KR20090061055A - 결정질 및 비결정질 이매티닙 염기, 이매티닙 메실레이트 및 이들의 제조 방법 - Google Patents
결정질 및 비결정질 이매티닙 염기, 이매티닙 메실레이트 및 이들의 제조 방법 Download PDFInfo
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- KR20090061055A KR20090061055A KR1020097008048A KR20097008048A KR20090061055A KR 20090061055 A KR20090061055 A KR 20090061055A KR 1020097008048 A KR1020097008048 A KR 1020097008048A KR 20097008048 A KR20097008048 A KR 20097008048A KR 20090061055 A KR20090061055 A KR 20090061055A
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- Prior art keywords
- imatinib
- formula
- desmethyl
- base
- compound
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- 238000000034 method Methods 0.000 title claims abstract description 108
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- YLMAHDNUQAMNNX-UHFFFAOYSA-N imatinib methanesulfonate Chemical compound CS(O)(=O)=O.C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 YLMAHDNUQAMNNX-UHFFFAOYSA-N 0.000 title claims abstract description 83
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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| US87442006P | 2006-12-11 | 2006-12-11 | |
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| US93491107P | 2007-06-14 | 2007-06-14 | |
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| US60/958,367 | 2007-07-05 | ||
| US96323807P | 2007-08-02 | 2007-08-02 | |
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| US99533207P | 2007-09-25 | 2007-09-25 | |
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| US60/997,849 | 2007-10-05 | ||
| US97925607P | 2007-10-11 | 2007-10-11 | |
| US60/979,256 | 2007-10-11 |
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| KR20090061055A true KR20090061055A (ko) | 2009-06-15 |
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| KR1020097008048A Ceased KR20090061055A (ko) | 2006-10-26 | 2007-10-26 | 결정질 및 비결정질 이매티닙 염기, 이매티닙 메실레이트 및 이들의 제조 방법 |
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| US (2) | US20080103305A1 (enExample) |
| EP (2) | EP2076507A2 (enExample) |
| JP (2) | JP2009503120A (enExample) |
| KR (2) | KR20090061068A (enExample) |
| MX (1) | MX2008008447A (enExample) |
| WO (2) | WO2008051597A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2530077A1 (en) | 2011-05-30 | 2012-12-05 | Bcworld Pharm. Co. Ltd. | Novel method for preparing imatinib base |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US8414918B2 (en) * | 2007-09-25 | 2013-04-09 | Teva Pharmaceutical Industries Ltd. | Stable imatinib compositions |
| US20100330130A1 (en) * | 2009-05-22 | 2010-12-30 | Actavis Group Ptc Ehf | Substantially pure imatinib or a pharmaceutically acceptable salt thereof |
| EP2509973A1 (en) | 2009-12-10 | 2012-10-17 | Arch Pharmalabs Limited | Process for the preparation of imatinib and salts thereof |
| WO2011095835A1 (en) | 2010-02-02 | 2011-08-11 | Actavis Group Ptc Ehf | Highly pure imatinib or a pharmaceutically acceptable salt thereof |
| EP2582689B1 (en) | 2010-06-18 | 2017-03-01 | KRKA, D.D., Novo Mesto | New polymorphic form of imatinib base and preparation of salts thereof |
| US20130203990A1 (en) * | 2010-07-29 | 2013-08-08 | Dr. Reddy's Laboratories, Inc. | Process for the preparation of imatinib mesylate |
| CN101899035B (zh) * | 2010-09-03 | 2012-09-05 | 天津市炜杰科技有限公司 | 一种高纯度伊马替尼的制备方法 |
| GB2488788B (en) * | 2011-03-07 | 2013-07-10 | Natco Pharma Ltd | Oral formulation of phenylaminopyrymidine compound with enhanced bioavailability and pharmacological response |
| JP2014509642A (ja) | 2011-03-31 | 2014-04-21 | アイエヌディー−スイフト ラボラトリーズ リミテッド | イマチニブ及びそのメシル酸塩の生成のための改良方法 |
| WO2013008242A1 (en) * | 2011-07-12 | 2013-01-17 | Natco Pharma Limited | A process for the preparation of highly pure 4-(4-methyl piperazinomethyl) benzoic acid dihydrochloride |
