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BR9814035A - Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type. - Google Patents

Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type.

Info

Publication number
BR9814035A
BR9814035A BR9814035-3A BR9814035A BR9814035A BR 9814035 A BR9814035 A BR 9814035A BR 9814035 A BR9814035 A BR 9814035A BR 9814035 A BR9814035 A BR 9814035A
Authority
BR
Brazil
Prior art keywords
alkyl
alkoxy
halogen
alkoxycarbonyl
mono
Prior art date
Application number
BR9814035-3A
Other languages
Portuguese (pt)
Inventor
Jean-Pierre Maffrand
Philippe Soubrie
Jean-Paul Terranova
Original Assignee
Sanofi Synthelabo
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 FR9714322A external-priority patent/FR2771007B1/en
Priority claimed from FR9714324A external-priority patent/FR2771006B1/en
Application filed by Sanofi Synthelabo filed Critical Sanofi Synthelabo
Publication of BR9814035A publication Critical patent/BR9814035A/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/64Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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

Landscapes

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

Abstract

Patente de Invenção: <B>"ASSOCIAçãO DE PRINCìPIOS ATIVOS, NOTADAMENTE DE TETRA-HIDROPIRIDINAS E DE AGENTES INIBIDORES DA ACETILCOLINESTERASE, PARA O TRATAMENTO DA DEMêNCIA SENIL DO TIPO ALZHEIMER"<D>. A invenção refere-se a uma composição farmacêutica contendo como princípios ativos: um constituinte (a) selecionado entre 1-(2-napht-2-iletil)-4-(3-trifluorometilfenil)-1,2,3,6-tetrahidropiridina e um composto (I) em que Y representa -CH- ou -N-; R~ 1~ representa o hidrogênio, um halogênio, hidroxila, CF~ 3~, alquila (C~ 3~-C~ 4~) ou grupo alcoxila (C~ 1~-C~ 4~); R~ 2~ representa hidrogênio, halogênio, hidroxila, CF~ 3~, alquila (C~ 3~-C~ 4~) ou grupo alcoxila (C~ 1~-C~ 4~); R~ 3~ e R~ 4~ representam cada um hidrogênio ou alquila (C~ 1~-C~ 4~); X representa (a) alquila (C~ 3~-C~ 6~); alcoxila (C~ 3~-C~ 6~); carboxialquila (C~ 3~-C~ 7~); alcoxicarbonila (C~ 1~-C~ 4~) alquila (C~ 3~-C~ 6~); carboxialcoxila (C~ 3~-C~ 7~); ou alcoxicarbonila (C~ 1~-C~ 4~) alcoxila (C~ 3~-C~ 6~); (b) um radical selecionado dentre cicloalquila (C~ 3~-C~ 7~), cicloalquilóxi (C~ 3~-C~ 7~), cicloalquilmetila (C~ 3~-C~ 7~), cicloalquilamino (C~ 3~-C~ 7~) e ciclohexenila, o radical mencionado capaz de ser substituído por halogênio, hidróxi, alcóxi (C~ 1~-C~ 4~), carbóxi, alcoxicarbonila (C~ 1~-C~ 4~), amino, mono- ou di- alquilamino (C~ 1~-C~ 4~) ou (c) um grupo selecionado dentre fenila, fenóxi, fenilamino, alquil-fenil-amino N-(C~ 1~-C~ 3~), fenilmetila, feniletila, fenilcarbonila, feniltio, fenilsulfonila, fenilsulfinila e estirila, o grupo mencionado capaz de ser mono- ou polissubstituído no grupo fenila por um halogênio, CF~ 3~, alquila (C~ 1~-C~ 4~), alcóxi (C~ 1~-C~ 4~), ciano, amino, mono- ou di-alquilamino (C~ 1~-C~ 4~), acilamino (C~ 1~-C~ 4~), carbóxi, alcoxicarbonila (C~ 1~-C~ 4~), aminocarbonila, mono- ou di-alquilaminocarbonila (C~ 1~-C~ 4~), alquil (C~ 1~-C~ 