AR106520A1 - Forma sólida amorfa de un inhibidor de proteína bet - Google Patents

Forma sólida amorfa de un inhibidor de proteína bet

Info

Publication number
AR106520A1
AR106520A1 ARP160103304A ARP160103304A AR106520A1 AR 106520 A1 AR106520 A1 AR 106520A1 AR P160103304 A ARP160103304 A AR P160103304A AR P160103304 A ARP160103304 A AR P160103304A AR 106520 A1 AR106520 A1 AR 106520A1
Authority
AR
Argentina
Prior art keywords
compound
amorfa
solid form
pyridin
protein inhibitor
Prior art date
Application number
ARP160103304A
Other languages
English (en)
Inventor
Zhou Jiacheng
Liu Pingli
Jia Zhongjiang
Frietze William
Chen Shili
Original Assignee
Incyte Corp
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 Incyte Corp filed Critical Incyte Corp
Publication of AR106520A1 publication Critical patent/AR106520A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente solicitud se relaciona con una forma sólida amorfa de (4S)-7-(3,5-dimetilisoxazol-4-il)-4-piridin-2-il-4,5-dihidroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-ona, y con procesos para su preparación, que es un inhibidor de proteínas BET tales como BRD2, BRD3, BRD4 y BRD-t y es útil en el tratamiento de varias enfermedades tal como cáncer. E intermediarios. Reivindicación 38: Un compuesto, en donde el compuesto es 5-nitro-3-(piridin-2-il)-3,4-dihidro-2H-benzo[b][1,4]oxazin-3-ol (Compuesto 1x) o una sal de este. Reivindicación 39: Un compuesto, en donde el compuesto es 7-yodo-4-piridin-2-il-4,5-dihidroimidazo[1,5,4-de][1,4]benzoxazin-2(1H)-ona (Compuesto 4x) o una sal de este.
ARP160103304A 2015-10-29 2016-10-28 Forma sólida amorfa de un inhibidor de proteína bet AR106520A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562248040P 2015-10-29 2015-10-29

Publications (1)

Publication Number Publication Date
AR106520A1 true AR106520A1 (es) 2018-01-24

Family

ID=57286856

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160103304A AR106520A1 (es) 2015-10-29 2016-10-28 Forma sólida amorfa de un inhibidor de proteína bet

Country Status (4)

Country Link
US (5) US20170121347A1 (es)
AR (1) AR106520A1 (es)
TW (1) TW201722966A (es)
WO (1) WO2017075377A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA119848C2 (uk) 2013-03-15 2019-08-27 Інсайт Холдинґс Корпорейшн Трициклічні гетероцикли як інгібітори білків бет
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein 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
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EA039678B1 (ru) 2014-04-23 2022-02-24 Инсайт Корпорейшн 1H-ПИРРОЛО[2,3-c]ПИРИДИН-7(6H)-ОНЫ И ПИРАЗОЛО[3,4-c]ПИРИДИН-7(6H)-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕЛКОВ BET
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為bet蛋白抑制劑之三環雜環
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
PT3472157T (pt) 2016-06-20 2023-05-30 Incyte Corp Formas sólidas cristalinas de um inibidor bet
TW202024078A (zh) * 2018-09-13 2020-07-01 加拿大商增你智表觀遺傳學公司 Bet溴結構域(bromodomain)抑制劑之固體形式之製備方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN113975278B (zh) * 2021-10-29 2023-04-07 中国科学院昆明动物研究所 溴隐亭在制备治疗非洲猪瘟的产品中的应用

Family Cites Families (155)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS59170313A (ja) 1983-03-14 1984-09-26 Kurimoto Iron Works Ltd スクリ−ンゲ−ト
JPS6085739U (ja) 1983-11-18 1985-06-13 クラリオン株式会社 テ−プレコ−ダにおけるピンチロ−ラ装置
JPH0314566A (ja) 1989-06-09 1991-01-23 Sankyo Co Ltd ベンズイミダゾール誘導体
US5244912A (en) 1991-03-28 1993-09-14 Eli Lilly And Company 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz(cd)indoles and pharmaceutical use thereof
FR2710915B1 (fr) 1993-10-04 1995-11-24 Synthelabo Dérivés de pipéridine, leur préparation et leur utilisation en thérapeutique.
FR2731708B1 (fr) 1995-03-13 1997-04-30 Synthelabo Derives de piperidine, leur procede de preparation et leur application en therapeutique
FR2747678B1 (fr) 1996-04-22 1998-05-22 Synthelabo Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique
NZ522112A (en) 2000-04-21 2004-10-29 Upjohn Co Substituted phenylazacycloalkane-type compounds for treating fibromyalgia and chronic fatigue syndrome
IL153231A0 (en) 2000-06-28 2003-07-06 Smithkline Beecham Plc Wet milling process
US6919334B2 (en) 2002-09-12 2005-07-19 Wyeth Antidepressant azaheterocyclymethyl derivatives of 4,5-dihydroimidazo[1,4,5-de][1,4]benzoxazine
EP1562956A4 (en) 2002-11-22 2007-10-10 Japan Tobacco Inc HETEROCYCLES CONTAINING FUSED BICYCLIC NITROGEN
EP1462103A1 (en) 2003-03-25 2004-09-29 Faust Pharmaceuticals NO donors, combination products and uses as modulators of neurotransmitter release
US20070191447A1 (en) 2004-02-23 2007-08-16 Toru Kodo Novel heterocyclic compound
EP1732541A4 (en) 2004-04-07 2008-03-05 Takeda Pharmaceutical CYCLIC COMPOUNDS
DE102005011058A1 (de) 2005-03-10 2006-09-14 Merck Patent Gmbh Substituierte Tetrahydro-pyrrolo-chinolinderivate
WO2006124874A2 (en) 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
US20080318999A1 (en) 2005-08-05 2008-12-25 Methvin Isaac Tricyclic Benzimidazoles and Their Use as Metabotropic Glutamate Receptor Modulators
JP4986693B2 (ja) 2007-04-17 2012-07-25 キヤノン株式会社 情報処理装置及びその制御方法、並びにプログラム
EP2147310A4 (en) 2007-04-27 2010-09-08 Univ Rochester COMPOSITIONS AND METHODS FOR INHIBITING G PROTEIN SIGNALING
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US8633186B2 (en) 2007-06-08 2014-01-21 Senomyx Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
WO2009020559A2 (en) 2007-08-03 2009-02-12 The J. David Gladstone Institutes Agents that inhibit p-tefb interactions and methods of use thereof
EP2239264A4 (en) 2007-12-28 2012-01-11 Mitsubishi Tanabe Pharma Corp ANTITUMOR AGENT
DE102008052618A1 (de) 2008-10-21 2010-04-22 Henkel Ag & Co. Kgaa Tricyclische Aldehyde und C,H-acide Verbindungen
EP2415767B1 (en) 2009-03-27 2014-09-03 Takeda Pharmaceutical Company Limited Poly (ADP-ribose) Polymerase (PARP) Inhibitors
TW201103941A (en) 2009-06-10 2011-02-01 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
TW201105681A (en) 2009-06-10 2011-02-16 Janssen Pharmaceutica Nv Benzimidazole derivatives useful as TRPM8 channel modulators
WO2011024987A1 (ja) 2009-08-31 2011-03-03 塩野義製薬株式会社 芳香族縮合へテロ環誘導体およびそれらを含有する医薬組成物
GB0919431D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB0919434D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
