JP2015511963A - Torキナーゼ阻害剤を用いた癌の治療 - Google Patents

Torキナーゼ阻害剤を用いた癌の治療 Download PDF

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Publication number
JP2015511963A
JP2015511963A JP2015500593A JP2015500593A JP2015511963A JP 2015511963 A JP2015511963 A JP 2015511963A JP 2015500593 A JP2015500593 A JP 2015500593A JP 2015500593 A JP2015500593 A JP 2015500593A JP 2015511963 A JP2015511963 A JP 2015511963A
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Japan
Prior art keywords
substituted
unsubstituted
pyrazin
breast cancer
tor kinase
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Pending
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JP2015500593A
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English (en)
Japanese (ja)
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JP2015511963A5 (cg-RX-API-DMAC7.html
Inventor
シュ,スイチャン
ヘゲ,クリステン,マエ
レイモン,ヘザー
ナーラ,ラマ,ケイ.
Original Assignee
シグナル ファーマシューティカルズ,エルエルシー
シグナル ファーマシューティカルズ,エルエルシー
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Publication of JP2015511963A publication Critical patent/JP2015511963A/ja
Publication of JP2015511963A5 publication Critical patent/JP2015511963A5/ja
Pending legal-status Critical Current

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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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Reproductive Health (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Investigating Or Analysing Biological Materials (AREA)
  • Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
JP2015500593A 2012-03-15 2013-03-14 Torキナーゼ阻害剤を用いた癌の治療 Pending JP2015511963A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261611374P 2012-03-15 2012-03-15
US61/611,374 2012-03-15
US201261715331P 2012-10-18 2012-10-18
US61/715,331 2012-10-18
PCT/US2013/031185 WO2013138553A1 (en) 2012-03-15 2013-03-14 Treatment of cancer with tor kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017218014A Division JP6470820B2 (ja) 2012-03-15 2017-11-13 Torキナーゼ阻害剤を用いた癌の治療

Publications (2)

Publication Number Publication Date
JP2015511963A true JP2015511963A (ja) 2015-04-23
JP2015511963A5 JP2015511963A5 (cg-RX-API-DMAC7.html) 2016-04-21

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JP2015500593A Pending JP2015511963A (ja) 2012-03-15 2013-03-14 Torキナーゼ阻害剤を用いた癌の治療
JP2017218014A Active JP6470820B2 (ja) 2012-03-15 2017-11-13 Torキナーゼ阻害剤を用いた癌の治療

Family Applications After (1)

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JP2017218014A Active JP6470820B2 (ja) 2012-03-15 2017-11-13 Torキナーゼ阻害剤を用いた癌の治療

Country Status (19)

Country Link
US (2) US20130245027A1 (cg-RX-API-DMAC7.html)
EP (1) EP2825169B1 (cg-RX-API-DMAC7.html)
JP (2) JP2015511963A (cg-RX-API-DMAC7.html)
KR (1) KR102057359B1 (cg-RX-API-DMAC7.html)
CN (1) CN104271139A (cg-RX-API-DMAC7.html)
AU (1) AU2013202993B2 (cg-RX-API-DMAC7.html)
BR (1) BR112014022707A2 (cg-RX-API-DMAC7.html)
CA (1) CA2867348A1 (cg-RX-API-DMAC7.html)
ES (1) ES2678250T3 (cg-RX-API-DMAC7.html)
IL (1) IL234641B (cg-RX-API-DMAC7.html)
MX (1) MX360880B (cg-RX-API-DMAC7.html)
MY (1) MY178012A (cg-RX-API-DMAC7.html)
NI (1) NI201400112A (cg-RX-API-DMAC7.html)
NZ (1) NZ628407A (cg-RX-API-DMAC7.html)
PH (1) PH12014502046B1 (cg-RX-API-DMAC7.html)
SG (1) SG11201405724RA (cg-RX-API-DMAC7.html)
TW (1) TWI635862B (cg-RX-API-DMAC7.html)
WO (1) WO2013138553A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201406701B (cg-RX-API-DMAC7.html)

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AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
EP3549940A1 (en) 2013-04-17 2019-10-09 Signal Pharmaceuticals, LLC Pharmaceutical formulations, of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl) pyridin-3-yl) -3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one
MY189663A (en) 2013-04-17 2022-02-23 Signal Pharm Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
WO2014172436A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a 5-substituted quinazolinone compound for treating cancer
JP6382946B2 (ja) 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
CA2908742C (en) * 2013-04-17 2021-06-01 Signal Pharmaceuticals, Llc Combination therapy comprising a tor kinase inhibitor and a cytidine analog for treating cancer
WO2014172425A1 (en) 2013-04-17 2014-10-23 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
CN107474051B (zh) 2013-05-29 2020-10-30 西格诺药品有限公司 二氢吡嗪并吡嗪化合物的药物组合物、其固体形式和它们的用途
NZ714742A (en) 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
WO2015160880A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 1-ETHYL-7-(2-METHYL-6-(1H-1,2,4-TRIAZOL-3-YL) PYRIDIN-3-YL)-3,4-DIHYDROPYRAZINO(2,3-b)PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, and a coformer, compositions and methods of use thereof
IL271491B2 (en) 2017-06-22 2023-09-01 Celgene Corp Treatment of carcinoma of the liver characterized by hepatitis b virus infection
CN112933088B (zh) * 2021-02-03 2022-02-22 南华大学附属第一医院 Y041-5921在制备抗肿瘤药物中的应用

Citations (1)

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WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway

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ES2627352T3 (es) 2006-10-19 2017-07-27 Signal Pharmaceuticals, Llc Compuestos heteroarilo, sus composiciones y su uso como inhibidores de proteínas quinasas
RU2474582C2 (ru) 2006-10-19 2013-02-10 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Гетероарильные соединения, их композиции и их применение в качестве ингибиторов протеинкиназы
CA2721072A1 (en) * 2008-04-11 2009-10-15 Bionovo, Inc. Anticancer methods employing extracts of gleditsia sinensis lam
WO2010022243A1 (en) * 2008-08-20 2010-02-25 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Chemoprevention of head and neck squamous cell carcinomas
NZ599549A (en) 2009-10-26 2013-11-29 Signal Pharm Llc Methods of synthesis and purification of heteroaryl compounds

Patent Citations (1)

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WO2010062571A1 (en) * 2008-10-27 2010-06-03 Signal Pharmaceuticals, Llc Mtor kinase inhibitors for oncology indications and diseases associated with the mtor/p13k/akt pathway

Non-Patent Citations (8)

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CHANG SB, ET AL.: "Rapamycin inhibits proliferation of estrogen-receptor-positive breast cancer cells", JOURNAL OF SURGICAL RESEARCH, vol. 138, no. 1, JPN6016045363, 2007, pages 37 - 44, ISSN: 0003446553 *
DEY N, ET AL.: "Preclinical efficacy of a dual PI3K-mTOR inhibitor, BEZ235 in triple negative breast cancer", EUROPEAN JOURNAL OF CANCER, vol. Vol.47, Suppl.4, JPN6016045371, 2011, pages 17, ISSN: 0003446548 *
LEHMANN BD, ET AL.: "Identification of human triple-negative breast cancer subtypes and preclinical models for selection", THE JOURNAL OF CLINICAL INVESTIGATION, vol. 121, no. 7, JPN6016045362, July 2011 (2011-07-01), pages 2750 - 2767, ISSN: 0003446552 *
LIU T, ET AL.: "Combinatorial effects of lapatinib and rapamycin in triple-negative breast cancer cells", MOLECULAR CANCER THERAPEUTICS, vol. 10, no. 8, JPN6016045356, August 2011 (2011-08-01), pages 1460 - 1469, ISSN: 0003446550 *
YU K, ET AL.: "mTOR, a novel target in breast cancer: the effect of CCI-779, an mTOR inhibitor, in preclinical mode", ENDOCRINE-RELATED CANCER, vol. 8, no. 3, JPN6016045366, 2001, pages 249 - 258, ISSN: 0003446554 *
ZENG Q, ET AL.: "Treating triple-negative breast cancer by a combination of rapamycin and cyclophosphamide: an in viv", EUROPEAN JOURNAL OF CANCER, vol. 46, no. 6, JPN6016045359, 2010, pages 1132 - 1143, ISSN: 0003446551 *
ZHAO H, ET AL.: "The effect of mTOR inhibition alone or combined with MEK inhibitors on brain metastasis: an in vivo", BREAST CANCER RESEARCH AND TREATMENT, vol. 131, no. 2, JPN6016045353, 11 March 2012 (2012-03-11), pages 425 - 436, ISSN: 0003446549 *

Also Published As

Publication number Publication date
SG11201405724RA (en) 2014-10-30
US20130245027A1 (en) 2013-09-19
KR20140138951A (ko) 2014-12-04
NI201400112A (es) 2015-01-15
WO2013138553A1 (en) 2013-09-19
JP6470820B2 (ja) 2019-02-13
PH12014502046A1 (en) 2014-12-10
BR112014022707A2 (pt) 2020-10-27
KR102057359B1 (ko) 2019-12-18
IL234641A0 (en) 2014-11-30
IL234641B (en) 2020-04-30
ES2678250T3 (es) 2018-08-09
EP2825169A1 (en) 2015-01-21
MX360880B (es) 2018-11-21
MX2014011118A (es) 2015-04-08
JP2018052963A (ja) 2018-04-05
ZA201406701B (en) 2016-05-25
TWI635862B (zh) 2018-09-21
PH12014502046B1 (en) 2020-10-16
CA2867348A1 (en) 2013-09-19
AU2013202993A1 (en) 2013-10-03
MY178012A (en) 2020-09-29
NZ628407A (en) 2016-04-29
TW201343165A (zh) 2013-11-01
CN104271139A (zh) 2015-01-07
US20230338370A1 (en) 2023-10-26
AU2013202993B2 (en) 2015-09-03
EP2825169B1 (en) 2018-05-09
HK1201753A1 (en) 2015-09-11

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