Top > Search of International Patents > NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME

NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME

Foreign code F160008835
File No. (S2015-0178-N0)
Posted date Aug 18, 2016
Country WIPO
International application number 2015JP085590
International publication number WO 2016098904
Date of international filing Dec 18, 2015
Date of international publication Jun 23, 2016
Priority data
  • P2014-257451 (Dec 19, 2014) JP
Title NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME
Abstract This novel bisphosphonic acid derivative, which has a heterocyclic group containing a heterocyclic group-substituted amino group or a nitrogen atom, the acid moiety being esterified by a POM group or a n-butanoyloxymethyl (BuOM) group, and which is represented by the following general formula (1): Y-Cy-(NH)m-(CH2)n-C(X) (PO(OR1) (OR2))2 (1) (where the symbols are defined in the description) exhibits excellent direct and indirect cytopathic effect against tumor cells and virus-infected cells.
Scope of claims [claim1]
1. The below-mentioned general formula (1):
Y-Cy- (NH) m - (CH 2) n - C (X) (PO (OR 1) (OR 2))2 (1)
(In formula, Cy is the phenyl group or complex ring basis, Y the hydrogen atom, the alkyl group and the halogen atom, the halogenation alkyl group, hydroxyl group, the halogen atom or the aryl basis which is possible to be substituted with alkoxy group, or, is the aralkyl oxy basis, X is the hydrogen atom or hydroxyl group, R 1 and R 2, differing identically or mutually, is the hydrogen atom or the alkyl carbonyl oxy alkyl group, R 1 and R 2 one is the alkyl carbonyl oxy alkyl group at least, m displays the quantity of 0 or 1, n displays the integer of the 1-6, (however, Cy2 - It is the [pirijiru] basis, m is 1, n is 1, X is the hydrogen atom, Y is the hydrogen atom, R 1 and the case where R 2 is [pibaroiruokishimechiru] is excluded))
So the bis phosphon acid ester derivative which is displayed.
[claim2]
2. In general system (1), Cy is phenyl group, the derivative of claim 1 statement.
[claim3]
3. In general system (1), the 1-3 where Cy is chosen from the nitrogen atom, the sulfur atom and the oxygen atom it is the complex ring basis of the 5-10 member ring to which includes the atom, the derivative of claim 1 statement.
[claim4]
4. In general system (1), it is the complex ring basis of 5 or 6 member rings which include 1 or 2 atoms where Cy is chosen from the nitrogen atom and the sulfur atom, the derivative of claim 1 statement.
[claim5]
5. In general system (1), Cy the [chiazoriru] basis, the [pirijiru] basis and the [pirimijiru] basis, or 7 - is the [azaindoriru] basis, the derivative of claim 1 statement.
[claim6]
6. In general system (1), X is the hydrogen atom, Y the hydrogen atom, C 1-3 alkyl group, the halogen atom, is the halogenation alkyl group or phenyl group, R (1) and R (2) is C 2-7 alkyl carbonyl oxy - C 1-3 alkyl group, either of the claim 1-5 in 1 sections the derivative of statement.
[claim7]
7. In general system (1), Cy is the [chiazoriru] basis or the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 is the alkyl carbonyl oxy alkyl group, the derivative of claim 1 statement.
[claim8]
8. In general system (1), Cy is the [chiazoriru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 is the alkyl carbonyl oxy alkyl group, the derivative of claim 1 statement.
[claim9]
9. In general system (1), Cy is the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 is the alkyl carbonyl oxy alkyl group, in claim 1 the derivative of statement.
[claim10]
10. In general system (1), Cy is the [chiazoriru] basis or the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 [pibaroiruokishimechiru] (POM) is the basis, the derivative of claim 1 statement.
[claim11]
11. In general system (1), Cy is the [chiazoriru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 [pibaroiruokishimechiru] (POM) is the basis, the derivative of claim 1 statement.
[claim12]
12. In general system (1), Cy is the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 [pibaroiruokishimechiru] (POM) is the basis, the derivative of claim 1 statement.
[claim13]
13. In general system (1), Cy is the [chiazoriru] basis or the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 butanoyl oxy methyl (BuOM) is the basis, the derivative of claim 1 statement.
[claim14]
14. In general system (1), Cy is the [chiazoriru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 butanoyl oxy methyl (BuOM) is the basis, the derivative of claim 1 statement.
[claim15]
15. In general system (1), Cy is the [pirimijiru] basis, X is the hydrogen atom, Y is the hydrogen atom or the halogen atom, R 1 and R 2 butanoyl oxy methyl (BuOM) is the basis, the derivative of claim 1 statement.
[claim16]
16. Either of the claim 1-15 the medicine composition which includes the derivative of statement in 1 sections as the active ingredient.
[claim17]
17. Either of the claim 1-15 in 1 sections the derivative of statement and the medicine composition which includes alkylation [shikurodekisutorin].
[claim18]
18. Alkylation [shikurodekisutorin] [torimechiru] - is β-shikurodekisutorin, the medicine composition of claim 17 statement.
[claim19]
19. It is the anti- tumor cell medicine, either of the claim 16-18 in 1 sections the medicine composition of statement.
[claim20]
20. It is the anti- virus infection cell medicine, either of the claim 16-18 in 1 sections the medicine composition of statement.
[claim21]
21. It is the lymphocyte treatment agent, either of the claim 16-18 in 1 sections the medicine composition of statement.
[claim22]
22. The process which mixes the difficult water soluble medicine in the water soluble organic solvent which melts process, and alkylation [shikurodekisutorin] which melt alkylation [shikurodekisutorin] in the water soluble organic solvent is included, the method the difficult water soluble medicine being made to melt in the solvent.
[claim23]
23. The difficult water soluble medicine is the bis phosphon acid ester derivative, method of claim 22 statement.
[claim24]
24. The bis phosphon acid ester derivative, either of the claim 1-15 is the derivative of statement in 1 sections, in claim 23 method of statement.
[claim25]
25. Alkylation [shikurodekisutorin] [torimechiru] - is β-shikurodekisutorin, either of the claim 22-24 in 1 sections method of statement.
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • NAGASAKI UNIVERSITY
  • KYOTO UNIVERSITY
  • Inventor
  • TANAKA YOSHIMASA
  • MATSUMOTO KENJI
  • HAYASHI KOSUKE
  • SAKAI YUKI
  • MINATO NAGAHIRO
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
We are looking for any manufacturer or licensee. Please contact us if you are interested in this patent.

PAGE TOP

close
close
close
close
close
close