ES2565992T3 - Derivados de pirrolo[2,3-b]piridina como inhibidores de proteínas cinasas - Google Patents

Derivados de pirrolo[2,3-b]piridina como inhibidores de proteínas cinasas Download PDF

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ES2565992T3
ES2565992T3 ES11173701.1T ES11173701T ES2565992T3 ES 2565992 T3 ES2565992 T3 ES 2565992T3 ES 11173701 T ES11173701 T ES 11173701T ES 2565992 T3 ES2565992 T3 ES 2565992T3
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nhc
optionally substituted
nhrk
nrkc
nrkrk
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Spanish (es)
Inventor
Prabha N. Ibrahim
Dean R. Artis
Ryan Bremer
Gaston Habets
Shumeye Mamo
Marika Nespi
Chao Zhang
Jiazhong Zhang
Yong-Liang Zhu
Rebecca Zuckerman
Brian West
Yoshihisa Suzuki
James Tsai
Klaus-Peter Hirth
Gideon Bollag
Wayne Spevak
Hanna Cho
Samuel J. Gillette
Guoxian Wu
Hongyao Zhu
Shenghua Shi
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Plexxikon Inc
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Plexxikon Inc
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    • 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
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Families Citing this family (417)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI1696920T1 (sl) 2003-12-19 2015-02-27 Plexxikon Inc. Spojine in postopki za razvoj modulatorjev ret
PT1730146E (pt) 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
US7498342B2 (en) 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
ATE428421T1 (de) 2004-09-17 2009-05-15 Eisai R&D Man Co Ltd Medizinische zusammensetzung mit verbesserter stabilität und reduzierten gelierungseigenschaften
CA2608733A1 (en) 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
EP3088400A1 (en) 2005-06-22 2016-11-02 Plexxikon Inc. Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors
US8163767B2 (en) 2005-07-14 2012-04-24 Astellas Pharma Inc. Heterocyclic Janus Kinase 3 inhibitors
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
EP1925676A4 (en) 2005-08-02 2010-11-10 Eisai R&D Man Co Ltd TEST METHOD FOR THE EFFECT OF A VASCULARIZATION INHIBITOR
CA2620594C (en) * 2005-09-01 2012-08-21 Eisai R&D Management Co., Ltd. Pharmaceutical composition having improved disintegratability
ES2970354T3 (es) 2005-12-13 2024-05-28 Incyte Holdings Corp Derivados de pirrolo[2,3-d]pirimidina como inhibidores de Janus quinasas
KR20130041313A (ko) 2006-01-17 2013-04-24 버텍스 파마슈티칼스 인코포레이티드 야누스 키나제의 억제제로서 유용한 아자인돌
JP2009523812A (ja) * 2006-01-19 2009-06-25 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド 融合へテロ二環式キナーゼ阻害剤
TWI382984B (zh) 2006-04-03 2013-01-21 Astellas Pharma Inc 雜環化合物
ES2556173T3 (es) 2006-05-18 2016-01-13 Eisai R&D Management Co., Ltd. Agente antitumoral para un cáncer de tiroides
EP2029593A1 (en) * 2006-05-22 2009-03-04 AstraZeneca AB Indole derivatives
US7964728B2 (en) 2006-07-06 2011-06-21 Solvay Pharmaceuticals B.V. Azaindole derivatives with a combination of partial nicotinic acetyl-choline receptor agonism and dopamine reuptake inhibition
ATE526327T1 (de) * 2006-07-06 2011-10-15 Abbott Healthcare Products Bv Azaindolderivate mit einer kombination eines teilweisen agonismus am nikotinischen acetylcholinrezeptor und einer inhibierung der dopaminwiederaufnahme
GB0617161D0 (en) * 2006-08-31 2006-10-11 Vernalis R&D Ltd Enzyme inhibitors
PL2529621T3 (pl) 2006-09-22 2017-06-30 Pharmacyclics Llc Inhibitory kinazy tyrozynowej brutona
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20081581A1 (es) * 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
TW200838517A (en) 2006-12-21 2008-10-01 Vertex Pharma Compounds useful as protein kinases inhibitors
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
US7872018B2 (en) * 2006-12-21 2011-01-18 Plexxikon, Inc. Compounds and methods for kinase modulation, and indications therefor
US8809273B2 (en) 2007-03-28 2014-08-19 Pharmacyclics, Inc. Inhibitors of Bruton's tyrosine kinase
JP5347202B2 (ja) * 2007-03-28 2013-11-20 ファーマサイクリックス，インク． ブルトンチロシンキナーゼインヒビター
JP5926487B2 (ja) 2007-04-13 2016-05-25 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド ＥｒｂＢ療法に耐性である癌を治療するための方法
GB0710528D0 (en) * 2007-06-01 2007-07-11 Glaxo Group Ltd Novel compounds
TR201903488T4 (tr) 2007-06-13 2019-04-22 Incyte Holdings Corp Janus kinaz inhibitörü (r)-3-(4-(7h-pirolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)-3-siklopentilpropannitril tuzlarının kullanımı.
MX2010000617A (es) * 2007-07-17 2010-05-17 Plexxikon Inc Compuestos y metodos para modulacion de cinasa, e indicaciones de estos.
MX2010001636A (es) * 2007-08-14 2010-03-15 Hoffmann La Roche Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos.
EP2184988B1 (en) 2007-08-17 2014-12-17 University of Maryland, Baltimore Small molecule inhibitors of lck sh2 domain binding
JP2009077712A (ja) 2007-09-11 2009-04-16 F Hoffmann La Roche Ag Ｂ−Ｒａｆキナーゼ阻害剤に対する感受性についての診断試験
DE102007045919B4 (de) 2007-09-26 2018-07-05 Bayer Intellectual Property Gmbh Wirkstoffkombinationen mit insektiziden und akariziden Eigenschaften
DE102007045956A1 (de) 2007-09-26 2009-04-09 Bayer Cropscience Ag Wirkstoffkombination mit insektiziden und akariziden Eigenschaften
CA2703125C (en) 2007-10-25 2012-08-28 David J. Guerin Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer
JP5608097B2 (ja) 2008-01-08 2014-10-15 アレイ バイオファーマ、インコーポレイテッド キナーゼ阻害薬としてのピロロピリジン
US8426396B2 (en) * 2008-01-08 2013-04-23 Shriners Hospitals For Children Treatment for achondroplasia
CA2711741A1 (en) 2008-01-09 2009-07-16 Array Biopharma Inc. Pyrazolopyridines as kinase inhibitors
EP2231282A1 (en) * 2008-01-22 2010-09-29 Merck Patent GmbH Protein kinase inhibitors and use thereof
JP5485178B2 (ja) * 2008-02-25 2014-05-07 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼ阻害剤
TW200940540A (en) 2008-02-29 2009-10-01 Array Biopharma Inc RAF inhibitor compounds and methods of use thereof
CA2716949A1 (en) 2008-02-29 2009-09-11 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
MX2010009411A (es) 2008-02-29 2010-11-30 Array Biopharma Inc Compuestos del inhibidor de raf y métodos de uso de los mismos.
