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ES2127396T3 - Inhibidores aromaticos de acetilcolinesterasa. - Google Patents

Inhibidores aromaticos de acetilcolinesterasa.

Info

Publication number
ES2127396T3
ES2127396T3 ES94917916T ES94917916T ES2127396T3 ES 2127396 T3 ES2127396 T3 ES 2127396T3 ES 94917916 T ES94917916 T ES 94917916T ES 94917916 T ES94917916 T ES 94917916T ES 2127396 T3 ES2127396 T3 ES 2127396T3
Authority
ES
Spain
Prior art keywords
aromatic
acetilcolinesterasa
inhibitors
compounds
methods
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
ES94917916T
Other languages
English (en)
Inventor
Jean-Noel Collard
Jean-Marie Hornsperger
Daniel Schirlin
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.)
Aventis Pharmaceuticals Inc
Original Assignee
Merrell Dow Pharmaceuticals Inc
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 Merrell Dow Pharmaceuticals Inc filed Critical Merrell Dow Pharmaceuticals Inc
Application granted granted Critical
Publication of ES2127396T3 publication Critical patent/ES2127396T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • 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
    • A61K31/12—Ketones
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00—Preparation of halogenated hydrocarbons
    • C07C17/35—Preparation of halogenated hydrocarbons by reactions not affecting the number of carbon or of halogen atoms in the reaction
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00—Preparation of halogenated hydrocarbons
    • C07C17/361—Preparation of halogenated hydrocarbons by reactions involving a decrease in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C33/00—Unsaturated compounds having hydroxy or O-metal groups bound to acyclic carbon atoms
    • C07C33/40—Halogenated unsaturated alcohols
    • C07C33/46—Halogenated unsaturated alcohols containing only six-membered aromatic rings as cyclic parts
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/80—Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/82—Ketones containing a keto group bound to a six-membered aromatic ring containing hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00—Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76—Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/84—Ketones containing a keto group bound to a six-membered aromatic ring containing ether groups, groups, groups, or groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/62—Halogen-containing esters
    • C07C69/63—Halogen-containing esters of saturated acids

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

COMPUESTOS DE LA FORMULA GENERAL (1), ESTEROISOMEROS Y SALES FARMACEUTICAMENTE ACEPTABLES DE LOS MISMOS, DONDE CADA Z Y Z'' SON INDEPENDIENTEMENTE H O F; Q ES (A), CH(OH), (B); X ES H, BR, CL, F O CF{SUB,3}; Y ES H, BR, CL, F, OH, OR{SUB,5}, OC(O)R{SUB,4}, N{SUB,3}, CN, NO{SUB,2}, SO{SUB,3}H, CO{SUB,2}R{SUB,4}, NH{SUB,2}, NHR{SUB,9}, NR{SUB,9}R''{SUB,9}, C(R{SUB,6})(R{SUB,7})(V''R{SUB,8}) O C(O)R{SUB,7}, SIEMPRE Y CUANDO TANTO Z COMO Z'' SEAN F, ENTONCES Y ES H O F; V Y V'' SON CADA UNA INDEPENDIENTEMENTE CH{SUB,2} O O, R{SUB,1} ES H O CH{SUB,3}; R{SUB,2}, R{SUB,9} Y R''{SUB,9} SON CADA UNO INDEPENDIENTEMENTE ALQUIL(C{SUB,1-10}), O R{SUB,2} Y V-R{SUB,3} TOMADOS JUNTO CON EL ATOMO DE CARBONO AL QUE ESTAN ADOSADOS FORMAN UN ANILLO DE 3-6 ELEMENTOS; R{SUB,3}, R{SUB,6} Y R{SUB,8} SON CADA UNO INDEPENDIENTEMENTE H, ALQUIL(C{SUB,1-6}), O CICLOALQUIL(C{SUB,3-6}); R{SUB,4} ES H, ALQUIL(C{SUB,1-10}), ARIL ALQUILENO(C{SUB,0-4}) O CICLOALQUIL(C{SUB,3-8}); Y R{SUB,5} ES ALQUIL(C{SUB,1-10}), BENCILO, FENETILO, O CICLOALQUIL(C{SUB,3-6}) , POSEE UNA ACTIVIDAD ANTICOLINAESTERASA Y PUEDE SER UTILIZADO EN EL TRATAMIENTO DE LAS DEMENCIAS DEGENERATIVAS.
ES94917916T 1993-06-04 1994-05-05 Inhibidores aromaticos de acetilcolinesterasa. Expired - Lifetime ES2127396T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP93401431A EP0627400A1 (en) 1993-06-04 1993-06-04 Aromatic acetylcholinesterase inhibitors