| CN102850297B (zh) * | 2012-10-10 | 2014-07-23 | 山东金城医药化工股份有限公司 | 伊马酸的制备方法 |
| KR101558960B1 (ko) | 2013-07-18 | 2015-10-08 | 하나제약 주식회사 | Ν-5-(4-[4-메틸-피페라지노-메틸]-벤조일아미도)-2-메틸페닐-4-[3-피리딜]-2-피리미딘-아민의 신규한 제조방법 |
| AU2014296032A1 (en) | 2013-07-31 | 2016-03-17 | Windward Pharma, Inc. | Aerosol tyrosine kinase inhibitor compounds and uses thereof |
| CN103483314B (zh) * | 2013-09-16 | 2015-02-18 | 南京优科生物医药研究有限公司 | 一种便捷的制备甲磺酸伊马替尼α晶型的方法 |
| SE539450C2 (en) * | 2016-02-29 | 2017-09-26 | Imatinib for use in the treatment of stroke | |
| AU2020274521A1 (en) | 2019-05-16 | 2021-12-16 | Aerovate Therapeutics, Inc. | Imatinib formulations, manufacture, and uses thereof |
| US11464776B2 (en) | 2019-05-16 | 2022-10-11 | Aerovate Therapeutics, Inc. | Inhalable imatinib formulations, manufacture, and uses thereof |
| CN115850258B (zh) * | 2022-12-27 | 2024-09-24 | 东北林业大学 | 一种马赛替尼的合成方法 |
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| US4623486A (en) * | 1985-05-29 | 1986-11-18 | Pfizer Inc. | [4-substituted benzoyloxy]-N-substituted-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides having anti-arthritic activity |
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (enExample) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| CO4940418A1 (es) * | 1997-07-18 | 2000-07-24 | Novartis Ag | Modificacion de cristal de un derivado de n-fenil-2- pirimidinamina, procesos para su fabricacion y su uso |
| GB0022438D0 (en) * | 2000-09-13 | 2000-11-01 | Novartis Ag | Organic Compounds |
| EP1425577A4 (en) * | 2001-08-10 | 2004-12-29 | Symyx Technologies Inc | APPARATUSES AND METHODS FOR PREPARING AND TESTING PRE-FORMULATIONS AND CORRESPONDING SYSTEMS |
| JP2003119184A (ja) * | 2001-10-11 | 2003-04-23 | Toray Ind Inc | 置換ピペラジニルメチル芳香族酸誘導体の製造方法 |
| GB0201508D0 (en) * | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| GB0202873D0 (en) * | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
| GB2398565A (en) * | 2003-02-18 | 2004-08-25 | Cipla Ltd | Imatinib preparation and salts |
| AU2003232650A1 (en) * | 2003-05-06 | 2004-11-26 | Il Yang Pharm Co., Ltd. | N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof |
| WO2004106326A1 (en) * | 2003-06-02 | 2004-12-09 | Hetero Drugs Limited | Novel polymorphs of imatinib mesylate |
| US7507821B2 (en) * | 2004-12-30 | 2009-03-24 | Chemagis Ltd. | Process for preparing Imatinib |
| US20060223816A1 (en) * | 2006-05-08 | 2006-10-05 | Chemagis Ltd. | Imatinib mesylate alpha form and production process therefor |
| US20060223817A1 (en) * | 2006-05-15 | 2006-10-05 | Chemagis Ltd. | Crystalline imatinib base and production process therefor |
| US7550591B2 (en) * | 2007-05-02 | 2009-06-23 | Chemagis Ltd. | Imatinib production process |
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2007
- 2007-10-26 EP EP07839811A patent/EP2076507A2/en not_active Withdrawn
- 2007-10-26 US US11/978,227 patent/US20080103305A1/en not_active Abandoned
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- 2007-10-26 US US11/978,170 patent/US20080207904A1/en not_active Abandoned
- 2007-10-26 KR KR1020097008519A patent/KR20090061068A/ko not_active Ceased
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2530077A1 (en) | 2011-05-30 | 2012-12-05 | Bcworld Pharm. Co. Ltd. | Novel method for preparing imatinib base |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20090061068A (ko) | 2009-06-15 |
| JP2009503120A (ja) | 2009-01-29 |
| MX2008008447A (es) | 2008-09-15 |
| WO2008057291B1 (en) | 2008-08-21 |
| JP2009514988A (ja) | 2009-04-09 |
| WO2008057291A2 (en) | 2008-05-15 |
| WO2008051597A1 (en) | 2008-05-02 |
| EP2076507A2 (en) | 2009-07-08 |
| US20080207904A1 (en) | 2008-08-28 |
| EP1966186A1 (en) | 2008-09-10 |
| US20080103305A1 (en) | 2008-05-01 |
| WO2008057291A3 (en) | 2008-07-03 |
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