ES2088961T3 - N-fenil-n-(4-piperidinil)amidas utiles como analgesicos. - Google Patents

N-fenil-n-(4-piperidinil)amidas utiles como analgesicos.

Info

Publication number
ES2088961T3
ES2088961T3 ES90301586T ES90301586T ES2088961T3 ES 2088961 T3 ES2088961 T3 ES 2088961T3 ES 90301586 T ES90301586 T ES 90301586T ES 90301586 T ES90301586 T ES 90301586T ES 2088961 T3 ES2088961 T3 ES 2088961T3
Authority
ES
Spain
Prior art keywords
lower alkyl
group
alkoxy
member selected
carbonyl
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
Application number
ES90301586T
Other languages
English (en)
Other versions
ES2088961T4 (es
Inventor
Paul L Feldman
Michael K James
Marcus F Brackeen
Michael Ross Johnson
Harry Jefferson Leighton
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
SmithKline Beecham Corp
Original Assignee
Glaxo Wellcome Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Glaxo Wellcome Inc filed Critical Glaxo Wellcome Inc
Publication of ES2088961T3 publication Critical patent/ES2088961T3/es
Application granted granted Critical
Publication of ES2088961T4 publication Critical patent/ES2088961T4/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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
    • C07D211/10—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE DESCUBREN DERIVADOS DE N-FENILO-N-(4-PIPERIDINILO) AMIDAS QUE TIENEN LA FORMULA GENERAL (I): EN DONDE X ES UN MIEMBRO SELECCIONADO DEL GRUPO COMPUESTO DE: ALQUILO ALCOXILO-CARBONILO INFERIOR, ALQUILO INFERIOR ALQUILO-CARBONILO INFERIOR, ALQUILO ALQUENILOOXILO INFERIOR, Y ALQUILO (C1-2)ALCOXILO-(C1-2)ALCOXILO-CARBONILO INFERIOR. AR ES UN MIEMBRO SELECCIONADO DEL GRUPO COMPUESTO DE FENILO, FENILO MONO-, DI- Y TRISUSTITUIDO, EN DONDE CADA SUSTITUYENTE SE SELECCIONA INDEPENDIENTEMENTE DEL GRUPO COMPUESTO DE HALOGENO, ALQUILO INFERIOR, ALCOXILO INFERIOR Y TRIFLUOROMETILO; R ES UN MIEMBRO SELECCIONADO DEL GRUPO COMPUESTO DE ALQUILO INFERIOR, Y ALCOXILO- INFERIOR ALQUILO INFERIOR, Y R1 ES MIEMBRO SELECCIONADO DEL GRUPO COMPUESTO DE HIDROGENO, ALCOXILO INFERIOR CARBONILO, Y METOXIMETILO; Y R2 ES UN MIEMBRO SELECCIONADO DEL GRUPO COMPUESTO DE HIDROGENO Y METILO. Y LOS ISOMEROS DIASTOMEROS Y ENANTIOMEROS DE ELLOS, Y LAS SALES DE ADICION ACIDA DE DICHOS COMPUESTOS E ISOMEROS. LOS COMPUESTOS EXHIBEN ACTIVIDAD ANALGESICA, TENIENDO RELATIVAMENTE CORTA DURACION EN SU ACCION ANALGESICA. LA INVENCION CONTIENE LOS COMPUESTOS (I), COMPOSICIONES FARMACEUTICAS DE (I) Y METODOS DE PROVEER ANALGESIA CON (I). TAMBIEN INCLUYE CIERTOS NUEVOS PRODUCTOS INTERMEDIOS PARA OBTENER (I).
ES90301586T 1989-02-15 1990-02-14 N-fenil-n-(4-piperidinil)amidas utiles como analgesicos. Expired - Lifetime ES2088961T4 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31131189A 1989-02-15 1989-02-15
US07/448,497 US5019583A (en) 1989-02-15 1989-12-11 N-phenyl-N-(4-piperidinyl)amides useful as analgesics

Publications (2)

Publication Number Publication Date
ES2088961T3 true ES2088961T3 (es) 1996-10-01
ES2088961T4 ES2088961T4 (es) 1996-12-01

Family

ID=26977841

Family Applications (1)

Application Number Title Priority Date Filing Date
ES90301586T Expired - Lifetime ES2088961T4 (es) 1989-02-15 1990-02-14 N-fenil-n-(4-piperidinil)amidas utiles como analgesicos.

