DE2610228C2 - - Google Patents
Info
- Publication number
- DE2610228C2 DE2610228C2 DE2610228A DE2610228A DE2610228C2 DE 2610228 C2 DE2610228 C2 DE 2610228C2 DE 2610228 A DE2610228 A DE 2610228A DE 2610228 A DE2610228 A DE 2610228A DE 2610228 C2 DE2610228 C2 DE 2610228C2
- Authority
- DE
- Germany
- Prior art keywords
- parts
- general formula
- phenylethyl
- filtered
- phenylamino
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/333—Radicals substituted by oxygen or sulfur 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
- C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
- C07D211/66—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4 having a hetero atom as the second substituent in position 4
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
- C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
- C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Pain & Pain Management (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Hydrogenated Pyridines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Pyrrole Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US55851175A | 1975-03-14 | 1975-03-14 | |
| US05/648,685 US3998834A (en) | 1975-03-14 | 1976-01-13 | N-(4-piperidinyl)-n-phenylamides and -carbamates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| DE2610228A1 DE2610228A1 (de) | 1976-09-30 |
| DE2610228C2 true DE2610228C2 (US06291672-20010918-C00159.png) | 1990-04-05 |
Family
ID=27071767
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| DE19762610228 Granted DE2610228A1 (de) | 1975-03-14 | 1976-03-11 | N-(4-piperidinyl)-n-phenylamide und -carbamate, verfahren zu deren herstellung und diese verbindungen enthaltende arzneimittel |
Country Status (28)
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4179569A (en) * | 1975-03-14 | 1979-12-18 | Janssen Pharmaceutica N.V. | N-(4-piperidinyl)-N-phenylamides |
| US4208418A (en) * | 1975-09-23 | 1980-06-17 | Janssen Pharmaceutica N.V. | N-Aryl-N-(1-alkyl-4-piperidinyl)arylacetamides |
| US4225606A (en) * | 1975-09-23 | 1980-09-30 | Janssen Pharmaceutica N.V. | N-Aryl-N-(1-L-4-piperidinyl)arylacetamides |
| FR2389622B1 (US06291672-20010918-C00159.png) * | 1977-05-05 | 1982-05-21 | Janssen Pharmaceutica Nv | |
| US4167574A (en) * | 1978-03-13 | 1979-09-11 | Janssen Pharmaceutica, N.V. | N-phenyl-N-(4-piperidinyl)amides |
| US4584303A (en) * | 1984-04-09 | 1986-04-22 | The Boc Group, Inc. | N-aryl-N-(4-piperidinyl)amides and pharmaceutical compositions and method employing such compounds |
| FR2608602A1 (fr) * | 1986-12-23 | 1988-06-24 | Cerm Cent Europ Rech Mauvernay | Nouvelles 3-piperidineamines ou 3-azepineamines substituees, leur preparation et leurs applications en therapeutique |
| US4849521A (en) * | 1987-11-02 | 1989-07-18 | Boc, Inc. | Stereoselective preparation of 3-substituted-4-piperidine compounds and derivatives |
| US4957929A (en) * | 1987-11-02 | 1990-09-18 | Boc, Inc. | 4-phenyl-4-[N-(phenyl)amido]piperidine compounds and pharmaceutical compositions employing such compounds |
