AU2007316417B2 - Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors - Google Patents

Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors Download PDF

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Publication number
AU2007316417B2
AU2007316417B2 AU2007316417A AU2007316417A AU2007316417B2 AU 2007316417 B2 AU2007316417 B2 AU 2007316417B2 AU 2007316417 A AU2007316417 A AU 2007316417A AU 2007316417 A AU2007316417 A AU 2007316417A AU 2007316417 B2 AU2007316417 B2 AU 2007316417B2
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compound
ocf
imidazo
pct
kinase
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AU2007316417A1 (en
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David J. Bearss
Xiao-Hui Liu
Hariprasad Vankayalapati
Yong Xu
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Tolero Pharmaceuticals Inc
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Tolero Pharmaceuticals Inc
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Assigned to TOLERO PHARMACEUTICALS, INC. reassignment TOLERO PHARMACEUTICALS, INC. Request for Assignment Assignors: ASTEX PHARMACEUTICALS, INC.
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
AU2007316417A 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 Expired - Fee Related AU2007316417B2 (en)

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 (2)

Publication Number Publication Date
AU2007316417A1 AU2007316417A1 (en) 2008-05-15
AU2007316417B2 true AU2007316417B2 (en) 2013-08-22

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AU2007316417A Expired - Fee Related AU2007316417B2 (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

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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
AU2005274927B2 (en) 2004-07-15 2011-11-03 Albany Molecular Research, Inc. Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
HRP20130902T1 (hr) * 2005-10-07 2013-11-08 Exelixis Inc. PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
JP2010500365A (ja) 2006-08-07 2010-01-07 インサイト・コーポレイション キナーゼ阻害剤としてのトリアゾロトリアジン
AU2007292924A1 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. IRAK modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
CN101528744A (zh) * 2006-10-20 2009-09-09 Irm责任有限公司 用于调节c-kit和pdgfr受体的组合物和方法
ES2560435T3 (es) 2006-11-22 2016-02-19 Incyte Holdings Corporation Imidazotriazinas e imidazopirimidinas como inhibidores de la quinasa
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
HUE029236T2 (en) 2007-06-13 2017-02-28 Incyte Holdings Corp (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor
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.
EP2300470A2 (en) * 2008-05-19 2011-03-30 Sepracor Inc. Imidazo[1,2-a]pyridine compounds as gaba-a receptor modulators
MX393622B (es) 2008-05-21 2025-03-24 Incyte Corp Sales de 2-fluoro-n-metil-4-[7-(quinolin-6-il-metil)-imidazo[1,2-b][1,2,4]triazin-2-il]benzamida y procesos relacionados con la preparacion de las mismas.
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
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
US8987251B2 (en) 2008-08-19 2015-03-24 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
RS53350B (sr) 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze
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.
HRP20140309T1 (hr) 2008-10-22 2014-05-09 Array Biopharma, Inc. SUPSTITUIRANI SPOJEVI PIRAZOLO[1,5-a]PIRIMIDINA KAO INHIBITORI TRK KINAZE
CN102458123A (zh) 2009-05-12 2012-05-16 阿尔巴尼分子研究公司 芳基、杂芳基和杂环取代的四氢异喹啉及其用途
AU2010249493A1 (en) * 2009-05-20 2011-12-08 Cylene Pharmaceuticals, Inc. Pyrazolopyrimidines and related heterocycles as kinase inhibitors
EP2432472B1 (en) 2009-05-22 2019-10-02 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
MY156727A (en) * 2009-05-22 2016-03-15 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase 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
TW201113285A (en) * 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2525659B1 (en) * 2010-01-19 2019-02-27 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
JP5714030B2 (ja) 2010-02-03 2015-05-07 インサイト コーポレーションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｃ−Ｍｅｔ阻害剤としてのイミダゾ［１，２−ｂ］［１，２，４］トリアジン
UY33221A (es) 2010-02-09 2011-09-30 Univ California MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2011137155A1 (en) * 2010-04-28 2011-11-03 Bristol-Myers Squibb Company Imidazopyridazinyl compounds and their uses for cancer
CN103391936B (zh) * 2010-04-30 2016-04-27 国立大学法人东京大学 抗癌剂
KR102015402B1 (ko) 2010-05-20 2019-08-28 어레이 바이오파마 인크. Trk 키나제 저해제로서의 매크로시클릭 화합물
AR084691A1 (es) 2010-05-21 2013-06-05 Incyte Corp Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
UA111075C2 (uk) 2011-02-25 2016-03-25 Еррей Біофарма Інк. Триазолопіридинові сполуки як інгібітори кінази рім
WO2012156367A1 (en) 2011-05-17 2012-11-22 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
CN103717604B (zh) 2011-06-01 2016-06-01 拜耳知识产权有限责任公司 取代的氨基咪唑并哒嗪
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp 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
EP2734205B1 (en) 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors
KR20140071361A (ko) * 2011-08-12 2014-06-11 에프. 호프만-라 로슈 아게 피라졸로[3,4-c]피리딘 화합물 및 사용 방법
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
CN103814029B (zh) 2011-09-23 2016-10-12 拜耳知识产权有限责任公司 取代的咪唑并哒嗪
PT2760453T (pt) * 2011-09-30 2016-08-02 Ipsen Pharma Sas Inibidores macrocíclicos da cinase lrrk2
BR112014007622A2 (pt) * 2011-09-30 2017-04-04 Oncodesign Sa inibidores de flt3 cinase macrocíclicos
TW201319063A (zh) * 2011-10-04 2013-05-16 Yakult Honsha Kk 以四氫噻唑衍生物或其鹽為有效成分之醫藥品
ES2650915T3 (es) * 2011-12-12 2018-01-23 Bayer Intellectual Property Gmbh Imidazopiridazinas amino-sustituidas
ES2663609T3 (es) 2012-03-29 2018-04-16 Bayer Intellectual Property Gmbh Imidazopiridazinas amino-sustituidas
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
US9409889B2 (en) 2012-04-04 2016-08-09 Bayer Pharma Aktiengesellschaft Amino-substituted imidazopyridazines
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
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
SG10201610869TA (en) 2012-06-26 2017-02-27 Del Mar Pharmaceuticals Methods for treating tyrosine-kinase-inhibitor-resistant malignancies in patients with genetic polymorphisms or ahi1 dysregulations or mutations employing dianhydrogalactitol, diacetyldianhydrogalacti
TWI761825B (zh) 2012-11-15 2022-04-21 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
JP6377068B2 (ja) 2012-11-16 2018-08-22 ユニバーシティ・ヘルス・ネットワーク ピラゾロピリミジン化合物
HK1208025A1 (en) 2012-11-19 2016-02-19 拜耳医药股份公司 Aminoimidazopyridazines
SI2925757T1 (en) 2012-11-19 2018-01-31 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc Compounds and compositions for the treatment of parasitic diseases
EP2943485B1 (en) 2013-01-14 2017-09-20 Incyte Holdings Corporation Bicyclic aromatic carboxamide compounds useful as pim kinase inhibitors
ME03780B (me) 2013-01-15 2021-04-20 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
CA2899352A1 (en) 2013-01-30 2014-08-07 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
MX384910B (es) 2013-03-06 2025-03-14 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak.
US9370515B2 (en) 2013-03-07 2016-06-21 Califia Bio, Inc. Mixed lineage kinase inhibitors and method of treatments
AU2014230125A1 (en) * 2013-03-15 2015-10-29 Oncodesign S.A. Macrocyclic salt-inducible kinase inhibitors
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
EP2983674A4 (en) 2013-04-08 2017-05-10 Dennis M. Brown Therapeutic benefit of suboptimally administered chemical compounds
US20160166632A1 (en) * 2013-07-19 2016-06-16 Onyx Therapeutics, Inc. Peptide epoxyketone proteasome inhibitors in combination with pim kinase inhibitors for treatment of cancers
SG11201600815WA (en) 2013-08-07 2016-03-30 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
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
US10214545B2 (en) 2014-01-09 2019-02-26 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
HRP20192334T1 (hr) * 2014-09-17 2020-03-20 Oncodesign S.A. Makrociklički inhibitori kinaze rip2
JP6914834B2 (ja) 2014-11-16 2021-08-04 アレイ バイオファーマ インコーポレイテッド （Ｓ）−Ｎ−（５−（（Ｒ）−２−（２，５−ジフルオロフェニル）−ピロリジン−１−イル）−ピラゾロ［１，５−ａ］ピリミジン−３−イル）−３−ヒドロキシピロリジン−１−カルボキサミド硫酸水素塩の結晶形
WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
AR105967A1 (es) 2015-09-09 2017-11-29 Incyte Corp Sales de un inhibidor de pim quinasa
WO2017059251A1 (en) 2015-10-02 2017-04-06 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
TN2018000138A1 (en) 2015-10-26 2019-10-04 Array Biopharma Inc Point mutations in trk inhibitor-resistant cancer and methods relating to the same
US10525047B2 (en) * 2016-03-25 2020-01-07 University Of Maryland, Baltimore County PIM kinase inhibitors in combination with RNA splicing modulators/inhibitors for treatment of cancers
ES2987501T3 (es) 2016-04-04 2024-11-15 Loxo Oncology Inc Métodos de tratamiento de cánceres pediátricos
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
AU2017246554B2 (en) 2016-04-04 2022-08-18 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
KR102566858B1 (ko) 2016-05-18 2023-08-11 어레이 바이오파마 인크. (s)-n-(5-((r)-2-(2,5-디플루오로페닐)피롤리딘-1-일)-피라졸로[1,5-a]피리미딘-3-일)-3-히드록시피롤리딘-1-카르복사미드의 제조 방법
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
FI3612030T3 (fi) 2017-04-21 2026-03-20 Pahr Therapeutics Inc Ahr:n indoliestäjiä ja niiden käyttötapoja
US11344553B2 (en) * 2017-08-11 2022-05-31 Teligene Ltd. Substituted pyrazolopyrimidines useful as kinases inhibitors
SG11202001310SA (en) 2017-08-17 2020-03-30 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
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
JP7393348B2 (ja) 2018-01-30 2023-12-06 インサイト・コーポレイション （１－（３－フルオロ－２（トリフルオロメチル）イソニコチニル）ピぺリジン―４－オン）を作製するためのプロセス及び中間体
CN113768934A (zh) 2018-03-30 2021-12-10 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
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
AU2020221247B2 (en) 2019-02-12 2024-12-12 Sumitomo Pharma America, Inc. Formulations comprising heterocyclic protein kinase inhibitors
BR112022009710A2 (pt) 2019-11-22 2022-08-09 Incyte Corp Terapia de combinação compreendendo um inibidor de alk2 e um inibidor de jak2
MX2022006308A (es) 2019-11-26 2022-06-22 Ikena Oncology Inc Derivados de carbazol polimorfos y usos de los mismos.
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US20230355617A1 (en) * 2020-09-14 2023-11-09 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
EP4289847A4 (en) * 2021-02-08 2025-01-01 Hangzhou Biosun Pharmaceutical Co., Ltd. PIM KINASE INHIBITOR
EP4413000A1 (en) * 2021-10-04 2024-08-14 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
JP2026509318A (ja) 2022-10-31 2026-03-18 スミトモ・ファーマ・アメリカ・インコーポレイテッド 骨髄増殖性新生物を治療するためのｐｉｍ１阻害剤
EP4434972A1 (en) * 2023-03-22 2024-09-25 Eberhard-Karls-Universität Tübingen Atm kinase inhibitors
WO2025231112A1 (en) * 2024-05-01 2025-11-06 Nimbus Salacia, Inc. Sik2 modulators and uses thereof
TW202547512A (zh) * 2024-05-01 2025-12-16 美商林伯士薩拉西亞公司 Sik2調節劑及其用途