WO2011054851A1 (en) 2009-11-05 2011-05-12 Glaxosmithkline Llc Novel process
JP5524343B2 (ja) 2009-11-05 2014-06-18 グラクソスミスクライン エルエルシー ベンゾジアゼピンブロモドメイン阻害剤
RS54645B1 (en) 2009-11-05 2016-08-31 Glaxosmithkline Llc BENZODIAZEPINE AS A BROMODOMEN INHIBITOR
GB0919423D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919426D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
US8927561B2 (en) 2010-04-23 2015-01-06 Kineta, Inc. Pyrimidinedione anti-viral compounds
BR112012029057A2 (pt) 2010-05-14 2020-10-13 Dana-Farber Cancer Institute, Inc. composições e métodos de tratamento de leucemia
WO2011143651A1 (en) 2010-05-14 2011-11-17 Dana-Farber Cancer Institute, Inc. Compositions and methods for modulating metabolism
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
CN104311562B (zh) 2010-05-14 2017-07-04 达那-法伯癌症研究所 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法
ES2526671T3 (es) 2010-06-22 2015-01-14 Glaxosmithkline Llc Compuestos de benzotriazoldiazepina inhibidores de bromodominios
AR084070A1 (es) 2010-12-02 2013-04-17 Constellation Pharmaceuticals Inc Inhibidores del bromodominio y usos de los mismos
WO2012075456A1 (en) 2010-12-02 2012-06-07 Constellation Pharmaceuticals Bromodomain inhibitors and uses thereof
CA2825028A1 (en) 2011-02-09 2012-08-16 F. Hoffman-La Roche Ag Heterocyclic compounds as pi3 kinase inhibitors
CN103547152A (zh) 2011-02-23 2014-01-29 西奈山伊坎医学院 溴结构域蛋白的抑制剂作为基因表达的调节剂
GB201106799D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106743D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
US9422292B2 (en) 2011-05-04 2016-08-23 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
WO2012174487A2 (en) 2011-06-17 2012-12-20 Constellation Pharmaceuticals, Inc. Bromodomain inhibitors and uses thereof
EP2723338A2 (en) 2011-06-24 2014-04-30 The Trustees of Stevens Institute of Technology Selective inhibitors of histone deacetylase isoform 6 and methods thereof
JP2013010719A (ja) 2011-06-30 2013-01-17 Dainippon Sumitomo Pharma Co Ltd ベンズイミダゾロンおよびオキシインドール誘導体ならびにそれらの医薬用途
EP2736528A4 (en) 2011-07-29 2015-03-18 Philadelphia Children Hospital COMPOSITIONS AND METHODS OF TREATING HIV
GB201114103D0 (en) 2011-08-17 2011-09-28 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
WO2013033269A1 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bioorthogonal monomers capable of dimerizing and targeting bromodomains and methods of using same
WO2013033270A2 (en) 2011-08-29 2013-03-07 Coferon, Inc. Bromodomain ligands capable of dimerizing in an aqueous solution, and methods of using same
SG10201505811QA (en) 2011-08-31 2015-09-29 Otsuka Pharma Co Ltd Quinolone compound
DE102011082013A1 (de) 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
WO2013043553A1 (en) 2011-09-22 2013-03-28 Glaxosmithkline Llc Pyrrolopyridinone compounds and methods for treating hiv
CN103857391B (zh) 2011-09-30 2016-06-08 沈阳蓝桑医药生物技术研发有限公司 含有瑞利格内酯的药物组合物及其应用
PL2773354T3 (pl) 2011-11-01 2019-12-31 Resverlogix Corp. Doustna formulacja o natychmiastowym uwalnianiu dla podstawowych chinazolinów
WO2013097052A1 (en) 2011-12-30 2013-07-04 Abbott Laboratories Bromodomain inhibitors