UA103319C2 (en) 2008-05-06 2013-10-10 Глаксосмитклайн Ллк Thiazole- and oxazole-benzene sulfonamide compounds
PE20091846A1 (es) 2008-05-19 2009-12-16 Plexxikon Inc DERIVADOS DE PIRROLO[2,3-d]-PIRIMIDINA COMO MODULADORES DE CINASAS
US8158636B2 (en) 2008-05-19 2012-04-17 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CN102036982A (zh) * 2008-05-21 2011-04-27 巴斯夫欧洲公司 作为杀真菌剂的取代吡啶-4-基甲基磺酰胺
CN102046623A (zh) * 2008-05-28 2011-05-04 巴斯夫欧洲公司 作为杀真菌剂的取代的吡啶-4-基甲基磺酰胺
US8119637B2 (en) 2008-06-10 2012-02-21 Plexxikon Inc. Substituted pyrrolo[2,3-b]pyrazines and methods for kinase modulation, and indications therefor
WO2009152087A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor
AR072008A1 (es) * 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
US9447049B2 (en) 2010-03-01 2016-09-20 University Of Tennessee Research Foundation Compounds for treatment of cancer
JPWO2009157196A1 (ja) 2008-06-25 2011-12-08 武田薬品工業株式会社 アミド化合物
CN102159214A (zh) 2008-07-16 2011-08-17 药品循环公司 用于实体肿瘤的治疗的布鲁顿酪氨酸激酶的抑制剂
DE102008052943A1 (de) 2008-10-23 2010-04-29 Merck Patent Gmbh Azaindolderivate
JP2012509342A (ja) * 2008-11-20 2012-04-19 オーエスアイ・フアーマスーテイカルズ・インコーポレーテツド 置換ピロロ［２，３−ｂ］−ピリジンおよび−ピラジン
JP5930278B2 (ja) * 2008-11-25 2016-06-08 ユニバーシティー オブ ロチェスター Ｍｌｋ阻害剤および使用方法
WO2010065927A2 (en) * 2008-12-05 2010-06-10 California Institute Of Technology Dna-damage-induced proteolysis
ES2542873T3 (es) * 2009-02-10 2015-08-12 Monsanto Technology Llc Composiciones y procedimientos de control de nemátodos
US8129404B2 (en) * 2009-03-11 2012-03-06 Plexxikon Inc. Compounds and uses thereof
RU2011141123A (ru) 2009-03-11 2013-04-20 Плексксикон, Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-b]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ RAF-КИНАЗ
WO2010111527A1 (en) * 2009-03-26 2010-09-30 Plexxikon, Inc. Pyrazolo [ 3, 4 -b] pyridines as kinase inhibitors and their medical use
SG173178A1 (en) * 2009-04-03 2011-09-29 Hoffmann La Roche Propane- i-sulfonic acid {3- [5- (4 -chloro-phenyl) -1h-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor
KR101771401B1 (ko) 2009-05-22 2017-08-25 인사이트 홀딩스 코포레이션 야누스 키나제 억제제로서 피라졸­４­일­피롤로［２,３­ｄ］피리미딘 및 피롤­３­일­피롤로［２,３­ｄ］피리미딘의 Ｎ­(헤테로)아릴­피롤리딘 유도체
TWI484962B (zh) 2009-05-22 2015-05-21 Incyte Corp 作為ｊａｋ抑制劑之３－〔４－（７ｈ－吡咯并〔２，３－ｄ〕嘧啶－４－基）－１ｈ－吡唑－１－基〕辛烷或庚腈
US8546399B2 (en) 2009-05-26 2013-10-01 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
US20220315555A1 (en) 2009-05-26 2022-10-06 Abbvie Inc. Apoptosis inducing agents for the treatment of cancer and immune and autoimmune diseases
KR102001418B1 (ko) 2009-05-26 2019-07-19 애브비 아일랜드 언리미티드 컴퍼니 암，면역 질환 및 자가면역 질환의 치료를 위한 아폽토시스-유도제
US9034875B2 (en) 2009-05-26 2015-05-19 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
AP3631A (en) 2009-06-17 2016-03-08 Vertex Pharma Inhibitors of influenza viruses replication
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
CN102066372B (zh) 2009-08-24 2014-09-17 苏州爱斯鹏药物研发有限责任公司 含脲基的5，6元杂芳双环化合物作为激酶抑制剂
EP2470539A1 (en) 2009-08-28 2012-07-04 Array Biopharma, Inc. Raf inhibitor compounds and methods of use thereof
US20120214811A1 (en) 2009-08-28 2012-08-23 Ignacio Aliagas Raf inhibitor compounds and methods of use thereof
CN102712646A (zh) * 2009-08-28 2012-10-03 阵列生物制药公司 Raf抑制剂化合物及其使用方法
US20130018033A1 (en) 2009-08-28 2013-01-17 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
CN102712635A (zh) 2009-08-28 2012-10-03 阵列生物制药公司 用于抑制raf激酶的1h-吡唑并[3,4-b]吡啶化合物
CN102753554A (zh) 2009-08-28 2012-10-24 阵列生物制药公司 Raf抑制剂化合物及其使用方法
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011050344A2 (en) 2009-10-23 2011-04-28 Mannkind Corporation Cancer immunotherapy and method of treatment
JP2013510166A (ja) 2009-11-06 2013-03-21 プレキシコン インコーポレーテッド キナーゼ調節のための化合物、方法およびその適用
WO2011060216A1 (en) 2009-11-12 2011-05-19 Concert Pharmaceuticals Inc. Substituted azaindoles
EP2501236B1 (en) 2009-11-18 2017-03-29 Plexxikon Inc. N-[2-fluoro-3-(4-amino-7H-pyrrolo[2,3-d]pyrimidine-5-carbonyl)-phenyl]-4-benzenesulfonamide derivatives as Raf protein kinase modulators for the treatment of cancer
DE102009058280A1 (de) * 2009-12-14 2011-06-16 Merck Patent Gmbh Thiazolderivate
JP5815558B2 (ja) * 2009-12-23 2015-11-17 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼ調節のための化合物及び方法ならびにそれらの適応症
WO2011090738A2 (en) 2009-12-29 2011-07-28 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
US8618302B2 (en) 2010-01-06 2013-12-31 Joseph P. Errico Methods and compositions of targeted drug development
US8658170B2 (en) 2010-01-06 2014-02-25 Joseph P. Errico Combination therapy with MDM2 and EFGR inhibitors
MX2012009378A (es) * 2010-02-11 2012-09-12 Univ Vanderbilt Compuestos de pirazolopiridina, pirazolopirazina, pirazolopirimidina, pirazolotiofeno y pirazolotiazol como potenciadores alostericos mglur4, composiciones y metodos para tratar disfunciones neurologicas.
US11084811B2 (en) 2010-03-01 2021-08-10 Oncternal Therapeutics, Inc. Compounds for treatment of cancer
DK2545045T3 (en) 2010-03-10 2016-01-25 Incyte Holdings Corp PIPERIDINE-4-YL-azetidine derivatives AS JAK1 INHIBITORS
WO2011119842A1 (en) 2010-03-25 2011-09-29 The J. David Gladstone Institutes Compositions and methods for treating neurological disorders
CN102939282B (zh) 2010-04-16 2015-12-02 Ac免疫有限公司 用于治疗与淀粉状蛋白或淀粉状蛋白样蛋白有关的疾病的化合物
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
CA2797281A1 (en) * 2010-05-06 2011-11-10 Merck Sharp & Dohme Corp. Aza-indole derivatives useful as modulators of faah
AR081039A1 (es) 2010-05-14 2012-05-30 Osi Pharmaceuticals Llc Inhibidores biciclicos fusionados de quinasa
JP2013526570A (ja) 2010-05-14 2013-06-24 オーエスアイ・ファーマシューティカルズ，エルエルシー 縮合二環式キナーゼ阻害剤
NZ604708A (en) 2010-05-20 2015-05-29 Array Biopharma Inc Macrocyclic compounds as trk kinase inhibitors
CN103002875B (zh) 2010-05-21 2016-05-04 因塞特控股公司 Jak抑制剂的局部用制剂
EP2576566B1 (en) * 2010-05-28 2015-10-28 Merck Sharp & Dohme B.V. Thieno(2,3b)pyrazine compounds as b-raf inhibitors
AU2011261185A1 (en) 2010-06-03 2013-01-10 Pharmacyclics, Inc. The use of inhibitors of Bruton's tyrosine kinase (Btk)
CA2801834A1 (en) 2010-06-09 2011-12-15 Kathleen D'halluin Methods and means to modify a plant genome at a nucleotide sequence commonly used in plant genome engineering
US8779150B2 (en) 2010-07-21 2014-07-15 Hoffmann-La Roche Inc. Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
JP5933544B2 (ja) 2010-07-26 2016-06-08 バイオマトリカ， インコーポレーテッド 外界温度で出荷および貯蔵中の血中ｄｎａ、ｒｎａおよびタンパク質ならびに他の生体試料を安定化させるための組成物
CA2806734A1 (en) 2010-07-26 2012-02-09 Biomatrica, Inc. Compositions for stabilizing dna, rna and proteins in saliva and other biological samples during shipping and storage at ambient temperatures
US20120045433A1 (en) 2010-08-17 2012-02-23 Kapil Dhingra Combination therapy
US8709419B2 (en) 2010-08-17 2014-04-29 Hoffmann-La Roche, Inc. Combination therapy
EP2616467A1 (en) 2010-09-13 2013-07-24 Concert Pharmaceuticals Inc. Substituted azaindoles
BR112013009093B1 (pt) 2010-10-29 2022-04-19 Abbvie Inc Processo para a preparação de uma dispersão sólida contendo um agente indutor de apoptose
UA113500C2 (xx) 2010-10-29 2017-02-10 Одержані екструзією розплаву тверді дисперсії, що містять індукуючий апоптоз засіб
KR101236731B1 (ko) 2010-11-02 2013-02-25 한국과학기술원 아자인돌 화합물, 이를 포함하는 ｐｉ３ｋ 저해제용 약학 조성물 및 ｐｉ３ｋ와 연관된 질환 치료용 약학 조성물
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
US8933085B2 (en) 2010-11-19 2015-01-13 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US8722657B2 (en) 2010-11-23 2014-05-13 Abbvie Inc. Salts and crystalline forms of an apoptosis-inducing agent
KR20190109590A (ko) 2010-11-23 2019-09-25 애브비 아일랜드 언리미티드 컴퍼니 선택적인 ｂｃｌ­２ 억제제를 사용하는 치료 방법
US9296811B2 (en) 2010-12-02 2016-03-29 University of Pittsburgh—of the Commonwealth System of Higher Education Methods for treating a tumor using an antibody that specifically binds HMW-MAA
US9295669B2 (en) * 2010-12-14 2016-03-29 Hoffman La-Roche Inc. Combination therapy for proliferative disorders
WO2012083117A1 (en) 2010-12-16 2012-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
JP2014505052A (ja) 2011-01-06 2014-02-27 ベータ ファルマ カナダ インコーポレーテッド 癌の治療および予防用の新規なウレア
RS58455B1 (sr) * 2011-02-07 2019-04-30 Plexxikon Inc Jedinjenja i postupci za modulaciju kinaze, i indikacije za njih
EP2672963A4 (en) 2011-02-08 2015-06-24 Childrens Medical Center METHOD FOR THE TREATMENT OF MELANOMA
PT2675451E (pt) 2011-02-18 2015-10-16 Incyte Corp Terapia de combinação com inibidores mtor/jak
TWI558702B (zh) * 2011-02-21 2016-11-21 普雷辛肯公司 醫藥活性物質的固態形式
WO2012123504A1 (en) * 2011-03-15 2012-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Compositions and methods for inhibiting tumor development caused by chemotherapy induced senescence
ES2657750T3 (es) * 2011-04-01 2018-03-06 Genentech, Inc. Combinación de compuesto inhibidor de AKT y vemurafenib para su uso en tratamientos terapéuticos
WO2012138809A1 (en) * 2011-04-05 2012-10-11 Dawei Zhang Heterocyclic compounds as kinase inhibitors
RU2580609C2 (ru) 2011-04-18 2016-04-10 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Противоопухолевое терапевтическое средство
EP2707508A4 (en) * 2011-05-10 2015-07-29 Brunangelo Falini BIOMARKERS OF TRICHOLEUCOCYTE LEUKEMIA AND METHODS OF USE THEREOF
EP2710003A1 (en) 2011-05-16 2014-03-26 OSI Pharmaceuticals, LLC Fused bicyclic kinase inhibitors
CA2836474A1 (en) 2011-05-17 2012-11-22 Plexxikon Inc. Kinase modulation and indications therefor
JP2014515368A (ja) 2011-05-26 2014-06-30 第一三共株式会社 プロテインキナーゼ阻害剤としての複素環化合物
ES2705950T3 (es) 2011-06-03 2019-03-27 Eisai R&D Man Co Ltd Biomarcadores para predecir y valorar la capacidad de respuesta de sujetos con cáncer de tiroides y de riñón a compuestos de lenvatinib
EP2717694A4 (en) 2011-06-10 2014-11-12 Glaxosmithkline Intellectual Property Ltd NEW COMPOUNDS
MX344479B (es) 2011-06-20 2016-12-16 Incyte Holdings Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de cinasa janus (jak).
