CA2667487C - 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

Info

Publication number
CA2667487C
CA2667487C CA2667487A CA2667487A CA2667487C CA 2667487 C CA2667487 C CA 2667487C CA 2667487 A CA2667487 A CA 2667487A CA 2667487 A CA2667487 A CA 2667487A CA 2667487 C CA2667487 C CA 2667487C
Authority
CA
Canada
Prior art keywords
compound
kinase
substituted
compounds
pim
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA2667487A
Other languages
English (en)
French (fr)
Other versions
CA2667487A1 (en
Inventor
David J. Bearss
Xiao-Hui Liu
Hariprasad Vankayalapati
Yong Xu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sumitomo Pharma Oncology Inc
Original Assignee
Tolero Pharmaceuticals 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 Tolero Pharmaceuticals Inc filed Critical Tolero Pharmaceuticals Inc
Publication of CA2667487A1 publication Critical patent/CA2667487A1/en
Application granted granted Critical
Publication of CA2667487C publication Critical patent/CA2667487C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (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)
CA2667487A 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 Active CA2667487C (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
CA2667487A1 CA2667487A1 (en) 2008-05-15
CA2667487C true CA2667487C (en) 2017-04-04

Family

ID=39277096

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2667487A Active CA2667487C (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

Country Status (14)

