JP5291345B2 - 癌治療法 - Google Patents
癌治療法 Download PDFInfo
- Publication number
- JP5291345B2 JP5291345B2 JP2007547043A JP2007547043A JP5291345B2 JP 5291345 B2 JP5291345 B2 JP 5291345B2 JP 2007547043 A JP2007547043 A JP 2007547043A JP 2007547043 A JP2007547043 A JP 2007547043A JP 5291345 B2 JP5291345 B2 JP 5291345B2
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- JP
- Japan
- Prior art keywords
- compound
- brain
- breast cancer
- cancer
- formula
- 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.)
- Expired - Fee Related
Links
- 0 *S(CCNCc1ccc(-c(cc2)cc3c2ncnc3NCc(cc2Cl)ccc2OCc2cccc(F)c2)[o]1)(=O)=O Chemical compound *S(CCNCc1ccc(-c(cc2)cc3c2ncnc3NCc(cc2Cl)ccc2OCc2cccc(F)c2)[o]1)(=O)=O 0.000 description 2
- VMBAUQZYJZISFO-UHFFFAOYSA-N Cc(cc1)ccc1S(=O)=O Chemical compound Cc(cc1)ccc1S(=O)=O VMBAUQZYJZISFO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/04—Antineoplastic agents specific for metastasis
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
Burstein J.C.,ら, Breast Cancer Res Treat., 82:S50-S51, 2003, Supp. 1, abstract 226 Bendell J.C.,ら, Cancer 97:2972-2977,2003 Weitzen R.,ら, Proc. Am. Soc. Clin. Oncol., 21:2002, abstract 1936 Wardley A.M.,ら, Proc. Am. Soc. Clin. Oncol., 21:2002, abstract 241 Heinrich B., Proc. Am. Soc. Clin. Oncol., 22: 2003, abstract 147 Hagemeister F. B.ら, Cancer 46:162-167, 1980 Bendell J. C.ら, Cancer 97:2972-2977, 2003 Wang M. L. H.ら, Am. J. Clin. Oncol. 24:421-424,2001 Cocconi G.ら, Cancer Invest. 8:327-334, 1990 Franciosi V.ら, Cancer 85:1599-1605, 1999 Zulkowski K.ら, J. Cancer Res. Clin. Oncol. 128:111-113,2001 Christodoulou C.ら, Ann. Oncol. 12:249-254, 2001 Potschkaら, Journal of Pharm. And Exp. Therapeutics 306(1):124-131, 2003 July Stewart D. J.ら, Am. J. Clin. Oncol. 11:152-158, 1988 Stewart D. J.ら, Cancer Res. 42:2472-2479 Grossi P. M.ら, Clin. Cancer Res. 9:5514-5520, 2003 Pestalozzi B. C.ら, J. Cin. Oncol. 18:2349-2351,2000 Lee Jun-Soo, International Assoc. for the Study of Lung Cancer, Baltimore, July 2004 Ceresoli G. L., Annals Oncol. 15:1042-1047 Steeg P., Third Int’l. Symp. On Translational Res. In Onc., Santa Barbara CA, Oct9-12, 2003 Steeg P.ら, Eur. J. Cancer 2(8):142, Sept 2004, abstract 468 Nagata Y.ら, Cancer Cell 6(2):117-127, 2004 Christianson T. A.ら, Cancer Research 58(22):5123-5129, 1998
本願発明の方法はまた、癌治療の他の治療法と共に用いられ得る。特に抗腫瘍療法において、上記したもの以外の他の化学療法剤、ホルモン剤、抗体および外科的治療および/または放射線治療との併用療法が想定される。抗腫瘍療法は、例えば2002年1月14日に出願された国際出願第PCT US 02/01130号に記載されており、この出願を参照により、抗腫瘍療法を開示した範囲に組み入れる。本願発明の併用療法は、少なくとも1つの式(I)の化合物の投与、および場合により他の抗腫瘍剤を含む他の治療薬の使用を含む。そのような薬剤の併用は一緒に、または別々に投与され得、そして別々に投与する場合には、同時に投与するか、または任意の順番で逐次的に、短時間間隔、長時間間隔の双方で投与することができる。式(I)の化合物および他の医薬活性物質の量、ならびに投与の相対的なタイミングは、所望の併用治療効果を得るために選択される。
(1)これらに限定されないが、パクリタキセル、およびその類似物であるドセタキセルなどのジテルペノイド;ビンブラスチン、ビンクリスチン、ビンデシン、およびビノレルビンなどのビンカアルカロイド;エトポシド、およびテニポシドなどのエピポドフィロトキシン;ゲムシタビン;カペシタビン;5-フルオロウラシル、およびフルオロデオキシウリジンなどのフルオロピリミジン;アロピリノール、フルデュラビン、メトトレキサート、クラドラビン、シタラビン、メルカプトプリン、およびチオグアミンなどの代謝拮抗薬;ならびに9-アミノカンプトセシン、イリノテカン、トポテカン、CPT-11、および7-(4-メチルピペラジノ-メチレン)-10,11-メチレンジオキシ-20-カンプトセシンの様々な光学形体などのカンプトセシン;を含む、細胞周期特異的な抗腫瘍剤。