EP2731612A4 (en) 2011-07-13 2015-04-08 Pharmacyclics Inc BRUTON TYROSINE KINASE HEMMER
WO2013019906A1 (en) 2011-08-01 2013-02-07 Genentech, Inc. Methods of treating cancer using pd-1 axis binding antagonists and mek inhibitors
UA118010C2 (uk) 2011-08-01 2018-11-12 Вертекс Фармасьютікалз Інкорпорейтед Інгібітори реплікації вірусів грипу
CA2844507A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag Jak pi3k/mtor combination therapy
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
WO2013029043A1 (en) * 2011-08-25 2013-02-28 Reaction Biology Corp. Selective kinase inhibitors
JP6002223B2 (ja) 2011-08-26 2016-10-05 ニューファーマ， インコーポレイテッド 特定の化学的実体、組成物、および方法
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN104080455B (zh) * 2011-09-14 2018-07-31 润新生物公司 某些化学实体、组合物及方法
EP2570127A1 (en) 2011-09-16 2013-03-20 Sanofi Compositions and methods for treating cancer using PI3KB beta inhibitor and MAPK pathway inhibitor, including MEK and RAF inhibitors
EP2758055A1 (en) 2011-09-19 2014-07-30 F.Hoffmann-La Roche Ag Combination treatments comprising c-met antagonists and b-raf antagonists
WO2013062945A1 (en) * 2011-10-24 2013-05-02 Glaxosmithkline Intellectual Property Development Limited Chemical compounds
US9382239B2 (en) 2011-11-17 2016-07-05 Dana-Farber Cancer Institute, Inc. Inhibitors of c-Jun-N-terminal kinase (JNK)
US8377946B1 (en) 2011-12-30 2013-02-19 Pharmacyclics, Inc. Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors
EA025597B1 (ru) 2011-12-31 2017-01-30 Бейджен, Лтд. КОНДЕНСИРОВАННЫЕ ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Raf КИНАЗЫ
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
CN102603734A (zh) * 2012-01-19 2012-07-25 盛世泰科生物医药技术(苏州)有限公司 一种蛋白激酶抑制剂及其应用
EP2806874B1 (en) 2012-01-25 2017-11-15 Neupharma, Inc. Quinoxaline-oxy-phenyl derivatives as kinase inhibitors
US9216170B2 (en) 2012-03-19 2015-12-22 Hoffmann-La Roche Inc. Combination therapy for proliferative disorders
US9358235B2 (en) 2012-03-19 2016-06-07 Plexxikon Inc. Kinase modulation, and indications therefor
WO2013148365A1 (en) 2012-03-28 2013-10-03 Neuropore Therapies, Inc. Phenyl-urea and phenyl-carbamate derivatives as inhibitors of protein aggregation
KR102096679B1 (ko) * 2012-04-23 2020-04-02 제넨테크, 인크. 화합물의 제조를 위한 중간체 및 방법
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
EP2858501A4 (en) * 2012-05-22 2015-12-09 Merck Sharp & Dohme TRK-A KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
US10077474B2 (en) * 2012-05-29 2018-09-18 Abbott Molecular, Inc. Method of designing primers, method of detecting single nucleotide polymorphisms (SNPs), method of distinguishing SNPs, and related primers, detectable oligonucleotides, and kits
WO2013178591A1 (en) 2012-05-31 2013-12-05 F. Hoffmann-La Roche Ag Aminoquinazoline and pyridopyrimidine derivatives
US9150570B2 (en) 2012-05-31 2015-10-06 Plexxikon Inc. Synthesis of heterocyclic compounds
CA3218491A1 (en) 2012-06-04 2013-12-12 Pharmacyclics Llc Crystalline forms of a bruton's tyrosine kinase inhibitor
EP2870154A1 (en) 2012-07-03 2015-05-13 Ratiopharm GmbH Solid state form of vemurafenib choline salt
KR20180088926A (ko) 2012-07-24 2018-08-07 파마싸이클릭스 엘엘씨 브루톤 티로신 키나제(btk)의 억제제에 대한 내성과 관련된 돌연변이
SG11201500883YA (en) * 2012-08-07 2015-04-29 Aurigene Discovery Tech Ltd 5-(1H-PYRAZOL-4-YL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
SG11201500582UA (en) 2012-08-17 2015-04-29 Hoffmann La Roche Combination therapies for melanoma comprising administering cobimetinib and vemurafinib
TWI601725B (zh) * 2012-08-27 2017-10-11 加拓科學公司 取代的氮雜吲哚化合物及其鹽、組合物和用途
CN103626765B (zh) * 2012-08-27 2016-08-10 广东东阳光药业有限公司 取代的氮杂吲哚化合物及其盐、组合物和用途
JP6318156B2 (ja) 2012-09-06 2018-04-25 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． キナーゼをモジュレートするための化合物および方法、ならびにその指標
CN104812389B (zh) 2012-09-24 2020-07-17 润新生物公司 某些化学实体、组合物及方法
CN103613591B (zh) * 2012-09-29 2016-04-13 上海科州药物研发有限公司 作为cMet抑制剂的化合物及其制备方法和用途
WO2014053968A1 (en) 2012-10-04 2014-04-10 Pfizer Limited Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors
US9566281B2 (en) * 2012-10-08 2017-02-14 Atriva Therapeutics Gmbh MEK inhibitors in the treatment of virus diseases
EP2909194A1 (en) 2012-10-18 2015-08-26 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
USRE48175E1 (en) 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
EP2916838B1 (en) 2012-11-12 2019-03-13 Neupharma, Inc. Certain chemical entities, compositions, and methods
JP2015537033A (ja) 2012-11-15 2015-12-24 ファーマサイクリックス，インク． キナーゼ阻害剤としてのピロロピリミジン化合物
KR20210037012A (ko) 2012-11-15 2021-04-05 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
US9260426B2 (en) 2012-12-14 2016-02-16 Arrien Pharmaceuticals Llc Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors
EP2934572A4 (en) 2012-12-20 2016-11-23 Biomatrica Inc FORMULATIONS AND METHODS FOR STABILIZING PCR REAGENTS
ES2664985T3 (es) 2012-12-21 2018-04-24 Plexxikon Inc. Compuestos y métodos para modulación de quinasa, e indicaciones de los mismos
JPWO2014098176A1 (ja) 2012-12-21 2017-01-12 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体のアモルファス及びその製造方法
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉｍキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
KR102311840B1 (ko) 2013-01-15 2021-10-14 인사이트 홀딩스 코포레이션 Pim 키나제 저해제로서 유용한 티아졸카복스아마이드 및 피리딘카복스아마이드 화합물
US20140357636A1 (en) * 2013-02-21 2014-12-04 Wayne Rothbaum Treatment of Skeletal-Related Disorders
WO2014128235A1 (en) 2013-02-22 2014-08-28 F. Hoffmann-La Roche Ag Methods of treating cancer and preventing drug resistance
CN109568312A (zh) * 2013-03-05 2019-04-05 田纳西大学研究基金会 用于治疗癌症的化合物
CA2903418C (en) 2013-03-06 2021-03-23 Incyte Corporation Processes and intermediates for making a jak inhibitor
CN105008356A (zh) 2013-03-14 2015-10-28 拉蒂奥法姆有限责任公司 固态形式的盐酸威罗菲尼
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
CN105339001A (zh) 2013-03-15 2016-02-17 基因泰克公司 治疗癌症和预防癌症耐药性的方法
AU2014230098A1 (en) 2013-03-15 2015-10-01 Sanofi Anti-tumoral composition comprising a PI3kbeta inhibitor and a RAF inhibitor, to overcome cancer cells resistance
KR102244719B1 (ko) 2013-03-15 2021-04-26 플렉시콘 인코퍼레이티드 헤테로시클릭 화합물 및 그의 용도
US9206188B2 (en) * 2013-04-18 2015-12-08 Arrien Pharmaceuticals Llc Substituted pyrrolo[2,3-b]pyridines as ITK and JAK inhibitors
KR102204279B1 (ko) 2013-05-14 2021-01-15 에자이 알앤드디 매니지먼트 가부시키가이샤 자궁내막암 대상의 렌바티닙 화합물에 대한 반응성을 예측 및 평가하기 위한 생체표지
KR20160013028A (ko) 2013-05-30 2016-02-03 플렉시콘, 인코퍼레이티드 키나제 조정을 위한 화합물 및 그에 대한 적응증
JP6604942B2 (ja) 2013-06-13 2019-11-13 バイオマトリカ，インク． 細胞安定化
EP3013797B1 (en) 2013-06-28 2018-01-03 BeiGene, Ltd. Fused tricyclic amide compounds as multiple kinase inhibitors
JP6568060B2 (ja) * 2013-07-12 2019-08-28 ピラマル エンタープライズイズ リミテッド 黒色腫の治療のための組合せ医薬
TWI649081B (zh) 2013-08-02 2019-02-01 製藥公司 治療固態腫瘤之方法
BR122020001831A8 (pt) 2013-08-07 2023-01-24 Incyte Corp {1-{1-[3-flúor-2-(trifluormetil)isonicotinol]piperidin-4-il}-3-[4-(7h-pirrolo[2,3-d]primidin-4-il) -1h-pirazol-1-il]azetidin-3-il}acetonitrila, seu uso, formas de dosagem de liberação sustentada e doses
WO2015023703A1 (en) 2013-08-12 2015-02-19 Pharmacyclics, Inc. Methods for the treatment of her2 amplified cancer
TW201605866A (zh) 2013-08-23 2016-02-16 英塞特公司 可用作ｐｉｍ激酶抑制劑之呋喃并－及噻吩并－吡啶甲醯胺化合物
US9629851B2 (en) 2013-09-20 2017-04-25 Stitching Het Nederlands Kanker Institut—Antoni Van Leeuwenhoek Ziekenhuis ROCK in combination with MAPK pathway
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
BR112016006978A2 (pt) 2013-09-30 2017-08-01 Pharmacyclics Llc inibidores de tirosina quinase de bruton
WO2015058126A1 (en) 2013-10-18 2015-04-23 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of prolferative diseases
WO2015058140A1 (en) 2013-10-18 2015-04-23 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
KR102338461B1 (ko) 2013-11-13 2021-12-13 버텍스 파마슈티칼스 인코포레이티드 인플루엔자 바이러스 복제 억제제의 제조 방법