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

Families Citing this family (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA91341C2 (ru) 2004-07-15 2010-07-26 Амр Текнолоджи, Інк. Арил- и гетероарилзамещенные тетрагидроизохинолины и их применение для блокирования обратного захвата норэпинефрина, допамина и серотонина
CN101395155A (zh) * 2005-10-07 2009-03-25 埃克塞里艾克西斯公司 PI3Kα的吡啶并嘧啶酮抑制剂
EP2455382B1 (en) 2005-12-13 2016-10-26 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US7683060B2 (en) 2006-08-07 2010-03-23 Incyte Corporation Triazolotriazines as kinase inhibitors
CA2663091A1 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
EA200900573A1 (ru) * 2006-10-20 2009-10-30 АйАрЭм ЭлЭлСи Композиции и способы для модуляции рецепторов c-kit и pdgfr
ME02372B (me) 2006-11-22 2016-06-20 Incyte Holdings Corp Imidazotriazini i imidazopiramidini kao inhibitori kinaze
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of 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
WO2009143211A2 (en) 2008-05-21 2009-11-26 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
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
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
WO2010022081A1 (en) * 2008-08-19 2010-02-25 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
US8895550B2 (en) 2008-08-19 2014-11-25 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
PT2350075E (pt) 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase
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.
AR074052A1 (es) 2008-10-22 2010-12-22 Array Biopharma Inc Compuestos pirazolo{1,5-a}pirimidina sustituida como inhibidores de trk cinasa
EP2429295B1 (en) 2009-05-12 2013-12-25 Albany Molecular Research, Inc. Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
BRPI1011066A2 (pt) 2009-05-20 2017-03-21 Cylene Pharmaceuticals Inc "pirazolopirimidinas e heterociclos relacionados como inibidores de quinase
JP5775070B2 (ja) * 2009-05-22 2015-09-09 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ ヤヌスキナーゼ阻害剤としてのピラゾール−４−イル−ピロロ［２，３−ｄ］ピリミジンおよびピロール−３−イル−ピロロ［２，３−ｄ］ピリミジンのＮ−（ヘテロ）アリール−ピロリジン誘導体
SG176111A1 (en) * 2009-05-22 2011-12-29 Incyte Corp 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
AR078012A1 (es) * 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
US9227971B2 (en) 2010-01-19 2016-01-05 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
EA025304B1 (ru) 2010-02-03 2016-12-30 Инсайт Холдингс Корпорейшн ИМИДАЗО[1,2-b][1,2,4]ТРИАЗИНЫ В КАЧЕСТВЕ c-Met ИНГИБИТОРОВ
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
PT3354652T (pt) 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de 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
US9156827B2 (en) 2010-04-30 2015-10-13 The University Of Tokyo Anticancer agent
NZ604708A (en) 2010-05-20 2015-05-29 Array Biopharma Inc Macrocyclic compounds as trk kinase inhibitors
RS54824B1 (sr) 2010-05-21 2016-10-31 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
PL2678329T3 (pl) 2011-02-25 2016-06-30 Array Biopharma Inc Związki triazolopirydyny jako inhibitory kinaz pim
CA2836203A1 (en) 2011-05-17 2012-11-22 Bayer Intellectual Property Gmbh Amino-substituted imidazopyridazines as mknk1 kinase inhibitors
WO2012163942A1 (en) 2011-06-01 2012-12-06 Bayer Intellectual Property Gmbh Substituted aminoimidazopyridazines
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
US9284319B2 (en) 2011-06-22 2016-03-15 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
EP2734205B1 (en) * 2011-07-21 2018-03-21 Tolero Pharmaceuticals, Inc. Heterocyclic protein kinase inhibitors
JP6133291B2 (ja) * 2011-08-12 2017-05-24 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ピラゾロ［３，４−ｃ］ピリジン化合物と使用方法
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
WO2013041634A1 (en) 2011-09-23 2013-03-28 Bayer Intellectual Property Gmbh Substituted imidazopyridazines
BR112014007654A8 (pt) * 2011-09-30 2018-06-12 Ipsen Pharma Inibidores de lrrk2 quinase macrocíclicos.
CA2849999A1 (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
JP6147761B2 (ja) * 2011-12-12 2017-06-14 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
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
JP6173430B2 (ja) * 2012-04-04 2017-08-02 バイエル・ファルマ・アクティエンゲゼルシャフト アミノ置換イミダゾピリダジン
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
JP6280546B2 (ja) 2012-06-26 2018-02-14 デル マー ファーマシューティカルズ ジアンヒドロガラクチトール、ジアセチルジアンヒドロガラクチトール、ジブロモズルシトール、又はこれらの類似体若しくは誘導体を用いた、遺伝子多型又はａｈｉ１の調節不全若しくは変異を有する患者におけるチロシンキナーゼインヒビター抵抗性悪性腫瘍を処置するための方法
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
US9573954B2 (en) 2012-11-16 2017-02-21 University Health Network Pyrazolopyrimidine compounds
ES2646916T3 (es) 2012-11-19 2017-12-18 Bayer Pharma Aktiengesellschaft Aminoimidazopiridazinas como inhibidores de MKNK1 cinasa
CN105164124B (zh) 2012-11-19 2017-03-15 诺华股份有限公司 用于治疗寄生虫疾病的化合物和组合物
US8871754B2 (en) 2012-11-19 2014-10-28 Irm Llc Compounds and compositions for the treatment of parasitic diseases
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
RS60244B1 (sr) 2013-01-15 2020-06-30 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
US9745304B2 (en) 2013-01-30 2017-08-29 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
