IL102473A - 2-(4-hydroxypiperidino)-1- alkanol derivatives, pharmaceutical compositions containing them and certain intermediates therefor - Google Patents
2-(4-hydroxypiperidino)-1- alkanol derivatives, pharmaceutical compositions containing them and certain intermediates thereforInfo
- Publication number
- IL102473A IL102473A IL102473A IL10247392A IL102473A IL 102473 A IL102473 A IL 102473A IL 102473 A IL102473 A IL 102473A IL 10247392 A IL10247392 A IL 10247392A IL 102473 A IL102473 A IL 102473A
- Authority
- IL
- Israel
- Prior art keywords
- carbons
- alkyl
- group
- alkoxy
- hydroxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compounds of the formula OH R1R(CH2)n MNO(CH2)m QR2R3 XY and the pharmaceutically-acceptable salts thereof; wherein R1, R2 and R3 are each selected from the group consisting of hydrogen, alkyl having 1 to 6 carbons, phenyl and phenyl substituted by hydroxy, alkyl having 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, amino, nitro or alkoxy having 1 to 4 carbons; or R1 and R2 when taken together form a methylene, ethylene, propylene or butylene group; R is OH, or when taken together with R1 form =O; m is 0 to 2; n is 1 or 2; X and Y are each selected from the group consisting of hydrogen, chloro, bromo, fluoro, trifluoromethyl, alkoxy having 1 to 4 carbons, alkyl having 1 to 4 carbons, hydroxy, amino, nitro and substituted phenoxy substituted by hydrogen, hydroxy, alkyl having 1 to 4 carbons, chloro, bromo, fluoro, trifluoromethyl, nitro, amino or alkoxy having 1 to 4 carbons; M and Q are each selected from the group consisting of hydrogen, hydroxy, amino, chloro, bromo, fluoro, trifluoromethyl, nitro, alkyl having 1 to 4 carbons, alkoxy having 1 to 4 carbons, N, N-dialkylamino having 1 to 4 carbons in each of said alkyls, N-alkylamino having 1 to 4 carbons, NHCOR4, NHCOOR5 and NHSO2R6; wherein R4 is selected from the group consisting of hydrogen, alkyl having 1 to 6 carbons, phenyl optionally substituted by hydroxy, chloro, bromo, fluoro, trifluoromethyl, amino, nitro, alkyl having 1 to 4 carbons or alkoxy having 1 to 4 carbons; and wherein R5 and R6 are each selected from the group consisting of alkyl having 1 to 4 carbons or alkoxy having 1 to 4 carbons; or M and Q when taken together form a divalent radical Z, wherein Z is selected from the group consisting of R7 R8 NNN OHOH OH NNN HH HNN ON HH2NN and wherein R7 and R8 are each selected from the group consisting of hydrogen and methyl. The compounds wherein R is hydroxy are for use in neuroprotective pharmaceutical compositions.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73157791A | 1991-07-17 | 1991-07-17 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL102473A0 IL102473A0 (en) | 1993-01-14 |
| IL102473A true IL102473A (en) | 1997-07-13 |
Family
ID=24940103
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL102473A IL102473A (en) | 1991-07-17 | 1992-07-12 | 2-(4-hydroxypiperidino)-1- alkanol derivatives, pharmaceutical compositions containing them and certain intermediates therefor |
Country Status (22)
| Country | Link |
|---|---|
| EP (1) | EP0594729A1 (en) |
| JP (1) | JP2571904B2 (en) |
| KR (1) | KR0165003B1 (en) |
| CN (1) | CN1043759C (en) |
| AU (1) | AU655840B2 (en) |
| BR (1) | BR9206272A (en) |
| CA (1) | CA2113568A1 (en) |
| CZ (1) | CZ284133B6 (en) |
| EG (1) | EG20048A (en) |
| FI (2) | FI940192A (en) |
| HU (1) | HUT70528A (en) |
| IE (1) | IE922311A1 (en) |
| IL (1) | IL102473A (en) |
| MX (1) | MX9204190A (en) |