RU2700415C1 (ru) 2013-11-13 2019-09-17 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы репликации вирусов гриппа
KR20160110357A (ko) 2013-11-15 2016-09-21 더 위스타 인스티튜트 오브 아나토미 앤드 바이올로지 Ｅｂｎａ１ 억제제 및 그의 사용 방법
WO2015075749A1 (en) * 2013-11-22 2015-05-28 Laurus Labs Private Limited Novel processes for the preparation of vemurafenib
CZ2013943A3 (cs) 2013-11-27 2015-06-03 Zentiva, K.S. Krystalické formy vemurafenibu
CN104710417B (zh) * 2013-12-11 2020-09-08 上海科州药物研发有限公司 氮杂吲哚类衍生物及其合成方法
US10668055B2 (en) * 2013-12-20 2020-06-02 Biomed Valley Discoveries, Inc. Cancer treatment using combinations of ERK and RAF inhibitors
CN104739823A (zh) * 2013-12-28 2015-07-01 复旦大学附属华山医院 淫羊藿素在制备维罗非尼增敏剂中的用途
CA2935804A1 (en) 2014-01-14 2015-07-23 Dana-Farber Cancer Institute, Inc. Compositions and methods for identification, assessment, prevention, and treatment of melanoma using pd-l1 isoforms
WO2015134536A1 (en) 2014-03-04 2015-09-11 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CA2942528A1 (en) 2014-03-20 2015-09-24 Pharmacyclics Inc. Phospholipase c gamma 2 and resistance associated mutations
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
US9862688B2 (en) 2014-04-23 2018-01-09 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
US10017477B2 (en) 2014-04-23 2018-07-10 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
JP2017514866A (ja) * 2014-05-06 2017-06-08 ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア Ｂｒａｆ阻害剤を使用する創傷治癒
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
WO2015181628A1 (en) * 2014-05-27 2015-12-03 Eisai R&D Management Co., Ltd. Treatment of acute myeloid leukemia with an hck inhibitor
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
TW201613916A (en) * 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CN106572650B (zh) 2014-06-10 2021-08-31 生物马特里卡公司 在环境温度下稳定凝血细胞
WO2015191986A1 (en) 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
WO2015191996A1 (en) * 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
WO2015196072A2 (en) 2014-06-19 2015-12-23 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
AR101106A1 (es) 2014-07-02 2016-11-23 Pharmacyclics Llc Inhibidores de tirosina quinasa de bruton
CN105777756B (zh) * 2014-07-02 2019-03-01 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用
US9822124B2 (en) 2014-07-14 2017-11-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as Pim kinase inhibitors
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
EP3563870A1 (en) 2014-07-15 2019-11-06 F. Hoffmann-La Roche AG Methods of treating cancer using pd-1 axis binding antagonists and mek inhibitors
EP3174539A4 (en) 2014-08-01 2017-12-13 Pharmacyclics, LLC Inhibitors of bruton's tyrosine kinase
CN106573002A (zh) 2014-08-07 2017-04-19 药品循环有限责任公司 布鲁顿氏酪氨酸激酶抑制剂的新型制剂
EP3825305A1 (en) 2014-08-28 2021-05-26 Eisai R&D Management Co., Ltd. Process for preparing lenvatinib
CA2961356C (en) 2014-09-15 2023-03-07 Plexxikon Inc. Heterocyclic compounds and their uses in modulating bromodomain and for treating diseases or conditions relevant thereto
JP6499282B2 (ja) 2014-09-26 2019-04-10 ギリアード サイエンシーズ， インコーポレイテッド Ｔａｎｋ結合キナーゼ阻害剤化合物として有用なアミノトリアジン誘導体
CA2963091A1 (en) 2014-10-06 2016-04-14 Dana-Farber Cancer Institute, Inc. Angiopoietin-2 biomarkers predictive of anti-immune checkpoint response
US10611765B2 (en) 2014-11-06 2020-04-07 Ohio State Innovation Foundation Pyrrolopyrimidine derivatives as Mps1/TTK kinase inhibitors
WO2016083956A1 (en) * 2014-11-29 2016-06-02 Shilpa Medicare Limited Substantially pure vemurafenib and its salts
JP6815318B2 (ja) * 2014-12-23 2021-01-20 ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド 二官能性分子によって標的化タンパク質分解を誘導する方法
US9694084B2 (en) 2014-12-23 2017-07-04 Dana-Farber Cancer Institute, Inc. Methods to induce targeted protein degradation through bifunctional molecules
CA2972239A1 (en) 2014-12-23 2016-06-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016136745A1 (ja) 2015-02-25 2016-09-01 エーザイ・アール・アンド・ディー・マネジメント株式会社 キノリン誘導体の苦味抑制方法
IL315294A (en) 2015-03-03 2024-10-01 Pharmacyclics Llc Pharmaceutical formulations of proton tyrosine kinase inhibitor
AU2015384801B2 (en) 2015-03-04 2022-01-06 Eisai R&D Management Co., Ltd. Combination of a PD-1 antagonist and a VEGFR/FGFR/RET tyrosine kinase inhibitor for treating cancer
EP3273966B1 (en) 2015-03-27 2023-05-03 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
US10160755B2 (en) 2015-04-08 2018-12-25 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
CZ2015250A3 (cs) 2015-04-14 2016-10-26 Zentiva, K.S. Amorfní formy vemurafenibu
AU2016258027B2 (en) 2015-05-06 2019-11-21 Daiichi Sankyo, Inc. Solid forms of a compound modulating kinases
EP3581573B1 (en) 2015-05-06 2022-07-06 Plexxikon Inc. Synthesis of a compound that modulates kinases
EP3294717B1 (en) 2015-05-13 2020-07-29 Vertex Pharmaceuticals Inc. Methods of preparing inhibitors of influenza viruses replication
WO2016183120A1 (en) 2015-05-13 2016-11-17 Vertex Pharmaceuticals Incorporated Inhibitors of influenza viruses replication
US10442763B2 (en) 2015-05-14 2019-10-15 The Wistar Institute Of Anatomy And Biology EBNA1 inhibitors and methods using same
US9814714B2 (en) 2015-05-22 2017-11-14 Plexxikon Inc. Kinase modulation, and indications therefor
JP6722200B2 (ja) 2015-05-22 2020-07-15 プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． 複素環化合物の合成
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
WO2016200851A1 (en) * 2015-06-09 2016-12-15 Abbvie Inc. Nuclear receptor modulators
AU2016276963C1 (en) 2015-06-12 2021-08-05 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
BR112017027227B1 (pt) 2015-06-16 2023-12-12 Eisai R&D Management Co., Ltd Agente anti-câncer
AU2016291676B2 (en) 2015-07-16 2020-04-30 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as RET kinase inhibitors
MX2018000880A (es) * 2015-07-20 2018-08-24 Genzyme Corp Inhibidores del receptor del factor estimulante de colonias 1 (csf-1r).
US10829484B2 (en) 2015-07-28 2020-11-10 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US10729669B2 (en) * 2015-07-28 2020-08-04 University Of Iowa Research Foundation Compositions and methods for treating cancer
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
KR20180052757A (ko) 2015-09-21 2018-05-18 플렉시콘 인코퍼레이티드 헤테로시클릭 화합물 및 그의 용도
TW201718546A (zh) 2015-10-02 2017-06-01 英塞特公司 適用作pim激酶抑制劑之雜環化合物
WO2017066193A1 (en) 2015-10-15 2017-04-20 Princeton Drug Discovery, Llc Novel inhibitors of protein kinases
RU2744852C2 (ru) 2015-10-26 2021-03-16 Локсо Онколоджи, Инк. Точечные мутации в устойчивых к ингибитору trk злокачественных опухолях и связанные с ними способы
MX2018006152A (es) 2015-11-19 2018-09-17 Genentech Inc Metodos para el tratamiento de cancer utilizando inhibidores b-raf e inhibidores de punto de control inmunologico.
RU2018123825A (ru) 2015-12-07 2020-01-15 Плексксикон Инк. Соединения и способы для модуляции киназ, и показания для этого
KR20230145258A (ko) 2015-12-08 2023-10-17 바이오매트리카 인코포레이티드 적혈구 침강 속도의 감소
EP3391643A4 (en) 2015-12-14 2019-07-31 Red.Com, Llc MODULAR DIGITAL CAMERA AND MOBILE PHONE
EP3394044A1 (en) 2015-12-17 2018-10-31 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
US10513528B2 (en) * 2016-02-25 2019-12-24 Taxis Pharmaceuticals, Inc. Synthetic processes and intermediates
AU2017232610B2 (en) 2016-03-16 2021-07-22 Plexxikon Inc. Compounds and methods for kinase modulation and indications therefore
CR20180501A (es) 2016-04-04 2019-04-05 Loxo Oncology Inc Formulaciones liquidas de (s)-n-(5-((r)-2(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a] pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
LT3439663T (lt) 2016-04-04 2024-10-10 Loxo Oncology, Inc. Vaikų vėžio gydymo būdai
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX2018012471A (es) 2016-04-15 2019-02-21 Genentech Inc Metodos de diagnostico y terapeuticos para el cancer.
SI3458456T1 (sl) 2016-05-18 2021-04-30 Loxo Oncology, Inc. Priprava (S)-N-(5-((R)-2-(2,5-difluorofenil) pirolidin-1-il) pirazolo (1,5-A) pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
RU2768479C2 (ru) * 2016-06-13 2022-03-24 Хемоцентрикс, Инк. Способы лечения рака поджелудочной железы
WO2017223565A1 (en) 2016-06-24 2017-12-28 University Of Iowa Research Foundation Compositions and methods of treating melanoma
WO2018002415A1 (en) 2016-07-01 2018-01-04 Fermion Oy New processes for the preparation of vemurafenib
TWI806832B (zh) 2016-07-12 2023-07-01 美商銳新醫藥公司 作為異位shp2抑制劑之2,5-雙取代型3-甲基吡嗪及2,5,6-三取代型3-甲基吡嗪
AU2017326116B2 (en) * 2016-09-16 2020-10-22 Helmholtz Zentrum Muenchen - Deutsches Forschungszentrum Für Gesundheit Und Umwelt (Gmbh) TRAF 6 inhibitors
TW201815766A (zh) 2016-09-22 2018-05-01 美商普雷辛肯公司 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
EP3308773A1 (en) 2016-10-11 2018-04-18 Recordati Industria Chimica E Farmaceutica SPA Formulations of cysteamine and cysteamine derivatives
US11672801B2 (en) 2016-10-19 2023-06-13 United States Government As Represented By The Department Of Veterans Affairs Compositions and methods for treating cancer
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
KR20240130832A (ko) 2016-11-23 2024-08-29 케모센트릭스, 인크. 국소 분절 사구체경화증의 치료 방법
US11758928B2 (en) 2016-12-15 2023-09-19 Société des Produits Nestlé S.A. Compositions and methods that modulate phosphorus or enzymes in a companion animal
US10703757B2 (en) 2016-12-23 2020-07-07 Plexxikon Inc. Compounds and methods for CDK8 modulation and indications therefor
AU2017382436C1 (en) 2016-12-23 2021-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of Rapidly Accelerated Fibrosarcoma polypeptides
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
WO2018134254A1 (en) 2017-01-17 2018-07-26 Heparegenix Gmbh Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
WO2018136661A1 (en) 2017-01-18 2018-07-26 Andrews Steven W SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS
CA3051054A1 (en) 2017-01-23 2018-07-26 Revolution Medicines, Inc. Pyridine compounds as allosteric shp2 inhibitors
CN110446709B (zh) 2017-01-23 2023-09-12 锐新医药公司 作为变构shp2抑制剂的二环化合物
US11471538B2 (en) 2017-02-10 2022-10-18 INSERM (Institut National de la Santéet de la Recherche Medicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the MAPK pathway
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
EP3601326A4 (en) * 2017-03-20 2020-12-16 The Broad Institute, Inc. COMPOUNDS AND METHODS OF REGULATING INSULIN SECRETION
CA3056777A1 (en) 2017-03-20 2018-09-27 Plexxikon Inc. Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain
WO2018183762A1 (en) * 2017-03-29 2018-10-04 United States Government As Represented By The Department Of Veterans Affairs Methods and compositions for treating cancer
WO2018183917A1 (en) 2017-03-30 2018-10-04 Taxis Pharmaceuticals, Inc. Synthetic processes and synthetic intermediates
WO2018200981A1 (en) * 2017-04-28 2018-11-01 Quartz Therapeutics, Inc. Raf-degrading conjugate compounds
WO2018210661A1 (en) * 2017-05-15 2018-11-22 Basf Se Heteroaryl compounds as agrochemical fungicides
CA3063535A1 (en) 2017-05-19 2018-11-22 Nflection Therapeutics, Inc. Fused heteroaromatic-aniline compounds for treatment of dermal disorders
MX2019013561A (es) 2017-05-19 2022-02-09 Nflection Therapeutics Inc Compuestos de pirrolopiridina-anilina para el tratamiento de trastornos dermicos.
US10428067B2 (en) 2017-06-07 2019-10-01 Plexxikon Inc. Compounds and methods for kinase modulation
KR20240033119A (ko) 2017-06-30 2024-03-12 더 리전트 오브 더 유니버시티 오브 캘리포니아 모발 성장을 조절하기 위한 조성물 및 방법
KR102615829B1 (ko) 2017-07-25 2023-12-20 플렉시콘 인코퍼레이티드 키나제를 조정하는 화합물의 제제
CN109384785B (zh) * 2017-08-10 2021-09-28 浙江海正药业股份有限公司 吡咯并吡啶酮类衍生物、其制备方法及其在医药上的用途
EP3679159A1 (en) 2017-09-08 2020-07-15 H. Hoffnabb-La Roche Ag Diagnostic and therapeutic methods for cancer
TW202410896A (zh) 2017-10-10 2024-03-16 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
EP3694504A4 (en) 2017-10-11 2021-07-14 ChemoCentryx, Inc. TREATMENT OF FOCAL SEGMENTAL GLOMERULOSCLEROSIS WITH CRC2 ANTAGONISTS
RU2020115095A (ru) 2017-10-12 2021-11-12 Революшн Медсинз, Инк. Пиридиновые, пиразиновые и триазиновые соединения в качестве аллостерических ингибиторов shp2
CN111194318B (zh) 2017-10-13 2023-06-09 Opna生物公司 用于调节激酶的化合物固体形式
EP4245758A3 (en) 2017-10-26 2023-12-20 Xynomic Pharmaceuticals, Inc. Crystalline salts of a b-raf kinase inhibitor
KR20200078566A (ko) 2017-10-27 2020-07-01 플렉시콘 인코퍼레이티드 키나제를 조정하는 화합물의 제제
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
BR112020009757A2 (pt) 2017-12-15 2020-11-03 Revolution Medicines, Inc. compostos policíclicos como inibidores alostéricos de shp2
US11725185B2 (en) 2017-12-28 2023-08-15 University Of Houston System Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
TWI802635B (zh) 2018-01-18 2023-05-21 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡咯并[2,3-d]嘧啶化合物
US11524963B2 (en) 2018-01-18 2022-12-13 Array Biopharma Inc. Substituted pyrazolo[3,4-d]pyrimidines as RET kinase inhibitors
US11472802B2 (en) 2018-01-18 2022-10-18 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridine compounds as RET kinase inhibitors
CN112105608B (zh) 2018-01-30 2023-07-14 因赛特公司 制备(1-(3-氟-2-(三氟甲基)异烟碱基)哌啶-4-酮)的方法
AU2019216264B2 (en) 2018-01-31 2023-08-31 Heparegenix Gmbh Protein kinase MKK4 inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
EP3752200A1 (en) 2018-02-13 2020-12-23 Vib Vzw Targeting minimal residual disease in cancer with rxr antagonists
US11149011B2 (en) 2018-03-20 2021-10-19 Plexxikon Inc. Compounds and methods for IDO and TDO modulation, and indications therefor
US11304949B2 (en) 2018-03-30 2022-04-19 Incyte Corporation Treatment of hidradenitis suppurativa using JAK inhibitors
EP3774767A1 (en) 2018-04-05 2021-02-17 Beth Israel Deaconess Medical Center, Inc. Aryl hydrocarbon receptor modulators and uses thereof
EP3560516A1 (en) * 2018-04-27 2019-10-30 Bergen Teknologioverforing AS Combination therapy including beta-sitosterol in combination with at least one of a braf inhibitor, a mek inhibitor or an erk inhibitor and methods and use thereof
US11242338B2 (en) 2018-05-17 2022-02-08 The Wistar Institute EBNA1 inhibitor crystalline forms, and methods of preparing and using same
GB201808321D0 (en) * 2018-05-21 2018-07-11 Univ College Dublin Nat Univ Ireland Dublin Compositions and uses thereof
RU2687107C1 (ru) * 2018-06-18 2019-05-07 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" Ингибитор braf киназы n-(3-(5-(4-хлорофенил)-1h-пиразоло[3,4-b]пиридин-3-карбонил)-2,4-дифторофенил) пропан-1-сульфонамид
WO2019243315A1 (en) 2018-06-21 2019-12-26 Heparegenix Gmbh Tricyclic protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death
WO2020010364A1 (en) * 2018-07-06 2020-01-09 The Regents Of The University Of Colorado, A Body Corporate Genetically encoded system for constructing and detecting biologically active agents
CN112424201B (zh) * 2018-07-16 2024-04-02 海帕瑞吉尼克斯股份有限公司 促进肝再生或者减少或预防肝细胞死亡的蛋白激酶抑制剂
KR102592556B1 (ko) * 2018-07-19 2023-10-23 썬전 링팡 바이오테크 컴퍼니 리미티드 아자인돌 유도체 및 이의 FGFR과 C-Met 억제제로서의 용도
CN117281803A (zh) 2018-07-31 2023-12-26 罗索肿瘤学公司 喷雾干燥的分散体和制剂
CN112996794A (zh) 2018-09-10 2021-06-18 阿雷生物药品公司 作为ret激酶抑制剂的稠合杂环化合物
WO2020070390A1 (en) 2018-10-03 2020-04-09 Jyväskylän Yliopisto Vemurafenib and salts thereof for use in the treatment of enteroviral infections
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN112867803A (zh) 2018-10-16 2021-05-28 诺华股份有限公司 单独的或与免疫标志物组合的肿瘤突变负荷作为生物标志物用于预测对靶向疗法的应答
SG11202104404XA (en) * 2018-11-16 2021-05-28 California Inst Of Techn Erk inhibitors and uses thereof
CA3120371A1 (en) 2018-11-20 2020-05-28 Nflection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
CN113166097A (zh) * 2018-12-03 2021-07-23 默克专利股份公司 作为端锚聚合酶抑制剂的4-杂芳基羰基-n-(苯基或杂芳基)哌啶-1-甲酰胺
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
WO2020165062A1 (en) * 2019-02-11 2020-08-20 Merck Patent Gmbh Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
EP3953351A1 (en) 2019-04-09 2022-02-16 Plexxikon Inc. Condensed azines for ep300 or cbp modulation and indications therefor
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020243519A1 (en) * 2019-05-29 2020-12-03 Ifm Due, Inc. Compounds and compositions for treating conditions associated with sting activity
MX2021014674A (es) * 2019-05-31 2022-01-11 Fochon Biosciences Ltd Pirrolo [2,3-b] piridina sustituida y derivados de pirazolo [3,4-b] piridina como inhibidores de proteinas quinasas.
MX2022001115A (es) 2019-07-29 2022-05-03 Heparegenix Gmbh Inhibidores de proteina quinasa de pirazolo-piridina sustituida con heteroarilo para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocito.
JP2023509260A (ja) 2019-08-14 2023-03-08 インサイト・コーポレイション Ｃｄｋ２阻害剤としてのイミダゾリルピリミジニルアミン化合物
WO2021067749A2 (en) * 2019-10-02 2021-04-08 The Board Of Trustees Of The Leland Stanford Junior University Methods and compositions for the treatment of osteoarthritis
AR120184A1 (es) 2019-10-11 2022-02-02 Incyte Corp Aminas bicíclicas como inhibidoras de la cdk2
CN111004210A (zh) * 2019-10-23 2020-04-14 中山大学 化合物单晶及其制备方法
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
TW202136240A (zh) 2019-12-19 2021-10-01 美商亞文納營運公司 用於靶向降解雄激素受體之化合物及方法
CA3161339A1 (en) 2019-12-27 2021-07-01 Schrodinger, Inc. Cyclic compounds and methods of using same
JP2023509760A (ja) 2020-01-08 2023-03-09 シンシス セラピューティクス，インコーポレイテッド Ａｌｋ５阻害剤複合体およびその使用
EP4090659B1 (en) 2020-01-15 2024-06-12 HepaRegeniX GmbH 3-benzoyl-1h-pyrrolo[2,3-b]pyridine derivatives as mkk4 inhibitors for treating liver diseases
WO2021145729A1 (en) * 2020-01-17 2021-07-22 Daegu-Gyeongbuk Medical Innovation Foundation Novel compound, preparation method thereof, and use thereof
AU2021213317A1 (en) 2020-01-28 2022-06-30 Centre National De La Recherche Scientifique Antisense oligonucleotide targeting LINC00518 for treating melanoma
WO2021211882A1 (en) * 2020-04-15 2021-10-21 Pyramid Biosciences, Inc. Methods for preparing tyrosine receptor kinase inhibitors
CA3177522A1 (en) 2020-04-23 2021-10-28 Opna Immuno-Oncology Sa Compounds and methods for cd73 modulation and indications therefor
KR20210135092A (ko) * 2020-05-04 2021-11-12 아주대학교산학협력단 톨-유사 수용체 7/9 억제 기능이 있는 길항성 소분자 화합물
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US11529335B2 (en) 2020-07-31 2022-12-20 University Of Iowa Research Foundation Compositions and methods for treating cancer
WO2022040512A1 (en) 2020-08-21 2022-02-24 Plexxikon Inc. Combinational drug anticancer therapies
US20230365584A1 (en) 2020-09-10 2023-11-16 Schrödinger, Inc. Heterocyclic pericondensed cdc7 kinase inhibitors for the treatment of cancer
US20240360154A1 (en) * 2020-09-23 2024-10-31 Genfleet Therapeutics (Shanghai) Inc. Aroyl substituted tricyclic compound, preparation method therefor and use thereof
CN114478528A (zh) * 2020-10-28 2022-05-13 劲方医药科技(上海)有限公司 芳甲酰取代的三环化合物及其制法和用途
CN116568686A (zh) * 2020-11-17 2023-08-08 重庆复尚源创医药技术有限公司 作为蛋白激酶抑制剂的取代的吡咯并[2,3-b]吡啶及吡唑并[3,4-b]吡啶衍生物
WO2022121900A1 (zh) * 2020-12-07 2022-06-16 南京明德新药研发有限公司 吡咯并吡啶类化合物及其应用
EP4255420A1 (en) * 2020-12-07 2023-10-11 Lieber Institute, Inc. Compounds for inhibiting inositol hexakisphosphate kinase (ip6k) and methods of use thereof
JP2024500919A (ja) 2020-12-23 2024-01-10 ジェンザイム・コーポレーション 重水素化コロニー刺激因子－１受容体（ｃｓｆ－１ｒ）阻害剤
US20240148732A1 (en) 2021-01-26 2024-05-09 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disorders
CN112574200B (zh) * 2021-02-26 2021-06-11 安润医药科技（苏州）有限公司 Btk和/或btk的突变体c481s的小分子抑制剂
CN115073469B (zh) * 2021-03-15 2023-12-22 药雅科技(上海)有限公司 吡咯并嘧啶类化合物作为激酶抑制剂的制备及其应用
US20240310266A1 (en) 2021-03-18 2024-09-19 Novartis Ag Biomarkers for cancer and methods of use thereof
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
TW202304890A (zh) * 2021-04-14 2023-02-01 美商百歐克斯製藥公司 Klk5雙環雜芳香族抑制劑
KR102635126B1 (ko) 2021-05-27 2024-02-13 한국과학기술연구원 엑토뉴클레오티드 피로포스파타아제-포스포디에스터라아제의 저해 활성을 갖는 신규한 피롤로피리미딘 유도체 및 이들의 용도
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023059786A1 (en) * 2021-10-06 2023-04-13 H. Lee Moffitt Cancer Center And Research Institute, Inc. Inhibitors of ulk1 and methods of use
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023174300A1 (zh) * 2022-03-15 2023-09-21 劲方医药科技(上海)有限公司 Btk抑制剂的晶型及其酸式盐和其酸式盐的晶型
WO2023178240A2 (en) * 2022-03-16 2023-09-21 The Children's Medical Center Corporation Pyk2 inhibition modulates immune cell function
WO2024003350A1 (en) 2022-06-30 2024-01-04 Universite De Strasbourg Combination therapy for melanoma
CN115141197B (zh) * 2022-07-27 2024-03-26 安徽医科大学 一种3-芳杂环取代苯基衍生物及其制备方法与用途
WO2024033381A1 (en) 2022-08-10 2024-02-15 Vib Vzw Inhibition of tcf4/itf2 in the treatment of cancer
WO2024054591A1 (en) 2022-09-07 2024-03-14 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
WO2024111671A1 (ja) * 2022-11-25 2024-05-30 ゼノリス プライベート リミテッド 核酸アプタマー
CN115991705A (zh) * 2022-12-26 2023-04-21 安徽医科大学 3-(1H吡咯并[2,3-b]吡啶-5-基)苯甲酰基衍生物及其制备与应用

Family Cites Families (166)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3124610A (en) * 1964-03-10 Preparation of intermediates
US2234705A (en) * 1940-04-12 1941-03-11 Eastman Kodak Co Cellulose organic derivative composition containing esters of monoalkoxy benzoic acids
US2413258A (en) * 1942-07-07 1946-12-24 United Gas Improvement Co Polystyrene-type resins plasticized with high boiling fatty acid alkyl esters
US3067237A (en) * 1959-04-14 1962-12-04 Sterling Drug Inc Lower-alkyl mono-or bis-(alkanesulfonamido) benzoate esters
GB1141949A (en) 1966-02-23 1969-02-05 Sterling Drug Inc 7-azaindole derivatives
DE1668420B2 (de) * 1966-10-21 1976-11-25 Minnesota Mining and Manufacturing Co., Saint Paul, Minn. (V.StA.) Trifluormethylsulfonanilide, verfahren zu ihrer herstellung und ihre verwendung
DE2413258A1 (de) * 1974-03-20 1975-10-02 Bayer Ag Alkoxycarbonylphenylharnstoffe, verfahren zu ihrer herstellung und ihre verwendung als herbizide
IL46853A0 (en) * 1974-03-20 1975-05-22 Bayer Ag Novel alkoxycarbonylphenylureas,their preparation and their use as herbicides
GB1573212A (en) 1976-04-15 1980-08-20 Technicon Instr Immunoassay for gentamicin
US4301159A (en) * 1980-06-20 1981-11-17 Shionogi & Co., Ltd. N-(Diethylaminoethyl)-2-alkoxy-benzamide derivatives
AU547405B2 (en) * 1981-07-08 1985-10-17 Sanofi Amidobenzamides
US4664504A (en) * 1983-01-20 1987-05-12 Tokyo Shibaura Denki Kabushiki Kaisha Image forming apparatus
US4568649A (en) 1983-02-22 1986-02-04 Immunex Corporation Immediate ligand detection assay
US4626513A (en) 1983-11-10 1986-12-02 Massachusetts General Hospital Method and apparatus for ligand detection
DE3484294D1 (de) * 1983-11-14 1991-04-25 Dow Chemical Co 1,2,4-triazolo(1,5-a)pyrimidin-2-sulfonamide und zubereitungen und methode zur bekaempfung unerwuenschter pflanzen und die nitrierung von ammonium-stickstoff im boden.
AU567140B2 (en) * 1984-01-06 1987-11-12 Shionogi & Co., Ltd. Sulphonamido-benzamide derivatives
DE3483099D1 (de) 1984-03-15 1990-10-04 Immunex Corp Test zur sofortigen feststellung von liganden, testsatz und seine herstellung.
IT1196133B (it) * 1984-06-06 1988-11-10 Ausonia Farma Srl Derivati furanici con attivita' antiulcera
US4714693A (en) 1986-04-03 1987-12-22 Uop Inc. Method of making a catalyst composition comprising uniform size metal components on carrier
US5688655A (en) * 1988-02-10 1997-11-18 Ict Pharmaceuticals, Inc. Method of screening for protein inhibitors and activators
US6054270A (en) * 1988-05-03 2000-04-25 Oxford Gene Technology Limited Analying polynucleotide sequences
US5700637A (en) * 1988-05-03 1997-12-23 Isis Innovation Limited Apparatus and method for analyzing polynucleotide sequences and method of generating oligonucleotide arrays
US5658775A (en) * 1988-05-17 1997-08-19 Sloan-Kettering Institute For Cancer Research Double copy retroviral vector
JP3082204B2 (ja) * 1988-09-01 2000-08-28 ホワイトヘッド・インスティチュート・フォー・バイオメディカル・リサーチ 両栄養性および環境栄養性宿主域を持つ組換え体レトロウイルス
US5703055A (en) * 1989-03-21 1997-12-30 Wisconsin Alumni Research Foundation Generation of antibodies through lipid mediated DNA delivery
US5744101A (en) * 1989-06-07 1998-04-28 Affymax Technologies N.V. Photolabile nucleoside protecting groups
US5800992A (en) * 1989-06-07 1998-09-01 Fodor; Stephen P.A. Method of detecting nucleic acids
US5143854A (en) * 1989-06-07 1992-09-01 Affymax Technologies N.V. Large scale photolithographic solid phase synthesis of polypeptides and receptor binding screening thereof
US5527681A (en) * 1989-06-07 1996-06-18 Affymax Technologies N.V. Immobilized molecular synthesis of systematically substituted compounds
US5360822A (en) * 1990-02-07 1994-11-01 Nippon Shinyaku Co. Ltd. Sulfonanilide derivatives and medicine
WO1991018088A1 (en) * 1990-05-23 1991-11-28 The United States Of America, Represented By The Secretary, United States Department Of Commerce Adeno-associated virus (aav)-based eucaryotic vectors
DE4022414A1 (de) * 1990-07-13 1992-01-16 Bayer Ag Substituierte pyrrolo-pyridine
US5124335A (en) 1991-01-30 1992-06-23 Merck & Co., Inc. Substituted pyrollo-fused 6 membered heterocycles as angiotensin ii antagonists
WO1993002556A1 (en) * 1991-07-26 1993-02-18 University Of Rochester Cancer therapy utilizing malignant cells
US5632957A (en) * 1993-11-01 1997-05-27 Nanogen Molecular biological diagnostic systems including electrodes
FR2687402B1 (fr) * 1992-02-14 1995-06-30 Lipha Nouveaux azaindoles, procedes de preparation et medicaments les contenant.
JPH05236997A (ja) * 1992-02-28 1993-09-17 Hitachi Ltd ポリヌクレオチド捕捉用チップ
CZ224195A3 (en) * 1993-03-01 1996-03-13 Merck Sharp & Dohme The use of pyrrolopyridine derivatives for preparing pharmaceutical preparations
DE69420394T2 (de) * 1993-03-01 2000-04-13 Merck Sharp & Dohme Ltd., Hoddesdon Pyrrolopyridinderivate als dopaminrezeptor liganden
US5576319A (en) * 1993-03-01 1996-11-19 Merck, Sharp & Dohme Ltd. Pyrrolo-pyridine derivatives
US5549614A (en) * 1993-03-18 1996-08-27 Tunis; Scott W. Apparatus for folding flexible intraocular lenses
US5840485A (en) * 1993-05-27 1998-11-24 Selectide Corporation Topologically segregated, encoded solid phase libraries
DK1310510T3 (da) * 1993-05-27 2007-09-24 Aventis Pharma Inc Topologisk adsilte, kodede biblioteker med fast fase
US5631236A (en) * 1993-08-26 1997-05-20 Baylor College Of Medicine Gene therapy for solid tumors, using a DNA sequence encoding HSV-Tk or VZV-Tk
US5426039A (en) * 1993-09-08 1995-06-20 Bio-Rad Laboratories, Inc. Direct molecular cloning of primer extended DNA containing an alkane diol
JP3545461B2 (ja) 1993-09-10 2004-07-21 エーザイ株式会社 二環式ヘテロ環含有スルホンアミド誘導体
US6045996A (en) * 1993-10-26 2000-04-04 Affymetrix, Inc. Hybridization assays on oligonucleotide arrays
US5965452A (en) * 1996-07-09 1999-10-12 Nanogen, Inc. Multiplexed active biologic array
US6468742B2 (en) * 1993-11-01 2002-10-22 Nanogen, Inc. Methods for determination of single nucleic acid polymorphisms using bioelectronic microchip
US5486525A (en) * 1993-12-16 1996-01-23 Abbott Laboratories Platelet activating factor antagonists: imidazopyridine indoles
US5807522A (en) * 1994-06-17 1998-09-15 The Board Of Trustees Of The Leland Stanford Junior University Methods for fabricating microarrays of biological samples
US5763198A (en) * 1994-07-22 1998-06-09 Sugen, Inc. Screening assays for compounds
GB9416162D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
GB9416189D0 (en) 1994-08-10 1994-09-28 Merck Sharp & Dohme Therapeutic agents
DE4430212A1 (de) * 1994-08-28 1996-02-29 Merck Patent Gmbh Ortho-substituierte Benzoesäure-Derivate
US5556752A (en) * 1994-10-24 1996-09-17 Affymetrix, Inc. Surface-bound, unimolecular, double-stranded DNA
US5830645A (en) * 1994-12-09 1998-11-03 The Regents Of The University Of California Comparative fluorescence hybridization to nucleic acid arrays
GB9503400D0 (en) 1995-02-21 1995-04-12 Merck Sharp & Dohme Therpeutic agents
GB2298199A (en) * 1995-02-21 1996-08-28 Merck Sharp & Dohme Synthesis of azaindoles
US5959098A (en) * 1996-04-17 1999-09-28 Affymetrix, Inc. Substrate preparation process
US6117681A (en) * 1995-03-29 2000-09-12 Bavarian Nordic Research Inst. A/S Pseudotyped retroviral particles
GB2299581A (en) 1995-04-07 1996-10-09 Merck Sharp & Dohme 3-(Tetrahydropyridin-1-yl-methyl)pyrrolo[2,3-b]pyridine derivatives as ligands for dopamine receptor subtypes
GB9507291D0 (en) * 1995-04-07 1995-05-31 Merck Sharp & Dohme Therapeutic agents
US6110456A (en) * 1995-06-07 2000-08-29 Yale University Oral delivery or adeno-associated viral vectors
US5856174A (en) * 1995-06-29 1999-01-05 Affymetrix, Inc. Integrated nucleic acid diagnostic device
US5866411A (en) * 1995-09-08 1999-02-02 Pedersen; Finn Skou Retroviral vector, a replication system for said vector and avian or mammalian cells transfected with said vector
US5747276A (en) * 1995-09-15 1998-05-05 The Scripps Research Institute Screening methods for the identification of novel antibiotics
US5721118A (en) * 1995-10-31 1998-02-24 The Regents Of The University Of California, San Diego Mammalian artificial chromosomes and methods of using same
US6022963A (en) * 1995-12-15 2000-02-08 Affymetrix, Inc. Synthesis of oligonucleotide arrays using photocleavable protecting groups
US6013440A (en) * 1996-03-11 2000-01-11 Affymetrix, Inc. Nucleic acid affinity columns
US6025155A (en) * 1996-04-10 2000-02-15 Chromos Molecular Systems, Inc. Artificial chromosomes, uses thereof and methods for preparing artificial chromosomes
US5804585A (en) * 1996-04-15 1998-09-08 Texas Biotechnology Corporation Thieno-pyridine sulfonamides derivatives thereof and related compounds that modulate the activity of endothelin
DK0948495T3 (da) * 1996-11-19 2004-06-01 Amgen Inc Aryl- og heteroarylsubstitueret, kondenseret pyrrol som antiinflammatoriske midler
US6294330B1 (en) * 1997-01-31 2001-09-25 Odyssey Pharmaceuticals Inc. Protein fragment complementation assays for the detection of biological or drug interactions
CA2283434A1 (en) * 1997-03-07 1998-09-11 Tropix, Inc. Protease inhibitor assay
US5977131A (en) 1997-04-09 1999-11-02 Pfizer Inc. Azaindole-ethylamine derivatives as nicotinic acetylcholine receptor binding agents
US6096718A (en) * 1997-06-05 2000-08-01 Gene Targeting Corp. Tissue specific adenovirus vectors for breast cancer treatment
RU2199532C2 (ru) 1997-06-27 2003-02-27 Фудзисава Фармасьютикал Ко., Лтд. Сульфонамидное соединение
US6235769B1 (en) * 1997-07-03 2001-05-22 Sugen, Inc. Methods of preventing and treating neurological disorders with compounds that modulate the function of the C-RET receptor protein tyrosine kinase
US6826296B2 (en) * 1997-07-25 2004-11-30 Affymetrix, Inc. Method and system for providing a probe array chip design database
US6161776A (en) * 1997-08-12 2000-12-19 Nibco Inc. Multi-layered, porous mat turf irrigation apparatus and method
CN100367023C (zh) * 1997-09-11 2008-02-06 生物风险公司 制备高密度阵列的方法
US6178384B1 (en) * 1997-09-29 2001-01-23 The Trustees Of Columbia University In The City Of New York Method and apparatus for selecting a molecule based on conformational free energy
US6465178B2 (en) * 1997-09-30 2002-10-15 Surmodics, Inc. Target molecule attachment to surfaces
US6048695A (en) * 1998-05-04 2000-04-11 Baylor College Of Medicine Chemically modified nucleic acids and methods for coupling nucleic acids to solid support
EP1085846A2 (en) * 1998-06-08 2001-03-28 Advanced Medicine, Inc. Multibinding inhibitors of microsomal triglyceride transferase protein
US6113913A (en) * 1998-06-26 2000-09-05 Genvec, Inc. Recombinant adenovirus
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
KR20010082184A (ko) 1998-08-28 2001-08-29 추후제출 p38-α 키나제의 저해체
US6350786B1 (en) * 1998-09-22 2002-02-26 Hoffmann-La Roche Inc. Stable complexes of poorly soluble compounds in ionic polymers
US6277628B1 (en) * 1998-10-02 2001-08-21 Incyte Genomics, Inc. Linear microarrays
US6277489B1 (en) * 1998-12-04 2001-08-21 The Regents Of The University Of California Support for high performance affinity chromatography and other uses
US20010001449A1 (en) 1998-12-30 2001-05-24 Thomas R. Kiliany Low-pressure hydrocracking process
PL200804B1 (pl) * 1999-03-17 2009-02-27 Astrazeneca Ab Pochodne amidowe, sposoby ich wytwarzania, ich kompozycje farmaceutyczne oraz ich zastosowanie
GB9906566D0 (en) 1999-03-23 1999-05-19 Zeneca Ltd Chemical compounds
US6221653B1 (en) * 1999-04-27 2001-04-24 Agilent Technologies, Inc. Method of performing array-based hybridization assays using thermal inkjet deposition of sample fluids
FR2793793B1 (fr) 1999-05-19 2004-02-27 Adir Nouveaux derives dimeriques substitues, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
TWI234557B (en) * 1999-05-26 2005-06-21 Telik Inc Novel naphthalene ureas as glucose uptake enhancers
US6653151B2 (en) * 1999-07-30 2003-11-25 Large Scale Proteomics Corporation Dry deposition of materials for microarrays using matrix displacement
US20010008765A1 (en) * 1999-12-06 2001-07-19 Fuji Photo Film Co., Ltd. DNA chip and reactive solid carrier
MXPA02006263A (es) * 1999-12-22 2004-02-26 Sugen Inc Metodos de modulacion de la funcion de la cinasa de tirosina c-kit de la proteina con compuestos de indolinona.
