Title:
NOVEL PYRIMIDINE DERIVATIVE HAVING ANTIMALARIAL ACTIVITY
Document Type and Number:
WIPO Patent Application WO/2018/079629
Kind Code:
A1
Abstract:
The present invention provides a novel 2,4,6-substituted pyrimidine derivative, which is a compound represented by formula (I) (in the formula, ring A is a 6-membered heteroaryl group having at least one N atom optionally substituted with R1, R2, and R3; Z is an optionally substituted alkoxy group, an optionally substituted amino group, an optionally substituted heterocycloalkyl group, or an optionally substituted heteroaryl group; and R1, R2, and R3 are each independently selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted heterocycloalkyloxy group, an optionally substituted phenoxy group, an optionally substituted amino group, a nitro group, and a hydroxy group) or a pharmaceutically acceptable salt thereof.
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Inventors:
SAWA MASAAKI (JP)
ASAMITSU YUKO (JP)
UNO YUKO (JP)
OMURA SATOSHI (JP)
OTOGURO KAZUHIKO (JP)
IWATSUKI MASATO (JP)
ISHIYAMA AKI (JP)
HOKARI REI (JP)
ASAMITSU YUKO (JP)
UNO YUKO (JP)
OMURA SATOSHI (JP)
OTOGURO KAZUHIKO (JP)
IWATSUKI MASATO (JP)
ISHIYAMA AKI (JP)
HOKARI REI (JP)
Application Number:
PCT/JP2017/038588
Publication Date:
May 03, 2018
Filing Date:
October 25, 2017
Export Citation:
Assignee:
CARNA BIOSCIENCES INC (JP)
THE KITASATO INST (JP)
THE KITASATO INST (JP)
International Classes:
C07D471/04; A61K31/506; A61K31/5377; A61P33/06; C07D491/056; C07D491/107
Domestic Patent References:
| WO2015165660A1 | 2015-11-05 | |||
| WO2016175264A1 | 2016-11-03 | |||
| WO2015165660A1 | 2015-11-05 |
Other References:
HAMEED, P. S. ET AL.: "Triaminopyrimidine is a fast-killing and long-acting antimalarial clinical candidate", NATURE COMMUNICATIONS, vol. 6, 2015, pages 6715, XP055478762
DENG, X. ET AL.: "Discovery of novel 1H-imidazol-2-yl-pyrimidine-4, 6-diamines as potential antimalarials", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, 2010, pages 4027 - 4031, XP027103977
SHAHUL HAMEED P. ET AL., NAT. COMMUN., vol. 6, 2015, pages 6715
XIANMING DENG ET AL., BIOORG. MED. CHEM. LETT., vol. 20, 2010, pages 4027 - 4031
T. W. GREENE: "Protective Groups in Organic Synthesis", 1999, JOHN WILEY & SONS, INC.
OTOGURO, K.KOHANA, A.MANABE, C.ISHIYAMA, A.UI, H.SHIOMI, K.YAMADA, H.OMURA, S.: "Potent antimalarial activity of polyether antibiotic, X-206", J. ANTIBIOT., vol. 54, 2001, pages 658 - 663
TRAGER, W.JENSEN, J.: "Human malaria parasites in continuous culture", SCIENCE, vol. 193, 1976, pages 673 - 677
DESJARDINS, R. E.CANFIELD, C. J.HAYNES, D. E.CHULAY, J. D.: "Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique", ANTIMICROB. AGENTS CHEMOTHER., vol. 16, 1979, pages 710 - 718, XP008021786
MAKLER, M. T.RISE, J. M.WILLIAMS, J. A.BANCROFT, J. E.PIPER, R. C.GIBBINS, B. L.HINRICHS, D. J.: "Parasite lactate dehydrogenase as an Assay for Plasmodium falciparum drug sensitivity", AM. J. MED. HYG., vol. 48, 1993, pages 739 - 741
PETERS, W.PORTUS, J. H.ROBINSON, B. L.: "The chemotherapy of rodent malaria. XXII. The value of drug-resistant strains of P. berghei in Screening for blood schizonticidal activity", ANN. TROP. MED. PARASITOL., vol. 69, 1975, pages 155 - 171
See also references of EP 3533795A4
DENG, X. ET AL.: "Discovery of novel 1H-imidazol-2-yl-pyrimidine-4, 6-diamines as potential antimalarials", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, 2010, pages 4027 - 4031, XP027103977
SHAHUL HAMEED P. ET AL., NAT. COMMUN., vol. 6, 2015, pages 6715
XIANMING DENG ET AL., BIOORG. MED. CHEM. LETT., vol. 20, 2010, pages 4027 - 4031
T. W. GREENE: "Protective Groups in Organic Synthesis", 1999, JOHN WILEY & SONS, INC.
OTOGURO, K.KOHANA, A.MANABE, C.ISHIYAMA, A.UI, H.SHIOMI, K.YAMADA, H.OMURA, S.: "Potent antimalarial activity of polyether antibiotic, X-206", J. ANTIBIOT., vol. 54, 2001, pages 658 - 663
TRAGER, W.JENSEN, J.: "Human malaria parasites in continuous culture", SCIENCE, vol. 193, 1976, pages 673 - 677
DESJARDINS, R. E.CANFIELD, C. J.HAYNES, D. E.CHULAY, J. D.: "Quantitative assessment of antimalarial activity in vitro by a semiautomated microdilution technique", ANTIMICROB. AGENTS CHEMOTHER., vol. 16, 1979, pages 710 - 718, XP008021786
MAKLER, M. T.RISE, J. M.WILLIAMS, J. A.BANCROFT, J. E.PIPER, R. C.GIBBINS, B. L.HINRICHS, D. J.: "Parasite lactate dehydrogenase as an Assay for Plasmodium falciparum drug sensitivity", AM. J. MED. HYG., vol. 48, 1993, pages 739 - 741
PETERS, W.PORTUS, J. H.ROBINSON, B. L.: "The chemotherapy of rodent malaria. XXII. The value of drug-resistant strains of P. berghei in Screening for blood schizonticidal activity", ANN. TROP. MED. PARASITOL., vol. 69, 1975, pages 155 - 171
See also references of EP 3533795A4
Attorney, Agent or Firm:
SAMEJIMA, Mutsumi et al. (JP)
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