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

Substituierte benzazole und ihre verwendung als raf-kinase-hemmer

Info

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
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

Links

Classifications

    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D417/02Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
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

Family

ID=34465300

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (de)
EP (1) EP1682126B1 (de)
JP (1) JP4755991B2 (de)
KR (1) KR20060118472A (de)
CN (1) CN1889951A (de)
AT (1) ATE435015T1 (de)
AU (1) AU2004281151A1 (de)
CA (1) CA2542653A1 (de)
DE (1) DE602004021838D1 (de)
ES (1) ES2327418T3 (de)
IL (1) IL174965A0 (de)
MX (1) MXPA06004236A (de)
PL (1) PL1682126T3 (de)
PT (1) PT1682126E (de)
TW (1) TW200526208A (de)
WO (1) WO2005037273A1 (de)

Families Citing this family (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8124630B2 (en) 1999-01-13 2012-02-28 Bayer Healthcare Llc ω-carboxyaryl substituted diphenyl ureas as raf kinase inhibitors
WO2000041698A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
EP2324825A1 (de) 2002-02-11 2011-05-25 Bayer Healthcare LLC Arylharnstoffe mit Angiogenese hemmender Aktivität
US20030216396A1 (en) 2002-02-11 2003-11-20 Bayer Corporation Pyridine, quinoline, and isoquinoline N-oxides as kinase inhibitors
UY28213A1 (es) 2003-02-28 2004-09-30 Bayer Pharmaceuticals Corp Nuevos derivados de cianopiridina útiles en el tratamiento de cáncer y otros trastornos.
US8796250B2 (en) 2003-05-20 2014-08-05 Bayer Healthcare Llc Diaryl ureas for diseases mediated by PDGFR
BR122016015715B8 (pt) 2003-07-23 2021-05-25 Bayer Healthcare Llc composições farmacêuticas de metilamida de ácido 4[4-[3-(4-cloro-3-trifluorometilfenil)-ureido]-3-fluorofenóxi)-piridina-2-carboxílico
DE602004021838D1 (de) * 2003-10-16 2009-08-13 Novartis Vaccines & Diagnostic Substituierte benzazole und ihre verwendung als raf-kinase-hemmer
WO2006124874A2 (en) * 2005-05-12 2006-11-23 Kalypsys, Inc. Inhibitors of b-raf kinase
ATE476652T1 (de) * 2005-06-23 2010-08-15 Siemens Healthcare Diagnostics Quantitative assays für ras p21 in körperflüssigkeiten
PE20070335A1 (es) * 2005-08-30 2007-04-21 Novartis Ag Benzimidazoles sustituidos y metodos para su preparacion
EP1987028A2 (de) * 2006-02-10 2008-11-05 Transtech Pharma, Inc. Benzazolderivate, zusammensetzungen und verfahren zur verwendung als aurora-kinasehemmer
BRPI0710540B1 (pt) * 2006-04-19 2022-04-12 Novartis Ag Compostos de benzoxazol e benzotiazol substituídos por 6-o, e composição farmacêutica
WO2008144062A1 (en) 2007-05-21 2008-11-27 Novartis Ag Csf-1r inhibitors, compositions, and methods of use
CN101674828A (zh) * 2007-05-23 2010-03-17 诺瓦提斯公司 用于治疗甲状腺癌的Raf抑制剂
EP2162445B1 (de) 2007-06-05 2013-11-27 Takeda Pharmaceutical Company Limited Heterobicyclische verbindungen als kinasehemmer
JP5270553B2 (ja) * 2007-08-23 2013-08-21 武田薬品工業株式会社 複素環化合物およびその用途
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
US20110003809A1 (en) * 2008-02-29 2011-01-06 Array Biopharma Inc. Imidazo [4,5-b] pyridine derivatives used as raf inhibitors
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
CA2716951A1 (en) * 2008-02-29 2009-09-11 Array Biopharma Inc. Raf inhibitor compounds and methods of use thereof
US20110003859A1 (en) * 2008-02-29 2011-01-06 Array Biopharma Inc. N- (6-aminopyridin-3-yl) -3- (sulfonamido) benzamide derivatives as b-raf inhibitors for the treatment of cancer
US9540322B2 (en) * 2008-08-18 2017-01-10 Yale University MIF modulators
JP5579619B2 (ja) 2008-12-01 2014-08-27 武田薬品工業株式会社 複素環化合物およびその用途
JO3101B1 (ar) 2008-12-02 2017-09-20 Takeda Pharmaceuticals Co مشتقات بنزوثيازول كعوامل مضادة للسرطان
EA030276B1 (ru) 2010-03-09 2018-07-31 Дана-Фарбер Кэнсер Инститьют, Инк. Способы идентификации страдающих раком пациентов и лечения рака у пациентов, у которых имеется или развивается резистентность к первой терапии рака
EP2661434A4 (de) * 2011-01-06 2014-07-09 Beta Pharma Canada Inc Neue harnstoffe zur behandlung und prävention von krebs
US9408885B2 (en) 2011-12-01 2016-08-09 Vib Vzw Combinations of therapeutic agents for treating melanoma
CA2876246C (en) * 2012-07-28 2019-05-07 Calitor Sciences, Llc Substituted pyrazolone compounds and methods of use
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
CA2971413A1 (en) 2014-12-16 2016-06-23 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
US10370370B2 (en) 2015-06-10 2019-08-06 Axovant Sciences Gmbh Aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors
EP3334740A4 (de) 2015-08-12 2019-02-06 Axovant Sciences GmbH Geminal substituted aminobenzisoxazole compounds as agonists of alpha 7-nicotinic acetylcholine receptors
EP4105203A1 (de) * 2016-09-30 2022-12-21 Epizyme Inc Spiro-kondensierten indol-verbindungen als ehmt2-inhibitoren
JP7341060B2 (ja) 2017-02-10 2023-09-08 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Mapk経路の活性化に関連付けられる癌の処置のための方法及び医薬組成物
AU2018254577A1 (en) 2017-04-21 2019-12-05 Epizyme, Inc. Combination therapies with EHMT2 inhibitors
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
JP7416716B2 (ja) 2017-12-28 2024-01-17 トラクト ファーマシューティカルズ インコーポレイテッド 円柱上皮幹細胞のための幹細胞培養系およびそれに関連した使用法
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
WO2020097396A1 (en) * 2018-11-07 2020-05-14 Dana-Farber Cancer Institute, Inc. Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof
EP3876939A4 (de) * 2018-11-07 2022-08-10 Dana-Farber Cancer Institute, Inc. Benzothiazolderivate und 7-aza-benzothiazol-derivate als inhibitoren der janus-kinase-2 und verwendungen davon
US11691963B2 (en) 2020-05-06 2023-07-04 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

