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
Inventor
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
CNPCT/CN2015/076639 2015-04-15
CN2015076639 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 (OSRAM)
EP (2) EP4119559A1 (OSRAM)
JP (3) JP7320741B2 (OSRAM)
KR (2) KR20240049684A (OSRAM)
CN (2) CN107531682B (OSRAM)
AU (1) AU2016248376B2 (OSRAM)
CA (1) CA2981746C (OSRAM)
EA (1) EA035680B1 (OSRAM)
IL (2) IL255555B (OSRAM)
MX (1) MX381053B (OSRAM)
NZ (1) NZ735715A (OSRAM)
SG (1) SG11201707984TA (OSRAM)
TW (4) TWI792406B (OSRAM)
WO (1) WO2016165626A1 (OSRAM)
ZA (1) ZA201706392B (OSRAM)

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ES2393768T3 (es) 2005-05-26 2012-12-27 Neuron Systems, Inc Derivado de quinolina para el tratamiento de enfermedades retinianas
WO2011072141A1 (en) 2009-12-11 2011-06-16 Neuron Systems, Inc. Compositions and methods for the treatment of macular degeneration
DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
CN117045653A (zh) 2013-01-23 2023-11-14 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
CN107531682B (zh) 2015-04-15 2021-05-04 百济神州有限公司 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途
JP6947406B2 (ja) 2015-08-21 2021-10-13 アルデイラ セラピューティクス, インコーポレイテッド 重水素化化合物およびその使用
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
US11266653B2 (en) 2017-05-02 2022-03-08 Novartis Ag Combination therapy
JP7311162B2 (ja) 2017-10-10 2023-07-19 アルデイラ セラピューティクス, インコーポレイテッド 炎症性障害の処置
CN112714762A (zh) * 2018-08-06 2021-04-27 奥尔德拉医疗公司 多晶型化合物及其用途
JOP20210072A1 (ar) * 2018-10-31 2023-01-30 Servier Lab ملح جديد لمثبط bcl-2، صورة بلورية ذات صلة، طريقة تحضيره وتركيبات صيدلية تحتوي عليه
CN111484489B (zh) * 2019-01-25 2023-05-23 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
WO2020190780A1 (en) * 2019-03-15 2020-09-24 Forma Therapeutics, Inc. Inhibiting cyclic amp-responsive element-binding protein (creb)
EP3962894A4 (en) 2019-05-02 2023-01-11 Aldeyra Therapeutics, Inc. POLYMORPHIC COMPOUNDS AND USES THEREOF
WO2020223717A1 (en) 2019-05-02 2020-11-05 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
CA3138123A1 (en) 2019-05-13 2020-11-19 Novartis Ag New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2 (trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
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
US20230128315A1 (en) * 2020-04-03 2023-04-27 Beigene, Ltd. Co-administration of mirdametinib and lifirafenib for use in treating cancers
CA3175856A1 (en) 2020-05-13 2021-11-18 Todd Brady Pharmaceutical formulations and uses thereof
WO2023240178A1 (en) * 2022-06-08 2023-12-14 Mapkure, Llc Methods of treating cancer with a b-raf inhibitor

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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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JP5111113B2 (ja) 2004-12-13 2012-12-26 サネシス ファーマシューティカルズ, インコーポレイテッド Rafキナーゼ阻害剤として有用なピリドピリミジノン、ジヒドロピリミドピリミジノンおよびプテリジノン
TW200639163A (en) 2005-02-04 2006-11-16 Genentech Inc RAF inhibitor compounds and methods
KR20080074220A (ko) 2005-12-08 2008-08-12 밀레니엄 파머슈티컬스 인코퍼레이티드 키나아제 억제 활성을 갖는 비시클릭 화합물
WO2007136572A2 (en) 2006-05-15 2007-11-29 Merck & Co., Inc. Antidiabetic bicyclic compounds
ATE530540T1 (de) 2006-08-23 2011-11-15 Pfizer Prod Inc Pyrimidonverbindungen als gsk-3-inhibitoren
EP2061761A1 (en) 2006-09-07 2009-05-27 Millennium Pharmaceuticals, Inc. Phenethylamide derivatives with kinase inhibitory activity
EP2148875A1 (en) 2007-05-04 2010-02-03 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
KR20130105675A (ko) * 2010-11-25 2013-09-25 라티오팜 게엠베하 아파티닙의 신규 염 및 다형
CN107531682B (zh) 2015-04-15 2021-05-04 百济神州有限公司 B-raf激酶抑制剂的马来酸盐、其结晶形式、制备方法和用途

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Also Published As

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

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