CA2347469C - Esters de (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol et leur utilisation comme promedicament de l'antagoniste du recepteur 5ht2a mdl 100,907 - Google Patents
Esters de (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol et leur utilisation comme promedicament de l'antagoniste du recepteur 5ht2a mdl 100,907 Download PDFInfo
- Publication number
- CA2347469C CA2347469C CA002347469A CA2347469A CA2347469C CA 2347469 C CA2347469 C CA 2347469C CA 002347469 A CA002347469 A CA 002347469A CA 2347469 A CA2347469 A CA 2347469A CA 2347469 C CA2347469 C CA 2347469C
- Authority
- CA
- Canada
- Prior art keywords
- compound
- ethyl
- fluorophenyl
- piperidinemethanol
- dimethoxyphenyl
- 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 - Fee Related
Links
- 0 *C(O[C@](C1CCN(CCc(cc2)ccc2F)CC1)c1cccc(C=O)c1*I)=O Chemical compound *C(O[C@](C1CCN(CCc(cc2)ccc2F)CC1)c1cccc(C=O)c1*I)=O 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
- C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D211/20—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
- C07D211/22—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Addiction (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
L'invention concerne des esters de (+)-alpha-(2,3-diméthoxyphényl)-1-[2-(4-fluorophényl)éthyl]-4-pipéridineméthanol de formule (I) dans laquelle R représente un alkyle C4-C20, des formulations pharmaceutiques, des procédés de préparation et d'utilisation de ces esters. Ces composés antagonisent les effets de la sérotonine au niveau du récepteur de 5HT2A et sont utilisés dans le traitement de différentes pathologies, dont notamment les psychoses telles que la schizophrénie.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
PCT/US1998/021608 WO2000021930A1 (fr) | 1998-10-14 | 1998-10-14 | Esters de (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol et leur utilisation comme promedicament de l'antagoniste du recepteur 5ht2a mdl 110,907 |
Publications (2)
Publication Number | Publication Date |
---|---|
CA2347469A1 CA2347469A1 (fr) | 2000-04-20 |
CA2347469C true CA2347469C (fr) | 2006-02-28 |
Family
ID=22268079
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CA002347469A Expired - Fee Related CA2347469C (fr) | 1998-10-14 | 1998-10-14 | Esters de (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol et leur utilisation comme promedicament de l'antagoniste du recepteur 5ht2a mdl 100,907 |
Country Status (21)
Country | Link |
---|---|
EP (1) | EP1121345A1 (fr) |
JP (1) | JP2002527422A (fr) |
KR (1) | KR100515429B1 (fr) |
CN (1) | CN1160333C (fr) |
AU (1) | AU1083099A (fr) |
BR (1) | BR9816049A (fr) |
CA (1) | CA2347469C (fr) |
CZ (1) | CZ20011331A3 (fr) |
EA (1) | EA003667B1 (fr) |
EE (1) | EE200100219A (fr) |
HK (1) | HK1039332A1 (fr) |
HR (1) | HRP20010278A2 (fr) |
HU (1) | HUP0200517A3 (fr) |
IL (2) | IL142479A0 (fr) |
NO (1) | NO320417B1 (fr) |
NZ (1) | NZ510631A (fr) |
PL (1) | PL193306B1 (fr) |
SK (1) | SK5082001A3 (fr) |
TR (1) | TR200101047T2 (fr) |
UA (1) | UA57859C2 (fr) |
WO (1) | WO2000021930A1 (fr) |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20020099076A1 (en) * | 2000-05-25 | 2002-07-25 | Richard Scheyer D. | Use of (+)-a-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl) ethyl]-4-piperidinemethanol or its prodrug in the treatment of symptoms of dementia and dopamine induced psychosis |
CN102241667B (zh) * | 2010-05-14 | 2013-10-23 | 中国人民解放军军事医学科学院毒物药物研究所 | 1-[(4-羟基哌啶-4基)甲基]吡啶-2(1h)-酮衍生物及其制备方法和用途 |
CN106892897A (zh) * | 2015-12-21 | 2017-06-27 | 上海科胜药物研发有限公司 | 一种羟哌吡酮游离碱新晶型及其制备方法 |
CN106928187A (zh) * | 2015-12-31 | 2017-07-07 | 上海奥博生物医药技术有限公司 | 一种盐酸羟哌吡酮新晶型及其制备方法 |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE114467T1 (de) * | 1990-06-01 | 1994-12-15 | Merrell Dow Pharma | (+)-alpha-(2,3 dimethoxyphenyl)-1-(2- (fluorophenyl)ethyl>-4-piperidinmethanol. |
-
1998
- 1998-10-14 PL PL347318A patent/PL193306B1/pl not_active IP Right Cessation
- 1998-10-14 EE EEP200100219A patent/EE200100219A/xx unknown
- 1998-10-14 UA UA2001042522A patent/UA57859C2/uk unknown
- 1998-10-14 CA CA002347469A patent/CA2347469C/fr not_active Expired - Fee Related
- 1998-10-14 CN CNB988142740A patent/CN1160333C/zh not_active Expired - Fee Related
- 1998-10-14 TR TR2001/01047T patent/TR200101047T2/xx unknown