WO2013148197A1 (en) 2012-03-28 2013-10-03 The J. David Gladstone Institutes Compositions and methods for reactivating latent immunodeficiency virus
US20130281396A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281397A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281398A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
US20130281399A1 (en) 2012-04-19 2013-10-24 Rvx Therapeutics Inc. Treatment of diseases by epigenetic regulation
WO2013155695A1 (en) 2012-04-20 2013-10-24 Abbott Laboratories Isoindolone derivatives
WO2013184878A1 (en) 2012-06-06 2013-12-12 Constellation Pharmaceuticals, Inc. Benzo [b] isoxazoloazepine bromodomain inhibitors and uses thereof
TWI602820B (zh) 2012-06-06 2017-10-21 星宿藥物公司 溴域抑制劑及其用途
CA2874953A1 (en) 2012-06-12 2013-12-19 Abbvie Inc. Pyridinone and pyridazinone derivatives
KR20150045423A (ko) 2012-06-25 2015-04-28 온코에틱스 에스에이 티에노트리아졸로디아제핀 화합물을 사용하여 림프종을 치료하는 방법
US9610332B2 (en) 2012-07-18 2017-04-04 Massachusetts Institute Of Technology Compositions and methods for modulating BRD4 bioactivity
US20150238507A1 (en) 2012-08-16 2015-08-27 Glaxosmithkline Llc Benzodiazepines for treating small cell lung cancer
EA201590356A1 (ru) 2012-08-16 2015-07-30 Байер Фарма Акциенгезельшафт 2,3-бензодиазепины
CN104781259B (zh) 2012-09-28 2018-06-01 拜耳制药股份公司 抑制bet蛋白的5-芳基三唑并氮杂*
WO2014068402A2 (en) 2012-09-28 2014-05-08 Oncoethix Sa Pharmaceutical formulation containing thienotriazolodiazepine compounds
US9422290B2 (en) 2012-11-13 2016-08-23 Boehringer Ingelheim International Gmbh Triazolopyridazine
EP2920183B1 (en) 2012-11-14 2017-03-08 Glaxosmithkline LLC Thieno[3,2-c]pyridin-4(5h)-ones as bet inhibitors
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
WO2014095775A1 (de) 2012-12-20 2014-06-26 Bayer Pharma Aktiengesellschaft Bet-proteininhibitorische dihydrochinoxalinone
US20160193206A1 (en) 2012-12-20 2016-07-07 Bayer Pharma Aktiengesellschaft Bet-protein-inhibiting dihydropyridopyrazinones
CA2895905A1 (en) 2012-12-21 2014-06-26 Zenith Epigenetics Corp. Novel heterocyclic compounds as bromodomain inhibitors
WO2014128655A1 (en) 2013-02-25 2014-08-28 Aurigene Discovery Technologies Limited Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors
US9492460B2 (en) 2013-02-27 2016-11-15 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
WO2014134267A1 (en) 2013-02-27 2014-09-04 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
MX2015012158A (es) 2013-03-11 2015-12-01 Abbvie Inc Inhibidores de bomodominio tetraciclicos fusionados.
US9675697B2 (en) 2013-03-11 2017-06-13 The Regents Of The University Of Michigan BET bromodomain inhibitors and therapeutic methods using the same
MX2015012005A (es) 2013-03-11 2016-04-04 Abbvie Inc Inhibidores de bromodominio.
KR20150126696A (ko) 2013-03-12 2015-11-12 애브비 인코포레이티드 디하이드로-피롤로피리디논 브로모도메인 억제제
MX2015012431A (es) 2013-03-12 2016-05-31 Abbvie Inc Pirrol amida como inhibidores.
US10035800B2 (en) 2013-03-12 2018-07-31 Abbvie Inc. Substituted 1,4,10-triazadibenzo[cd,f]azulenes, substituted 1,4,5,10-tetraazadibenzo[cd,f]azulenes and substituted 1,4,5,7,10-pentaazadibenzo[cd,f]azulenes as bromodomain inhibitors
KR101780784B1 (ko) 2013-03-14 2017-09-21 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 2,3-이치환된 1-아실-4-아미노-1,2,3,4-테트라하이드로퀴놀린 유도체 및 이의 브로모도메인 억제제로서의 용도
WO2014159392A1 (en) 2013-03-14 2014-10-02 Dana-Farber Cancer Institute, Inc. Bromodomain binding reagents and uses thereof
JP6280573B2 (ja) 2013-03-14 2018-02-14 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited ブロモドメイン阻害薬としてのフロピリジン
US9695179B2 (en) 2013-03-14 2017-07-04 Convergene Llc Methods and compositions for inhibition of bromodomain-containing proteins
JP2016519660A (ja) 2013-03-15 2016-07-07 エピジェネティクス・インコーポレイテッド ブロモドメイン阻害剤としてのオキサゾロ[5,4−c]キノリン−2−オン化合物
UA119848C2 (uk) 2013-03-15 2019-08-27 Інсайт Холдинґс Корпорейшн Трициклічні гетероцикли як інгібітори білків бет
PL2970265T3 (pl) 2013-03-15 2018-11-30 Plexxikon Inc. Heterocykliczne związki i ich zastosowania
EP2978757B1 (en) 2013-03-27 2017-02-08 Boehringer Ingelheim International GmbH Indolinone analogues as brd4 inhibitors
JP6453845B2 (ja) 2013-03-27 2019-01-16 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Brd4阻害薬としてのジヒドロキナゾリノン類似体
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
WO2014170350A1 (en) 2013-04-17 2014-10-23 Albert Ludwigs Universität Freiburg Compounds for use as bromodomain inhibitors
US9393232B2 (en) 2013-04-26 2016-07-19 Beigene, Ltd. Substituted 5-(3,5-dimethylisoxazol-4-yl)indoline-2-ones
TWI527811B (zh) 2013-05-09 2016-04-01 吉李德科學股份有限公司 作爲溴結構域抑制劑的苯並咪唑衍生物
EP3004109A1 (en) 2013-05-27 2016-04-13 Novartis AG Imidazopyrrolidinone derivatives and their use in the treatment of disease
US8975417B2 (en) 2013-05-27 2015-03-10 Novartis Ag Pyrazolopyrrolidine derivatives and their use in the treatment of disease
MX2015016421A (es) 2013-05-28 2016-03-03 Novartis Ag Derivados de pirazolo-pirrolidin-4-ona como inhibidores de bet y su uso en el tratamiento de enfermedades.
US9714249B2 (en) 2013-05-28 2017-07-25 Novartis Ag Pyrazolo-pyrrolidin-4-one derivatives and their use in the treatment of disease
WO2014202578A1 (de) 2013-06-17 2014-12-24 Bayer Pharma Aktiengesellschaft Substituierte phenyl-2,3-benzodiazepine
ITMI20130991A1 (it) 2013-06-17 2014-12-18 Industrie De Nora Spa Sistema per la misurazione di correnti presenti sugli elettrodi in celle elettrolitiche interconnesse.
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
BR112015031073B1 (pt) 2013-06-21 2022-11-29 Zenith Epigenetics Ltd Compostos inibidores bicíclicos de bromodomínio e composição farmacêutica contendo os referidos compostos
AR096758A1 (es) 2013-06-28 2016-02-03 Abbvie Inc Inhibidores cristalinos de bromodominios
KR20160027062A (ko) 2013-06-28 2016-03-09 애브비 인코포레이티드 브로모도메인 억제제
US9290514B2 (en) 2013-07-08 2016-03-22 Incyte Holdings Corporation Tricyclic heterocycles as BET protein inhibitors
AU2014292193B2 (en) 2013-07-16 2018-04-26 Basf Se Herbicidal azines
WO2015013635A2 (en) 2013-07-25 2015-01-29 Dana-Farber Cancer Institute, Inc. Inhibitors of transcription factors and uses thereof
KR101672096B1 (ko) 2013-09-30 2016-11-02 주식회사 엘지화학 헤테로환 화합물 및 이를 포함하는 유기 발광 소자
SI3290407T1 (sl) 2013-10-18 2020-07-31 Celgene Quanticel Research, Inc Inhibitorji bromodomene
