BRPI0618993A2 - formas de cristais f, g, h, i e k de mesilato de imatinib - Google Patents
formas de cristais f, g, h, i e k de mesilato de imatinib Download PDFInfo
- Publication number
- BRPI0618993A2 BRPI0618993A2 BRPI0618993-8A BRPI0618993A BRPI0618993A2 BR PI0618993 A2 BRPI0618993 A2 BR PI0618993A2 BR PI0618993 A BRPI0618993 A BR PI0618993A BR PI0618993 A2 BRPI0618993 A2 BR PI0618993A2
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- BR
- Brazil
- Prior art keywords
- formula
- compound
- acid addition
- addition salt
- methanesulfonic acid
- Prior art date
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- 239000013078 crystal Substances 0.000 title claims abstract description 192
- 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 description 36
- 229960003685 imatinib mesylate Drugs 0.000 title description 31
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims abstract description 198
- 150000003839 salts Chemical class 0.000 claims abstract description 110
- 229940098779 methanesulfonic acid Drugs 0.000 claims abstract description 99
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- 238000002360 preparation method Methods 0.000 claims abstract description 25
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- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 16
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- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 11
- 235000019359 magnesium stearate Nutrition 0.000 claims description 9
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- GFZFAQOKWZGMQL-UHFFFAOYSA-N 3-[3,5-bis(trifluoromethyl)phenyl]-3-oxopropanenitrile Chemical compound FC(F)(F)C1=CC(C(=O)CC#N)=CC(C(F)(F)F)=C1 GFZFAQOKWZGMQL-UHFFFAOYSA-N 0.000 claims 2
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- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound 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 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 abstract description 4
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Classifications
-
- 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
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0524062A GB0524062D0 (en) | 2005-11-25 | 2005-11-25 | Organic compounds |
| GB0524061.9 | 2005-11-25 | ||
| GB0524061A GB0524061D0 (en) | 2005-11-25 | 2005-11-25 | Organic compounds |
| GB0524062.7 | 2005-11-25 | ||
| US74001605P | 2005-11-28 | 2005-11-28 | |
| US74001705P | 2005-11-28 | 2005-11-28 | |
| US74001805P | 2005-11-28 | 2005-11-28 | |
| US60/740,017 | 2005-11-28 | ||
| US60/740,016 | 2005-11-28 | ||
| US60/740,018 | 2005-11-28 | ||
| PCT/EP2006/011240 WO2007059963A1 (en) | 2005-11-25 | 2006-11-23 | F,g,h,i and k crystal forms of imatinib mesylate |
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| NO (1) | NO20082684L (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| PE20051096A1 (es) | 2004-02-04 | 2006-01-23 | Novartis Ag | Formas de sal de 4-(4-metilpiperazin-1-ilmetil)-n-[4-metil-3-(4-piridin-3-il)pirimidin-2-ilamino)fenil]-benzamida |
| JP5844508B2 (ja) * | 2005-11-25 | 2016-01-20 | ノバルティス アーゲー | メシル酸イマチニブのｆ結晶形 |
| US20090087489A1 (en) * | 2007-09-25 | 2009-04-02 | Bella Gerber | Imatinib compositions |
| RU2365587C1 (ru) * | 2008-02-22 | 2009-08-27 | Закрытое Акционерное Общество "Фарм-Синтез" | Рентгеноаморфная безводная модификация 4-[(4-метил-1-пиперазинил)метил]-n-[4-метил-3-[[4-(3-пиридинил)-2-пиримидинил]-амино]-фенил]бензамида метансульфоната и способ ее получения |
| CZ2009570A3 (cs) | 2009-08-26 | 2011-03-09 | Zentiva, K. S. | Príprava, stabilizace a využití polymorfu imatinib mesylátu pro vývoj lékových forem |
| PL389357A1 (pl) | 2009-10-22 | 2011-04-26 | Tomasz Koźluk | Sole imatinibu z pochodnymi kwasów winowych i sposób ich wytwarzania |
| JP2013519665A (ja) | 2010-02-15 | 2013-05-30 | リライアンス ライフ サイエンシズ ピーヴィーティー リミティッド | メシル酸イマチニブのα形の製造方法 |
| PL390611A1 (pl) | 2010-03-04 | 2011-09-12 | Tomasz Koźluk | Sposób otrzymywania polimorficznej formy alfa i nowa forma polimorficzna mesylanu imatinibu |
| WO2012090221A1 (en) | 2010-12-29 | 2012-07-05 | Cadila Healthcare Limited | Novel salts of imatinib |
| EP2604596A1 (en) * | 2011-12-16 | 2013-06-19 | Deva Holding Anonim Sirketi | Polymorphs of imatinib |
| EP2864313A1 (en) | 2012-06-22 | 2015-04-29 | Basf Se | Multicomponent crystals comprising imatinib mesilate and selected co-crystal formers |
