EA014641B1 - Сукцинатная и малонатная соли транс-4-((1r,3s )-6 хлор-3-фенилиндан -1-ил)-1,2,2-триметилпиперазина и их применение в качестве лекарственного средства - Google Patents

Сукцинатная и малонатная соли транс-4-((1r,3s )-6 хлор-3-фенилиндан -1-ил)-1,2,2-триметилпиперазина и их применение в качестве лекарственного средства Download PDF

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Publication number
EA014641B1
EA014641B1 EA200600441A EA200600441A EA014641B1 EA 014641 B1 EA014641 B1 EA 014641B1 EA 200600441 A EA200600441 A EA 200600441A EA 200600441 A EA200600441 A EA 200600441A EA 014641 B1 EA014641 B1 EA 014641B1
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EA
Eurasian Patent Office
Prior art keywords
compound
salt
formula
schizophrenia
disorder
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Application number
EA200600441A
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English (en)
Russian (ru)
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EA200600441A1 (ru
Inventor
Хейди Лопес Де Диего
Оле Нильсен
Лоне Мюнк Ринггар
Хенрик Сване
Аллан Карстен Даль
Марк Хауэллз
Бенни Бан-Андерсен
Ларс Оле Люнгсе
Original Assignee
Х. Лундбекк А/С
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Application filed by Х. Лундбекк А/С filed Critical Х. Лундбекк А/С
Priority claimed from PCT/DK2004/000545 external-priority patent/WO2005016900A1/en
Publication of EA200600441A1 publication Critical patent/EA200600441A1/ru
Publication of EA014641B1 publication Critical patent/EA014641B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/073Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C17/00Preparation of halogenated hydrocarbons
    • C07C17/093Preparation of halogenated hydrocarbons by replacement by halogens
    • C07C17/16Preparation of halogenated hydrocarbons by replacement by halogens of hydroxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C25/00Compounds containing at least one halogen atom bound to a six-membered aromatic ring
    • C07C25/18Polycyclic aromatic halogenated hydrocarbons
    • C07C25/22Polycyclic aromatic halogenated hydrocarbons with condensed rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C29/00Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
    • C07C29/132Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group
    • C07C29/136Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH
    • C07C29/143Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by reduction of an oxygen containing functional group of >C=O containing groups, e.g. —COOH of ketones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/22Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system
    • C07C35/23Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with hydroxy on a condensed ring system having two rings
    • C07C35/32Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with hydroxy on a condensed ring system having two rings the condensed ring system being a (4.3.0) system, e.g. indenols
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P41/00Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
    • C12P41/003Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions
    • C12P41/004Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions by esterification of alcohol- or thiol groups in the enantiomers or the inverse reaction
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12PFERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P7/00Preparation of oxygen-containing organic compounds
    • C12P7/02Preparation of oxygen-containing organic compounds containing a hydroxy group
    • C12P7/22Preparation of oxygen-containing organic compounds containing a hydroxy group aromatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biotechnology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Medicinal Chemistry (AREA)
  • Analytical Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
EA200600441A 2003-08-18 2004-08-18 Сукцинатная и малонатная соли транс-4-((1r,3s )-6 хлор-3-фенилиндан -1-ил)-1,2,2-триметилпиперазина и их применение в качестве лекарственного средства EA014641B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA200301180 2003-08-18
DKPA200301305 2003-09-11
PCT/DK2004/000545 WO2005016900A1 (en) 2003-08-18 2004-08-18 Succinate and malonate salt of trans-4-(ir,3s)-6-chloro-3-phenylindan-1-yl)-1,2,2-trimethylpiperazine and the use as a medicament

Publications (2)

Publication Number Publication Date
EA200600441A1 EA200600441A1 (ru) 2006-08-25
EA014641B1 true EA014641B1 (ru) 2010-12-30

Family

ID=58707237

Family Applications (2)

Application Number Title Priority Date Filing Date
EA200600441A EA014641B1 (ru) 2003-08-18 2004-08-18 Сукцинатная и малонатная соли транс-4-((1r,3s )-6 хлор-3-фенилиндан -1-ил)-1,2,2-триметилпиперазина и их применение в качестве лекарственного средства
EA200600443A EA200600443A1 (ru) 2003-08-18 2004-08-18 Транс-1-(6-хлор-3-фенилиндан-1-ил)-3,3-диметилпиперазин

