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GT201400057A - 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante - Google Patents

3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante

Info

Publication number
GT201400057A
GT201400057A GT201400057A GT201400057A GT201400057A GT 201400057 A GT201400057 A GT 201400057A GT 201400057 A GT201400057 A GT 201400057A GT 201400057 A GT201400057 A GT 201400057A GT 201400057 A GT201400057 A GT 201400057A
Authority
GT
Guatemala
Prior art keywords
oxazolidin
pirmidin
onas
inhibitors
compounds
Prior art date
Application number
GT201400057A
Other languages
English (en)
Inventor
Young Shin Cho
Julian Roy Levell
Bakary-Barry Toure
Fan Yang
Thomas CAFERRO
Huangshu Lei
Francois Lenoir
Gang Liu
Mark G Palermo
Michael David Shultz
Troy Smith
Abran Q Costales
Keith Bruce Pfister
Martin Sendzik
Cynthia Shafer
James Sutton
Qian Zhao
Original Assignee
Novartis Ag
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 Ag filed Critical Novartis Ag
Publication of GT201400057A publication Critical patent/GT201400057A/es

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • 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
    • C07D487/08Bridged systems
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    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/18Bridged systems
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
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  • Oncology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Peptides Or Proteins (AREA)

Abstract

LA PRESENTE INVENCIÓN SE REFIERE A COMPUESTOS NOVEDOSOS DE 3-PRIMIDINIL-A-IL-OXAZOLIDIN-2-ONA, COMPOSICIONES QUE CONTIENEN ESTOS COMPUESTOS, EL USO DE TALES COMPUESTOS EN LA INHIBICIÓN DE LAS PROTEÍNAS IDH MUTANTES QUE TIENEN UNA ACTIVIDAD NEOMÓRFICA Y EN EL TRATAMIENTO DE ENFERMEDADES O TRASTORNOS ASOCIADOS CON TALES PROTEÍNAS IDH MUTANTES INCLUYENDO, PERO SIN LIMITAR A, TRASTORNOS DE PROLIFERACIÓN CELULAR, COMO CÁNCER.
GT201400057A 2011-09-27 2014-03-27 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante GT201400057A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201161539553P 2011-09-27 2011-09-27

Publications (1)

Publication Number Publication Date
GT201400057A true GT201400057A (es) 2017-09-28

Family

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Family Applications (1)

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GT201400057A GT201400057A (es) 2011-09-27 2014-03-27 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante

Country Status (32)