WO2014138168A1 (en) 2013-03-06 2014-09-12 Incyte Corporation Processes and intermediates for making a jak inhibitor
JP2016510764A (ja) * 2013-03-07 2016-04-11 カリフィア バイオ, インク.Califia Bio, Inc. 混合系キナーゼ阻害剤および治療法
WO2014140313A1 (en) * 2013-03-15 2014-09-18 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
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.
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
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
JP2017503809A (ja) 2014-01-09 2017-02-02 バイエル・ファルマ・アクティエンゲゼルシャフト アミド置換イミダゾピリダジン
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
US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
CN106687464B (zh) * 2014-09-17 2020-03-03 昂科迪塞恩股份有限公司 大环rip2激酶抑制剂
HUE061448T2 (hu) 2014-11-16 2023-07-28 Array Biopharma Inc (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-il)-pirazolo[1,5-A]pirimidin-3-il) -3-hidroxipirrolidin-1-karboxamid-hidrogénszulfát kristályos formája
WO2016196244A1 (en) 2015-05-29 2016-12-08 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
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
CN108697708A (zh) 2015-10-26 2018-10-23 洛克索肿瘤学股份有限公司 Trk抑制剂抗性癌症中的点突变以及与此相关的方法
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
RS65988B1 (sr) 2016-04-04 2024-10-31 Loxo Oncology Inc Postupak lečenja pedijatrijskih karcinoma
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
ES2987474T3 (es) 2016-04-04 2024-11-15 Loxo Oncology Inc Formulaciones líquidas de (S)-N-(5-((R)-2-(2,5-difluorofenil)-pirrolidin-1-IL)-pirazolo[1,5-A]pirimidin-3-IL)-3-hidroxipirrolidina-1-carboxamida
ES2836222T3 (es) 2016-05-18 2021-06-24 Loxo Oncology Inc Preparación de (S)-N-(5-((R)-2-(2,5-difluorofenil)pirrolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroxipirrolidina-1-carboxamida
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
EP3661935B1 (en) * 2017-08-11 2022-10-12 Teligene Ltd Substituted pyrazolopyrimidines useful as kinases inhibitors
WO2019036657A1 (en) 2017-08-17 2019-02-21 Kyn Therapeutics AHR INHIBITORS AND USES THEREOF
US11319320B2 (en) 2017-11-06 2022-05-03 Snap Bio, Inc. PIM kinase inhibitor compositions, methods, and uses thereof
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
EA202091830A1 (ru) 2018-01-30 2020-12-29 Инсайт Корпорейшн Способы и промежуточные соединения для получения ингибитора jak
MD3773593T2 (ro) 2018-03-30 2024-10-31 Incyte Corp Tratament hidradenitei supurative utilizând inhibitori ai JAK
CN117838695A (zh) 2018-04-13 2024-04-09 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
NZ778055A (en) 2019-02-12 2025-11-28 Sumitomo Pharma America Inc Formulations comprising heterocyclic protein kinase inhibitors
CN115038443A (zh) 2019-11-22 2022-09-09 因西特公司 包含alk2抑制剂和jak2抑制剂的组合疗法
PT4065582T (pt) 2019-11-26 2025-05-22 Ikena Oncology Inc Derivados polimórficos do carbazol e utilizações dos mesmos
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
JP2023541262A (ja) * 2020-09-14 2023-09-29 ザ ユニバーシティー オブ サセックス Ｌｅｍｕｒチロシンキナーゼ３の小分子阻害剤
US20240116921A1 (en) * 2020-12-22 2024-04-11 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
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
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
EA199700209A1 (ru) 1995-04-04 1998-04-30 Глаксо Груп Лимитед ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-a]ПИРИДИНА
US5747498A (en) 1996-05-28 1998-05-05 Pfizer Inc. Alkynyl and azido-substituted 4-anilinoquinazolines
ID19609A (id) 1996-07-13 1998-07-23 Glaxo Group Ltd Senyawa-senyawa heterosiklik
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
CA2309690A1 (en) 1997-11-11 1999-05-20 Pfizer Products Inc. Thienopyrimidine and thienopyridine derivatives useful as anticancer agents
SI1255752T1 (sl) 2000-02-15 2007-12-31 Pharmacia & Upjohn Co Llc S pirolom substituirani zaviralci 2-indolinon protein kinaza
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
WO2004058769A2 (en) 2002-12-18 2004-07-15 Vertex Pharmaceuticals Incorporated Triazolopyridazines as protein kinases inhibitors
JP2009502734A (ja) * 2005-07-29 2009-01-29 アステラス製薬株式会社 Ｌｃｋ阻害剤としての縮合複素環
WO2007025090A2 (en) * 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
DE102005042742A1 (de) * 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
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
WO2007041721A1 (en) * 2005-10-05 2007-04-12 Lg Home Products, Llc Sound privacy machine and methods of use thereof
CN101321760A (zh) * 2005-10-06 2008-12-10 先灵公司 作为蛋白激酶抑制剂的吡唑并嘧啶
DE102006029447A1 (de) * 2006-06-21 2007-12-27 Bayer Schering Pharma Ag Oxo-substituierte Imidazo[1,2b]pyridazine, deren Herstellung und Verwendung als Arzneimittel
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
EP1900739A1 (en) * 2006-08-30 2008-03-19 Cellzome Ag Diazolodiazine derivatives as kinase inhibitors
CA2663091A1 (en) * 2006-09-07 2008-03-13 Biogen Idec Ma Inc. Modulators of interleukin-1 receptor-associated kinase
WO2008037477A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
CN101522682A (zh) * 2006-10-30 2009-09-02 诺瓦提斯公司 作为抗炎剂的杂环化合物
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
PT2350075E (pt) * 2008-09-22 2014-06-09 Array Biopharma Inc Compostos imidazo[1,2b]piridazina substituídos como inibidores da trk cinase

