WO2019120234A3 - 作为溴结构域蛋白质抑制剂的化合物和组合物 - Google Patents

作为溴结构域蛋白质抑制剂的化合物和组合物 Download PDF

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Publication number
WO2019120234A3
WO2019120234A3 PCT/CN2018/122211 CN2018122211W WO2019120234A3 WO 2019120234 A3 WO2019120234 A3 WO 2019120234A3 CN 2018122211 W CN2018122211 W CN 2018122211W WO 2019120234 A3 WO2019120234 A3 WO 2019120234A3
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WO
WIPO (PCT)
Prior art keywords
composition
protein inhibitor
bromodomain protein
compound functioning
compound
Prior art date
Application number
PCT/CN2018/122211
Other languages
English (en)
French (fr)
Other versions
WO2019120234A2 (zh
Inventor
徐琰
徐晓峰
王家炳
丁列明
Original Assignee
贝达药业股份有限公司
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
Priority to US16/954,901 priority Critical patent/US11466034B2/en
Priority to KR1020207021126A priority patent/KR20200101434A/ko
Priority to AU2018391833A priority patent/AU2018391833A1/en
Priority to SG11202005793SA priority patent/SG11202005793SA/en
Application filed by 贝达药业股份有限公司 filed Critical 贝达药业股份有限公司
Priority to MX2020006612A priority patent/MX2020006612A/es
Priority to CN201880081489.6A priority patent/CN111712496B/zh
Priority to JP2020534282A priority patent/JP2021506903A/ja
Priority to CA3086054A priority patent/CA3086054A1/en
Priority to EP18891050.9A priority patent/EP3719017A4/en
Priority to IL275478A priority patent/IL275478B1/en
Priority to BR112020012527-0A priority patent/BR112020012527A2/pt
Publication of WO2019120234A2 publication Critical patent/WO2019120234A2/zh
Publication of WO2019120234A3 publication Critical patent/WO2019120234A3/zh
Priority to ZA2020/04374A priority patent/ZA202004374B/en
Priority to US17/898,258 priority patent/US11845762B2/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • 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
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • 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
    • C07D471/06—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

一种具有式（I）结构的溴结构域抑制剂，也提供包含这类化合物的组合物和制剂，及使用和制备这样的化合物的方法。
PCT/CN2018/122211 2017-12-20 2018-12-20 作为溴结构域蛋白质抑制剂的化合物和组合物 WO2019120234A2 (zh)

Priority Applications (13)

Application Number Priority Date Filing Date Title
CN201880081489.6A CN111712496B (zh) 2017-12-20 2018-12-20 作为溴结构域蛋白质抑制剂的化合物和组合物
AU2018391833A AU2018391833A1 (en) 2017-12-20 2018-12-20 Compound functioning as bromodomain protein inhibitor, and composition
SG11202005793SA SG11202005793SA (en) 2017-12-20 2018-12-20 Compound functioning as bromodomain protein inhibitor, and composition
CA3086054A CA3086054A1 (en) 2017-12-20 2018-12-20 Compound functioning as bromodomain protein inhibitor, and composition
MX2020006612A MX2020006612A (es) 2017-12-20 2018-12-20 Compuesto que funciona como inhibidor de proteína de bromodominio y composición.
KR1020207021126A KR20200101434A (ko) 2017-12-20 2018-12-20 브로모도메인 단백질 억제제로서 작동하는 화합물 및 조성물
JP2020534282A JP2021506903A (ja) 2017-12-20 2018-12-20 ブロモドメインタンパク質阻害剤である化合物、および組成物
US16/954,901 US11466034B2 (en) 2017-12-20 2018-12-20 Compound functioning as bromodomain protein inhibitor, and composition
EP18891050.9A EP3719017A4 (en) 2017-12-20 2018-12-20 COMPOUND ACTING AS A BROMODOMAIN PROTEIN INHIBITOR AND COMPOSITION
IL275478A IL275478B1 (en) 2017-12-20 2018-12-20 A preparation that functions as a bromodomain protein inhibitor, and the composition
BR112020012527-0A BR112020012527A2 (pt) 2017-12-20 2018-12-20 composto que funciona como inibidor de proteína com bromodomínio, e composição
ZA2020/04374A ZA202004374B (en) 2017-12-20 2020-07-16 Compound functioning as bromodomain protein inhibitor, and composition
US17/898,258 US11845762B2 (en) 2017-12-20 2022-08-29 Compound functioning as bromodomain protein inhibitor, and composition

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CNPCT/CN2017/117451 2017-12-20
CNPCT/CN2017/117451 2017-12-20

Related Child Applications (2)

Application Number Title Priority Date Filing Date
US16/954,901 A-371-Of-International US11466034B2 (en) 2017-12-20 2018-12-20 Compound functioning as bromodomain protein inhibitor, and composition
US17/898,258 Division US11845762B2 (en) 2017-12-20 2022-08-29 Compound functioning as bromodomain protein inhibitor, and composition

Publications (2)

Publication Number Publication Date
WO2019120234A2 WO2019120234A2 (zh) 2019-06-27
WO2019120234A3 true WO2019120234A3 (zh) 2019-08-29

Family

ID=66994221

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2018/122211 WO2019120234A2 (zh) 2017-12-20 2018-12-20 作为溴结构域蛋白质抑制剂的化合物和组合物

Country Status (13)

