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NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME

外国特許コード F160008835
整理番号 (S2015-0178-N0)
掲載日 2016年8月18日
出願国 世界知的所有権機関(WIPO)
国際出願番号 2015JP085590
国際公開番号 WO 2016098904
国際出願日 平成27年12月18日(2015.12.18)
国際公開日 平成28年6月23日(2016.6.23)
優先権データ
  • 特願2014-257451 (2014.12.19) JP
発明の名称 (英語) NOVEL BISPHOSPHONIC ACID DERIVATIVE AND APPLICATION FOR SAME
発明の概要(英語) 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.
特許請求の範囲(英語) [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.
  • 出願人(英語)
  • ※2012年7月以前掲載分については米国以外のすべての指定国
  • NAGASAKI UNIVERSITY
  • KYOTO UNIVERSITY
  • 発明者(英語)
  • TANAKA YOSHIMASA
  • MATSUMOTO KENJI
  • HAYASHI KOSUKE
  • SAKAI YUKI
  • MINATO NAGAHIRO
国際特許分類(IPC)
指定国 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
上記の特許・技術に関心のある方は、下記問い合わせ先にご相談下さい。

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