DE60116080T2 - 4-benzyl-1-[2-(4-hydroxy-phenoxy)-ethyl]-piperidin-3,4-diol - Google Patents
4-benzyl-1-[2-(4-hydroxy-phenoxy)-ethyl]-piperidin-3,4-diol Download PDFInfo
- Publication number
- DE60116080T2 DE60116080T2 DE60116080T DE60116080T DE60116080T2 DE 60116080 T2 DE60116080 T2 DE 60116080T2 DE 60116080 T DE60116080 T DE 60116080T DE 60116080 T DE60116080 T DE 60116080T DE 60116080 T2 DE60116080 T2 DE 60116080T2
- Authority
- DE
- Germany
- Prior art keywords
- benzyl
- piperidine
- hydroxy
- ethyl
- phenoxy
- 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 - Lifetime
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- 210000004962 mammalian cell Anatomy 0.000 description 1
- 238000002483 medication Methods 0.000 description 1
- 230000028161 membrane depolarization Effects 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 238000003801 milling Methods 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- LLYKPZOWCPVRPD-UHFFFAOYSA-N n,n-dimethylpyridin-2-amine;n,n-dimethylpyridin-4-amine Chemical compound CN(C)C1=CC=NC=C1.CN(C)C1=CC=CC=N1 LLYKPZOWCPVRPD-UHFFFAOYSA-N 0.000 description 1
- 230000016273 neuron death Effects 0.000 description 1
- 239000004090 neuroprotective agent Substances 0.000 description 1
- 230000000324 neuroprotective effect Effects 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 230000009871 nonspecific binding Effects 0.000 description 1
- 239000010502 orange oil Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 238000007911 parenteral administration Methods 0.000 description 1
- 238000012402 patch clamp technique Methods 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
- 229950007002 phosphocreatine Drugs 0.000 description 1
- 235000011007 phosphoric acid Nutrition 0.000 description 1
- HDOWRFHMPULYOA-UHFFFAOYSA-N piperidin-4-ol Chemical class OC1CCNCC1 HDOWRFHMPULYOA-UHFFFAOYSA-N 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- IENZQIKPVFGBNW-UHFFFAOYSA-N prazosin Chemical compound N=1C(N)=C2C=C(OC)C(OC)=CC2=NC=1N(CC1)CCN1C(=O)C1=CC=CO1 IENZQIKPVFGBNW-UHFFFAOYSA-N 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000001536 pro-arrhythmogenic effect Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 description 1
- 230000002336 repolarization Effects 0.000 description 1
- 239000012266 salt solution Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 230000009870 specific binding Effects 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000012085 test solution Substances 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000000080 wetting agent Substances 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
- C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/48—Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
- C07D211/50—Aroyl radical
-
- 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
- C07D211/36—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/40—Oxygen atoms
- C07D211/44—Oxygen atoms attached in position 4
- C07D211/48—Oxygen atoms attached in position 4 having an acyclic carbon atom attached in position 4
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00108769 | 2000-04-25 | ||
| EP00108769 | 2000-04-25 | ||
