JP6388915B2 - 置換５−（３，５−ジメチルイソオキサゾール−４−イル）インドリン−２−オン - Google Patents
置換５−（３，５−ジメチルイソオキサゾール−４−イル）インドリン−２−オン Download PDFInfo
- Publication number
- JP6388915B2 JP6388915B2 JP2016509276A JP2016509276A JP6388915B2 JP 6388915 B2 JP6388915 B2 JP 6388915B2 JP 2016509276 A JP2016509276 A JP 2016509276A JP 2016509276 A JP2016509276 A JP 2016509276A JP 6388915 B2 JP6388915 B2 JP 6388915B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- optionally
- alkyl
- alkynyl
- alkenyl
- 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.)
- Expired - Fee Related
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
- A61K31/41—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
Landscapes
- 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)
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2016517857A JP2016517857A (ja) | 2016-06-20 |
| JP2016517857A5 JP2016517857A5 (enExample) | 2017-06-01 |
| JP6388915B2 true JP6388915B2 (ja) | 2018-09-12 |
Family
ID=51791046
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016509276A Expired - Fee Related JP6388915B2 (ja) | 2013-04-26 | 2014-04-14 | 置換５−（３，５−ジメチルイソオキサゾール−４−イル）インドリン−２−オン |
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)
| 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)
| 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 |
-
2014
- 2014-04-14 EA EA201592024A patent/EA027139B1/ru not_active IP Right Cessation
- 2014-04-14 US US14/404,798 patent/US9393232B2/en active Active
- 2014-04-14 MX MX2015014947A patent/MX366623B/es active IP Right Grant
- 2014-04-14 JP JP2016509276A patent/JP6388915B2/ja not_active Expired - Fee Related
- 2014-04-14 HK HK16105442.5A patent/HK1217484A1/zh unknown
- 2014-04-14 EP EP14788064.5A patent/EP2989096B1/en active Active
- 2014-04-14 CN CN201480017203.XA patent/CN105102452B/zh active Active
- 2014-04-14 CA CA2901083A patent/CA2901083A1/en not_active Abandoned
- 2014-04-14 AU AU2014256750A patent/AU2014256750B2/en not_active Ceased
- 2014-04-14 WO PCT/CN2014/075257 patent/WO2014173241A1/en not_active Ceased
- 2014-04-14 SG SG11201506829XA patent/SG11201506829XA/en unknown
- 2014-04-14 BR BR112015027130-8A patent/BR112015027130A2/en not_active Application Discontinuation
-
2015
- 2015-07-23 IL IL240126A patent/IL240126A0/en unknown
-
2016
- 2016-06-06 US US15/174,229 patent/US9827226B2/en active Active
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 |
| WO2014173241A1 (en) | 2014-10-30 |
| EP2989096B1 (en) | 2019-04-10 |
| IL240126A0 (en) | 2015-09-24 |
| US20170027912A1 (en) | 2017-02-02 |
| CA2901083A1 (en) | 2014-10-30 |
| HK1217484A1 (zh) | 2017-01-13 |
| JP2016517857A (ja) | 2016-06-20 |
| EA201592024A1 (ru) | 2016-05-31 |
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