CN101291911B - 拉奎尼莫钠晶体及其制备方法 - Google Patents
拉奎尼莫钠晶体及其制备方法 Download PDFInfo
- Publication number
- CN101291911B CN101291911B CN200680039201.6A CN200680039201A CN101291911B CN 101291911 B CN101291911 B CN 101291911B CN 200680039201 A CN200680039201 A CN 200680039201A CN 101291911 B CN101291911 B CN 101291911B
- Authority
- CN
- China
- Prior art keywords
- mixture
- sodium
- content
- laquinimole
- nickel
- 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
- C07D215/20—Oxygen atoms
- C07D215/22—Oxygen atoms attached in position 2 or 4
-
- 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
- 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
-
- 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
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Quinoline Compounds (AREA)
- Medicinal Preparation (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710533188.XA CN107176923A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72865705P | 2005-10-19 | 2005-10-19 | |
| US60/728,657 | 2005-10-19 | ||
| PCT/US2006/040925 WO2007047863A2 (en) | 2005-10-19 | 2006-10-18 | Crystals of laquinimod sodium, and process for the manufacture thereof |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201710533188.XA Division CN107176923A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
| CN2013102471796A Division CN103333107A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101291911A CN101291911A (zh) | 2008-10-22 |
| CN101291911B true CN101291911B (zh) | 2014-08-13 |
Family
ID=37963287
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200680039201.6A Expired - Fee Related CN101291911B (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
| CN2013102471796A Pending CN103333107A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
| CN201710533188.XA Pending CN107176923A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2013102471796A Pending CN103333107A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
| CN201710533188.XA Pending CN107176923A (zh) | 2005-10-19 | 2006-10-18 | 拉奎尼莫钠晶体及其制备方法 |
Country Status (23)
Cited By (1)
| 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 |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8314124B2 (en) | 2004-02-06 | 2012-11-20 | Active Biotech Ab | Crystalline salts of quinoline compounds and methods for preparing them |
| CN101466379B (zh) | 2006-06-12 | 2012-10-31 | 泰华制药工业有限公司 | 稳定的拉喹莫德的制剂 |
| WO2009082471A1 (en) * | 2007-12-20 | 2009-07-02 | Teva Pharmaceutical Industries, Ltd. | Stable laquinimod preparations |
| US8354428B2 (en) | 2008-07-01 | 2013-01-15 | Actavis Group Ptc Ehf | Solid state forms of laquinimod and its sodium salt |
| AU2009288108B2 (en) * | 2008-09-03 | 2013-10-17 | Teva Pharmaceutical Industries, Ltd. | 2-oxo-1,2-dihydro-quinoline modulators of immune function |
| WO2010070449A2 (en) | 2008-12-17 | 2010-06-24 | Actavis Group Ptc Ehf | Highly pure laquinimod or a pharmaceutically acceptable salt thereof |
| DE102009008851A1 (de) | 2009-02-13 | 2010-08-19 | Amw Gmbh | Transdermales System mit Immunmodulator |
| DE102010048788A1 (de) | 2009-02-13 | 2011-05-19 | Amw Gmbh | Transdermales System mit Immunmodulator |
| NZ597378A (en) | 2009-06-19 | 2014-08-29 | Teva Pharma | Treatment of multiple sclerosis with laquinimod |
| BR112012002124A2 (pt) * | 2009-07-30 | 2015-09-15 | Teva Pharma | tratamento da doença de crohn com laquinimode. |
| WO2011019375A1 (en) * | 2009-08-10 | 2011-02-17 | Teva Pharmaceutical Industries Ltd. | Treatment of bdnf-related disorders using laquinimod |
| DE102010026879A1 (de) | 2010-02-11 | 2011-08-11 | AMW GmbH, 83627 | Transdermales System mit Immunmodulator |
| EA201290860A1 (ru) * | 2010-03-03 | 2013-04-30 | Тева Фармасьютикал Индастриз Лтд. | Лечение ревматоидного артрита комбинацией лаквинимода и метотрексата |
| US20110217295A1 (en) * | 2010-03-03 | 2011-09-08 | Asi Haviv | Treatment of lupus arthritis using laquinimod |
| KR20130006640A (ko) | 2010-03-03 | 2013-01-17 | 테바 파마슈티컬 인더스트리즈 리미티드 | 라퀴니모드를 이용한 루푸스 신장염의 치료 |
| JP5934202B2 (ja) | 2010-07-09 | 2016-06-15 | 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 | 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 |
| AU2011274496B2 (en) * | 2010-07-09 | 2016-03-10 | 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 |
