JP2009502804A5 - - Google Patents
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- Publication number
- JP2009502804A5 JP2009502804A5 JP2008522965A JP2008522965A JP2009502804A5 JP 2009502804 A5 JP2009502804 A5 JP 2009502804A5 JP 2008522965 A JP2008522965 A JP 2008522965A JP 2008522965 A JP2008522965 A JP 2008522965A JP 2009502804 A5 JP2009502804 A5 JP 2009502804A5
- Authority
- JP
- Japan
- Prior art keywords
- sulfate
- single crystal
- pharmaceutical composition
- crystal form
- salt
- 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.)
- Pending
Links
- 239000013078 crystal Substances 0.000 claims 35
- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 22
- -1 4-isopropoxyphenyl Chemical group 0.000 claims 12
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 11
- 238000000634 powder X-ray diffraction Methods 0.000 claims 11
- QHDLEBMYVJYICY-UHFFFAOYSA-N 4-[6-methoxy-7-(3-piperidin-1-ylpropoxy)quinazolin-4-yl]piperazine-1-carboxylic acid Chemical compound COC1=CC2=C(N3CCN(CC3)C(O)=O)N=CN=C2C=C1OCCCN1CCCCC1 QHDLEBMYVJYICY-UHFFFAOYSA-N 0.000 claims 8
- 238000000034 method Methods 0.000 claims 7
- 239000003937 drug carrier Substances 0.000 claims 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 6
- 238000002844 melting Methods 0.000 claims 5
- 230000008018 melting Effects 0.000 claims 5
- UXXQOJXBIDBUAC-UHFFFAOYSA-N tandutinib Chemical compound COC1=CC2=C(N3CCN(CC3)C(=O)NC=3C=CC(OC(C)C)=CC=3)N=CN=C2C=C1OCCCN1CCCCC1 UXXQOJXBIDBUAC-UHFFFAOYSA-N 0.000 claims 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 4
- 238000000113 differential scanning calorimetry Methods 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 230000036571 hydration Effects 0.000 claims 4
- 238000006703 hydration reaction Methods 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- CBXWGGFGZDVPNV-UHFFFAOYSA-N so4-so4 Chemical compound OS(O)(=O)=O.OS(O)(=O)=O CBXWGGFGZDVPNV-UHFFFAOYSA-N 0.000 claims 4
- 230000007704 transition Effects 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical class OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 3
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 2
- 229920000881 Modified starch Polymers 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 2
- 229930006000 Sucrose Natural products 0.000 claims 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 2
- 239000008108 microcrystalline cellulose Substances 0.000 claims 2
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 2
- 239000000377 silicon dioxide Substances 0.000 claims 2
- 235000012239 silicon dioxide Nutrition 0.000 claims 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 2
- 239000005720 sucrose Substances 0.000 claims 2
- FSPQCTGGIANIJZ-UHFFFAOYSA-N 2-[[(3,4-dimethoxyphenyl)-oxomethyl]amino]-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide Chemical compound C1=C(OC)C(OC)=CC=C1C(=O)NC1=C(C(N)=O)C(CCCC2)=C2S1 FSPQCTGGIANIJZ-UHFFFAOYSA-N 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000032612 Glial tumor Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 102100020718 Receptor-type tyrosine-protein kinase FLT3 Human genes 0.000 claims 1
- 101710151245 Receptor-type tyrosine-protein kinase FLT3 Proteins 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- JRKICGRDRMAZLK-UHFFFAOYSA-L peroxydisulfate Chemical compound [O-]S(=O)(=O)OOS([O-])(=O)=O JRKICGRDRMAZLK-UHFFFAOYSA-L 0.000 claims 1
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 1
