EA201190267A1 - Способ получения ибодутанта (men15596) и родственных промежуточных соединений - Google Patents

Способ получения ибодутанта (men15596) и родственных промежуточных соединений

Info

Publication number
EA201190267A1
EA201190267A1 EA201190267A EA201190267A EA201190267A1 EA 201190267 A1 EA201190267 A1 EA 201190267A1 EA 201190267 A EA201190267 A EA 201190267A EA 201190267 A EA201190267 A EA 201190267A EA 201190267 A1 EA201190267 A1 EA 201190267A1
Authority
EA
Eurasian Patent Office
Prior art keywords
ibodutant
men15596
obtaining
intermediate compounds
alpha
Prior art date
Application number
EA201190267A
Other languages
English (en)
Other versions
EA019777B1 (ru
Inventor
Фабрицио Бонаккорси
Валентина Феди
Данило Джаннотти
Original Assignee
Малеши Иституто Фармакобиолоджико С. П. А
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 Малеши Иституто Фармакобиолоджико С. П. А filed Critical Малеши Иституто Фармакобиолоджико С. П. А
Publication of EA201190267A1 publication Critical patent/EA201190267A1/ru
Publication of EA019777B1 publication Critical patent/EA019777B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4433—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
    • 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
    • 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

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)
  • Steroid Compounds (AREA)
  • Compounds Of Unknown Constitution (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Это изобретение относится к новому способу синтеза продукта ибодутанта, показанному на прилагаемой фигуре, состоящему из небольшого числа стадий с высоким выходом, включающему реагенты и растворители с низким воздействием на окружающую среду, характеризующемуся сочетанием двух составных частей, соединений (3) и (4), одно из которых, соединение (3), синтезируют путем сочетания 6-метил-2-бензо[b]тиофенкарбоновой кислоты (1) с 1-амино-альфа-альфа-циклопентанкарбоновой кислотой и последующей циклизации с оксазолоном, тогда как другое, соединение (4), получают из подходящего 4-аминометилпиперидина (2), функционализированного с высокой степенью селективности.
EA201190267A 2009-05-21 2010-05-11 Способ получения ибодутанта (men15596) и родственных промежуточных соединений EA019777B1 (ru)

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 (en) 2009-05-21 2010-05-11 Process for the preparation of ibodutant (men15596) and related intermediates

Publications (2)

Publication Number Publication Date
EA201190267A1 true EA201190267A1 (ru) 2012-05-30
EA019777B1 EA019777B1 (ru) 2014-06-30

Family

ID=41264221

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190267A EA019777B1 (ru) 2009-05-21 2010-05-11 Способ получения ибодутанта (men15596) и родственных промежуточных соединений

Country Status (29)

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

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
TW201100406A (en) 2011-01-01
WO2010133306A8 (en) 2011-02-03
NZ596523A (en) 2013-07-26
PT2432778E (pt) 2013-06-03
DK2432778T3 (da) 2013-05-27
EP2432778A1 (en) 2012-03-28
JP2012527410A (ja) 2012-11-08
EP2432778B1 (en) 2013-03-20
SI2432778T1 (sl) 2013-05-31
TWI424996B (zh) 2014-02-01
WO2010133306A1 (en) 2010-11-25
IL216400A (en) 2014-07-31
US20120065370A1 (en) 2012-03-15
MX2011012317A (es) 2012-03-07
CN102428081A (zh) 2012-04-25
EG27000A (en) 2015-03-23
UA105523C2 (ru) 2014-05-26
ZA201108483B (en) 2013-01-30
AU2010251514B2 (en) 2014-06-12
BRPI1013073A2 (pt) 2016-04-05
EA019777B1 (ru) 2014-06-30
CN102428081B (zh) 2014-09-17
ITMI20090897A1 (it) 2010-11-22
IT1394304B1 (it) 2012-06-06
HRP20130380T1 (hr) 2013-05-31
HK1169828A1 (en) 2013-02-08
SG176171A1 (en) 2011-12-29
MA33375B1 (fr) 2012-06-01
PL2432778T3 (pl) 2013-08-30
CA2762625A1 (en) 2010-11-25
KR20120023675A (ko) 2012-03-13
IL216400A0 (en) 2012-01-31
US8431684B2 (en) 2013-04-30
JP5645926B2 (ja) 2014-12-24
AR076785A1 (es) 2011-07-06
KR101695346B1 (ko) 2017-01-12
ES2409705T3 (es) 2013-06-27
CY1114079T1 (el) 2016-07-27
AU2010251514A1 (en) 2011-12-08

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Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU