KR101440982B1 - 라퀴니모드 나트륨의 결정 및 이의 제조방법 - Google Patents

라퀴니모드 나트륨의 결정 및 이의 제조방법 Download PDF

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Publication number
KR101440982B1
KR101440982B1 KR1020087011727A KR20087011727A KR101440982B1 KR 101440982 B1 KR101440982 B1 KR 101440982B1 KR 1020087011727 A KR1020087011727 A KR 1020087011727A KR 20087011727 A KR20087011727 A KR 20087011727A KR 101440982 B1 KR101440982 B1 KR 101440982B1
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sodium
mixture
solution
water
content
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Expired - Fee Related
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Korean (ko)
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KR20080064978A (ko
Inventor
안톤 프렌켈
에드워드 구레비흐
아비탈 랙서
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테바 파마슈티컬 인더스트리즈 리미티드
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4704—2-Quinolinones, e.g. carbostyril
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020087011727A 2005-10-19 2006-10-18 라퀴니모드 나트륨의 결정 및 이의 제조방법 Expired - Fee Related KR101440982B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US72865705P 2005-10-19 2005-10-19
US60/728,657 2005-10-19
PCT/US2006/040925 WO2007047863A2 (en) 2005-10-19 2006-10-18 Crystals of laquinimod sodium, and process for the manufacture thereof

Publications (2)

Publication Number Publication Date
KR20080064978A KR20080064978A (ko) 2008-07-10
KR101440982B1 true KR101440982B1 (ko) 2014-09-17

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US (4) US7884208B2 (OSRAM)
EP (2) EP2687512A1 (OSRAM)
JP (3) JP5832716B2 (OSRAM)
KR (1) KR101440982B1 (OSRAM)
CN (3) CN101291911B (OSRAM)
AR (1) AR056708A1 (OSRAM)
AU (1) AU2006304672B2 (OSRAM)
BR (1) BRPI0617477A2 (OSRAM)
CA (1) CA2625287C (OSRAM)
DK (1) DK1937642T3 (OSRAM)
ES (1) ES2523762T3 (OSRAM)
HR (1) HRP20141160T1 (OSRAM)
IL (1) IL190137A (OSRAM)
NZ (2) NZ567088A (OSRAM)
PL (1) PL1937642T3 (OSRAM)
PT (1) PT1937642E (OSRAM)
RS (1) RS53666B1 (OSRAM)
RU (1) RU2415841C2 (OSRAM)
SG (1) SG10201508623RA (OSRAM)
SI (1) SI1937642T1 (OSRAM)
UA (1) UA92761C2 (OSRAM)
WO (1) WO2007047863A2 (OSRAM)
ZA (1) ZA200803527B (OSRAM)

Families Citing this family (37)

