EA035680B1 - Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения - Google Patents

Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения Download PDF

Info

Publication number
EA035680B1
EA035680B1 EA201792254A EA201792254A EA035680B1 EA 035680 B1 EA035680 B1 EA 035680B1 EA 201792254 A EA201792254 A EA 201792254A EA 201792254 A EA201792254 A EA 201792254A EA 035680 B1 EA035680 B1 EA 035680B1
Authority
EA
Eurasian Patent Office
Prior art keywords
compound
crystalline form
maleate
cancer
ray powder
Prior art date
Application number
EA201792254A
Other languages
English (en)
Russian (ru)
Other versions
EA201792254A1 (ru
Inventor
Голян Чжан
Чаню Чжоу
Original Assignee
Бейджин, Лтд.
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 Бейджин, Лтд. filed Critical Бейджин, Лтд.
Publication of EA201792254A1 publication Critical patent/EA201792254A1/ru
Publication of EA035680B1 publication Critical patent/EA035680B1/ru

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
EA201792254A 2015-04-15 2016-04-14 Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения EA035680B1 (ru)

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 (2)

Publication Number Publication Date
EA201792254A1 EA201792254A1 (ru) 2018-02-28
EA035680B1 true EA035680B1 (ru) 2020-07-24

Family

ID=57125563

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201792254A EA035680B1 (ru) 2015-04-15 2016-04-14 Малеатные соли ингибитора braf киназы, кристаллические формы, способы их получения и применения

Country Status (15)

Country Link
US (1) US10351559B2 (https=)
EP (2) EP3283486B1 (https=)
JP (3) JP7320741B2 (https=)
KR (2) KR102643609B1 (https=)
CN (2) CN113307805A (https=)
AU (1) AU2016248376B2 (https=)
CA (1) CA2981746C (https=)
EA (1) EA035680B1 (https=)
IL (2) IL287740B2 (https=)
MX (1) MX381053B (https=)
NZ (1) NZ735715A (https=)
SG (1) SG11201707984TA (https=)
TW (4) TWI792406B (https=)
WO (1) WO2016165626A1 (https=)
ZA (1) ZA201706392B (https=)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1888548E (pt) 2005-05-26 2012-10-30 Neuron Systems Inc Derivado de quinolina para o tratamento de doenças da retina
WO2011072141A1 (en) 2009-12-11 2011-06-16 Neuron Systems, Inc. Compositions and methods for the treatment of macular degeneration
US9273046B2 (en) 2011-12-31 2016-03-01 Beigene, Ltd. Fused tricyclic compounds as Raf kinase inhibitors
CA2898631C (en) 2013-01-23 2023-06-13 Aldeyra Therapeutics, Inc. Toxic aldehyde related diseases and treatment
NZ735715A (en) * 2015-04-15 2022-09-30 Beigene Ltd 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
US10864203B2 (en) 2016-07-05 2020-12-15 Beigene, Ltd. Combination of a PD-1 antagonist and a RAF inhibitor for treating cancer
ES2952265T3 (es) 2017-05-02 2023-10-30 Novartis Ag Terapia combinada que comprende un inhibidor de Raf y trametinib
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
WO2020033344A1 (en) * 2018-08-06 2020-02-13 Aldeyra Therapeutics, Inc. Polymorphic compounds and uses thereof
HUE062000T2 (hu) * 2018-10-31 2023-09-28 Servier Lab BCL-2 inhibitor új sója, vonatkozó kristályforma, ezek elõállítási eljárása és ezeket tartalmazó gyógyszerkészítmények
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)
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
ES3025633T3 (en) 2019-05-13 2025-06-09 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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007067444A1 (en) * 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
US20100197924A1 (en) * 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2005316668B2 (en) 2004-12-13 2012-09-06 Millennium 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
ATE552245T1 (de) 2006-05-15 2012-04-15 Merck Sharp & Dohme Antidiabetische bicyclische verbindungen
US20100292205A1 (en) 2006-08-23 2010-11-18 Pfizer Inc. Pyrimidone Compounds As GSK-3 Inhibitors
EP2061761A1 (en) 2006-09-07 2009-05-27 Millennium Pharmaceuticals, Inc. Phenethylamide derivatives with kinase inhibitory activity
EA016329B1 (ru) 2007-05-04 2012-04-30 Айрм Ллк СОЕДИНЕНИЯ И КОМПОЗИЦИИ, КАК ИНГИБИТОРЫ КИНАЗЫ c-KIT И PDGFR
CN103476770B (zh) * 2010-11-25 2017-02-15 拉蒂欧制药有限责任公司 阿法替尼盐和多晶型物
NZ735715A (en) 2015-04-15 2022-09-30 Beigene Ltd Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007067444A1 (en) * 2005-12-08 2007-06-14 Millennium Pharmaceuticals, Inc. Bicyclic compounds with kinase inhibitory activity
US20100197924A1 (en) * 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
WO2013097224A1 (en) * 2011-12-31 2013-07-04 Beigene, Ltd. Fused tricyclic compounds as raf kinase inhibitors

