IL287740B2 - 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

Info

Publication number
IL287740B2
IL287740B2 IL287740A IL28774021A IL287740B2 IL 287740 B2 IL287740 B2 IL 287740B2 IL 287740 A IL287740 A IL 287740A IL 28774021 A IL28774021 A IL 28774021A IL 287740 B2 IL287740 B2 IL 287740B2
Authority
IL
Israel
Prior art keywords
crystalline form
compound
maleate
dihydro
ray diffraction
Prior art date
Application number
IL287740A
Other languages
English (en)
Hebrew (he)
Other versions
IL287740B1 (en
IL287740A (en
Original Assignee
Beigene Ltd
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
Application filed by Beigene Ltd filed Critical Beigene Ltd
Publication of IL287740A publication Critical patent/IL287740A/en
Publication of IL287740B1 publication Critical patent/IL287740B1/en
Publication of IL287740B2 publication Critical patent/IL287740B2/en

Links

Classifications

    • 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
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/557—Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/558—Eicosanoids, e.g. leukotrienes or prostaglandins having heterocyclic rings containing oxygen as the only ring hetero atom, e.g. thromboxanes
    • A61K31/5585—Eicosanoids, 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
    • 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
    • C07C51/42—Separation; Purification; Stabilisation; Use of additives
    • C07C51/43—Separation; Purification; Stabilisation; Use of additives by change of the physical state, e.g. crystallisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic 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

Landscapes

  • 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)
IL287740A 2015-04-15 2016-04-14 Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore IL287740B2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (3)

Publication Number Publication Date
IL287740A IL287740A (en) 2021-12-01
IL287740B1 IL287740B1 (en) 2025-07-01
IL287740B2 true IL287740B2 (en) 2025-11-01

Family

ID=57125563

Family Applications (2)

Application Number Title Priority Date Filing Date
IL287740A IL287740B2 (en) 2015-04-15 2016-04-14 Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
IL255555A IL255555B (en) 2015-04-15 2017-11-09 Maleate salts of b-raf kinase inhibitors, crystalline forms, methods for their preparation and uses

Family Applications After (1)

Application Number Title Priority Date Filing Date
IL255555A IL255555B (en) 2015-04-15 2017-11-09 Maleate salts of b-raf kinase inhibitors, crystalline forms, methods for their preparation and uses

Country Status (15)

Country Link
US (1) US10351559B2 (enExample)
EP (2) EP4119559A1 (enExample)
JP (3) JP7320741B2 (enExample)
KR (2) KR20240049684A (enExample)
CN (2) CN107531682B (enExample)
AU (1) AU2016248376B2 (enExample)
CA (1) CA2981746C (enExample)
EA (1) EA035680B1 (enExample)
IL (2) IL287740B2 (enExample)
MX (1) MX381053B (enExample)
NZ (1) NZ735715A (enExample)
SG (1) SG11201707984TA (enExample)
TW (4) TWI876835B (enExample)
WO (1) WO2016165626A1 (enExample)
ZA (1) ZA201706392B (enExample)

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AU2006249866B2 (en) 2005-05-26 2011-10-13 Aldeyra Therapeutics, Inc. Compositions and methods of 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
DK2797888T3 (en) 2011-12-31 2016-09-19 Beigene Ltd Fused tricyclic compounds as RAF kinase inhibitors
CN111135171B (zh) 2013-01-23 2023-09-08 奥尔德拉医疗公司 与毒性醛相关的疾病和治疗
AU2016248376B2 (en) * 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
CN118724806A (zh) 2015-08-21 2024-10-01 奥尔德拉医疗公司 氘化化合物和其用途
WO2018007885A1 (en) 2016-07-05 2018-01-11 Beigene, Ltd. COMBINATION OF A PD-l ANTAGONIST AND A RAF INHIBITOR FOR TREATING CANCER
WO2018203219A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
CN111356451A (zh) 2017-10-10 2020-06-30 奥尔德拉医疗公司 炎性病症的治疗
CN112105349A (zh) * 2018-04-12 2020-12-18 阿纳韦克斯生命科学公司 A2-73结晶多晶型物质组合物及其使用方法
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
GEP20237494B (en) * 2018-10-31 2023-04-10 Servier Lab Novel salt of a bcl-2 inhibitor, related crystalline form, method for preparing the same and pharmaceutical compositions containing the same
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
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
EP3937936A4 (en) * 2019-03-15 2022-12-28 Forma Therapeutics, Inc. INHIBITION OF CYCLIC AMP-RESPONSIVE ELEMENT-BINDING PROTEIN (CREB)
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
US12098132B2 (en) 2019-05-02 2024-09-24 Aldeyra Therapeutics, Inc. Process for preparation of aldehyde scavenger and intermediates
EP4563150A3 (en) 2019-05-13 2025-07-23 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
PL4125842T3 (pl) * 2020-04-03 2024-10-14 Beigene, Ltd. Równoczesne podawanie mirdametynibu i lifirafenibu do stosowania w leczeniu nowotworów
WO2021231792A1 (en) 2020-05-13 2021-11-18 Aldeyra Therapeutics, Inc. 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

