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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    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (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
WO2006020049A2 (en) 2004-07-15 2006-02-23 Amr Technology, Inc. Aryl-and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
BRPI0617159B8 (pt) * 2005-10-07 2021-05-25 Exelixis Inc compostos de piridopirimidinone inibidores de pi3ka, composições que os contem e processo para preparo
EP2474545B1 (en) 2005-12-13 2016-11-09 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
TW200817410A (en) 2006-08-07 2008-04-16 Incyte Corp Triazolotriazines as kinase inhibitors
AU2007292924A1 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. IRAK modulators for treating an inflammatory condition, cell proliferative disorder, immune disorder
EA200900573A1 (ru) * 2006-10-20 2009-10-30 АйАрЭм ЭлЭлСи Композиции и способы для модуляции рецепторов c-kit и pdgfr
SI2497470T1 (sl) 2006-11-22 2016-02-29 Incyte Holdings Corporation Imidazotriazini in imidazopirimidini kot inhibitorji kinaz
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
DK2173752T4 (en) 2007-06-13 2022-08-01 Incyte Holdings Corp Salte af janus-kinase-inhibitor (r)-3-(4-(7h-pyrrolo(2,3-d)pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropannitril
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.
US8497278B2 (en) * 2008-05-19 2013-07-30 Sunovion Pharmaceuticals Inc. Imidazo[1,2-a]pyridine compounds
CN113248510B (zh) 2008-05-21 2025-01-17 因西特控股公司 2-氟-N-甲基-4-[7-(喹啉-6-基甲基)咪唑并[1,2-b][1,2,4]三嗪-2-基]苯甲酰胺的盐及与其相关的制备方法
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
US8557809B2 (en) * 2008-08-19 2013-10-15 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
US8895550B2 (en) 2008-08-19 2014-11-25 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
CN102224153B (zh) 2008-09-22 2014-04-30 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物
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.
PL3372605T3 (pl) 2008-10-22 2022-03-07 Array Biopharma Inc. Podstawione związki pirazolo[1,5-a]pirymidynowe jako inhibitory kinaz trk
US9034899B2 (en) 2009-05-12 2015-05-19 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
SG176584A1 (en) * 2009-05-20 2012-01-30 Cylene Pharmaceuticals Inc Pyrazolopyrimidines and related heterocycles as kinase inhibitors
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
CA2762174C (en) * 2009-05-22 2018-02-20 Incyte Corporation 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
WO2011090935A1 (en) * 2010-01-19 2011-07-28 Merck Sharp & Dohme Corp. PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS mTOR INHIBITORS
CN102812027B (zh) 2010-02-03 2015-01-07 因西特公司 作为C-MET抑制剂的咪唑并[1,2-b][1,2,4]三嗪
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
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
JP5583845B2 (ja) * 2010-04-28 2014-09-03 ブリストル−マイヤーズ スクイブ カンパニー イミダゾピリダジニル化合物および癌に対するそれらの使用
JP5656233B2 (ja) 2010-04-30 2015-01-21 国立大学法人 東京大学 抗がん剤
HUE044025T2 (hu) 2010-05-20 2019-09-30 Array Biopharma Inc Makrociklusos vegyületek mint TRK-kináz inhibitorok
SG185567A1 (en) 2010-05-21 2012-12-28 Incyte Corp Topical formulation for a jak inhibitor
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
US8889704B2 (en) 2011-02-25 2014-11-18 Array Biopharma Inc. Triazolopyridine compounds as PIM kinase inhibitors
JP6121991B2 (ja) 2011-05-17 2017-04-26 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 Mknk1キナーゼ阻害剤としてのアミノ置換イミダゾピリダジン
EP2714692B1 (en) 2011-06-01 2017-03-22 Bayer Intellectual Property GmbH Substituted aminoimidazopyridazines
BR112013032720A2 (pt) 2011-06-20 2016-09-13 Incyte Corp "derivados de azetidinil fenil, piridil ou pirazinil carboxamida como inibidores de jak, composição e uso dos referidos derivados"
WO2012175591A1 (en) 2011-06-22 2012-12-27 Bayer Intellectual Property Gmbh Heterocyclyl aminoimidazopyridazines
WO2013005041A1 (en) * 2011-07-07 2013-01-10 Centro Nacional De Investigaciones Oncológicas (Cnio) Tricyclic heterocyclic compounds as kinase inhibitors
HUE052198T2 (hu) 2011-07-21 2021-04-28 Sumitomo Dainippon Pharma Oncology Inc Heterociklusos protein kináz inhibitorok
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
CA2849345A1 (en) 2011-09-23 2013-03-28 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
US9096609B2 (en) * 2011-09-30 2015-08-04 Ipsen Pharma S.A.S. Macrocyclic LRRK2 kinase inhibitors
WO2013045653A1 (en) * 2011-09-30 2013-04-04 Oncodesign S.A. Macrocyclic flt3 kinase inhibitors
JP6057907B2 (ja) * 2011-10-04 2017-01-11 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
US9643974B2 (en) 2011-12-12 2017-05-09 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines
CA2868673A1 (en) 2012-03-29 2013-10-03 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
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
ES2660981T3 (es) 2012-04-04 2018-03-26 Bayer Pharma Aktiengesellschaft Imidazopiridazinas sustituidas con amino
AR091079A1 (es) 2012-05-18 2014-12-30 Incyte Corp Derivados de pirrolopirimidina y pirrolopiridina sustituida con piperidinilciclobutilo como inhibidores de jak
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
SG10201805807PA (en) 2012-06-26 2018-08-30 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
TW202228704A (zh) 2012-11-15 2022-08-01 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
NZ707432A (en) 2012-11-16 2020-01-31 Univ Health Network Pyrazolopyrimidine compounds
HUE037600T2 (hu) 2012-11-19 2018-09-28 Novartis Ag Vegyületek és készítmények paraziták által okozott fertõzések kezelésére
ES2646916T3 (es) 2012-11-19 2017-12-18 Bayer Pharma Aktiengesellschaft Aminoimidazopiridazinas como inhibidores de MKNK1 cinasa
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
AU2014207691B2 (en) 2013-01-15 2018-08-30 Incyte Holdings Corporation Thiazolecarboxamides and pyridinecarboxamide compounds useful as Pim kinase inhibitors
JP2016506943A (ja) 2013-01-30 2016-03-07 バイエル・ファルマ・アクティエンゲゼルシャフト Mknk−1キナーゼ阻害剤としてのアミドイミダゾピリダジン類
CA2901527A1 (en) 2013-02-20 2014-08-28 Bayer Pharma Aktiengesellschaft Substituted-imidazo[1,2-b]pyridazines as mknk1 inhibitors
PT3489239T (pt) 2013-03-06 2021-12-17 Incyte Holdings Corp Processos e intermediários para a preparação de um inibidor de jak
CA2901427A1 (en) 2013-03-07 2014-09-12 Califia Bio, Inc. Mixed lineage kinase inhibitors and method of treatments
KR20150133767A (ko) * 2013-03-15 2015-11-30 온코디자인 에스.에이. 거대고리 염-유도성 키나아제 억제제
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
CN105492011A (zh) 2013-04-08 2016-04-13 丹尼斯·M·布朗 不理想给药化学化合物的治疗增效
WO2015009888A2 (en) * 2013-07-19 2015-01-22 Onyx Therapeutics, Inc. Peptide epoxyketone proteasome inhibitors in combination with pim kinase inhibitors for treatment of cancers
MY203694A (en) 2013-08-07 2024-07-14 Incyte Holdings Corp Sustained release dosage forms for a jak1 inhibitor
EP3036238A1 (en) 2013-08-23 2016-06-29 Incyte Corporation Furo- and thieno-pyridine carboxamide compounds useful as pim kinase inhibitors
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
CN105899512A (zh) 2014-01-09 2016-08-24 拜耳医药股份公司 可用于治疗过度增殖性和/或血管生成疾病的酰胺基团取代的咪唑并哒嗪
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
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
GB201410817D0 (en) * 2014-06-17 2014-07-30 Ucb Biopharma Sprl And Katholieke Universiteit Leuven K U Leuven R & D Therapeutic agents
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
US10676486B2 (en) * 2014-09-17 2020-06-09 Oncodesign S.A. Macrocyclic RIP2 kinase inhibitors
PT3699181T (pt) 2014-11-16 2023-04-05 Array Biopharma Inc Forma cristalina de hidrogenossulfato de (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
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
JP2018534296A (ja) 2015-10-26 2018-11-22 ロクソ オンコロジー, インコーポレイテッドLoxo Oncology, Inc. Trk阻害薬耐性がんにおける点変異およびそれに関連する方法
EP3432886B1 (en) 2016-03-25 2021-06-02 University of Maryland, Baltimore County Pim kinase inhibitors in combination with rna splicing modulators/inhibitors for treatment of cancers
HRP20241295T1 (hr) 2016-04-04 2024-12-06 Loxo Oncology, Inc. Postupci za liječenje pedijatrijskih karcinoma
CU20180125A7 (es) 2016-04-04 2019-05-03 Loxo Oncology Inc Formulaciones líquidas de (s)-n-(5-((r)-2-(2,5-difluorofenil) -pirrolidin-1-il)-pirazolo[1,5-alpirimidin-3-il)-3 hidroxipirrolidina-1-carboxamida
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
MX392604B (es) 2016-05-18 2025-03-24 Array Biopharma Inc Procesos para la preparacion de (s)-n-(5-((r)-2-(2,5-difluorofenil)pirrolidin-1-il)-pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidin-1-carboxamida y sales del mismo.
