CN102985090B - 5-氯-4-羟基-1-甲基-2-氧代-n-苯基-1,2-二氢喹啉-3-甲酰胺、其盐和用途 - Google Patents

5-氯-4-羟基-1-甲基-2-氧代-n-苯基-1,2-二氢喹啉-3-甲酰胺、其盐和用途 Download PDF

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Publication number
CN102985090B
CN102985090B CN201180034077.5A CN201180034077A CN102985090B CN 102985090 B CN102985090 B CN 102985090B CN 201180034077 A CN201180034077 A CN 201180034077A CN 102985090 B CN102985090 B CN 102985090B
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CN
China
Prior art keywords
laquinimod
methyl
pharmaceutically acceptable
batch
chloro
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Expired - Fee Related
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CN201180034077.5A
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English (en)
Chinese (zh)
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CN102985090A (zh
Inventor
U·T·福瑞斯泰迪特
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Teva Pharmaceutical Industries Ltd
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Teva Pharmaceutical Industries Ltd
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Publication of CN102985090A publication Critical patent/CN102985090A/zh
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    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • 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]
    • 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
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Quinoline Compounds (AREA)
CN201180034077.5A 2010-07-09 2011-07-08 5-氯-4-羟基-1-甲基-2-氧代-n-苯基-1,2-二氢喹啉-3-甲酰胺、其盐和用途 Expired - Fee Related CN102985090B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US39926410P 2010-07-09 2010-07-09
US61/399,264 2010-07-09
PCT/US2011/043391 WO2012006544A1 (en) 2010-07-09 2011-07-08 5-chloro-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide, salts and uses thereof

Publications (2)

Publication Number Publication Date
CN102985090A CN102985090A (zh) 2013-03-20
CN102985090B true CN102985090B (zh) 2014-11-26

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180034077.5A Expired - Fee Related CN102985090B (zh) 2010-07-09 2011-07-08 5-氯-4-羟基-1-甲基-2-氧代-n-苯基-1,2-二氢喹啉-3-甲酰胺、其盐和用途

Country Status (14)

Country Link
US (3) US20120010239A1 (https=)
EP (2) EP3056205A1 (https=)
JP (2) JP5934202B2 (https=)
KR (1) KR20130041193A (https=)
CN (1) CN102985090B (https=)
AU (2) AU2011274502A1 (https=)
BR (1) BR112013000607A2 (https=)
CA (1) CA2804989A1 (https=)
EA (1) EA201390074A1 (https=)
HK (1) HK1225308A1 (https=)
MX (1) MX2013000332A (https=)
NZ (1) NZ606589A (https=)
WO (1) WO2012006544A1 (https=)
ZA (1) ZA201300957B (https=)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7884208B2 (en) * 2005-10-19 2011-02-08 Teva Pharmaceutical Industries, Ltd. Crystals of laquinimod sodium, and process for the manufacture thereof
RS52169B (sr) 2006-06-12 2012-08-31 Teva Pharmaceutical Industries Limited Stabilni preparati lakvinimoda
ES2445451T3 (es) 2007-12-20 2014-03-03 Teva Pharmaceutical Industries, Ltd. Preparaciones estables de laquinimod
RS54328B1 (sr) * 2009-06-19 2016-02-29 Teva Pharmaceutical Industries Ltd. Tretman multiple skleroze lakvinimodom
ME02414B (me) * 2009-07-30 2016-09-20 Teva Pharma Tretman kronove bolesti lakvinimodom
PT2467372T (pt) 2009-08-10 2016-08-23 Teva Pharma Tratamento de distúrbios relacionados com bdnf usando laquinimod
CN102791130B (zh) 2010-03-03 2015-02-25 泰华制药工业有限公司 使用拉喹莫德治疗狼疮肾炎
JP5819328B2 (ja) * 2010-03-03 2015-11-24 テバ ファーマシューティカル インダストリーズ リミティド ラキニモドとメトトレキセートとの組合せによる関節リウマチの治療
SG10201505236YA (en) 2010-07-09 2015-08-28 Teva Pharma Deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, salts and uses thereof
CN106344576A (zh) 2011-10-12 2017-01-25 泰华制药工业有限公司 以拉喹莫德和芬戈莫德的组合治疗多发性硬化症
CN106063787A (zh) 2012-02-03 2016-11-02 泰华制药工业有限公司 拉喹莫德用于治疗一线抗TNFα疗法失败的克罗恩氏病患者的用途
HK1198296A1 (en) 2012-02-16 2015-03-27 Teva Pharmaceutical Industries Ltd. N-ethyl-n-phenyl-1,2-dihydro-4,5-di-hydroxy-1-methyl-2-oxo-3-quinoline carboxamide, preparation and uses thereof
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
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
JP2015535287A (ja) 2012-11-07 2015-12-10 テバ ファーマシューティカル インダストリーズ リミティド ラキニモドのアミン塩
HK1220125A1 (zh) 2013-03-14 2017-04-28 Teva Pharmaceutical Industries Ltd. 拉喹莫德的透皮配方
NZ630427A (en) 2013-03-14 2017-06-30 Teva Pharma Crystals of laquinimod sodium and improved process for the manufacture thereof
EA201692180A1 (ru) 2014-04-29 2017-08-31 Тева Фармасьютикал Индастриз Лтд. Лахинимод для лечения пациентов с рецидивирующе-ремиттирующим рассеянным склерозом (рррс) с высоким статусом инвалидизации
US20190090046A1 (en) * 2017-09-21 2019-03-21 Bragi GmbH Tactile Feedback for Audio Defined Menu System and Method
GB202006390D0 (en) * 2020-04-30 2020-06-17 Aqilion Ab Novel treatments