Country Link
US (2) US11466034B2 (zh)
EP (1) EP3719017A4 (zh)
JP (1) JP2021506903A (zh)
KR (1) KR20200101434A (zh)
CN (1) CN111712496B (zh)
AU (1) AU2018391833A1 (zh)
BR (1) BR112020012527A2 (zh)
CA (1) CA3086054A1 (zh)
IL (1) IL275478B1 (zh)
MX (1) MX2020006612A (zh)
SG (1) SG11202005793SA (zh)
TW (1) TWI713952B (zh)
WO (1) WO2019120234A2 (zh)

Cited By (1)

* Cited by examiner, † Cited by third party
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JP7405468B2 (ja) 2019-10-08 2023-12-26 ハイヘ バイオファーマ カンパニー、リミテッド Ｂｒｄ４阻害活性を有する化合物、その調製方法および用途

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US10793561B2 (en) 2017-07-18 2020-10-06 Nuvation Bio Inc. 1,8-naphthyridinone compounds and uses thereof
WO2019018584A1 (en) 2017-07-18 2019-01-24 GiraFpharma LLC HETEROCYCLIC COMPOUNDS AS ADENOSINE ANTAGONISTS
US11192900B2 (en) 2018-10-30 2021-12-07 Nuvation Bio Inc. Substituted 1,6-dihydropyridinones and 1,2-dihydroisoquinolinones as bet inhibitors
JP2022517419A (ja) 2019-01-18 2022-03-08 ニューベイション・バイオ・インコーポレイテッド アデノシンアンタゴニストとしてのヘテロ環式化合物
EP3911324A4 (en) 2019-01-18 2022-08-17 Nuvation Bio Inc. 1,8-NAPHTHYRIDINONE COMPOUNDS AND THEIR USES
CA3145827A1 (en) 2019-07-02 2021-01-07 Nuvation Bio Inc. Heterocyclic compounds as bet inhibitors
WO2021233371A1 (zh) * 2020-05-21 2021-11-25 贝达药业股份有限公司 作为溴结构域蛋白质抑制剂的化合物和组合物
JP2023529471A (ja) * 2020-06-11 2023-07-10 貝達薬業股▲ふん▼有限公司 二環化合物及びその使用
CN115667190A (zh) * 2020-06-17 2023-01-31 贝达药业股份有限公司 双环类化合物及其应用
EP4360634A1 (en) * 2021-06-21 2024-05-01 Betta Pharmaceuticals Co., Ltd Application of compound in preparation of drug for treating myelofibrosis and related symptoms/signs thereof, and use of compound

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WO2015081189A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
CN105324379A (zh) * 2013-05-09 2016-02-10 吉里德科学公司 作为溴结构域抑制剂的苯并咪唑衍生物
CN105611835A (zh) * 2013-07-25 2016-05-25 达纳-法伯癌症研究所股份有限公司 转录因子抑制剂及其用途
CN107207493A (zh) * 2014-11-10 2017-09-26 基因泰克公司 作为布罗莫结构域抑制剂的经取代的吡咯并吡啶

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TWI530499B (zh) 2013-03-28 2016-04-21 吉李德科學股份有限公司 作為溴結構域（ｂｒｏｍｏｄｏｍａｉｎ）抑制劑之苯並咪唑酮衍生物類
PT3004108T (pt) 2013-05-28 2018-01-24 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inibidores de bet e a sua utilização no tratamento de doenças
EP3010503B1 (en) 2013-06-21 2020-03-11 Zenith Epigenetics Ltd. Novel bicyclic bromodomain inhibitors
AR100160A1 (es) 2014-04-23 2016-09-14 Incyte Corp 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS Y PIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEÍNAS BET
MA40940A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
EP3265453B1 (en) * 2015-03-05 2022-06-29 Boehringer Ingelheim International GmbH New pyridinones and isoquinolinones as inhibitors of the bromodomain brd9
AR104259A1 (es) * 2015-04-15 2017-07-05 Celgene Quanticel Res Inc Inhibidores de bromodominio

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Publication number Priority date Publication date Assignee Title
CN105324379A (zh) * 2013-05-09 2016-02-10 吉里德科学公司 作为溴结构域抑制剂的苯并咪唑衍生物
CN105611835A (zh) * 2013-07-25 2016-05-25 达纳-法伯癌症研究所股份有限公司 转录因子抑制剂及其用途
WO2015081203A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
WO2015081189A1 (en) * 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
CN107207493A (zh) * 2014-11-10 2017-09-26 基因泰克公司 作为布罗莫结构域抑制剂的经取代的吡咯并吡啶

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7405468B2 (ja) 2019-10-08 2023-12-26 ハイヘ バイオファーマ カンパニー、リミテッド Ｂｒｄ４阻害活性を有する化合物、その調製方法および用途

Also Published As

Publication number Publication date
IL275478A (en) 2020-08-31
TW201927792A (zh) 2019-07-16
CN111712496A (zh) 2020-09-25
US11845762B2 (en) 2023-12-19
BR112020012527A2 (pt) 2020-11-24
US11466034B2 (en) 2022-10-11
AU2018391833A1 (en) 2020-07-30
SG11202005793SA (en) 2020-07-29
CN111712496B (zh) 2023-05-02
US20200385408A1 (en) 2020-12-10
US20230022091A1 (en) 2023-01-26
IL275478B1 (en) 2024-02-01
JP2021506903A (ja) 2021-02-22
KR20200101434A (ko) 2020-08-27
CA3086054A1 (en) 2019-06-27
TWI713952B (zh) 2020-12-21
EP3719017A4 (en) 2020-12-02
MX2020006612A (es) 2020-11-09
WO2019120234A2 (zh) 2019-06-27
EP3719017A2 (en) 2020-10-07

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