GB2055044A - Glucuronidase activity and/or phdependent pharmaceuticals and their methods of production and use for selective treatment of diseases - Google Patents

Glucuronidase activity and/or phdependent pharmaceuticals and their methods of production and use for selective treatment of diseases

Info

Publication number
GB2055044A
GB2055044A GB8015763A GB8015763A GB2055044A GB 2055044 A GB2055044 A GB 2055044A GB 8015763 A GB8015763 A GB 8015763A GB 8015763 A GB8015763 A GB 8015763A GB 2055044 A GB2055044 A GB 2055044A
Authority
GB
United Kingdom
Prior art keywords
glucuronidase activity
aglycones
disclosed
tumor
glucuronides
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.)
Granted
Application number
GB8015763A
Other versions
GB2055044B (en
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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
Priority claimed from US05/951,269 external-priority patent/US4584368A/en
Priority claimed from US05/951,270 external-priority patent/US4424348A/en
Priority claimed from US06/011,619 external-priority patent/US4327074A/en
Application filed by Individual filed Critical Individual
Publication of GB2055044A publication Critical patent/GB2055044A/en
Application granted granted Critical
Publication of GB2055044B publication Critical patent/GB2055044B/en
Expired legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00—Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02—Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04—Organic compounds
    • A61K51/0491—Sugars, nucleosides, nucleotides, oligonucleotides, nucleic acids, e.g. DNA, RNA, nucleic acid aptamers
    • 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
    • A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/18—Acyclic radicals, substituted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20—Carbocyclic rings
    • C07H15/203—Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/34—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving hydrolase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5091—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing the pathological state of an organism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2123/00—Preparations for testing in vivo
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2334/00—O-linked chromogens for determinations of hydrolase enzymes, e.g. glycosidases, phosphatases, esterases
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2333/00—Assays involving biological materials from specific organisms or of a specific nature
    • G01N2333/90—Enzymes; Proenzymes
    • G01N2333/914—Hydrolases (3)
    • G01N2333/924—Hydrolases (3) acting on glycosyl compounds (3.2)
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Genetics & Genomics (AREA)
  • Physics & Mathematics (AREA)
  • Analytical Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Microbiology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Physiology (AREA)
  • Cell Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Optics & Photonics (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)
  • Pathology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Hyperacidified tumors having high ss-glucuronidase activity can be treated with glucuronides with aglycones toxic to the tumor cells with great safety toward the rest of the body by first administering an alkalinizing agent in an amount sufficient to maintain the pH level of non-tumor tissues at approximately 7.4 during the glucuronide treatment. This will cause inactivation of ss-glucuronidase activity in the rest of the body. When nitrile-containing aglycones are used sodium thiosulfate is also administered to avoid cyanide poisoning. Novel glucuronides are disclosed the aglycones of which exert a higher toxic effect in an acid environment or are water-soluble only in an alkaline environment. Such compounds have particular utility with the above process. By substituting radioisotopes into the aglycone, diagnosis and in situ radiation therapy may be accomplished. Bacterial cells having ss-glucuronidase activity may also be diagnosed and treated in accordance with the present invention. A urine test is disclosed to determine the amount of free glucuronic acid in the urine which is an indication of the presence of a tumor in the body having high ss-glucuronidase activity. Novel methods of synthesizing the glucuronide used in the present invention are also disclosed.
GB8015763A 1978-10-13 1979-10-02 Glucuronidase activity and/or phdependent pharmaceuticals and their methods of production and use for selective treatment of diseases Expired GB2055044B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US05/951,269 US4584368A (en) 1978-10-13 1978-10-13 β-Glucuronidase activity and/or pH-dependent pharmaceuticals and thier methods of production
US05/951,270 US4424348A (en) 1978-10-13 1978-10-13 Methods of manufacture of nitrile-containing glucuronic acid conjugates
US06/011,619 US4327074A (en) 1978-10-13 1979-02-12 Method for diagnosis and selective treatment of infections of bacteria having β-glucuronidase activity

