JP2010501572A5 - - Google Patents
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- Publication number
- JP2010501572A5 JP2010501572A5 JP2009525631A JP2009525631A JP2010501572A5 JP 2010501572 A5 JP2010501572 A5 JP 2010501572A5 JP 2009525631 A JP2009525631 A JP 2009525631A JP 2009525631 A JP2009525631 A JP 2009525631A JP 2010501572 A5 JP2010501572 A5 JP 2010501572A5
- Authority
- JP
- Japan
- Prior art keywords
- cancer
- compound according
- deuterium
- formulation
- composition
- 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
- 150000001875 compounds Chemical class 0.000 claims 10
- 229910052805 deuterium Chemical group 0.000 claims 8
- YZCKVEUIGOORGS-OUBTZVSYSA-N deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 7
- 239000000203 mixture Substances 0.000 claims 7
- 239000000969 carrier Substances 0.000 claims 3
- 238000009472 formulation Methods 0.000 claims 3
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 208000007276 Esophageal Squamous Cell Carcinoma Diseases 0.000 claims 1
- 206010017758 Gastric cancer Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 208000002409 Gliosarcoma Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029592 Non-Hodgkin's lymphomas Diseases 0.000 claims 1
- 208000002154 Non-Small-Cell Lung Carcinoma Diseases 0.000 claims 1
- 108009000071 Non-small cell lung cancer Proteins 0.000 claims 1
- 206010030137 Oesophageal adenocarcinoma Diseases 0.000 claims 1
- 206010061534 Oesophageal squamous cell carcinoma Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 208000008443 Pancreatic Carcinoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 125000004429 atoms Chemical group 0.000 claims 1
- 201000000053 blastoma Diseases 0.000 claims 1
- 201000000220 brain stem cancer Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atoms Chemical group C* 0.000 claims 1
- 201000007455 central nervous system cancer Diseases 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 201000011231 colorectal cancer Diseases 0.000 claims 1
- -1 deuterium compound Chemical class 0.000 claims 1
- 201000008184 embryoma Diseases 0.000 claims 1
- 230000002518 glial Effects 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 230000000155 isotopic Effects 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 239000002831 pharmacologic agent Substances 0.000 claims 1
- 230000000144 pharmacologic effect Effects 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000011780 sodium chloride Substances 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000005490 tosylate group Chemical class 0.000 claims 1
Claims (11)
- Y1a、Y1bおよびY1cが、同時に重水素である、請求項1に記載の化合物。
- Y2aおよびY2bが、同時に重水素である、請求項1または請求項2に記載の化合物。
- Y3aおよびY3bが、同時に重水素である、請求項1から請求項3のいずれか1項に記載の化合物。
- Y4aおよびY4bが、同時に重水素である、請求項1から請求項4のいずれか1項に記載の化合物。
- Y5aおよびY5bが、同時に重水素である、請求項1から請求項5のいずれか1項に記載の化合物。
- 重水素として指定されない任意の原子が、その天然の同位体存在量で存在する、請求項1から請求項7のいずれか1項に記載の化合物。
- 請求項1に記載の化合物と、許容できる担体とを含む、発熱物質を含まない組成物であって、前記組成物は薬理学的な投与のために処方されており、前記担体は薬理学的に許容できる担体である、発熱物質を含まない組成物。
- 乳癌、食道腺癌、食道扁平上皮癌、子宮頚癌、頭頚部癌、固形腫瘍、非ホジキンリンパ腫、胃癌、卵巣癌、腹膜癌、脳腫瘍および中枢神経系癌(神経膠腫、多形神経膠芽腫、膠肉腫)、前立腺癌、子宮内膜癌、結腸直腸癌、非小細胞肺癌、肝癌、腎癌、および膵癌を患っているか、またはこれらを起こしやすい状態にある被験体を治療するための製剤であって、請求項9に記載の組成物を含む、製剤。
- 前記被験体が乳癌を患っているか、またはこれらを起こしやすい状態にある、請求項10に記載の製剤。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US83950306P | 2006-08-22 | 2006-08-22 | |
PCT/US2007/018655 WO2008024439A2 (en) | 2006-08-22 | 2007-08-22 | 4-aminoquinazoline derivatives and methods of use thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2010501572A JP2010501572A (ja) | 2010-01-21 |
JP2010501572A5 true JP2010501572A5 (ja) | 2010-09-30 |
Family
ID=39107412
