RU2415841C2 - Кристаллы лаквинимода натрия и способ их производства - Google Patents
Кристаллы лаквинимода натрия и способ их производства Download PDFInfo
- Publication number
- RU2415841C2 RU2415841C2 RU2008119456/04A RU2008119456A RU2415841C2 RU 2415841 C2 RU2415841 C2 RU 2415841C2 RU 2008119456/04 A RU2008119456/04 A RU 2008119456/04A RU 2008119456 A RU2008119456 A RU 2008119456A RU 2415841 C2 RU2415841 C2 RU 2415841C2
- Authority
- RU
- Russia
- Prior art keywords
- sodium
- laquinimod sodium
- laquinimod
- mixture
- million
- Prior art date
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- GKWPCEFFIHSJOE-UHFFFAOYSA-N laquinimod Chemical compound OC=1C2=C(Cl)C=CC=C2N(C)C(=O)C=1C(=O)N(CC)C1=CC=CC=C1 GKWPCEFFIHSJOE-UHFFFAOYSA-N 0.000 title claims abstract description 137
- 229960004577 laquinimod Drugs 0.000 title claims abstract description 134
- 238000000034 method Methods 0.000 title claims abstract description 63
- 239000013078 crystal Substances 0.000 title claims abstract description 31
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 title claims abstract description 26
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Images
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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72865705P | 2005-10-19 | 2005-10-19 | |
| US60/728,657 | 2005-10-19 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2008119456A RU2008119456A (ru) | 2009-11-27 |
| RU2415841C2 true RU2415841C2 (ru) | 2011-04-10 |
Family
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| RU2008119456/04A RU2415841C2 (ru) | 2005-10-19 | 2006-10-18 | Кристаллы лаквинимода натрия и способ их производства |
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| DK (1) | DK1937642T3 (enExample) |
| ES (1) | ES2523762T3 (enExample) |
| HR (1) | HRP20141160T1 (enExample) |
| IL (1) | IL190137A (enExample) |
| NZ (2) | NZ592897A (enExample) |
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| PT (1) | PT1937642E (enExample) |
| RS (1) | RS53666B1 (enExample) |
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| SG (1) | SG10201508623RA (enExample) |
| SI (1) | SI1937642T1 (enExample) |
| UA (1) | UA92761C2 (enExample) |
| WO (1) | WO2007047863A2 (enExample) |
| ZA (1) | ZA200803527B (enExample) |
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| US8314124B2 (en) | 2004-02-06 | 2012-11-20 | Active Biotech Ab | Crystalline salts of quinoline compounds and methods for preparing them |
| SI1937642T1 (sl) * | 2005-10-19 | 2015-01-30 | Teva Pharmaceutical Industries Ltd. | Kristali natrijevega lakvinimoda in postopek za njihovo pripravo |
| HRP20120093T1 (hr) * | 2006-06-12 | 2012-03-31 | Teva Pharmaceutical Industries Limited | Postojani pripravci lakvinimoda |
| SI2234485T1 (sl) | 2007-12-20 | 2014-03-31 | Teva Pharmaceutical Industries Ltd. | Stabilni lakvinimodni pripravki |
| EP2318371A2 (en) | 2008-07-01 | 2011-05-11 | Actavis Group PTC EHF | Novel solid state forms of laquinimod and its sodium salt |
| EA021227B1 (ru) * | 2008-09-03 | 2015-05-29 | Тева Фармасьютикал Индастриз Лтд. | 2-оксо-1,2-дигидрохинолиновые модуляторы иммунной функции |
| US20120009226A1 (en) | 2008-12-17 | 2012-01-12 | 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 |