Also Published As

Publication number Publication date
MX381053B (es) 2025-03-12
TW202330526A (zh) 2023-08-01
US10351559B2 (en) 2019-07-16
EP3283486B1 (en) 2022-07-27
TW202138370A (zh) 2021-10-16
TW202434587A (zh) 2024-09-01
KR20240049684A (ko) 2024-04-16
JP2021073246A (ja) 2021-05-13
EP3283486A1 (en) 2018-02-21
KR20170139073A (ko) 2017-12-18
NZ735715A (en) 2022-09-30
AU2016248376B2 (en) 2020-10-08
IL255555B (en) 2021-12-01
CA2981746A1 (en) 2016-10-20
CN113307805A (zh) 2021-08-27
TWI876835B (zh) 2025-03-11
AU2016248376A1 (en) 2017-10-12
JP2018511634A (ja) 2018-04-26
EP4119559A1 (en) 2023-01-18
ZA201706392B (en) 2019-05-29
SG11201707984TA (en) 2017-11-29
JP7383652B2 (ja) 2023-11-20
IL255555A (en) 2018-01-31
TWI736531B (zh) 2021-08-21
CA2981746C (en) 2023-08-01
IL287740A (en) 2021-12-01
JP2024012540A (ja) 2024-01-30
CN107531682A (zh) 2018-01-02
CN107531682B (zh) 2021-05-04
BR112017020945A2 (pt) 2018-07-10
JP7320741B2 (ja) 2023-08-04
EA201792254A1 (ru) 2018-02-28
IL287740B2 (en) 2025-11-01
IL287740B1 (en) 2025-07-01
US20180127412A1 (en) 2018-05-10
KR102643609B1 (ko) 2024-03-05
TW201702241A (zh) 2017-01-16
TWI792406B (zh) 2023-02-11
EP3283486A4 (en) 2018-08-22
TWI832668B (zh) 2024-02-11
WO2016165626A1 (en) 2016-10-20
MX2017013219A (es) 2018-02-15

Similar Documents

Publication Publication Date Title
JP7383652B2 (ja) B-rafキナーゼのマレイン酸塩、結晶形、調整方法、及びその使用
US10457680B2 (en) Process for preparing a PARP inhibitor, crystalline forms, and uses thereof
JP2011515370A (ja) 4−アミノ−5−フルオロ−3−[5−(4−メチルピペラジン−1−イル)−1h−ベンズイミダゾール−2−イル]キノリン−2(1h)−オン乳酸塩の結晶形態及び2つの溶媒和物形態
WO2008021369A2 (en) Tricyclic compounds and its use as tyrosine kinase modulators
TW201236684A (en) Pharmaceutically acceptable salts of (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide, preparation process and pharmaceutical use there of
US20180282310A1 (en) Forms and compositions of biaryl inhibitors of bruton's tyrosine kinase
WO2017016463A1 (zh) Egfr抑制剂及其药学上可接受的盐和多晶型物及其应用
TWI786303B (zh) 抑制cdk4/6活性化合物的晶型及其應用
CN110885331A (zh) 一种新颖的6-氨基-1H-吡唑并[3,4-d]嘧啶类JAK激酶抑制剂的制备与应用
TW201211036A (en) Useful salts of indazole derivative
CN110256408B (zh) 一种二芳基吡唑化合物及包含该化合物的组合物及其用途
HK40084617A (en) Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
HK40049820A (en) Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
BR112017020945B1 (pt) Sais cristalinos de sesqui-maleato de um inibidor de quinase b-raf, método e processo de preparação e usos dos mesmos
EA052616B1 (ru) Кристаллические формы производных хиназолина, их получение, композиции и применение