Family Applications After (1)

Application Number Title Priority Date Filing Date
EA200600443A EA200600443A1 (ru) 2003-08-18 2004-08-18 Транс-1-(6-хлор-3-фенилиндан-1-ил)-3,3-диметилпиперазин

Country Status (16)

Country Link
KR (2) KR101227789B1 (es)
CN (1) CN101935305B (es)
AR (2) AR045278A1 (es)
AT (1) ATE552247T1 (es)
DK (1) DK1658277T3 (es)
EA (2) EA014641B1 (es)
ES (1) ES2383369T3 (es)
HK (2) HK1096089A1 (es)
IS (1) IS8264A (es)
ME (1) MEP2408A (es)
MY (2) MY154535A (es)
PT (1) PT1658277E (es)
RS (3) RS20060121A (es)
SG (2) SG145723A1 (es)
SI (1) SI1658277T1 (es)
TW (2) TWI403505B (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI453198B (zh) * 2005-02-16 2014-09-21 Lundbeck & Co As H 製造反式-1-((1r,3s)-6-氯基-3-苯基茚滿-1-基) -3 , 3 -二甲基六氫吡與其鹽類之方法及製造4-((1r , 3s)-6 -氯基-3-苯基茚滿-1-基 )-1,2,2-三甲基六氫吡與其鹽類之方法
JP5668177B2 (ja) 2011-06-20 2015-02-12 ハー・ルンドベック・アクチエゼルスカベット 統合失調症の治療のための重水素化1−ピペラジノ−3−フェニルインダン

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0638073B1 (en) * 1992-04-28 2000-06-21 H. Lundbeck A/S 1-piperazino-1,2-dihydroindene derivatives

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE50867B1 (en) * 1980-02-29 1986-08-06 Kefalas As Indane derivatives

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0638073B1 (en) * 1992-04-28 2000-06-21 H. Lundbeck A/S 1-piperazino-1,2-dihydroindene derivatives

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KLAUS P. BOGOSO ET AL.: "Enhanced D1 Affinity in a Series of Piperazine Ring Substituted 1-Piperazi- no-3-Arylindanes with Potential Atypical Antipsychotic Activity", JOURNAL OF MEDICINAL CHEMISTRY., vol. 38, no. 22, 1995, pages 4380-4392, XP008037648 *
USAMERICAN CHEMICAL SOCIETY. WASHINGTON, cited in the application, page 4383, scheme 1; page 4383, compound (-)-38; page 4386, table 5, compound (-)-38, page 4387, table 6, compound (-)-38 *

Also Published As

Publication number Publication date
RS20060121A (en) 2008-09-29
TW201111351A (en) 2011-04-01
MY149089A (en) 2013-07-15
RS53369B (en) 2014-10-31
SI1658277T1 (sl) 2012-10-30
EA200600443A1 (ru) 2006-08-25
HK1096089A1 (en) 2007-05-25
EA200600441A1 (ru) 2006-08-25
KR20060066104A (ko) 2006-06-15
CN101935305B (zh) 2013-04-10
SG148183A1 (en) 2008-12-31
CN101935305A (zh) 2011-01-05
TW200519098A (en) 2005-06-16
DK1658277T3 (da) 2012-06-18
RS20060083A (en) 2008-08-07
ES2383369T3 (es) 2012-06-20
KR101227789B1 (ko) 2013-01-30
ATE552247T1 (de) 2012-04-15
MEP2408A (xx) 2010-02-10
TWI388550B (zh) 2013-03-11
TWI403505B (zh) 2013-08-01
IS8264A (is) 2006-01-26
AR045279A1 (es) 2005-10-19
HK1152699A1 (en) 2012-03-09
MY154535A (en) 2015-06-30
KR20060066094A (ko) 2006-06-15
AR045278A1 (es) 2005-10-19
SG145723A1 (en) 2008-09-29
PT1658277E (pt) 2012-05-25

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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 KZ KG MD TJ TM

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): BY RU