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AGENT FOR KILLING HIV-1-INFECTED CELL AND APPLICATION THEREOF

Foreign code F160008850
File No. (S2015-0401-N0)
Posted date Sep 23, 2016
Country WIPO
International application number 2016JP051768
International publication number WO 2016117666
Date of international filing Jan 22, 2016
Date of international publication Jul 28, 2016
Priority data
  • P2015-011506 (Jan 23, 2015) JP
  • P2015-119111 (Jun 12, 2015) JP
Title AGENT FOR KILLING HIV-1-INFECTED CELL AND APPLICATION THEREOF
Abstract The present invention pertains to: an agent for killing HIV-1-infected cells, the agent containing a compound shown by formula (I): (in the formula, Ar1 and Ar2 are the same or different, and are optionally substituted aromatic groups; X is -CH2O- or -CH=CH-), a salt thereof, or a solvate of these; and a combination formulation for simultaneous, separate, or sequential administration in the treatment or prevention of HIV-1 infection, wherein the combination formulation contains two separate formulations: (a) a formulation including a compound shown by formula (I), a salt thereof, or a solvate of these, and (b) a formulation including an anti-HIV-1 drug.
Outline of related art and contending technology BACKGROUND ART
2013 All over the world in the year individuals infected HIV-1 million people have about 3,500, about 210 million new HIV-1 infected persons and as high as, the infection may be HIV-1, still, worldwide major public health problem.
However, the present anti-HIV-1 agents, growth can be inhibited HIV-1 is, infected HIV-1 infected cells in the patient body cannot be eliminated more effectively. Therefore, the lifetime of the infected persons HIV-1 HIV-1 anti-over must be taking drugs, anti-HIV-1 to long-term ingestion by chronic toxicity of the drug in the drug-resistance HIV-1 problem due to the appearance. Therefore, the current, of the complete HIV-1 infection therapy development is increasingly required. In addition, about 40 year treatment period when the provisional, individuals infected with HIV-1 medical care cost is about 1 million yen per person and such social medical care cost is expensive and causes a significant problem, the development of HIV-1 radical therapy has been desired from around the world.
A complete cure of the infection HIV-1 are difficult HIV-1 is caused mainly by the presence of a cell in latent infection. Latent infection cells, resting memory CD4 mainly long lifetime+ THIV-1 cells and infected cells, the cells are in the genomic DNA in HIV-1 present as proviral DNA, growth-stimulating a cell such as an activation stimulus in the absence of HIV-1 particles most HIV-1 proteins are not produced, activated upon stimulation HIV-1 production starts. Most of the drugs the present anti-HIV-1 HIV-1 since enzymes derived from a target, the production can be suppressed HIV-1 is, latent infection HIV-1 is not possible to reduce the number of cells. Therefore, the establishment of a therapy to cure HIV-1, latent infection HIV-1 is used as a target in the development of therapeutic cells is required.
Is suppressed so that the function of histone deacetylase, highly acetylated histones by causing (histone deacetylase, HDAC) gene affects the expression of histone deacetylase inhibitors, tumor suppressor gene or cancer by changing the expression of the, anti-tumor effect. Already, some HDAC inhibitors, as methods of treatment for solid and hematologic tumors, alone or as a combination therapy, in the early stage of clinical development.
On the other hand, hepatocellular carcinoma and hepatitis C, such as H. pylori infection and gastric cancer, chronic infection and there is a correlation in rats is known. This includes, activation of inflammatory signaling system such as the induction of expression of various genes, as cancer and chronic inflammation has a common molecular mechanism is believed to be involved.
Recently, entinostat, vorinostat several HIV-1 HDAC latent infection of the cell inhibitor is activated (reservoir cells), can induce the production of HIV-1 has been reported (non-patent document 1).
Patent Document 1 and 2, as well as the non-patent document 2, entinostat HDAC inhibitor, such as benzamide derivatives chidamido (chidamide) malignant tumors, autoimmune diseases, skin diseases, for the treatment of parasitic infection, to be useful as an ameliorating agent is described.
Heretofore, entinostat HIV-1 infected human mononuclear cells by specific cell death induction for there are no reports of the effects.
Scope of claims (In Japanese)[請求項1]
下記式(I):
[化1]
(式中、Ar1及びAr2は同一又は異なり、置換又は無置換の芳香族基であり、Xは-CH2O-又は-CH=CH-である。)
で示される化合物、その塩又はそれらの溶媒和物を含有するHIV-1感染細胞殺傷剤。
[請求項2]
前記式(I)において、Ar1及びAr2は同一又は異なり、フェニル基又はピリジル基を表し、当該フェニル基又はピリジル基はアミノ基、C1-6-アルキル基及びハロゲン原子から選ばれる1以上の置換基で置換されていてもよい請求項1記載のHIV-1感染細胞殺傷剤。
[請求項3]
前記式(I)において、Ar1はピリジル基であり、Ar2はアミノ基及びハロゲン原子から選ばれる1以上の置換基で置換されていてもよいフェニル基である請求項1記載のHIV-1感染細胞殺傷剤。
[請求項4]
HIV-1感染者であって、がんに罹患していない者を投与対象とする請求項1~3のいずれか1項に記載のHIV-1感染細胞殺傷剤。
[請求項5]
請求項1に記載の式(I)で示される化合物、その塩又はそれらの溶媒和物と、抗HIV-1薬とを含有するHIV-1感染の治療又は予防用組成物。
[請求項6]
抗HIV-1薬がHIV-1プロテアーゼ阻害剤から選ばれる少なくとも1種である請求項5記載のHIV-1感染の治療又は予防用組成物。
[請求項7]
HIV-1感染の治療又は予防において同時に、別々に、又は順次に投与するための組み合わせ製剤であって、2つの別個の製剤:
(a)請求項1に記載の式(I)で示される化合物、その塩又はそれらの溶媒和物を含有する製剤、及び
(b)抗HIV-1薬を含有する製剤
を含む組み合わせ製剤。
[請求項8]
抗HIV-1薬がHIV-1プロテアーゼ阻害剤から選ばれる少なくとも1種である請求項7記載の組み合わせ製剤。
  • Applicant
  • ※All designated countries except for US in the data before July 2012
  • KAGOSHIMA UNIVERSITY
  • Inventor
  • OKAMOTO Mika
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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