CN109195964A - 抑制蛋白激酶活性化合物的晶型及其应用 - Google Patents

抑制蛋白激酶活性化合物的晶型及其应用 Download PDF

Info

Publication number
CN109195964A
CN109195964A CN201780006852.3A CN201780006852A CN109195964A CN 109195964 A CN109195964 A CN 109195964A CN 201780006852 A CN201780006852 A CN 201780006852A CN 109195964 A CN109195964 A CN 109195964A
Authority
CN
China
Prior art keywords
crystal form
item
structural formula
compound shown
water
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.)
Granted
Application number
CN201780006852.3A
Other languages
English (en)
Other versions
CN109195964B (zh
Inventor
梁从新
马勇斌
何伟
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Betta Pharmaceuticals Co Ltd
Original Assignee
Betta Pharmaceuticals Co 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 Betta Pharmaceuticals Co Ltd filed Critical Betta Pharmaceuticals Co Ltd
Publication of CN109195964A publication Critical patent/CN109195964A/zh
Application granted granted Critical
Publication of CN109195964B publication Critical patent/CN109195964B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C403/00—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone
    • C07C403/06—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms
    • C07C403/10—Derivatives of cyclohexane or of a cyclohexene or of cyclohexadiene, having a side-chain containing an acyclic unsaturated part of at least four carbon atoms, this part being directly attached to the cyclohexane or cyclohexene or cyclohexadiene rings, e.g. vitamin A, beta-carotene, beta-ionone having side-chains substituted by singly-bound oxygen atoms by etherified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

本发明涉及结构式I所示化合物({5‑[(1R)‑1‑(2,6‑二氯‑3‑氟苯基)乙氧基]‑6‑氨基哒嗪‑3‑基}‑N‑{4‑[((3S,5R)‑3,5‑二甲基哌嗪基)羰基]苯基}甲酰胺盐酸盐)及其水合物或溶剂化物的新晶型；本发明还涉及所述化合物和晶型的制备方法以及相关的中间体化合物，含有所述化合物的药物组合物，以及所述化合物或晶型在制备治疗疾病、病症或病状的药物中的应用或用于治疗疾病、病症或病状的治疗方法。

Description

PCT国内申请，说明书已公开。

Claims (51)

  1. PCT国内申请，权利要求书已公开。
CN201780006852.3A 2016-06-01 2017-06-01 抑制蛋白激酶活性化合物的晶型及其应用 Active CN109195964B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2016/084300 2016-06-01
CNPCT/CN2016/084300 2016-06-01
PCT/CN2017/086760 WO2017206924A1 (zh) 2016-06-01 2017-06-01 抑制蛋白激酶活性化合物的晶型及其应用

Publications (2)

Publication Number Publication Date
CN109195964A true CN109195964A (zh) 2019-01-11
CN109195964B CN109195964B (zh) 2021-08-10

Family

ID=60477983

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780006852.3A Active CN109195964B (zh) 2016-06-01 2017-06-01 抑制蛋白激酶活性化合物的晶型及其应用

Country Status (17)

Country Link
US (1) US10899744B2 (zh)
EP (1) EP3470410B1 (zh)
JP (1) JP7054528B2 (zh)
KR (1) KR102466958B1 (zh)
CN (1) CN109195964B (zh)
AU (1) AU2017274110B2 (zh)
BR (1) BR112018074612A2 (zh)
CA (1) CA3026142C (zh)
EA (1) EA201892687A1 (zh)
HK (1) HK1259249A1 (zh)
IL (1) IL263356B (zh)
MY (1) MY188379A (zh)
PH (1) PH12018502529A1 (zh)
RU (1) RU2744264C2 (zh)
SG (1) SG11201810800VA (zh)
TW (1) TWI646094B (zh)
WO (1) WO2017206924A1 (zh)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113861191B (zh) * 2018-06-21 2023-09-19 贝达药业股份有限公司 抑制cdk4/6活性化合物的晶型及其应用
US20230227413A1 (en) 2020-08-03 2023-07-20 Teva Pharmaceuticals International Gmbh Solid state forms of ensartinib and ensartinib salts
WO2023016321A1 (zh) * 2021-08-10 2023-02-16 贝达药业股份有限公司 恩沙替尼或其盐在治疗携带met 14外显子跳跃突变的疾病中的用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101652068A (zh) * 2007-01-19 2010-02-17 艾科睿制药公司 激酶抑制物化合物
CN102098917A (zh) * 2008-06-19 2011-06-15 艾科睿控股公司 作为激酶抑制剂化合物的取代的哒嗪羧酰胺化合物
WO2012048258A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
CN103298806A (zh) * 2010-10-08 2013-09-11 艾科睿控股公司 取代的哒嗪羧酰胺化合物

