BRPI0718029A2 - Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase - Google Patents

Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase Download PDF

Info

Publication number
BRPI0718029A2
BRPI0718029A2 BRPI0718029-2A BRPI0718029A BRPI0718029A2 BR PI0718029 A2 BRPI0718029 A2 BR PI0718029A2 BR PI0718029 A BRPI0718029 A BR PI0718029A BR PI0718029 A2 BRPI0718029 A2 BR PI0718029A2
Authority
BR
Brazil
Prior art keywords
formula
compound
compound according
phenyl
substituted
Prior art date
Application number
BRPI0718029-2A
Other languages
English (en)
Portuguese (pt)
Inventor
David J Bearss
Xiao-Hui Liu
Haiprasad Vankayalapati
Yong Xu
Original Assignee
Supergen Inc
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 Supergen Inc filed Critical Supergen Inc
Publication of BRPI0718029A2 publication Critical patent/BRPI0718029A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/5025Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
BRPI0718029-2A 2006-11-06 2007-11-06 Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase BRPI0718029A2 (pt)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US86456606P 2006-11-06 2006-11-06
US60/864.566 2006-11-06
US89252307P 2007-03-01 2007-03-01
US60/892.523 2007-03-01
US95798807P 2007-08-24 2007-08-24
US60/957.988 2007-08-24
PCT/US2007/083773 WO2008058126A2 (en) 2006-11-06 2007-11-06 Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors

Publications (1)

Publication Number Publication Date
BRPI0718029A2 true BRPI0718029A2 (pt) 2013-11-26

Family

ID=39277096

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0718029-2A BRPI0718029A2 (pt) 2006-11-06 2007-11-06 Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase

Country Status (14)

Country Link
US (3) US7750007B2 (enExample)
EP (1) EP2086979B1 (enExample)
JP (1) JP5357763B2 (enExample)
KR (1) KR101546493B1 (enExample)
CN (1) CN101600718B (enExample)
AU (1) AU2007316417B2 (enExample)
BR (1) BRPI0718029A2 (enExample)
CA (1) CA2667487C (enExample)
MX (1) MX2009004700A (enExample)
MY (1) MY146474A (enExample)
NZ (1) NZ576234A (enExample)
RU (1) RU2487875C2 (enExample)
SG (1) SG176461A1 (enExample)
WO (1) WO2008058126A2 (enExample)

