HK61897A - New derivatives of physostigmine, their use and pharmaceutical formulations containing them - Google Patents

New derivatives of physostigmine, their use and pharmaceutical formulations containing them Download PDF

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Publication number
HK61897A
HK61897A HK61897A HK61897A HK61897A HK 61897 A HK61897 A HK 61897A HK 61897 A HK61897 A HK 61897A HK 61897 A HK61897 A HK 61897A HK 61897 A HK61897 A HK 61897A
Authority
HK
Hong Kong
Prior art keywords
physostigmine
salt
phosphatidic acid
pharmacologically acceptable
group
Prior art date
Application number
HK61897A
Other languages
German (de)
English (en)
Inventor
Bombardelli Ezio
Original Assignee
Indena S.P.A.
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 Indena S.P.A. filed Critical Indena S.P.A.
Publication of HK61897A publication Critical patent/HK61897A/en

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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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • C07F9/10—Phosphatides, e.g. lecithin
    • C07F9/106—Adducts, complexes, salts of phosphatides

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Cephalosporin Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (13)

  1. Sel de physostigmine, ou dérivé de celle-ci, pharmaceutiquement acceptable, ayant une activité anticholinestérase, et acide phosphatidique de formule : dans laquelle R1 et R2 qui peuvent être identiques ou différents représentent chacun un groupe alkyle C10-24, un groupe alkényle C10-24, ou un groupe alkadiényle C10-24.
  2. Sel selon la revendication 1, ayant la formule : dans laquelle :
    - PS représente un cation dérivé de la physostigmine, ou d'un dérivé de celle-ci, pharmaceutiquement acceptable, ayant une activité anti-cholinestérase,
    - PA représente un acide phosphatidique, ou un mélange de différents acides phosphatidiques. et x/y est compris entre 2/1 et 1/2.
  3. Sel selon la revendication 2, dans lequel x/y est compris entre 1,2/1 et 1/1,2, de préférence, entre 1,1/1 et 1/1,1.
  4. Sel selon la revendication 2, ou la revendication 3, dans lequel PS représente physostigmine.
  5. Sel selon l'une quelconque des revendications précédentes, dans lequel R1 et R2, qui peuvent être identiques ou différents. représentent chacun un groupe alkyle C15-24, un groupe alkényle C15-24, ou un groupe alkadiényle C15-24.
  6. Sel selon la revendication 5, dans lequel R1 et R2, qui peuvent être identiques ou différents, représentent chacun un groupe alkyle C15 ou 17, un groupe alkényle C15 ou 17, ou un groupe alkadiényle C15 ou 17.
  7. Méthode de production d'un sel selon l'une quelconque des revendications précédentes, qui comprend la réaction de la physostigmine, ou d'un sel de celle-ci, pharmaceutiquement acceptable, avec un acide phosphatidique, ladite réaction étant effectuée dans un solvant des deux réactants.
  8. Méthode selon la revendication 7, dans laquelle le solvant est choisi parmi les hydrocarbures halogénés, les cétones, les éthers, et les mélanges de ceux-ci.
  9. Composition pharmaceutique comprenant un sel selon l'une quelconque des revendications 1 à 6, et un excipient pharmaceutiquement acceptable.
  10. Forme pharmaceutique à libération prolongée, capable de libérer une substance pharmacologiquement active pendant une certaine période de temps, caractérisée en ce que la substance pharmacologiquement active est un sel selon l'une quelconque des revendications 1 à 6.
  11. Forme pharmaceutique à libération prolongée selon la revendication 10, adaptée à la libération de la substance pharmacologiquement active par voie transcutanée.
  12. Forme pharmaceutique à libération prolongée selon la revendication 11, sous la forme d'un timbre, emplâtre, ou bandage cutané.
  13. Utilisation d'un sel de physostigmine, ou d'un dérivé de celle-ci, pharmaceutiquement acceptable, selon l'une quelconque des revendications 1 à 6, ayant une activité anticholinestérase, et d'un acide phosphatidique, dans la fabrication d'une composition pharmaceutique pour le traitement de la démence sénile, et de la maladie d'Alzheimer.
HK61897A 1992-03-16 1997-05-08 New derivatives of physostigmine, their use and pharmaceutical formulations containing them HK61897A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB929205670A GB9205670D0 (en) 1992-03-16 1992-03-16 New derivatives of physostigmine,their use and pharmaceutical formulations containing them

