DK169331B1 - Fremgangsmåde til fremstilling af optisk aktive R(+)-carbazolderivater, nye R(+)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser - Google Patents

Fremgangsmåde til fremstilling af optisk aktive R(+)-carbazolderivater, nye R(+)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser Download PDF

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Publication number
DK169331B1
DK169331B1 DK255184A DK255184A DK169331B1 DK 169331 B1 DK169331 B1 DK 169331B1 DK 255184 A DK255184 A DK 255184A DK 255184 A DK255184 A DK 255184A DK 169331 B1 DK169331 B1 DK 169331B1
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Denmark
Prior art keywords
group
lower alkyl
pharmacologically acceptable
carbazole
alkyl group
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DK255184A
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Danish (da)
English (en)
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DK255184D0 (da
DK255184A (da
Inventor
Herbert Leinert
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Boehringer Mannheim Gmbh
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Application filed by Boehringer Mannheim Gmbh filed Critical Boehringer Mannheim Gmbh
Publication of DK255184D0 publication Critical patent/DK255184D0/da
Publication of DK255184A publication Critical patent/DK255184A/da
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/08—Vasodilators for multiple indications
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/82—Carbazoles; Hydrogenated carbazoles
    • C07D209/88—Carbazoles; Hydrogenated carbazoles 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 carbon atoms of the ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/14—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by free hydroxyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/16—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18—Radicals substituted by singly bound oxygen or sulfur atoms
    • C07D317/20—Free hydroxyl or mercaptan

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (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)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epoxy Compounds (AREA)
DK255184A 1983-05-26 1984-05-24 Fremgangsmåde til fremstilling af optisk aktive R(+)-carbazolderivater, nye R(+)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser DK169331B1 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE3319027 1983-05-26
DE19833319027 DE3319027A1 (de) 1983-05-26 1983-05-26 Verfahren zur herstellung von optisch aktiven carbazol-derivaten, neue r- und s-carbazol-derivate, sowie arzneimittel, die diese verbindungen enthalten

Publications (3)

Publication Number Publication Date
DK255184D0 DK255184D0 (da) 1984-05-24
DK255184A DK255184A (da) 1984-11-27
DK169331B1 true DK169331B1 (da) 1994-10-10

Family

ID=6199873

Family Applications (2)

Application Number Title Priority Date Filing Date
DK255184A DK169331B1 (da) 1983-05-26 1984-05-24 Fremgangsmåde til fremstilling af optisk aktive R(+)-carbazolderivater, nye R(+)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser
DK091393A DK169333B1 (da) 1983-05-26 1993-08-06 Fremgangsmåde til fremstilling af optisk aktive S(-)-carbazolderivater, nye S(-)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser

Family Applications After (1)

Application Number Title Priority Date Filing Date
DK091393A DK169333B1 (da) 1983-05-26 1993-08-06 Fremgangsmåde til fremstilling af optisk aktive S(-)-carbazolderivater, nye S(-)-carbazolderivater, samt lægemidler, der indeholder disse forbindelser

Country Status (20)

Country Link
US (4) US4697022A (fr)
EP (1) EP0127099B1 (fr)
JP (2) JPS59222473A (fr)
KR (1) KR860001761B1 (fr)
AT (1) ATE27273T1 (fr)
AU (1) AU551116B2 (fr)
CA (1) CA1259071A (fr)
DE (2) DE3319027A1 (fr)
DK (2) DK169331B1 (fr)
ES (1) ES8502683A1 (fr)
FI (1) FI80018C (fr)
GR (1) GR81577B (fr)
HU (1) HU193011B (fr)
IE (1) IE57533B1 (fr)
IL (1) IL71876A (fr)
NO (1) NO164537C (fr)
NZ (1) NZ208254A (fr)
PH (1) PH22749A (fr)
PT (1) PT78633B (fr)
ZA (1) ZA843976B (fr)