| KR101242955B1 (ko) * | 2012-06-25 | 2013-03-12 | 제일약품주식회사 | 이마티닙 메실레이트 결정형 α의 제조 방법 |
| ES2683361T3 (es) | 2013-05-14 | 2018-09-26 | Hetero Research Foundation | Composiciones de Imatinib |
| US10478290B2 (en) * | 2013-11-26 | 2019-11-19 | Children's Medical Center Corporation | Expandable stent valve |
| WO2018089404A1 (en) | 2016-11-11 | 2018-05-17 | Mallinckrodt Nuclear Medicine Llc | Processes for generating germanium-68 with reduced volatiles |
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| 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 |
| US20060073185A1 (en) | 2002-12-13 | 2006-04-06 | Bausch & Lomb Incorporated | Method and composition for contact lenses |
| TR200504337T1 (tr) * | 2003-06-02 | 2006-12-21 | Hetero Drugs Limited | Imatinib mezilat'ın yeni polimorfları |
| PE20051096A1 (es) | 2004-02-04 | 2006-01-23 | Novartis Ag | Formas de sal de 4-(4-metilpiperazin-1-ilmetil)-n-[4-metil-3-(4-piridin-3-il)pirimidin-2-ilamino)fenil]-benzamida |
| CA2555804C (en) * | 2004-02-11 | 2012-06-26 | Natco Pharma Limited | Polymorphic form of imatinib mesylate and a process for its preparation |
| UA84462C2 (ru) * | 2004-04-02 | 2008-10-27 | Институт Фармацевтични | Полиморфные модификации кислотно-аддитивных солей иматиниба с метансульфоновой кислотой |
| WO2005117885A1 (en) | 2004-06-04 | 2005-12-15 | Bioniche Life Sciences Inc. | Use of imatinib to treat liver disorders and viral infections |
| KR101348625B1 (ko) * | 2004-09-02 | 2014-01-07 | 씨아이피엘에이 엘티디. | 이매티닙 메실레이트의 안정한 결정형 및 그의 제조방법 |
| WO2006048890A1 (en) * | 2004-11-04 | 2006-05-11 | Sun Pharmaceutical Industries Limited | Imatinib mesylate crystal form and process for preparation thereof |
| WO2006054314A1 (en) * | 2004-11-17 | 2006-05-26 | Natco Pharma Limited | Polymorphic forms of imatinib mesylate |
| US9804295B2 (en) | 2005-05-05 | 2017-10-31 | Novartis Ag | Ophthalmic devices for sustained delivery of active compounds |
| GB0511066D0 (en) | 2005-05-31 | 2005-07-06 | Novartis Ag | Organic compounds |
| UY29766A1 (es) * | 2005-08-26 | 2007-03-30 | Novartis Ag | Formas cristalinas delta y épsilon de mesilato de imatinib |
| JP5844508B2 (ja) * | 2005-11-25 | 2016-01-20 | ノバルティス アーゲー | メシル酸イマチニブのｆ結晶形 |
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2006
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- 2006-11-23 KR KR1020087012363A patent/KR20080078804A/ko not_active Ceased
- 2006-11-23 EP EP12177131.5A patent/EP2578580A1/en not_active Withdrawn
- 2006-11-23 EP EP12177119A patent/EP2546248A1/en not_active Withdrawn
- 2006-11-23 KR KR1020137031544A patent/KR20130140909A/ko not_active Ceased
- 2006-11-23 WO PCT/EP2006/011240 patent/WO2007059963A1/en not_active Ceased
- 2006-11-23 CA CA2824307A patent/CA2824307C/en not_active Expired - Fee Related
- 2006-11-23 BR BRPI0618993-8A patent/BRPI0618993A2/pt not_active IP Right Cessation
- 2006-11-23 CA CA2824301A patent/CA2824301C/en not_active Expired - Fee Related
- 2006-11-23 KR KR1020137031545A patent/KR20130137721A/ko not_active Ceased
- 2006-11-23 KR KR1020137031543A patent/KR20130141712A/ko not_active Ceased
- 2006-11-23 UY UY29964A patent/UY29964A1/es not_active Application Discontinuation
- 2006-11-23 AU AU2006316823A patent/AU2006316823A1/en not_active Abandoned
- 2006-11-23 US US12/094,629 patent/US7893076B2/en not_active Expired - Fee Related
- 2006-11-23 CN CN201110232553.6A patent/CN102351842B/zh not_active Expired - Fee Related
- 2006-11-23 MY MYPI20081624A patent/MY146403A/en unknown
- 2006-11-23 CA CA2628330A patent/CA2628330C/en not_active Expired - Fee Related
- 2006-11-23 EP EP06818763A patent/EP1960380A1/en not_active Withdrawn
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2008
- 2008-05-20 EC EC2008008473A patent/ECSP088473A/es unknown
- 2008-06-16 NO NO20082684A patent/NO20082684L/no not_active Application Discontinuation
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- 2011-01-14 US US13/006,505 patent/US8198289B2/en not_active Expired - Fee Related
- 2011-03-22 AU AU2011201286A patent/AU2011201286A1/en not_active Ceased
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- 2011-07-15 US US13/183,557 patent/US8507515B2/en not_active Expired - Fee Related
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- 2014-01-16 JP JP2014005741A patent/JP2014074067A/ja active Pending
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