CN104395291B - N‑乙基‑4‑羟基‑1‑甲基‑5‑(甲基(2,3,4,5,6‑五羟基己基)氨基)‑2‑氧代‑n‑苯基‑1,2‑二氢喹啉‑3‑甲酰胺 - Google Patents

N‑乙基‑4‑羟基‑1‑甲基‑5‑(甲基(2,3,4,5,6‑五羟基己基)氨基)‑2‑氧代‑n‑苯基‑1,2‑二氢喹啉‑3‑甲酰胺 Download PDF

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Publication number
CN104395291B
CN104395291B CN201380029448.XA CN201380029448A CN104395291B CN 104395291 B CN104395291 B CN 104395291B CN 201380029448 A CN201380029448 A CN 201380029448A CN 104395291 B CN104395291 B CN 104395291B
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CN
China
Prior art keywords
methyl
laquinimod
pharmaceutical composition
phenyl
ethyl
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Expired - Fee Related
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CN201380029448.XA
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English (en)
Chinese (zh)
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CN104395291A (zh
Inventor
阿维塔尔·拉克泽尔
康斯坦丁·尤兰思克
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Teva Pharmaceutical Industries Ltd
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Teva Pharmaceutical Industries Ltd
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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
    • C07D215/48—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201380029448.XA 2012-05-08 2013-05-07 N‑乙基‑4‑羟基‑1‑甲基‑5‑(甲基(2,3,4,5,6‑五羟基己基)氨基)‑2‑氧代‑n‑苯基‑1,2‑二氢喹啉‑3‑甲酰胺 Expired - Fee Related CN104395291B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261644054P 2012-05-08 2012-05-08
US61/644,054 2012-05-08
PCT/US2013/039911 WO2013169746A2 (en) 2012-05-08 2013-05-07 N-ethyl-4-hydroxyl-1-methyl-5-(methyl(2,3,4,5,6-pentahydroxyhexyl) amino)-2-oxo-n-phenyl-1,2-dihydroquinoline-3-carboxamide

Publications (2)

Publication Number Publication Date
CN104395291A CN104395291A (zh) 2015-03-04
CN104395291B true CN104395291B (zh) 2017-07-28

Family

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Family Applications (1)

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CN201380029448.XA Expired - Fee Related CN104395291B (zh) 2012-05-08 2013-05-07 N‑乙基‑4‑羟基‑1‑甲基‑5‑(甲基(2,3,4,5,6‑五羟基己基)氨基)‑2‑氧代‑n‑苯基‑1,2‑二氢喹啉‑3‑甲酰胺

Country Status (19)

Country Link
US (1) US8809537B2 (https=)
EP (1) EP2697201A4 (https=)
KR (1) KR20150022816A (https=)
CN (1) CN104395291B (https=)
AR (1) AR090975A1 (https=)
AU (1) AU2013259779B2 (https=)
BR (1) BR112014028121A2 (https=)
CA (1) CA2873258A1 (https=)
EA (1) EA201492029A1 (https=)
HK (1) HK1207080A1 (https=)
IL (1) IL235338A0 (https=)
IN (1) IN2014MN02485A (https=)
MX (1) MX2014013664A (https=)
NZ (1) NZ630549A (https=)
SG (1) SG11201407447XA (https=)
TW (1) TW201350467A (https=)
UY (1) UY34791A (https=)
WO (1) WO2013169746A2 (https=)
ZA (1) ZA201408825B (https=)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104093310A (zh) 2012-02-03 2014-10-08 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
JP6215238B2 (ja) 2012-02-16 2017-10-18 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 Ｎ−エチル−ｎ−フェニル−１，２−ジヒドロ−４，５−ジ−ヒドロキシ−１−メチル−２−オキソ−３−キノリンカルボキサミド、その製剤、および使用
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）
EP2916915A4 (en) 2012-11-07 2016-06-22 Teva Pharma LAQUINIMOD AMINE SALTS
US20160046582A1 (en) 2013-03-14 2016-02-18 Teva Pharmaceutical Industries Ltd. Crystals of laquinimod sodium and improved process for the manufacture thereof
WO2015168103A1 (en) 2014-04-29 2015-11-05 Teva Pharmaceutical Industries Ltd. Laquinimod for the treatment of relapsing-remitting multiple sclerosis (rrms) patients with a high disability status

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2159804A (en) * 1937-11-23 1939-05-23 Du Pont N-nitroaryl polyhydroxy alkyl amino compounds and process of preparing the same
US4547511A (en) * 1981-03-03 1985-10-15 Aktiebolaget Leo Heterocyclic carboxamides, compositions containing such compounds, processes for their preparation and methods of treatment therewith
US6043006A (en) * 1997-09-04 2000-03-28 Fuji Photo Film Co., Ltd. 4-(N,N-dialkylamino)aniline compound, photographic processing composition containing the same and color image-forming method
US6875869B2 (en) * 2002-06-12 2005-04-05 Active Biotech Ab Process for the manufacture of quinoline derivatives
US20050192315A1 (en) * 2004-02-06 2005-09-01 Active Biotech Ab New compositions containing quinoline compounds
CN101466379A (zh) * 2006-06-12 2009-06-24 泰华制药工业有限公司 稳定的拉喹莫德的制剂
US20090162432A1 (en) * 2007-12-20 2009-06-25 Muhammad Safadi Stable laquinimod preparations
US20120009226A1 (en) * 2008-12-17 2012-01-12 Actavis Group Ptc Ehf Highly pure laquinimod or a pharmaceutically acceptable salt thereof
CN102348689A (zh) * 2009-03-13 2012-02-08 奥米罗有限公司 含有羟基和/或羧基的胺与作为dhodh抑制剂的胺基烟碱酸衍生物的加成盐

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4782155A (en) 1986-03-19 1988-11-01 Banyu Pharmaceutical Co., Ltd. Cephalosporin derivatives, processes for their preparation and antibacterial agents
SE8902076D0 (sv) 1989-06-09 1989-06-09 Pharmacia Ab Derivatives of quinoline-3-carboxanilide
US5139878A (en) 1991-08-12 1992-08-18 Allied-Signal Inc. Multilayer film constructions
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
US6121287A (en) 1998-07-15 2000-09-19 Active Biotech Ab Quinoline derivatives
US6133285A (en) 1998-07-15 2000-10-17 Active Biotech Ab Quinoline derivatives
SE9802550D0 (sv) 1998-07-15 1998-07-15 Active Biotech Ab Quinoline derivatives
SE9802549D0 (sv) 1998-07-15 1998-07-15 Active Biotech Ab Quinoline derivatives
ES2246238T3 (es) 1999-06-07 2006-02-16 Altana Pharma Ag Nueva preparacion y forma de administracion que comprende un inhibidor de las bombas de protones labil en medio acido.
US7560557B2 (en) 2002-06-12 2009-07-14 Active Biotech Ag 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
US8314124B2 (en) 2004-02-06 2012-11-20 Active Biotech Ab Crystalline salts of quinoline compounds and methods for preparing them
US7514068B2 (en) 2005-09-14 2009-04-07 Concert Pharmaceuticals Inc. Biphenyl-pyrazolecarboxamide compounds
NZ567088A (en) 2005-10-19 2012-06-29 Teva Pharma Crystals of laquinimod sodium, and process for the manufacture thereof
AU2008242703B2 (en) 2007-04-19 2011-08-18 Concert Pharmaceuticals Inc. Deuterated morpholinyl compounds
KR20110048571A (ko) 2008-09-03 2011-05-11 테바 파마슈티컬 인더스트리즈 리미티드 면역 기능을 지닌 ２―옥소―１,２―다이하이드로―퀴놀린 조절제
UY32427A (es) 2009-02-13 2010-09-30 Boheringer Ingelheim Internat Gmbh Composicion farmaceutica, forma farmaceutica, procedimiento para su preparacion, metodos de tratamiento y usos de la misma
JP2012530701A (ja) 2009-06-19 2012-12-06 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 多発性硬化症のラキニモドでの治療
PL2458992T3 (pl) 2009-07-30 2016-07-29 Teva Pharma Leczenie choroby Leśniowskiego-Crohna z użyciem lakwinimodu
WO2011019375A1 (en) 2009-08-10 2011-02-17 Teva Pharmaceutical Industries Ltd. Treatment of bdnf-related disorders using laquinimod
CA2791711A1 (en) 2010-03-03 2011-09-09 Teva Pharmaceutical Industries Ltd. Treatment of lupus arthritis using laquinimod
DK2542079T3 (da) 2010-03-03 2014-08-25 Teva Pharma Behandling af reumatoid artritis med en kombination af laquinimod og methotrexat
SG183512A1 (en) 2010-03-03 2012-09-27 Teva Pharma Treatment of lupus nephritis using laquinimod
EP2590653A4 (en) 2010-07-09 2014-01-01 Teva Pharma 5-CHLORO-4-HYDROXY-1-METHYL-2-OXO-N-PHENYL-1,2-DIHYDROCHINOLINE-3-CARBOXAMIDE, SALT THEREOF AND APPLICATIONS THEREOF
WO2012006538A1 (en) 2010-07-09 2012-01-12 Teva Pharmaceutical Industries Ltd. Deuterated n-ethyl-n-phenyl-1,2-dihydro-4-hydroxy-5-chloro-1-methyl-2-oxoquinoline-3-carboxamide, salts and uses thereof
JP2012047974A (ja) * 2010-08-26 2012-03-08 Toshiba Corp 映像表示装置及び映像表示方法
WO2012050500A1 (en) * 2010-10-14 2012-04-19 Lars Pettersson 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides as ahr activators.
AU2011338647A1 (en) 2010-12-07 2013-07-04 Teva Pharmaceutical Industries Ltd. Use of laquinimod for reducing fatigue, improving functional status, and improving quality of life in multiple sclerosis patients
IN2014MN00333A (https=) 2011-07-28 2015-09-25 Teva Pharma
AU2012286701A1 (en) 2011-07-28 2014-03-06 Teva Pharmaceutical Industries Ltd. Treatment of multiple sclerosis with combination of laquinimod and interferon-beta
CA2851525A1 (en) 2011-10-12 2013-04-18 Teva Pharmaceutical Industries Ltd. Treatment of multiple sclerosis with combination of laquinimod and fingolimod