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2009525631A Pending JP2010501572A (ja) | 2006-08-22 | 2007-08-22 | 4−アミノキナゾリン誘導体およびその使用方法 |
Country Status (9)
Country | Link |
---|---|
US (2) | US20080051422A1 (ja) |
EP (1) | EP2054063A4 (ja) |
JP (1) | JP2010501572A (ja) |
KR (1) | KR20090042994A (ja) |
CN (1) | CN101594870A (ja) |
AU (1) | AU2007288204A1 (ja) |
CA (1) | CA2661223A1 (ja) |
MX (1) | MX2009001814A (ja) |
WO (1) | WO2008024439A2 (ja) |
Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20080051422A1 (en) * | 2006-08-22 | 2008-02-28 | Concert Pharmaceuticals Inc. | 4-Aminoquinazoline derivatives and methods of use thereof |
US20110053964A1 (en) * | 2006-08-22 | 2011-03-03 | Roger Tung | 4-aminoquinazoline derivatives and methods of use thereof |
SG174774A1 (en) | 2006-09-11 | 2011-10-28 | Curis Inc | Quinazoline based egfr inhibitors containing a zinc binding moiety |
US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
US8119616B2 (en) | 2007-09-10 | 2012-02-21 | Curis, Inc. | Formulation of quinazoline based EGFR inhibitors containing a zinc binding moiety |
US20090215802A1 (en) * | 2007-09-13 | 2009-08-27 | Protia, Llc | Deuterium-enriched lapatinib |
US8288397B2 (en) | 2007-12-17 | 2012-10-16 | Janssen Pharmaceutica Nv | Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1 |
WO2009121042A1 (en) * | 2008-03-28 | 2009-10-01 | Concert Pharmaceuticals, Inc. | Quinazoline derivatives and methods of treatment |
US8252805B2 (en) | 2008-05-07 | 2012-08-28 | Teva Pharmaceutical Industries Ltd. | Forms of lapatinib ditosylate and processes for preparation thereof |
US20100087459A1 (en) * | 2008-08-26 | 2010-04-08 | Leonid Metsger | Forms of lapatinib compounds and processes for the preparation thereof |
CN104098578A (zh) * | 2008-08-29 | 2014-10-15 | 康瑟特制药公司 | 取代的三唑并哒嗪衍生物 |
JP5586606B2 (ja) * | 2008-09-02 | 2014-09-10 | アクチミス ファーマシューティカルズ インコーポレーテッド | Crth2アンタゴニストとしての同位体富化されたピリミジン−5−イル酢酸誘導体 |
NZ591315A (en) * | 2008-09-03 | 2012-08-31 | Teva Pharma | 2-oxo-1,2-dihydro-quinoline modulators of immune function |
CN101735200B (zh) * | 2008-11-17 | 2013-01-02 | 岑均达 | 喹唑啉类化合物 |
US20110053968A1 (en) | 2009-06-09 | 2011-03-03 | Auspex Pharmaceuticals, Inc. | Aminopyrimidine inhibitors of tyrosine kinase |
EP2484678B1 (en) | 2009-09-28 | 2015-01-21 | Qilu Pharmaceutical Co., Ltd | 4-(substituted anilino)quinazoline derivatives as tyrosine kinase inhibitors |
US20110195066A1 (en) * | 2010-02-05 | 2011-08-11 | Auspex Pharmaceuticals, Inc. | Quinoline inhibitors of tyrosine kinase |
UY33226A (es) * | 2010-02-19 | 2011-09-30 | Novartis Ag | Compuestos de pirrolopirimidina deuterada como inhibidores de la cdk4/6 |
CN102453025B (zh) * | 2010-10-18 | 2014-08-13 | 齐鲁制药有限公司 | 拉帕替尼中间体晶型及其制备方法 |
EP2654754B1 (en) * | 2010-12-17 | 2016-12-21 | Novartis AG | Combination for treating osteosarcoma, rhabdomyosarcoma and neuroblastoma |
CN102321076B (zh) * | 2011-07-07 | 2013-08-21 | 中国科学技术大学 | 拉帕替尼中间体及其类似物的制备方法 |
CN102659764A (zh) * | 2012-04-16 | 2012-09-12 | 中国科学院广州生物医药与健康研究院 | 酪氨酸激酶不可逆抑制剂及其制备方法和用途 |
CZ2012712A3 (cs) | 2012-10-17 | 2014-04-30 | Zentiva, K.S. | Nový způsob výroby klíčového intermediátu výroby lapatinibu |
CN102911164A (zh) * | 2012-11-07 | 2013-02-06 | 江苏金桥盐化集团利海化工有限公司 | 一种拉帕替尼关键中间体的制备方法 |
ITVI20130003A1 (it) * | 2013-01-14 | 2014-07-14 | F I S Fabbrica Italiana Sint I S P A | Procedimento per la preparazione di lapatinib e suoi sali mediante nuovi intermedi. |
US9024023B2 (en) | 2013-01-14 | 2015-05-05 | F.I.S.—Fabbrica Italiana Sintetici S.p.A. | Efficient process for the preparation of lapatinib and salts thereof by means of new intermediates |
CN104513231A (zh) * | 2015-01-09 | 2015-04-15 | 安润医药科技(苏州)有限公司 | 拉帕替尼及其中间体的合成方法 |