| NO (1) | NO180445C (en) |
| NZ (1) | NZ243580A (en) |
| PL (1) | PL169884B1 (en) |
| PT (1) | PT100689B (en) |
| RU (1) | RU2065859C1 (en) |
| TW (1) | TW201732B (en) |
| WO (1) | WO1993002052A1 (en) |
| ZA (1) | ZA925306B (en) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5436255A (en) * | 1992-07-23 | 1995-07-25 | Pfizer Inc. | Method of treating diseases susceptable to treatment by blocking NMDA-receptors |
| NZ255074A (en) * | 1992-10-30 | 1996-10-28 | Pfizer | 6-[2-(4-hydroxy-4-(4-substituted phenyl)piperidino)-1-hydroxypropyl]-3,4-dihydro-2(1h)-quinolones |
| US5498610A (en) * | 1992-11-06 | 1996-03-12 | Pfizer Inc. | Neuroprotective indolone and related derivatives |
| ZA9610745B (en) * | 1995-12-22 | 1997-06-24 | Warner Lambert Co | 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists |
| ZA9610738B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | Subtype selective nmda receptor ligands and the use thereof |
| ZA9610741B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | 4-Substituted piperidine analogs and their use as subtype selective nmda receptor antagonists |
| ZA9610736B (en) | 1995-12-22 | 1997-06-27 | Warner Lambert Co | 2-Substituted piperidine analogs and their use as subtypeselective nmda receptor antagonists |
| EP1182193A4 (en) * | 1999-04-09 | 2002-09-11 | Mochida Pharm Co Ltd | Remedies for neuropathic pain |
| EP1235572A2 (en) | 1999-10-29 | 2002-09-04 | MERCK SHARP & DOHME LTD. | Method to treat pain utilizing benzimidazole nmda/nr2b antagonists |
| US6489477B1 (en) | 1999-10-29 | 2002-12-03 | Merck & Co., Inc. | 2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists |
| US6432976B1 (en) | 1999-10-29 | 2002-08-13 | Merck & Co., Inc. | 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists |
| US6495561B2 (en) | 1999-10-29 | 2002-12-17 | Merck & Co., Inc. | 2-cyclohexyl imidazopyridine NMDA/NR2B antagonists |
| US6316474B1 (en) | 1999-10-29 | 2001-11-13 | Merck & Co., Inc. | 2-benzyl and 2-heteroaryl benzimidazole NMDA/NR2B antagonists |
| US6380205B1 (en) | 1999-10-29 | 2002-04-30 | Merck & Co., Inc. | 2-cyclohexyl quinazoline NMDA/NR2B antagonists |
| US6476041B1 (en) | 1999-10-29 | 2002-11-05 | Merck & Co., Inc. | 1,4 substituted piperidinyl NMDA/NR2B antagonists |
| US6291499B1 (en) | 1999-10-29 | 2001-09-18 | Merck & Co., Inc. | 2-cyclohexyl benzimidazole NMDA/NR2B antagonists |
| US6369076B1 (en) | 1999-10-29 | 2002-04-09 | Merck & Co. Inc. | 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists |
| EA005974B1 (en) | 2001-02-23 | 2005-08-25 | Мерк Энд Ко., Инк. | N-substituted nonaryl-heterocyclic nmda/nr2b antagonists |
| AU2002338334B8 (en) | 2001-04-03 | 2008-09-18 | Merck & Co., Inc. | N-substituted nonaryl-heterocyclo amidyl NMDA/NR2B antagonists |
| ATE522502T1 (en) | 2002-11-25 | 2011-09-15 | Mochida Pharm Co Ltd | THERAPEUTIC AGENT AGAINST RESPIRATORY DISEASES CONTAINING A 4-HYDROXYPIPERIDINE DERIVATIVE AS AN ACTIVE INGREDIENT |
| WO2005035523A1 (en) * | 2003-10-08 | 2005-04-21 | Pfizer Japan Inc. | Fused lactam compounds |
| TWI409289B (en) | 2010-09-02 | 2013-09-21 | Taiwan Union Technology Corp | Stable solution of the polymer prepared from n,o-heterocycles and its preparinging method and use |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PH17194A (en) * | 1980-03-06 | 1984-06-19 | Otsuka Pharma Co Ltd | Novel carbostyril derivatives,and pharmaceutical composition containing the same |
