RO91184B - Procedeu pentru prepararea unor derivati de 2,2'-iminobisetanol - Google Patents

Procedeu pentru prepararea unor derivati de 2,2'-iminobisetanol

Info

Publication number
RO91184B
RO91184B RO116496A RO11649684A RO91184B RO 91184 B RO91184 B RO 91184B RO 116496 A RO116496 A RO 116496A RO 11649684 A RO11649684 A RO 11649684A RO 91184 B RO91184 B RO 91184B
Authority
RO
Romania
Prior art keywords
radical
aryl
amino
alkyl
formula
Prior art date
Application number
RO116496A
Other languages
English (en)
Other versions
RO91184A (ro
Inventor
Lommen Guy Rosalia Eugene Van
Bruyn Marcel Frans Leopold De
Francis Josephine Schroven Marc
Original Assignee
Janssen Pharmaceutica N.V
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 Janssen Pharmaceutica N.V filed Critical Janssen Pharmaceutica N.V
Publication of RO91184A publication Critical patent/RO91184A/ro
Publication of RO91184B publication Critical patent/RO91184B/ro

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/79—Benzo [b] furans; Hydrogenated benzo [b] furans with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D307/81—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/66—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78—Ring systems having three or more relevant rings
    • C07D311/92—Naphthopyrans; Hydrogenated naphthopyrans

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Public Health (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Furan Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Inventia se refera la un procedeu pentru prepararea unor derivati de 2,2'-iminobisetanol cu proprietati utile în tratamentul si/sau prevenirea bililor sistemului coronaro-vasculant, care prezinta formula generala I: (vezi formula), în care R1 reprezinta un atom de hidfrogen, un radical alchil cu 1 ... 6 atomi de carbon la radicalul alchil, alchilcarbonil czu 1 ... 6 atomi de carbon, R4, R5, R6 si R7 reprezinta independent hidrogen sau alchil cu 1 ... 6 atomi de carbon, A1 si A2 reprezinta fiecare independent o legatura directa sau -CH2-, R10, R11, R12, R13, R14, R15, R16 si R17 reprezinta independent un atom de hidrogen sau halogen sau un radical alchil cu 1 ... 6 atomi de carbon, alchiloxi cu 1 ... 6 atomi de carbon, alchenil C2-6-meoxi, trifluormetil, hidroxi, amino, mono- sau di(alchil C1-6)amino, arilamino, aril-alchil C1-6-amino, ciano, nitro, aril, ariloxi, arilalchil (C1-6) oxi sau un radicalcu formula -(NHp-X-(Y)q-I (a) în care p si q sunt independent de O sau 1, X reprezinta radicalul -C=0, Y reprezinta - NH sau 0, L reprezinta un atom de hidrogen sau un radical alchil cu 1 ... 6 atomi de carbon, sau doi radicali vecini dintre R10, R11, R12 si R13 si dintre R14, R15, R16 si R17, luati împreuna pot forma un radical bivalent -CH=CH-CH=CH- sau -(CH2)4- cu conditia ca nu mai mult de doi radiali dintre R14, R15, R16 si R17 reprezinta amino, arilamino, mono- sau di (alchil C1-6)-amino, aril-alchil (C1-6)-amino, nitro, aril, ariloxi sau un radical de formula 8a) în care aril reprezinta fenil, eventual substituit cu pâna la trei substituenti, ales fiecare independent dintre halogen, alchil cu 1 ... 6 atomi de carbon, alchil (C1-6)-oxi, a
RO116496A 1983-12-05 1984-12-03 Procedeu pentru prepararea unor derivati de 2,2'-iminobisetanol RO91184B (ro)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US55808183A 1983-12-05 1983-12-05

Publications (2)

Publication Number Publication Date
RO91184A RO91184A (ro) 1987-07-30
RO91184B true RO91184B (ro) 1987-07-31

Family

ID=24228139

Family Applications (1)

Application Number Title Priority Date Filing Date
RO116496A RO91184B (ro) 1983-12-05 1984-12-03 Procedeu pentru prepararea unor derivati de 2,2'-iminobisetanol

Country Status (32)

Country Link
EP (1) EP0145067B1 (ro)
JP (1) JPS60132977A (ro)
KR (1) KR870000923B1 (ro)
AR (1) AR241414A1 (ro)
AT (1) ATE40361T1 (ro)
AU (1) AU573658B2 (ro)
BG (1) BG43866A3 (ro)
CA (1) CA1337429C (ro)
CS (1) CS250242B2 (ro)
CY (1) CY1609A (ro)
DD (1) DD235453A5 (ro)
DE (1) DE3476388D1 (ro)
DK (2) DK165112C (ro)
DZ (1) DZ712A1 (ro)
ES (1) ES8603870A1 (ro)
FI (1) FI82460C (ro)
GR (1) GR81098B (ro)
HK (1) HK52791A (ro)
HU (1) HU202219B (ro)
IE (1) IE57831B1 (ro)
IL (1) IL73706A (ro)
MA (1) MA20292A1 (ro)
NO (2) NO169839C (ro)
NZ (1) NZ210388A (ro)
PH (1) PH22432A (ro)
PL (1) PL146342B1 (ro)
PT (1) PT79609B (ro)
RO (1) RO91184B (ro)
SG (1) SG47091G (ro)
SU (1) SU1428199A3 (ro)
ZA (1) ZA849445B (ro)
ZW (1) ZW19784A1 (ro)