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
WO2018195397A2 (en) 2017-04-21 2018-10-25 Kyn Therapeutics Indole ahr inhibitors and uses thereof
US11344553B2 (en) * 2017-08-11 2022-05-31 Teligene Ltd. Substituted pyrazolopyrimidines useful as kinases inhibitors
JP7269917B2 (ja) 2017-08-17 2023-05-09 イケナ オンコロジー, インコーポレイテッド Ahr阻害剤およびその使用
US11319320B2 (en) 2017-11-06 2022-05-03 Snap Bio, Inc. PIM kinase inhibitor compositions, methods, and uses thereof
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
PL3746429T3 (pl) 2018-01-30 2022-06-20 Incyte Corporation Procesy do otrzymywania (1-(3-fluoro-2-(trifluorometylo)izonikotynoilo)piperydyn-4-onu)
RS65624B1 (sr) 2018-03-30 2024-07-31 Incyte Corp Lečenje supurativnog hidradenitisa upotrebom jak inhbitora
CN117959303A (zh) 2018-04-13 2024-05-03 住友制药肿瘤公司 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂
US11471456B2 (en) 2019-02-12 2022-10-18 Sumitomo Pharma Oncology, Inc. Formulations comprising heterocyclic protein kinase inhibitors
PH12022551052A1 (en) 2019-11-22 2023-05-29 Incyte Corp Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
US11591339B2 (en) 2019-11-26 2023-02-28 Ikena Oncology, Inc. Solid forms of (R)-N-(2-(5-fluoropyridin-3-yl)-8-isopropylpyrazolo[ 1,5-a][1,3,5]triazin-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-amine maleate as aryl hydrocarbon receptor (AHR) inhibitors
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
CN114409656B (zh) * 2021-02-08 2022-09-23 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
EP4611753A1 (en) 2022-10-31 2025-09-10 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
WO2025231112A1 (en) * 2024-05-01 2025-11-06 Nimbus Salacia, Inc. Sik2 modulators and uses thereof
WO2025231117A1 (en) * 2024-05-01 2025-11-06 Nimbus Salacia, Inc. Sik2 modulators and uses thereof

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
CZ313397A3 (cs) 1995-04-04 1998-03-18 Glaxo Group Limited Imidazo/1,2a/pyridinové deriváty, způsob jejich výroby a farmaceutický prostředek s jejich obsahem
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
CA2291709A1 (en) * 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
EA005889B1 (ru) 1997-11-11 2005-06-30 Пфайзер Продактс Инк. Производные тиенопиримидина и тиенопиридина, полезные в качестве противораковых агентов
EP1255752B1 (en) 2000-02-15 2007-08-08 Sugen, Inc. Pyrrole substituted 2-indolinone protein kinase inhibitors
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
MXPA05006478A (es) * 2002-12-18 2005-09-08 Vertex Pharma Triazolopiridazinas como inhibidores de proteinas cinasas.
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
US20070132596A1 (en) * 2005-10-05 2007-06-14 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
MX2009003185A (es) * 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
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
US20110046127A1 (en) * 2007-11-08 2011-02-24 Paolo Pevarello Imidazopyridazines for Use as Protein Kinase Inhibitors
CN102224153B (zh) * 2008-09-22 2014-04-30 阵列生物制药公司 作为trk激酶抑制剂的取代的咪唑并[1,2-b]哒嗪化合物

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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