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060063766A1 (en) 2004-07-15 2006-03-23 Molino Bruce F Use of aryl- and heteroaryl-substituted tetrahydroisoquinolines to block reuptake of norepinephrine, dopamine, and serotonin
NZ594628A (en) * 2005-10-07 2013-04-26 Exelixis Inc PYRIDOPYRIMIDINONE INHIBITORS OF PI3Ka
DK3184526T3 (en) 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
WO2008021781A1 (en) 2006-08-07 2008-02-21 Incyte Corporation Triazolotriazines as kinase inhibitors
JP2010502716A (ja) * 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン1受容体関連キナーゼの調節物質
JP2010506948A (ja) * 2006-10-20 2010-03-04 アイアールエム・リミテッド・ライアビリティ・カンパニー C−kitおよびpdgfr受容体を調節するための組成物および方法
CA2669991C (en) 2006-11-22 2016-01-26 Incyte Corporation Imidazotriazines and imidazopyrimidines as kinase inhibitors
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
FR2918061B1 (fr) 2007-06-28 2010-10-22 Sanofi Aventis Derives de 6-cycloamino-3-(pyridin-4-yl)imidazo°1,2-b!- pyridazine,leur preparation et leur application en therapeutique.
CA2724842A1 (en) * 2008-05-19 2009-11-26 Sunovion Pharmaceuticals Inc. Imidazo[1,2-a]pyridine compounds
CA2724742C (en) 2008-05-21 2016-07-19 Incyte Corporation Salts of 2-fluoro-n-methyl-4-[7-(quinolin-6-yl-methyl)- imidazo[1,2-b][1,2,4]triazin-2-yl]benzamide and processes related to preparing the same
AR071997A1 (es) * 2008-06-04 2010-07-28 Bristol Myers Squibb Co Forma cristalina de 6-((4s)-2-metil-4-(2-naftil)-1,2,3,4-tetrahidroisoquinolin-7-il)piridazin-3-amina
US9156812B2 (en) 2008-06-04 2015-10-13 Bristol-Myers Squibb Company Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine
US8987251B2 (en) 2008-08-19 2015-03-24 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
TWI496779B (zh) * 2008-08-19 2015-08-21 Array Biopharma Inc 作為pim激酶抑制劑之三唑吡啶化合物
US8895550B2 (en) 2008-08-19 2014-11-25 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
US8557809B2 (en) * 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
ES2464461T3 (es) 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
SG196855A1 (en) 2008-10-22 2014-02-13 Array Biopharma Inc Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors
JP2012526823A (ja) 2009-05-12 2012-11-01 アルバニー モレキュラー リサーチ, インコーポレイテッド アリール、ヘテロアリール、および複素環置換テトラヒドロイソキノリンならびにそれらの使用
WO2010135581A1 (en) * 2009-05-20 2010-11-25 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
ES2487542T3 (es) * 2009-05-22 2014-08-21 Incyte Corporation Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus
WO2010135621A1 (en) * 2009-05-22 2010-11-25 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011028685A1 (en) * 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
WO2011090935A1 (en) * 2010-01-19 2011-07-28 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
ES2608329T3 (es) 2010-02-03 2017-04-07 Incyte Holdings Corporation Imidazo[1,2-b][1,2,4]triazinas como inhibidores de c-Met
AR080151A1 (es) 2010-02-09 2012-03-14 Exelixis Inc Metodos para tratar cancer usando inhibidores de piridopirimidinona de pi 3k y mtor en combinacion con inhibidores de autofagia
SMT201800137T1 (it) 2010-03-10 2018-07-17 Incyte Holdings Corp Derivati di piperidin-4-il azetidina come inibitori di jak1
CN102971326A (zh) * 2010-04-28 2013-03-13 百时美施贵宝公司 咪唑并哒嗪化合物及其在癌症中的用途
JP5656233B2 (ja) * 2010-04-30 2015-01-21 国立大学法人 東京大学 抗がん剤
AU2011256380C1 (en) 2010-05-20 2016-09-08 Array Biopharma Inc. Macrocyclic compounds as Trk kinase inhibitors
PH12012502296B1 (en) 2010-05-21 2017-10-06 Incyte Holdings Corp Topical formulation for a jak inhibitor
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
AU2012254082B2 (en) 2011-02-25 2016-12-08 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
CA2836203A1 (en) 2011-05-17 2012-11-22 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
US9730929B2 (en) 2011-06-01 2017-08-15 Bayer Intellectual Property Gmbh Substituted aminoimidazopyridazines
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
HK1197063A1 (en) 2011-06-22 2015-01-02 拜耳知识产权有限责任公司 Heterocyclyl aminoimidazopyridazines
WO2013005041A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) Tricyclic heterocyclic compounds as kinase inhibitors
ES2834093T3 (es) 2011-07-21 2021-06-16 Sumitomo Dainippon Pharma Oncology Inc Inhibidores de proteína quinasa heterocíclicos
WO2013024002A1 (en) * 2011-08-12 2013-02-21 F. Hoffmann-La Roche Ag PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE
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
UA117092C2 (uk) 2011-09-06 2018-06-25 Байєр Інтеллектуал Проперті Гмбх Амінозаміщені імідазопіридазини
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
JP6174586B2 (ja) 2011-09-23 2017-08-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 置換イミダゾピリダジン
KR20140078710A (ko) * 2011-09-30 2014-06-25 온코디자인 에스.에이. 거대고리 flt3 키나제 억제제
ES2583477T3 (es) * 2011-09-30 2016-09-21 Ipsen Pharma S.A.S. Inhibidores macrocíclicos de cinasa de LRRK2
WO2013051672A1 (ja) * 2011-10-04 2013-04-11 株式会社ヤクルト本社 チアゾリジン誘導体又はその塩を有効成分とする医薬品
ES2650915T3 (es) * 2011-12-12 2018-01-23 Bayer Intellectual Property Gmbh Imidazopiridazinas amino-sustituidas
JP6173426B2 (ja) 2012-03-29 2017-08-02 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH アミノ置換イミダゾピリダジン
US10280168B2 (en) * 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
GB201205669D0 (en) * 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
CN104321326B (zh) * 2012-04-04 2017-05-31 拜耳医药股份有限公司 氨基取代的咪唑并哒嗪
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
TWI585088B (zh) * 2012-06-04 2017-06-01 第一三共股份有限公司 作爲激酶抑制劑之咪唑并[1,2-b]嗒衍生物
SG11201408679XA (en) 2012-06-26 2015-01-29 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalactitol, dibromodulcitol, or analogs or derivatives thereof
PE20151157A1 (es) 2012-11-15 2015-08-19 Incyte Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