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
CO4940469A1 (es) * 1997-03-05 2000-07-24 Sugen Inc Composicion oral de estabilidad mejorada que comprende un derivado de indolinona y una mezcla de gliceridos o esteres de polietilenglicol
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 (de) 1999-01-13 2006-03-22 Bayer Pharmaceuticals Corp. -g(v)-carboxyaryl substituierte diphenyl harnstoffe als raf kinase inhibitoren
KR100710100B1 (ko) 1999-04-15 2007-04-23 브리스톨-마이어스스퀴브컴파니 환형 단백질 티로신 키나제 억제제
ATE339406T1 (de) * 1999-09-23 2006-10-15 Astrazeneca Ab Chinazoline verbindungen als heilmittel
DE60103136T2 (de) 2000-03-06 2004-10-28 Smithkline Beecham Plc, Brentford Imidazolderivate als Raf-Kinase Inhibitoren
HUP0400651A2 (hu) 2000-11-07 2004-06-28 Bristol-Myers Squibb Company Szerin proteáz inhibitorokként alkalmazható savszármazékok és ezeket tartalmazó gyógyszerkészítmények
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
ES2336094T3 (es) * 2002-03-29 2010-04-08 Novartis Vaccines And Diagnostics, Inc. Benzazoles sustituidos y uso de los mismos como inhibidores de quinasa raf.
US8299108B2 (en) 2002-03-29 2012-10-30 Novartis Ag Substituted benzazoles and methods of their use as inhibitors of raf kinase
US7531553B2 (en) * 2003-03-21 2009-05-12 Amgen Inc. Heterocyclic compounds and methods of use
DE602004021838D1 (de) 2003-10-16 2009-08-13 Novartis Vaccines & Diagnostic Substituierte benzazole und ihre verwendung als raf-kinase-hemmer