4~)amino, alquil (C~ 1~-C~ 4~) hidróxi, ou alquil (C~ 1~-C~ 4~) halogênio; opcionalmente na forma de um de seus sais farmaceuticamente aceitáveis; e um constituinte (b) ativo no tratamento sintomático de DAT, opcionalmente na forma de um de seus sais farmaceuticamente aceitáveis, contanto que quando o constituinte (a) é outro que 1-(2naft-2-iletil)-4-(3-trifluorometilfenil)-1,2,3,6-tetrahidropiridina ou um de seus sais farmaceuticamente aceitáveis, o constituinte (b) é um agente inibidor acetilcolinesterase.Invention Patent: <B> "ASSOCIATION OF ACTIVE PRINCIPLES, NOTES OF TETRA-HYDROPYRIDINES AND ACETYL CHOLINESTERASE INHIBITING AGENTS, FOR THE TREATMENT OF SENIL DEMENCE OF THE ALZHEIMER TYPE" <D>. The invention relates to a pharmaceutical composition containing as active ingredients: a constituent (a) selected from 1- (2-napht-2-ylethyl) -4- (3-trifluoromethylphenyl) -1,2,3,6-tetrahydropyridine and a compound (I) in which Y represents -CH- or -N-; R ~ 1 ~ represents hydrogen, a halogen, hydroxyl, CF ~ 3 ~, alkyl (C ~ 3 ~ -C ~ 4 ~) or alkoxy group (C ~ 1 ~ -C ~ 4 ~); R ~ 2 ~ represents hydrogen, halogen, hydroxyl, CF ~ 3 ~, alkyl (C ~ 3 ~ -C ~ 4 ~) or alkoxy group (C ~ 1 ~ -C ~ 4 ~); R ~ 3 ~ and R ~ 4 ~ each represent hydrogen or alkyl (C ~ 1 ~ -C ~ 4 ~); X represents (a) (C ~ 3 ~ -C ~ 6 ~) alkyl; alkoxy (C ~ 3 ~ -C ~ 6 ~); carboxyalkyl (C ~ 3 ~ -C ~ 7 ~); alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) alkyl (C ~ 3 ~ -C ~ 6 ~); carboxyalkoxy (C ~ 3 ~ -C ~ 7 ~); or alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) alkoxy (C ~ 3 ~ -C ~ 6 ~); (b) a radical selected from cycloalkyl (C ~ 3 ~ -C ~ 7 ~), cycloalkyloxy (C ~ 3 ~ -C ~ 7 ~), cycloalkylmethyl (C ~ 3 ~ -C ~ 7 ~), cycloalkylamino (C ~ 3 ~ -C ~ 7 ~) and cyclohexenyl, the radical mentioned capable of being substituted by halogen, hydroxy, alkoxy (C ~ 1 ~ -C ~ 4 ~), carboxy, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~) , amino, mono- or di-alkylamino (C ~ 1 ~ -C ~ 4 ~) or (c) a group selected from phenyl, phenoxy, phenylamino, alkyl-phenyl-amino N- (C ~ 1 ~ -C ~ 3 ~), phenylmethyl, phenylethyl, phenylcarbonyl, phenylthio, phenylsulfonyl, phenylsulfinyl and styryl, the mentioned group capable of being mono- or polysubstituted in the phenyl group by a halogen, CF ~ 3 ~, alkyl (C ~ 1 ~ -C ~ 4 ~ ), alkoxy (C ~ 1 ~ -C ~ 4 ~), cyano, amino, mono- or di-alkylamino (C ~ 1 ~ -C ~ 4 ~), acylamino (C ~ 1 ~ -C ~ 4 ~), carboxy, alkoxycarbonyl (C ~ 1 ~ -C ~ 4 ~), aminocarbonyl, mono- or di-alkylaminocarbonyl (C ~ 1 ~ -C ~ 4 ~), alkyl (C ~ 1 ~ -C ~ 4 ~) amino, alkyl (C ~ 1 ~ -C ~ 4 ~) hydroxy, or (C ~ 1 ~ -C ~ 4 ~) halogen; optionally in the form of one of its pharmaceutically acceptable salts; and a constituent (b) active in the symptomatic treatment of DAT, optionally in the form of one of its pharmaceutically acceptable salts, provided that when constituent (a) is other than 1- (2naft-2-ylethyl) -4- (3- trifluoromethylphenyl) -1,2,3,6-tetrahydropyridine or one of its pharmaceutically acceptable salts, constituent (b) is an acetylcholinesterase inhibiting agent.

