KR102643609B1 - B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도 - Google Patents

B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도 Download PDF

Info

Publication number
KR102643609B1
KR102643609B1 KR1020177033101A KR20177033101A KR102643609B1 KR 102643609 B1 KR102643609 B1 KR 102643609B1 KR 1020177033101 A KR1020177033101 A KR 1020177033101A KR 20177033101 A KR20177033101 A KR 20177033101A KR 102643609 B1 KR102643609 B1 KR 102643609B1
Authority
KR
South Korea
Prior art keywords
compound
cancer
maleate
delete delete
crystalline form
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
KR1020177033101A
Other languages
English (en)
Korean (ko)
Other versions
KR20170139073A (ko
Inventor
구올리앙 장
창유 조우
Original Assignee
베이진 엘티디
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 베이진 엘티디 filed Critical 베이진 엘티디
Priority to KR1020247006890A priority Critical patent/KR20240049684A/ko
Publication of KR20170139073A publication Critical patent/KR20170139073A/ko
Application granted granted Critical
Publication of KR102643609B1 publication Critical patent/KR102643609B1/ko
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/435—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
    • A61K31/33—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
    • A61K31/557—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)
  • 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)
KR1020177033101A 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도 Active KR102643609B1 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
KR1020247006890A KR20240049684A (ko) 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020247006890A Division KR20240049684A (ko) 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도

Publications (2)

Publication Number Publication Date
KR20170139073A KR20170139073A (ko) 2017-12-18
KR102643609B1 true KR102643609B1 (ko) 2024-03-05

Family

ID=57125563

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020177033101A Active KR102643609B1 (ko) 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도
KR1020247006890A Pending KR20240049684A (ko) 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020247006890A Pending KR20240049684A (ko) 2015-04-15 2016-04-14 B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도

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 (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

Family Cites Families (10)

* 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
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
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
US20100197924A1 (en) 2008-12-22 2010-08-05 Millennium Pharmaceuticals, Inc. Preparation of aminotetralin compounds
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 (2)

* 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
JP2015506353A (ja) * 2011-12-31 2015-03-02 ベイジーン リミテッド Ｒａｆキナーゼ阻害剤としての縮合三環式化合物

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
EA035680B1 (ru) 2020-07-24
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
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
KR102643609B1 (ko) B-raf 키나아제 억제제의 말레에이트 염, 결정질 형태, 제조방법, 및 이의 용도
CN116096372B (zh) 一种egfr抑制剂、其制备方法和在药学上的应用
JP2022071072A (ja) （ｓ）－７－（１－アクリロイルピペリジン－４－イル）－２－（４－フェノキシフェニル）－４，５，６，７－テトラ－ヒドロピラゾロ［１，５－ａ］ピリミジン－３－カルボキサミドの結晶形、その調製、及びその使用
US20210163464A1 (en) Pyridine compound
US10906901B2 (en) Crystal form and salt form of N-phenyl-2-aminopyrimidine compound, and preparation method therefor
HK40084617A (en) Maleate salts of a b-raf kinase inhibitor, crystalline forms, methods of preparation, and uses therefore
KR20230026384A (ko) 화합물의 결정 형태
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
US20210340142A1 (en) Salt form and crystal form of novel azatricyclic compound and use thereof

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P18-X000 Priority claim added or amended

St.27 status event code: A-2-2-P10-P18-nap-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

R18-X000 Changes to party contact information recorded

St.27 status event code: A-3-3-R10-R18-oth-X000

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PA0104 Divisional application for international application

St.27 status event code: A-0-1-A10-A18-div-PA0104

St.27 status event code: A-0-1-A10-A16-div-PA0104

PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18 Changes to party contact information recorded

Free format text: ST27 STATUS EVENT CODE: A-5-5-R10-R18-OTH-X000 (AS PROVIDED BY THE NATIONAL OFFICE)

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PN2301 Change of applicant

St.27 status event code: A-5-5-R10-R11-asn-PN2301

R11 Change to the name of applicant or owner or transfer of ownership requested

Free format text: ST27 STATUS EVENT CODE: A-5-5-R10-R11-ASN-PN2301 (AS PROVIDED BY THE NATIONAL OFFICE)