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

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US7767687B2 (en) 2004-12-13 2010-08-03 Biogen Idec Ma 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
WO2007067444A1 (en) 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
AU2007254325B2 (en) 2006-05-15 2012-05-10 Merck Sharp & Dohme Corp. Antidiabetic bicyclic compounds
CA2661334C (en) 2006-08-23 2011-11-29 Pfizer Products Inc. Pyrimidone compounds as gsk-3 inhibitors
JP2010502706A (ja) 2006-09-07 2010-01-28 ミレニアム・ファーマシューティカルズ・インコーポレイテッド キナーゼ阻害活性を有するフェネチルアミド誘導体
CA2686379A1 (en) 2007-05-04 2008-11-13 Irm Llc Phenylaminopyrimidine derivatives and compositions thereof 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
AU2016248376B2 (en) 2015-04-15 2020-10-08 Beone Medicines I Gmbh Maleate salts of a B-RAF kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

Non-Patent Citations (1)

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BRITTAIN, HARRY G., POLYMORPHISM IN PHARMACEUTICAL SOLIDS., 31 December 2009 (2009-12-31) *

Also Published As

Publication number Publication date
EA035680B1 (ru) 2020-07-24
CA2981746C (en) 2023-08-01
US20180127412A1 (en) 2018-05-10
ZA201706392B (en) 2019-05-29
KR20240049684A (ko) 2024-04-16
AU2016248376A1 (en) 2017-10-12
JP2021073246A (ja) 2021-05-13
EP3283486A4 (en) 2018-08-22
TWI876835B (zh) 2025-03-11
EP3283486A1 (en) 2018-02-21
IL287740B1 (en) 2025-07-01
IL287740A (en) 2021-12-01
TW202330526A (zh) 2023-08-01
JP2018511634A (ja) 2018-04-26
TWI736531B (zh) 2021-08-21
EP4119559A1 (en) 2023-01-18
TW201702241A (zh) 2017-01-16
CN107531682A (zh) 2018-01-02
TWI832668B (zh) 2024-02-11
CN113307805A (zh) 2021-08-27
WO2016165626A1 (en) 2016-10-20
IL255555A (en) 2018-01-31
AU2016248376B2 (en) 2020-10-08
IL255555B (en) 2021-12-01
NZ735715A (en) 2022-09-30
EP3283486B1 (en) 2022-07-27
BR112017020945A2 (pt) 2018-07-10
EA201792254A1 (ru) 2018-02-28
JP7383652B2 (ja) 2023-11-20
CN107531682B (zh) 2021-05-04
TWI792406B (zh) 2023-02-11
JP2024012540A (ja) 2024-01-30
JP7320741B2 (ja) 2023-08-04
KR20170139073A (ko) 2017-12-18
MX381053B (es) 2025-03-12
TW202138370A (zh) 2021-10-16
CA2981746A1 (en) 2016-10-20
SG11201707984TA (en) 2017-11-29
TW202434587A (zh) 2024-09-01
MX2017013219A (es) 2018-02-15
KR102643609B1 (ko) 2024-03-05
US10351559B2 (en) 2019-07-16

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