BR9814035-3A 1997-11-14 1998-11-09 Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type. BR9814035A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR9714322A FR2771007B1 (en) 1997-11-14 1997-11-14 COMBINATION OF ACTIVE INGREDIENTS FOR THE TREATMENT OF SENILE DEMENTIA OF THE ALZHEIMER TYPE
FR9714324A FR2771006B1 (en) 1997-11-14 1997-11-14 COMBINATION OF ACTIVE INGREDIENTS FOR THE TREATMENT OF SENILE DEMENTIA OF THE ALZHEIMER TYPE
PCT/FR1998/002384 WO1999025363A1 (en) 1997-11-14 1998-11-09 Combination of active principles, in particular of tetrahydropyridins and acetylcholinesterase inhibiting agents, for treating senile dementia such as alzheimer dementia

Publications (1)

Publication Number Publication Date
BR9814035A true BR9814035A (en) 2000-09-26

Family

ID=26233932

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9814035-3A BR9814035A (en) 1997-11-14 1998-11-09 Association of active ingredients, notably tetrahydropyridines and acetylcholinesterase inhibiting agents, for the treatment of senile dementia of the alzheimer type.

Country Status (27)

Country Link
EP (1) EP1030671A1 (en)
JP (1) JP2001523642A (en)
KR (1) KR100599350B1 (en)
CN (1) CN1243540C (en)
AU (1) AU743228B2 (en)
BG (1) BG64819B1 (en)
BR (1) BR9814035A (en)
CA (1) CA2309966A1 (en)
CO (1) CO4980891A1 (en)
DZ (1) DZ2649A1 (en)
EA (1) EA003255B1 (en)
EE (1) EE04235B1 (en)
HU (1) HUP0100098A3 (en)
ID (1) ID24933A (en)
IL (2) IL136122A0 (en)
IS (1) IS5482A (en)
MY (1) MY120461A (en)
NO (1) NO20002450L (en)
NZ (1) NZ504420A (en)
OA (1) OA11464A (en)
PL (1) PL194597B1 (en)
SA (1) SA98190747B1 (en)
SK (1) SK286040B6 (en)
TR (1) TR200001262T2 (en)
TW (1) TW585766B (en)
UY (1) UY25247A1 (en)
WO (1) WO1999025363A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE42327E1 (en) * 2002-06-14 2011-05-03 Toyama Chemical Co., Ltd. Medicinal compositions improving brain function and method for improving brain function
AU2003266967B2 (en) * 2002-08-07 2006-11-16 Novartis Ag Methods for the treatment of dementia based on Apo E genotype
CN1520818A (en) * 2003-02-09 2004-08-18 山东绿叶天然药物研究开发有限公司 Cholinesterase inhibitor pharmaceutical composition for senile dementia
EP1830886B1 (en) 2004-12-27 2016-04-13 Eisai R&D Management Co., Ltd. Method for stabilizing anti-dementia drug
DK3099296T3 (en) 2014-01-31 2019-04-15 Cognition Therapeutics Inc ISO-INDOLINE DERIVATIVES, COMPOSITIONS AND METHODS FOR TREATING NEURODEGENERATIVE DISEASE
KR102614814B1 (en) 2017-05-15 2023-12-20 카그니션 테라퓨틱스, 인코퍼레이티드 Composition for treating neurodegenerative diseases
KR102224918B1 (en) 2018-03-20 2021-03-09 (주)인벤티지랩 Pharmaceutiical composition comprising memantine and donepezil for preventing or treating cognitive impairment-related disease and preparation method thereof
WO2019182319A1 (en) * 2018-03-20 2019-09-26 (주)인벤티지랩 Method for preparing pharmaceutical composition for preventing or treating cognitive disorder-associated diseases, and pharmaceutical composition for preventing or treating cognitive disorder-associated diseases, prepared by preparation method
CN109265391B (en) * 2018-11-13 2021-11-19 枣庄学院 Biphenyl polysubstituted 1,2,5, 6-tetrahydropyridine compound and synthetic method and application thereof

