CA2661223A1 - 4-aminoquinazoline derivatives and methods of use thereof - Google Patents
4-aminoquinazoline derivatives and methods of use thereof Download PDFInfo
- Publication number
- CA2661223A1 CA2661223A1 CA002661223A CA2661223A CA2661223A1 CA 2661223 A1 CA2661223 A1 CA 2661223A1 CA 002661223 A CA002661223 A CA 002661223A CA 2661223 A CA2661223 A CA 2661223A CA 2661223 A1 CA2661223 A1 CA 2661223A1
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- compound
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- 238000000034 method Methods 0.000 title claims abstract description 73
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- CILBMBUYJCWATM-PYGJLNRPSA-N vinorelbine ditartrate Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O.OC(=O)[C@H](O)[C@@H](O)C(O)=O.C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC CILBMBUYJCWATM-PYGJLNRPSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
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| US83950306P | 2006-08-22 | 2006-08-22 | |
| US60/839,503 | 2006-08-22 | ||
| PCT/US2007/018655 WO2008024439A2 (en) | 2006-08-22 | 2007-08-22 | 4-aminoquinazoline derivatives and methods of use thereof |
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| CN (1) | CN101594870A (enExample) |
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| MX (1) | MX2009001814A (enExample) |
| WO (1) | WO2008024439A2 (enExample) |
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| WO2008024439A2 (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 |
| US7547781B2 (en) | 2006-09-11 | 2009-06-16 | Curis, Inc. | Quinazoline based EGFR inhibitors containing a zinc binding moiety |
| BRPI0715016A2 (pt) * | 2006-09-11 | 2013-05-28 | Curis Inc | composiÇço, composiÇço farmacÊutica, mÉtodo para tratar uma doenÇa ou distérbio relacionada com tirosina quinase de egfr em um individuo necessitando o mesmo, mÉtodo para tratar uma doenÇa mediada por hdac e mÉtodo para tratar doenÇas medidas tanto por tirosina quinase de egfr quanto hdac |
| 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 |
| JP2011516426A (ja) * | 2008-03-28 | 2011-05-26 | コンサート ファーマシューティカルズ インコーポレイテッド | キナゾリン誘導体および治療方法 |
| 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 |
| PL2328414T3 (pl) * | 2008-08-29 | 2014-05-30 | Concert Pharmaceuticals Inc | Podstawione pochodne triazolo-pirydazyny |
| US8541419B2 (en) * | 2008-09-02 | 2013-09-24 | Actimis Pharmaceuticals, Inc. | Isotopically enriched pyrimidin-5-yl acetic acid derivatives as CRTH2 antagonists |
| CA2736091A1 (en) * | 2008-09-03 | 2010-03-11 | Teva Pharmaceutical Industries Ltd. | 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 |
| US8916574B2 (en) | 2009-09-28 | 2014-12-23 | Qilu Pharmaceutical Co., Ltd. | 4-(substituted anilino)-quinazoline derivatives useful 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 |
| WO2012082337A2 (en) * | 2010-12-17 | 2012-06-21 | Glaxo Wellcome Manufacturing Pte Ltd | Combination |
| 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 |
| JP2020536855A (ja) * | 2017-09-26 | 2020-12-17 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | がんを治療するための組成物及び方法 |
| 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 |
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| EP0912559B1 (en) * | 1996-07-13 | 2002-11-06 | Glaxo Group Limited | Fused heterocyclic compounds as protein tyrosine kinase inhibitors |
| US6225318B1 (en) * | 1996-10-17 | 2001-05-01 | Pfizer Inc | 4-aminoquinazolone derivatives |
| GB9800569D0 (en) * | 1998-01-12 | 1998-03-11 | Glaxo Group Ltd | Heterocyclic compounds |
| US6440710B1 (en) * | 1998-12-10 | 2002-08-27 | The Scripps Research Institute | Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds |
| EP1104760B1 (en) * | 1999-12-03 | 2003-03-12 | Pfizer Products Inc. | Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents |
| 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 |
| JP2007510667A (ja) * | 2003-11-07 | 2007-04-26 | スミスクライン ビーチャム (コーク) リミテッド | 癌の治療法 |
| US20100063074A1 (en) * | 2004-06-03 | 2010-03-11 | Berger Mark S | Cancer Treatment Method |
| CA2569139A1 (en) * | 2004-06-04 | 2005-12-22 | Smithkline Beecham (Cork) Limited | Lapatinib with letrozole for use in a treatment of breast cancer |
| EP1765313A2 (en) * | 2004-06-24 | 2007-03-28 | Novartis Vaccines and Diagnostics, Inc. | Compounds for immunopotentiation |
| CA2624179A1 (en) * | 2005-10-06 | 2007-04-12 | 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 |
| US20110053964A1 (en) * | 2006-08-22 | 2011-03-03 | Roger Tung | 4-aminoquinazoline derivatives and methods of use thereof |
| WO2008024439A2 (en) * | 2006-08-22 | 2008-02-28 | Concert Pharmaceuticals Inc. | 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 WO PCT/US2007/018655 patent/WO2008024439A2/en not_active Ceased
- 2007-08-22 JP JP2009525631A patent/JP2010501572A/ja active Pending
- 2007-08-22 MX MX2009001814A patent/MX2009001814A/es active IP Right Grant
- 2007-08-22 CN CNA2007800393013A patent/CN101594870A/zh active Pending
- 2007-08-22 US US11/895,174 patent/US20080051422A1/en not_active Abandoned
- 2007-08-22 KR KR1020097005957A patent/KR20090042994A/ko not_active Ceased
- 2007-08-22 EP EP07811504A patent/EP2054063A4/en not_active Withdrawn
- 2007-08-22 CA CA002661223A patent/CA2661223A1/en not_active Abandoned
- 2007-08-22 AU AU2007288204A patent/AU2007288204A1/en not_active Abandoned
-
2010
- 2010-09-02 US US12/874,981 patent/US20110097320A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| MX2009001814A (es) | 2009-03-02 |
| US20110097320A1 (en) | 2011-04-28 |
| KR20090042994A (ko) | 2009-05-04 |
| EP2054063A2 (en) | 2009-05-06 |
| US20080051422A1 (en) | 2008-02-28 |
| WO2008024439A3 (en) | 2009-02-26 |
| CN101594870A (zh) | 2009-12-02 |
| WO2008024439A2 (en) | 2008-02-28 |
| EP2054063A4 (en) | 2010-10-27 |
| AU2007288204A1 (en) | 2008-02-28 |
| JP2010501572A (ja) | 2010-01-21 |
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| Date | Code | Title | Description |
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| EEER | Examination request | ||
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