CN110049981A - 一种溴结构域蛋白抑制剂药物的晶型及其制备方法和用途 - Google Patents

一种溴结构域蛋白抑制剂药物的晶型及其制备方法和用途 Download PDF

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Publication number
CN110049981A
CN110049981A CN201780075689.6A CN201780075689A CN110049981A CN 110049981 A CN110049981 A CN 110049981A CN 201780075689 A CN201780075689 A CN 201780075689A CN 110049981 A CN110049981 A CN 110049981A
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China
Prior art keywords
crystal form
apabetalone
preparation
ray powder
powder diffraction
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CN201780075689.6A
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陈敏华
张炎锋
翟晓婷
鄢楷强
张晓宇
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Risflojex Co.
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Crystal Pharmaceutical Suzhou Co Ltd
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    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • 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
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

一种式I所示的溴结构域蛋白抑制剂2‑[4‑(2‑羟基乙氧基)‑3,5‑二甲基苯基]‑5,7‑二甲氧基喹唑啉‑4(3H)‑酮药物的晶型及其制备方法和用途。所述晶型为晶型CS2、晶型CS8、晶型CS13、晶型CS20、晶型CS1、晶型CS7、晶型CS9晶型CS11及晶型CS4，可用于治疗心血管、胆固醇或脂质相关紊乱疾病的药物。

Description

PCT国内申请，说明书已公开。

Claims (46)

  1. PCT国内申请，权利要求书已公开。
CN201780075689.6A 2016-12-09 2017-12-08 一种溴结构域蛋白抑制剂药物的晶型及其制备方法和用途 Pending CN110049981A (zh)

Applications Claiming Priority (5)

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CN2016111316986 2016-12-09
CN201611131698 2016-12-09
CN201611229263 2016-12-27
CN2016112292635 2016-12-27
PCT/CN2017/115143 WO2018103726A1 (zh) 2016-12-09 2017-12-08 一种溴结构域蛋白抑制剂药物的晶型及其制备方法和用途

Publications (1)

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CN110049981A true CN110049981A (zh) 2019-07-23

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US (1) US10752595B2 (zh)
EP (1) EP3553058A1 (zh)
JP (1) JP6849804B2 (zh)
CN (1) CN110049981A (zh)
AU (1) AU2017373239B2 (zh)
WO (1) WO2018103726A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2454966T3 (es) 2007-02-01 2014-04-14 Resverlogix Corp. Compuestos para la prevención y el tratamiento de enfermedades cardiovasculares
CA3146333A1 (en) 2009-03-18 2010-09-23 Resverlogix Corp. Phenyl-quinazolin-4(3h)-one and phenyl-pyrido[2,3-d]pyrimidin-4(3h)-one derivatives and compositions thereof useful as anti-inflammatory agents
CN109824608B (zh) * 2019-03-15 2022-06-21 深圳晶泰科技有限公司 一种Apabetalone晶型及其制备方法
CN109897009B (zh) * 2019-03-15 2022-06-28 深圳晶泰科技有限公司 一种Apabetalone水合物晶型及其制备方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101641339A (zh) * 2007-02-01 2010-02-03 雷斯韦洛吉克斯公司 用于预防和治疗心血管疾病的化合物
CN101970416A (zh) * 2008-06-26 2011-02-09 雷斯韦洛吉克斯公司 制备喹唑啉酮衍生物的方法

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130281397A1 (en) * 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101641339A (zh) * 2007-02-01 2010-02-03 雷斯韦洛吉克斯公司 用于预防和治疗心血管疾病的化合物
CN101970416A (zh) * 2008-06-26 2011-02-09 雷斯韦洛吉克斯公司 制备喹唑啉酮衍生物的方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SARAH PICAUD ET AL.: "RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain", 《PNAS》 *

Also Published As

Publication number Publication date
WO2018103726A1 (zh) 2018-06-14
JP2020500912A (ja) 2020-01-16
US10752595B2 (en) 2020-08-25
JP6849804B2 (ja) 2021-03-31
EP3553058A1 (en) 2019-10-16
US20190330161A1 (en) 2019-10-31
AU2017373239A1 (en) 2019-07-25
AU2017373239B2 (en) 2022-03-10

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