Patent Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2159804A (en) * 1937-11-23 1939-05-23 Du Pont N-nitroaryl polyhydroxy alkyl amino compounds and process of preparing the same
US4547511A (en) * 1981-03-03 1985-10-15 Aktiebolaget Leo Heterocyclic carboxamides, compositions containing such compounds, processes for their preparation and methods of treatment therewith
US6043006A (en) * 1997-09-04 2000-03-28 Fuji Photo Film Co., Ltd. 4-(N,N-dialkylamino)aniline compound, photographic processing composition containing the same and color image-forming method
US6875869B2 (en) * 2002-06-12 2005-04-05 Active Biotech Ab Process for the manufacture of quinoline derivatives
US20050192315A1 (en) * 2004-02-06 2005-09-01 Active Biotech Ab New compositions containing quinoline compounds
CN1980669A (zh) * 2004-02-06 2007-06-13 活跃生物技术有限公司 含喹啉化合物的新组合物
CN101466379A (zh) * 2006-06-12 2009-06-24 泰华制药工业有限公司 稳定的拉喹莫德的制剂
US20090162432A1 (en) * 2007-12-20 2009-06-25 Muhammad Safadi Stable laquinimod preparations
US20120009226A1 (en) * 2008-12-17 2012-01-12 Actavis Group Ptc Ehf Highly pure laquinimod or a pharmaceutically acceptable salt thereof
CN102348689A (zh) * 2009-03-13 2012-02-08 奥米罗有限公司 含有羟基和/或羧基的胺与作为dhodh抑制剂的胺基烟碱酸衍生物的加成盐

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Copper-catalyzed aryl amination in aqueous media with 2-dimethylaminoethanol ligand;Zhikuan Lu，等;《Tetrahedron Letters》;20050425;第46卷(第17期);第3000页表4 *
Design, Synthesis and In Vitro Evaluation of Potent, Novel, Small Molecule Inhibitors of Plasminogen Activator Inhibitor-1;Adrian Folkes，等;《Bioorganic & Medicinal Chemistry Letters》;20021231;第12卷;第1063-1066页 *

Also Published As

Publication number Publication date
SG11201407447XA (en) 2015-02-27
AU2013259779B2 (en) 2017-06-08
WO2013169746A2 (en) 2013-11-14
EP2697201A4 (en) 2014-11-26
TW201350467A (zh) 2013-12-16
BR112014028121A2 (pt) 2017-06-27
UY34791A (es) 2013-11-29
CN104395291A (zh) 2015-03-04
US8809537B2 (en) 2014-08-19
AR090975A1 (es) 2014-12-17
ZA201408825B (en) 2016-07-27
NZ630549A (en) 2016-01-29
EA201492029A1 (ru) 2015-06-30
CA2873258A1 (en) 2013-11-14
HK1207080A1 (en) 2016-01-22
IL235338A0 (en) 2014-12-31
WO2013169746A3 (en) 2013-12-05
EP2697201A2 (en) 2014-02-19
US20130345256A1 (en) 2013-12-26
IN2014MN02485A (https=) 2015-07-17
KR20150022816A (ko) 2015-03-04
MX2014013664A (es) 2015-04-17
AU2013259779A1 (en) 2014-12-18

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