| US8865742B2 (en) | 2010-11-28 | 2014-10-21 | Mapi Pharma Ltd. | Intermediate compounds and processes for the preparation of quinoline derivatives such as Laquinimod sodium |
| SG11201401330YA (en) * | 2011-10-12 | 2014-05-29 | Teva Pharma | Treatment of multiple sclerosis with combination of laquinimod and fingolimod |
| WO2013116657A1 (en) | 2012-02-03 | 2013-08-08 | Teva Pharmaceutical Industries Ltd. | USE OF LAQUINIMOD FOR TREATING CROHN'S DISEASE PATIENTS WHO FAILED FIRST-LINE ANTI-TNFα THERAPY |
| MX2014009889A (es) * | 2012-02-16 | 2014-11-13 | Teva Pharma | N-etil-n-fenil-1,2-dihidro-4,5-di-hidroxi-1-metil-2-oxo-3-quinoli ncarboxamida, preparacion y usos de los mismos. |
| US20130259856A1 (en) | 2012-03-27 | 2013-10-03 | Teva Pharmaceutical Industries, Ltd. | Treatment of multiple sclerosis with combination of laquinimod and dimethyl fumarate |
| 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 |
| AR091706A1 (es) * | 2012-07-11 | 2015-02-25 | Teva Pharma | Formulaciones de laquinimod sin agentes alcalinizantes |
| 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 |
| WO2014033954A1 (ja) | 2012-09-03 | 2014-03-06 | トヨタ自動車株式会社 | 衝突判定装置及び衝突判定方法 |
| EA201590788A1 (ru) | 2012-11-07 | 2015-12-30 | Тева Фармасьютикал Индастриз Лтд. | Аминные соли лахинимода |
| JP2016514162A (ja) * | 2013-03-14 | 2016-05-19 | 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 | ラキニモドナトリウムの結晶およびその製造のための改善された方法 |
| WO2014152009A1 (en) | 2013-03-14 | 2014-09-25 | Teva Pharmaceutical Industries Ltd. | Transdermal formulations of laquinimod |
| TWI665190B (zh) | 2013-11-15 | 2019-07-11 | 阿克比治療有限公司 | {[5-(3-氯苯基)-3-羥基吡啶-2-羰基]胺基}乙酸之固體型式,其組合物及用途 |
| HK1231413A1 (zh) | 2014-04-29 | 2017-12-22 | Teva Pharmaceutical Industries Ltd. | 用於治疗具有高残疾状况的复发-缓解型多发性硬化症(rrms)的患者的拉喹莫德 |
| JP7842983B2 (ja) * | 2021-02-25 | 2026-04-09 | 学校法人神戸学院 | 腸管吸収用補助剤及びその利用方法 |
| KR102876408B1 (ko) * | 2022-01-24 | 2025-10-24 | 한국과학기술원 | 입도가 조절된 헥사나이트로스틸벤 타입 iv의 제조방법 |
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| CN101466379B (zh) | 2006-06-12 | 2012-10-31 | 泰华制药工业有限公司 | 稳定的拉喹莫德的制剂 |
| WO2009082471A1 (en) * | 2007-12-20 | 2009-07-02 | Teva Pharmaceutical Industries, Ltd. | Stable laquinimod preparations |
| US8354428B2 (en) | 2008-07-01 | 2013-01-15 | Actavis Group Ptc Ehf | Solid state forms of laquinimod and its sodium salt |
| AU2009288108B2 (en) | 2008-09-03 | 2013-10-17 | Teva Pharmaceutical Industries, Ltd. | 2-oxo-1,2-dihydro-quinoline modulators of immune function |
| NZ597378A (en) | 2009-06-19 | 2014-08-29 | Teva Pharma | Treatment of multiple sclerosis with laquinimod |
| BR112012002124A2 (pt) | 2009-07-30 | 2015-09-15 | Teva Pharma | tratamento da doença de crohn com laquinimode. |
| WO2011019375A1 (en) | 2009-08-10 | 2011-02-17 | Teva Pharmaceutical Industries Ltd. | Treatment of bdnf-related disorders using laquinimod |
| US20110217295A1 (en) | 2010-03-03 | 2011-09-08 | Asi Haviv | Treatment of lupus arthritis using laquinimod |
| KR20130006640A (ko) | 2010-03-03 | 2013-01-17 | 테바 파마슈티컬 인더스트리즈 리미티드 | 라퀴니모드를 이용한 루푸스 신장염의 치료 |
| EA201290860A1 (ru) | 2010-03-03 | 2013-04-30 | Тева Фармасьютикал Индастриз Лтд. | Лечение ревматоидного артрита комбинацией лаквинимода и метотрексата |
| JP5934202B2 (ja) | 2010-07-09 | 2016-06-15 | 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 | 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 |
| AU2011274496B2 (en) | 2010-07-09 | 2016-03-10 | 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 |
| US20120055072A1 (en) * | 2010-09-08 | 2012-03-08 | Rankin Sammy D | Directional guide for fishing lures |
| PE20140872A1 (es) | 2010-12-07 | 2014-08-09 | Teva Pharma | Uso de laquinimod para reducir la fatiga, mejorar el estado funcional y mejorar la calidad de vida en pacientes con esclerosis multiple |
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| CN1298393A (zh) * | 1998-04-27 | 2001-06-06 | 活跃生物技术有限公司 | 喹啉衍生物 |
| US6875869B2 (en) * | 2002-06-12 | 2005-04-05 | Active Biotech Ab | Process for the manufacture of quinoline derivatives |
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| 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 |
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