| US4791121A (en) * | 1987-11-02 | 1988-12-13 | The Boc Group, Inc. | 4-phenyl-4-(N-(phenyl)amido) piperidine derivatives and pharmaceutical compositions and method employing such compounds |
| USRE33495E (en) * | 1987-11-02 | 1990-12-18 | Boc, Inc. | Stereoselective preparation of 3-substituted-4-anilino-piperidine compounds and derivatives |
| US4921864A (en) * | 1987-11-02 | 1990-05-01 | Boc, Inc. | 4-Phenyl-4-(N-(phenyl)amido) piperidine derivatives and pharmaceutical compositions and method employing such compounds |
| US5013742A (en) * | 1987-11-02 | 1991-05-07 | Boc, Inc. | 4-phenyl-4-N-(phenyl) amido piperidine derivatives and pharmaceutical compositions and method employing such compounds |
| US4801615A (en) * | 1987-12-31 | 1989-01-31 | The Boc Group, Inc. | 4-heterohexacyclic-4-(N-(phenyl)amido) piperidine derivatives and pharmaceutical compositions and method employing such compounds |
| US4791120A (en) * | 1987-12-31 | 1988-12-13 | The Boc Group, Inc. | 4-heteropentacyclic-4-[N-(phenyl)amino] piperidine derivatives and pharmaceutical compositions and method employing such compounds |
| US5019583A (en) * | 1989-02-15 | 1991-05-28 | Glaxo Inc. | N-phenyl-N-(4-piperidinyl)amides useful as analgesics |
| US5053411A (en) * | 1989-04-20 | 1991-10-01 | Anaquest, Inc. | N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides and pharmaceutical compositions and methods employing such compounds |
| US5145967A (en) * | 1989-04-20 | 1992-09-08 | Anaquest, Inc. | Method for preparing 4-alkoxyalkyl-4-phenylaminopiperdines and derivatives thereof |
| USRE34201E (en) * | 1989-04-20 | 1993-03-23 | Anaquest, Inc. | N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides and pharmaceutical compositions and methods employing such compounds |
| US4994471A (en) * | 1989-05-12 | 1991-02-19 | Boc, Inc. | N-aryl-N-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds |
| US4939161A (en) * | 1989-05-12 | 1990-07-03 | Boc, Inc. | Analgesic N-aryl-N-[1-substituted-3,5-dimethyl-4-piperidinyl]amides |
| US5100903A (en) * | 1989-05-12 | 1992-03-31 | Anaquest, Inc. | N-aryl-n-(1-substituted-3-alkoxy-4-piperidinyl)amides and pharmaceutical compositions and methods employing such compounds |
| US5039804A (en) * | 1989-12-13 | 1991-08-13 | Glaxo Inc. | Preparation of substituted alkali metal piperidine-4-carboxylates |
| US5126455A (en) * | 1989-12-13 | 1992-06-30 | Glaxo Inc. | Preparation of substituted alkali metal piperidine-4-carboxylates |
| US5130321A (en) * | 1990-12-18 | 1992-07-14 | Glaxo Inc. | Analgesic n-phenyl-n-(3-or 1-3-me-4-piperidinyl)amides |
| US5214148A (en) * | 1990-12-18 | 1993-05-25 | Glaxo Inc. | Analgesic N-phenyl-N-(3-OR1 -3-ME-4-piperidinyl)amides |
| FR2676054B1 (fr) * | 1991-05-03 | 1993-09-03 | Sanofi Elf | Nouveaux composes n-alkylenepiperidino et leurs enantiomeres, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| GB9316863D0 (en) * | 1993-08-13 | 1993-09-29 | Glaxo Group Ltd | Chemical process |
| US5489689A (en) * | 1993-09-30 | 1996-02-06 | Mallinckrodt Chemical, Inc. | Preparation of piperidine derivatives |
