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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs 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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US (1) US8563556B2 (enExample)
EP (1) EP2257544B1 (enExample)
JP (1) JP2011515370A (enExample)
KR (1) KR20100137517A (enExample)
CN (1) CN101970425B (enExample)
AR (1) AR070924A1 (enExample)
AU (1) AU2009227003B2 (enExample)
BR (1) BRPI0909762A2 (enExample)
CA (1) CA2718076A1 (enExample)
CL (1) CL2009000651A1 (enExample)
CO (1) CO6321253A2 (enExample)
EC (1) ECSP10010555A (enExample)
IL (1) IL208020A0 (enExample)
MA (1) MA32230B1 (enExample)
MX (1) MX2010010152A (enExample)
MY (1) MY150554A (enExample)
NZ (2) NZ600887A (enExample)
PE (1) PE20091628A1 (enExample)
PH (2) PH12012502568A1 (enExample)
RU (1) RU2497820C2 (enExample)
SG (1) SG188919A1 (enExample)
TW (1) TWI426072B (enExample)
WO (1) WO2009115562A2 (enExample)
ZA (1) ZA201006263B (enExample)

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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
SG184311A1 (en) 2010-04-16 2012-11-29 Novartis Ag Combination of organic compounds
CA2793779A1 (en) 2010-04-16 2011-10-20 Novartis Ag Organic compound for use in the treatment of liver cancer
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
CN103429759A (zh) 2011-03-17 2013-12-04 诺华股份有限公司 Fgfr及其配体作为hr阳性对象中乳腺癌的生物标记
SG194445A1 (en) 2011-05-19 2013-12-30 Novartis Ag Method for treating adenoid cystic carcinoma
IN2014DN02060A (enExample) 2011-09-15 2015-05-15 Novartis Ag
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
AU2013289175A1 (en) 2012-07-11 2015-01-22 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
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
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
EA201790834A1 (ru) 2014-10-14 2018-01-31 Новартис Аг Молекулы антител к pd-l1 и их применение
WO2016100882A1 (en) 2014-12-19 2016-06-23 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"
US20180222982A1 (en) 2015-07-29 2018-08-09 Novartis Ag Combination therapies comprising antibody molecules to pd-1
ES2878188T3 (es) 2015-07-29 2021-11-18 Novartis Ag Terapias de combinación que comprenden moléculas de anticuerpos contra LAG-3
EP3316902A1 (en) 2015-07-29 2018-05-09 Novartis AG Combination therapies comprising antibody molecules to tim-3
MA43186B1 (fr) 2015-11-03 2022-03-31 Janssen Biotech Inc Anticorps se liant spécifiquement à pd-1 et leurs utilisations
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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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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DE60132937T2 (de) 2000-09-11 2009-02-12 Novartis Vaccines and Diagnostics, Inc., Emeryville Verfahren zur Herstellung von Benzimidazol-2-yl -Chinolinonderivaten
AU2003288899B2 (en) 2002-08-23 2009-09-03 Novartis Vaccines And Diagnostics, Inc. Benzimidazole quinolinones and uses thereof
US7825132B2 (en) 2002-08-23 2010-11-02 Novartis Vaccines And Diagnostics, Inc. Inhibition of FGFR3 and treatment of multiple myeloma
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
MXPA06004194A (es) * 2003-11-07 2006-06-28 Chiron Corp Inhibicion de fgfr3 y tratamiento de mieloma multiple.
RU2377988C2 (ru) * 2004-02-20 2010-01-10 Новартис Вэксинес Энд Дайэгностикс, Инк. Модуляция воспалительных и метастатических процессов
WO2006081445A2 (en) * 2005-01-27 2006-08-03 Novartis Vaccines And Diagnostics Inc. Treatment of metastasized tumors
US8268834B2 (en) 2008-03-19 2012-09-18 Novartis Ag Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme
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

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

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

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