Country Status (22)

Country Link
US (1) US5019583A (es)
EP (1) EP0383579B1 (es)
JP (1) JP2895145B2 (es)
KR (1) KR0160979B1 (es)
AT (1) ATE140451T1 (es)
AU (1) AU636330B2 (es)
CA (1) CA2010011C (es)
CY (1) CY2002A (es)
CZ (1) CZ402591A3 (es)
DE (2) DE19675028I2 (es)
DK (1) DK0383579T3 (es)
ES (1) ES2088961T4 (es)
GR (1) GR3020719T3 (es)
HK (1) HK78297A (es)
IE (1) IE77156B1 (es)
LU (1) LU90011I2 (es)
MX (1) MX9203024A (es)
NL (1) NL960030I2 (es)
NZ (1) NZ232542A (es)
PT (1) PT93137B (es)
SG (1) SG47967A1 (es)
SK (1) SK402591A3 (es)

Families Citing this family (37)

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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
GB9316863D0 (en) * 1993-08-13 1993-09-29 Glaxo Group Ltd Chemical process
US5466700A (en) * 1993-08-30 1995-11-14 Glaxo Wellcome Inc. Anesthetic use of N-phenyl-N-(4-piperidinyl)amides
US5866591A (en) * 1996-09-11 1999-02-02 Glaxo Wellcome Inc. Stable formulations of remifentanil
CA2316341A1 (en) * 1997-12-24 1999-07-08 Ortho-Mcneil Pharmaceutical, Inc. 4-[aryl(piperidin-4-yl)] aminobenzamides which bind to the delta-opioid receptor
US6858018B1 (en) * 1998-09-28 2005-02-22 Vyteris, Inc. Iontophoretic devices
US6436959B1 (en) 1998-12-23 2002-08-20 Ortho-Mcneil Pharmaceutical, Inc. 4-[aryl(piperidin-4-yl)]aminobenzamides
EP1246801B1 (en) * 1999-12-06 2006-09-20 Mallinckrodt Inc. Methods for the syntheses of alfentanil, sufentanil and remifentanil
AU2001238690A1 (en) 2000-03-14 2001-09-24 Sepracor, Inc. 3-substituted piperidines comprising urea functionality, and methods of use thereof
ES2427976T5 (es) * 2000-07-31 2022-04-13 Takeda Pharma As Composición de sal de fentanilo para administración nasal
AU2002258714B2 (en) 2001-04-03 2007-03-01 Aryx Therapeutics Ultrashort-acting opioids for transdermal application
CA2469200A1 (en) * 2001-12-17 2003-06-26 Aryx Therapeutics Analgesic delivery systems and methods of use
JPWO2005030722A1 (ja) * 2003-09-29 2006-12-07 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
CA2570075A1 (en) 2004-06-18 2005-12-29 Neurosearch A/S Alkyl substituted piperidine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
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
WO2007061555A1 (en) * 2005-11-17 2007-05-31 Mallinckrodt Inc. Process for synthesizing remifentanil
EP1984336A2 (en) * 2006-01-24 2008-10-29 Mallinckrodt, Inc. Process for synthesizing remifentanil
AU2007212746A1 (en) * 2006-02-03 2007-08-16 Mallinckrodt Inc. Crystalline form of remifentanil hydrochloride
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
CA2657347C (en) 2006-07-10 2014-11-18 Paion Uk Limited Short-acting benzodiazepine salts and their polymorphic forms
GB0613693D0 (en) * 2006-07-10 2006-08-16 Cenes Ltd Benzodiazepine salts (3)
US20100099880A1 (en) * 2006-10-05 2010-04-22 Brian Cheng Alternate Process for Remifentanil Preparation
CA2670704A1 (en) * 2006-11-29 2008-06-05 Mallinckrodt Inc. New process for remifentanil synthesis
JP5580287B2 (ja) * 2008-03-31 2014-08-27 ザ ジェネラル ホスピタル コーポレイション 改善された薬物速度論的および薬力学的特性を有するエトミデート類似体
JP2011526257A (ja) * 2008-07-03 2011-10-06 シラグ アーゲー Ｎ−フェニル−ｎ−（４−ピペリジニル）アミド塩の製造方法
WO2010053944A1 (en) * 2008-11-04 2010-05-14 Cambrex Charles City, Inc. Improved method of making piperidine derivatives
CA2767112C (en) 2009-07-10 2018-06-19 The General Hospital Corporation Etomidate analogues that do not inhibit adrenocortical steroid synthesis
EP2450039A1 (en) 2010-11-08 2012-05-09 PAION UK Ltd. Dosing regimen for sedation with CNS 7056 (Remimazolam)
CN104168899B (zh) 2012-01-13 2017-04-05 通用医疗公司 麻醉剂化合物及其相关的使用方法
US20150259277A1 (en) 2012-10-08 2015-09-17 James Wallace Sleigh Ketamine Derivatives
AR094963A1 (es) 2013-03-04 2015-09-09 Ono Pharmaceutical Co Reacción de oxidación excelente en el índice de conversión
CN103728403B (zh) * 2013-08-30 2015-10-07 宜昌人福药业有限责任公司 一种盐酸瑞芬太尼原料药中有关物质的检测方法
SI3199523T1 (sl) 2016-01-29 2018-12-31 Bioka S.R.O. Nov postopek za pridobivanje n-fenil-n-(4-piperinidil)amidnih derivatov kot sta remifentanil in karfentanil
PT3643704T (pt) 2018-10-26 2021-03-08 Hameln Pharma Gmbh Novos intermediários para a preparação de hidrocloreto de remifentanil
GB202010168D0 (en) 2020-07-02 2020-08-19 Johnson Matthey Plc Process for preparing remifentanil hydrochloride
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 (8)