L(リットル) mL(ミリリットル)
μL(マイクロリットル) psi(ポンド/平方インチ)
M(モル) mM(ミリモル)
N(規定) Kg(キログラム)
i.v.(静脈内) Hz(ヘルツ)
MHz(メガヘルツ) mol(モル)
mmol(ミリモル) RT(室温)
min(分) h(時間)
mp(融点) TLC(薄層クロマトグラフィー)
Tr(保持時間) RP(逆相)
DCM(ジクロロメタン) DCE(ジクロロエタン)
DMF(N,N−ジメチルホルムアミド) HOAc(酢酸)
TMSE(2−(トリメチルシリル)エチル) TMS(トリメチルシリル)
TIPS(トリイソプロピルシリル) TBS(t−ブチルジメチルシリル)
HPLC(高圧液体クロマトグラフィー)
THF(テトラヒドロフラン) DMSO(ジメチルスルホキシド)
EtOAc(酢酸エチル) DME(1,2−ジメトキシエタン)
EDTA エチレンジアミンテトラ酢酸
FBS ウシ胎仔血清
IMDM イスコフ改変ダルベッコ培地
PBS リン酸緩衝食塩水
RPMI Roswell Park Memorial Institute
RIPA緩衝液 *
RT 室温
*150mM NaCl、50mM Tris-HCl、pH7.5、0.25%(w/v)-デオキシコール酸、1%NP-40、5mMオルトバナジン酸ナトリウム、2mMフッ化ナトリウム、およびプロテアーゼ阻害薬カクテル。
現在進行中の臨床研究において、以前にトラスツズマブを用いて治療した、erbB-2が過剰発現した転移性乳癌から脳転移した患者に、毒性、病気の進行または退薬を主題として、1日2回、750mgのラパチニブを投与したか、もしくは投与し続けている。安全性および有効性の評価(独立評価)は、それぞれ2週間および4週間間隔で行うことになっていた。PETスキャンはベースライン時、1週目および8週目に、そしてMRIはベースライン時、8週目および16週目に行うことになっていた。
Claims (9)
- 乳癌がerbB-2を過剰発現している、請求項1に記載の組成物。
- 脳転移部位がerbB-2を過剰発現している、請求項1に記載の組成物。
- 乳癌がerbB-2を過剰発現している、請求項4に記載の組成物。
- 脳転移部位がerbB-2を過剰発現している、請求項4に記載の組成物。
- 乳癌がerbB-2を過剰発現している、請求項7に記載の組成物。
- 脳転移部位がerbB-2を過剰発現している、請求項8に記載の組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US63705204P | 2004-12-17 | 2004-12-17 | |
US60/637,052 | 2004-12-17 | ||
PCT/US2005/046350 WO2006066267A2 (en) | 2004-12-17 | 2005-12-16 | Cancer treatment method |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2008524258A JP2008524258A (ja) | 2008-07-10 |
JP5291345B2 true JP5291345B2 (ja) | 2013-09-18 |
Family
ID=36588668
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2007547043A Expired - Fee Related JP5291345B2 (ja) | 2004-12-17 | 2005-12-16 | 癌治療法 |
Country Status (14)
Country | Link |
---|---|
US (2) | US20080306097A1 (ja) |
EP (1) | EP1824492B1 (ja) |
JP (1) | JP5291345B2 (ja) |
KR (1) | KR20070107004A (ja) |
CN (1) | CN101083995A (ja) |
AU (1) | AU2005316238B2 (ja) |
ES (1) | ES2426007T3 (ja) |
IL (1) | IL183059A0 (ja) |
MX (1) | MX2007006043A (ja) |
NO (1) | NO20072631L (ja) |
NZ (1) | NZ555462A (ja) |
RU (1) | RU2007119432A (ja) |
WO (1) | WO2006066267A2 (ja) |
ZA (1) | ZA200705059B (ja) |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1906185A1 (en) * | 2006-09-26 | 2008-04-02 | ProteoSys AG | Use of at least one isoform of progesterone receptor membrane component 1 (PGRMC1) |
WO2009137714A2 (en) | 2008-05-07 | 2009-11-12 | Teva Pharmaceutical Industries Ltd. | Forms of lapatinib ditosylate and processes for preparation thereof |
EP2158913A1 (en) | 2008-08-25 | 2010-03-03 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[3-chhloro-4-[(3-fluorophenyl)methoxy]phenyl]6-(5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine |
EP2158912A1 (en) | 2008-08-25 | 2010-03-03 | Ratiopharm GmbH | Pharmaceutical composition comprising N-[3-chhloro-4-[3-fluorophenyl)methoxy)phenyl]6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine |
MX2011009498A (es) | 2009-03-11 | 2011-10-14 | Ardea Biosciences Inc | Combinaciones farmaceuticas que comprenden rdea119/bay 869766 para el tratamiento de canceres especificos. |
