BR9814035A - Associação de princìpios ativos, notadamente de tetra-hidropiridinas e de agentes inibidores da acetilcolinesterase, para o tratamento da demência senil do tipo alzheimer. - Google Patents
Associação de princìpios ativos, notadamente de tetra-hidropiridinas e de agentes inibidores da acetilcolinesterase, para o tratamento da demência senil do tipo alzheimer.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
- 108010022752 Acetylcholinesterase Proteins 0.000 title abstract 3
- 229940022698 acetylcholinesterase Drugs 0.000 title abstract 3
- 239000004480 active ingredient Substances 0.000 title abstract 2
- 230000002401 inhibitory effect Effects 0.000 title abstract 2
- 102000012440 Acetylcholinesterase Human genes 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 206010039966 Senile dementia Diseases 0.000 title 1
- 125000004853 tetrahydropyridinyl group Chemical class N1(CCCC=C1)* 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 125000003545 alkoxy group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 4
- 239000000470 constituent Substances 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- -1 phenoxy, phenylamino Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 102100033639 Acetylcholinesterase Human genes 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 150000002431 hydrogen Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000004442 acylamino group Chemical group 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 1
- 125000005111 carboxyalkoxy group Chemical group 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 239000000544 cholinesterase inhibitor Substances 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000004981 cycloalkylmethyl group Chemical group 0.000 abstract 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000005504 styryl group Chemical group 0.000 abstract 1
- 238000002636 symptomatic treatment Methods 0.000 abstract 1
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.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR9714324A FR2771006B1 (fr) | 1997-11-14 | 1997-11-14 | Association de principes actifs pour le traitement de la demence senile du type alzheimer |
| FR9714322A FR2771007B1 (fr) | 1997-11-14 | 1997-11-14 | Association de principes actifs pour le traitement de la demence senile du type alzheimer |
| PCT/FR1998/002384 WO1999025363A1 (fr) | 1997-11-14 | 1998-11-09 | Association de principes actifs, notamment de tetrahydropyridines et d'agents inhibiteurs de l'acetylcholinesterase, pour le traitement de la demence senile du type alzheimer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR9814035A true BR9814035A (pt) | 2000-09-26 |
Family
ID=26233932
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR9814035-3A BR9814035A (pt) | 1997-11-14 | 1998-11-09 | Associação de princìpios ativos, notadamente de tetra-hidropiridinas e de agentes inibidores da acetilcolinesterase, para o tratamento da demência senil do tipo alzheimer. |
Country Status (27)
| Country | Link |
|---|---|
| EP (1) | EP1030671A1 (pt) |
| JP (1) | JP2001523642A (pt) |
| KR (1) | KR100599350B1 (pt) |
| CN (1) | CN1243540C (pt) |
| AU (1) | AU743228B2 (pt) |
| BG (1) | BG64819B1 (pt) |
| BR (1) | BR9814035A (pt) |
| CA (1) | CA2309966A1 (pt) |
| CO (1) | CO4980891A1 (pt) |
| DZ (1) | DZ2649A1 (pt) |
| EA (1) | EA003255B1 (pt) |
| EE (1) | EE04235B1 (pt) |
| HU (1) | HUP0100098A3 (pt) |
| ID (1) | ID24933A (pt) |
| IL (2) | IL136122A0 (pt) |
| IS (1) | IS5482A (pt) |
| MY (1) | MY120461A (pt) |
| NO (1) | NO20002450L (pt) |
| NZ (1) | NZ504420A (pt) |
| OA (1) | OA11464A (pt) |
| PL (1) | PL194597B1 (pt) |
| SA (1) | SA98190747B1 (pt) |
| SK (1) | SK286040B6 (pt) |
| TR (1) | TR200001262T2 (pt) |
| TW (1) | TW585766B (pt) |
| UY (1) | UY25247A1 (pt) |
