ES2155844T3 - Preparacion de n-alquilcarboxilatos de piperidinilo 3,4,4-trisustituidos e intermedios, utiles como antagonistas de opiaceos. - Google Patents

Preparacion de n-alquilcarboxilatos de piperidinilo 3,4,4-trisustituidos e intermedios, utiles como antagonistas de opiaceos.

Info

Publication number
ES2155844T3
ES2155844T3 ES94308951T ES94308951T ES2155844T3 ES 2155844 T3 ES2155844 T3 ES 2155844T3 ES 94308951 T ES94308951 T ES 94308951T ES 94308951 T ES94308951 T ES 94308951T ES 2155844 T3 ES2155844 T3 ES 2155844T3
Authority
ES
Spain
Prior art keywords
intermediates
trisustituidos
piperidinilo
optigian
alquilcarboxilatos
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
ES94308951T
Other languages
English (en)
Inventor
Scott Alan Frank
Douglas Edward Prather
Jeffrey Alan Ward
John Arnold Werner
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2155844T3 publication Critical patent/ES2155844T3/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
    • C07D211/08—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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D211/18—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 substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—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 substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

LA INVENCION SE REFIERE A UN PROCESO PARA LA PREPARACION DE 3,4,4TRISUBSTITUIDO-PIPERIDINIL-N-ALQUILCARBOXILATOS, INTERMEDIARIOS Y CONGENERES. FINALMENTE, EL INVENTO PROPORCIONA NUEVOS 3,4,4TRISUBSTITUIDO-PIPERIDINIL-N-ALQUILCARBOXILATOS DE FORMULA (4) Y COMPONENTES RELACIONADOS, UTILES COMO ANTAGONISTAS OPIOIDES.
ES94308951T 1993-12-08 1994-12-02 Preparacion de n-alquilcarboxilatos de piperidinilo 3,4,4-trisustituidos e intermedios, utiles como antagonistas de opiaceos. Expired - Lifetime ES2155844T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/164,074 US5434171A (en) 1993-12-08 1993-12-08 Preparation of 3,4,4-trisubstituted-piperidinyl-N-alkylcarboxylates and intermediates

Publications (1)

Publication Number Publication Date
ES2155844T3 true ES2155844T3 (es) 2001-06-01

Family

ID=22592858

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94308951T Expired - Lifetime ES2155844T3 (es) 1993-12-08 1994-12-02 Preparacion de n-alquilcarboxilatos de piperidinilo 3,4,4-trisustituidos e intermedios, utiles como antagonistas de opiaceos.

Country Status (31)

Country Link
US (1) US5434171A (es)
EP (3) EP0657428B1 (es)
JP (2) JP3834075B2 (es)
KR (1) KR100356239B1 (es)
CN (2) CN1057294C (es)
AT (1) ATE200279T1 (es)
AU (1) AU681198B2 (es)
BR (1) BR9404842A (es)
CA (1) CA2137221C (es)
CO (1) CO4290427A1 (es)
CZ (1) CZ290559B6 (es)
DE (1) DE69427017T2 (es)
DK (1) DK0657428T3 (es)
ES (1) ES2155844T3 (es)
FI (2) FI106455B (es)
GR (1) GR3036136T3 (es)
HK (1) HK1013826A1 (es)
HU (1) HUT71489A (es)
IL (1) IL111843A (es)
MY (1) MY121543A (es)
NO (1) NO302884B1 (es)
NZ (1) NZ270039A (es)
PE (1) PE41495A1 (es)
PL (1) PL181734B1 (es)
PT (1) PT657428E (es)
RU (1) RU2145958C1 (es)
SI (1) SI0657428T1 (es)
TW (1) TW290540B (es)
UA (1) UA52577C2 (es)
YU (2) YU49312B (es)
ZA (1) ZA949584B (es)

