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ANTIMALARIAL meetings

Foreign code F160008823
File No. (S2015-0073-N0)
Posted date Aug 10, 2016
Country WIPO
International application number 2015JP079511
International publication number WO 2016063848
Date of international filing Oct 20, 2015
Date of international publication Apr 28, 2016
Priority data
  • P2014-214605 (Oct 21, 2014) JP
  • P2014-214606 (Oct 21, 2014) JP
Title ANTIMALARIAL meetings
Abstract Provided is an antimalarial that effectively acts against malaria caused by Plasmodium infection, particularly chloroquine-resistant and/or artemisinin-resistant Plasmodium infection. Further provided is an antimalarial with which the efficacy of an active ingredient is effectively sustainable. The antimalarial contains a peroxide derivative represented by general formula (I) or pharmaceutically acceptable salt thereof as the active ingredient. When used in the form of a percutaneous absorption-type pharmaceutical preparation, the antimalarial acts effectively against malaria because the active ingredient gradually moves into the blood and the effective plasma concentration is sustainable for 12 hours or longer. (In the formula, C is an optionally substituted alicyclic hydrocarbon group and n is an integer of 0 to 6.)
Scope of claims [claim1]
1. The Pell oxide derivative which is displayed with general formula (i) below or the pharmacy it includes the salt which is allowed as the active ingredient the chloroquine and/or the anti- malarial medicine which is effective to the tolerance plasmodium for [atemishinin].
[In formula, as for C the fat cyclic hydrocarbon ring basis which it is good substituting, n shows the integer of the 1-6, R is the hydrogen atom or the hydroxy alkyl group. ]
[claim2]
2. The chloroquine and/or the tolerance plasmodium for [atemishinin], the chloroquine and/or is Plasmodium falciparum of the tolerance for [atemishinin], in claim 1 the anti- malarial medicine of statement.
[claim3]
3. The Pell oxide derivative which is displayed with general formula (i) below or the pharmacy it includes the salt which is allowed as the active ingredient the anti- malarial medicine which consists of the dermal absorption type formulation where the particular active ingredient is prescribed the effective quantity dermally.
[In formula, as for C the fat cyclic hydrocarbon ring basis which it is good substituting, n shows the integer of the 1-6, R is the hydrogen atom or the hydroxy alkyl group. ]
[claim4]
4. The Pell oxide derivative, in general formula (i), C is the fat cyclic hydrocarbon ring basis which is good possessing the low-grade alkyl group as a substituent, in either of the claim 1-3 the anti- malarial medicine of statement.
[claim5]
5. The Pell oxide derivative, in general formula (i), C ***4-tert-buchirushikurohekishiriden, is the [shikurododeshiriden] or [adamanchiriden] basis, n is the 1-4, in claim 4 in statement the anti- malarial medicine of statement.
[claim6]
6. The Pell oxide derivative, is the chemical compound which is shown with formula (ii) or formula (iii) below, in claim 4 the anti- malarial medicine of statement.
[claim7]
7. The Pell oxide derivative as a active ingredient or the pharmacy the effective quantity of the salt which is allowed, is the quantity where density in the blood plasma 12 hours can maintain 3-15 ng/mL at least, in either of the claim 3-6 the anti- malarial medicine of statement.
[claim8]
8. The Pell oxide derivative as a active ingredient or the pharmacy the dosage quantity per 1 times of the salt which is allowed is 10-150 mg/kg, in either of the claim 3-7 the anti- malarial medicine of statement.
[claim9]
9. 10-150 mg/kg 1 days 1 time or 2 times it depends on prescribing the Pell oxide derivative as the active ingredient or the pharmacy as the dosage quantity per 1 times of the salt which is allowed, in claim 7 or 8 the anti- malarial medicine of statement.
[claim10]
10. It is something which at least possesses the dermal dosage form of 1 where it is selected from the group which consists of the ointment medicine, the liquid medicine, the emulsion, the suspension medicine, the cream medicine, the tape medicine, the sticking medicine, the micro needle medicine, the spray medicine and the gel medicine kinds, in either of the claim 1-9 the anti- malarial medicine of statement.
[claim11]
11. Prevention of the malaria which the Pell oxide derivative the anti- malarial medicine of statement, as a active ingredient or the pharmacy features that the quantity where density in the blood plasma of the salt which is allowed 12 hours can maintain 3-15 ng/mL at least is prescribed, dermally in either of the claim 3-6, originates in the infection of the plasmodium and/or remedy method.
[claim12]
12. The Pell oxide derivative as a active ingredient or the pharmacy the salt which is allowed, 10-150 mg/kg 1 days 1 time or 2 times it features that it prescribes, in claim 11 prevention of the malaria of statement and/or remedy method.
[claim13]
13. The plasmodium, the chloroquine and/or is the tolerance plasmodium for [atemishinin], in claim 11 or 12 prevention of the malaria of statement and/or remedy method.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • OKAYAMA UNIVERSITY
  • Inventor
  • KIM HYE-SOOK
  • WATAYA YUSUKE
  • SATO AKIRA
  • DOI HIROYUKI
IPC(International Patent Classification)
Specified countries National States: AE AG AL AM AO AT AU AZ BA BB BG BH BN BR BW BY BZ CA CH CL CN CO CR CU CZ DE DK DM DO DZ EC EE EG ES FI GB GD GE GH GM GT HN HR HU ID IL IN IR IS JP KE KG KN KP KR KZ LA LC LK LR LS LU LY MA MD ME MG MK MN MW MX MY MZ NA NG NI NO NZ OM PA PE PG PH PL PT QA RO RS RU RW SA SC SD SE SG SK SL SM ST SV SY TH TJ TM TN TR TT TZ UA UG US UZ VC VN ZA ZM ZW
ARIPO: BW GH GM KE LR LS MW MZ NA RW SD SL SZ TZ UG ZM ZW
EAPO: AM AZ BY KG KZ RU TJ TM
EPO: AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
OAPI: BF BJ CF CG CI CM GA GN GQ GW KM ML MR NE SN ST TD TG

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