ATE435015T1 - Substituierte benzazole und ihre verwendung als raf-kinase-hemmer - Google Patents

Substituierte benzazole und ihre verwendung als raf-kinase-hemmer

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Publication number
ATE435015T1
ATE435015T1 AT04795357T AT04795357T ATE435015T1 AT E435015 T1 ATE435015 T1 AT E435015T1 AT 04795357 T AT04795357 T AT 04795357T AT 04795357 T AT04795357 T AT 04795357T AT E435015 T1 ATE435015 T1 AT E435015T1
Authority
AT
Austria
Prior art keywords
raf
kinase inhibitors
compositions
substituted benzazoles
raf kinase
Prior art date
Application number
AT04795357T
Other languages
German (de)
English (en)
Inventor
Savithri Ramurthy
Sharadha Subramanian
Joelle Verhagen
Daniel Poon
Teresa Hansen
Cynthia Shafer
Christopher Mcbride
Barry Levine
Abran Costales
Paul Renhowe
Original Assignee
Novartis Vaccines & Diagnostic
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 Novartis Vaccines & Diagnostic filed Critical Novartis Vaccines & Diagnostic
Application granted granted Critical
Publication of ATE435015T1 publication Critical patent/ATE435015T1/de

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Manufacturing & Machinery (AREA)
  • Ceramic Engineering (AREA)
  • Endocrinology (AREA)
  • Structural Engineering (AREA)
  • Materials Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
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  • Pulmonology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AT04795357T 2003-10-16 2004-10-15 Substituierte benzazole und ihre verwendung als raf-kinase-hemmer ATE435015T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US51196603P 2003-10-16 2003-10-16
PCT/US2004/034179 WO2005037273A1 (en) 2003-10-16 2004-10-15 Substituted benzazoles and use thereof as inhibitors of raf kinase

Publications (1)

Publication Number Publication Date
ATE435015T1 true ATE435015T1 (de) 2009-07-15

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Family Applications (1)

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AT04795357T ATE435015T1 (de) 2003-10-16 2004-10-15 Substituierte benzazole und ihre verwendung als raf-kinase-hemmer

Country Status (16)

