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)
  • 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)
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 (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
JP2010509242A (ja) 2010-03-25
MY146474A (en) 2012-08-15
CA2667487C (en) 2017-04-04
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
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
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
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
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.
CN117412970B (zh) 含氟大环结构化合物的固体形态、制备方法和应用
BRPI0619955A2 (pt) derivados tricìclicos da lactama, sua produção e seus usos como agentes farmacêuticos
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
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.