WO2002070499A3 - Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier - Google Patents

Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier Download PDF

Info

Publication number
WO2002070499A3
WO2002070499A3 PCT/EP2002/002234 EP0202234W WO02070499A3 WO 2002070499 A3 WO2002070499 A3 WO 2002070499A3 EP 0202234 W EP0202234 W EP 0202234W WO 02070499 A3 WO02070499 A3 WO 02070499A3
Authority
WO
WIPO (PCT)
Prior art keywords
ascorbic acid
passage
acid suitable
hematoencephalic barrier
prodrugs derivatives
Prior art date
Application number
PCT/EP2002/002234
Other languages
French (fr)
Other versions
WO2002070499A2 (en
Inventor
Stefano Manfredini
Original Assignee
Univ Ferrara
Stefano Manfredini
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 Univ Ferrara, Stefano Manfredini filed Critical Univ Ferrara
Publication of WO2002070499A2 publication Critical patent/WO2002070499A2/en
Publication of WO2002070499A3 publication Critical patent/WO2002070499A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/62—Three oxygen atoms, e.g. ascorbic acid

Abstract

Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier, consisting of ascorbic acid and a substance active on the central nervous system bound by covalent bond, suitable for the treatment of important neurologic pathologies among which Alzheimer"s disease, Parkinson"s disease and AIDS dementia.
PCT/EP2002/002234 2001-03-05 2002-03-01 Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier WO2002070499A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2001A000450 2001-03-05
IT2001MI000450A ITMI20010450A1 (en) 2001-03-05 2001-03-05 PROPHARMACIES DERIVED FROM ASCORBIC ACID AT THE PASSAGE OF THE BLOOD-ENCEPHALIC BARRIER

Publications (2)

Publication Number Publication Date
WO2002070499A2 WO2002070499A2 (en) 2002-09-12
WO2002070499A3 true WO2002070499A3 (en) 2002-10-31

Family

ID=11447121

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/002234 WO2002070499A2 (en) 2001-03-05 2002-03-01 Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier

Country Status (2)

Country Link
IT (1) ITMI20010450A1 (en)
WO (1) WO2002070499A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8980952B2 (en) 2002-03-20 2015-03-17 University Of Maryland, Baltimore Methods for treating brain swelling with a compound that blocks a non-selective cation channel
JP4485806B2 (en) 2002-03-20 2010-06-23 ユニヴァーシティ オブ メリーランド，ボルチモア Non-selective cation channels and brain swelling of neural cells
AU2005290238A1 (en) 2004-09-18 2006-04-06 Department Of Veterans Affairs Therapeutic agents trageting the NCCa-ATP channel and methods of use thereof
WO2006116057A2 (en) 2005-04-21 2006-11-02 Duke University Facilitated transport of bisphosphonates by vitamin c
EP1939192A1 (en) * 2006-12-28 2008-07-02 Neuropharma S.A. Cyclopentanone derivatives, method of synthesis and uses thereof
US9511075B2 (en) 2007-01-12 2016-12-06 The University Of Maryland, Baltimore Targeting NCCA-ATP channel for organ protection following ischemic episode
EP2167107B1 (en) 2007-06-22 2016-12-14 University of Maryland, Baltimore Inhibitors of ncca-atp channels for therapy
EP2719380A3 (en) * 2008-09-16 2014-07-30 University of Maryland, Baltimore SUR1 inhibitors for therapy

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07126162A (en) * 1993-10-28 1995-05-16 Showa Denko Kk Intracerebral administration agent of ascorbic acids
US5869525A (en) * 1996-05-15 1999-02-09 Showa Denko Kabushiki Kaisha Ascorbic acid drugs for intracerebral administration
WO2001037830A1 (en) * 1999-11-24 2001-05-31 Sloan-Kettering Institute For Cancer Research Method for increasing the concentration of ascorbic acid in brain tissues of a subject

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH07126162A (en) * 1993-10-28 1995-05-16 Showa Denko Kk Intracerebral administration agent of ascorbic acids
US5869525A (en) * 1996-05-15 1999-02-09 Showa Denko Kabushiki Kaisha Ascorbic acid drugs for intracerebral administration
WO2001037830A1 (en) * 1999-11-24 2001-05-31 Sloan-Kettering Institute For Cancer Research Method for increasing the concentration of ascorbic acid in brain tissues of a subject