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CA1337432C (en) * 1988-03-23 1995-10-24 Raymond M. Xhonneux Method of lowering the blood pressure
JPH02103116U (ro) * 1989-02-01 1990-08-16
JPH02218675A (ja) * 1989-02-21 1990-08-31 Nippon Kayaku Co Ltd ６―フルオロクロモン―２―カルボン酸及びその製造法
TW199152B (ro) * 1990-11-01 1993-02-01 Takeda Pharm Industry Co Ltd
TW355683B (en) * 1994-02-17 1999-04-11 Janssen Pharmaceutica Nv Composition containing micronized nebivolol
DE69524528T2 (de) * 1994-10-14 2002-08-01 Merck Patent Gmbh ZNS wirksames (R)-(-)-2-[5-(4-Fluorophenyl)-3-pyridylmethylaminomethyl]chroman
WO1999032476A1 (en) * 1997-12-19 1999-07-01 Bayer Corporation Carboxyl substituted chroman derivatives useful as beta 3 adrenoreceptor agonists
US6362371B1 (en) 1998-06-08 2002-03-26 Advanced Medicine, Inc. β2- adrenergic receptor agonists
US6713651B1 (en) 1999-06-07 2004-03-30 Theravance, Inc. β2-adrenergic receptor agonists
US6683115B2 (en) 1999-06-02 2004-01-27 Theravance, Inc. β2-adrenergic receptor agonists
US6593497B1 (en) 1999-06-02 2003-07-15 Theravance, Inc. β2-adrenergic receptor agonists
UA73965C2 (en) 1999-12-08 2005-10-17 Theravance Inc b2 ADRENERGIC RECEPTOR ANTAGONISTS
UA73981C2 (en) 2000-03-10 2005-10-17 Merck Patent Gmbh (r)-(-)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]-chromane for treatment of extrapyramidal movement disorders (variants), pharmaceutical composition and kit
EP1406608B1 (en) 2001-05-02 2009-07-29 Nitromed, Inc. Nitrosated and nitrosylated nebivolol and its metabolites, compositions and methods of use
CA2455621C (en) 2001-07-26 2010-11-16 Merck Patent Gesellschaft Mit Beschraenkter Haftung Use of (r/s)-(-/+) or (s)-(+)-2-[5-(4-fluorophenyl)-3-pyridylmethylaminomethyl]chromane for the treatment of extrapyramidal movement disorders
TWI249515B (en) 2001-11-13 2006-02-21 Theravance Inc Aryl aniline beta2 adrenergic receptor agonists
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
EP1741712B1 (en) * 2004-07-30 2011-06-15 Torrent Pharmaceuticals Ltd amorphous form of nebivolol hydrochloride and its preparation
ATE465157T1 (de) * 2004-08-11 2010-05-15 Hetero Drugs Ltd Neues verfahren zur herstellung von nebivololzwischenprodukten
CN100341866C (zh) * 2004-08-30 2007-10-10 中国科学院理化技术研究所 α，α’－[亚氨基二（亚甲基）]－双－（6－氟－3，4－二氢－2H－1－苯并吡喃－2－甲醇）甲烷磺酸盐的合成方法
EP1848424B1 (en) * 2005-01-31 2017-04-05 Mylan Laboratories, Inc Pharmaceutical composition comprising hydroxylated nebivolol
EP1850842A1 (de) * 2005-02-11 2007-11-07 Stada Arzneimittel Ag Pharmazeutische zusammensetzungen nebivolo und ein hydrophiles polymer
AT502220A1 (de) * 2005-07-19 2007-02-15 Pharmacon Forschung & Beratung Verfahren zur herstellung von nebivolol
US7560575B2 (en) * 2005-12-28 2009-07-14 Acino Pharma Ag Process for preparation of racemic Nebivolol
EP1803716B1 (en) * 2005-12-28 2012-07-25 Acino Pharma AG A process for preparation of racemic nebivolol
WO2007083318A1 (en) 2006-01-18 2007-07-26 Hetero Drugs Limited Process for isolation of desired isomers of nebivolol intermediates
ITMI20061889A1 (it) * 2006-10-03 2008-04-04 Zambon Spa Processo di preparazione di nebivololo
DE602007007666D1 (de) 2006-11-27 2010-08-19 Zach System Spa Verfahren zur herstellung von nebivolol
WO2008089549A1 (en) 2007-01-22 2008-07-31 Genpharm Ulc Pharmaceutical compositions comprising nebivolol or a nebivolol analogue
CN101463024B (zh) 2007-12-21 2011-06-08 上海现代制药股份有限公司 一种制备rrrs和sssr型的奈必洛尔中间体混合物的方法
ITMI20080547A1 (it) * 2008-03-31 2009-10-01 Zach System Spa Processo di preparazione di nebivololo
IT1392067B1 (it) * 2008-10-31 2012-02-09 Zach System Spa Processo di preparazione di nebivololo
IT1395354B1 (it) * 2009-07-23 2012-09-14 Zach System Spa Processo di preparazione di nebivololo
DE102010005953A1 (de) 2010-01-27 2011-07-28 Corden PharmaChem GmbH, 68305 Verfahren zur Herstellung von Nebivolol
IT1397962B1 (it) 2010-02-11 2013-02-04 Menarini Int Operations Lu Sa Processo per la preparazione del nebivololo.
IT1402974B1 (it) 2010-11-30 2013-09-27 Menarini Int Operations Lu Sa Processo per la preparazione del nebivololo.
ITRM20110418A1 (it) 2011-08-02 2013-02-03 Menarini Int Operations Lu Sa Processo per la preparazione di epossidi quali intermedi per la sintesi del nebivololo.
EP2907809B1 (en) 2014-02-14 2018-08-22 Corden Pharma International GmbH Base-free process for the preparation of ketone intermediates usable for manufacture of nebivolol
EP2907810A1 (en) 2014-02-14 2015-08-19 Corden Pharma International GmbH A new method for producing nebivolol hydrochloride of high purity
DE102014107132A1 (de) 2014-05-20 2015-11-26 Corden Pharma International Gmbh Verfahren zur Herstellung von Epoxiden die in der Herstellung von Nebivolol und dessen Derivaten einsetzbar sind
KR20230068441A (ko) 2015-05-19 2023-05-17 저장 아우선 파마슈티칼 씨오., 엘티디. 네비볼롤 합성방법 및 그의 중간 화합물
CN105085499B (zh) * 2015-08-07 2018-09-25 上海现代制药海门有限公司 盐酸奈必洛尔中间体混合物的结晶分离方法