WO2015081246A1 (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
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
EP3089970B1 (en) 2013-12-09 2018-10-17 AbbVie Inc. Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
EP3083559B1 (en) 2013-12-20 2021-03-10 Merck Sharp & Dohme Corp. Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
SI3092227T1 (sl) 2014-01-09 2018-10-30 Orion Corporation Biciklični heterociklični derivati kot zaviralci bromodomaina
JP2017511801A (ja) 2014-02-28 2017-04-27 ザ リージェンツ オブ ザ ユニヴァシティ オブ ミシガン BETブロモドメイン阻害剤としての9H−ピリミド[4,5−b]インドールおよび関連類似体
EA201692129A1 (ru) 2014-04-23 2017-03-31 Басф Се Диаминотриазины в качестве гербицидов
KR102349237B1 (ko) 2014-04-23 2022-01-07 다케다 야쿠힌 고교 가부시키가이샤 알츠하이머 병의 치료를 위한 콜린작동성 무스카린 m1 수용체 양성 알로스테릭 조절인자 활성을 갖는 이소인돌린-1-온 유도체
EA039678B1 (ru) 2014-04-23 2022-02-24 Инсайт Корпорейшн 1H-ПИРРОЛО[2,3-c]ПИРИДИН-7(6H)-ОНЫ И ПИРАЗОЛО[3,4-c]ПИРИДИН-7(6H)-ОНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ БЕЛКОВ BET
WO2015168621A1 (en) 2014-05-02 2015-11-05 Oncoethix Sa Method of treating acute myeloid leukemia and/or acute lymphoblastic leukemia using thienotriazolodiazepine compounds
JP2017514907A (ja) 2014-05-02 2017-06-08 オンコエシックス ゲーエムベーハー チエノトリアゾロジアゼピン化合物を用いる耐性非ホジキンリンパ腫、髄芽腫及び/又はalk+非小細胞肺癌の治療方法
WO2015169953A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating glioma using thienotriazolodiazepine compounds
WO2015169951A1 (en) 2014-05-08 2015-11-12 Oncoethix Gmbh Method of treating triple-negative breast cancer using thienotriazolodiazepine compounds
US10065951B2 (en) 2014-05-30 2018-09-04 Icahn School Of Medicine At Mount Sinai Small molecule transcription modulators of bromodomains
TWI712603B (zh) 2014-09-15 2020-12-11 美商英塞特公司 作為bet蛋白抑制劑之三環雜環
MA40943A (fr) 2014-11-10 2017-09-19 Constellation Pharmaceuticals Inc Pyrrolopyridines substituées utilisées en tant qu'inhibiteurs de bromodomaines
US10259809B2 (en) 2015-02-03 2019-04-16 Trillium Therapeutics Inc. Fluorinated imidazo[4,5-C]quinoline derivatives as inhibitors of bromodomain containing proteins
WO2016186453A1 (en) 2015-05-20 2016-11-24 Kainos Medicine, Inc. Quinoline derivatives as bromodomain inhibitors
CN107922423B (zh) 2015-05-29 2020-10-27 盐野义制药株式会社 具有hiv复制抑制作用的含氮三环性衍生物
CN105039258B (zh) 2015-07-03 2018-04-17 北京大学 将非神经元细胞重编程为神经元样细胞的方法和组合物
US20170121347A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
CN105254635A (zh) 2015-10-30 2016-01-20 中国药科大学 一类咪唑并吡嗪类化合物及其药物组合物和用途
US20170127985A1 (en) 2015-11-11 2017-05-11 Medtronic Minimed, Inc. Sensor set
CA3007168A1 (en) 2015-12-14 2017-06-22 Zenith Epigenetics Ltd. 1h-imidazo[4,5-b]pyridinyl and 2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridinyl heterocyclic bet bromodomain inhibitors
WO2017127930A1 (en) 2016-01-28 2017-08-03 Neomed Institute Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals
CN108770356A (zh) 2016-02-05 2018-11-06 正大天晴药业集团股份有限公司 溴区结构域蛋白抑制剂的三环类化合物及其制备、药物组合物和用途
PT3472157T (pt) 2016-06-20 2023-05-30 Incyte Corp Formas sólidas cristalinas de um inibidor bet
CN108069958A (zh) 2016-11-10 2018-05-25 凯惠科技发展(上海)有限公司 一种含氮杂环类化合物、其制备方法、药物组合物及应用

