MA33375B1 - Procédé de préparation de l'ibodutant (men15596) et intermédiaires apparentés - Google Patents

Procédé de préparation de l'ibodutant (men15596) et intermédiaires apparentés

Info

Publication number
MA33375B1
MA33375B1 MA34472A MA34472A MA33375B1 MA 33375 B1 MA33375 B1 MA 33375B1 MA 34472 A MA34472 A MA 34472A MA 34472 A MA34472 A MA 34472A MA 33375 B1 MA33375 B1 MA 33375B1
Authority
MA
Morocco
Prior art keywords
ibodutant
men15596
preparing
alpha
coupling
Prior art date
Application number
MA34472A
Other languages
Arabic (ar)
English (en)
Inventor
Fabrizio Bonaccorsi
Valentina Fedi
Danilo Giannotti
Original Assignee
Malesci Sas
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 Malesci Sas filed Critical Malesci Sas
Publication of MA33375B1 publication Critical patent/MA33375B1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Steroid Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La présente invention concerne un nouveau procédé de synthèse du produit nommé ibodutant présenté sur la figure ci-jointe, constitué de peu d'étapes à haut rendement faisant intervenir des réactifs et des solvants présentant un faible impact sur l'environnement. Ledit procédé est caractérisé par le couplage de deux parties, à savoir les composés (3) et (4), l'un d'eux (3) étant synthétisé par couplage de l'acide 6-méthyl-2-benzo[b]thiophènecarboxylique (1) avec l'acide 1-amino-alpha-alpha-cyclopentanecarboxylique et cyclisation ultérieure avec l'oxazolone, tandis que l'autre, le composé (4), est obtenu à partir de fonctionnalisations hautement sélectives appropriées de la 4-aminométhylpipéridine (2).
MA34472A 2009-05-21 2010-05-11 Procédé de préparation de l'ibodutant (men15596) et intermédiaires apparentés MA33375B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2009A000897A IT1394304B1 (it) 2009-05-21 2009-05-21 Processo per la preparazione di ibodutant (men15596) e relativi intermedi
PCT/EP2010/002884 WO2010133306A1 (fr) 2009-05-21 2010-05-11 Procédé de préparation de l'ibodutant (men15596) et intermédiaires apparentés

Publications (1)

Publication Number Publication Date
MA33375B1 true MA33375B1 (fr) 2012-06-01

Family

ID=41264221

Family Applications (1)

Application Number Title Priority Date Filing Date
MA34472A MA33375B1 (fr) 2009-05-21 2010-05-11 Procédé de préparation de l'ibodutant (men15596) et intermédiaires apparentés

Country Status (29)

Country Link
US (1) US8431684B2 (fr)
EP (1) EP2432778B1 (fr)
JP (1) JP5645926B2 (fr)
KR (1) KR101695346B1 (fr)
CN (1) CN102428081B (fr)
AR (1) AR076785A1 (fr)
AU (1) AU2010251514B2 (fr)
BR (1) BRPI1013073A2 (fr)
CA (1) CA2762625A1 (fr)
CY (1) CY1114079T1 (fr)
DK (1) DK2432778T3 (fr)
EA (1) EA019777B1 (fr)
EG (1) EG27000A (fr)
ES (1) ES2409705T3 (fr)
HK (1) HK1169828A1 (fr)
HR (1) HRP20130380T1 (fr)
IL (1) IL216400A (fr)
IT (1) IT1394304B1 (fr)
MA (1) MA33375B1 (fr)
MX (1) MX2011012317A (fr)
NZ (1) NZ596523A (fr)
PL (1) PL2432778T3 (fr)
PT (1) PT2432778E (fr)
SG (1) SG176171A1 (fr)
SI (1) SI2432778T1 (fr)
TW (1) TWI424996B (fr)
UA (1) UA105523C2 (fr)
WO (1) WO2010133306A1 (fr)
ZA (1) ZA201108483B (fr)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY130373A (en) * 2001-10-29 2007-06-29 Malesci Sas Linear basic compounds having nk-2 antagonist activity and formulations thereof
ITFI20040221A1 (it) * 2004-10-27 2005-01-27 Guidotti & C Spa Composizioni farmaceutiche a base di nk2 antagonisti per uso pediatrico
US8829209B2 (en) * 2006-01-11 2014-09-09 Seikagaku Corporation Cycloalkylcarbonylamino acid ester derivative and process for producing the same

Also Published As

Publication number Publication date
EP2432778B1 (fr) 2013-03-20
CN102428081A (zh) 2012-04-25
KR101695346B1 (ko) 2017-01-12
SG176171A1 (en) 2011-12-29
JP5645926B2 (ja) 2014-12-24
KR20120023675A (ko) 2012-03-13
NZ596523A (en) 2013-07-26
IT1394304B1 (it) 2012-06-06
CY1114079T1 (el) 2016-07-27
AU2010251514B2 (en) 2014-06-12
PL2432778T3 (pl) 2013-08-30
WO2010133306A8 (fr) 2011-02-03
DK2432778T3 (da) 2013-05-27
US20120065370A1 (en) 2012-03-15
PT2432778E (pt) 2013-06-03
EG27000A (en) 2015-03-23
CA2762625A1 (fr) 2010-11-25
EA201190267A1 (ru) 2012-05-30
EP2432778A1 (fr) 2012-03-28
BRPI1013073A2 (pt) 2016-04-05
SI2432778T1 (sl) 2013-05-31
MX2011012317A (es) 2012-03-07
AU2010251514A1 (en) 2011-12-08
UA105523C2 (uk) 2014-05-26
ZA201108483B (en) 2013-01-30
CN102428081B (zh) 2014-09-17
ES2409705T3 (es) 2013-06-27
ITMI20090897A1 (it) 2010-11-22
HRP20130380T1 (hr) 2013-05-31
WO2010133306A1 (fr) 2010-11-25
US8431684B2 (en) 2013-04-30
EA019777B1 (ru) 2014-06-30
HK1169828A1 (en) 2013-02-08
TW201100406A (en) 2011-01-01
IL216400A0 (en) 2012-01-31
JP2012527410A (ja) 2012-11-08
IL216400A (en) 2014-07-31
TWI424996B (zh) 2014-02-01
AR076785A1 (es) 2011-07-06

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