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

Info

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
Authority
CN
China
Prior art keywords
amino
benzimidazol
fluoro
methylpiperazin
crystalline
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
CN200980108402.0A
Other languages
English (en)
Chinese (zh)
Other versions
CN101970425A (zh
Inventor
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
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
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=CN101970425(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 CN101970425A publication Critical patent/CN101970425A/zh
Application granted granted Critical
Publication of CN101970425B publication Critical patent/CN101970425B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

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)
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

Publications (2)

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

Family

ID=40622140

Family Applications (1)

Application Number Title Priority Date Filing Date
CN200980108402.0A Expired - Fee Related CN101970425B (zh) 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

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
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

Citations (3)

* Cited by examiner, † Cited by third party
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

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ304344B6 (cs) * 2000-09-11 2014-03-19 Novartis Vaccines & Diagnostics, Inc. Chinolinonový derivát a jeho použití a farmaceutický prostředek s obsahem tohoto derivátu
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
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
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)

* Cited by examiner, † Cited by third party
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
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
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
TWI426072B (zh) 2014-02-11
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

Similar Documents

Publication Publication Date Title
CN101970425B (zh) 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
EP3121171B1 (en) Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine
US11028069B2 (en) Salt of substituted piperidine compound
CN113840604A (zh) Jak2抑制剂的结晶形式
MXPA05009129A (es) Procedimiento para la produccion de sal acida de adicion de compuesto acido poliacido.
WO2026036924A1 (zh) 一种酪氨酸激酶抑制剂的可药用盐、晶体、制备方法及其用途
JP7750535B2 (ja) 化合物の結晶形態
CN111320596A (zh) 盐酸美呋哌瑞多晶型物及其制备方法
HK40003121A (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
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
CN106905294A (zh) 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法
HK1230180A1 (en) Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine
HK1230180B (en) Crystalline forms of 5-chloro-n2-(2-isopropoxy-5-methyl-4-piperidin-4-yl-phenyl)-n4[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20140416

Termination date: 20170318