Country Link
US (3) US7423150B2 (2)
EP (1) EP1682126B1 (2)
JP (1) JP4755991B2 (2)
KR (1) KR20060118472A (2)
CN (1) CN1889951A (2)
AT (1) ATE435015T1 (2)
AU (1) AU2004281151A1 (2)
CA (1) CA2542653A1 (2)
DE (1) DE602004021838D1 (2)
ES (1) ES2327418T3 (2)
IL (1) IL174965A0 (2)
MX (1) MXPA06004236A (2)
PL (1) PL1682126T3 (2)
PT (1) PT1682126E (2)
TW (1) TW200526208A (2)
WO (1) WO2005037273A1 (2)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ME00275B (me) 1999-01-13 2011-02-10 Bayer Corp ω-KARBOKSIARIL SUPSTITUISANI DIFENIL KARBAMIDI KAO INHIBITORI RAF KINAZE
EP1158985B1 (en) 1999-01-13 2011-12-28 Bayer HealthCare LLC OMEGA-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
SI1478358T1 (sl) 2002-02-11 2013-09-30 Bayer Healthcare Llc Sorafenib tozilat za zdravljenje bolezni, značilnih po abnormalni angiogenezi
WO2003068229A1 (en) 2002-02-11 2003-08-21 Bayer Pharmaceuticals Corporation Pyridine, quinoline, and isoquinoline n-oxides as kinase inhibitors
US7557129B2 (en) 2003-02-28 2009-07-07 Bayer Healthcare Llc Cyanopyridine derivatives useful in the treatment of cancer and other disorders
EP1636585B2 (en) 2003-05-20 2012-06-13 Bayer HealthCare LLC Diaryl ureas with kinase inhibiting activity
EP1663978B1 (en) 2003-07-23 2007-11-28 Bayer Pharmaceuticals Corporation Fluoro substituted omega-carboxyaryl diphenyl urea for the treatment and prevention of diseases and conditions
KR20060118472A (ko) * 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 raf 키나아제의 저해제로서 그것의 사용
WO2006124874A2 (en) * 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
CA2612693C (en) * 2005-06-23 2012-05-08 Bayer Healthcare Llc Quantitative assays for ras p21 in body fluids
TWI387592B (zh) * 2005-08-30 2013-03-01 Novartis Ag 經取代之苯并咪唑及其作為與腫瘤形成相關激酶之抑制劑之方法
CN101379060B (zh) * 2006-02-10 2012-05-23 转化技术制药公司 作为Aurora激酶抑制剂的苯并唑系衍生物、组合物和使用方法
CA2649288C (en) 2006-04-19 2015-11-24 Novartis Ag 6-o-substituted benzoxazole and benzothiazole compounds and methods of inhibiting csf-1r signaling
AU2008254425A1 (en) * 2007-05-21 2008-11-27 Novartis Ag CSF-1R inhibitors, compositions, and methods of use
BRPI0811097A2 (pt) * 2007-05-23 2014-12-09 Novartis Ag Inibidores de raf para o tratamento de câncer de tireoide
CL2008001626A1 (es) * 2007-06-05 2009-06-05 Takeda Pharmaceuticals Co Compuestos derivados de heterociclos fusionados, agente farmaceutico que los comprende y su uso en la profilaxis y tratamiento del cancer.
EP2181987B9 (en) 2007-08-23 2014-09-03 Takeda Pharmaceutical Company Limited 2-Carbonylaminobenzothiazoles and their use for the prophylaxis and treatment of cancer
WO2009028655A1 (ja) * 2007-08-30 2009-03-05 Takeda Pharmaceutical Company Limited 複素環化合物およびその用途
BRPI0818003A2 (pt) * 2007-10-18 2019-09-24 Novartis Ag inibidores de csf-1r, composições e métodos de uso
CA2716947A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
JP2011513332A (ja) * 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体
JP2011513331A (ja) * 2008-02-29 2011-04-28 アレイ バイオファーマ、インコーポレイテッド ピラゾール[3,4−b]ピリジンRAF阻害剤
KR20100122505A (ko) * 2008-02-29 2010-11-22 어레이 바이오파마 인크. Raf 저해물질 화합물 및 이들의 이용 방법
US9540322B2 (en) * 2008-08-18 2017-01-10 Yale University MIF modulators
US8697874B2 (en) 2008-12-01 2014-04-15 Takeda Pharmaceutical Company Limited Heterocyclic compound and use thereof
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
BR112012022801B8 (pt) * 2010-03-09 2019-10-29 Dana Farber Cancer Inst Inc método de identificar um indivíduo que tem câncer que é provável beneficiar-se do tratamento com uma terapia de combinação com um inibidor de raf e um segundo inibidor e uso de um inibidor de raf e um segundo inibidor para a fabricação de um medicamento para tratar câncer
EP2661434A4 (en) * 2011-01-06 2014-07-09 Beta Pharma Canada Inc NEW UREAS FOR THE TREATMENT AND PREVENTION OF CANCER
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
JP6342392B2 (ja) * 2012-07-28 2018-06-13 カリター・サイエンシーズ・エルエルシー 置換型ピラゾロン化合物及び使用方法
US9242969B2 (en) 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
UY36294A (es) 2014-09-12 2016-04-29 Novartis Ag Compuestos y composiciones como inhibidores de quinasa
EP3623371A1 (en) 2014-12-16 2020-03-18 Axovant Sciences GmbH Geminal substituted quinuclidine amide compounds as agonists of alpha-7 nicotinic acetylcholine receptors
CN105949178B (zh) * 2015-03-09 2020-05-26 西格莱(苏州)生物医药有限公司 一种苯并咪唑类化合物、其制备方法、中间体及应用
CN107847494A (zh) 2015-06-10 2018-03-27 阿考温特科学股份有限公司 作为α7‑烟碱乙酰胆碱受体激动剂的氨基苯并异噁唑化合物
JP2018523707A (ja) 2015-08-12 2018-08-23 アクソバント サイエンシズ ゲーエムベーハー α7−ニコチン性アセチルコリン受容体のアゴニストとしてのジェミナル置換アミノベンゾイソオキサゾール化合物
AU2017329090B9 (en) 2016-09-19 2019-09-05 Novartis Ag Therapeutic combinations comprising a RAF inhibitor and a ERK inhibitor
CA3037587A1 (en) * 2016-09-30 2018-04-05 Epizyme, Inc. Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors
WO2018146253A1 (en) 2017-02-10 2018-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment of cancers associated with activation of the mapk pathway
CN110621316B (zh) 2017-04-21 2024-01-26 Epizyme股份有限公司 用ehmt2抑制剂进行的组合疗法
CA3057969A1 (en) 2017-05-02 2018-11-08 Novartis Ag Combination therapy
CN108102093A (zh) * 2017-12-19 2018-06-01 中科院广州化学有限公司 一种含芴及吡啶基团的二胺单体及由其合成的聚酰亚胺
WO2019133810A1 (en) 2017-12-28 2019-07-04 Tract Pharmaceuticals, Inc. Stem cell culture systems for columnar epithelial stem cells, and uses related thereto
JP2022500385A (ja) 2018-09-10 2022-01-04 ミラティ セラピューティクス, インコーポレイテッド 組み合わせ療法
EP3877371A4 (en) 2018-11-07 2022-07-27 Dana-Farber Cancer Institute, Inc. IMIDAZOPYRIDINE DERIVATIVES AND AZA-IMIDAZOPYRIDINE DERIVATIVES AS JANUS KINASE 2 INHIBITORS AND USES THEREOF
EP3876939A4 (en) 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof
US12522583B2 (en) 2018-11-07 2026-01-13 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof
EP3969449B1 (en) 2019-05-13 2025-02-12 Novartis AG New crystalline forms of n-(3-(2-(2-hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methvlphenyl)-2(trifluoromethyl)isonicotinamide as raf inhibitors for the treatment of cancer
US11691963B2 (en) 2020-05-06 2023-07-04 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
US12043632B2 (en) 2020-12-23 2024-07-23 Ajax Therapeutics, Inc. 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors
WO2023009708A1 (en) * 2021-07-29 2023-02-02 Ajax Therapeutics, Inc. Heteroaryloxy triazolo- and imidazo-azines as jak2 inhibitors
WO2023086319A1 (en) * 2021-11-09 2023-05-19 Ajax Therapeutics, Inc. 6-he tero aryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors
US12162881B2 (en) 2021-11-09 2024-12-10 Ajax Therapeutics, Inc. Forms and compositions of inhibitors of JAK2