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2662355B1 (en) * 1990-05-22 1994-11-10 Sanofi Sa USE OF 1- [2- (2-NAPHTYL) ETHYL] -4- (3-TRIFLUOROMETHYLPHENYL) -1,2,3,6-TETRAHYDROPYRIDINE FOR THE PREPARATION OF MEDICINES FOR THE TREATMENT OF BRAIN AND NEURAL DISORDERS.
US5453428A (en) * 1991-02-14 1995-09-26 The Mount Sinai School Of Medicine Of The City Of New York Method and composition for the treatment of apathy-amotivation syndrome
CA2213000A1 (en) * 1995-03-06 1996-09-12 Interneuron Pharmaceuticals, Inc. Reduction of infarct volume using citicoline
FR2736053B1 (en) * 1995-06-28 1997-09-19 Sanofi Sa NEWS 1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES

Also Published As

Publication number Publication date
IS5482A (en) 2000-05-09
CN1243540C (en) 2006-03-01
IL136122A (en) 2006-07-05
UY25247A1 (en) 2001-05-31
SA98190747B1 (en) 2006-11-04
ID24933A (en) 2000-08-31
CO4980891A1 (en) 2000-11-27
AU1160999A (en) 1999-06-07
SK7112000A3 (en) 2000-10-09
EA003255B1 (en) 2003-02-27
CA2309966A1 (en) 1999-05-27
BG64819B1 (en) 2006-05-31
NO20002450D0 (en) 2000-05-11
MY120461A (en) 2005-10-31
NZ504420A (en) 2003-08-29
HUP0100098A2 (en) 2001-07-30
IL136122A0 (en) 2001-05-20
EA200000412A1 (en) 2000-12-25
HUP0100098A3 (en) 2001-12-28
EE200000290A (en) 2001-06-15
EP1030671A1 (en) 2000-08-30
KR20010032099A (en) 2001-04-16
PL194597B1 (en) 2007-06-29
TR200001262T2 (en) 2001-01-22
AU743228B2 (en) 2002-01-24
TW585766B (en) 2004-05-01
EE04235B1 (en) 2004-02-16
NO20002450L (en) 2000-07-14
WO1999025363A1 (en) 1999-05-27
CN1285742A (en) 2001-02-28
BG104428A (en) 2001-08-31
OA11464A (en) 2003-11-18
PL340500A1 (en) 2001-02-12
JP2001523642A (en) 2001-11-27
KR100599350B1 (en) 2006-07-12
DZ2649A1 (en) 2004-12-28
SK286040B6 (en) 2008-01-07

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Legal Events

Date Code Title Description
B25D Requested change of name of applicant approved

Owner name: SANOFI-AVENTIS (FR)

Free format text: ALTERADO DE: SANOFI-SYNTHELABO

B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09B Patent application refused [chapter 9.2 patent gazette]

Free format text: INDEFIRO O PRESENTE PEDIDO DE ACORDO COM OS ARTIGOS 8O E 13O DA LPI

B15K Others concerning applications: alteration of classification

Ipc: A61K 31/00 (2006.01), A61K 31/445 (2006.0