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GB8418472D0 (en) * 1984-07-19 1984-08-22 Beecham Group Plc Compounds

Also Published As

Publication number Publication date
ATE40361T1 (de) 1989-02-15
AU3632684A (en) 1985-06-13
BG43866A3 (en) 1988-08-15
ES538256A0 (es) 1986-01-01
EP0145067A3 (en) 1986-03-26
ZW19784A1 (en) 1986-07-02
CA1337429C (en) 1995-10-24
DK577084D0 (da) 1984-12-04
ES8603870A1 (es) 1986-01-01
SG47091G (en) 1991-07-26
AR241414A1 (es) 1992-07-31
KR850004485A (ko) 1985-07-15
DK11892D0 (da) 1992-01-31
IL73706A0 (en) 1985-03-31
NO844845L (no) 1985-06-06
FI82460B (fi) 1990-11-30
IL73706A (en) 1988-07-31
EP0145067A2 (en) 1985-06-19
RO91184A (ro) 1987-07-30
IE57831B1 (en) 1993-04-21
PT79609B (en) 1986-12-12
JPH0250114B2 (ro) 1990-11-01
DZ712A1 (fr) 2004-09-13
KR870000923B1 (ko) 1987-05-07
FI844777A0 (fi) 1984-12-04
DD235453A5 (de) 1986-05-07
IE843103L (en) 1985-06-05
PL250524A1 (en) 1986-02-25
CS250242B2 (en) 1987-04-16
HUT37418A (en) 1985-12-28
NO169839C (no) 1992-08-12
DK577084A (da) 1985-06-06
CY1609A (en) 1992-04-03
PL146342B1 (en) 1989-01-31
MA20292A1 (fr) 1985-07-01
HU202219B (en) 1991-02-28
ZA849445B (en) 1986-07-30
NO2004007I2 (no) 2005-05-09
EP0145067B1 (en) 1989-01-25
JPS60132977A (ja) 1985-07-16
SU1428199A3 (ru) 1988-09-30
AU573658B2 (en) 1988-06-16
HK52791A (en) 1991-07-19
PT79609A (en) 1985-01-01
PH22432A (en) 1988-09-12
DK11892A (da) 1992-01-31
GR81098B (en) 1984-12-17
NZ210388A (en) 1987-07-31
DK165112B (da) 1992-10-12
DK165321B (da) 1992-11-09
FI82460C (fi) 1991-03-11
FI844777L (fi) 1985-06-06
NO169839B (no) 1992-05-04
NO2004007I1 (no) 2004-12-20
DK165321C (da) 1993-03-29
DE3476388D1 (en) 1989-03-02
DK165112C (da) 1993-03-01

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