| FR2546166B1 (en) * | 1983-05-19 | 1985-10-25 | Synthelabo | ENANTIOMERS OF ERYTHRO (BENZYL-4 PIPERIDINO) -2 (HYDROXY-4 OR BENZYLOXY-4 PHENYL) -1 PROPANOL, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION |
| FR2640266B2 (en) * | 1988-07-12 | 1992-07-10 | Synthelabo | INDOLONES-2, QUINOLEINONES-2, BENZO (B) AZEPINONES-2 AND BENZIMIDAZOLONES-2 DERIVATIVES OF (HYDROXY-1 PIPERIDINYL-2 ALKYL), THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION |
| ES2098248T3 (en) * | 1989-05-17 | 1997-05-01 | Pfizer | DERIVATIVES OF 2-PIPERIDINE-1-ALCANOLS AS ANTI-ISCHEMICAL AGENTS. |
| US5306723A (en) * | 1990-05-10 | 1994-04-26 | Pfizer Inc. | Neuroprotective indolone and related derivatives |
-
1992
- 1992-06-19 BR BR9206272A patent/BR9206272A/en not_active Application Discontinuation
- 1992-06-19 EP EP92915510A patent/EP0594729A1/en not_active Ceased
- 1992-06-19 CA CA002113568A patent/CA2113568A1/en not_active Abandoned
- 1992-06-19 WO PCT/US1992/004973 patent/WO1993002052A1/en not_active Application Discontinuation
- 1992-06-19 JP JP5502784A patent/JP2571904B2/en not_active Expired - Lifetime
- 1992-06-19 CZ CS924008A patent/CZ284133B6/en not_active IP Right Cessation
- 1992-06-19 RU RU9294012366A patent/RU2065859C1/en active
- 1992-06-19 HU HU9400136A patent/HUT70528A/en unknown
- 1992-06-19 PL PL92302290A patent/PL169884B1/en unknown
- 1992-06-19 AU AU23225/92A patent/AU655840B2/en not_active Ceased
- 1992-06-23 TW TW081104921A patent/TW201732B/zh active
- 1992-07-12 IL IL102473A patent/IL102473A/en not_active IP Right Cessation
- 1992-07-15 PT PT100689A patent/PT100689B/en not_active IP Right Cessation
- 1992-07-16 NZ NZ243580A patent/NZ243580A/en unknown
- 1992-07-16 ZA ZA925306A patent/ZA925306B/en unknown
- 1992-07-16 IE IE231192A patent/IE922311A1/en not_active Application Discontinuation
- 1992-07-16 CN CN92105921A patent/CN1043759C/en not_active Expired - Fee Related
- 1992-07-16 EG EG39792A patent/EG20048A/en active
- 1992-07-16 MX MX9204190A patent/MX9204190A/en unknown
-
1994
- 1994-01-14 FI FI940192A patent/FI940192A/en unknown
- 1994-01-14 NO NO940144A patent/NO180445C/en not_active IP Right Cessation
- 1994-01-15 KR KR1019940700124A patent/KR0165003B1/en not_active IP Right Cessation
-
1998
- 1998-09-11 FI FI981956A patent/FI981956A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP0594729A1 (en) | 1994-05-04 |
| PL169884B1 (en) | 1996-09-30 |
| IL102473A0 (en) | 1993-01-14 |
| NO180445C (en) | 1997-04-23 |
| FI981956A0 (en) | 1998-09-11 |
| WO1993002052A1 (en) | 1993-02-04 |
| BR9206272A (en) | 1995-04-11 |
| EG20048A (en) | 1997-03-27 |
| FI940192A0 (en) | 1994-01-14 |
| PT100689A (en) | 1993-10-29 |
| RU2065859C1 (en) | 1996-08-27 |
| CA2113568A1 (en) | 1993-02-04 |
| KR0165003B1 (en) | 1999-01-15 |
| NO940144D0 (en) | 1994-01-14 |
| AU2322592A (en) | 1993-02-23 |
| NO180445B (en) | 1997-01-13 |
| TW201732B (en) | 1993-03-11 |
| FI940192A (en) | 1994-01-14 |
| AU655840B2 (en) | 1995-01-12 |
| ZA925306B (en) | 1994-01-17 |
| CN1043759C (en) | 1999-06-23 |
| CN1068566A (en) | 1993-02-03 |
| HUT70528A (en) | 1995-10-30 |
| MX9204190A (en) | 1993-01-01 |
| JPH06504293A (en) | 1994-05-19 |
| CZ284133B6 (en) | 1998-08-12 |
| IE922311A1 (en) | 1993-01-27 |
| NZ243580A (en) | 1994-10-26 |
| NO940144L (en) | 1994-01-14 |
| FI981956A (en) | 1998-09-11 |
| HU9400136D0 (en) | 1994-05-30 |
| PT100689B (en) | 1999-06-30 |
| JP2571904B2 (en) | 1997-01-16 |
| CZ400892A3 (en) | 1994-03-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| MM9K | Patent not in force due to non-payment of renewal fees |