CN101970425B - 4-氨基-5-氟-3-[5-(4-甲基哌嗪-1-基)-1h-苯并咪唑-2-基]喹啉-2(1h)-酮乳酸盐的结晶形式和两种溶剂化形式 - Google Patents

4-氨基-5-氟-3-[5-(4-甲基哌嗪-1-基)-1h-苯并咪唑-2-基]喹啉-2(1h)-酮乳酸盐的结晶形式和两种溶剂化形式 Download PDF

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Publication number
CN101970425B
CN101970425B CN200980108402.0A CN200980108402A CN101970425B CN 101970425 B CN101970425 B CN 101970425B CN 200980108402 A CN200980108402 A CN 200980108402A CN 101970425 B CN101970425 B CN 101970425B
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amino
benzimidazol
fluoro
methylpiperazin
crystalline
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CN101970425A (zh
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D·吉龙
W·哈默施密特
P·皮埃肖恩
J·波拉谢克
A·施赖纳
F·施托瓦塞尔
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Novartis AG
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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)
CN200980108402.0A 2008-03-19 2009-03-18 4-氨基-5-氟-3-[5-(4-甲基哌嗪-1-基)-1h-苯并咪唑-2-基]喹啉-2(1h)-酮乳酸盐的结晶形式和两种溶剂化形式 Expired - Fee Related CN101970425B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US3774608P 2008-03-19 2008-03-19
US61/037,746 2008-03-19
PCT/EP2009/053222 WO2009115562A2 (en) 2008-03-19 2009-03-18 Crystalline forms and two solvated forms of 4-amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1h-benzimidazol-2-yl]quinolin-2(1h)-one lactic acid salts

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CN101970425A CN101970425A (zh) 2011-02-09
CN101970425B true CN101970425B (zh) 2014-04-16

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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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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
CN102834094B (zh) 2010-04-16 2015-05-06 诺华有限公司 有机化合物的组合产品及其制药用途
BR112012026289A2 (pt) 2010-04-16 2016-07-12 Novartis Ag composto orgânico para uso no tratamento de câncer do fígado
AR081776A1 (es) * 2010-06-30 2012-10-17 Novartis Ag Composiciones farmaceuticas que comprenden monohidrato de lactato de 4-amino-5-fluoro-3-[6-(4-metil-piperazin-1-il)-1h-bencimidazol-2-il]-1h-quinolin-2-ona, proceso para la produccion de la composicion
AU2012229107A1 (en) 2011-03-17 2013-09-19 Novartis Ag FGFR and ligands thereof as biomarkers for breast cancer in HR positive subjects
MX2013013437A (es) 2011-05-19 2013-12-06 Novartis Ag 4-amino-5-fluoro-3- [6- (4-metil-piperazin-1-il) -1h-bencimidazol-2-il] -1h-quinolin-2-ona parea usarse en el tratamiento de un carcinoma adenoide quistico.
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
EP2809312A1 (en) 2012-01-31 2014-12-10 Novartis AG Combination of a rtk inhibitor with an anti - estrogen and use thereof for the treatment of cancer
IN2014DN10801A (https=) 2012-07-11 2015-09-04 Novartis Ag
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
PE20170255A1 (es) 2014-01-24 2017-03-22 Dana Farber Cancer Inst Inc Moleculas de anticuerpo que se unen a pd-1 y usos de las mismas
HUE045065T2 (hu) 2014-01-31 2019-12-30 Novartis Ag TIM-3 antitest molekulák és felhasználásaik
KR102442436B1 (ko) 2014-03-14 2022-09-15 노파르티스 아게 Lag-3에 대한 항체 분자 및 그의 용도
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
EP4245376A3 (en) 2014-10-14 2023-12-13 Novartis AG Antibody molecules to pd-l1 and uses thereof
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
EA035817B1 (ru) 2015-03-10 2020-08-14 Адуро Байотек, Инк. Композиции и способы для активации сигналинга, зависимого от "гена стимулятора интерферона"
HRP20211058T8 (hr) 2015-07-29 2021-11-26 Novartis Ag Kombinirane terapije koje sadrže molekule antitijela protiv lag-3
EP3878465A1 (en) 2015-07-29 2021-09-15 Novartis AG Combination therapies comprising antibody molecules to tim-3
EP3328418A1 (en) 2015-07-29 2018-06-06 Novartis AG Combination therapies comprising antibody molecules to pd-1
PE20181326A1 (es) 2015-11-03 2018-08-20 Janssen Biotech Inc Anticuerpos que se unen especificamente a pd-1 y sus usos
ES2986067T3 (es) 2015-12-17 2024-11-08 Novartis Ag Moléculas de anticuerpos frente a PD-1 y usos de las mismas
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS 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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CN1711088A (zh) * 2002-11-13 2005-12-21 希龙公司 治疗癌症的方法及相关方法
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
WO2007064719A2 (en) * 2005-11-29 2007-06-07 Novartis Ag Formulations of quinolinones