| US6835194B2 (en) * | 1999-03-18 | 2004-12-28 | Durect Corporation | Implantable devices and methods for treatment of pain by delivery of fentanyl and fentanyl congeners |
| US6541021B1 (en) * | 1999-03-18 | 2003-04-01 | Durect Corporation | Devices and methods for pain management |
| WO2000061557A1 (fr) * | 1999-04-09 | 2000-10-19 | Mochida Pharmaceutical Co., Ltd. | Derives de 4-hydroxypiperidine ayant un effet anti-arythmique |
| US7361666B2 (en) * | 1999-05-25 | 2008-04-22 | Sepracor, Inc. | Heterocyclic analgesic compounds and methods of use thereof |
| US6677332B1 (en) | 1999-05-25 | 2004-01-13 | Sepracor, Inc. | Heterocyclic analgesic compounds and methods of use thereof |
| US6635661B2 (en) | 2000-05-25 | 2003-10-21 | Sepracor Inc. | Heterocyclic analgesic compounds and methods of use thereof |
| US7074935B2 (en) * | 1999-12-06 | 2006-07-11 | Mallinckrodt Inc. | Methods for the syntheses of alfentanil, sufentanil and remifentanil |
| US7074803B2 (en) * | 2001-03-02 | 2006-07-11 | Durect Corporation | Opioid formulations |
| US20040102476A1 (en) * | 2002-11-25 | 2004-05-27 | Chan Tai Wah | High concentration formulations of opioids and opioid derivatives |
| JPWO2006030931A1 (ja) * | 2004-09-14 | 2008-05-15 | 日本ケミファ株式会社 | Ｎ−置換−ｎ−（４−ピペリジニル）アミド誘導体 |
| JP2008088057A (ja) * | 2005-03-23 | 2008-04-17 | Nippon Chemiphar Co Ltd | Ｎ−置換−ｎ−（４−ピペリジニル）アミド誘導体 |
| AU2006317591A1 (en) * | 2005-11-17 | 2007-05-31 | Mallinckrodt Inc. | Process for synthesizing remifentanil |
| JP2009524659A (ja) * | 2006-01-24 | 2009-07-02 | マリンクロッド・インコーポレイテッド | レミフェンタニルの合成方法 |
| EP1867635A1 (en) * | 2006-06-15 | 2007-12-19 | Kern Pharma, S.L. | Process for preparing remifentanil, intermediates thereof, use of said intermediates and processes for their preparation |
| US20080009782A1 (en) * | 2006-06-28 | 2008-01-10 | Alza Corporation | Methods and Devices for Transdermal Electrotransport Delivery of Lofentanil and Carfentanil |
| WO2008005423A1 (en) * | 2006-07-03 | 2008-01-10 | Cambrex Charles City, Inc. | Improved method of making sufentanil |
| CA2670704A1 (en) * | 2006-11-29 | 2008-06-05 | Mallinckrodt Inc. | New process for remifentanil synthesis |
| WO2010027770A1 (en) * | 2008-09-04 | 2010-03-11 | Mallinckrodt Inc. | Crystalline forms of sufentanil citrate |
| US8299258B2 (en) * | 2008-11-04 | 2012-10-30 | Cambrex Charles City | Method of making piperidine derivatives |
| EP2616464B1 (en) | 2010-09-17 | 2018-01-03 | Mallinckrodt LLC | Improved process for the preparation of a precursor of sufentanil base |
| EP2455377B1 (de) | 2010-11-11 | 2014-07-09 | hameln rds gmbh | Synthese von Fentanyl Analoga |
| JP2014504184A (ja) | 2010-12-01 | 2014-02-20 | スパイナル・モデュレーション・インコーポレイテッド | 神経構造への薬剤の直接送達 |
| US10081654B2 (en) * | 2013-03-13 | 2018-09-25 | President And Fellows Of Harvard College | Stapled and stitched polypeptides and uses thereof |
| EP3233799B1 (en) | 2014-12-19 | 2021-05-19 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
| WO2016100940A1 (en) | 2014-12-19 | 2016-06-23 | The Broad Institute, Inc. | Dopamine d2 receptor ligands |