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Publication number Priority date Publication date Assignee Title
NL135583C (es) * 1961-10-10
US3655675A (en) * 1968-09-09 1972-04-11 Sterling Drug Inc N-(n-heteryl)-acylanilides
US4179569A (en) * 1975-03-14 1979-12-18 Janssen Pharmaceutica N.V. N-(4-piperidinyl)-N-phenylamides
US3998834A (en) * 1975-03-14 1976-12-21 Janssen Pharmaceutica N.V. N-(4-piperidinyl)-n-phenylamides and -carbamates
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
US4801721A (en) * 1984-08-16 1989-01-31 Ryan James W Stereospecific synthesis of carboxyalkyl peptides
CA1317940C (en) * 1987-09-25 1993-05-18 Georges H. P. Van Daele Substituted n-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides

Also Published As

Publication number Publication date
IE77156B1 (en) 1997-12-03
NZ232542A (en) 1992-06-25
EP0383579B1 (en) 1996-07-17
DE19675028I2 (de) 2002-11-07
KR0160979B1 (ko) 1998-12-01
HK78297A (en) 1997-06-20
CA2010011C (en) 1997-12-02
MX9203024A (es) 1992-07-01
SK402591A3 (en) 2000-09-12
US5019583A (en) 1991-05-28
JP2895145B2 (ja) 1999-05-24
LU90011I2 (fr) 1997-03-11
JPH02300167A (ja) 1990-12-12
DE69027794D1 (de) 1996-08-22
PT93137B (pt) 1996-02-29
AU636330B2 (en) 1993-04-29
DK0383579T3 (da) 1996-10-14
NL960030I1 (nl) 1997-02-03
ATE140451T1 (de) 1996-08-15
SG47967A1 (en) 1998-04-17
DE69027794T2 (de) 1997-01-02
CZ402591A3 (en) 1993-04-14
PT93137A (pt) 1990-08-31
KR900012906A (ko) 1990-09-03
ES2088961T4 (es) 1996-12-01
AU4973190A (en) 1990-08-23
NL960030I2 (nl) 1997-05-01
EP0383579A1 (en) 1990-08-22
IE900532L (en) 1990-08-15
CA2010011A1 (en) 1990-08-15
CY2002A (en) 1997-12-05
GR3020719T3 (en) 1996-11-30

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