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DE60115069T2 (de) 2000-09-11 2006-08-03 Chiron Corp., Emeryville Chinolinonderivate als tyrosin-kinase inhibitoren
EP1539754A4 (en) 2002-08-23 2009-02-25 Novartis Vaccines & Diagnostic BENZIMIDAZOCHINOLINONE AND ITS USE
US20050256157A1 (en) 2002-08-23 2005-11-17 Chiron Corporation Combination therapy with CHK1 inhibitors
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
SG148864A1 (en) 2002-11-13 2009-01-29 Chiron Corp Methods of treating cancer and related methods
US20050209247A1 (en) * 2003-11-07 2005-09-22 Chiron Corporation Pharmaceutically acceptable salts of quinolinone compounds having improved pharmaceutical properties
EP1718306A2 (en) * 2004-02-20 2006-11-08 Chiron Corporation Modulation of inflammatory and metastatic processes
EP2301546B1 (en) * 2005-01-27 2014-09-10 Novartis AG Treatment of metastasized tumors
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

Patent Citations (3)

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Publication number Priority date Publication date Assignee Title
CN1711088A (zh) * 2002-11-13 2005-12-21 希龙公司 治疗癌症的方法及相关方法
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
WO2007064719A2 (en) * 2005-11-29 2007-06-07 Novartis Ag Formulations of quinolinones

Also Published As

Publication number Publication date
NZ600887A (en) 2013-10-25
PE20091628A1 (es) 2009-11-19
PH12012502568A1 (en) 2014-10-27
NZ587829A (en) 2012-08-31
WO2009115562A3 (en) 2009-11-26
KR20100137517A (ko) 2010-12-30
RU2497820C2 (ru) 2013-11-10
CO6321253A2 (es) 2011-09-20
US8563556B2 (en) 2013-10-22
EP2257544B1 (en) 2014-12-03
TW201000463A (en) 2010-01-01
JP2011515370A (ja) 2011-05-19
CA2718076A1 (en) 2009-09-24
AU2009227003B2 (en) 2013-03-14
RU2010142396A (ru) 2012-04-27
PH12012502569A1 (en) 2015-09-21
BRPI0909762A2 (pt) 2018-04-03
CL2009000651A1 (es) 2010-07-19
AR070924A1 (es) 2010-05-12
US20110021536A1 (en) 2011-01-27
TWI426072B (zh) 2014-02-11
AU2009227003A1 (en) 2009-09-24
MY150554A (en) 2014-01-30
HK1147492A1 (en) 2011-08-12
SG188919A1 (en) 2013-04-30
CN101970425A (zh) 2011-02-09
IL208020A0 (en) 2010-12-30
ZA201006263B (en) 2011-05-25
MA32230B1 (fr) 2011-04-01
EP2257544A2 (en) 2010-12-08
MX2010010152A (es) 2010-10-25
ECSP10010555A (es) 2010-11-30
WO2009115562A2 (en) 2009-09-24

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