CA2901083A1 - Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones - Google Patents

Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones Download PDF

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Publication number
CA2901083A1
CA2901083A1 CA2901083A CA2901083A CA2901083A1 CA 2901083 A1 CA2901083 A1 CA 2901083A1 CA 2901083 A CA2901083 A CA 2901083A CA 2901083 A CA2901083 A CA 2901083A CA 2901083 A1 CA2901083 A1 CA 2901083A1
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CA
Canada
Prior art keywords
optionally
alkyl
alkynyl
alkenyl
substituted
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.)
Abandoned
Application number
CA2901083A
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English (en)
French (fr)
Inventor
Bo REN
Changyou Zhou
Hexiang Wang
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.)
Individual
Original Assignee
Beigene 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 Beigene Ltd filed Critical Beigene Ltd
Publication of CA2901083A1 publication Critical patent/CA2901083A1/en
Abandoned legal-status Critical Current

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    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2901083A 2013-04-26 2014-04-14 Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones Abandoned CA2901083A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2013/074780 2013-04-26
CN2013074780 2013-04-26
PCT/CN2014/075257 WO2014173241A1 (en) 2013-04-26 2014-04-14 Substituted5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones

Publications (1)

Publication Number Publication Date
CA2901083A1 true CA2901083A1 (en) 2014-10-30

Family

ID=51791046

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2901083A Abandoned CA2901083A1 (en) 2013-04-26 2014-04-14 Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones

Country Status (13)

Country Link
US (2) US9393232B2 (enExample)
EP (1) EP2989096B1 (enExample)
JP (1) JP6388915B2 (enExample)
CN (1) CN105102452B (enExample)
AU (1) AU2014256750B2 (enExample)
BR (1) BR112015027130A2 (enExample)
CA (1) CA2901083A1 (enExample)
EA (1) EA027139B1 (enExample)
HK (1) HK1217484A1 (enExample)
IL (1) IL240126A0 (enExample)
MX (1) MX366623B (enExample)
SG (1) SG11201506829XA (enExample)
WO (1) WO2014173241A1 (enExample)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
US9765039B2 (en) 2012-11-21 2017-09-19 Zenith Epigenetics Ltd. Biaryl derivatives as bromodomain inhibitors
JP2016507496A (ja) 2012-12-21 2016-03-10 ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． ブロモドメイン阻害剤としての新規複素環式化合物
EA035469B1 (ru) 2013-03-15 2020-06-22 Инсайт Холдингс Корпорейшн Трициклические гетероциклы как ингибиторы белков бэт
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны
KR102307566B1 (ko) 2013-06-21 2021-10-05 제니쓰 에피제네틱스 리미티드 신규한 바이사이클릭 브로모도메인 억제제
CN105473581B (zh) 2013-06-21 2019-04-23 齐尼思表观遗传学有限公司 作为溴结构域抑制剂的新取代的双环化合物
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
US9315501B2 (en) 2013-11-26 2016-04-19 Incyte Corporation Bicyclic heterocycles as BET protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
SMT202000133T1 (it) 2014-04-23 2020-05-08 Incyte Corp 1h-pirrolo[2,3-c]piridin-7(6h)-oni e pirazolo[3,4-c]piridin-7(6h)-oni come inibitori di proteine bet
JP6599979B2 (ja) 2014-09-15 2019-10-30 インサイト・コーポレイション Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物
US10179125B2 (en) 2014-12-01 2019-01-15 Zenith Epigenetics Ltd. Substituted pyridines as bromodomain inhibitors
HK1245246A1 (zh) 2014-12-01 2018-08-24 恒翼生物医药科技(上海)有限公司 作为溴域抑制剂的取代吡啶酮
WO2016092375A1 (en) 2014-12-11 2016-06-16 Zenith Epigenetics Corp. Substituted heterocycles as bromodomain inhibitors
CN107406438B (zh) 2014-12-17 2021-05-14 恒翼生物医药科技(上海)有限公司 溴结构域的抑制剂
CN111662226B (zh) * 2015-01-28 2022-03-18 中国科学院广州生物医药与健康研究院 一种2-氧代-1,2-二氢苯并[cd]吲哚类化合物
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2016203335A1 (en) 2015-06-18 2016-12-22 Pfizer Inc. Novel pyrido[2,3-b]pyrazinones as bet-family bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN109715625B (zh) 2016-06-20 2022-04-19 因赛特公司 Bet抑制剂的结晶固体形式
CN109789127B (zh) 2016-07-29 2022-03-25 英克特诺治疗公司 吲哚啉酮化合物的用途
CN113321640B (zh) * 2017-06-22 2023-06-09 中国科学院广州生物医药与健康研究院 一种吲哚类化合物及其应用
GB201716392D0 (en) * 2017-10-06 2017-11-22 Glaxosmithkline Intellectual Property (No 2) Ltd Compounds
CN109928979B (zh) * 2017-12-15 2021-08-06 四川科伦博泰生物医药股份有限公司 吲哚酮类衍生物及其制备方法和用途
ES3053198T3 (en) 2018-08-27 2026-01-20 Arcus Biosciences Inc Cd73 inhibitors
CN113018301A (zh) * 2019-12-09 2021-06-25 中国科学院大连化学物理研究所 JQ1与Erlotinib组合物在制备治疗肝癌药物中应用和治疗肝癌药物
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022087234A1 (en) 2020-10-23 2022-04-28 The Board Of Trustees Of The University Of Illinois Anticancer compounds selective for er-positive cancers
CN113149888B (zh) * 2021-05-06 2023-03-03 中山大学 一种羟基吲哚酮类衍生物及其制备方法和应用
WO2023125681A1 (en) * 2021-12-29 2023-07-06 Beigene, Ltd. Heterocyclic compounds
WO2025064918A1 (en) * 2023-09-20 2025-03-27 The Board Of Regents Of The University Of Texas System First-in-class phospho-brd4 inhibitors