Publications (2)

Publication Number Publication Date
GB2055044A true GB2055044A (en) 1981-02-25
GB2055044B GB2055044B (en) 1983-04-20

Family

ID=27359461

Family Applications (1)

Application Number Title Priority Date Filing Date
GB8015763A Expired GB2055044B (en) 1978-10-13 1979-10-02 Glucuronidase activity and/or phdependent pharmaceuticals and their methods of production and use for selective treatment of diseases

Country Status (12)

Country Link
JP (1) JPS55500837A (en)
AU (1) AU534068B2 (en)
CA (1) CA1148086A (en)
CH (1) CH652724A5 (en)
DE (1) DE2953223T1 (en)
FR (2) FR2440374B1 (en)
GB (1) GB2055044B (en)
IL (1) IL58352A (en)
IT (1) IT1164730B (en)
NL (1) NL7920107A (en)
SE (1) SE461983B (en)
WO (1) WO1980000791A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4490523A (en) * 1981-11-10 1984-12-25 Ely J. Rubin Mandelonitrile triacetyl glucuronate and process for preparing same
AU594855B2 (en) * 1988-01-15 1990-03-15 Baker Norton Pharmaceuticals, Inc. Glucuronic acid derivatives of opioid antagonists
AU5099696A (en) * 1995-03-30 1996-10-16 Werner Kreutz Medicaments for the selective treatment of tumour tissues
WO2014138722A1 (en) * 2013-03-08 2014-09-12 Cognate3 Llc Process for the preparation of a non-corrosive base solution and methods of using same

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB788855A (en) * 1953-06-30 1958-01-08 Ernst Theodore Krebs Improvements in or relating to mandelo-nitrile-glucuronosides and method of making the same
US2985664A (en) * 1957-05-29 1961-05-23 Ernst T Krebs Hexuronic acid derivatives
US3758455A (en) * 1970-05-14 1973-09-11 Chugai Pharmaceutical Co Ltd Reof mycophenolic acid glucuronide and the process for the preparation the
DE2212014A1 (en) * 1971-04-21 1972-10-26 Deutsche Akademie der Wissenschaf ten zu Berlin, χ 1199 Berlin Enzymatic cleavage of chemotherapeutics transport forms - under acid conditions to give tumour-specific chemotherapy
USRE29465E (en) * 1972-08-14 1977-11-01 Eli Lilly And Company Psoriasis treatment with mycophenolic acid
US3880995A (en) * 1973-05-14 1975-04-29 Lilly Co Eli Treatment of arthritis with mycophenolic acid and derivatives
US3959253A (en) * 1973-07-02 1976-05-25 Merck & Co., Inc. β-D-glucosyluronic acid derivatives
DD122386A1 (en) * 1975-06-24 1976-10-05
JPS5325534A (en) * 1976-08-24 1978-03-09 Rikagaku Kenkyusho Mandelic acid glucosides and their anti-cancerous preparations

Also Published As

Publication number Publication date
CA1148086A (en) 1983-06-14
IT1164730B (en) 1987-04-15
WO1980000791A1 (en) 1980-05-01
IL58352A (en) 1985-11-29
FR2440374B1 (en) 1986-03-21
JPS55500837A (en) 1980-10-23
DE2953223T1 (en) 1980-11-27
FR2449284A1 (en) 1980-09-12
IT7950529A0 (en) 1979-10-11
SE461983B (en) 1990-04-23
GB2055044B (en) 1983-04-20
AU5112079A (en) 1981-04-16
DE2953223C2 (en) 1989-05-18
CH652724A5 (en) 1985-11-29
SE8004369L (en) 1980-06-12
NL7920107A (en) 1980-08-29
AU534068B2 (en) 1984-01-05
FR2440374A1 (en) 1980-05-30

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Legal Events

Date Code Title Description
732 Registration of transactions, instruments or events in the register (sect. 32/1977)
PCNP Patent ceased through non-payment of renewal fee

Effective date: 19931002