ES2088961T4 - N-fenil-n-(4-piperidinil)amidas utiles como analgesicos. - Google Patents

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

Info

Publication number
ES2088961T4
ES2088961T4 ES90301586T ES90301586T ES2088961T4 ES 2088961 T4 ES2088961 T4 ES 2088961T4 ES 90301586 T ES90301586 T ES 90301586T ES 90301586 T ES90301586 T ES 90301586T ES 2088961 T4 ES2088961 T4 ES 2088961T4
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
ES2088961T3 (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
Application granted granted Critical
Publication of ES2088961T3 publication Critical patent/ES2088961T3/es
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)
  • 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)
  • 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 ES2088961T3 (es) 1996-10-01
ES2088961T4 true 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) DE69027794T2 (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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US5214148A (en) * 1990-12-18 1993-05-25 Glaxo Inc. Analgesic N-phenyl-N-(3-OR1 -3-ME-4-piperidinyl)amides
US5130321A (en) * 1990-12-18 1992-07-14 Glaxo Inc. Analgesic n-phenyl-n-(3-or 1-3-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
ES2251121T3 (es) * 1997-12-24 2006-04-16 Ortho-Mcneil Pharmaceutical, Inc. (4)-aril(piperidin-4-il) aminobenzamidas que se unen al receptor opioide delta.
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
ES2272354T3 (es) 1999-12-06 2007-05-01 Mallinckrodt Inc. Metodos para la sintesis de alfentanilo,sufentanilo remifentanilo.
WO2001068604A2 (en) 2000-03-14 2001-09-20 Sepracor, Inc. 3-substituted piperidines comprising urea functionality, and methods of use thereof
PL207845B1 (pl) * 2000-07-31 2011-02-28 Nycomed Danmark As Spray donosowy do dostarczania kompozycji farmaceutycznej zawierającej fentanyl i zastosowanie soli fentanylu do wytwarzania środka leczniczego
CA2443350A1 (en) * 2001-04-03 2002-12-05 Aryx Therapeutics Ultrashort-acting opioids for transdermal application
AU2002361709A1 (en) * 2001-12-17 2003-06-30 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
EP1761493A2 (en) 2004-06-18 2007-03-14 Neurosearch A/S Alkyl substituted piperidine derivatives and their use as monoamine neurotransmitter re-uptake inhibitors
WO2006030931A1 (ja) * 2004-09-14 2006-03-23 Nippon Chemiphar Co., Ltd. Ｎ－置換－ｎ－（４－ピペリジニル）アミド誘導体
JP2009515960A (ja) * 2005-11-17 2009-04-16 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
AU2007208438A1 (en) * 2006-01-24 2007-08-02 Mallinckrodt Inc. Process for synthesizing remifentanil
JP2009525329A (ja) * 2006-02-03 2009-07-09 マリンクロッド・インコーポレイテッド レミフェンタニル塩酸塩の結晶形
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
KR20090045233A (ko) 2006-07-10 2009-05-07 파이온 유케이 리미티드 속효형 벤조디아제핀 염 및 이의 중합체 형태
GB0613693D0 (en) * 2006-07-10 2006-08-16 Cenes Ltd Benzodiazepine salts (3)
WO2008045192A2 (en) * 2006-10-05 2008-04-17 Mallinckrodt Inc. Alternate process for remifentanil preparation
KR20090083422A (ko) * 2006-11-29 2009-08-03 말린크로트, 인코포레이티드 레미펜타닐의 신규 합성 방법
CN102046607B (zh) 2008-03-31 2014-06-11 通用医疗公司 具有提高的药物动力学性能和药效学性能的依托咪酯类似物
US20110144346A1 (en) * 2008-07-03 2011-06-16 Cilag Ag Method for producing n-phenyl-n-(4-piperidinyl) amide salts
US8299258B2 (en) * 2008-11-04 2012-10-30 Cambrex Charles City Method of making piperidine derivatives
CN102548964B (zh) 2009-07-10 2014-09-24 通用医疗公司 不抑制肾上腺皮质类固醇合成的依托咪酯类似物
EP2450039A1 (en) 2010-11-08 2012-05-09 PAION UK Ltd. Dosing regimen for sedation with CNS 7056 (Remimazolam)
WO2013106717A1 (en) 2012-01-13 2013-07-18 The General Hospital Corporation Anesthetic compounds and related methods of use
WO2014057414A1 (en) 2012-10-08 2014-04-17 Auckland Uniservices Limited 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
RS61517B1 (sr) 2018-10-26 2021-03-31 Hameln Pharma Gmbh Novi intermedijeri za pripremu remifentanil hidrohlorida
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

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BE623427A (es) * 1961-10-10
US3655675A (en) * 1968-09-09 1972-04-11 Sterling Drug Inc N-(n-heteryl)-acylanilides
US3998834A (en) * 1975-03-14 1976-12-21 Janssen Pharmaceutica N.V. N-(4-piperidinyl)-n-phenylamides and -carbamates
US4179569A (en) * 1975-03-14 1979-12-18 Janssen Pharmaceutica N.V. N-(4-piperidinyl)-N-phenylamides
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
SG47967A1 (en) 1998-04-17
CA2010011C (en) 1997-12-02
CZ402591A3 (en) 1993-04-14
CY2002A (en) 1997-12-05
AU636330B2 (en) 1993-04-29
CA2010011A1 (en) 1990-08-15
EP0383579A1 (en) 1990-08-22
ATE140451T1 (de) 1996-08-15
PT93137B (pt) 1996-02-29
ES2088961T3 (es) 1996-10-01
DE69027794D1 (de) 1996-08-22
KR900012906A (ko) 1990-09-03
IE900532L (en) 1990-08-15
IE77156B1 (en) 1997-12-03
US5019583A (en) 1991-05-28
PT93137A (pt) 1990-08-31
HK78297A (en) 1997-06-20
NL960030I1 (nl) 1997-02-03
DK0383579T3 (da) 1996-10-14
JP2895145B2 (ja) 1999-05-24
JPH02300167A (ja) 1990-12-12
MX9203024A (es) 1992-07-01
DE19675028I2 (de) 2002-11-07
DE69027794T2 (de) 1997-01-02
SK402591A3 (en) 2000-09-12
EP0383579B1 (en) 1996-07-17
KR0160979B1 (ko) 1998-12-01
NZ232542A (en) 1992-06-25
AU4973190A (en) 1990-08-23
LU90011I2 (fr) 1997-03-11
NL960030I2 (nl) 1997-05-01
GR3020719T3 (en) 1996-11-30

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