KR100641802B1 (ko) 1999-12-28 2006-11-02 에자이 가부시키가이샤 술폰아미드 함유 복소환 화합물
JP2001278886A (ja) * 2000-03-28 2001-10-10 Dai Ichi Seiyaku Co Ltd ベンゾオキサジン誘導体及びこれを含有する医薬
GB0007934D0 (en) * 2000-03-31 2000-05-17 Darwin Discovery Ltd Chemical compounds
ES2317368T3 (es) 2001-02-21 2009-04-16 EISAI R&D MANAGEMENT CO., LTD. Metodo para evaluar el efecto de un inhibidor de la angiogenesis a traves de la inhibicion de la expresion de la integrina.
CN100411686C (zh) 2001-04-11 2008-08-20 千寿制药株式会社 视觉功能障碍改善剂
WO2002085896A1 (en) 2001-04-24 2002-10-31 Wyeth Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1,4-benzodioxan
GB0114417D0 (en) * 2001-06-13 2001-08-08 Boc Group Plc Lubricating systems for regenerative vacuum pumps
WO2002102783A1 (en) 2001-06-19 2002-12-27 Merck & Co., Inc. Tyrosine kinase inhibitors
US7291639B2 (en) 2001-06-20 2007-11-06 Wyeth Aryloxy-acetic acid compounds useful as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
GB0115109D0 (en) 2001-06-21 2001-08-15 Aventis Pharma Ltd Chemical compounds
UA75425C2 (en) 2001-07-09 2006-04-17 Piperazine oxime derivatives with antagonistic activity to nk-1 receptor, use thereof, a pharmaceutical composition based thereon, a method for producing and a method for producing intermediary compounds
GB0117583D0 (en) 2001-07-19 2001-09-12 Astrazeneca Ab Novel compounds
US6858860B2 (en) * 2001-07-24 2005-02-22 Seiko Epson Corporation Apparatus and method for measuring natural period of liquid
GB0118479D0 (en) 2001-07-28 2001-09-19 Astrazeneca Ab Novel compounds
WO2003028724A1 (en) 2001-10-04 2003-04-10 Smithkline Beecham Corporation Chk1 kinase inhibitors
US20050014942A1 (en) 2001-10-30 2005-01-20 Yasufumi Maruyama Amide derivatives and drugs
US20030236277A1 (en) 2002-02-14 2003-12-25 Kadow John F. Indole, azaindole and related heterocyclic pyrrolidine derivatives
US6884889B2 (en) 2002-03-25 2005-04-26 Bristol-Myers Squibb Co. Processes for the preparation of antiviral 7-azaindole derivatives
KR20040111445A (ko) 2002-03-28 2004-12-31 에자이 가부시키가이샤 신경퇴행성 질환 치료용 ｃ─Ｊｕｎ Ｎ─말단 키나아제억제제로서의 ７─아자인돌
US7291630B2 (en) 2002-03-28 2007-11-06 Eisai Co., Ltd. Azaindoles as inhibitors of c-Jun N-terminal kinases
GB0212785D0 (en) * 2002-05-31 2002-07-10 Glaxo Group Ltd Compounds
UA78999C2 (en) 2002-06-04 2007-05-10 Wyeth Corp 1-(aminoalkyl)-3-sulfonylazaindoles as ligands of 5-hydroxytryptamine-6
TW200403243A (en) 2002-07-18 2004-03-01 Wyeth Corp 1-Heterocyclylalkyl-3-sulfonylazaindole or-azaindazole derivatives as 5-hydroxytryptamine-6 ligands
TWI329112B (en) 2002-07-19 2010-08-21 Bristol Myers Squibb Co Novel inhibitors of kinases
US6878887B2 (en) * 2002-08-07 2005-04-12 Matsushita Electric Industrial Co., Ltd. Anti-malfunction mechanism for variable output device
SE0202463D0 (sv) * 2002-08-14 2002-08-14 Astrazeneca Ab Novel compounds
EP3332811A1 (en) * 2002-09-06 2018-06-13 Cerulean Pharma Inc. Cyclodextrin-based polymers for delivering covalently attached camptothecin
EP1558751A4 (en) 2002-09-16 2007-08-22 Plexxikon Inc CRYSTALLINE STRUCTURE OF PROTEIN KINASE PIM-1
AU2003300902A1 (en) * 2002-12-13 2004-07-09 Smithkline Beecham Corporation Piperidine derivatives as CCR5 antagonists
ES2311755T3 (es) * 2002-12-13 2009-02-16 Smithkline Beecham Corporation Compuestos de ciclohexilo como antagonistas de ccrs.
US7696225B2 (en) * 2003-01-06 2010-04-13 Osi Pharmaceuticals, Inc. (2-carboxamido)(3-Amino) thiophene compounds
SE0300119D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
SE0300120D0 (sv) 2003-01-17 2003-01-17 Astrazeneca Ab Novel compounds
US20050085463A1 (en) * 2003-01-23 2005-04-21 Weiner David M. Use of N-desmethylclozapine to treat human neuropsychiatric disease
CN100482662C (zh) * 2003-02-14 2009-04-29 惠氏公司 作为5-羟基色胺-6配体的杂环基-3-磺酰基氮杂吲哚或-氮杂吲唑衍生物
US20050170431A1 (en) 2003-02-28 2005-08-04 Plexxikon, Inc. PYK2 crystal structure and uses
US20050164300A1 (en) 2003-09-15 2005-07-28 Plexxikon, Inc. Molecular scaffolds for kinase ligand development
DE10357510A1 (de) 2003-12-09 2005-07-07 Bayer Healthcare Ag Heteroarylsubstituierte Benzole
SI1696920T1 (sl) * 2003-12-19 2015-02-27 Plexxikon Inc. Spojine in postopki za razvoj modulatorjev ret
GB0330043D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions comprising them
EP2119771B1 (en) 2003-12-24 2018-08-22 DuPont Nutrition Biosciences ApS Proteins
GB0330042D0 (en) 2003-12-24 2004-01-28 Pharmacia Italia Spa Pyrrolo [2,3-b] pyridine derivatives active as kinase inhibitors process for their preparation and pharmaceutical compositions them
GB0403635D0 (en) 2004-02-18 2004-03-24 Devgen Nv Pyridinocarboxamides with improved activity as kinase inhibitors
GB0405055D0 (en) 2004-03-05 2004-04-07 Eisai London Res Lab Ltd JNK inhibitors
PT1730146E (pt) 2004-03-30 2011-07-11 Vertex Pharma Azaindoles úteis como inibidores de jak e outras proteínas quinases
JP2008503473A (ja) * 2004-06-17 2008-02-07 プレキシコン，インコーポレーテッド Ｃ−ｋｉｔ活性を調節する化合物
US7498342B2 (en) * 2004-06-17 2009-03-03 Plexxikon, Inc. Compounds modulating c-kit activity
EP2325184A1 (en) 2004-06-30 2011-05-25 Vertex Pharmceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7709645B2 (en) * 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
US7361764B2 (en) * 2004-07-27 2008-04-22 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
AU2005269386A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
AU2005269387A1 (en) * 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7626021B2 (en) * 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
GB0419192D0 (en) * 2004-08-27 2004-09-29 Merck Sharp & Dohme Therapeutic agents
CA2605738C (en) 2005-04-25 2013-10-01 Merck Patent Gesellschaft Mit Beschraenkter Haftung Novel azaheterocyclic compounds as kinase inhibitors
CA2608733A1 (en) * 2005-05-17 2007-02-01 Plexxikon, Inc. Pyrrol (2,3-b) pyridine derivatives protein kinase inhibitors
US8921376B2 (en) 2005-05-20 2014-12-30 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
EP3088400A1 (en) * 2005-06-22 2016-11-02 Plexxikon Inc. Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors
GB0516156D0 (en) 2005-08-05 2005-09-14 Eisai London Res Lab Ltd JNK inhibitors
WO2007109604A2 (en) * 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
WO2008063888A2 (en) * 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
PE20081581A1 (es) * 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
WO2008079909A1 (en) * 2006-12-21 2008-07-03 Plexxikon, Inc. Pyrrolo [2,3-b] pyridines as kinase modulators
CL2008001540A1 (es) * 2007-05-29 2009-05-22 Sgx Pharmaceuticals Inc Compuestos derivados de pirrolopiridinas y pirazolopiridinas; composicion farmaceutica; y uso en el tratamiento del cancer.
TW201041888A (en) * 2009-05-06 2010-12-01 Plexxikon Inc Compounds and methods for kinase modulation, and indications therefor

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