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HN1999000149A (es) 1998-09-09 2000-01-12 Pfizer Prod Inc Derivados de 4,4-biarilpiperidina
GB9912416D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912413D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912411D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912410D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912415D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
GB9912417D0 (en) 1999-05-28 1999-07-28 Pfizer Ltd Compounds useful in therapy
US6451806B2 (en) 1999-09-29 2002-09-17 Adolor Corporation Methods and compositions involving opioids and antagonists thereof
US6469030B2 (en) 1999-11-29 2002-10-22 Adolor Corporation Methods for the treatment and prevention of ileus
WO2002098422A1 (en) * 2001-06-05 2002-12-12 University Of Chicago Use of methylnaltrexone to treat immune suppression
US20030068829A1 (en) * 2001-06-25 2003-04-10 Symyx Technologies, Inc. High throughput crystallographic screening of materials
JP4814488B2 (ja) 2001-10-18 2011-11-16 ネクター セラピューティックス 重合体共役物オピオイドアンタゴニスト
US6794510B2 (en) * 2002-08-08 2004-09-21 Adolor Corporation Processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto
US7381721B2 (en) * 2003-03-17 2008-06-03 Adolor Corporation Substituted piperidine compounds
CA2521369A1 (en) * 2003-04-08 2004-10-28 Progenics Pharmaceuticals, Inc. The use of peripheral opiois antagonists, especially methylnaltrexone to treat irritable bowel syndrome
PL2368553T3 (pl) 2003-04-08 2015-05-29 Progenics Pharm Inc Preparaty farmaceutyczne zawierające metylonaltrekson
US6992090B2 (en) * 2003-06-16 2006-01-31 Adolor Corporation Substituted piperidine compounds and methods of their use
FR2861304B1 (fr) * 2003-10-23 2008-07-18 Univ Grenoble 1 Modulateurs des canaux cftr
US20050148630A1 (en) * 2003-12-02 2005-07-07 Carpenter Randall L. Methods of preventing and treating non-opioid induced gastrointestinal dysfunction
US8946262B2 (en) * 2003-12-04 2015-02-03 Adolor Corporation Methods of preventing and treating gastrointestinal dysfunction
US20060182692A1 (en) * 2003-12-16 2006-08-17 Fishburn C S Chemically modified small molecules
CN102895666B (zh) * 2003-12-16 2015-08-19 尼克塔治疗公司 化学改性的小分子
US7087749B2 (en) * 2004-03-11 2006-08-08 Adolor Corporation Substituted piperidine compounds and methods of their use
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US7700626B2 (en) * 2004-06-04 2010-04-20 Adolor Corporation Compositions containing opioid antagonists
US8039456B2 (en) 2004-08-12 2011-10-18 Helsinn Therapeutics (U.S.), Inc. Method of stimulating the motility of the gastrointestinal system using ipamorelin
ES2388501T3 (es) * 2004-08-12 2012-10-16 Helsinn Healthcare S.A. Uso de secretagogos de la hormona de crecimiento para estimular la motilidad del sistema gastrointestinal
US20060063792A1 (en) * 2004-09-17 2006-03-23 Adolor Corporation Substituted morphinans and methods of their use
US20060211733A1 (en) * 2005-03-04 2006-09-21 Adolor Corporation Methods of preventing and treating opioid bowel dysfunction
US8518962B2 (en) 2005-03-07 2013-08-27 The University Of Chicago Use of opioid antagonists
US9662325B2 (en) 2005-03-07 2017-05-30 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
MX2007010833A (es) * 2005-03-07 2009-02-17 Univ Chicago Uso de antagonistas opioides para atenuar proliferacion y migracion de células endoteliales.
US8524731B2 (en) 2005-03-07 2013-09-03 The University Of Chicago Use of opioid antagonists to attenuate endothelial cell proliferation and migration
AR057325A1 (es) 2005-05-25 2007-11-28 Progenics Pharm Inc Sintesis de (s)-n-metilnaltrexona, composiciones farmaceuticas y usos
AR057035A1 (es) 2005-05-25 2007-11-14 Progenics Pharm Inc SíNTESIS DE (R)-N-METILNALTREXONA, COMPOSICIONES FARMACÉUTICAS Y USOS
CN101262867A (zh) * 2005-07-01 2008-09-10 叶林发现公司 用于治疗肥胖的mao-b抑制剂
US7914776B2 (en) * 2005-10-07 2011-03-29 Adolor Corporation Solid dispersions of opioid antagonists
US20070092576A1 (en) * 2005-10-20 2007-04-26 Adolor Corporation Compositions containing opioid antagonists
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CN100383121C (zh) * 2006-03-07 2008-04-23 天津泰普药品科技发展有限公司 阿韦苄酯化合物及其制备方法和以该化合物制备阿韦莫哌的工艺
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CZ284993B6 (cs) * 1991-03-29 1999-04-14 Eli Lilly And Company Derivát piperidinu
US5250542A (en) * 1991-03-29 1993-10-05 Eli Lilly And Company Peripherally selective piperidine carboxylate opioid antagonists

Also Published As

Publication number Publication date
JPH07215937A (ja) 1995-08-15
BR9404842A (pt) 1995-08-08
DE69427017D1 (de) 2001-05-10
EP0984004A2 (en) 2000-03-08
EP0984004A3 (en) 2003-10-15
FI106860B (fi) 2001-04-30
PL181734B1 (pl) 2001-09-28
KR950017957A (ko) 1995-07-22
UA52577C2 (uk) 2003-01-15
US5434171A (en) 1995-07-18
YU49312B (sh) 2005-06-10
NO302884B1 (no) 1998-05-04
CN1057294C (zh) 2000-10-11
YU82304A (sh) 2006-03-03
HK1013826A1 (en) 1999-09-10
DE69427017T2 (de) 2001-09-06
CZ290559B6 (cs) 2002-08-14
NO944644L (no) 1995-06-09
EP1607387A2 (en) 2005-12-21
YU70294A (sh) 1997-07-31
CN1223257A (zh) 1999-07-21
IL111843A (en) 2000-02-29
NO944644D0 (no) 1994-12-02
FI945703A (fi) 1995-06-09
CA2137221A1 (en) 1995-06-09
CN1121387C (zh) 2003-09-17
JP3834075B2 (ja) 2006-10-18
FI20000353A (fi) 2000-02-17
PT657428E (pt) 2001-07-31
RU94042903A (ru) 1996-10-27
PE41495A1 (es) 1995-11-28
MY121543A (en) 2006-02-28
GR3036136T3 (en) 2001-09-28
KR100356239B1 (ko) 2002-12-26
TW290540B (es) 1996-11-11
EP1607387A3 (en) 2007-01-03
ATE200279T1 (de) 2001-04-15
NZ270039A (en) 1996-08-27
IL111843A0 (en) 1995-03-15
JP2006070042A (ja) 2006-03-16
SI0657428T1 (en) 2001-08-31
HUT71489A (en) 1995-11-28
EP0657428A1 (en) 1995-06-14
ZA949584B (en) 1996-06-03
CA2137221C (en) 2011-02-22
FI945703A0 (fi) 1994-12-02
FI106455B (fi) 2001-02-15
DK0657428T3 (da) 2001-05-07
PL306068A1 (en) 1995-06-12
AU7917094A (en) 1995-06-15
CN1111239A (zh) 1995-11-08
CZ299294A3 (en) 1995-10-18
AU681198B2 (en) 1997-08-21
EP0657428B1 (en) 2001-04-04
CO4290427A1 (es) 1996-04-17
HU9403466D0 (en) 1995-02-28
RU2145958C1 (ru) 2000-02-27

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