| PCT/EP2001/004305 WO2001081309A2 (en) | 2000-04-25 | 2001-04-17 | 4-benzyl-1-[2-(4-hydroxy-phenoxy)-ethyl]-piperidine-3,4-diol |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE60116080D1 DE60116080D1 (de) | 2006-01-26 |
| DE60116080T2 true DE60116080T2 (de) | 2006-08-24 |
Family
ID=8168543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE60116080T Expired - Lifetime DE60116080T2 (de) | 2000-04-25 | 2001-04-17 | 4-benzyl-1-[2-(4-hydroxy-phenoxy)-ethyl]-piperidin-3,4-diol |
Country Status (18)
| Country | Link |
|---|---|
| US (1) | US6432985B2 (OSRAM) |
| EP (1) | EP1278730B1 (OSRAM) |
| JP (1) | JP3831255B2 (OSRAM) |
| KR (1) | KR100527527B1 (OSRAM) |
| CN (1) | CN1178914C (OSRAM) |
| AR (1) | AR028357A1 (OSRAM) |
| AT (1) | ATE313527T1 (OSRAM) |
| AU (1) | AU785153B2 (OSRAM) |
| BR (1) | BR0110233A (OSRAM) |
| CA (1) | CA2407345C (OSRAM) |
| DE (1) | DE60116080T2 (OSRAM) |
| DK (1) | DK1278730T3 (OSRAM) |
| ES (1) | ES2254422T3 (OSRAM) |
| MX (1) | MXPA02010573A (OSRAM) |
| PE (1) | PE20011229A1 (OSRAM) |
| UY (1) | UY26681A1 (OSRAM) |
| WO (1) | WO2001081309A2 (OSRAM) |
| ZA (1) | ZA200208134B (OSRAM) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7640062B2 (en) | 2000-05-08 | 2009-12-29 | Brainsgate Ltd. | Methods and systems for management of alzheimer's disease |
| US7684859B2 (en) | 2002-04-25 | 2010-03-23 | Brainsgate Ltd. | Stimulation of the OTIC ganglion for treating medical conditions |
| US7005432B2 (en) * | 2002-05-16 | 2006-02-28 | Hoffman-La Roche Inc. | Substituted imidazol-pyridazine derivatives |
| EP1585430B1 (en) | 2002-11-14 | 2017-01-11 | Brainsgate Ltd. | Surgical tools and techniques for stimulation |
| US8010189B2 (en) * | 2004-02-20 | 2011-08-30 | Brainsgate Ltd. | SPG stimulation for treating complications of subarachnoid hemorrhage |
| US8055347B2 (en) | 2005-08-19 | 2011-11-08 | Brainsgate Ltd. | Stimulation for treating brain events and other conditions |
| US9233245B2 (en) | 2004-02-20 | 2016-01-12 | Brainsgate Ltd. | SPG stimulation |
| EP1976495A2 (en) * | 2006-01-06 | 2008-10-08 | Aarhus Universitet | Compounds acting on the serotonin transporter |
| BRPI0811844A2 (pt) * | 2007-05-21 | 2014-11-18 | Reviva Pharmaceuticals Inc | Composto, e, método para tratar um paciente |
| US8008253B2 (en) * | 2007-07-03 | 2011-08-30 | Andrew Tasker | Treatment for anxiety |
| US7860569B2 (en) | 2007-10-18 | 2010-12-28 | Brainsgate, Ltd. | Long-term SPG stimulation therapy for prevention of vascular dementia |
| KR20100135847A (ko) * | 2008-03-27 | 2010-12-27 | 에보텍 뉴로사이언시즈 게엠베하 | Ｎｍｄａ ｎｒ２ｂ―서브타입 선택적 길항제를 사용한 질병 치료 방법 |
| US8815508B2 (en) | 2008-08-12 | 2014-08-26 | Zinfandel Pharmaceuticals, Inc. | Method of identifying disease risk factors |
| US8846315B2 (en) | 2008-08-12 | 2014-09-30 | Zinfandel Pharmaceuticals, Inc. | Disease risk factors and methods of use |
| MA34828B1 (fr) | 2011-01-10 | 2014-01-02 | Zinfandel Pharmaceuticals Inc | Procédés et produits médicamenteux destinés au traitement de la maladie d'alzheimer |
| US8703763B2 (en) * | 2011-03-02 | 2014-04-22 | Hoffmann-La Roche Inc. | Bridged piperidine derivatives |
| EP2878335B1 (en) | 2013-11-10 | 2018-01-03 | Brainsgate Ltd. | Implant and delivery system for neural stimulator |
| EP3233799B1 (en) | 2014-12-19 | 2021-05-19 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