| EP3302473B1 (en) * | 2015-05-27 | 2020-07-08 | SpecGx LLC | Preparation of sufentanil citrate and sufentanil base |
| CN106854203B (zh) * | 2015-12-08 | 2020-12-01 | 江苏恩华药业股份有限公司 | 枸橼酸舒芬太尼的新晶型及其制备方法 |
| DK3199523T3 (en) | 2016-01-29 | 2018-11-26 | Bioka S R O | NEW PROCEDURE FOR THE PREPARATION OF N-PHENYL-N- (4-PIPERIDINYL) AMIDE DERIVATIVES, SUCH AS REMIFENTANIL AND CARFENTANIL |
| CN108503579B (zh) * | 2018-03-28 | 2021-03-26 | 南京医科大学 | 芬太尼类似物及其应用 |
| CN113214140B (zh) * | 2020-02-03 | 2022-09-09 | 江苏谛奇医药科技有限公司 | 哌啶酰胺类衍生物、其药物组合物及其应用 |
| US11708366B2 (en) | 2020-08-14 | 2023-07-25 | Novartis Ag | Heteroaryl substituted spiropiperidinyl derivatives and pharmaceutical uses thereof |
| CN114262320A (zh) * | 2021-12-28 | 2022-04-01 | 宜昌人福药业有限责任公司 | 一种利用连续流微通道反应器制备苯胺基哌啶类药物的合成方法 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE623427A (US06291672-20010918-C00159.png) * | 1961-10-10 | |||
| US3171838A (en) * | 1961-10-10 | 1965-03-02 | Res Lab Dr C Janssen N V | Aroylalkyl and hydroxyaralkyl derivatives of 4-(n-arylalkanamido)-piperidines and related compounds |
-
1976
- 1976-01-13 US US05/648,685 patent/US3998834A/en not_active Expired - Lifetime
- 1976-02-23 NO NO760591A patent/NO146162C/no unknown
- 1976-02-24 NZ NZ180096A patent/NZ180096A/xx unknown
- 1976-02-27 CA CA246,697A patent/CA1080232A/en not_active Expired
- 1976-02-27 SE SE7602740A patent/SE426486B/xx active Protection Beyond IP Right Term
- 1976-03-09 LU LU74511A patent/LU74511A1/xx unknown
- 1976-03-10 FR FR7606870A patent/FR2303546A1/fr active Granted
- 1976-03-10 GB GB9593/76A patent/GB1538938A/en not_active Expired
- 1976-03-11 HU HU76JA00000751A patent/HU172963B/hu unknown
- 1976-03-11 DE DE19762610228 patent/DE2610228A1/de active Granted
- 1976-03-12 DK DK110376A patent/DK148960C/da not_active IP Right Cessation
- 1976-03-12 IL IL49204A patent/IL49204A/xx unknown
- 1976-03-12 BG BG7632601A patent/BG28259A3/xx unknown
- 1976-03-12 AT AT184676A patent/AT359493B/de not_active IP Right Cessation
- 1976-03-12 PH PH18204A patent/PH12746A/en unknown
- 1976-03-12 IT IT48556/76A patent/IT1057988B/it active
- 1976-03-12 CH CH310476A patent/CH629486A5/de not_active IP Right Cessation
- 1976-03-12 YU YU652/76A patent/YU39960B/xx unknown
- 1976-03-12 JP JP51026226A patent/JPS5946217B2/ja not_active Expired
- 1976-03-12 FI FI760646A patent/FI61481C/fi not_active IP Right Cessation
- 1976-03-12 CZ CS761632A patent/CZ278060B6/cs unknown
- 1976-03-12 SU SU762332950A patent/SU1227109A3/ru active
- 1976-03-12 PL PL1976187910A patent/PL102474B1/pl unknown
- 1976-03-12 NL NLAANVRAGE7602612,A patent/NL185279C/xx not_active IP Right Cessation
- 1976-03-12 PT PT64898A patent/PT64898B/pt unknown
- 1976-03-12 ES ES446034A patent/ES446034A1/es not_active Expired
- 1976-03-12 IE IE527/76A patent/IE42512B1/en not_active IP Right Cessation
- 1976-03-15 AU AU12006/76A patent/AU503632B2/en not_active Expired
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 8110 | Request for examination paragraph 44 | ||
| D2 | Grant after examination | ||
| 8364 | No opposition during term of opposition |