- 1998-10-14 KR KR10-2001-7004703A patent/KR100515429B1/ko not_active IP Right Cessation
- 1998-10-14 IL IL14247998A patent/IL142479A0/xx active IP Right Grant
- 1998-10-14 EP EP98953458A patent/EP1121345A1/fr not_active Withdrawn
- 1998-10-14 WO PCT/US1998/021608 patent/WO2000021930A1/fr active IP Right Grant
- 1998-10-14 CZ CZ20011331A patent/CZ20011331A3/cs unknown
- 1998-10-14 EA EA200100361A patent/EA003667B1/ru not_active IP Right Cessation
- 1998-10-14 NZ NZ510631A patent/NZ510631A/en active IP Right Revival
- 1998-10-14 AU AU10830/99A patent/AU1083099A/en not_active Abandoned
- 1998-10-14 BR BR9816049-4A patent/BR9816049A/pt not_active Application Discontinuation
- 1998-10-14 HU HU0200517A patent/HUP0200517A3/hu unknown
- 1998-10-14 JP JP2000575839A patent/JP2002527422A/ja active Pending
- 1998-10-14 SK SK508-2001A patent/SK5082001A3/sk not_active Application Discontinuation
-
2001
- 2001-04-05 IL IL142479A patent/IL142479A/en not_active IP Right Cessation
- 2001-04-09 NO NO20011805A patent/NO320417B1/no not_active IP Right Cessation
- 2001-04-12 HR HR20010278A patent/HRP20010278A2/hr not_active Application Discontinuation
-
2002
- 2002-02-05 HK HK02100869A patent/HK1039332A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
NO320417B1 (no) | 2005-12-05 |
NO20011805D0 (no) | 2001-04-09 |
IL142479A (en) | 2006-06-11 |
AU1083099A (en) | 2000-05-01 |
HUP0200517A2 (en) | 2002-06-29 |
TR200101047T2 (tr) | 2001-08-21 |
JP2002527422A (ja) | 2002-08-27 |
NZ510631A (en) | 2003-07-25 |
KR20010106517A (ko) | 2001-11-29 |
KR100515429B1 (ko) | 2005-09-20 |
PL347318A1 (en) | 2002-03-25 |
CN1314887A (zh) | 2001-09-26 |
EP1121345A1 (fr) | 2001-08-08 |
UA57859C2 (uk) | 2003-07-15 |
WO2000021930A1 (fr) | 2000-04-20 |
HRP20010278A2 (en) | 2002-06-30 |
SK5082001A3 (en) | 2001-11-06 |
BR9816049A (pt) | 2001-07-03 |
CA2347469A1 (fr) | 2000-04-20 |
HUP0200517A3 (en) | 2002-12-28 |
PL193306B1 (pl) | 2007-01-31 |
CZ20011331A3 (cs) | 2001-08-15 |
HK1039332A1 (en) | 2002-04-19 |
IL142479A0 (en) | 2002-03-10 |
EA200100361A1 (ru) | 2001-10-22 |
EE200100219A (et) | 2002-08-15 |
EA003667B1 (ru) | 2003-08-28 |
CN1160333C (zh) | 2004-08-04 |
NO20011805L (no) | 2001-06-08 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
WO1991018602A1 (fr) | (+)-α-(2,3-DIMETHOXYPHENYLE)-1-[2-(4-FLUOROPHENYLE)ETHYLE]-4-PIPERIDINEMETHANOL | |
US6063793A (en) | Esters of (+)-α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidi nemethanol | |
EP1289527B1 (fr) | (+)-alpha-(2,3-dimethoxyphenyl)-1-(2-(4-fluorophenyl)ethyl)-4-piperidine-methanol ou ses prodrogues pour traiter les demences ou les troubles cognitifs | |
AU2001264842A1 (en) | Use of (+)-alpha -(2,3-dimethoxyphenyl)-1-(2-(4-fluorophenyl)ethyl)-4- piperidinemerthanol or its prodrug in the treatment of symptoms of dementia and dopamine induced psychosis | |
AU704435B2 (en) | Use of (+)-alpha-(2,3-dimethoxyphenyl)-1-(2-(4-fluorophenyl) ethyl)-4-piperidinemethanol in treating depressive disorders and bipolar disorders | |
CA2347469C (fr) | Esters de (+)-alpha-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol et leur utilisation comme promedicament de l'antagoniste du recepteur 5ht2a mdl 100,907 | |
AU2004200993A1 (en) | Esters of (+)-alpha-(2,3-dimethoxyphenyl-[2-(4-flurophenyl) ethyl]-4-piperidinemethanol and their use as prodrugs of the 5HT2a receptor antagonist MDL 110,907 | |
MXPA01003535A (en) | Esters of (+)-alpha-( 2,3- dimethoxyphenyl) -1-[2-(4- fluorophenyl) ethyl]-4- piperidinemethanol and their use as prodrugs of the 5ht2a receptor antagonist mdl 110,907 | |
BG65206B1 (bg) | Естери на (+)-алфа-(2,3-диметоксифенил)-1-[2-(4-флуорoфенил)етил]-4- пиперидинметанол, метод за тяхното получаване и приложението им като предшественици на 5ht2a рецепторния антагонист mdl 110,907 | |
EP1105132B1 (fr) | Utilisation de r(+)-g(a)-(2,3-dimethoxyphenyl)-1- 2-(4-fluorophenyl)ethyl]-4-piperidinemethanol pour le traitement de l'apnee obstructive du sommeil | |
TW461885B (en) | Esters of (+)-Α-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol | |
HU211916A9 (hu) | Érzéstelenítőként alkalmazható N-fenil-N-(4-piperidinil)-amidok Az átmeneti oltalom az 1-29., 39., 46. és 47. igénypontra vonatkozik. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
EEER | Examination request | ||
MKLA | Lapsed |