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6358932B1 (en) * 1994-05-31 2002-03-19 Isis Pharmaceticals, Inc. Antisense oligonucleotide inhibition of raf gene expression
US5717100A (en) * 1995-10-06 1998-02-10 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
DE19613976C1 (de) * 1996-04-09 1997-11-20 Gruenenthal Gmbh Thalidomid-Prodrugs mit immunmodulatorischer Wirkung
AU743024B2 (en) * 1997-03-05 2002-01-17 Sugen, Inc. Formulations for hydrophobic pharmaceutical agents
AR012634A1 (es) * 1997-05-02 2000-11-08 Sugen Inc Compuesto basado en quinazolina, composicion famaceutica que lo comprende, metodo para sintetizarlo, su uso, metodos de modulacion de la funcion deserina/treonina proteinaquinasa con dicho compuesto y metodo in vitro para identificar compuestos que modulan dicha funcion
GB9711650D0 (en) 1997-06-05 1997-07-30 Pfizer Ltd Compounds useful in therapy
GB9716557D0 (en) * 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
US6022884A (en) * 1997-11-07 2000-02-08 Amgen Inc. Substituted pyridine compounds and methods of use
US6211177B1 (en) * 1998-11-24 2001-04-03 Cell Pathways, Inc. Method for treating neoplasia by exposure to substituted 2-aryl-benzimidazole derivatives
EP1140840B1 (en) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
EP1169038B9 (en) 1999-04-15 2013-07-10 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
AU7031500A (en) * 1999-09-23 2001-04-24 Astrazeneca Ab Therapeutic quinazoline compounds
ATE266022T1 (de) 2000-03-06 2004-05-15 Smithkline Beecham Plc Imidazol derivate als raf kinase inhibitoren
EP1332131A2 (en) 2000-11-07 2003-08-06 Bristol-Myers Squibb Company Acid derivatives useful as serine protease inhibitors
JP2004517080A (ja) 2000-11-29 2004-06-10 グラクソ グループ リミテッド Tie−2および/またはvegfr−2の阻害剤として有用なベンゾイミダゾール誘導体
US20030009034A1 (en) 2001-03-22 2003-01-09 Neil Wishart Transition metal mediated process
GB0112348D0 (en) * 2001-05-19 2001-07-11 Smithkline Beecham Plc Compounds
US8299108B2 (en) * 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
WO2003082272A1 (en) * 2002-03-29 2003-10-09 Chiron Corporation Substituted benzazoles and use thereof as raf kinase inhibitors
US7531553B2 (en) * 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
KR20060118472A (ko) * 2003-10-16 2006-11-23 카이론 코포레이션 치환 벤자졸 및 raf 키나아제의 저해제로서 그것의 사용

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US8415382B2 (en) 2013-04-09
US20130224195A1 (en) 2013-08-29
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US7423150B2 (en) 2008-09-09
EP1682126A1 (en) 2006-07-26
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CN1889951A (zh) 2007-01-03
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