- 238000009490 roller compaction Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US70092605P | 2005-07-20 | 2005-07-20 | |
| PCT/US2006/028231 WO2007012042A1 (en) | 2005-07-20 | 2006-07-20 | New crystal forms of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2009502804A JP2009502804A (ja) | 2009-01-29 |
| JP2009502804A5 true JP2009502804A5 (enExample) | 2009-08-27 |
Family
ID=37188923
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008522965A Pending JP2009502804A (ja) | 2005-07-20 | 2006-07-20 | ４−［６−メトキシ−７−（３−ピペリジン−１−イル−プロポキシ）キナゾリン−４−イル］ピペラジン−１−カルボン酸（４−イソプロポキシフェニル）−アミドの新規な結晶形 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20100179162A1 (enExample) |
| EP (1) | EP1904459A1 (enExample) |
| JP (1) | JP2009502804A (enExample) |
| CN (1) | CN101208310A (enExample) |
| AU (1) | AU2006269917A1 (enExample) |
| CA (1) | CA2612459A1 (enExample) |
| WO (1) | WO2007012042A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100273808A1 (en) * | 2008-11-21 | 2010-10-28 | Millennium Pharmaceticals, Inc. | Lactate salt of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid(4-isopropoxyphenyl)-amide and pharmaceutical compositions thereof for the treatment of cancer and other diseases or disorders |
| JP2014513044A (ja) * | 2011-02-10 | 2014-05-29 | マイラン ラボラトリーズ リミテッド | ホスアンプレナビルカルシウム結晶およびその調製方法 |
| WO2015009889A1 (en) | 2013-07-18 | 2015-01-22 | Concert Pharmaceuticals, Inc. | Deuterated intedanib derivatives and their use for the treatment of proliferative disorders |
| CN109549941A (zh) * | 2017-09-26 | 2019-04-02 | 广西梧州制药（集团）股份有限公司 | 一种吡唑并嘧啶衍生物在制备治疗疾病药物方面的用途 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US642376A (en) * | 1898-10-24 | 1900-01-30 | John W Skilton | Car-axle box. |
| WO1998014431A1 (en) * | 1996-10-01 | 1998-04-09 | Kyowa Hakko Kogyo Co., Ltd. | Nitrogenous heterocyclic compounds |
| JP3011904B2 (ja) * | 1997-06-10 | 2000-02-21 | 明久 井上 | 金属ガラスの製造方法および装置 |
| EP1309568B1 (en) * | 2000-08-18 | 2011-02-16 | Millennium Pharmaceuticals, Inc. | [(quinazolin-4-yl)piperazin-4-yl]thiocarboxamide compounds as inhibitors of the phosphorylation of a PDGF receptor |
| MXPA03001359A (es) * | 2000-08-18 | 2004-12-13 | Millennium Pharm Inc | Derivados de quinazolina como inhibidores de cinasa. |
| WO2002016362A2 (en) * | 2000-08-18 | 2002-02-28 | Cor Therapeutics, Inc. | Nitrogenous heterocyclic compounds |
| ATE502928T1 (de) * | 2000-11-01 | 2011-04-15 | Millennium Pharm Inc | Stickstoffhaltige heterozyklische verbindungen und verfahren zu deren herstellung |
| US20040259881A1 (en) * | 2001-02-02 | 2004-12-23 | Anjali Pandey | Nitrogenous heterocyclic compounds |
| AU2002254152A1 (en) * | 2001-03-08 | 2002-09-24 | Millennium Pharmaceuticals | (homo) piperazine substituted quinolines for inhibiting the phosphorylation of kinases |
| US7456189B2 (en) * | 2003-09-30 | 2008-11-25 | Boehringer Ingelheim International Gmbh | Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation |
-
2006
- 2006-07-20 WO PCT/US2006/028231 patent/WO2007012042A1/en not_active Ceased
- 2006-07-20 EP EP06788010A patent/EP1904459A1/en not_active Withdrawn
- 2006-07-20 CA CA002612459A patent/CA2612459A1/en not_active Abandoned
- 2006-07-20 AU AU2006269917A patent/AU2006269917A1/en not_active Abandoned
- 2006-07-20 US US11/988,956 patent/US20100179162A1/en not_active Abandoned
- 2006-07-20 JP JP2008522965A patent/JP2009502804A/ja active Pending
- 2006-07-20 CN CNA2006800232271A patent/CN101208310A/zh active Pending
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