JP5173794B2 - Src/abl阻害剤 - Google Patents
Src/abl阻害剤 Download PDFInfo
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- JP5173794B2 JP5173794B2 JP2008510188A JP2008510188A JP5173794B2 JP 5173794 B2 JP5173794 B2 JP 5173794B2 JP 2008510188 A JP2008510188 A JP 2008510188A JP 2008510188 A JP2008510188 A JP 2008510188A JP 5173794 B2 JP5173794 B2 JP 5173794B2
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Classifications
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; Derivatives thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
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- A—HUMAN NECESSITIES
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
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- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Immunology (AREA)
- Biophysics (AREA)
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- Inorganic Chemistry (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
本出願は、米国特許仮出願第60/678,030号(2005年5月5日出願)の利益を請求するものであり、それはそのまま本明細書に引用される。
本明細書では、‘N−(2−クロロ−6−メチルフェニル)−2−[[6−[4−(2−ヒドロキシエチル)−1−ピペラジニル]−2−メチル−4−ピリミジニル]アミノ]−5−チアゾールカルボキサミドの医薬組成物、および腫瘍性および免疫性障害の治療における該医薬組成物の使用方法を開示する。
本明細書では、式(I)の化合物の医薬組成物、並びに腫瘍性および免疫性障害の治療方法を開示する。
一つの態様は、医薬的に許容される担体、および治療上の有効量の式(I):
1.適当な混合器中、一水和物結晶の化合物(I)、乳糖一水和物、部分または全微結晶セルロース、クロスカルメロースナトリウム、およびヒドロキシプロピルセルロースを混合する。
2.適当な混合器中、工程[1]から得た混合物を水で造粒する(内部造粒工程)。
3.工程[2]からの造粒物を乾燥する。
4.工程[3]からの乾燥した造粒物を、適当なスクリーンまたはミルに通す。
5.工程[4]からの乾燥した造粒物に、微結晶セルロースの残分を加え、適当な混合器でブレンドする(外部造粒工程)。
6.スクリーン処理前のステアリン酸マグネシウムを工程[5]からの混合物に加え、適当な混合器中ブレンドする(外部造粒工程)。
7.工程[6]の混合物を錠剤に圧縮成形する。
8.フィルムコーティング用の懸濁液を調製する。
9.錠剤をフィルムコーティングする。
Claims (5)
- 該非反応性コーティング剤が式(I)の化合物と反応しない、請求項1の組成物。
- 該医薬的に許容される担体が、乳糖一水和物、微結晶セルロース、ヒドロキシプロピルセルロース、クロスカルメロースナトリウム、およびステアリン酸マグネシウムを含む、請求項1の組成物。
- 非反応性コーティング剤が、ヒドロキシプロピルメチルセルロース、二酸化チタン、およびポリエチレングリコールを含む、請求項4の組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US67803005P | 2005-05-05 | 2005-05-05 | |
US60/678,030 | 2005-05-05 | ||
PCT/US2006/017073 WO2006121742A2 (en) | 2005-05-05 | 2006-05-04 | Formulations of a src/abl inhibitor |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2008540440A JP2008540440A (ja) | 2008-11-20 |
JP5173794B2 true JP5173794B2 (ja) | 2013-04-03 |
Family
ID=37076246
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2008510188A Active JP5173794B2 (ja) | 2005-05-05 | 2006-05-04 | Src/abl阻害剤 |
Country Status (18)
Country | Link |
---|---|
US (2) | US20060251723A1 (ja) |
EP (1) | EP1885339B1 (ja) |
JP (1) | JP5173794B2 (ja) |
CN (2) | CN101170996A (ja) |
AR (1) | AR054445A1 (ja) |
DK (1) | DK1885339T3 (ja) |
ES (1) | ES2546847T3 (ja) |
GE (1) | GEP20104927B (ja) |
HR (1) | HRP20151051T1 (ja) |
HU (1) | HUE026040T2 (ja) |
NO (1) | NO343939B1 (ja) |
PE (1) | PE20061373A1 (ja) |
PL (1) | PL1885339T3 (ja) |
PT (1) | PT1885339E (ja) |
RS (1) | RS54258B1 (ja) |
SI (1) | SI1885339T1 (ja) |
TW (1) | TWI386205B (ja) |
WO (1) | WO2006121742A2 (ja) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2000062778A1 (en) | 1999-04-15 | 2000-10-26 | Bristol-Myers Squibb Co. | Cyclic protein tyrosine kinase inhibitors |
GEP20104927B (en) | 2005-05-05 | 2010-03-25 | Bristol Myers Squibb Co | Formulations of a src/abl inhibitor |
CA2610157A1 (en) * | 2005-06-09 | 2006-12-21 | Bristol-Myers Squibb Company | Methods of identifying and treating individuals exhibiting mutant kit protein |
US20070105867A1 (en) * | 2005-09-21 | 2007-05-10 | Bristol-Myers Squibb Company | Oral administration of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-1,3-thiazole-5-carboxamide and salts thereof |
US20090306094A1 (en) * | 2006-03-17 | 2009-12-10 | Bristol-Myers Squibb Company | Methods Of Identifying And Treating Individuals Exhibiting Mutant Bcr/Abl Kinase Polypeptides |
WO2008106059A1 (en) * | 2007-02-26 | 2008-09-04 | Merck & Co., Inc. | Formulations for cathepsin k inhibitors |
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WO2000062778A1 (en) | 1999-04-15 | 2000-10-26 | Bristol-Myers Squibb Co. | Cyclic protein tyrosine kinase inhibitors |
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2006
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- 2006-05-04 US US11/418,338 patent/US20060251723A1/en not_active Abandoned
- 2006-05-04 PL PL06769997T patent/PL1885339T3/pl unknown
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- 2006-05-04 WO PCT/US2006/017073 patent/WO2006121742A2/en active Application Filing
- 2006-05-04 HU HUE06769997A patent/HUE026040T2/en unknown
- 2006-05-04 SI SI200631971T patent/SI1885339T1/sl unknown
- 2006-05-04 AR ARP060101816A patent/AR054445A1/es not_active Application Discontinuation
- 2006-05-04 RS RS20150635A patent/RS54258B1/en unknown
- 2006-05-04 JP JP2008510188A patent/JP5173794B2/ja active Active
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CN101170996A (zh) | 2008-04-30 |
GEP20104927B (en) | 2010-03-25 |
SI1885339T1 (sl) | 2015-10-30 |
AR054445A1 (es) | 2007-06-27 |
CN102813655A (zh) | 2012-12-12 |
ES2546847T3 (es) | 2015-09-29 |
HRP20151051T1 (hr) | 2015-11-06 |
PE20061373A1 (es) | 2006-12-15 |
DK1885339T3 (en) | 2015-10-19 |
PT1885339E (pt) | 2015-10-12 |
WO2006121742A2 (en) | 2006-11-16 |
HUE026040T2 (en) | 2016-05-30 |
TW200716117A (en) | 2007-05-01 |
EP1885339A2 (en) | 2008-02-13 |
JP2008540440A (ja) | 2008-11-20 |
RS54258B1 (en) | 2016-02-29 |
NO20075154L (no) | 2008-02-01 |
WO2006121742A3 (en) | 2007-02-22 |
NO343939B1 (no) | 2019-07-15 |
US20060251723A1 (en) | 2006-11-09 |
US20130122093A1 (en) | 2013-05-16 |
TWI386205B (zh) | 2013-02-21 |
EP1885339B1 (en) | 2015-07-29 |
PL1885339T3 (pl) | 2015-12-31 |
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