Also Published As

Publication number Publication date
TW201722966A (zh) 2017-07-01
US20230219976A1 (en) 2023-07-13
US10858372B2 (en) 2020-12-08
WO2017075377A1 (en) 2017-05-04
US10329305B2 (en) 2019-06-25
US20170121347A1 (en) 2017-05-04
US20190300545A1 (en) 2019-10-03
US20180273546A1 (en) 2018-09-27
US20210079016A1 (en) 2021-03-18

Similar Documents

Publication Publication Date Title
AR106520A1 (es) Forma sólida amorfa de un inhibidor de proteína bet
ECSP16088983A (es) 1H-PIRROLO[2,3-c]PIRIDIN-7(6H)-ONAS YPIRAZOLO[3,4-c]PIRIDIN-7(6H)-ONAS COMO INHIBIDORES DE PROTEÍNAS BET
MA46054A (fr) Procédé de préparation de pyrazolo[1,5-a]pyrimidines et de sels de celles-ci
BR112018076486A2 (pt) formas sólidas cristalinas de um inibidor de bet
CL2013002341A1 (es) Compuestos derivados de 6-ciclobutil-1,5-dihidro-pirazolo [3,4 d]pirimidin-4-ona, inhibidores de pde9a; composicion farmaceutica; y su uso para el tratamiento de una enfermedad o afección relacionado con deterioro cognitivo, enfermedad de alzheimer, demencia vascular, entre otros
EP3107914B8 (en) Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use
EA201591785A1 (ru) Трициклические гетероциклы как ингибиторы белков бэт
CR20160222U (es) Formas solidas de acido { [ -(3- clorofenil) -3- hidroxipiridin -2-carbonil] amino} acetico, composiciones, y usos de las mismas
WO2014144721A3 (en) Treating th2-mediated diseases by inhibition of bromodomain-comprising proteins brd7 and brd9
TW201613935A (en) Tricyclic heterocycles as BET protein inhibitors
EP3515444A4 (en) COMPOSITION FOR TREATING EYE DISEASES AND METHOD FOR USE AND PRODUCTION
EA201790259A1 (ru) СОСТАВ ТАБЛЕТОК 2-ФТОР-N-МЕТИЛ-4-[7-(ХИНОЛИН-6-ИЛМЕТИЛ)ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИН-2-ИЛ]БЕНЗАМИДА
ES2699722R1 (es) Composicion para tratar enfermedades de las neuronas motoras y uso de la misma
CL2016001024A1 (es) Compuestos derivados de pirido[4,3-b]pirazin-2-carboxamidas; procedimiento de preparacion; composicion farmaceutica y uso para el tratamiento de trastornos neurodegenerativos, esquizofrenia, depresion, entre otras enfermedades.
CL2015000143A1 (es) Compuestos derivados de piperazino [1,2-a] indol-1-onas y [1,4] diazepino [1,2-a] indol-1-ona; proceso de obtencion; composicion farmaceutica; y su uso en el tratamiento de esquizofrenia, trastornos de personalidad, depresion mayor, entre otros.
EP3500579A4 (en) CHROMAN-SUBSTITUTED TETRACYCLIC COMPOUNDS AND USES THEREOF FOR TREATING VIRUS DISEASES
IL265985A (en) Process for the preparation of (3s,4s)-tetrahydrofuran-3-yl 4-isopropyl-6,7-dihydro-3h-imidazo[4,5-c]pyridine-5(4h)-carboxylate
IL253427A0 (en) The result of pyrazolo[3,4-d]pyrimidine and its use in the treatment of Jericho rose
TH182466B (th) สารกลุ่ม 1เอช-ไพร์โรโล[2,3-ซี]ไพริดิน-7(6เอช)-โอน และไพราโซโล[3,4-ซี] ไพริดิน-7(6เอช)-โอน ที่เป็นตัวยับยั้งของโปรตีน bet
EA201990076A1 (ru) Кристаллические твердые формы ингибитора bet
TH182466A (th) สารกลุ่ม 1เอช-ไพร์โรโล[2,3-ซี]ไพริดิน-7(6เอช)-โอน และไพราโซโล[3,4-ซี] ไพริดิน-7(6เอช)-โอน ที่เป็นตัวยับยั้งของโปรตีน bet
TH1501007226A (th) สารประกอบ 6,7-ไดไฮโดรไพราโซโล[1,5-a]ไพราซีน-4(5H)-โอน และการใช้ของ สิ่งนั้นในฐานะเป็นสารยับยั้งแอลโลสเตอริกของ mGluR2 รีเซ็ปเตอร์

Legal Events

Date Code Title Description
FB Suspension of granting procedure