AU2016248376B2 - Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore - Google Patents

Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore Download PDF

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Publication number
AU2016248376B2
AU2016248376B2 AU2016248376A AU2016248376A AU2016248376B2 AU 2016248376 B2 AU2016248376 B2 AU 2016248376B2 AU 2016248376 A AU2016248376 A AU 2016248376A AU 2016248376 A AU2016248376 A AU 2016248376A AU 2016248376 B2 AU2016248376 B2 AU 2016248376B2
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crystalline form
maleate
compound
cancer
salt
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AU2016248376A1 (en
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Guoliang Zhang
Changyou Zhou
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Beone Medicines I GmbH
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Beigene Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/4375Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/557Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • A61K31/5585Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes having five-membered rings containing oxygen as the only ring hetero atom, e.g. prostacyclin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/42Separation; Purification; Stabilisation; Use of additives
    • C07C51/43Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13Dicarboxylic acids
    • C07C57/145Maleic acid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
AU2016248376A 2015-04-15 2016-04-14 Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore Active AU2016248376B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN2015076639 2015-04-15
CNPCT/CN2015/076639 2015-04-15
PCT/CN2016/079251 WO2016165626A1 (en) 2015-04-15 2016-04-14 Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Publications (2)

Publication Number Publication Date
AU2016248376A1 AU2016248376A1 (en) 2017-10-12
AU2016248376B2 true AU2016248376B2 (en) 2020-10-08

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AU2016248376A Active AU2016248376B2 (en) 2015-04-15 2016-04-14 Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Country Status (15)

Country Link
US (1) US10351559B2 (cg-RX-API-DMAC7.html)
EP (2) EP3283486B1 (cg-RX-API-DMAC7.html)
JP (3) JP7320741B2 (cg-RX-API-DMAC7.html)
KR (2) KR20240049684A (cg-RX-API-DMAC7.html)
CN (2) CN107531682B (cg-RX-API-DMAC7.html)
AU (1) AU2016248376B2 (cg-RX-API-DMAC7.html)
CA (1) CA2981746C (cg-RX-API-DMAC7.html)
EA (1) EA035680B1 (cg-RX-API-DMAC7.html)
IL (2) IL255555B (cg-RX-API-DMAC7.html)
MX (1) MX381053B (cg-RX-API-DMAC7.html)
NZ (1) NZ735715A (cg-RX-API-DMAC7.html)
SG (1) SG11201707984TA (cg-RX-API-DMAC7.html)
TW (4) TWI792406B (cg-RX-API-DMAC7.html)
WO (1) WO2016165626A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201706392B (cg-RX-API-DMAC7.html)

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CA2609659C (en) 2005-05-26 2014-01-28 Neuron Systems, Inc. Azanaphthalenes, compositions and methods for treating retinal disease
CA2782015C (en) 2009-12-11 2020-08-25 Neuron Systems, Inc. Topical ophthalmic compositions and methods for the treatment of macular degeneration
CN103596926B (zh) 2011-12-31 2015-11-25 百济神州有限公司 作为raf激酶抑制剂的稠合三环化合物
AU2014209387B2 (en) 2013-01-23 2018-11-01 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
EP3283486B1 (en) 2015-04-15 2022-07-27 BeiGene, Ltd. Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
EP4400106A1 (en) 2015-08-21 2024-07-17 Aldeyra Therapeutics, Inc. Deuterated compounds and uses thereof
AU2017293423B2 (en) 2016-07-05 2023-05-25 Beone Medicines I Gmbh Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
DK3618875T3 (da) 2017-05-02 2023-07-10 Novartis Ag Kombinationsterapi omfattende en raf-inhibitor og trametinib
WO2019075136A1 (en) 2017-10-10 2019-04-18 Aldeyra Therapeutics, Inc. TREATMENT OF INFLAMMATORY DISORDERS
US12006298B2 (en) 2018-08-06 2024-06-11 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
MY202547A (en) * 2018-10-31 2024-05-07 Servier Lab Novel salt of a bcl-2 inhibitor, related crystalline form, method for preparing the same and pharmaceutical compositions containing the same
CN116715662A (zh) * 2019-01-25 2023-09-08 百济神州(北京)生物科技有限公司 无定形的b-raf激酶二聚体抑制剂
CN111484488A (zh) * 2019-01-25 2020-08-04 百济神州(北京)生物科技有限公司 一种b-raf激酶二聚体抑制剂的稳定结晶形式a
MX2021010829A (es) * 2019-03-15 2021-12-10 Forma Therapeutics Inc Inhibición de la proteína de unión al elemento de respuesta a adenosín monofosfato (amp) cíclica (creb).
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CN113784954A (zh) 2019-05-02 2021-12-10 奥尔德拉医疗公司 多晶型化合物和其用途
KR102881316B1 (ko) 2019-05-13 2025-11-05 노파르티스 아게 암 치료를 위한 raf 억제제로서의 n-(3-(2-(2-하이드록시에톡시)-6-모르폴리노피리딘-4-일)-4-메틸페닐)-2 (트리플루오로메틸)이소니코틴아미드의 새로운 결정질 형태
CN111184693B (zh) * 2019-05-29 2023-07-21 百济神州(苏州)生物科技有限公司 一种raf激酶抑制剂制剂及其制备方法
PE20231211A1 (es) * 2020-04-03 2023-08-17 Springworks Therapeutics Inc Administracion conjunta de mirdametinib y lifirafenib para uso en el tratamiento de canceres
CA3175856A1 (en) 2020-05-13 2021-11-18 Todd Brady Pharmaceutical formulations and uses thereof
JP2025519981A (ja) * 2022-06-08 2025-06-30 マップキュア,エルエルシー B-raf阻害剤によるがんの治療方法