Also Published As

Publication number Publication date
US20100227861A1 (en) 2010-09-09
EP2086979A2 (en) 2009-08-12
WO2008058126A2 (en) 2008-05-15
NZ576234A (en) 2011-06-30
AU2007316417A1 (en) 2008-05-15
KR20090086219A (ko) 2009-08-11
AU2007316417B2 (en) 2013-08-22
RU2009121577A (ru) 2010-12-20
EP2086979B1 (en) 2015-06-03
US7750007B2 (en) 2010-07-06
SG176461A1 (en) 2011-12-29
US20080261988A1 (en) 2008-10-23
JP5357763B2 (ja) 2013-12-04
MX2009004700A (es) 2009-05-15
CN101600718B (zh) 2013-07-03
BRPI0718029A2 (pt) 2013-11-26
JP2010509242A (ja) 2010-03-25
MY146474A (en) 2012-08-15
CN101600718A (zh) 2009-12-09
KR101546493B1 (ko) 2015-08-21
RU2487875C2 (ru) 2013-07-20
US8710057B2 (en) 2014-04-29
US20110281863A1 (en) 2011-11-17
WO2008058126A3 (en) 2008-06-26
CA2667487A1 (en) 2008-05-15

Similar Documents

Publication Publication Date Title
CA2667487C (en) Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
US20250129085A1 (en) Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors
US20100204221A1 (en) Pyrrolopyrimidinyl axl kinase inhibitors
JP4845736B2 (ja) プロテインキナーゼ阻害剤
US20120058997A1 (en) Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
CA2682733A1 (en) Axl kinase inhibitors
EP3985003A1 (en) Dna-pk inhibitors
WO2010098866A1 (en) Cyclopentathiophene/cyclohexathiophene dna methyltransferase inhibitors
CA2604284A1 (en) Protein kinase inhibitors
CA3093323C (en) Oxazino-quinazoline and oxazino-quinoline type compound, preparation method and uses thereof
US7714010B2 (en) Pyrrolobenzimidazolones and their use as anti-proliferative agents
CN117229264A (zh) 一类含有2-氨基嘧啶结构的芳基席夫碱类化合物及其应用
HK40041458A (en) Heterocyclic protein kinase inhibitors
HK40001531A (en) Heterocyclic protein kinase inhibitors
HK1121747A (en) Protein kinase inhibitors

Legal Events

Date Code Title Description
EEER Examination request
MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 17TH ANNIV.) - STANDARD

Year of fee payment: 17

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20241101

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT DETERMINED COMPLIANT

Effective date: 20241101

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20241101

R11 Change to the name of applicant or owner or transfer of ownership requested

Free format text: ST27 STATUS EVENT CODE: A-4-4-R10-R11-R127 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: TRANSFER RECORDAL REQUEST OR RESPONSE

Effective date: 20241105

W00 Other event occurred

Free format text: ST27 STATUS EVENT CODE: A-4-4-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT

Effective date: 20241105

R14 Transfer of ownership recorded

Free format text: ST27 STATUS EVENT CODE: A-4-4-R10-R14-R129 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: TRANSFER REQUIREMENTS DETERMINED COMPLIANT

Effective date: 20250403