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

Info

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
Authority
CN
China
Prior art keywords
methyl
laquinimod
pharmaceutical composition
phenyl
ethyl
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN201380029448.XA
Other languages
English (en)
Chinese (zh)
Other versions
CN104395291A (zh
Inventor
阿维塔尔·拉克泽尔
康斯坦丁·尤兰思克
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Teva Pharmaceutical Industries Ltd
Original Assignee
Teva Pharmaceutical Industries Ltd
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 Teva Pharmaceutical Industries Ltd filed Critical Teva Pharmaceutical Industries Ltd
Publication of CN104395291A publication Critical patent/CN104395291A/zh
Application granted granted Critical
Publication of CN104395291B publication Critical patent/CN104395291B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/48Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56Carbon 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
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/47042-Quinolinones, e.g. carbostyril
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators

Landscapes

  • 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

ID=49551433

Family Applications (1)

Application Number Title Priority Date Filing Date
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
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
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)
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
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

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
SE9802549D0 (sv) 1998-07-15 1998-07-15 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
CA2376202C (en) 1999-06-07 2008-11-18 Byk Gulden Lomberg Chemische Fabrik Gmbh Novel preparation and administration form comprising an acid-labile active compound
SE0201778D0 (sv) 2002-06-12 2002-06-12 Active Biotech Ab Process for the manufacture of quinoline derivatives
US7560557B2 (en) 2002-06-12 2009-07-14 Active Biotech Ag 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
US7884208B2 (en) 2005-10-19 2011-02-08 Teva Pharmaceutical Industries, Ltd. Crystals of laquinimod sodium, and process for the manufacture thereof
JP2010524972A (ja) 2007-04-19 2010-07-22 コンサート ファーマシューティカルズ インコーポレイテッド 重水素化したモルホリニル化合物
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
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
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
NZ602512A (en) 2010-03-03 2014-07-25 Teva Pharma Treatment of lupus arthritis using 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
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
EP3056205A1 (en) 2010-07-09 2016-08-17 Teva Pharmaceutical Industries, Ltd. 5-chloro-4-hydroxy-1-methyl-2-oxo-n-phenyl-1,2-dihydroquinoline-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
CA2813711A1 (en) * 2010-10-14 2012-04-19 Immunahr Ab 1,2-dihydro-4-hydroxy-2-oxo-quinoline-3-carboxanilides as ahr activators.
WO2012078591A1 (en) 2010-12-07 2012-06-14 Teva Pharmaceutical Industries Ltd. Use of laquinimod for reducing fatigue, improving functional status, and improving quality of life in multiple sclerosis patients
EA201490377A1 (ru) 2011-07-28 2014-11-28 Тева Фармасьютикал Индастриз Лтд. Лечение рассеянного склероза комбинацией лаквинимода и глатирамера ацетата
WO2013016686A1 (en) 2011-07-28 2013-01-31 Teva Pharmaceutical Industries Ltd. Treatment of multiple sclerosis with combination of laquinimod and interferon-beta
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

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

Similar Documents

Publication Publication Date Title
CN104395291B (zh) 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
CN102985090B (zh) 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
JP7035108B2 (ja) プリドピジンの類似体、それらの製造および使用
JP2014534197A (ja) R(+)−n−メチル−プロパルギルアミノインダン
US9346746B2 (en) R(+)-N-formyl-propargyl-aminoindan
JP2014534195A (ja) ラサギリンシトルアミド
WO2023143455A1 (zh) 3-[(苯并[d][1,3]二氧戊环-4-基)氧基]丙胺盐酸盐及其光学异构体、晶体及制备方法
EP3137453B1 (en) Polymorphic form of [5-fluoro-3-({2-[(4-fluorobenzene) sulfonyl]pyridin-3-yl}methyl)-2-methylindol-1-yl]-acetic acid
DK2220027T3 (en) Polymorphic form of N- [4- (trifluoromethyl) benzyl) -4-METHOXYBUTYRAMID
CN118647618A (zh) Rabeximod化合物
EP3074379B1 (en) Opioid agonists and uses thereof
EP3184516A1 (en) Crystalline inclusion complexes of mirabegron with beta-cyclodextrin
HK40078313A (en) Analogs of pridopidine, their preparation and use
NZ624206B2 (en) R(+)-n-formyl-propargyl-aminoindan
HK1233503A1 (en) Analogs of pridopidine, their preparation and use

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1207080

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20170728

Termination date: 20180507

CF01 Termination of patent right due to non-payment of annual fee
REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1207080

Country of ref document: HK