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WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

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WO2006065703A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
CN101365682A (zh) * 2005-12-08 2009-02-11 千禧药品公司 具有激酶抑制活性的双环化合物
EP2021327B1 (en) 2006-05-15 2012-04-04 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
WO2008023239A1 (en) 2006-08-23 2008-02-28 Pfizer Products Inc. Pyrimidone compounds as gsk-3 inhibitors
WO2008030448A1 (en) 2006-09-07 2008-03-13 Millennium Pharmaceuticals, Inc. Phenethylamide derivatives with kinase inhibitory activity
AU2008247500A1 (en) 2007-05-04 2008-11-13 Irm Llc Compounds and compositions as c-kit and PDGFR kinase inhibitors
US20100197924A1 (en) 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
JP5808818B2 (ja) * 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー アファチニブの新規塩及び多形形態
EP3283486B1 (en) 2015-04-15 2022-07-27 BeiGene, Ltd. Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

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WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

Also Published As

Publication number Publication date
WO2016165626A1 (en) 2016-10-20
EP3283486B1 (en) 2022-07-27
IL287740B2 (en) 2025-11-01
US10351559B2 (en) 2019-07-16
CA2981746C (en) 2023-08-01
EA035680B1 (ru) 2020-07-24
AU2016248376A1 (en) 2017-10-12
JP2021073246A (ja) 2021-05-13
IL255555A (en) 2018-01-31
JP2018511634A (ja) 2018-04-26
TW202138370A (zh) 2021-10-16
EP4119559A1 (en) 2023-01-18
CN107531682B (zh) 2021-05-04
TWI832668B (zh) 2024-02-11
NZ735715A (en) 2022-09-30
IL255555B (en) 2021-12-01
US20180127412A1 (en) 2018-05-10
SG11201707984TA (en) 2017-11-29
CA2981746A1 (en) 2016-10-20
TWI876835B (zh) 2025-03-11
KR102643609B1 (ko) 2024-03-05
EP3283486A4 (en) 2018-08-22
TWI736531B (zh) 2021-08-21
EA201792254A1 (ru) 2018-02-28
CN107531682A (zh) 2018-01-02
JP2024012540A (ja) 2024-01-30
JP7320741B2 (ja) 2023-08-04
TWI792406B (zh) 2023-02-11
TW202434587A (zh) 2024-09-01
KR20240049684A (ko) 2024-04-16
BR112017020945A2 (pt) 2018-07-10
CN113307805A (zh) 2021-08-27
JP7383652B2 (ja) 2023-11-20
IL287740B1 (en) 2025-07-01
MX2017013219A (es) 2018-02-15
ZA201706392B (en) 2019-05-29
TW202330526A (zh) 2023-08-01
KR20170139073A (ko) 2017-12-18
EP3283486A1 (en) 2018-02-21
MX381053B (es) 2025-03-12
TW201702241A (zh) 2017-01-16
IL287740A (en) 2021-12-01

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