JP5934202B2 - 5−クロロ−4−ヒドロキシ−1−メチル−2−オキソ−n−フェニル−1,2−ジヒドロキノリン−3−カルボキサミドと、その塩及びその使用 - Google Patents
5−クロロ−4−ヒドロキシ−1−メチル−2−オキソ−n−フェニル−1,2−ジヒドロキノリン−3−カルボキサミドと、その塩及びその使用 Download PDFInfo
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- JP5934202B2 JP5934202B2 JP2013519726A JP2013519726A JP5934202B2 JP 5934202 B2 JP5934202 B2 JP 5934202B2 JP 2013519726 A JP2013519726 A JP 2013519726A JP 2013519726 A JP2013519726 A JP 2013519726A JP 5934202 B2 JP5934202 B2 JP 5934202B2
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- Prior art keywords
- laquinimod
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- pharmaceutically acceptable
- methyl
- ethylaniline
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- 235000010487 tragacanth Nutrition 0.000 description 1
- 239000000196 tragacanth Substances 0.000 description 1
- 229940116362 tragacanth Drugs 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
- 238000000825 ultraviolet detection Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
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Images
Classifications
-
- 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
- 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
- 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
Landscapes
- 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)
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| Application Number | Priority Date | Filing Date | Title |
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| 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 |
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| JP2015204932A Pending JP2016053049A (ja) | 2010-07-09 | 2015-10-16 | 5−クロロ−4−ヒドロキシ−1−メチル−2−オキソ−n−フェニル−1,2−ジヒドロキノリン−3−カルボキサミドと、その塩及びその使用 |
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| EP (2) | EP3056205A1 (enExample) |
| JP (2) | JP5934202B2 (enExample) |
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| AU (2) | AU2011274502A1 (enExample) |
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| EA (1) | EA201390074A1 (enExample) |
| HK (1) | HK1225308A1 (enExample) |
| MX (1) | MX2013000332A (enExample) |
| NZ (1) | NZ606589A (enExample) |
| WO (1) | WO2012006544A1 (enExample) |
| ZA (1) | ZA201300957B (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107176923A (zh) * | 2005-10-19 | 2017-09-19 | 泰华制药工业有限公司 | 拉奎尼莫钠晶体及其制备方法 |
| KR101495327B1 (ko) | 2006-06-12 | 2015-02-24 | 테바 파마슈티컬 인더스트리즈 리미티드 | 안정한 라퀴니모드 제제 |
| US8178127B2 (en) | 2007-12-20 | 2012-05-15 | Teva Pharmaceuticals Industries, Ltd. | Stable laquinimod preparations |
| HUE026406T2 (en) * | 2009-06-19 | 2016-06-28 | Teva Pharma | Treatment of multiple sclerosis with laquinimod |
| CN105616410A (zh) * | 2009-07-30 | 2016-06-01 | 泰华制药工业有限公司 | 利用拉喹莫德治疗克隆氏病 |
| ES2731052T3 (es) | 2009-08-10 | 2019-11-13 | Active Biotech Ab | Tratamiento de la enfermedad de Huntington usando laquinimod |
| KR20150135552A (ko) | 2010-03-03 | 2015-12-02 | 테바 파마슈티컬 인더스트리즈 리미티드 | 라퀴니모드를 이용한 루푸스 신장염의 치료 |
| WO2011109531A1 (en) * | 2010-03-03 | 2011-09-09 | Teva Pharmaceutical Industries Ltd. | Treatment of rheumatoid arthritis with a combination of laquinimod and methotrexate |
| JP2013535437A (ja) | 2010-07-09 | 2013-09-12 | 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 | 重水素化されたn−エチル−n−フェニル−1,2−ジヒドロ−4−ヒドロキシ−5−クロロ−1−メチル−2−オキソキノリン−3−カルボキサミド、その塩および使用 |
| SG11201401330YA (en) | 2011-10-12 | 2014-05-29 | Teva Pharma | Treatment of multiple sclerosis with combination of laquinimod and fingolimod |
| US9161935B2 (en) | 2012-02-03 | 2015-10-20 | Teva Pharmaceutical Industries, Ltd. | Use of laquinimod for treating Crohn's disease patients who failed first-line anti-TNF therapy |
| AR090073A1 (es) | 2012-02-16 | 2014-10-15 | Teva Pharma | N-etil-n-fenil-1,2-dihidro-4,5-di-hidroxi-1-metil-2-oxo-3-quinolinacarboxamida, su preparacion y usos |
| 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 |
| CA2890194A1 (en) | 2012-11-07 | 2014-05-15 | Teva Pharmaceutical Industries Ltd. | Amine salts of laquinimod |