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US2380420A (en) * 1940-12-16 1945-07-31 William S Emerson Production of secondary and tertiary amines from nitrogen compounds
IE52670B1 (en) * 1981-03-03 1988-01-20 Leo Ab Heterocyclic carboxamides,compositions containing such compounds,and processes for their preparation
DE3724018A1 (de) * 1987-07-21 1989-02-02 Bayer Ag Verfahren zur trennung von anilin-derivaten
SE9801474D0 (sv) * 1998-04-27 1998-04-27 Active Biotech Ab Quinoline Derivatives
US6077851A (en) * 1998-04-27 2000-06-20 Active Biotech Ab Quinoline derivatives
US7560557B2 (en) * 2002-06-12 2009-07-14 Active Biotech Ag Process for the manufacture of quinoline derivatives
US6875869B2 (en) 2002-06-12 2005-04-05 Active Biotech Ab Process for the manufacture of quinoline derivatives
SE0201778D0 (sv) * 2002-06-12 2002-06-12 Active Biotech Ab Process for the manufacture of quinoline derivatives
SE0400235D0 (sv) 2004-02-06 2004-02-06 Active Biotech Ab New composition containing quinoline compounds
US7884208B2 (en) 2005-10-19 2011-02-08 Teva Pharmaceutical Industries, Ltd. Crystals of laquinimod sodium, and process for the manufacture thereof
RS52169B (sr) 2006-06-12 2012-08-31 Teva Pharmaceutical Industries Limited Stabilni preparati lakvinimoda
ES2445451T3 (es) * 2007-12-20 2014-03-03 Teva Pharmaceutical Industries, Ltd. Preparaciones estables de laquinimod
US8354428B2 (en) * 2008-07-01 2013-01-15 Actavis Group Ptc Ehf Solid state forms of laquinimod and its sodium salt
WO2010070449A2 (en) * 2008-12-17 2010-06-24 Actavis Group Ptc Ehf Highly pure laquinimod or a pharmaceutically acceptable salt thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Synthesis and Reactivity of Laquinimod, a Quinoline-3-carboxamide: Intramolecular Transfer of the Enol Proton to a Nitrogen Atom as a Plausible Mechanism for Ketene Formation;Karl Janssony等;《J. Org. Chem.》;20061231;第71卷(第4期);1658-1667 *

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Publication number Publication date
JP2013534536A (ja) 2013-09-05
KR20130041193A (ko) 2013-04-24
AU2017261621A1 (en) 2017-12-07
AU2011274502A1 (en) 2013-02-28
US20160279121A1 (en) 2016-09-29
EP3056205A1 (en) 2016-08-17
JP2016053049A (ja) 2016-04-14
BR112013000607A2 (pt) 2016-06-28
EA201390074A1 (ru) 2013-06-28
CA2804989A1 (en) 2012-01-12
WO2012006544A1 (en) 2012-01-12
JP5934202B2 (ja) 2016-06-15
MX2013000332A (es) 2013-02-26
EP2590653A1 (en) 2013-05-15
US20180140592A1 (en) 2018-05-24
NZ606589A (en) 2015-03-27
CN102985090A (zh) 2013-03-20
EP2590653A4 (en) 2014-01-01
US20120010239A1 (en) 2012-01-12
ZA201300957B (en) 2014-04-30
HK1225308A1 (en) 2017-09-08

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Granted publication date: 20141126

Termination date: 20180708