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US8314124B2 (en) * 2004-02-06 2012-11-20 Active Biotech Ab Crystalline salts of quinoline compounds and methods for preparing them
SG10201508623RA (en) * 2005-10-19 2015-11-27 Teva Pharma Crystals of laquinimod sodium, and process for the manufacture thereof
KR20150065951A (ko) * 2006-06-12 2015-06-15 테바 파마슈티컬 인더스트리즈 리미티드 안정한 라퀴니모드 제제
WO2009082471A1 (en) * 2007-12-20 2009-07-02 Teva Pharmaceutical Industries, Ltd. Stable laquinimod preparations
EP2318371A2 (en) 2008-07-01 2011-05-11 Actavis Group PTC EHF Novel solid state forms of laquinimod and its sodium salt
MX2011002033A (es) * 2008-09-03 2011-05-02 Teva Pharma 2-oxo-1,2-dihidro-quinolinas moduladoras de la funcion inmune.
US20120009226A1 (en) 2008-12-17 2012-01-12 Actavis Group Ptc Ehf Highly pure laquinimod or a pharmaceutically acceptable salt thereof
DE102010048788A1 (de) 2009-02-13 2011-05-19 Amw Gmbh Transdermales System mit Immunmodulator
DE102009008851A1 (de) 2009-02-13 2010-08-19 Amw Gmbh Transdermales System mit Immunmodulator
EP2442651B1 (en) 2009-06-19 2015-07-29 Teva Pharmaceutical Industries Ltd. Treatment of multiple sclerosis with laquinimod
ES2564931T3 (es) * 2009-07-30 2016-03-30 Teva Pharmaceutical Industries Ltd. Tratamiento de enfermedad de Crohn con laquinimod
CA2771203C (en) 2009-08-10 2019-04-09 Teva Pharmaceutical Industries Ltd. Treatment of bdnf-related disorders using laquinimod
DE102010026879A1 (de) 2010-02-11 2011-08-11 AMW GmbH, 83627 Transdermales System mit Immunmodulator
US20110217295A1 (en) * 2010-03-03 2011-09-08 Asi Haviv Treatment of lupus arthritis using laquinimod
WO2011109526A1 (en) * 2010-03-03 2011-09-09 Teva Pharmaceutical Industries Ltd. Treatment of lupus nephritis using laquinimod
MX2012010066A (es) * 2010-03-03 2012-10-03 Teva Pharma Tratamiento de artritis reumatoide con una combinacion de laquinimod y metotrexato.
EA201390074A1 (ru) 2010-07-09 2013-06-28 Тева Фармасьютикал Индастриз Лтд. 5-хлор-4-гидрокси-1-метил-2-оксо-n-фенил-1,2-дигидрохинолин-3-карбоксамид, его соли и применения
CN104610144A (zh) * 2010-07-09 2015-05-13 泰华制药工业有限公司 氘化的n-乙基-n-苯基-1,2-二氢-4-羟基-5-氯-1-甲基-2-氧代喹啉-3-甲酰胺、其盐和用途
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EP2766020A4 (en) * 2011-10-12 2015-04-01 Teva Pharma TREATMENT OF MULTIPLE SCLEROSIS BY COMBINING LAQUINIMOD AND FINGOLIMOD
AR089862A1 (es) 2012-02-03 2014-09-24 Teva Pharma USO DE LAQUINIMOD PARA EL TRATAMIENTO DE PACIENTES CON ENFERMEDAD DE CROHN EN QUIENES FRACASO UNA TERAPIA ANTI-FACTOR DE NECROSIS TUMORAL a (ANTI-TNFa) DE PRIMERA LINEA
MX2014009889A (es) 2012-02-16 2014-11-13 Teva Pharma N-etil-n-fenil-1,2-dihidro-4,5-di-hidroxi-1-metil-2-oxo-3-quinoli ncarboxamida, preparacion y usos de los mismos.
US20130259856A1 (en) 2012-03-27 2013-10-03 Teva Pharmaceutical Industries, Ltd. Treatment of multiple sclerosis with combination of laquinimod and dimethyl fumarate
TW201350467A (zh) 2012-05-08 2013-12-16 Teva Pharma N-乙基-4-羥基-1-甲基-5-(甲基(2,3,4,5,6-五羥基己基)胺基)-2-側氧-n-苯基-1,2-二氫喹啉-3-甲醯胺
TW201400117A (zh) 2012-06-05 2014-01-01 Teva Pharma 使用拉喹莫德治療眼發炎疾病
AR091706A1 (es) * 2012-07-11 2015-02-25 Teva Pharma Formulaciones de laquinimod sin agentes alcalinizantes
TW201410244A (zh) 2012-08-13 2014-03-16 Teva Pharma 用於治療gaba媒介之疾病之拉喹莫德(laquinimod)
CN103626701A (zh) * 2012-08-28 2014-03-12 天津药物研究院 一种制备喹啉衍生物的方法
CN103626702A (zh) * 2012-08-30 2014-03-12 天津药物研究院 一种制备喹啉酮衍生物的方法
CN104584098B (zh) 2012-09-03 2017-09-15 丰田自动车株式会社 碰撞判定装置和碰撞判定方法
MX2015005632A (es) 2012-11-07 2016-02-05 Teva Pharma Sales de amina de laquinimod.
EP2970129A2 (en) * 2013-03-14 2016-01-20 Teva Pharmaceutical Industries Ltd. Crystals of laquinimod sodium and improved process for the manufacture thereof
MX2015010967A (es) 2013-03-14 2015-10-26 Teva Pharma Formulaciones transdermicas de laquinimod.
EP3578546A1 (en) 2013-11-15 2019-12-11 Akebia Therapeutics Inc. Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof
KR20170005434A (ko) 2014-04-29 2017-01-13 테바 파마슈티컬 인더스트리즈 리미티드 높은 장애 상태를 갖는 재발-완화형 다발성 경화증(rrms) 환자 치료용 라퀴니모드
JP7842983B2 (ja) * 2021-02-25 2026-04-09 学校法人神戸学院 腸管吸収用補助剤及びその利用方法
KR102876408B1 (ko) * 2022-01-24 2025-10-24 한국과학기술원 입도가 조절된 헥사나이트로스틸벤 타입 iv의 제조방법

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CA2771203C (en) 2009-08-10 2019-04-09 Teva Pharmaceutical Industries Ltd. Treatment of bdnf-related disorders using laquinimod
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ZA200803527B (en) 2009-09-30
US7884208B2 (en) 2011-02-08
PL1937642T3 (pl) 2015-02-27
UA92761C2 (ru) 2010-12-10
US8673322B2 (en) 2014-03-18
EP1937642B1 (en) 2014-09-10
CN101291911A (zh) 2008-10-22
DK1937642T3 (en) 2014-12-15
AR056708A1 (es) 2007-10-17
PT1937642E (pt) 2014-11-25
CN107176923A (zh) 2017-09-19
IL190137A (en) 2015-06-30
ES2523762T3 (es) 2014-12-01
HRP20141160T1 (hr) 2015-01-16
JP2013100299A (ja) 2013-05-23
SI1937642T1 (sl) 2015-01-30
WO2007047863A3 (en) 2007-06-28
RS53666B1 (sr) 2015-04-30
AU2006304672A1 (en) 2007-04-26
CA2625287C (en) 2016-07-26
HK1117160A1 (en) 2009-01-09
US8647646B2 (en) 2014-02-11
JP5832716B2 (ja) 2015-12-16
EP1937642A2 (en) 2008-07-02
US20140171647A1 (en) 2014-06-19
JP2016020353A (ja) 2016-02-04
WO2007047863A2 (en) 2007-04-26
CA2625287A1 (en) 2007-04-26
RU2415841C2 (ru) 2011-04-10
AU2006304672B2 (en) 2013-01-10
RU2008119456A (ru) 2009-11-27
US20110112141A1 (en) 2011-05-12
NZ592897A (en) 2012-12-21
JP2009512708A (ja) 2009-03-26
IL190137A0 (en) 2008-08-07
US20070088050A1 (en) 2007-04-19
SG10201508623RA (en) 2015-11-27
BRPI0617477A2 (pt) 2011-07-26
CN101291911B (zh) 2014-08-13
EP2687512A1 (en) 2014-01-22
KR20080064978A (ko) 2008-07-10
CN103333107A (zh) 2013-10-02
US20110118308A1 (en) 2011-05-19
NZ567088A (en) 2012-06-29
EP1937642A4 (en) 2009-03-18

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