Publications (1)

Publication Number Publication Date
ES2127396T3 true ES2127396T3 (es) 1999-04-16

Family

ID=8214719

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94917916T Expired - Lifetime ES2127396T3 (es) 1993-06-04 1994-05-05 Inhibidores aromaticos de acetilcolinesterasa.

Country Status (19)

Country Link
US (1) US5663448A (es)
EP (2) EP0627400A1 (es)
JP (1) JP3735372B2 (es)
KR (1) KR960702820A (es)
CN (1) CN1124953A (es)
AT (1) ATE174895T1 (es)
AU (1) AU676578B2 (es)
CA (1) CA2164303C (es)
DE (1) DE69415522T2 (es)
DK (1) DK0701546T3 (es)
ES (1) ES2127396T3 (es)
FI (1) FI955795A0 (es)
HU (1) HUT73484A (es)
IL (1) IL109863A (es)
NO (1) NO306058B1 (es)
NZ (1) NZ267221A (es)
TW (1) TW385247B (es)
WO (1) WO1994029255A1 (es)
ZA (1) ZA943787B (es)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5804560A (en) * 1995-01-06 1998-09-08 Sibia Neurosciences, Inc. Peptide and peptide analog protease inhibitors
US6017887A (en) * 1995-01-06 2000-01-25 Sibia Neurosciences, Inc. Peptide, peptide analog and amino acid analog protease inhibitors
US6218383B1 (en) 1998-08-07 2001-04-17 Targacept, Inc. Pharmaceutical compositions for the prevention and treatment of central nervous system disorders
EP1827468B1 (en) * 2004-12-23 2012-08-22 Curaxis Pharmaceutical Corporation Acetylcholinesterase Inhibitors and leuprolide acetate for the treatment of Alzheimer's disease
US20060194723A1 (en) * 2005-02-28 2006-08-31 Rabinoff Michael D Novel medication treatment and delivery strategies for Alzheimer's Disease, other disorders with memory impairment, and possible treatment strategies for memory improvement
EP2089383B1 (en) 2006-11-09 2015-09-16 Probiodrug AG 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases
EP2091948B1 (en) 2006-11-30 2012-04-18 Probiodrug AG Novel inhibitors of glutaminyl cyclase
NZ579310A (en) 2007-03-01 2012-03-30 Probiodrug Ag Use of glutaminyl cyclase inhibitors for the treatment of mild cognitive impairment and diagnostic purposes thereof
DK2142514T3 (da) 2007-04-18 2015-03-23 Probiodrug Ag Thioureaderivater som glutaminylcyclase-inhibitorer
CN102695546B (zh) 2009-09-11 2014-09-10 前体生物药物股份公司 作为谷氨酰胺酰环化酶抑制剂的杂环衍生物
WO2011100373A1 (en) * 2010-02-09 2011-08-18 The Johns Hopkins University Methods and compositions for improving cognitive function
ES2586231T3 (es) 2010-03-03 2016-10-13 Probiodrug Ag Inhibidores de glutaminil ciclasa
SG183229A1 (en) 2010-03-10 2012-09-27 Probiodrug Ag Heterocyclic inhibitors of glutaminyl cyclase (qc, ec 2.3.2.5)
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
DK2686313T3 (en) 2011-03-16 2016-05-02 Probiodrug Ag Benzimidazole derivatives as inhibitors of glutaminyl cyclase
CN102826985B (zh) * 2012-09-18 2015-08-19 厦门大学 一种1-(3,4,5-三羟基)苯基-1-烷基酮的制备方法
EP2919788A4 (en) 2012-11-14 2016-05-25 Univ Johns Hopkins METHODS AND COMPOSITIONS FOR THE TREATMENT OF SCHIZOPHRENIA
WO2014144801A1 (en) 2013-03-15 2014-09-18 Agenebio Inc. Methods and compositions for improving cognitive function
US10806717B2 (en) 2013-03-15 2020-10-20 The Johns Hopkins University Methods and compositions for improving cognitive function
CA2986598C (en) 2015-05-22 2023-09-26 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
EP3461819B1 (en) 2017-09-29 2020-05-27 Probiodrug AG Inhibitors of glutaminyl cyclase