GB201611580D0 (en) * | 2016-07-01 | 2016-08-17 | Aslan Pharmaceuticals Pte Ltd | Method |
AU2018341454B2 (en) * | 2017-09-26 | 2023-09-28 | The Regents Of The University Of California | Compositions and methods for treating cancer |
CN107827877B (zh) * | 2017-11-21 | 2021-05-07 | 陕西师范大学 | 二烷基氨基喹唑啉类化合物及其在制备抗肿瘤药物中的应用 |
CN108285421A (zh) * | 2018-01-26 | 2018-07-17 | 黑龙江鑫创生物科技开发有限公司 | 一种微通道反应器合成拉帕替尼中间体的方法 |
CN108187055B (zh) * | 2018-03-06 | 2019-12-27 | 北京大学 | 一种具有协同增效作用的抗癌组合物 |
CN108690001A (zh) * | 2018-06-26 | 2018-10-23 | 苏州市贝克生物科技有限公司 | 拉帕替尼类似物的合成 |
Family Cites Families (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6221335B1 (en) * | 1994-03-25 | 2001-04-24 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
JP4386967B2 (ja) * | 1996-07-13 | 2009-12-16 | グラクソ、グループ、リミテッド | プロテインチロシンキナーゼ阻害剤としての縮合複素環式化合物 |
US6225318B1 (en) * | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
RS49779B (sr) * | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
US6440710B1 (en) * | 1998-12-10 | 2002-08-27 | The Scripps Research Institute | Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds |
DK1104760T3 (da) * | 1999-12-03 | 2003-06-30 | Pfizer Prod Inc | Sulfamoylheteroarylpyrazolforbindelser som anti-inflammatoriske/analgetiske midler |
TW200413273A (en) * | 2002-11-15 | 2004-08-01 | Wako Pure Chem Ind Ltd | Heavy hydrogenation method of heterocyclic rings |
CA2534405A1 (en) * | 2003-08-08 | 2005-02-17 | Ulysses Pharmaceutical Products Inc. | Halogenated quinazolinyl nitrofurans as antibacterial agents |
WO2005046678A1 (en) * | 2003-11-07 | 2005-05-26 | Smithkline Beecham (Cork) Limited | Cancer treatment method |
MXPA06013635A (es) * | 2004-06-03 | 2007-02-28 | Smithkline Beecam Cork Ltd | Metodo para el tratamiento de cancer. |
WO2005120512A2 (en) * | 2004-06-04 | 2005-12-22 | Smithkline Beecham (Cork) Limited | Cancer treatment method |
EP2277595A3 (en) * | 2004-06-24 | 2011-09-28 | Novartis Vaccines and Diagnostics, Inc. | Compounds for immunopotentiation |
EP1934201A1 (en) * | 2005-10-06 | 2008-06-25 | Auspex Pharmaceuticals Inc. | Deuterated inhibitors of gastric h+, k+-atpase with enhanced therapeutic properties |
US7750168B2 (en) * | 2006-02-10 | 2010-07-06 | Sigma-Aldrich Co. | Stabilized deuteroborane-tetrahydrofuran complex |
US20080051422A1 (en) * | 2006-08-22 | 2008-02-28 | Concert Pharmaceuticals Inc. | 4-Aminoquinazoline derivatives and methods of use thereof |
US20110053964A1 (en) * | 2006-08-22 | 2011-03-03 | Roger Tung | 4-aminoquinazoline derivatives and methods of use thereof |
CA2661404A1 (en) * | 2006-09-05 | 2008-03-13 | Schering Corporation | Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis |
US20090215802A1 (en) * | 2007-09-13 | 2009-08-27 | Protia, Llc | Deuterium-enriched lapatinib |
WO2010005585A2 (en) * | 2008-07-09 | 2010-01-14 | Concert Pharmaceuticals Inc. | 4-aminoquinazoline prodrugs |
-
2007
- 2007-08-22 US US11/895,174 patent/US20080051422A1/en not_active Abandoned
- 2007-08-22 MX MX2009001814A patent/MX2009001814A/es active IP Right Grant
- 2007-08-22 KR KR1020097005957A patent/KR20090042994A/ko not_active Application Discontinuation
- 2007-08-22 AU AU2007288204A patent/AU2007288204A1/en not_active Abandoned
- 2007-08-22 CN CNA2007800393013A patent/CN101594870A/zh active Pending
- 2007-08-22 CA CA002661223A patent/CA2661223A1/en not_active Abandoned
- 2007-08-22 JP JP2009525631A patent/JP2010501572A/ja active Pending
- 2007-08-22 EP EP07811504A patent/EP2054063A4/en not_active Withdrawn
- 2007-08-22 WO PCT/US2007/018655 patent/WO2008024439A2/en active Application Filing
-
2010
- 2010-09-02 US US12/874,981 patent/US20110097320A1/en not_active Abandoned
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