| US20100322900A1 (en) | 2009-06-19 | 2010-12-23 | Teva Pharmaceutical Industries, Ltd. | Treatment of multiple sclerosis with laquinimod |
| US8598203B2 (en) * | 2009-07-30 | 2013-12-03 | Teva Pharmaceutical Industries, Ltd. | Treatment of Crohn's disease with laquinimod |
| CA2771203C (en) | 2009-08-10 | 2019-04-09 | 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 |
| ES2558556T3 (es) * | 2010-03-03 | 2016-02-05 | Teva Pharmaceutical Industries Ltd. | Tratamiento de nefritis lúpica usando laquinimod |
| JP2013521305A (ja) * | 2010-03-03 | 2013-06-10 | 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 | ラキニモドを用いるループス関節炎の治療 |
| BR112012022187A2 (pt) * | 2010-03-03 | 2015-09-22 | Teva Pharma | tratamento de artrite reumatóide com a combinação de laquinimod e metotrexato |
| 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 |
| PE20130396A1 (es) | 2010-07-09 | 2013-04-19 | Teva Pharma | N-etil-n-fenil-1,2-dihidro-4-hidroxi-5-cloro-1-metil-2-oxoquinolina-3-carboxamida deuterada, sales y usos de la misma |
| IN2013MN00811A (enExample) | 2010-11-28 | 2015-06-12 | Mapi Pharma Ltd | |
| 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 |
| TW201345527A (zh) | 2012-02-03 | 2013-11-16 | Teva Pharma | 拉喹莫德於治療對第一線抗－ＴＮＦα療法無效之克隆氏症患者之用途 |
| 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 |
| 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 |
| CN104584098B (zh) | 2012-09-03 | 2017-09-15 | 丰田自动车株式会社 | 碰撞判定装置和碰撞判定方法 |
| HK1215210A1 (zh) | 2012-11-07 | 2016-08-19 | Teva Pharmaceutical Industries Ltd. | 拉喹莫德胺盐 |
| EA201591699A1 (ru) * | 2013-03-14 | 2016-02-29 | Тева Фармасьютикал Индастриз Лтд. | Кристаллы лаквинимода натрия и улучшенный способ их производства |
| WO2014152009A1 (en) | 2013-03-14 | 2014-09-25 | Teva Pharmaceutical Industries Ltd. | Transdermal formulations of laquinimod |
| CN114890943A (zh) | 2013-11-15 | 2022-08-12 | 阿克比治疗有限公司 | {[5-(3-氯苯基)-3-羟基吡啶-2-羰基]氨基}乙酸固体形式，组合物和用途 |
| US20150306088A1 (en) | 2014-04-29 | 2015-10-29 | Teva Pharmaceutical Industries, Ltd. | Laquinimod for the treatment of relapsing-remitting multiple sclerosis (rrms) patients with a high disability status |
| JP2022130270A (ja) * | 2021-02-25 | 2022-09-06 | シンバイオシス株式会社 | 腸管吸収用補助剤及びその利用方法 |
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| SI1937642T1 (sl) | 2005-10-19 | 2015-01-30 | Teva Pharmaceutical Industries Ltd. | Kristali natrijevega lakvinimoda in postopek za njihovo pripravo |
| HRP20120093T1 (hr) | 2006-06-12 | 2012-03-31 | Teva Pharmaceutical Industries Limited | Postojani pripravci lakvinimoda |
| SI2234485T1 (sl) | 2007-12-20 | 2014-03-31 | Teva Pharmaceutical Industries Ltd. | Stabilni lakvinimodni pripravki |
| EP2318371A2 (en) | 2008-07-01 | 2011-05-11 | Actavis Group PTC EHF | Novel solid state forms of laquinimod and its sodium salt |
| EA021227B1 (ru) * | 2008-09-03 | 2015-05-29 | Тева Фармасьютикал Индастриз Лтд. | 2-оксо-1,2-дигидрохинолиновые модуляторы иммунной функции |
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| US8598203B2 (en) | 2009-07-30 | 2013-12-03 | Teva Pharmaceutical Industries, Ltd. | Treatment of Crohn's disease with laquinimod |
| CA2771203C (en) * | 2009-08-10 | 2019-04-09 | Teva Pharmaceutical Industries Ltd. | Treatment of bdnf-related disorders using laquinimod |
| ES2558556T3 (es) * | 2010-03-03 | 2016-02-05 | Teva Pharmaceutical Industries Ltd. | Tratamiento de nefritis lúpica usando laquinimod |