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
C. HANSCH ET AL.: "Hydrophobicity and Central Nervous System Agents: On the Principle of Minimal Hydrophobicity in Drug Design", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 76, no. 9, 1987, WASHINGTON US, pages 663 - 687, XP002207715 *
DATABASE WPI Week 9528, Derwent World Patents Index; AN 1995-212878, XP002207717 *
F.P. BONINA ET AL.: "Synthesis, Stability, and Pharmacological Evaluation of Nipecotic Acid Prodrugs", JOURNAL OF PHARMACEUTICAL SCIENCES, vol. 88, no. 5, 1999, WASHINGTON US, pages 561 - 567, XP002207716 *
G. BATTAGLIA ET AL.: "Systemically administered d-glucose conjugates of 7-chlorokynurenic acid are centrally available and exert anticonvulsant activity in rodents", BRAIN RESEARCH, vol. 860, 2000, AMSTERDAM, NL, pages 149 - 156, XP002207714, ISSN: 0006-8993 *
PATENT ABSTRACTS OF JAPAN vol. 1995, no. 08 29 September 1995 (1995-09-29) *

Also Published As

Publication number Publication date
WO2002070499A2 (en) 2002-09-12
ITMI20010450A1 (en) 2002-09-05

Similar Documents

Publication Publication Date Title
HUS1500038I1 (en) Benzoylpyridine derivative or its salt, fungicide containing it as an active ingredient, its production process and intermediate for producing it
MXPA04005456A (en) Acetylene derivatives having mglur 5 antagonistic activity.
EP1897550A3 (en) Prodrugs of Excitatory Amino Acids
WO2001010816A3 (en) Substituted 2-dialkylaminoalkylbiphenyl derivatives
AU2002238855A1 (en) N-phenylarylsulfonamide compound, drug containing the compound as active ingredient, intermediate for the compound, and processes for producing the same
WO2002070499A3 (en) Prodrugs derivatives of the ascorbic acid suitable to the passage of the hematoencephalic barrier
MA26346A1 (en) PREPARATION COMPOSITIONS CONTAINING PHYSIOLOGICALLY ACTIVE AND ACID-INSTABLE COMPOUNDS AND PROCESS FOR PRODUCING THE SAME.
WO2003094842A3 (en) Conjugates comprising central nervous system active drug
WO2003037863A3 (en) Substituted indoles, method for production and use thereof for the inhibition of pain
WO2003024933A1 (en) 2-phenyl-3-heteroarylpropionic acid derivative or salt thereof and medicine containing the same
EP1076057A4 (en) Febrifugine and isofebrifugine and processes for the preparation of both
WO2001049654A3 (en) Substituted aminomethyl-phenyl-cyclohexane derivatives
WO2002076376A3 (en) A stable pharmaceutical composition of pravastatin
ZA200002674B (en) Process for the synthesis of finely divided antiperspirant active ingredient suspensions.
WO2004022542A3 (en) Substituted 1,2,3,4-tetrahydroquinoline derivatives
WO2001049651A3 (en) Aminomethyl-phenyl-cyclohexanone derivatives
AU6076000A (en) Cyclic amine derivatives for the treatment of neurological diseases
WO2004046077A8 (en) A method for preparing indan-1,3-dicarboxylic acid
WO2004048318A8 (en) Improved process for the preparation of 1,3-substituted indenes
GB2364492B (en) Audio processing, e.g. for discouraging vocalisation or the production of complex sounds
WO2000076966A3 (en) Indolinylamide derivatives and the use thereof as antiviral drugs
WO2002088134A3 (en) Antipsychotic aminomethyl derivatives of 1,3,7,8-tetrahydro-6,9-dioxa-1,3-diaza-cyclopenta[a]-naphthalen-2-one
AU2003272967A1 (en) Processes for producing optically active n-(2,3-epoxypropan-1-yl)phthalimide
WO2003006489A3 (en) Prodrugs of excitatory amino acids
AU2001284477A1 (en) Novel crystals of N-hydroxy-2(S)-methyl-5-ethoxymethoxy -4(S)-(N-(4-phenoxyphenylcarbonyl)amino]pentanamide, process for their production and medicines containing the crystals as the active ingredient

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

AK Designated states

Kind code of ref document: A3

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CO CR CU CZ DE DK DM DZ EC EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ OM PH PL PT RO RU SD SE SG SI SK SL TJ TM TN TR TT TZ UA UG US UZ VN YU ZA ZM ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZM ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GQ GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: JP

WWW Wipo information: withdrawn in national office

Country of ref document: JP