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2843776A1 (de) * 1977-10-07 1979-04-12 Science Union & Cie (arylalkyl)-alkansaeurederivate, verfahren zu ihrer herstellung und sie enthaltende arzneimittel
US4835099A (en) * 1986-11-20 1989-05-30 Becton, Dickinson And Company Signal enhancement in immunoassay by modulation of enzymatic catalysis
DE3725941A1 (de) * 1987-08-05 1989-02-16 Hoechst Ag Ester von arylperfluoralkylcarbinolen, verfahren zur herstellung dieser verbindungen und der zugrundeliegenden arylbisperfluoralkylcarbinole
JP2509282B2 (ja) * 1987-09-24 1996-06-19 鹿島石油株式会社 光学活性なジフルオロアルコ―ル誘導体
NZ231735A (en) * 1988-12-23 1992-04-28 Ici Plc Alcohol/ether derivatives, preparation and pharmaceutical compositions thereof
US5214069A (en) * 1988-12-23 1993-05-25 Imperial Chemical Industries Plc Alcohol and ether derivatives
JPH02200646A (ja) * 1989-01-31 1990-08-08 Nippon Oil & Fats Co Ltd フルオロアルキル基含有芳香族誘導体及びその製造方法
EP0403713A1 (en) * 1989-06-22 1990-12-27 Merrell Dow Pharmaceuticals Inc. Novel acetylcholinesterase inhibitors
DE3927049A1 (de) * 1989-08-16 1991-02-21 Sandoz Ag Halogenalkyl-phenyl-ketone und deren hydrate, ihre herstellung und verwendung
EP0611769A1 (en) * 1993-02-16 1994-08-24 Merrell Dow Pharmaceuticals Inc. Silylated acetylcholinesterase inhibitors

Also Published As

Publication number Publication date
NO954896D0 (no) 1995-12-01
IL109863A (en) 1998-12-27
DE69415522D1 (de) 1999-02-04
EP0627400A1 (en) 1994-12-07
HU9503452D0 (en) 1996-01-29
NZ267221A (en) 1997-11-24
CN1124953A (zh) 1996-06-19
US5663448A (en) 1997-09-02
CA2164303C (en) 2000-11-28
DK0701546T3 (da) 1999-08-16
AU6944294A (en) 1995-01-03
EP0701546B1 (en) 1998-12-23
ATE174895T1 (de) 1999-01-15
CA2164303A1 (en) 1994-12-22
IL109863A0 (en) 1994-10-07
FI955795A (fi) 1995-12-01
KR960702820A (ko) 1996-05-23
AU676578B2 (en) 1997-03-13
EP0701546A1 (en) 1996-03-20
TW385247B (en) 2000-03-21
NO306058B1 (no) 1999-09-13
JP3735372B2 (ja) 2006-01-18
FI955795A0 (fi) 1995-12-01
JPH08511019A (ja) 1996-11-19
ZA943787B (en) 1995-01-30
WO1994029255A1 (en) 1994-12-22
DE69415522T2 (de) 1999-06-02
HUT73484A (en) 1996-08-28
NO954896L (no) 1996-02-02

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