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US5359097A (en) * 1988-12-26 1994-10-25 Kowa Company Ltd. Process for preparation of glycidyl ether
WO1994020096A1 (fr) * 1993-03-05 1994-09-15 Boehringer Mannheim Pharmaceuticals Corporation - Smithkline Beckman Corporation Limited Procede d'utilisation de carbazolyle-(4)-oxypropanolamine pour inhiber la proliferation de cellules de muscles lisses
US5308862A (en) * 1993-03-05 1994-05-03 Boehringer Mannheim Pharmaceuticals Corporation - Smithkline Beecham Corp., Ltd. Partnership No. 1 Use of, and method of treatment using, carbazolyl-(4)-oxypropanolamine compounds for inhibition of smooth muscle cell proliferation
US5629345A (en) * 1993-07-23 1997-05-13 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5965620A (en) * 1993-07-23 1999-10-12 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5760069A (en) 1995-02-08 1998-06-02 Boehringer Mannheim Pharmaceuticals Corporation-Smithkline Beecham Corporation Limited Partnership #1 Method of treatment for decreasing mortality resulting from congestive heart failure
ZA967892B (en) * 1995-09-21 1998-03-18 Lilly Co Eli Selective β3 adrenergic agonists.
US6075040A (en) * 1996-09-05 2000-06-13 Eli Lilly And Company Selective β3 adrenergic agonists
WO1998002157A1 (fr) * 1996-07-13 1998-01-22 Roche Diagnostics Gmbh Formulations pharmaceutiques pour utilisation topique contenant comme principe actif un derive de carbazolyl-(4)-oxy-propanolamine
ATE215369T1 (de) 1996-09-05 2002-04-15 Lilly Co Eli Carbazolanaloge als selektive beta3-adrenergische agonisten
US6730326B2 (en) 1997-07-22 2004-05-04 Roche Diagnostics Gmbh Thermodynamically stable modification of 1-(4-carbazolyl-oxy-3[2-(2-methoxyphenoxy)-ethylamino]-2-propanol process for its preparation and pharmaceutical compositions containing it
EP0893440A1 (fr) * 1997-07-22 1999-01-27 Roche Diagnostics GmbH Une modification thermodynamique stabilisée de 1-(4-carbazolyloxy)-3[2-(2-methoxyphenoxy)ethylamino]- 2-propanole, un procédé pour sa préparation et une composition pharmaceutique qui la contient
ZA989365B (en) * 1997-10-15 1999-04-15 Boehringer Mannheim Pharm Corp Preparation for treating alzheimer's disease
HU227441B1 (en) * 1997-11-24 2011-06-28 Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag Process for producing carvedilol, enantiomers and salts thereof
CO5011072A1 (es) * 1997-12-05 2001-02-28 Lilly Co Eli Etanolaminas pirazinil substituidas como agfonistas de los receptores
US6664284B2 (en) * 1998-07-23 2003-12-16 Roche Diagnostics Gmbh Stabilized carvedilol injection solution
US20010036959A1 (en) * 2000-04-03 2001-11-01 Gabel Rolf Dieter Carvedilol-hydrophilic solutions
ES2227206T3 (es) * 2000-04-03 2005-04-01 F. Hoffmann-La Roche Ag Soluciones concentradas de carvedilol.
PL365694A1 (en) 2000-06-28 2005-01-10 Teva Pharmaceutical Industries Ltd. Carvedilol
KR100342659B1 (en) 2000-12-15 2002-07-04 Rstech Co Ltd Chiral polymer salene catalyst and process for preparing chiral compounds from racemic epoxide using the same
BR0212927A (pt) * 2001-09-28 2004-10-13 Hoffmann La Roche Formas pseudopolimórficas de carvedilol
US8101209B2 (en) * 2001-10-09 2012-01-24 Flamel Technologies Microparticulate oral galenical form for the delayed and controlled release of pharmaceutical active principles
US6710184B2 (en) 2002-01-15 2004-03-23 Teva Pharmaceutical Industries Ltd. Crystalline solids of carvedilol and processes for their preparation
EP1499310A4 (fr) * 2002-04-30 2005-12-07 Sb Pharmco Inc Monocitrate monohydrate de carvedilol
AU2003251627A1 (en) * 2002-06-27 2004-01-19 Sb Pharmco Puerto Rico Inc. Carvedilol hydrobromide
MXPA04012923A (es) * 2002-06-27 2005-03-31 Sb Pharmco Inc Sales de fosfato de carvedilol y/o solvatos de las mismas, composiciones correspondientes y/o metodos de tratamiento.
SK285547B6 (sk) 2002-11-08 2007-03-01 Zentiva, A. S. Spôsob prípravy Carvedilolu
WO2004094378A1 (fr) * 2003-04-21 2004-11-04 Matrix Laboratories Ltd Procede de fabrication de carvedilol, forme-ii
WO2004113296A1 (fr) * 2003-06-20 2004-12-29 Sun Pharmaceutical Industries Limited Procede de preparation de 1-[9h-carbazol-4-yloxy]- 3-[{2-(2-(-(methoxy)phenoxy)-ethyl}-amino]-propane-2-ol
JP2007512372A (ja) * 2003-11-25 2007-05-17 エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド カルベジロール塩、対応する組成物、送達および／または治療方法
EP1691789B1 (fr) * 2003-11-25 2017-12-20 SmithKline Beecham (Cork) Limited Base libre de carvedilol, ses sels, formes anhydres ou solvates, compositions pharmaceutiques correspondantes, formulations a liberation controlee, et procedes de traitement ou d'administration
WO2005051325A2 (fr) * 2003-11-25 2005-06-09 Sb Pharmco Puerto Rico Inc. Base libre de carvedilol, ses sels, formes anhydres ou solvats, compositions pharmaceutiques correspondantes, formulations a liberation controlee, et methodes de traitement ou d'administration
EP1723107A2 (fr) 2004-02-23 2006-11-22 Cadila Healthcare Ltd. Procede de preparation de carvedilol racemique
US20070191456A1 (en) * 2004-04-22 2007-08-16 Tarur Venkatasubramanian R Novel process for the preparation of 1-(9h-carbazol-4-yloxy)-3-[[2-(-methoxyphenoxy)-ethyl] amino]-propan-2-ol
GB0411273D0 (en) * 2004-05-20 2004-06-23 Cipla Ltd Process and product
DK1838670T3 (da) * 2004-12-09 2010-03-01 Zach System Spa Fremgangsmåde til fremstilling af carvedilol og dets enantiomere
US20070043099A1 (en) * 2005-06-09 2007-02-22 Igor Lifshitz Crystalline forms of carvedilol and processes for their preparation
WO2007077111A1 (fr) * 2005-12-30 2007-07-12 F. Hoffmann-La Roche Ag Composés et méthodes pour la synthèse de carbazole
WO2008002683A2 (fr) * 2006-06-28 2008-01-03 Teva Pharmaceutical Industries Ltd. Carvédilol phosphate
WO2008038301A1 (fr) * 2006-09-26 2008-04-03 Morepen Laboratories Limited Procédé pour la préparation de carvédilol
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CN102285910B (zh) * 2011-07-04 2013-06-19 南京工业大学 一种制备(s)-卡维地洛的方法
CN102617368B (zh) * 2012-02-27 2014-07-09 华中科技大学 一种α/β受体双重抑制剂及其盐的制备方法
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US20230381139A1 (en) * 2020-09-17 2023-11-30 Uti Limited Partnership Methods of treating and/or preventing alzheimer’s disease with r-carvedilol
CN116041248B (zh) * 2023-04-03 2023-06-06 成都摩诃大龙医药科技有限公司 一种具有抗癌活性的咔唑衍生物及其制备方法和应用