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007013673A1 (en) * 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
WO2007025540A2 (de) * 2005-09-02 2007-03-08 Bayer Schering Pharma Aktiengesellschaft Substituierte imidazo[1,2b]pyridazine als kinase-inhibitoren, deren herstellung und verwendung als arzneimittel
WO2007147646A1 (de) * 2006-06-21 2007-12-27 Bayer Schering Pharma Aktiengesellschaft OXO-SUBSTITUIERTE IMIDAZO[1,2b]PYRIDAZINE, DEREN HERSTELLUNG UND VERWENDUNG ALS ARZNEIMITTEL
WO2008025822A1 (en) * 2006-08-30 2008-03-06 Cellzome Limited Diazolodiazine derivatives as kinase inhibitors
WO2008030579A2 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
WO2008052734A1 (en) * 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents

Family Cites Families (22)

* 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
KR19980703559A (ko) 1995-04-04 1998-11-05 그레이엄브레레톤 이미다조［1,2-ａ］피리딘 유도체
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
DE69716916T2 (de) 1996-07-13 2003-07-03 Glaxo Group Ltd., Greenford Kondensierte heterozyklische verbindungen als protein kinase inhibitoren
ID18494A (id) 1996-10-02 1998-04-16 Novartis Ag Turunan pirazola leburan dan proses pembuatannya
JP2002501532A (ja) * 1997-05-30 2002-01-15 メルク エンド カンパニー インコーポレーテッド 新規血管形成阻害薬
WO1999024440A1 (en) 1997-11-11 1999-05-20 Pfizer Products Inc. Thienopyrimidine and thienopyridine derivatives useful as anticancer agents
AR034118A1 (es) 2000-02-15 2004-02-04 Sugen Inc Compuestos de 2-indolinonas sustituidas con pirroles inhibidoras de proteinquinasas; sus composiciones farmaceuticas e intermediarios de sintesis
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
CA2503905A1 (en) 2002-09-16 2004-03-25 Plexxikon, Inc. Crystal structure of pim-1 kinase
ATE473980T1 (de) * 2002-12-18 2010-07-15 Vertex Pharma Triazolopyridazine als proteinkinase-inhibitoren
US20070049591A1 (en) * 2005-08-25 2007-03-01 Kalypsys, Inc. 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
GB2445703A (en) * 2005-10-05 2008-07-16 Lg Home Products Llc Sound privacy machine and methods of use thereof
CA2624882C (en) * 2005-10-06 2014-05-20 Schering Corporation Pyrazolopyrimidines 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
KR20090073121A (ko) 2006-09-29 2009-07-02 노파르티스 아게 Ｐｉ3ｋ 지질 키나제 억제제로서의 피라졸로피리미딘
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
WO2009060197A1 (en) * 2007-11-08 2009-05-14 Centro Nacional De Investigaciones Oncologicas (Cnio) Imidazopyridazines for use as protein kinase inhibitors
RS53350B (sr) * 2008-09-22 2014-10-31 Array Biopharma, Inc. Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007013673A1 (en) * 2005-07-29 2007-02-01 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
WO2007025540A2 (de) * 2005-09-02 2007-03-08 Bayer Schering Pharma Aktiengesellschaft Substituierte imidazo[1,2b]pyridazine als kinase-inhibitoren, deren herstellung und verwendung als arzneimittel
WO2007147646A1 (de) * 2006-06-21 2007-12-27 Bayer Schering Pharma Aktiengesellschaft OXO-SUBSTITUIERTE IMIDAZO[1,2b]PYRIDAZINE, DEREN HERSTELLUNG UND VERWENDUNG ALS ARZNEIMITTEL
WO2008025822A1 (en) * 2006-08-30 2008-03-06 Cellzome Limited Diazolodiazine derivatives as kinase inhibitors
WO2008030579A2 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Irak modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
WO2008052734A1 (en) * 2006-10-30 2008-05-08 Novartis Ag Heterocyclic compounds as antiinflammatory agents

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