| WO2014153145A2 (en) | 2013-03-14 | 2014-09-25 | Teva Pharmaceutical Industries Ltd. | Crystals of laquinimod sodium and improved process for the manufacture thereof |
| HK1220125A1 (zh) | 2013-03-14 | 2017-04-28 | Teva Pharmaceutical Industries Ltd. | 拉喹莫德的透皮配方 |
| UY36099A (es) | 2014-04-29 | 2016-02-29 | Teva Pharma | Laquinimod para el tratamiento de pacientes con esclerosis múltiple remitente recurrente (rrms) con un alto grado de discapacidad |
| 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 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US6077851A (en) * | 1998-04-27 | 2000-06-20 | Active Biotech Ab | Quinoline derivatives |
| SE9801474D0 (sv) * | 1998-04-27 | 1998-04-27 | Active Biotech Ab | Quinoline Derivatives |
| US6875869B2 (en) | 2002-06-12 | 2005-04-05 | 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 |
| 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 |
| CN107176923A (zh) | 2005-10-19 | 2017-09-19 | 泰华制药工业有限公司 | 拉奎尼莫钠晶体及其制备方法 |
| KR101495327B1 (ko) * | 2006-06-12 | 2015-02-24 | 테바 파마슈티컬 인더스트리즈 리미티드 | 안정한 라퀴니모드 제제 |
| US8178127B2 (en) * | 2007-12-20 | 2012-05-15 | Teva Pharmaceuticals Industries, Ltd. | Stable laquinimod preparations |
| WO2010001257A2 (en) * | 2008-07-01 | 2010-01-07 | Actavis Group Ptc Ehf | Novel solid state forms of laquinimod and its sodium salt |
| US20120009226A1 (en) * | 2008-12-17 | 2012-01-12 | Actavis Group Ptc Ehf | Highly pure laquinimod or a pharmaceutically acceptable salt thereof |
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2011
- 2011-07-08 BR BR112013000607A patent/BR112013000607A2/pt not_active IP Right Cessation
- 2011-07-08 AU AU2011274502A patent/AU2011274502A1/en not_active Abandoned
- 2011-07-08 EA EA201390074A patent/EA201390074A1/ru unknown
- 2011-07-08 MX MX2013000332A patent/MX2013000332A/es unknown
- 2011-07-08 NZ NZ606589A patent/NZ606589A/en not_active IP Right Cessation
- 2011-07-08 CN CN201180034077.5A patent/CN102985090B/zh not_active Expired - Fee Related
- 2011-07-08 WO PCT/US2011/043391 patent/WO2012006544A1/en not_active Ceased
- 2011-07-08 CA CA2804989A patent/CA2804989A1/en not_active Abandoned
- 2011-07-08 EP EP16159268.8A patent/EP3056205A1/en not_active Withdrawn
- 2011-07-08 EP EP11804416.3A patent/EP2590653A4/en not_active Withdrawn
- 2011-07-08 US US13/178,865 patent/US20120010239A1/en not_active Abandoned
- 2011-07-08 KR KR1020137003331A patent/KR20130041193A/ko not_active Ceased
- 2011-07-08 JP JP2013519726A patent/JP5934202B2/ja not_active Expired - Fee Related
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2013
- 2013-02-05 ZA ZA2013/00957A patent/ZA201300957B/en unknown
- 2013-05-20 HK HK16113723.9A patent/HK1225308A1/en unknown
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2015
- 2015-10-16 JP JP2015204932A patent/JP2016053049A/ja active Pending
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2016
- 2016-06-13 US US15/180,727 patent/US20160279121A1/en not_active Abandoned
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2017
- 2017-11-17 AU AU2017261621A patent/AU2017261621A1/en not_active Abandoned
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2018
- 2018-01-04 US US15/861,952 patent/US20180140592A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CA2804989A1 (en) | 2012-01-12 |
| BR112013000607A2 (pt) | 2016-06-28 |
| EP3056205A1 (en) | 2016-08-17 |
| MX2013000332A (es) | 2013-02-26 |
| WO2012006544A1 (en) | 2012-01-12 |
| US20160279121A1 (en) | 2016-09-29 |
| ZA201300957B (en) | 2014-04-30 |
| JP2013534536A (ja) | 2013-09-05 |
| US20180140592A1 (en) | 2018-05-24 |
| US20120010239A1 (en) | 2012-01-12 |
| JP2016053049A (ja) | 2016-04-14 |
| CN102985090B (zh) | 2014-11-26 |
| KR20130041193A (ko) | 2013-04-24 |
| EA201390074A1 (ru) | 2013-06-28 |
| AU2017261621A1 (en) | 2017-12-07 |
| EP2590653A1 (en) | 2013-05-15 |
| CN102985090A (zh) | 2013-03-20 |
| AU2011274502A1 (en) | 2013-02-28 |
| EP2590653A4 (en) | 2014-01-01 |
| NZ606589A (en) | 2015-03-27 |
| HK1225308A1 (en) | 2017-09-08 |
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