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003528101A (ja) 2000-03-06 2003-09-24 ワーナー−ランバート・カンパニー、リミテッド、ライアビリティ、カンパニー ５−アルキルピリド［２，３−ｄ］ピリミジンチロシンキナーゼ阻害剤
DK2476667T3 (da) 2003-02-26 2014-09-15 Sugen Inc Aminoheteroaryl-forbindelser som proteinkinase-inhibitorer
US8414489B2 (en) 2003-11-13 2013-04-09 Medtronic Minimed, Inc. Fabrication of multi-sensor arrays
RS51601B (en) 2004-08-26 2011-08-31 Pfizer Inc. PYRAZOLS SUBSTITUTED BY AMINOHETEROARYL UNITS AS PROTEIN KINASE INHIBITORS
CA2578075A1 (en) 2004-08-26 2006-03-02 Pfizer Inc. Aminoheteroaryl compounds as protein tyrosine kinase inhibitors
NZ568289A (en) 2005-12-05 2011-06-30 Pfizer Prod Inc Polymorphs of (R)-3-[1-(2,6-dichloro-3-fluoro-phenyl)-ethoxy]-5-(1- piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101652068A (zh) * 2007-01-19 2010-02-17 艾科睿制药公司 激酶抑制物化合物
CN102098917A (zh) * 2008-06-19 2011-06-15 艾科睿控股公司 作为激酶抑制剂化合物的取代的哒嗪羧酰胺化合物
WO2012048258A2 (en) * 2010-10-08 2012-04-12 Xcovery Holding Company, Llc Substituted pyridazine carboxamide compounds as kinase inhibitor compounds
CN103298806A (zh) * 2010-10-08 2013-09-11 艾科睿控股公司 取代的哒嗪羧酰胺化合物

Also Published As

Publication number Publication date
EP3470410A4 (en) 2019-12-04
RU2018145183A3 (zh) 2020-07-16
EP3470410B1 (en) 2024-04-17
IL263356A (en) 2018-12-31
SG11201810800VA (en) 2019-01-30
IL263356B (en) 2022-08-01
TWI646094B (zh) 2019-01-01
EA201892687A1 (ru) 2019-06-28
JP7054528B2 (ja) 2022-04-14
BR112018074612A2 (pt) 2019-03-19
CA3026142C (en) 2024-02-13
MY188379A (en) 2021-12-07
KR102466958B1 (ko) 2022-11-14
KR20190012231A (ko) 2019-02-08
RU2018145183A (ru) 2020-07-14
TW201742865A (zh) 2017-12-16
US20190135792A1 (en) 2019-05-09
RU2744264C2 (ru) 2021-03-04
EP3470410A1 (en) 2019-04-17
AU2017274110A1 (en) 2019-01-24
JP2019518026A (ja) 2019-06-27
HK1259249A1 (zh) 2019-11-29
CA3026142A1 (en) 2017-12-07
CN109195964B (zh) 2021-08-10
US10899744B2 (en) 2021-01-26
PH12018502529A1 (en) 2019-04-08
WO2017206924A1 (zh) 2017-12-07
AU2017274110B2 (en) 2021-05-06

Similar Documents

Publication Publication Date Title
CN107286077B (zh) 一种选择性的c-kit激酶抑制剂
CA2858033C (en) Quinolyl-containing hydroxamic acid compound and preparation method thereof, and pharmaceutical composition containing this compound and use thereof
KR101829595B1 (ko) 3-（1-｛3-［5-（1-메틸-피페리딘-4일메톡시）-피리미딘-2-일］-벤질｝-6-옥소-1,6-디히드로-피리다진-3-일）-벤조니트릴 히드로클로라이드 염의 신규한 다형체 및 이의 제조 방법
CN106232599A (zh) 4‑氨基‑咪唑并喹啉化合物
CN110167924A (zh) 用于治疗ezh2介导的癌症的组合物和方法
CN109336824B (zh) Mek抑制剂的制备和包含mek抑制剂的制剂
WO2017152707A1 (zh) 吡啶胺基嘧啶衍生物甲磺酸盐的结晶形式及其制备和应用
CN107922348A (zh) 双环杂环酰胺衍生物
WO2016078160A1 (zh) 胞苷衍生物及其应用
CN109195964A (zh) 抑制蛋白激酶活性化合物的晶型及其应用
JP6887980B2 (ja) 薬学的に活性な化合物の固体形態
WO2021143954A2 (zh) 一种氟伐替尼或其甲磺酸盐的晶型及其制备方法
JP2019509306A (ja) Ｊａｋ関連疾患の治療又は予防に用いる薬物の塩酸塩の結晶形及びその製造方法
WO2022194252A1 (zh) 一种化合物的多晶型及其制备方法和应用
TW202104216A (zh) Plk4抑制劑之結晶型
WO2016078397A1 (zh) 新型胞苷衍生物及其应用
NZ788961A (en) Crystalline form of compound suppressing protein kinase activity, and application thereof
EA041596B1 (ru) Кристаллическая форма соединения, подавляющего активность протеинкиназы, и её применение
WO2023134688A1 (zh) 一种rock抑制剂的盐及盐的晶型、组合物和药物用途
WO2019137027A1 (zh) Galunisertib的晶型及其制备方法和用途
CN107922430B (zh) 2-取代苯并咪唑-4-甲酰胺类化合物及制备方法和应用
WO2019105217A1 (zh) Galunisertib的晶型及其制备方法和用途
WO2024016986A1 (zh) 大环化合物及其药物组合物和应用
WO2024133302A1 (en) Crystalline forms of a her2 inhibitor
JPWO2017206924A5 (zh)

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1259249

Country of ref document: HK

GR01 Patent grant
GR01 Patent grant