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
Links
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
- A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
-
- 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
-
- 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (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.
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0311780B8 (en) | 2002-06-14 | 2021-05-25 | Toyama Chemical Co Ltd | pharmaceutical composition to improve brain function |
| DK1529116T3 (en) * | 2002-08-07 | 2009-11-09 | Novartis Ag | Method for predicting response to rivastigmine treatment based on the ApoE genotype in dementia patients |
| 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 |
| AU2005320547B2 (en) | 2004-12-27 | 2009-02-05 | Eisai R & D Management Co., Ltd. | Method for stabilizing anti-dementia drug |
| BR112016017808B1 (en) | 2014-01-31 | 2022-07-12 | Cognition Therapeutics, Inc | PHARMACEUTICALLY ACCEPTABLE COMPOUND OR SALT, USE OF A COMPOUND AND COMPOSITION FOR INHIBITING A BETAAMYLOID EFFECT IN A NEURONAL CELL |
| KR102614814B1 (en) * | 2017-05-15 | 2023-12-20 | 카그니션 테라퓨틱스, 인코퍼레이티드 | Composition for treating neurodegenerative diseases |
| KR102224917B1 (en) | 2018-03-20 | 2021-03-09 | (주)인벤티지랩 | Production methods of preventing or treating cognitive impairment-related disease and preventing or treating cognitive impairment-related disease producing thereto |
| 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)
| 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 |
| CN1126546C (en) * | 1995-03-06 | 2003-11-05 | 英特纽隆制剂药有限公司 | Reduction of infarct volume using citicoline |
| FR2736053B1 (en) * | 1995-06-28 | 1997-09-19 | Sanofi Sa | NEWS 1-PHENYLALKYL-1,2,3,6-TETRAHYDROPYRIDINES |
-
1998
- 1998-10-26 CO CO98062479A patent/CO4980891A1/en unknown
- 1998-10-28 TW TW087117874A patent/TW585766B/en not_active IP Right Cessation
- 1998-11-09 SK SK711-2000A patent/SK286040B6/en unknown
- 1998-11-09 CA CA002309966A patent/CA2309966A1/en not_active Abandoned
- 1998-11-09 IL IL13612298A patent/IL136122A0/en not_active IP Right Cessation
- 1998-11-09 TR TR2000/01262T patent/TR200001262T2/en unknown
- 1998-11-09 JP JP2000520796A patent/JP2001523642A/en not_active Withdrawn
- 1998-11-09 ID IDW20000860A patent/ID24933A/en unknown
- 1998-11-09 BR BR9814035-3A patent/BR9814035A/en not_active Application Discontinuation
- 1998-11-09 CN CNB988130947A patent/CN1243540C/en not_active Expired - Fee Related
- 1998-11-09 WO PCT/FR1998/002384 patent/WO1999025363A1/en not_active Application Discontinuation
- 1998-11-09 PL PL98340500A patent/PL194597B1/en not_active IP Right Cessation
- 1998-11-09 HU HU0100098A patent/HUP0100098A3/en unknown
- 1998-11-09 EP EP98954538A patent/EP1030671A1/en not_active Withdrawn
- 1998-11-09 KR KR1020007005231A patent/KR100599350B1/en not_active IP Right Cessation
- 1998-11-09 EE EEP200000290A patent/EE04235B1/en not_active IP Right Cessation
- 1998-11-09 AU AU11609/99A patent/AU743228B2/en not_active Ceased
- 1998-11-09 EA EA200000412A patent/EA003255B1/en not_active IP Right Cessation
- 1998-11-09 NZ NZ504420A patent/NZ504420A/en unknown
- 1998-11-11 DZ DZ980259A patent/DZ2649A1/en active
- 1998-11-12 UY UY25247A patent/UY25247A1/en not_active IP Right Cessation
- 1998-11-14 SA SA98190747A patent/SA98190747B1/en unknown
- 1998-11-14 MY MYPI98005180A patent/MY120461A/en unknown
-
2000
- 2000-05-09 IS IS5482A patent/IS5482A/en unknown
- 2000-05-11 NO NO20002450A patent/NO20002450L/en unknown
- 2000-05-11 BG BG104428A patent/BG64819B1/en unknown
- 2000-05-12 OA OA1200000141A patent/OA11464A/en unknown
- 2000-05-14 IL IL136122A patent/IL136122A/en unknown
Also Published As
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Legal Events
| Date | Code | Title | Description |
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| 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 |
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| B15K | Others concerning applications: alteration of classification |
Ipc: A61K 31/00 (2006.01), A61K 31/445 (2006.0 |