Publications (1)

Publication Number Publication Date
HK61897A true HK61897A (en) 1997-05-16

Family

ID=10712207

Family Applications (1)

Application Number Title Priority Date Filing Date
HK61897A HK61897A (en) 1992-03-16 1997-05-08 New derivatives of physostigmine, their use and pharmaceutical formulations containing them

Country Status (13)

Country Link
US (1) US5314906A (fr)
EP (1) EP0561597B1 (fr)
JP (1) JPH0640914A (fr)
KR (1) KR100251395B1 (fr)
AT (1) ATE147076T1 (fr)
CA (1) CA2091550A1 (fr)
DE (1) DE69306990T2 (fr)
DK (1) DK0561597T3 (fr)
ES (1) ES2096203T3 (fr)
GB (1) GB9205670D0 (fr)
GR (1) GR3022205T3 (fr)
HK (1) HK61897A (fr)
SG (1) SG67287A1 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5861431A (en) * 1995-06-07 1999-01-19 Iotek, Inc. Incontinence treatment
US5709878A (en) * 1996-08-02 1998-01-20 Rosenbaum; Jerry Transdermal delivery of dehydroepiandrosterone
WO1998048784A2 (fr) * 1997-04-28 1998-11-05 The University Of British Columbia Methodes et composition de modulation de l'amyloidose
IL121322A (en) * 1997-07-16 2002-07-25 Modus Biolog Membranes Ltd Modular pharmacological preparation of the immune system based on fats and its preparation
AU8562998A (en) * 1997-08-12 1999-03-01 Takeda Chemical Industries Ltd. Idebenone-containing preparation for percutaneous administration
US5869090A (en) * 1998-01-20 1999-02-09 Rosenbaum; Jerry Transdermal delivery of dehydroepiandrosterone
DE10025644A1 (de) * 2000-05-24 2001-12-06 Lohmann Therapie Syst Lts Schmales bandförmiges transdermales therapeutisches System zur Applikation von Wirkstoffen direkt über dem arteriellen oder venösen Gefäßsystem
CA2458068A1 (fr) * 2001-08-20 2003-02-27 Tatton Technologies, Llc. Methodes et compositions permettant de traiter des troubles associes a l'apoptose
KR100758089B1 (ko) * 2005-08-04 2007-09-11 아이알 마이크로시스템 에스.에이. 기체 검출 방법 및 기체 검출 장치

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1109003B (it) * 1977-09-20 1985-12-16 Univ Firenze Derivati dell 1 2 3 8 3 a 8 a esai dropirrolo 23 b indolo
IT1199076B (it) * 1984-03-01 1988-12-30 Consiglio Nazionale Ricerche Derivati della fisostigmina con proprieta'di inibizione della aceticolinesterasi e relativo procedimento di produzione
IT1225462B (it) * 1987-04-03 1990-11-14 Mediolanum Farmaceutici Srl Sali organici di derivati della fisostigmina
EP0350672A1 (fr) * 1988-06-28 1990-01-17 MAGIS FARMACEUTICI S.p.A. Sels de diacyl-glycéro-(di)-phosphates de L-(acyl) carnitine et d'esters de L-acyl-carnitine
IT1238684B (it) * 1990-02-09 1993-09-01 Indena Spa Derivati del bilobalide,loro usi e formulazioni che li contegono
EP0513703A3 (en) * 1991-05-13 1993-01-13 Magis Farmaceutici S.P.A. Carbamate esters of eseroline having anticholinesterase activity, a process for their preparation and relative pharmaceutical compositions containing them as the active principle

Also Published As

Publication number Publication date
DE69306990T2 (de) 1997-06-12
ES2096203T3 (es) 1997-03-01
EP0561597A1 (fr) 1993-09-22
KR930019212A (ko) 1993-10-18
DE69306990D1 (de) 1997-02-13
DK0561597T3 (da) 1997-01-20
SG67287A1 (en) 1999-09-21
CA2091550A1 (fr) 1993-09-17
GR3022205T3 (en) 1997-04-30
JPH0640914A (ja) 1994-02-15
GB9205670D0 (en) 1992-04-29
EP0561597B1 (fr) 1997-01-02
KR100251395B1 (ko) 2000-05-01
ATE147076T1 (de) 1997-01-15
US5314906A (en) 1994-05-24

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PC Patent ceased (i.e. patent has lapsed due to the failure to pay the renewal fee)