| WO (1) | WO1999025363A1 (pt) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0311780B8 (pt) * | 2002-06-14 | 2021-05-25 | Toyama Chemical Co Ltd | composição farmacêutica para melhorar a função cerebral |
| DE60328198D1 (de) * | 2002-08-07 | 2009-08-13 | Novartis Ag | Verfahren zur Vorhersage des Behandlungserfolgs mit Rivastigmine basierend auf einer Bestimmung des ApoE Genotyps eines Demenzkranken |
| CN1520818A (zh) * | 2003-02-09 | 2004-08-18 | 山东绿叶天然药物研究开发有限公司 | 治疗老年性痴呆的胆碱酯酶抑制剂药物组合物 |
| US8481565B2 (en) | 2004-12-27 | 2013-07-09 | Eisai R&D Management Co., Ltd. | Method for stabilizing anti-dementia drug |
| EP4023294A1 (en) | 2014-01-31 | 2022-07-06 | Cognition Therapeutics, Inc. | Isoindoline compositions and methods for treating alzheimer's disease |
| KR102614814B1 (ko) | 2017-05-15 | 2023-12-20 | 카그니션 테라퓨틱스, 인코퍼레이티드 | 신경변성 질환 치료용 조성물 |
| WO2019182319A1 (ko) * | 2018-03-20 | 2019-09-26 | (주)인벤티지랩 | 인지 장애 관련 질병의 예방 또는 치료용 약학적 조성물의 제조 방법 및 이의 제조 방법으로 제조된 인지 장애 관련 질병의 예방 또는 치료용 약학적 조성물 |
| KR102224918B1 (ko) | 2018-03-20 | 2021-03-09 | (주)인벤티지랩 | 도네페질 및 메만틴을 포함하는 인지 장애 관련 질병의 예방 또는 치료용 약학적 복합 조성물 및 이의 제조 방법 |
| CN109265391B (zh) * | 2018-11-13 | 2021-11-19 | 枣庄学院 | 联苯多取代1,2,5,6-四氢吡啶化合物及其合成方法与应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2662355B1 (fr) * | 1990-05-22 | 1994-11-10 | Sanofi Sa | Utilisation de la 1-[2-(2-naphtyl)ethyl]-4-(3-trifluoromethylphenyl)-1,2,3,6-tetrahydropyridine pour la preparation de medicaments destines au traitement de troubles cerebraux et neuronaux. |
| 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 (zh) * | 1995-03-06 | 2003-11-05 | 英特纽隆制剂药有限公司 | 使用胞磷胆碱减少梗塞面积 |
| FR2736053B1 (fr) * | 1995-06-28 | 1997-09-19 | Sanofi Sa | Nouvelles 1-phenylalkyl-1,2,3,6-tetrahydropyridines |
-
1998
- 1998-10-26 CO CO98062479A patent/CO4980891A1/es unknown
- 1998-10-28 TW TW087117874A patent/TW585766B/zh not_active IP Right Cessation
- 1998-11-09 EE EEP200000290A patent/EE04235B1/xx not_active IP Right Cessation
- 1998-11-09 EP EP98954538A patent/EP1030671A1/fr not_active Withdrawn
- 1998-11-09 IL IL13612298A patent/IL136122A0/xx not_active IP Right Cessation
- 1998-11-09 KR KR1020007005231A patent/KR100599350B1/ko not_active Expired - Fee Related
- 1998-11-09 CA CA002309966A patent/CA2309966A1/en not_active Abandoned
- 1998-11-09 BR BR9814035-3A patent/BR9814035A/pt not_active Application Discontinuation
- 1998-11-09 CN CNB988130947A patent/CN1243540C/zh not_active Expired - Fee Related
- 1998-11-09 HU HU0100098A patent/HUP0100098A3/hu unknown
- 1998-11-09 SK SK711-2000A patent/SK286040B6/sk unknown
- 1998-11-09 WO PCT/FR1998/002384 patent/WO1999025363A1/fr not_active Ceased
- 1998-11-09 PL PL98340500A patent/PL194597B1/pl not_active IP Right Cessation
- 1998-11-09 JP JP2000520796A patent/JP2001523642A/ja not_active Withdrawn
- 1998-11-09 AU AU11609/99A patent/AU743228B2/en not_active Ceased
- 1998-11-09 NZ NZ504420A patent/NZ504420A/en unknown
- 1998-11-09 TR TR2000/01262T patent/TR200001262T2/xx unknown
- 1998-11-09 EA EA200000412A patent/EA003255B1/ru not_active IP Right Cessation
- 1998-11-09 ID IDW20000860A patent/ID24933A/id unknown
- 1998-11-11 DZ DZ980259A patent/DZ2649A1/xx active
- 1998-11-12 UY UY25247A patent/UY25247A1/es not_active IP Right Cessation
- 1998-11-14 SA SA98190747A patent/SA98190747B1/ar unknown
- 1998-11-14 MY MYPI98005180A patent/MY120461A/en unknown
-
2000
- 2000-05-09 IS IS5482A patent/IS5482A/is unknown
- 2000-05-11 BG BG104428A patent/BG64819B1/bg unknown
- 2000-05-11 NO NO20002450A patent/NO20002450L/no unknown
- 2000-05-12 OA OA1200000141A patent/OA11464A/en unknown
- 2000-05-14 IL IL136122A patent/IL136122A/en unknown
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Legal Events
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Owner name: SANOFI-AVENTIS (FR) Free format text: ALTERADO DE: SANOFI-SYNTHELABO |
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| 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 |