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0420970D0 (en) 2004-09-21 2004-10-20 Smithkline Beecham Corp Novel triazoloquinoline compounds
CN101910182B (zh) * 2007-12-28 2013-07-17 田边三菱制药株式会社 抗癌剂
EP2303841A1 (en) * 2008-07-14 2011-04-06 Gilead Sciences, Inc. Oxindolyl inhibitor compounds
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
AU2010317096B2 (en) 2009-11-05 2015-03-26 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
CA2779355C (en) 2009-11-05 2018-01-16 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
CN102656147A (zh) * 2009-12-11 2012-09-05 霍夫曼-拉罗奇有限公司 可用作ampk调节剂的螺吲哚-环丙烷二氢吲哚酮
WO2011069298A1 (en) 2009-12-11 2011-06-16 F. Hoffmann-La Roche Ag Novel cyclopropane indolinone derivatives
ES2606958T3 (es) 2010-05-14 2017-03-28 Dana-Farber Cancer Institute, Inc. Compuestos de tienotriazolodiazepina para tratar una neoplasia
CN103180318B (zh) 2010-05-14 2017-05-10 达那-法伯癌症研究所 雄性避孕组合物以及使用方法
EP2585465B1 (en) 2010-06-22 2014-11-12 GlaxoSmithKline LLC Benzotriazolodiazepine compounds inhibitors of bromodomains
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012143436A1 (en) 2011-04-21 2012-10-26 Sanofi-Aventis Deutschland Gmbh Medicated module with lock ring
WO2012151512A2 (en) 2011-05-04 2012-11-08 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EA201591746A1 (ru) * 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
EP2978757B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Indolinone analogues as brd4 inhibitors
EA027139B1 (ru) 2013-04-26 2017-06-30 Бейджин, Лтд. Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны

Also Published As

Publication number Publication date
US20160030395A1 (en) 2016-02-04
US9393232B2 (en) 2016-07-19
BR112015027130A2 (en) 2018-07-24
EP2989096A4 (en) 2016-11-02
EP2989096A1 (en) 2016-03-02
CN105102452B (zh) 2018-01-26
AU2014256750B2 (en) 2018-08-23
US9827226B2 (en) 2017-11-28
MX2015014947A (es) 2016-03-07
AU2014256750A1 (en) 2015-12-10
MX366623B (es) 2019-07-16
SG11201506829XA (en) 2015-12-30
CN105102452A (zh) 2015-11-25
EA027139B1 (ru) 2017-06-30
JP6388915B2 (ja) 2018-09-12
WO2014173241A1 (en) 2014-10-30
EP2989096B1 (en) 2019-04-10
IL240126A0 (en) 2015-09-24
US20170027912A1 (en) 2017-02-02
HK1217484A1 (zh) 2017-01-13
JP2016517857A (ja) 2016-06-20
EA201592024A1 (ru) 2016-05-31

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Effective date: 20190409

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Effective date: 20210907