AU2016238437B2 - Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide - Google Patents

Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide Download PDF

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AU2016238437B2
AU2016238437B2 AU2016238437A AU2016238437A AU2016238437B2 AU 2016238437 B2 AU2016238437 B2 AU 2016238437B2 AU 2016238437 A AU2016238437 A AU 2016238437A AU 2016238437 A AU2016238437 A AU 2016238437A AU 2016238437 B2 AU2016238437 B2 AU 2016238437B2
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methyl
particles
amino
citric acid
carboxamide
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AU2016238437A1 (en
Inventor
Nicole Buschmann
Robin Alec Fairhurst
Pascal Furet
Bo Han
Thomas Knoepfel
Catherine Leblanc
Lv LIAO
Robert Mah
Franck Mallet
Julie MARTZ
Can Wang
Jing XIONG
Xianglin ZHAO
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Novartis AG
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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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/235—Saturated compounds containing more than one carboxyl group
    • C07C59/245—Saturated compounds containing more than one carboxyl group containing hydroxy or O-metal groups
    • C07C59/265—Citric acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Neurology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
AU2016238437A 2015-03-25 2016-03-23 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2H)-carboxamide Active AU2016238437B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2019200936A AU2019200936A1 (en) 2015-03-25 2019-02-07 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7- formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8- naphthyridine-1(2H)-carboxamide

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/000202 2015-03-25
CN2015000202 2015-03-25
PCT/IB2016/051633 WO2016151500A1 (en) 2015-03-25 2016-03-23 Particles of n-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7-formyl-6-((4-methyl-2- oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8-naphthyridine-1(2h)-carboxamide

Related Child Applications (1)

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AU2019200936A Division AU2019200936A1 (en) 2015-03-25 2019-02-07 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7- formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8- naphthyridine-1(2H)-carboxamide

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AU2016238437A1 AU2016238437A1 (en) 2017-08-17
AU2016238437B2 true AU2016238437B2 (en) 2018-11-08

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AU2019200936A Abandoned AU2019200936A1 (en) 2015-03-25 2019-02-07 Particles of N-(5-cyano-4-((2-methoxyethyl)amino)pyridin-2-yl)-7- formyl-6-((4-methyl-2-oxopiperazin-1-yl)methyl)-3,4-dihydro-1,8- naphthyridine-1(2H)-carboxamide

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US (1) US9802917B2 (enExample)
EP (1) EP3274349B1 (enExample)
JP (1) JP6696995B2 (enExample)
KR (1) KR102606643B1 (enExample)
CN (1) CN107406448B (enExample)
AR (1) AR104060A1 (enExample)
AU (2) AU2016238437B2 (enExample)
CA (1) CA2977326C (enExample)
ES (1) ES2803028T3 (enExample)
MX (1) MX2017012293A (enExample)
PL (1) PL3274349T3 (enExample)
RU (1) RU2720456C2 (enExample)
TW (1) TWI699206B (enExample)
WO (1) WO2016151500A1 (enExample)

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ES2756748T3 (es) 2014-10-03 2020-04-27 Novartis Ag Uso de derivados de piridilo bicíclicos de anillo fusionado como inhibidores de fgfr4
CN113105454B (zh) * 2016-05-20 2022-10-11 江苏豪森药业集团有限公司 Fgfr4抑制剂、其制备方法和应用
CN107619388A (zh) 2016-07-13 2018-01-23 南京天印健华医药科技有限公司 作为fgfr抑制剂的杂环化合物
EP3691616A1 (en) * 2017-10-02 2020-08-12 Novartis AG Method for preparing a pharmaceutical product
CN110234649B (zh) * 2017-10-31 2021-10-15 江苏豪森药业集团有限公司 Fgfr4抑制剂的盐、晶体、制备方法及其用途
CN110225913B (zh) * 2017-10-31 2021-10-15 江苏豪森药业集团有限公司 Fgfr4抑制剂晶型及其制备方法
CN109745321B (zh) * 2017-11-08 2022-04-29 上海翰森生物医药科技有限公司 包含fgfr4抑制剂的药物组合物
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RU2720456C2 (ru) 2020-04-30
EP3274349A1 (en) 2018-01-31
CA2977326C (en) 2023-08-29
RU2017133243A (ru) 2019-04-05
BR112017016991A2 (pt) 2018-04-10
CN107406448B (zh) 2021-03-09
EP3274349B1 (en) 2020-04-22
CN107406448A (zh) 2017-11-28
JP6696995B2 (ja) 2020-05-20
ES2803028T3 (es) 2021-01-22
RU2017133243A3 (enExample) 2019-07-29
TW201641106A (zh) 2016-12-01
KR102606643B1 (ko) 2023-11-28
US9802917B2 (en) 2017-10-31
AU2016238437A1 (en) 2017-08-17
MX2017012293A (es) 2018-01-09
AR104060A1 (es) 2017-06-21
TWI699206B (zh) 2020-07-21
KR20170129758A (ko) 2017-11-27
CA2977326A1 (en) 2016-09-29
US20160304489A1 (en) 2016-10-20
AU2019200936A1 (en) 2019-02-28
WO2016151500A1 (en) 2016-09-29
JP2018509446A (ja) 2018-04-05
PL3274349T3 (pl) 2020-10-05

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