TWI426072B - ４－胺基－５－氟－３－〔５－（４－甲基哌嗪－１－基）－１ｈ－苯并咪唑－２－基〕喹啉－２（１ｈ）－酮乳酸鹽之結晶型及兩種溶合物型 - Google Patents

４－胺基－５－氟－３－〔５－（４－甲基哌嗪－１－基）－１ｈ－苯并咪唑－２－基〕喹啉－２（１ｈ）－酮乳酸鹽之結晶型及兩種溶合物型 Download PDF

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Publication number
TWI426072B
TWI426072B TW098108804A TW98108804A TWI426072B TW I426072 B TWI426072 B TW I426072B TW 098108804 A TW098108804 A TW 098108804A TW 98108804 A TW98108804 A TW 98108804A TW I426072 B TWI426072 B TW I426072B
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Taiwan
Prior art keywords
cancer
leukemia
small cell
fluoro
amino
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TW098108804A
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English (en)
Chinese (zh)
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TW201000463A (en
Inventor
Danielle Giron
Walter Hammerschmidt
Philippe Piechon
Johanne Polasek
Andreas Schreiner
Frank Stowasser
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Novartis Ag
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Publication of TW201000463A publication Critical patent/TW201000463A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
TW098108804A 2008-03-19 2009-03-18 ４－胺基－５－氟－３－〔５－（４－甲基哌嗪－１－基）－１ｈ－苯并咪唑－２－基〕喹啉－２（１ｈ）－酮乳酸鹽之結晶型及兩種溶合物型 TWI426072B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3774608P 2008-03-19 2008-03-19

Publications (2)

Publication Number Publication Date
TW201000463A TW201000463A (en) 2010-01-01
TWI426072B true TWI426072B (zh) 2014-02-11

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ID=40622140

Family Applications (1)

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TW098108804A TWI426072B (zh) 2008-03-19 2009-03-18 ４－胺基－５－氟－３－〔５－（４－甲基哌嗪－１－基）－１ｈ－苯并咪唑－２－基〕喹啉－２（１ｈ）－酮乳酸鹽之結晶型及兩種溶合物型

Country Status (24)

Country Link
US (1) US8563556B2 (https=)
EP (1) EP2257544B1 (https=)
JP (1) JP2011515370A (https=)
KR (1) KR20100137517A (https=)
CN (1) CN101970425B (https=)
AR (1) AR070924A1 (https=)
AU (1) AU2009227003B2 (https=)
BR (1) BRPI0909762A2 (https=)
CA (1) CA2718076A1 (https=)
CL (1) CL2009000651A1 (https=)
CO (1) CO6321253A2 (https=)
EC (1) ECSP10010555A (https=)
IL (1) IL208020A0 (https=)
MA (1) MA32230B1 (https=)
MX (1) MX2010010152A (https=)
MY (1) MY150554A (https=)
NZ (2) NZ600887A (https=)
PE (1) PE20091628A1 (https=)
PH (2) PH12012502568A1 (https=)
RU (1) RU2497820C2 (https=)
SG (1) SG188919A1 (https=)
TW (1) TWI426072B (https=)
WO (1) WO2009115562A2 (https=)
ZA (1) ZA201006263B (https=)

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ES2707625T3 (es) 2010-04-16 2019-04-04 Novartis Ag Compuesto orgánico para su utilización en el tratamiento del cáncer de hígado
NZ602807A (en) 2010-04-16 2014-02-28 Novartis Ag 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one and an mtor inhibitor
UY33472A (es) * 2010-06-30 2012-01-31 Novartis Ag ?composiciones farmacéuticas que comprenden monohidrato de lactato de 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1hbencimidazol-2-il]-1h-quinolin-2-ona?.
WO2012125812A1 (en) 2011-03-17 2012-09-20 Novartis Ag Fgfr and ligands thereof as biomarkers for breast cancer in hr positive subjects
BR112013029246A2 (pt) 2011-05-19 2017-02-14 Novartis Ag 4-amino-5-flúor-3-[6- (4-metilpiperazin- 1 - il) - 1h - benzimidazol - 2 - il] - 1h - quinolin-2-ona para uso no tratamento de carcinoma adenoide cístico
JP2014526506A (ja) 2011-09-15 2014-10-06 ノバルティス アーゲー 中等度肝障害患者の癌治療における４−アミノ−５−フルオロ−３−［６−（４−メチルピペラジン−１−イル）−１ｈ−ベンゾイミダゾール−２−イル］−１ｈ−キノリン−２−オンの使用
WO2013063003A1 (en) 2011-10-28 2013-05-02 Novartis Ag Method of treating gastrointestinal stromal tumors
JP2015505562A (ja) 2012-01-31 2015-02-23 ノバルティス アーゲー Ｒｔｋ阻害剤と抗エストロゲン剤との組合せ、およびがん治療のためのその使用
US20150202203A1 (en) 2012-07-11 2015-07-23 Novartis Ag Method of Treating Gastrointestinal Stromal Tumors
WO2014058785A1 (en) 2012-10-10 2014-04-17 Novartis Ag Combination therapy
EP2764866A1 (en) 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
SG10201900002QA (en) 2014-01-24 2019-02-27 Dana Farber Cancer Institue Inc Antibody molecules to pd-1 and uses thereof
EP3099717B1 (en) 2014-01-31 2019-03-27 Novartis AG Antibody molecules to tim-3 and uses thereof
US20150259420A1 (en) 2014-03-14 2015-09-17 Novartis Ag Antibody molecules to lag-3 and uses thereof
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
TWI716362B (zh) 2014-10-14 2021-01-21 瑞士商諾華公司 針對ｐｄ－ｌ１之抗體分子及其用途
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
HK1248603A1 (zh) 2015-03-10 2018-10-19 Aduro Biotech, Inc. 用於活化"干扰素基因的刺激剂"依懒性信号传导的组合物和方法
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
EP3370768B9 (en) 2015-11-03 2022-03-16 Janssen Biotech, Inc. Antibodies specifically binding pd-1 and their uses
WO2017106656A1 (en) 2015-12-17 2017-06-22 Novartis Ag Antibody molecules to pd-1 and uses thereof
WO2018009466A1 (en) 2016-07-05 2018-01-11 Aduro Biotech, Inc. Locked nucleic acid cyclic dinucleotide compounds and uses thereof
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies

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US7825132B2 (en) * 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
CA2496164C (en) * 2002-08-23 2010-11-09 Chiron Corporation Benzimidazole quinolinones and uses thereof
US20050256157A1 (en) * 2002-08-23 2005-11-17 Chiron Corporation Combination therapy with CHK1 inhibitors
AU2003290699B2 (en) 2002-11-13 2009-08-27 Novartis Vaccines And Diagnostics, Inc. Methods of treating cancer and related methods
CN100377709C (zh) * 2002-11-13 2008-04-02 希龙公司 受体酪氨酸激酶抑制剂的制药用途及相关检测方法
CN102225926A (zh) * 2003-11-07 2011-10-26 诺华疫苗和诊断公司 具有改进药物特性的喹啉酮类化合物的药学上可接受的盐
US7875624B2 (en) * 2004-02-20 2011-01-25 Novartis Vaccines And Diagnostics, Inc. Modulating and measuring cellular adhesion
KR101387985B1 (ko) * 2005-01-27 2014-04-25 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 전이 종양의 치료
RU2433826C2 (ru) * 2005-11-29 2011-11-20 Новартис Аг Композиции хинолинонов
PE20091628A1 (es) 2008-03-19 2009-11-19 Novartis Ag Formas cristalinas y dos formas solvatadas de sales de acido lactico de 4-amino-5-fluoro-3-[5-(4-metilpiperazin-1-il)-1h-benzimidazol-2-il]quinolin-2(1h)-ona
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme

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WO2006127926A2 (en) * 2005-05-23 2006-11-30 Novartis Ag Crystalline and other forms of 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]-1h-quinolin-2-one lactic acid salts

Also Published As

Publication number Publication date
NZ587829A (en) 2012-08-31
KR20100137517A (ko) 2010-12-30
WO2009115562A2 (en) 2009-09-24
EP2257544A2 (en) 2010-12-08
WO2009115562A3 (en) 2009-11-26
AU2009227003A1 (en) 2009-09-24
AR070924A1 (es) 2010-05-12
PH12012502569A1 (en) 2015-09-21
MA32230B1 (fr) 2011-04-01
MX2010010152A (es) 2010-10-25
RU2497820C2 (ru) 2013-11-10
CN101970425A (zh) 2011-02-09
TW201000463A (en) 2010-01-01
AU2009227003B2 (en) 2013-03-14
CO6321253A2 (es) 2011-09-20
ECSP10010555A (es) 2010-11-30
HK1147492A1 (en) 2011-08-12
IL208020A0 (en) 2010-12-30
NZ600887A (en) 2013-10-25
CN101970425B (zh) 2014-04-16
CA2718076A1 (en) 2009-09-24
CL2009000651A1 (es) 2010-07-19
JP2011515370A (ja) 2011-05-19
EP2257544B1 (en) 2014-12-03
ZA201006263B (en) 2011-05-25
US8563556B2 (en) 2013-10-22
US20110021536A1 (en) 2011-01-27
RU2010142396A (ru) 2012-04-27
PH12012502568A1 (en) 2014-10-27
PE20091628A1 (es) 2009-11-19
MY150554A (en) 2014-01-30
BRPI0909762A2 (pt) 2018-04-03
SG188919A1 (en) 2013-04-30

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