MULLER, Alessandra
Priority Data
090323702.07.2009FR
095706909.10.2009FR
61/241,09810.09.2009US
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) NOVEL 1,2,3,4-TETRAHYDRO-PYRIMIDO(1,2-A)PYRIMIDIN-6-ONE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF
(FR) NOUVEAUX DERIVES DE 1,2,3,4-TETRAHYDRO-PYRIMIDO{1,2-a}PYRIMIDIN-6-ONE,LEUR PREPARATION ET LEUR UTILISATION PHARMACEUTIQUE
Abstract
(EN)
The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted L-aryl or –L-heteroaryl, such that L is a single bond, alkyl, CO, or CO-alk, or L’-X, with L’ being an alkyl and X being O or S; R2 is H or alkyl; R3 is an alkyl optionally substituted by Hal; and R4 is Hou Hal, wherein said materials are in any isomeric form and the salts thereof, to be used as drugs.
(FR)
L'invention concerne les nouveaux produits de formule (I): dans laquelle R1 représente L-aryle ou -L-hétéroaryle éventuellement substitués, tel que L représente simple liaison, alkyle,CO ou CO-alk ou L'-X avec L' représente alkyle et X représente O ou S; R2 représente H ou alkyle; R3 représente alkyle éventuellement substitué par Hal; R4 représente Hou Hal; ces produits étant sous toutes les formes isomères et les sels, à titre de médicaments.
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