JP2668214B2 - Ａｉｄｓ治療薬 - Google Patents

Ａｉｄｓ治療薬

Info

Publication number
JP2668214B2
JP2668214B2 JP62193991A JP19399187A JP2668214B2 JP 2668214 B2 JP2668214 B2 JP 2668214B2 JP 62193991 A JP62193991 A JP 62193991A JP 19399187 A JP19399187 A JP 19399187A JP 2668214 B2 JP2668214 B2 JP 2668214B2
Authority
JP
Japan
Prior art keywords
aids
drug
agent
virus
present
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
JP62193991A
Other languages
English (en)
Other versions
JPS6438031A (en
Inventor
益代 中井
Original Assignee
益代 中井
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 益代 中井 filed Critical 益代 中井
Priority to JP62193991A priority Critical patent/JP2668214B2/ja
Priority to US07/215,953 priority patent/US5051425A/en
Priority to ES88111167T priority patent/ES2046246T3/es
Priority to DE8888111167T priority patent/DE3875016T2/de
Priority to EP19910118061 priority patent/EP0476711A3/en
Priority to EP88111167A priority patent/EP0302263B1/en
Publication of JPS6438031A publication Critical patent/JPS6438031A/ja
Application granted granted Critical
Publication of JP2668214B2 publication Critical patent/JP2668214B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/13—Amines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/16—Purine radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Description

【発明の詳細な説明】 〔産業上の利用分野〕 本発明は新規後天性免疫不全症候群（AIDS）治療剤に
関する。 〔従来の技術〕 後天性免疫不全症候群（AIDS）の治療薬の研究・開発
が進められているが、まだ有効な治療薬は見出されてい
ない。 〔発明が解決しようとする問題点〕 本発明者は、AIDS治療剤を開発するため、種々の化合
物について研究を重ねて来たところ、制癌剤中のアルキ
ル化剤、５−フルオロウラシルが優れた抗HTLV−IIIウ
ィルス作用を有することを見出し、さらに研究を重ねて
本発明を完成した。 従って、本発明の目的は優れたAIDS治療剤を提供する
ことである。 〔問題点を解決するための手段〕 本発明はアルキル化剤および５−フルオロウラシルか
ら選ばれる少なくとも一種の制癌剤よりなるAIDS治療剤
に関する。 （１） 本発明で使用される制癌剤 アルキル化剤としては、ナイトロジェンマスタード−
Ｎ−オキサイド、サイクロホスファマイド、塩酸ニムス
チンなどが例示される。 また、５−フルオロウラシルも使用される。 これら制癌剤は、いずれも市販製剤を利用できる。 （２） 投与量 インビトロでのウィルス抑制効果は、薬剤の細胞毒性
限界内で十分に見られるので、各々の制癌剤の最大投与
量までの投与が可能である。 （３） 投与方法 各々の制癌剤の従来の投与方法に準じて、経口、静注
等の投与が可能である。 〔実施例・実験例〕 実施例１・実験例１ a.材料と方法 １）被検薬剤：表１に示したアルキル化剤、５−フルオ
ロウラシル ２）ウィルス:HIV−Ｉ（HTLV−III株） ３）標的細胞:MT−４細胞 ４）効果測定法 前処理法：各々の被検薬剤の２倍希釈系列（50μ/w
ell）に標的細胞（５×106/ml）を50μ/wellづつ分注
し、CO2下、37℃で18〜24時間反応後、ウィルス液を100
μ/well（50〜500TCID50）接種した。 同時法：各々の被検薬剤の２倍希釈系列（50μ/wel
l）に標的細胞（５×106/ml）を50μ/wellづつ分注
後、ウィルス液を100μ/well（50〜500TCID50）接種
した。 上記およびで前処理したものをともに37℃で３日
間培養後、培養液を交換し、さらに、３〜４日間培養後
の標的細胞の細胞変性抑制よりHIV−Ｉウィルス抑制を
効果を判定した。 b.結果 表１にHTLV−III株の増殖抑制濃度を示した。なお、
表１中前処理とは、HTLV−III株接種前に標的細胞に薬
剤処理をする場合であり、同時とはウィルス接種と薬剤
処理を同時にする場合を意味する。細胞毒性とは薬剤に
よる細胞毒性のおこる投与量を意味する。 〔効果〕 制癌剤のうちアルキル化剤、５−フルオロウラシル
は、in vitroでの抗HTLV−III作用を有し、有効なAIDS
治療薬になりうることを示唆した。