CN102146075B (zh) * | 2010-02-06 | 2014-04-02 | 浙江九洲药业股份有限公司 | 一种喹唑啉化合物的制备方法 |
US8710221B2 (en) | 2010-03-23 | 2014-04-29 | Scinopharm Taiwan, Ltd. | Process and intermediates for preparing lapatinib |
AU2011232219B2 (en) | 2010-03-23 | 2016-02-04 | Scinopharm Taiwan, Ltd. | Process and intermediates for preparing lapatinib |
CN102344444B (zh) * | 2010-07-23 | 2015-07-01 | 岑均达 | 光学纯喹唑啉类化合物 |
CN102344445B (zh) * | 2010-07-23 | 2015-11-25 | 岑均达 | 光学纯喹唑啉类化合物 |
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 |
CZ2012712A3 (cs) | 2012-10-17 | 2014-04-30 | Zentiva, K.S. | Nový způsob výroby klíčového intermediátu výroby lapatinibu |
CN106632276B (zh) * | 2015-10-28 | 2021-06-15 | 上海天慈生物谷生物工程有限公司 | 一种治疗乳腺癌药物的制备方法 |
Family Cites Families (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
RS49779B (sr) * | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
JP4458746B2 (ja) * | 2001-01-16 | 2010-04-28 | グラクソ グループ リミテッド | 癌の治療方法 |
US20090317383A1 (en) * | 2004-06-04 | 2009-12-24 | Berger Mark S | Cancer treatment method |
-
2005
- 2005-12-16 JP JP2007547043A patent/JP5291345B2/ja not_active Expired - Fee Related
- 2005-12-16 ES ES05854982T patent/ES2426007T3/es active Active
- 2005-12-16 KR KR1020077016268A patent/KR20070107004A/ko not_active Application Discontinuation
- 2005-12-16 RU RU2007119432/14A patent/RU2007119432A/ru not_active Application Discontinuation
- 2005-12-16 CN CNA2005800434300A patent/CN101083995A/zh active Pending
- 2005-12-16 MX MX2007006043A patent/MX2007006043A/es not_active Application Discontinuation
- 2005-12-16 AU AU2005316238A patent/AU2005316238B2/en not_active Ceased
- 2005-12-16 WO PCT/US2005/046350 patent/WO2006066267A2/en active Application Filing
- 2005-12-16 EP EP05854982.5A patent/EP1824492B1/en active Active
- 2005-12-16 NZ NZ555462A patent/NZ555462A/en not_active IP Right Cessation
- 2005-12-16 US US11/721,675 patent/US20080306097A1/en not_active Abandoned
-
2007
- 2007-05-08 IL IL183059A patent/IL183059A0/en unknown
- 2007-05-22 NO NO20072631A patent/NO20072631L/no not_active Application Discontinuation
- 2007-06-11 ZA ZA200705059A patent/ZA200705059B/xx unknown
-
2015
- 2015-04-20 US US14/690,917 patent/US20150283139A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
CN101083995A (zh) | 2007-12-05 |
EP1824492A4 (en) | 2009-10-28 |
RU2007119432A (ru) | 2009-01-27 |
WO2006066267A3 (en) | 2006-12-14 |
NZ555462A (en) | 2009-03-31 |
WO2006066267A2 (en) | 2006-06-22 |
KR20070107004A (ko) | 2007-11-06 |
NO20072631L (no) | 2007-07-02 |
EP1824492B1 (en) | 2013-07-10 |
IL183059A0 (en) | 2007-10-31 |
AU2005316238B2 (en) | 2009-05-07 |
MX2007006043A (es) | 2007-06-13 |
JP2008524258A (ja) | 2008-07-10 |
US20150283139A1 (en) | 2015-10-08 |
US20080306097A1 (en) | 2008-12-11 |
EP1824492A2 (en) | 2007-08-29 |
ZA200705059B (en) | 2009-09-30 |
AU2005316238A1 (en) | 2006-06-22 |
ES2426007T3 (es) | 2013-10-18 |
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