US9573954B2 (en) 2012-11-16 2017-02-21 University Health Network Pyrazolopyrimidine compounds
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc Compounds and compositions for the treatment of parasitic diseases
US9783543B2 (en) 2012-11-19 2017-10-10 Bayer Pharma Aktiengesellschaft Aminoimidazopyridazines
PT2925757T (pt) 2012-11-19 2018-01-09 Novartis Ag Compostos e composições para o tratamento de doenças parasitárias
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
HUE050215T2 (hu) 2013-01-15 2020-11-30 Incyte Holdings Corp Pim kináz inhibitorokként hasznos tiazolkarboxamid és piridinkarboxamid vegyületek
EP2951181A1 (en) 2013-01-30 2015-12-09 Bayer Pharma Aktiengesellschaft Amidoimidazopyridazines as mknk-1 kinase inhibitors
JP2016509036A (ja) 2013-02-20 2016-03-24 バイエル・ファルマ・アクティエンゲゼルシャフト Mknk1阻害剤としての置換イミダゾ[1,2−b]ピリダジン
LT3489239T (lt) 2013-03-06 2022-03-10 Incyte Holdings Corporation Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai
EP2964230A4 (en) * 2013-03-07 2016-10-26 Califia Bio Inc KINASEHEMMER WITH MIXED ABSTRACT AND TREATMENT PROCESS THEREWITH
CN105209040A (zh) * 2013-03-15 2015-12-30 昂科迪塞恩股份有限公司 大环的盐可诱导的激酶抑制剂
JP6023630B2 (ja) * 2013-04-03 2016-11-09 株式会社ヤクルト本社 チアゾロン誘導体
US11491154B2 (en) 2013-04-08 2022-11-08 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
MX372671B (es) * 2013-07-19 2020-04-23 Onyx Therapeutics Inc Inhibidores de proteasoma de epoxicetona peptídica en combinacion con inhibidores de cinasa pim para el tratamiento de canceres.
UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
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
AR097543A1 (es) * 2013-09-06 2016-03-23 Lexicon Pharmaceuticals Inc COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO
EP3092242A1 (en) 2014-01-09 2016-11-16 Bayer Pharma Aktiengesellschaft Amido-substituted imidazopyridazines useful in the treatment of hyper-proliferative and/or angiogenesis disorders
CN103864800A (zh) * 2014-04-03 2014-06-18 定陶县友帮化工有限公司 6-氯咪唑并[1,2-b]哒嗪的合成方法
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
GB201410817D0 (en) * 2014-06-17 2014-07-30 Ucb Biopharma Sprl And Katholieke Universiteit Leuven K U Leuven R & D Therapeutic agents
WO2016010897A1 (en) 2014-07-14 2016-01-21 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
WO2016042087A1 (en) * 2014-09-17 2016-03-24 Oncodesign S.A. Macrocyclic rip2 kinase inhibitors
EP3699181B1 (en) 2014-11-16 2023-03-01 Array Biopharma, Inc. Crystalline form of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate
US9540347B2 (en) 2015-05-29 2017-01-10 Incyte Corporation Pyridineamine compounds useful as Pim kinase inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
US10724102B2 (en) 2015-10-26 2020-07-28 Loxo Oncology, Inc. Point mutations in TRK inhibitor-resistant cancer and methods relating to the same
CA3017641C (en) 2016-03-25 2023-12-12 Charles J. Bieberich Pim kinase inhibitors in combination with rna splicing modulators/inhibitors for treatment of cancers
SG11201808559PA (en) 2016-04-04 2018-10-30 Loxo Oncology Inc Liquid formulations of (s)-n-(5-((r)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
PL3439663T3 (pl) 2016-04-04 2024-11-18 Loxo Oncology, Inc. Sposoby leczenia nowotworów wieku dziecięcego
FI3800189T3 (fi) 2016-05-18 2023-07-31 Loxo Oncology Inc (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin valmistaminen
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
SG11201909710XA (en) 2017-04-21 2019-11-28 Kyn Therapeutics Indole ahr inhibitors and uses thereof
FI3661935T3 (fi) * 2017-08-11 2023-01-13 Kinaasin estäjinä käyttökelpoiset pyratsolipyrimidiinit
CA3073051A1 (en) 2017-08-17 2019-02-21 Ikena Oncology, Inc. Ahr inhibitors and uses thereof
US11319320B2 (en) 2017-11-06 2022-05-03 Snap Bio, Inc. PIM kinase inhibitor compositions, methods, and uses thereof
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
IL276302B2 (en) 2018-01-30 2023-11-01 Incyte Corp Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one)
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
CA3095580A1 (en) 2018-04-13 2019-10-17 Sumitomo Dainippon Pharma Oncology, Inc. Pim kinase inhibitors for treatment of myeloproliferative neoplasms and fibrosis associated with cancer
HUE072069T2 (hu) 2019-02-12 2025-10-28 Sumitomo Pharma America Inc 2-((1R,4R)-4-((3-(3-(trifluormetil)fenil)imidazo[1,2- b]piridazin-6-il)amino)ciklohexil)propán-2-ol sósavas sójának kristályos formája
CR20220280A (es) 2019-11-22 2022-09-02 Incyte Corp Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2
AU2020394424A1 (en) 2019-11-26 2022-06-16 Ikena Oncology, Inc. Polymorphic carbazole derivatives and uses thereof
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022053838A1 (en) * 2020-09-14 2022-03-17 The University Of Sussex Small molecule inhibitors of lemur tyrosine kinase 3
WO2022140769A1 (en) * 2020-12-22 2022-06-30 Enliven Therapeutics, Inc. Lactam (hetero)arylfusedpyrimidine derivatives as inhibitors of erbb2
CN115991706A (zh) * 2021-02-08 2023-04-21 杭州邦顺制药有限公司 Pim激酶抑制剂
US20250002491A1 (en) * 2021-10-04 2025-01-02 Forx Therapeutics Ag N,n-dimethyl-4-(7-(n-(1-methylcyclopropyl)sulfamoyl)-imidazo[1,5-a]pyridin-5-yl)piperazine-1-carboxamide derivatives and the corresponding pyrazolo[1,5-a]pyridine derivatives as parg inhibitors for the treatment of cancer
CN116262753A (zh) * 2021-12-13 2023-06-16 杭州邦顺制药有限公司 一种新颖的pim激酶抑制剂
AU2023372386A1 (en) 2022-10-31 2025-05-08 Sumitomo Pharma America, Inc. Pim1 inhibitor for treating myeloproliferative neoplasms
EP4434972A1 (en) * 2023-03-22 2024-09-25 Eberhard-Karls-Universität Tübingen Atm kinase inhibitors
WO2025231117A1 (en) * 2024-05-01 2025-11-06 Nimbus Salacia, Inc. Sik2 modulators and uses thereof
WO2025231112A1 (en) * 2024-05-01 2025-11-06 Nimbus Salacia, Inc. Sik2 modulators and uses thereof

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8719368D0 (en) * 1987-08-15 1987-09-23 Wellcome Found Heterocyclic compounds
IL112248A0 (en) 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
SK133297A3 (en) 1995-04-04 1998-07-08 Glaxo Group Ltd Imidazo[1,2-a]pyridine derivatives, pharmaceutical composition containing same and their use
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
AR007857A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios uso en medicina ycomposiciones farmaceuticas que los contienen.
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
EP0984692A4 (en) * 1997-05-30 2001-02-21 Merck & Co Inc ANGIOGENESIS INHIBITORS
WO1999024440A1 (en) 1997-11-11 1999-05-20 Pfizer Products Inc. Thienopyrimidine and thienopyridine derivatives useful as anticancer agents
BRPI0117360B8 (pt) 2000-02-15 2021-07-06 Upjohn Co inibidores de proteína de quinase de 2-indolinona de pirrol substituído, seus sais e composições farmacêuticas compreendendo os mesmos
GB0020556D0 (en) * 2000-08-22 2000-10-11 Glaxo Group Ltd Fused pyrazole derivatives
GB0119249D0 (en) * 2001-08-07 2001-10-03 Novartis Ag Organic compounds
AU2003272548A1 (en) 2002-09-16 2004-04-30 Plexxikon, Inc. Crystal structure of pim-1 kinase
NZ541151A (en) * 2002-12-18 2008-09-26 Vertex Pharma Triazolopyridazines as protein kinase inhibitors
WO2007013673A1 (en) * 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
WO2007025090A2 (en) * 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
US7750000B2 (en) * 2005-09-02 2010-07-06 Bayer Schering Pharma Ag Substituted imidazo[1,2b]pyridazines as kinase inhibitors, their preparation and use as medicaments
DE102005042742A1 (de) 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
US20070132596A1 (en) * 2005-10-05 2007-06-14 Lg Home Products, Llc Sound Privacy Machine and Methods of Use Thereof
US7776865B2 (en) * 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
EP1873157A1 (en) 2006-06-21 2008-01-02 Bayer Schering Pharma Aktiengesellschaft Pyrazolopyrimidines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
DE102006029447A1 (de) * 2006-06-21 2007-12-27 Bayer Schering Pharma Ag Oxo-substituierte Imidazo[1,2b]pyridazine, deren Herstellung und Verwendung als Arzneimittel
EP1900739A1 (en) * 2006-08-30 2008-03-19 Cellzome Ag Diazolodiazine derivatives as kinase inhibitors
JP2010502716A (ja) * 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン1受容体関連キナーゼの調節物質
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Pi3k 지질 키나제 억제제로서의 피라졸로피리미딘
CA2667962A1 (en) * 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents
US20120058997A1 (en) * 2006-11-06 2012-03-08 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
EP2217601A1 (en) * 2007-11-08 2010-08-18 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyridazines for use as protein kinase inhibitors
ES2464461T3 (es) * 2008-09-22 2014-06-02 Array Biopharma, Inc. Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa

Also Published As

Publication number Publication date
AU2007316417A1 (en) 2008-05-15
US20110281863A1 (en) 2011-11-17
WO2008058126A2 (en) 2008-05-15
US20100227861A1 (en) 2010-09-09
MX2009004700A (es) 2009-05-15
WO2008058126A3 (en) 2008-06-26
US8710057B2 (en) 2014-04-29
JP5357763B2 (ja) 2013-12-04
KR20090086219A (ko) 2009-08-11
MY146474A (en) 2012-08-15
SG176461A1 (en) 2011-12-29
EP2086979B1 (en) 2015-06-03
CN101600718A (zh) 2009-12-09
CA2667487A1 (en) 2008-05-15
US20080261988A1 (en) 2008-10-23
NZ576234A (en) 2011-06-30
US7750007B2 (en) 2010-07-06
JP2010509242A (ja) 2010-03-25
RU2009121577A (ru) 2010-12-20
AU2007316417B2 (en) 2013-08-22
EP2086979A2 (en) 2009-08-12
CA2667487C (en) 2017-04-04
KR101546493B1 (ko) 2015-08-21
RU2487875C2 (ru) 2013-07-20
CN101600718B (zh) 2013-07-03

Similar Documents

Publication Publication Date Title
BRPI0718029A2 (pt) Derivados de imidazo(1,2-b)piridazina e pirazolo(1,5-a)pirimidina e seu uso como inibidores da proteína cinase
JP4845736B2 (ja) プロテインキナーゼ阻害剤
AU2017284702B2 (en) Pyrrolopyrimidine crystal for preparing JAK inhibitor
US20120058997A1 (en) Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20100204221A1 (en) Pyrrolopyrimidinyl axl kinase inhibitors
CN114057771B (zh) 大环化合物及其制备方法和应用
CN108707151B (zh) 嘧啶并-哒嗪酮化合物及其用途
BRPI0711809A2 (pt) derivados de triazolopirazina úteis como agentes anti-cáncer
CN101679313A (zh) 用于治疗癌症或过度增殖性疾病的axl激酶抑制剂
HUP0203225A2 (hu) Benzodiazepinszármazékok, előállításuk és alkalmazásuk
MX2015003570A (es) Derivados de quinazolinona como inhidores poli (adp-ribosa) polimerasa (parp).
CN115028648B (zh) 三并环化合物及其药物组合物和应用
BRPI0609956A2 (pt) inibidores de proteìna quinase
US20070275961A1 (en) Triazolo ' 1, 5-A ! Pyrimidines and Their Use in Medicine
EP1589967B1 (en) Benzthiazole-3 oxides useful for the treatment of proliferative disorders
CN120302969A (zh) 可用作iap抑制剂的化合物和组合物
CN118724899B (zh) 2(1h)-喹喔啉酮化合物、其药物组合物及应用
ES2309518T3 (es) Compuestos de diaminopirroloquinazolinas como inhibidores de la proteina tirosina fosfatasa.
KR20240062104A (ko) 교모세포종 약물내성 극복을 위한 테모졸로마이드 유사 항암제
KR101812266B1 (ko) 4-((2-아크릴아미도페닐)아미노)티에노[3,2-d]피리미딘-7-카복스아미드 유도체 및 그의 약학적 활용
BRPI0619955A2 (pt) derivados tricìclicos da lactama, sua produção e seus usos como agentes farmacêuticos
KR101812128B1 (ko) 단백질 키나아제 저해제인 신규 5-아미노-3-(이속사졸-3-일)-1h-피라졸-4-카보아마이드 유도체들의 제조방법 및 약학적 활용
AU2012204137B2 (en) Organic compounds
BR112019021703B1 (pt) Compostos heteroaromáticos, composição farmacêutica e uso destes

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 7A ANUIDADE.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2280 DE 16/09/2014.