Country Link
US (1) US8957068B2 (es)
EP (1) EP2771337B1 (es)
JP (1) JP6026544B2 (es)
KR (1) KR20140069235A (es)
CN (1) CN103958506B (es)
AP (1) AP3907A (es)
AR (1) AR088175A1 (es)
AU (1) AU2012313888B2 (es)
BR (1) BR112014007310A2 (es)
CA (1) CA2849995A1 (es)
CL (1) CL2014000746A1 (es)
CO (1) CO6920291A2 (es)
CR (1) CR20140143A (es)
CU (1) CU24269B1 (es)
DO (1) DOP2014000058A (es)
EA (1) EA025183B1 (es)
ES (1) ES2645968T3 (es)
GE (1) GEP20166432B (es)
GT (1) GT201400057A (es)
IL (1) IL231786A (es)
MA (1) MA35452B1 (es)
MX (1) MX342326B (es)
NI (1) NI201400026A (es)
PE (1) PE20141581A1 (es)
PH (1) PH12014500682A1 (es)
SG (1) SG11201400989TA (es)
TN (1) TN2014000128A1 (es)
TW (1) TWI547493B (es)
UA (1) UA111503C2 (es)
UY (1) UY34352A (es)
WO (1) WO2013046136A1 (es)
ZA (1) ZA201402144B (es)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9474779B2 (en) 2012-01-19 2016-10-25 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their methods of use
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
US9340549B2 (en) * 2012-03-05 2016-05-17 Amgen Inc. Oxazolidinone compounds and derivatives thereof
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
KR20150127197A (ko) * 2013-03-14 2015-11-16 노파르티스 아게 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
ES2665619T3 (es) * 2013-03-14 2018-04-26 Novartis Ag 3-Pirimidin-4-il-oxazolidin-2-onas como inhibidores de IDH mutante
WO2015003360A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003355A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CA2917671A1 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. 2,4-or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015010297A1 (en) * 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
PL3363790T3 (pl) 2013-09-06 2020-07-27 Aurigene Discovery Technologies Limited Pochodne 1,2,4-oksadiazolu jako immunomodulatory
WO2015127172A1 (en) * 2014-02-20 2015-08-27 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CA2946538A1 (en) 2014-04-04 2015-10-08 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof to treat non-small-cell carcinoma of the lung and ovarian cancer
AR100879A1 (es) * 2014-06-17 2016-11-09 Chiesi Farm Spa Derivados de la indolizina como inhibidores de las fosfoinositido-3 quinasas
ES2953347T3 (es) 2014-09-19 2023-11-10 Forma Therapeutics Inc Derivados de piridin-2(1H)-ona quinolinona como inhibidores de isocitrato deshidrogenasa mutante
WO2016044782A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
WO2016044787A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
JP6648116B2 (ja) * 2014-09-19 2020-02-14 フォーマ セラピューティクス,インコーポレイテッド 変異イソクエン酸デヒドロゲナーゼ阻害剤としてのキノリノンピリミジン組成物
BR112017005713B1 (pt) 2014-09-22 2023-09-26 National Health Research Institutes Composto de fórmula (i) e composição farmacêutica
HUE048997T2 (hu) 2014-10-01 2020-09-28 Daiichi Sankyo Co Ltd Izoxazol származék mutáns izocitrát dehidrogenáz 1 inhibitorként
CN107108554B (zh) * 2014-10-23 2020-11-06 德国癌症研究中心 作为midh1抑制剂用于治疗肿瘤的1-环己基-2-苯基氨基苯并咪唑
US10086000B2 (en) 2014-12-05 2018-10-02 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
JP6901394B2 (ja) 2014-12-22 2021-07-14 ザ ユナイテッド ステイツ オブ アメリカ, アズ リプレゼンテッド バイ ザ セクレタリー, デパートメント オブ ヘルス アンド ヒューマン サービシーズ 癌の処置に有用な変異型idh1阻害剤
EP4023645A1 (en) 2015-03-10 2022-07-06 Aurigene Discovery Technologies Limited 1,2,4-oxadiazole and thiadiazole compounds as immunomodulators
MX2017011612A (es) * 2015-03-10 2018-03-23 Aurigene Discovery Tech Ltd Compuestos de tiadiazol y 1,2,4-oxadiazol 3-sustituidos como inmunomoduladores.
US10294206B2 (en) 2015-04-21 2019-05-21 Forma Tm2, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US9624216B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
TWI681959B (zh) * 2015-06-09 2020-01-11 日商第一三共股份有限公司 作為變異型異檸檬酸脫氫酶1阻礙劑之異噁唑衍生物
EP3319945B1 (en) * 2015-07-07 2021-04-28 Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors
TW201708193A (zh) 2015-07-27 2017-03-01 拜耳製藥公司 突變之異檸檬酸脫氫酶idh1 r132h之抑制劑
EP3328866B1 (en) * 2015-07-27 2019-10-30 Eli Lilly and Company 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds and theit use as mutant idh1 inhibitors
TWI620748B (zh) 2016-02-05 2018-04-11 National Health Research Institutes 氨基噻唑化合物及其用途
WO2017140758A1 (en) 2016-02-19 2017-08-24 Debiopharm International S.A. Derivatives of 2-amino-4-(2-oxazolidinon-3-yl)-pyrimidine fused with a five-membered heteroaromatic ring in 5,6-position which are useful for the treatment of various cancers
CN107216312B (zh) 2016-03-22 2023-08-01 上海海和药物研究开发股份有限公司 一种具有突变型idh抑制活性的化合物、其制备方法及用途
US10696665B2 (en) 2016-06-06 2020-06-30 Eli Lilly And Company Mutant IDH1 inhibitors
CN117777121A (zh) 2016-10-24 2024-03-29 詹森药业有限公司 化合物及其用途
MY197313A (en) * 2016-12-16 2023-06-13 Lilly Co Eli 7-phenylethlamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors
CA3047136A1 (en) * 2016-12-19 2018-06-28 Isocure Biosciences Inc. Inhibitors of mutant isocitrate dehydrogenases and compositions and methods thereof
KR20190108118A (ko) 2017-01-06 2019-09-23 유마니티 테라퓨틱스, 인크. 신경계 장애의 치료를 위한 방법
CN109467538A (zh) 2017-09-07 2019-03-15 和记黄埔医药(上海)有限公司 环烯烃取代的杂芳环类化合物及其用途
WO2019061324A1 (en) 2017-09-29 2019-04-04 Curis Inc. CRYSTALLINE FORMS OF IMMUNOMODULATORS
CN111148743B (zh) 2017-10-06 2023-12-15 福马治疗有限公司 抑制泛素特异性肽酶30
JP7618445B2 (ja) 2017-10-11 2025-01-21 オーリジーン オンコロジー リミテッド 3-置換1,2,4-オキサジアゾールの結晶形態
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
KR20200083503A (ko) 2017-11-03 2020-07-08 오리진 디스커버리 테크놀로지스 리미티드 Tim-3 경로와 pd-1 경로의 이중 저해제
WO2019087092A1 (en) 2017-11-06 2019-05-09 Aurigene Discovery Technologies Limited Conjoint therapies for immunomodulation
JP7517992B2 (ja) 2018-03-23 2024-07-17 ヤンセン ファーマシューティカ エヌ.ベー. 化合物及びその使用
CN110407855A (zh) * 2018-04-26 2019-11-05 上海嗣新生物科技有限公司 2-氨基嘧啶啶衍生物及其制备方法和用途
US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
WO2019222551A1 (en) 2018-05-16 2019-11-21 Forma Therapeutics, Inc. Solid forms of ((s)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US11576906B2 (en) 2018-05-16 2023-02-14 Forma Therapeutics, Inc. Inhibiting mutant IDH-1
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Fused bicyclic compounds useful as ubiquitin-specific peptidase 30 inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
JP7258059B2 (ja) * 2018-06-26 2023-04-14 昆薬集団股▲フン▼有限公司 ベンズイミダゾール誘導体及びそのidh1阻害剤としての応用
SG11202102815SA (en) 2018-10-05 2021-04-29 Forma Therapeutics Inc Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors
BR112021014583A2 (pt) 2019-01-24 2021-10-05 Yumanity Therapeutics, Inc. Compostos e utilizações dos mesmos
AU2020245349A1 (en) * 2019-03-22 2021-11-04 Janssen Pharmaceutica Nv Compounds and uses thereof
CN111825666B (zh) * 2019-04-23 2024-03-08 上海仕谱生物科技有限公司 二聚或多聚体形式的突变型idh抑制剂
AU2020311297A1 (en) * 2019-07-10 2022-02-03 Aucentra Therapeutics Pty Ltd DERIVATIVES OF 4-(IMIDAZO[l,2-a]PYRIDIN-3-YL)-N-(PYRIDINYL)PYRIMIDIN- 2-AMINE AS THERAPEUTIC AGENTS
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
CN115335060B (zh) 2020-03-23 2024-11-12 伊莱利利公司 使用突变idh抑制剂的组合疗法
EP4319766A4 (en) * 2021-04-08 2025-05-28 Memorial Sloan Kettering Cancer Center NADK2 INHIBITION IN CANCER AND FIBROTIC DISEASES
US11746115B2 (en) 2021-08-13 2023-09-05 Eli Lilly And Company Solid forms of 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one
CN120554346A (zh) * 2024-02-28 2025-08-29 中国科学院上海药物研究所 一类噁唑酮取代的嘧啶胺化合物及其制备方法、药物组合物和用途

Family Cites Families (118)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB581334A (en) 1943-09-29 1946-10-09 Francis Henry Swinden Curd New pyrimidine compounds
JPS4921148B1 (es) 1970-12-28 1974-05-30
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
US4994386A (en) 1987-07-13 1991-02-19 Pharmacia Diagnostics, Inc. Production of HBLV virus in the HSB-2 cell line
US4929726A (en) 1988-02-09 1990-05-29 Georgia State University Foundation, Inc. Novel diazines and their method of preparation
EP0330263A1 (en) 1988-02-25 1989-08-30 Merck & Co. Inc. Piperazinylalkylpyrimidines as hypoglycemic agents
GB9012311D0 (en) 1990-06-01 1990-07-18 Wellcome Found Pharmacologically active cns compounds
US5358945A (en) 1990-07-03 1994-10-25 Mitsui Petrochemical Industries, Ltd. Pyrimidine compound and pharmaceutically acceptable salts thereof
AU692090B2 (en) 1995-04-13 1998-05-28 Taiho Pharmaceutical Co., Ltd. Novel 4,6-diarylpyrimidine derivatives and salts thereof
JP3734907B2 (ja) 1996-12-19 2006-01-11 富士写真フイルム株式会社 現像処理方法
WO1999005138A1 (en) 1997-07-24 1999-02-04 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compounds and antitumor agent containing the same as active ingredient
JPH11158073A (ja) 1997-09-26 1999-06-15 Takeda Chem Ind Ltd アデノシンa3拮抗剤
US6440965B1 (en) 1997-10-15 2002-08-27 Krenitsky Pharmaceuticals, Inc. Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system
US6150362A (en) 1997-12-12 2000-11-21 Henkin; Jack Triazine angiogenesis inhibitors
SI0930302T1 (en) 1998-01-16 2003-10-31 F. Hoffmann-La Roche Ag Benzosulfone derivatives
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
KR100581199B1 (ko) 1998-06-19 2006-05-17 카이론 코포레이션 글리코겐 신타제 키나제 3의 억제제
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
CA2359680A1 (en) 1999-01-22 2000-07-27 David M. Armistead Kinase inhibitors
EP1194152A4 (en) 1999-06-30 2002-11-06 Merck & Co Inc Links to SRC kinase inhibition
CA2383546A1 (en) 1999-06-30 2001-01-04 William H. Parsons Src kinase inhibitor compounds
US6329380B1 (en) 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
AU777735B2 (en) 1999-07-15 2004-10-28 Pharmacopeia, Inc. Bradykinin B1 receptor antagonists
JP2001089452A (ja) 1999-09-22 2001-04-03 Sankyo Co Ltd ピリミジン誘導体
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
US20030004174A9 (en) * 2000-02-17 2003-01-02 Armistead David M. Kinase inhibitors
IL151946A0 (en) 2000-03-29 2003-04-10 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
KR100774855B1 (ko) 2000-04-27 2007-11-08 아스텔라스세이야쿠 가부시키가이샤 축합 헤테로아릴 유도체
WO2001083460A1 (en) 2000-04-28 2001-11-08 Tanabe Seiyaku Co., Ltd. Cyclic compounds
WO2002000647A1 (en) 2000-06-23 2002-01-03 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
WO2002020495A2 (en) 2000-09-06 2002-03-14 Chiron Corporation Inhibitors of glycogen synthase kinase 3
ES2242771T5 (es) 2000-09-15 2011-10-14 Vertex Pharmaceuticals Incorporated Compuestos de pirazol útiles como inhibidores de proteína quinasas.
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
CN102250071A (zh) 2000-12-21 2011-11-23 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吡唑化合物
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
WO2002062766A2 (en) 2001-02-07 2002-08-15 Millennium Pharmaceuticals, Inc. Melanocortin-4 receptor binding compounds and methods of use thereof
AU2002258400A1 (en) 2001-02-16 2002-08-28 Tularik Inc. Methods of using pyrimidine-based antiviral agents
JP2004531571A (ja) 2001-05-25 2004-10-14 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン生産のインヒビターとしてのカルバメート及びオキサミド化合物
EP1397142A4 (en) 2001-06-19 2004-11-03 Bristol Myers Squibb Co PYRIMIDINE PHOSPHODIESTERASE (PDE) INHIBITORS 7
US6603000B2 (en) 2001-07-11 2003-08-05 Boehringer Ingelheim Pharmaceuticals, Inc. Synthesis for heteroarylamine compounds
WO2003030909A1 (en) 2001-09-25 2003-04-17 Bayer Pharmaceuticals Corporation 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer
ATE433973T1 (de) 2002-03-15 2009-07-15 Vertex Pharma Azolylaminoazine als inhibitoren von proteinkinasen
WO2003077921A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
ATE365733T1 (de) 2002-03-15 2007-07-15 Vertex Pharma Zusammensetzungen brauchbar als protein-kinase- inhibitoren
AU2003218215A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
AU2003245669A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
WO2004029204A2 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
AU2003288925A1 (en) 2002-10-08 2004-05-04 Massachusetts Institute Of Technology Compounds for modulation of cholesterol transport
US7223870B2 (en) 2002-11-01 2007-05-29 Pfizer Inc. Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction
MXPA05005477A (es) 2002-11-21 2005-07-25 Chiron Corp Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer.
AU2004224392A1 (en) 2003-03-24 2004-10-07 Merck & Co., Inc. Biaryl substituted 6-membered heterocyles as sodium channel blockers
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
CA2520323C (en) 2003-04-09 2013-07-09 Exelixis, Inc. Tie-2 modulators and methods of use
AU2004259712A1 (en) 2003-07-15 2005-02-03 Neurogen Corporation Substituted pyrimidin-4-ylamine analogues
CA2531619A1 (en) 2003-07-16 2005-01-27 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
EP1675830A4 (en) * 2003-09-30 2008-08-20 Scios Inc HETEROCYCLIC AMIDES AND SULFONAMIDES
DE602005024382D1 (de) 2004-04-13 2010-12-09 Astellas Pharma Inc Polycyclische pyrimidine als kaliumionenkanal-modulatoren
GB0415364D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
MY145822A (en) 2004-08-13 2012-04-30 Neurogen Corp Substituted biaryl piperazinyl-pyridine analogues
JP2008521900A (ja) 2004-11-30 2008-06-26 アムジエン・インコーポレーテツド キノリン及びキナゾリン類似体並びにがん治療のための医薬としてのその使用
CN101080401A (zh) 2004-12-13 2007-11-28 神经能质公司 经取代的二芳基类似物
CN101080228A (zh) 2004-12-13 2007-11-28 神经能质公司 哌嗪基-吡啶类似物
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
WO2006078992A2 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
CA2599320A1 (en) 2005-02-25 2006-08-31 Kudos Pharmaceuticals Limited Hydrazinomethyl, hydr zonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
TW200716594A (en) 2005-04-18 2007-05-01 Neurogen Corp Substituted heteroaryl CB1 antagonists
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
CA2635997A1 (en) 2006-01-11 2007-07-19 Astrazeneca Ab Morpholino pyrimidine derivatives and their use in therapy
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008080937A1 (en) * 2006-12-28 2008-07-10 Basf Se 2-substituted pyrimidines i in therapy
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
ATE551334T1 (de) 2007-02-06 2012-04-15 Novartis Ag Pi3-kinase-hemmer und verfahren zu ihrer verwendung
US7957951B2 (en) 2007-03-16 2011-06-07 Robert Bosch Gmbh Address translation system for use in a simulation environment
AU2008273889B2 (en) 2007-07-09 2012-03-08 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
CN101959533A (zh) 2008-03-05 2011-01-26 诺瓦提斯公司 嘧啶衍生物在治疗egfr依赖性疾病或对靶向egfr家族成员的物质具有获得性耐药性的疾病中的用途
KR20100126553A (ko) 2008-03-26 2010-12-01 노파르티스 아게 Vegf-유도성 혈관신생 과정의 유력한 조절제로서의 이미다조퀴놀린 및 피리미딘 유도체
WO2009120094A2 (en) 2008-03-27 2009-10-01 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
JP5277256B2 (ja) 2008-04-09 2013-08-28 田辺三菱製薬株式会社 maxi−Kチャネル開口薬としてのピリミジン、ピリジン及びトリアジン誘導体
GB0815369D0 (en) 2008-08-22 2008-10-01 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2349275B1 (en) 2008-10-31 2017-03-08 Novartis AG Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor.
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
US8513242B2 (en) 2008-12-12 2013-08-20 Cystic Fibrosis Foundation Therapeutics, Inc. Pyrimidine compounds and methods of making and using same
JP5747440B2 (ja) 2009-02-06 2015-07-15 住友化学株式会社 ヒドラジド化合物及びその有害生物防除用途
HRP20140265T1 (hr) 2009-02-06 2014-04-25 Nippon Shinyaku Co., Ltd. Derivat aminopirazina i odgovarajuä†i lijek
JP6067226B2 (ja) 2009-03-13 2017-01-25 アジオス ファーマシューティカルズ, インコーポレイテッド 細胞増殖関連疾患のための方法および組成物
WO2010120994A2 (en) 2009-04-17 2010-10-21 Wyeth Llc Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
CA2760911A1 (en) 2009-05-19 2010-11-25 George E. Davis Compounds and methods for controlling fungi
US8486939B2 (en) 2009-07-07 2013-07-16 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
AR077999A1 (es) 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
WO2011031896A2 (en) 2009-09-09 2011-03-17 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
WO2011072174A1 (en) * 2009-12-09 2011-06-16 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
US9133123B2 (en) 2010-04-23 2015-09-15 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
WO2011143160A2 (en) 2010-05-10 2011-11-17 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
JP6081354B2 (ja) 2010-07-16 2017-02-15 アジオス ファーマシューティカルズ, インコーポレイテッド 治療活性組成物およびそれらの使用方法
AU2011308856B2 (en) 2010-10-01 2015-04-23 Novartis Ag Manufacturing process for pyrimidine derivatives
LT2629776T (lt) 2010-10-18 2017-11-10 Cerenis Therapeutics Holding Sa Junginiai, kompozicijos ir būdai, tinkami cholesterolio mobilizavimui
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
WO2012109423A1 (en) 2011-02-11 2012-08-16 Dana-Farber Cancer Institute, Inc. Method of inhibiting hamartoma tumor cells
CN102827073A (zh) 2011-06-17 2012-12-19 安吉奥斯医药品有限公司 治疗活性组合物和它们的使用方法
JP2014527542A (ja) 2011-09-01 2014-10-16 ノバルティス アーゲー 骨がんの治療に使用するためまたは原発がん細胞の骨への転移性播種を予防するためのpi3k阻害剤
AU2012318874A1 (en) 2011-10-06 2014-05-15 Merck Sharp & Dohme Corp. 1,3-substituted azetidine PDE10 inhibitors
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
US10213432B2 (en) 2012-05-16 2019-02-26 Novartis Ag Dosage regimen for a PI-3 kinase inhibitor
JP2015518888A (ja) 2012-06-06 2015-07-06 ノバルティス アーゲー 腫瘍疾患を治療するための17−アルファ−ヒドロキシラーゼ(c17,20−リアーゼ)インヒビターと特定のpi−3kインヒビターとの組み合わせ
WO2014028566A1 (en) 2012-08-16 2014-02-20 Novartis Ag Combination of pi3k inhibitor and c-met inhibitor
ES2605638T3 (es) 2012-10-23 2017-03-15 Novartis Ag Proceso Mejorado para fabricar 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
CN103483345B (zh) 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
CN103694218B (zh) 2013-12-05 2016-04-27 中山大学 嘧啶化合物、pi3k抑制剂、包含pi3k抑制剂的药物组合物及应用

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