Also Published As

Publication number Publication date
PT1682126E (pt) 2009-10-02
US20050192287A1 (en) 2005-09-01
IL174965A0 (en) 2006-08-20
CA2542653A1 (en) 2005-04-28
PL1682126T3 (pl) 2009-12-31
US7423150B2 (en) 2008-09-09
WO2005037273A1 (en) 2005-04-28
CN1889951A (zh) 2007-01-03
JP4755991B2 (ja) 2011-08-24
US20090035309A1 (en) 2009-02-05
TW200526208A (en) 2005-08-16
US8415382B2 (en) 2013-04-09
AU2004281151A1 (en) 2005-04-28
EP1682126A1 (de) 2006-07-26
ES2327418T3 (es) 2009-10-29
US20130224195A1 (en) 2013-08-29
EP1682126B1 (de) 2009-07-01
JP2007509058A (ja) 2007-04-12
DE602004021838D1 (de) 2009-08-13
MXPA06004236A (es) 2006-06-28
KR20060118472A (ko) 2006-11-23

Similar Documents

Publication Publication Date Title
ATE435015T1 (de) Substituierte benzazole und ihre verwendung als raf-kinase-hemmer
AP1913A (en) Substituted benzazoles and use thereof as raf kinase inhibitors
EA200600689A1 (ru) Замещённые бензазолы и их применение в качестве ингибиторов raf киназы
TNSN08088A1 (en) Substituted benzimidazoles as kinase inhibitors
EA201100427A1 (ru) Гетероциклические ингибиторы киназы
ATE517896T1 (de) P38-kinase-inhibitoren
ATE521608T1 (de) Glucokinaseaktivatoren
MX2010010317A (es) Compuestos heterociclicos novedosos y usos de los mismos.
MY150136A (en) Picolinamide derivatives as kinase inhibitors
NO20092639L (no) 4-fenyl-6-(2,2,2-trifluor-1-fenyletoksy)pynmidinbaserte forbindelser og anvendelser derav
HK1166465A1 (en) 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position as parp inhibitors for use in treating cancer
TW200714590A (en) Heterocyclic inhibitors of MEK and methods of use thereof
DE602005009318D1 (de) Kondensierte heteroyralderivate zur verwendung als p38-kinase-inhibitoren
DE60314500D1 (de) Diaminopyrimidine und deren verwendung als angiogenesehemmer
ATE413392T1 (de) Kondensierte heteroyralderivate und deren verwendung als p38-kinase-inhibitoren
DK2026803T3 (da) Sammensætninger af R(+) og S(-) pramipexol og fremgangsmåder til anvendelse heraf
ATE362929T1 (de) Pyridinderivate als inhibitoren der raf-kinase
UA84954C2 (ru) Конденсированные пиримидоны, пригодные для лечения и профилактики злокачественного новообразования
DE502005007105D1 (de) 4-amino-5-oxo-8-phenyl-5h-pyrido-ä2,3-dü-pyrimidin-derivate als inhibitoren der tyrosinkinasen und der raf-kinasen zur behandlung von tumoren
DE602006017367D1 (de) Amino-oxo-indolyliden-verbindungen zur verwendung in der behandlung von juckender kopfhaut
WO2005118592A8 (en) Tetrahydropyridothiophenes for use in the treatment of cancer
ATE534649T1 (de) Imidazothiazole und imidazoxazolderivative als inhibitoren von p38
DE60214019D1 (de) Stickstoff enthaltende heterozyklen und ihre verwendung als raf inhibitoren
EA200701813A1 (ru) Новые амидозамещенные 6-фенилфенантридины
UA94055C2 (en) Substituted benzimidazoles and methods of preparation

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1682126

Country of ref document: EP

REN Ceased due to non-payment of the annual fee