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NO20084496L - Pyridyl- og pyrimidinylsubstituerte pyrrol-, tiofen- og furanderivater som kinaseinhibitorer - Google Patents

Pyridyl- og pyrimidinylsubstituerte pyrrol-, tiofen- og furanderivater som kinaseinhibitorer

Info

Publication number
NO20084496L
NO20084496L NO20084496A NO20084496A NO20084496L NO 20084496 L NO20084496 L NO 20084496L NO 20084496 A NO20084496 A NO 20084496A NO 20084496 A NO20084496 A NO 20084496A NO 20084496 L NO20084496 L NO 20084496L
Authority
NO
Norway
Prior art keywords
kinase inhibitors
thiophene
pyridyl
formula
substituted pyrrole
Prior art date
Application number
NO20084496A
Other languages
English (en)
Other versions
NO342798B1 (no
Inventor
Ermes Vanotti
Marina Caldarelli
Alessandra Cirla
Barbara Forte
Antonella Ermoli
Maria Menichincheri
Antonio Pillan
Alessandra Scolaro
Original Assignee
Nerviano Medical Sciences Srl
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 Nerviano Medical Sciences Srl filed Critical Nerviano Medical Sciences Srl
Publication of NO20084496L publication Critical patent/NO20084496L/no
Publication of NO342798B1 publication Critical patent/NO342798B1/no

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

HETEROPENTASYKLER SOM ER AKTIVE KINASE INHIBITORER Den foreliggende oppfinnelsen tilveiebringer forbindelser med formel (I): eller de farmasøytisk akseptable salter derav, hvori G, W, R2, R3, R4, R5 og R6 er som definert i spesifikasjonen. Ytterligere formål ifølge oppfinnelsen er fremgangsmåter og intermediater for fremstillingen av forbindelsene med formel (I), farmasøytiske sammensetninger omfattende dem og metoder for å behandle celleproliferative forstyrrelser. Faktum er at forbindelsene med formel (I) er nyttige i terapi, i behandlingen av sykdommer assosiert med en feilregulert proteinkinase-aktivitet, som kreft. 113 118
NO20084496A 2006-03-27 2008-10-27 Heteropentasykler som er aktive kinaseinhibitorer egnet til behandling av kreft NO342798B1 (no)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06111766 2006-03-27
PCT/EP2007/052587 WO2007110344A1 (en) 2006-03-27 2007-03-19 Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors

Publications (2)

Publication Number Publication Date
NO20084496L true NO20084496L (no) 2008-12-11
NO342798B1 NO342798B1 (no) 2018-08-06

Family

ID=38066663

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20084496A NO342798B1 (no) 2006-03-27 2008-10-27 Heteropentasykler som er aktive kinaseinhibitorer egnet til behandling av kreft

Country Status (21)

Country Link
US (4) US8263604B2 (no)
EP (1) EP2004623B1 (no)
JP (1) JP5261370B2 (no)
KR (2) KR20090008286A (no)
CN (1) CN101410387B (no)
AR (1) AR060150A1 (no)
AU (1) AU2007229559B2 (no)
BR (1) BRPI0709680B8 (no)
CA (1) CA2646952C (no)
CL (1) CL2007000806A1 (no)
EA (1) EA015126B1 (no)
ES (1) ES2436532T3 (no)
IL (1) IL194157A (no)
MX (1) MX2008012422A (no)
NO (1) NO342798B1 (no)
NZ (1) NZ572202A (no)
SG (1) SG173320A1 (no)
TW (1) TWI394749B (no)
UA (1) UA94097C2 (no)
WO (1) WO2007110344A1 (no)
ZA (1) ZA200808966B (no)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2007229559B2 (en) * 2006-03-27 2013-03-21 Nerviano Medical Sciences S.R.L. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors
JP2010533715A (ja) 2007-07-17 2010-10-28 アムジエン・インコーポレーテツド 複素環系ｐｋｂ調節剤
CA2693473A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of pkb
US8426417B2 (en) 2007-09-28 2013-04-23 Nerviano Medical Sciences S.R.L. Substituted pyrrolo-pyrimidine derivatives, process for their preparation and their use as kinase inhibitors
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
TWI426074B (zh) * 2008-04-30 2014-02-11 Nerviano Medical Sciences Srl ５－（２－胺基－嘧啶－４－基）－２－芳基－１ｈ－吡咯－３－羧醯胺之製造方法
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
EP3241826B1 (en) * 2009-02-25 2019-10-30 Takeda Pharmaceutical Company Limited Process for producing pyrrole compound
US8772280B2 (en) 2009-03-27 2014-07-08 Nerviano Medical Sciences S.R.L. N-aryl-2-(2-arylaminopyrimidin-4-yl)pyrrol-4-carboxamide derivatives as MPS1 kinase inhibitors
US8119812B2 (en) 2009-04-20 2012-02-21 Sbi Biotech Co., Ltd. Thiazolidinone derivative
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
BR112012010445B1 (pt) 2009-11-04 2021-09-21 Nerviano Medical Sciences S.R.L Processo para a preparação de 5-(2-amtno-pirimidin-4-il)-2-aril-1 h-pirrol-3-carboxamidas
CN102666528B (zh) * 2009-11-11 2014-04-16 内尔维阿诺医学科学有限公司 晶体cdc7 抑制剂盐
TW201127384A (en) 2009-11-18 2011-08-16 Nerviano Medical Sciences Srl Therapeutic combination comprising a Cdc7 inhibitor and an antineoplastic agent
SG187795A1 (en) 2010-08-11 2013-03-28 Millennium Pharm Inc Heteroaryls and uses thereof
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2012021615A1 (en) 2010-08-11 2012-02-16 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
JP2013542941A (ja) 2010-10-13 2013-11-28 ミレニアム ファーマシューティカルズ， インコーポレイテッド ヘテロアリールおよびその使用
KR101964479B1 (ko) 2011-03-31 2019-04-01 카나 바이오사이언스, 인코포레이션 신규 푸라논 유도체
JP5976778B2 (ja) * 2011-04-11 2016-08-24 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害剤としてのピラゾリル−ピリミジン誘導体
JP5970537B2 (ja) * 2011-04-19 2016-08-17 ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ キナーゼ阻害薬として活性な置換ピリミジニル−ピロール
EP2736514B1 (en) * 2011-07-28 2017-10-18 Nerviano Medical Sciences S.r.l. Alkynyl substituted pyrimidinyl-pyrroles active as kinases inhibitors
TW201348226A (zh) 2012-02-28 2013-12-01 Amgen Inc 作為ｐｉｍ抑制劑之醯胺
BR112015002152B1 (pt) * 2012-08-02 2021-04-27 Nerviano Medical Sciences S.R.L. Compostos de pirróis substituídos ativos como inibidores de quinases, processo para a preparação de tais compostos, composição farmacêutica, método in vitro para a inibição da atividade de proteínas quinases da família jak e produto compreendendo os referidos compostos
KR101592536B1 (ko) * 2013-12-23 2016-02-05 김영정 유체 순환식 난방장치
EP3100742B1 (en) 2014-01-31 2020-05-20 Carna Biosciences Inc. Anticancer agent composition comprising a cdc7 inhibitor and a wee1 inhibitor
WO2017011776A1 (en) 2015-07-16 2017-01-19 Array Biopharma, Inc. Substituted pyrazolo[1,5-a]pyridine compounds as ret 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
HRP20241295T1 (hr) 2016-04-04 2024-12-06 Loxo Oncology, Inc. Postupci za liječenje pedijatrijskih karcinoma
SI3439662T1 (sl) 2016-04-04 2024-11-29 Loxo Oncology, Inc. Tekoče formulacije (s)-n-(5-((r)-2-(2,5-difluorofenil)-pirolidin -1-il)-pirazološ1,5-aćpirimidin-3-il)-3-hidroksipirolidin-1-karboksamida
US10045991B2 (en) 2016-04-04 2018-08-14 Loxo Oncology, Inc. Methods of treating pediatric cancers
DK3458456T3 (da) 2016-05-18 2020-12-14 Array Biopharma Inc Fremstilling af (s)-n-(5-((r)-2-(2,5-difluorphenyl)pyrrolidin-1-yl)pyrazol[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidin-1-carboxamid
TWI704148B (zh) 2016-10-10 2020-09-11 美商亞雷生物製藥股份有限公司 作為ｒｅｔ激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物
JOP20190077A1 (ar) 2016-10-10 2019-04-09 Array Biopharma Inc مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret
JOP20190092A1 (ar) 2016-10-26 2019-04-25 Array Biopharma Inc عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها
WO2018136663A1 (en) 2017-01-18 2018-07-26 Array Biopharma, Inc. Ret inhibitors
EP3571203B1 (en) 2017-01-18 2023-06-07 Array BioPharma Inc. Substituted pyrazolo[1,5-a]pyrazine compounds as ret kinase inhibitors
JOP20190213A1 (ar) 2017-03-16 2019-09-16 Array Biopharma Inc مركبات حلقية ضخمة كمثبطات لكيناز ros1
TWI791053B (zh) 2017-10-10 2023-02-01 美商亞雷生物製藥股份有限公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物
TWI876442B (zh) 2017-10-10 2025-03-11 美商絡速藥業公司 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物
CN107857758B (zh) * 2017-12-31 2018-08-24 广东莱恩医药研究院有限公司 一种酰胺类化合物及其作为hsp90抑制剂和抗肿瘤药物的应用
CN107987063A (zh) * 2017-12-31 2018-05-04 窦玉玲 一种hsp90抑制剂及其在抗肿瘤药物的应用
WO2019143994A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrazolyl[4,3-c]pyridinecompounds as ret kinase inhibitors
WO2019143977A1 (en) 2018-01-18 2019-07-25 Array Biopharma Inc. Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors
EP3740490A1 (en) 2018-01-18 2020-11-25 Array Biopharma, Inc. Substituted pyrazolo[3,4-d]pyrimidine compounds as ret kinase inhibitors
GB201807147D0 (en) 2018-05-01 2018-06-13 Oncologica Uk Ltd Therapeutic combination
WO2020028258A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide
EP3849986B1 (en) 2018-09-10 2022-06-08 Array Biopharma, Inc. Fused heterocyclic compounds as ret kinase inhibitors
WO2020131627A1 (en) 2018-12-19 2020-06-25 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
JP2022515197A (ja) 2018-12-19 2022-02-17 アレイ バイオファーマ インコーポレイテッド がんを治療するためのｆｇｆｒ阻害剤としての７－（（３，５－ジメトキシフェニル）アミノ）キノキサリン誘導体
CN110437281B (zh) * 2019-07-18 2022-03-15 南开大学 一种吡啶盐改性的含有不同硝基芳杂环的前药小分子
EP4069369A4 (en) 2019-12-06 2024-02-14 Schrödinger, Inc. CYCLIC COMPOUNDS AND METHODS OF USE THEREOF
PH12022551523A1 (en) 2019-12-27 2024-01-29 Schra–Dinger Inc Cyclic compounds and methods of using same
JP2023541047A (ja) 2020-09-10 2023-09-27 シュレーディンガー， インコーポレイテッド がんの治療のための複素環式ペリ縮環ｃｄｃ７キナーゼ阻害剤
CN112778286B (zh) * 2021-01-13 2023-03-14 北京工业大学 一种对不同阴离子具有荧光特异性响应的多基团化合物及其制备方法与应用
WO2022164789A1 (en) 2021-01-26 2022-08-04 Schrödinger, Inc. Tricyclic compounds useful in the treatment of cancer, autoimmune and inflammatory disoders
TW202300150A (zh) 2021-03-18 2023-01-01 美商薛定諤公司 環狀化合物及其使用方法
WO2022207404A1 (en) 2021-04-02 2022-10-06 Nerviano Medical Sciences S.R.L. Substituted pyrrole carboxamides, process for their preparation and their use as kinase inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
WO2025059027A1 (en) 2023-09-11 2025-03-20 Schrödinger, Inc. Cyclopenta[e]pyrazolo[1,5-a]pyrimidine derivatives as malt1 inhibitors

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2260213C (en) * 1996-07-11 2005-03-29 Pfizer Inc. Pyridylpyrrole compounds useful as interleukin- and tnf antagonists
PT853083E (pt) * 1997-01-06 2001-12-28 Pfizer Composto de piridilfurano e piridiltiofeno e sua utilizacao farmaceutica
JP2002521408A (ja) * 1998-07-28 2002-07-16 スミスクライン・ビーチャム・コーポレイション 化合物および方法
US20040181066A1 (en) 2001-08-01 2004-09-16 Fraley Mark E. Tyrosine kinase inhibitors
ATE416168T1 (de) * 2002-02-15 2008-12-15 Glaxo Group Ltd Modulatoren des vanilloidrezeptors
CA2509565A1 (en) 2002-12-20 2004-07-15 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
CA2561977A1 (en) * 2004-03-30 2005-10-13 Chiron Corporation Substituted thiophene derivatives as anti-cancer agents
AU2007229559B2 (en) * 2006-03-27 2013-03-21 Nerviano Medical Sciences S.R.L. Pyridyl- and pyrimidinyl-substituted pyrrole-, thiophene- and furane-derivatives as kinase inhibitors

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