Claims (1)

  1. (57)【特許請求の範囲】 １．アルキル化剤および５−フルオロウラシルから選ば
    れる少なくとも一種の制癌剤よりなる後天性免疫不全症
    候群（AIDS）治療薬。
JP62193991A 1987-08-03 1987-08-03 Ａｉｄｓ治療薬 Expired - Lifetime JP2668214B2 (ja)

Priority Applications (6)

Application Number Priority Date Filing Date Title
JP62193991A JP2668214B2 (ja) 1987-08-03 1987-08-03 Ａｉｄｓ治療薬
US07/215,953 US5051425A (en) 1987-08-03 1988-07-06 Therapeutic composition for combatting AIDS
ES88111167T ES2046246T3 (es) 1987-08-03 1988-07-12 Composicion terapeutica para combatir el sida.
DE8888111167T DE3875016T2 (de) 1987-08-03 1988-07-12 Therapeutikum zur behandlung von aids.
EP19910118061 EP0476711A3 (en) 1987-08-03 1988-07-12 Use of 5-fluorouracil for the treatment of AIDS
EP88111167A EP0302263B1 (en) 1987-08-03 1988-07-12 Therapeutic composition for combatting aids

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP62193991A JP2668214B2 (ja) 1987-08-03 1987-08-03 Ａｉｄｓ治療薬

Publications (2)

Publication Number Publication Date
JPS6438031A JPS6438031A (en) 1989-02-08
JP2668214B2 true JP2668214B2 (ja) 1997-10-27

Family

ID=16317151

Family Applications (1)

Application Number Title Priority Date Filing Date
JP62193991A Expired - Lifetime JP2668214B2 (ja) 1987-08-03 1987-08-03 Ａｉｄｓ治療薬

Country Status (5)

Country Link
US (1) US5051425A (ja)
EP (2) EP0476711A3 (ja)
JP (1) JP2668214B2 (ja)
DE (1) DE3875016T2 (ja)
ES (1) ES2046246T3 (ja)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5227160A (en) * 1988-07-15 1993-07-13 The Biomembrane Institute Monoclonal antibody nuh2 capable of inactivating motility of human sperm, antigen defined by said monoclonal antibody and methods of using said monoclonal antibody and antigen
JP2938583B2 (ja) * 1989-12-22 1999-08-23 株式会社リコー 給紙装置
US5603963A (en) * 1994-07-28 1997-02-18 University Of Cincinnati Method for the treatment of retroviral diseases such as acquired immune deficiency syndrome utilizing (pseudo)halogen complexes of gold(1)
WO1996028162A1 (en) * 1995-03-14 1996-09-19 University Of Medicine & Dentistry Of New Jersey New drug combination for the treatment of viral diseases
US6093564A (en) 1997-10-03 2000-07-25 V.I. Technologies, Inc. Methods and compositions for the selective modification of nucleic acids
US6369048B1 (en) 1998-01-12 2002-04-09 V.I. Technologies, Inc. Methods and compositions for inactivating viruses
US6617100B2 (en) 1998-09-25 2003-09-09 V.I. Technologies, Inc. Solid phase quenching systems
US6403359B1 (en) 1998-09-25 2002-06-11 V. I. TECHNOLOGIES, Inc. Solid phase quenching systems
US6150109A (en) 1999-01-25 2000-11-21 V. I. TECHNOLOGIES, Inc. Lipophilic quenching of viral inactivating agents

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
MOL.PHARMACOL=1987 *
NATO.ASI.SER=1986 *
PHARM.RES=1984 *
VIROLOGY=1985 *

Also Published As

Publication number Publication date
ES2046246T3 (es) 1995-04-01
EP0302263A3 (en) 1989-10-25
JPS6438031A (en) 1989-02-08
EP0302263A2 (en) 1989-02-08
DE3875016T2 (de) 1993-04-08
EP0476711A3 (en) 1992-04-08
DE3875016D1 (de) 1992-11-05
EP0302263B1 (en) 1992-09-30
US5051425A (en) 1991-09-24
EP0476711A2 (en) 1992-03-25

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