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 PDFInfo
- 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
Links
Classifications
-
- 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
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)
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)
| 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)
| 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)
| 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 |
-
2013
- 2013-05-02 TW TW102115767A patent/TW201350467A/zh unknown
- 2013-05-07 CA CA2873258A patent/CA2873258A1/en not_active Abandoned
- 2013-05-07 WO PCT/US2013/039911 patent/WO2013169746A2/en not_active Ceased
- 2013-05-07 EA EA201492029A patent/EA201492029A1/ru unknown
- 2013-05-07 EP EP13750833.9A patent/EP2697201A4/en not_active Withdrawn
- 2013-05-07 AR ARP130101569A patent/AR090975A1/es unknown
- 2013-05-07 MX MX2014013664A patent/MX2014013664A/es unknown
- 2013-05-07 IN IN2485MUN2014 patent/IN2014MN02485A/en unknown
- 2013-05-07 BR BR112014028121A patent/BR112014028121A2/pt not_active IP Right Cessation
- 2013-05-07 CN CN201380029448.XA patent/CN104395291B/zh not_active Expired - Fee Related
- 2013-05-07 NZ NZ630549A patent/NZ630549A/en not_active IP Right Cessation
- 2013-05-07 SG SG11201407447XA patent/SG11201407447XA/en unknown
- 2013-05-07 AU AU2013259779A patent/AU2013259779B2/en not_active Expired - Fee Related
- 2013-05-07 KR KR20147034461A patent/KR20150022816A/ko not_active Withdrawn
- 2013-05-07 UY UY0001034791A patent/UY34791A/es not_active Application Discontinuation
- 2013-05-07 HK HK15107804.4A patent/HK1207080A1/xx unknown
- 2013-05-07 US US13/888,709 patent/US8809537B2/en not_active Expired - Fee Related
-
2014
- 2014-10-26 IL IL235338A patent/IL235338A0/en unknown
- 2014-12-02 ZA ZA2014/08825A patent/ZA201408825B/en unknown
Patent Citations (10)
| 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)
| 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 |
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