| EP3233077A4 (en) | 2014-12-19 | 2018-08-08 | The Broad Institute Inc. | Dopamine d2 receptor ligands |
| US10271907B2 (en) | 2015-05-13 | 2019-04-30 | Brainsgate Ltd. | Implant and delivery system for neural stimulator |
| EP3538516B1 (en) * | 2016-11-08 | 2021-06-16 | F. Hoffmann-La Roche AG | Phenoxytriazoles |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA9610738B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | Subtype selective nmda receptor ligands and the use thereof |
| ZA9610745B (en) | 1995-12-22 | 1997-06-24 | Warner Lambert Co | 4-Subsituted piperidine analogs and their use as subtype selective nmda receptor antagonists |
| TW498067B (en) | 1996-07-19 | 2002-08-11 | Hoffmann La Roche | 4-hydroxy-piperidine derivatives |
-
2001
- 2001-03-19 US US09/811,888 patent/US6432985B2/en not_active Expired - Fee Related
- 2001-04-17 JP JP2001578404A patent/JP3831255B2/ja not_active Expired - Fee Related
- 2001-04-17 WO PCT/EP2001/004305 patent/WO2001081309A2/en not_active Ceased
- 2001-04-17 DK DK01933833T patent/DK1278730T3/da active
- 2001-04-17 CA CA002407345A patent/CA2407345C/en not_active Expired - Fee Related
- 2001-04-17 KR KR10-2002-7014261A patent/KR100527527B1/ko not_active Expired - Fee Related
- 2001-04-17 CN CNB018085911A patent/CN1178914C/zh not_active Expired - Fee Related
- 2001-04-17 DE DE60116080T patent/DE60116080T2/de not_active Expired - Lifetime
- 2001-04-17 AT AT01933833T patent/ATE313527T1/de not_active IP Right Cessation
- 2001-04-17 MX MXPA02010573A patent/MXPA02010573A/es active IP Right Grant
- 2001-04-17 ES ES01933833T patent/ES2254422T3/es not_active Expired - Lifetime
- 2001-04-17 EP EP01933833A patent/EP1278730B1/en not_active Expired - Lifetime
- 2001-04-17 AU AU60213/01A patent/AU785153B2/en not_active Ceased
- 2001-04-17 BR BR0110233-8A patent/BR0110233A/pt not_active Application Discontinuation
- 2001-04-19 PE PE2001000359A patent/PE20011229A1/es not_active Application Discontinuation
- 2001-04-23 AR ARP010101869A patent/AR028357A1/es active IP Right Grant
- 2001-04-24 UY UY26681A patent/UY26681A1/es not_active Application Discontinuation
-
2002
- 2002-10-09 ZA ZA200208134A patent/ZA200208134B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| KR20040007216A (ko) | 2004-01-24 |
| CN1443166A (zh) | 2003-09-17 |
| AR028357A1 (es) | 2003-05-07 |
| EP1278730A2 (en) | 2003-01-29 |
| US20010047014A1 (en) | 2001-11-29 |
| ZA200208134B (en) | 2004-01-22 |
| ES2254422T3 (es) | 2006-06-16 |
| DE60116080D1 (de) | 2006-01-26 |
| WO2001081309A3 (en) | 2002-01-17 |
| KR100527527B1 (ko) | 2005-11-09 |
| CN1178914C (zh) | 2004-12-08 |
| BR0110233A (pt) | 2003-01-21 |
| JP2004509837A (ja) | 2004-04-02 |
| CA2407345A1 (en) | 2001-11-01 |
| JP3831255B2 (ja) | 2006-10-11 |
| ATE313527T1 (de) | 2006-01-15 |
| AU785153B2 (en) | 2006-10-05 |
| MXPA02010573A (es) | 2003-03-10 |
| EP1278730B1 (en) | 2005-12-21 |
| WO2001081309A2 (en) | 2001-11-01 |
| CA2407345C (en) | 2009-04-07 |
| UY26681A1 (es) | 2001-10-25 |
| AU6021301A (en) | 2001-11-07 |
| DK1278730T3 (da) | 2006-05-01 |
| PE20011229A1 (es) | 2001-12-08 |
| US6432985B2 (en) | 2002-08-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8364 | No opposition during term of opposition |