| BR112012022187A2 (pt) * | 2010-03-03 | 2015-09-22 | Teva Pharma | tratamento de artrite reumatóide com a combinação de laquinimod e metotrexato |
| JP2013521305A (ja) * | 2010-03-03 | 2013-06-10 | 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 | ラキニモドを用いるループス関節炎の治療 |
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| 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 |
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-
2006
- 2006-10-18 SI SI200631860T patent/SI1937642T1/sl unknown
- 2006-10-18 CN CN200680039201.6A patent/CN101291911B/zh not_active Expired - Fee Related
- 2006-10-18 EP EP13153698.9A patent/EP2687512A1/en not_active Withdrawn
- 2006-10-18 BR BRPI0617477-9A patent/BRPI0617477A2/pt not_active Application Discontinuation
- 2006-10-18 NZ NZ592897A patent/NZ592897A/xx unknown
- 2006-10-18 US US11/583,282 patent/US7884208B2/en not_active Expired - Fee Related
- 2006-10-18 NZ NZ567088A patent/NZ567088A/en unknown
- 2006-10-18 CN CN2013102471796A patent/CN103333107A/zh active Pending
- 2006-10-18 RS RS20140629A patent/RS53666B1/sr unknown
- 2006-10-18 ZA ZA200803527A patent/ZA200803527B/xx unknown
- 2006-10-18 HR HRP20141160TT patent/HRP20141160T1/hr unknown
- 2006-10-18 SG SG10201508623RA patent/SG10201508623RA/en unknown
- 2006-10-18 EP EP06826297.1A patent/EP1937642B1/en active Active
- 2006-10-18 JP JP2008536806A patent/JP5832716B2/ja not_active Expired - Fee Related
- 2006-10-18 DK DK06826297.1T patent/DK1937642T3/en active
- 2006-10-18 WO PCT/US2006/040925 patent/WO2007047863A2/en not_active Ceased
- 2006-10-18 PT PT68262971T patent/PT1937642E/pt unknown
- 2006-10-18 PL PL06826297T patent/PL1937642T3/pl unknown
- 2006-10-18 RU RU2008119456/04A patent/RU2415841C2/ru not_active IP Right Cessation
- 2006-10-18 UA UAA200806003A patent/UA92761C2/ru unknown
- 2006-10-18 CA CA2625287A patent/CA2625287C/en not_active Expired - Fee Related
- 2006-10-18 AU AU2006304672A patent/AU2006304672B2/en not_active Ceased
- 2006-10-18 ES ES06826297.1T patent/ES2523762T3/es active Active
- 2006-10-18 KR KR1020087011727A patent/KR101440982B1/ko not_active Expired - Fee Related
- 2006-10-18 CN CN201710533188.XA patent/CN107176923A/zh active Pending
- 2006-10-19 AR ARP060104574A patent/AR056708A1/es unknown
-
2008
- 2008-03-13 IL IL190137A patent/IL190137A/en not_active IP Right Cessation
-
2011
- 2011-01-21 US US13/011,233 patent/US8647646B2/en not_active Expired - Fee Related
- 2011-01-21 US US13/011,187 patent/US8673322B2/en not_active Expired - Fee Related
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2012
- 2012-12-19 JP JP2012277069A patent/JP2013100299A/ja not_active Withdrawn
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2014
- 2014-02-20 US US14/185,470 patent/US20140171647A1/en not_active Abandoned
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2015
- 2015-07-31 JP JP2015152209A patent/JP2016020353A/ja active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2056411C1 (ru) * | 1991-06-22 | 1996-03-20 | Байер Аг | Производные хинолон- или нафтиридонкарбоновой кислоты или их гидраты, или соли, способ их получения и антимикробная композиция |
| US6077851A (en) * | 1998-04-27 | 2000-06-20 | Active Biotech Ab | Quinoline derivatives |
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