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

Info

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
Authority
TW
Taiwan
Prior art keywords
cancer
leukemia
small cell
fluoro
amino
Prior art date
Application number
TW098108804A
Other languages
English (en)
Chinese (zh)
Other versions
TW201000463A (en
Inventor
Danielle Giron
Walter Hammerschmidt
Philippe Piechon
Johanne Polasek
Andreas Schreiner
Frank Stowasser
Original Assignee
Novartis Ag
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40622140&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TWI426072(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of TW201000463A publication Critical patent/TW201000463A/zh
Application granted granted Critical
Publication of TWI426072B publication Critical patent/TWI426072B/zh

Links

Classifications

    • 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

Landscapes

  • 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

Family

ID=40622140

Family Applications (1)

Application Number Title Priority Date Filing Date
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=)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
NZ567550A (en) * 2005-11-29 2011-08-26 Novartis Ag Formulations of lactic acid salts of 4-amino-5-fluoro-3-[6-(4-methyl-piperazin-1-yl)-1 H-benzimidazol-2-yl]1H-quinolin-2-one
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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
AU2009227003A1 (en) 2009-09-24
MY150554A (en) 2014-01-30
CN101970425B (zh) 2014-04-16
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

Similar Documents

Publication Publication Date Title
TWI426072B (zh) 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
EP2970123B2 (en) Crystalline dihydrochloride hydrate salt of omecamtiv mecarbil and process for its preparation
JP2024012540A (ja) B-rafキナーゼのマレイン酸塩、結晶形、調整方法、及びその使用
EP3453708A1 (en) Process for the preparation of 5-chloro-n-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n-2-(isopropylsulfonyl)phenyl)-2,4-diamine di-hydrochloride
EA031059B1 (ru) Кристаллическая форма альфа дималеата афатиниба
WO2016090257A1 (en) Salts and crystalline forms of 6-acetyl-8-cyclopentyl-5-methyl-2((5-(piperazin-1-yl)pyridin-2-yl)amino)pyrido[2,3-d] pyrimidin-7(8h)-one (palbociclib)
MXPA05009129A (es) Procedimiento para la produccion de sal acida de adicion de compuesto acido poliacido.
EP3271351A1 (en) Novel polymorphic form x of nilotinib dihydrochloride hydrate
EP3398946A1 (en) Salt of morpholine derivative and crystalline form thereof, as well as preparation method, pharmaceutical composition and use of the same
EP4438600A1 (en) Compound used as kinase inhibitor and use thereof
CN103664890A (zh) 喹啉衍生物的结晶及制备方法
JP7750535B2 (ja) 化合物の結晶形態
JP6532459B2 (ja) 3−[(3−{[4−(4−モルホリニルメチル)−1h−ピロール−2−イル]メチレン}−2−オキソ−2,3−ジヒドロ−1h−インドール−5−イル)メチル]−1,3−チアゾリジン−2,4−ジオンの新規塩、その調製及びそれを含有する製剤
JP7699054B2 (ja) フロピリミジン化合物の酸付加塩の結晶形
KR102918032B1 (ko) 트리사이클릭 유도체 화합물의 결정형 및 이의 제조방법및 이를 포함하는 약학적 조성물
EA050369B1 (ru) Кристаллическая форма трициклического производного соединения, способ его получения и содержащая его фармацевтическая композиция
TW202327593A (zh) Kras抑制劑的多晶型物及其製備方法和用途
HK1147492B (en) 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
HK1218544B (en) Salt of omecamtiv mecarbil and process for preparing salt

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees