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PE20141581A1 - 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
PE20141581A1
PE20141581A1 PE2014000427A PE2014000427A PE20141581A1 PE 20141581 A1 PE20141581 A1 PE 20141581A1 PE 2014000427 A PE2014000427 A PE 2014000427A PE 2014000427 A PE2014000427 A PE 2014000427A PE 20141581 A1 PE20141581 A1 PE 20141581A1
Authority
PE
Peru
Prior art keywords
deuterium
oxazolidin
phenyl
pirmidin
onas
Prior art date
Application number
PE2014000427A
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 D 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 PE20141581A1 publication Critical patent/PE20141581A1/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
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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
    • C07D487/02Heterocyclic 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
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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
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    • 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
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    • 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)
  • Veterinary Medicine (AREA)
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  • Life Sciences & Earth Sciences (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

SE REFIERE A UN COMPUESTO DE FORMULA (I) , DONDE R1 Y R2 SON CADA UNO H, DEUTERIO, HALO, HIDROXILO, ENTRE OTROS; R3a ES H, DEUTERIO, FENILO, ENTRE OTROS; R3b ES H, DEUTERIO, ENTRE OTROS; R4a ES H, ALQUILO, FENILO, BENCILO, ENTRE OTROS; R4b ES H, DEUTERIO, ALQUILO, ENTRE OTROS; R5a ES H, DEUTERIO; R5b ES H, DEUTERIO, METILO, ETILO, ENTRE OTROS; R6 ES ALQUILO C1-C6; HETEROARILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS (S)-5,5-DIMETIL-4-FENIL-2-(2-((S)-1-FENILETILAMINO) PIRIMIDIN-4-IL) OXAZOLIDIN-2-ONA; (S)-3-(2-((S)-1-(4-HIDROXIFENIL) ETILAMINO)PIRIMIDIN-4-IL)-4-ISOPROPILOXAZOLIDIN-2-ONA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE ES UTIL PARA EL TRATAMIENTO DE ENFERMEDADES ASOCIADAS CON LAS PROTEINAS IDH MUTANTES QUE TIENE ACTIVIDAD NEOMORFICA.
PE2014000427A 2011-09-27 2012-09-26 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante PE20141581A1 (es)

Applications Claiming Priority (1)

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US201161539553P 2011-09-27 2011-09-27

Publications (1)

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PE20141581A1 true PE20141581A1 (es) 2014-11-14

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Country Status (32)

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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
WO2014141104A1 (en) 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
CA2903176A1 (en) * 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
AU2014287121B2 (en) * 2013-07-11 2018-11-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as IDH2 mutants inhibitors for the treatment of cancer
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
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
HRP20181052T1 (hr) 2013-09-06 2018-09-07 Aurigene Discovery Technologies Limited Derivati 1,2,4-oksadiazola kao imunomodulatori
WO2015127172A1 (en) * 2014-02-20 2015-08-27 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
EP3125920B1 (en) 2014-04-04 2020-12-23 Del Mar Pharmaceuticals Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer
EP3157920B1 (en) * 2014-06-17 2019-08-07 Chiesi Farmaceutici S.p.A. Indolizine derivatives as phosphoinositide 3-kinases inhibitors
WO2016044781A1 (en) * 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
ES2706888T3 (es) 2014-09-19 2019-04-01 Forma Therapeutics Inc Referencia cruzada a aplicaciones relacionadas
ES2953347T3 (es) 2014-09-19 2023-11-10 Forma Therapeutics Inc Derivados de piridin-2(1H)-ona quinolinona como inhibidores de isocitrato deshidrogenasa mutante
MX373789B (es) 2014-09-19 2020-03-23 Forma Therapeutics Inc Derivados de piridinil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh).
EP3197885B1 (en) 2014-09-22 2020-11-18 National Health Research Institutes Heterocyclic compounds and use thereof
SMT202000275T1 (it) * 2014-10-01 2020-07-08 Daiichi Sankyo Co Ltd Derivato isossazolico come inibitore dell'isocitrato deidrogenasi 1 mutata
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
CN107428690B (zh) 2014-12-22 2021-04-13 美国政府健康及人类服务部 可用于治疗癌症的突变idh1抑制剂
CU20170118A7 (es) * 2015-03-10 2018-02-08 Aurigene Discovery Tech Ltd Compuestos de tiadiazol y 1,2,4-oxadiazol 3-sustituidos como inmunomoduladores
KR102708045B1 (ko) 2015-03-10 2024-09-23 오리진 온콜로지 리미티드 면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
WO2016171755A1 (en) 2015-04-21 2016-10-27 Forma Therapeutics, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US10407419B2 (en) 2015-04-21 2019-09-10 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
WO2017005674A1 (en) * 2015-07-07 2017-01-12 Bayer Pharma Aktiengesellschaft 2-aryl- and 2-arylalkyl-benzimidazoles as midh1 inhibitors
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
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
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
JP2019533022A (ja) 2016-10-24 2019-11-14 ユマニティ セラピューティクス,インコーポレーテッド 化合物及びその使用
ES2941631T3 (es) * 2016-12-16 2023-05-24 Lilly Co Eli Compuestos de Pirido[4,3-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes
WO2018118793A1 (en) * 2016-12-19 2018-06-28 Isocure Biosciences Inc. Inhibitors of mutant isocitrate dehydrogenases and compositions and methods thereof
ES3025460T3 (en) 2017-01-06 2025-06-09 Janssen Pharmaceutica Nv Scd inhibitor for the treatment of neurological disorders
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
US11247987B2 (en) 2017-10-06 2022-02-15 Forma Therapeutics, Inc. Inhibiting ubiquitin specific peptidase 30
CN111194308A (zh) 2017-10-11 2020-05-22 奥瑞基尼探索技术有限公司 3-取代的1,2,4-噁二唑的结晶形式
CA3083000A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. Compounds and uses thereof
WO2019087087A1 (en) 2017-11-03 2019-05-09 Aurigene Discovery Technologies Limited Dual inhibitors of tim-3 and pd-1 pathways
EA202090749A1 (ru) 2017-11-06 2020-08-19 Ориджен Дискавери Текнолоджис Лимитед Способы совместной терапии для иммуномодуляции
EP3768269B1 (en) 2018-03-23 2025-08-20 Janssen Pharmaceutica NV Compounds and uses thereof
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
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
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
HUE061331T2 (hu) 2018-05-16 2023-06-28 Forma Therapeutics Inc Mutáns IDH-1 gátlása
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)
EP3793997B1 (en) 2018-05-17 2024-03-13 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
CN112533903B (zh) 2018-06-26 2022-08-16 昆药集团股份有限公司 苯并咪唑衍生物及其作为idh1抑制剂的应用
LT3860989T (lt) 2018-10-05 2023-06-12 Forma Therapeutics, Inc. Sulieti pirolinai, kurie veikia kaip ubikvitinui specifinės proteazės 30 (ups30) inhibitoriai
WO2020154571A1 (en) 2019-01-24 2020-07-30 Yumanity Therapeutics, Inc. Compounds and uses thereof
CA3134510A1 (en) * 2019-03-22 2020-10-01 Yumanity Therapeutics, Inc. 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
IL296092A (en) 2020-03-23 2022-11-01 Lilly Co Eli Combination therapy with a mutant idh inhibitor
US20240209353A1 (en) * 2021-04-08 2024-06-27 Memorial Sloan-Kettering Cancer Center Nadk2 inhibition in cancer and fibrotic disorders
WO2023018955A1 (en) 2021-08-13 2023-02-16 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
US5786355A (en) 1995-04-13 1998-07-28 Taiho Pharmaceutical Co., Ltd. 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
KR100563514B1 (ko) 1997-07-24 2006-03-27 젠야쿠코교가부시키가이샤 헤테로고리 화합물 및 이를 유효성분으로 하는 항종양제
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
DE69906397T2 (de) 1998-01-16 2004-02-19 F. Hoffmann-La Roche Ag Benzosulfonderivate
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
WO2000043373A2 (en) 1999-01-22 2000-07-27 Amgen Inc. Kinase inhibitors
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
AU6605200A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
EP1194152A4 (en) 1999-06-30 2002-11-06 Merck & Co Inc Links to SRC kinase inhibition
WO2001000213A1 (en) 1999-06-30 2001-01-04 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
DE60005355T2 (de) 1999-07-15 2004-07-01 Pharmacopeia, Inc. Bradikinin b1 rezeptor antagonisten
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
AU2001237041B9 (en) * 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
CA2401748A1 (en) 2000-03-29 2001-10-04 Cyclacel Limited 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
MXPA02010693A (es) 2000-04-28 2003-03-10 Tanabe Seiyaku Co Compuestos ciclicos.
WO2002000647A1 (en) 2000-06-23 2002-01-03 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
AU2001295026B2 (en) 2000-09-06 2008-04-03 Novartis Vaccines And Diagnostics, Inc. Inhibitors of glycogen synthase kinase 3
WO2002022607A1 (en) 2000-09-15 2002-03-21 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
MXPA03005609A (es) 2000-12-21 2003-10-06 Vertex Pharma Compuestos de pirazol utiles como inhibidores de la proteina cinasa.
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
CA2448626A1 (en) 2001-05-25 2002-12-05 Boehringer Ingelheim Pharmaceuticals, Inc. Carbamate and oxamide compounds as inhibitors of cytokine production
JP2005500294A (ja) 2001-06-19 2005-01-06 ブリストル−マイヤーズ スクイブ カンパニー ホスホジエステラーゼ7に対するピリミジン阻害剤
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
US7091343B2 (en) 2002-03-15 2006-08-15 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
AU2003225800A1 (en) 2002-03-15 2003-09-29 Hayley Binch Azolylaminoazine as inhibitors of protein kinases
EP1485376B1 (en) 2002-03-15 2007-06-27 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
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
US7405221B2 (en) 2002-09-27 2008-07-29 Merck & Co., Inc. Substituted pyrimidines
WO2004032716A2 (en) 2002-10-08 2004-04-22 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
EP2316831B1 (en) 2002-11-21 2013-03-06 Novartis AG 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles as sodium channel blockers
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
EP1610774A4 (en) 2003-04-09 2008-07-16 Exelixis Inc TIE-2 MODULATORS AND METHODS OF USE
JP2007523875A (ja) 2003-07-15 2007-08-23 ニューロジェン・コーポレーション バニロイド受容体リガンドとしての置換ピリミジン−4−イルアミン類縁体
EP1644358A2 (en) 2003-07-16 2006-04-12 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
WO2005033072A2 (en) * 2003-09-30 2005-04-14 Scios Inc. Heterocyclic amides and sulfonamides
WO2005099711A1 (en) 2004-04-13 2005-10-27 Icagen, Inc. Polycyclic pyrimidines as potassium ion channel modulators
GB0415365D0 (en) 2004-07-09 2004-08-11 Astrazeneca Ab Pyrimidine derivatives
GB0415364D0 (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
EP1827434B1 (en) 2004-11-30 2014-01-15 Amgen Inc. Quinolines and quinazoline analogs and their use as medicaments for treating cancer
AU2005317176A1 (en) 2004-12-13 2006-06-22 Neurogen Corporation Piperazinyl-pyridine analogues
US20080132509A1 (en) 2004-12-13 2008-06-05 Neurogen Corporation Substituted Biaryl Analogues
CN103274961B (zh) 2004-12-28 2016-05-18 阿西纳斯公司 治疗细胞增殖紊乱的化合物和方法
WO2006078992A2 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
WO2006090167A2 (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
US20070078135A1 (en) 2005-04-18 2007-04-05 Neurogen Corporation 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
EP1979325A1 (en) 2006-01-11 2008-10-15 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
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
TW200833342A (en) * 2006-12-28 2008-08-16 Basf Ag 2-substituted pyrimidines I in therapy
KR20090108124A (ko) 2007-02-06 2009-10-14 노파르티스 아게 Pi 3-키나제 억제제 및 그의 사용 방법
US7957951B2 (en) 2007-03-16 2011-06-07 Robert Bosch Gmbh Address translation system for use in a simulation environment
KR20100031639A (ko) 2007-07-09 2010-03-23 아스트라제네카 아베 증식성 질환의 치료용 삼중 치환된 피리미딘 유도체
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
BRPI0908049A2 (pt) 2008-03-05 2015-08-11 Novartis Ag Uso de derivados de pririmidina para o tratamento de doenças dependentes de egfr ou de doenças que possuem resistência adquirida a agentes que são direcionados aos membros da família de egfr
WO2009118324A1 (en) 2008-03-26 2009-10-01 Novartis Ag 5imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
US20110053907A1 (en) 2008-03-27 2011-03-03 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
WO2009125870A1 (en) 2008-04-09 2009-10-15 Mitsubishi Tanabe Pharma Corporation Pyrimidine, pyridine and triazine derivatives as maxi-k channel openers.
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
AU2010211672B2 (en) 2009-02-06 2016-08-04 Nippon Shinyaku Co., Ltd. Aminopyrazine derivative and medicine
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
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
US8759356B2 (en) 2009-05-19 2014-06-24 Dow Agrosciences, Llc. Compounds and methods for controlling fungi
EP2532659A1 (en) 2009-07-07 2012-12-12 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
US20110230476A1 (en) 2009-09-09 2011-09-22 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
ES2642109T3 (es) 2009-12-09 2017-11-15 Agios Pharmaceuticals, Inc. Compuestos terapéuticamente activos para su uso en el tratamiento de cáncer caracterizados por tener una mutación de IDH
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
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
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
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
CN103097340B (zh) 2010-07-16 2018-03-16 安吉奥斯医药品有限公司 治疗活性组合物及其使用方法
CN103140479B (zh) 2010-10-01 2015-04-08 诺华有限公司 制造嘧啶衍生物的方法
SMT201700533T1 (it) 2010-10-18 2018-01-11 Cerenis Therapeutics Holding Sa Composti, composizioni e metodi utili per la mobilitazione del colesterolo
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
BR112014004577A2 (pt) 2011-09-01 2017-04-04 Novartis Ag inibidor pi3k para uso no tratamento de câncer ósseo ou para prevenção por metástase de células cancerosas primárias para os ossos
WO2013052395A1 (en) 2011-10-06 2013-04-11 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
EP2849756A1 (en) 2012-05-16 2015-03-25 Novartis AG Dosage regimen for a pi-3 kinase inhibitor
EP2858631A1 (en) 2012-06-06 2015-04-15 Novartis AG Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease
US20150216870A1 (en) 2012-08-16 2015-08-06 Novartis Ag Combination of PI3K Inhibitor and C-Met Inhibitor
IN2015DN01331A (es) 2012-10-23 2015-07-03 Novartis Ag
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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