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Also Published As

Publication number Publication date
AU2848084A (en) 1984-11-29
NO164537C (no) 1990-10-17
JPH0613508B2 (ja) 1994-02-23
DK169333B1 (da) 1994-10-10
JPH05208957A (ja) 1993-08-20
FI842046A (fi) 1984-11-27
US5071868A (en) 1991-12-10
IE57533B1 (en) 1993-03-24
DK91393A (da) 1993-08-06
US4697022A (en) 1987-09-29
PT78633B (de) 1986-06-18
PT78633A (de) 1984-06-01
HU193011B (en) 1987-08-28
PH22749A (en) 1988-11-28
FI80018B (fi) 1989-12-29
IE841295L (en) 1984-11-26
NO164537B (no) 1990-07-09
FI842046A0 (fi) 1984-05-22
ATE27273T1 (de) 1987-06-15
US4985454A (en) 1991-01-15
DE3319027A1 (de) 1984-11-29
HUT34160A (en) 1985-02-28
DK255184D0 (da) 1984-05-24
IL71876A0 (en) 1984-09-30
EP0127099A1 (fr) 1984-12-05
NO842084L (no) 1984-11-27
AU551116B2 (en) 1986-04-17
US4824963A (en) 1989-04-25
NZ208254A (en) 1988-11-29
DK91393D0 (da) 1993-08-06
KR840009088A (ko) 1984-12-24
JPH0527622B2 (fr) 1993-04-21
ES532838A0 (es) 1985-02-01
FI80018C (fi) 1990-04-10
IL71876A (en) 1987-10-30
DE3463768D1 (en) 1987-06-25
CA1259071A (fr) 1989-09-05
ES8502683A1 (es) 1985-02-01
KR860001761B1 (ko) 1986-10-21
GR81577B (fr) 1984-12-11
EP0127099B1 (fr) 1987-05-20
JPS59222473A (ja) 1984-12-14
ZA843976B (en) 1985-01-30
DK255184A (da) 1984-11-27

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B1 Patent granted (law 1993)
PUP Patent expired