CL2014000746A1 - Compuestos derivados de 3-pirimidin-4-il-oxazolidin-2-ona y sus sales, como inhibidores de las proteinas idh mutantes; composicion farmaceutica que los comprende, utiles para el tratamiento de trastornos de la proliferacion celular tal como el cancer. - Google Patents

Compuestos derivados de 3-pirimidin-4-il-oxazolidin-2-ona y sus sales, como inhibidores de las proteinas idh mutantes; composicion farmaceutica que los comprende, utiles para el tratamiento de trastornos de la proliferacion celular tal como el cancer.

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Publication number
CL2014000746A1
CL2014000746A1 CL2014000746A CL2014000746A CL2014000746A1 CL 2014000746 A1 CL2014000746 A1 CL 2014000746A1 CL 2014000746 A CL2014000746 A CL 2014000746A CL 2014000746 A CL2014000746 A CL 2014000746A CL 2014000746 A1 CL2014000746 A1 CL 2014000746A1
Authority
CL
Chile
Prior art keywords
oxazolidin
pyrimidin
disorders
inhibitors
cancer
Prior art date
Application number
CL2014000746A
Other languages
English (en)
Inventor
Zhao Qian
Shin Cho Young
Yang Fan
Roy Levell Julian
Toure Bakary-Barry
Caferro Thomas
Lei Huangshu
Lenoir Francois
Liu Gang
G Palermo Mark
David Shultz Michael
D Smith Troy
Q Costales Abran
Bruce Pfister Keith
Sendzik Martin
Shafer Cynthia
Sutton James
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 CL2014000746A1 publication Critical patent/CL2014000746A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/04—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic 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
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/02—Heterocyclic 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
    • C07D513/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (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)
CL2014000746A 2011-09-27 2014-03-26 Compuestos derivados de 3-pirimidin-4-il-oxazolidin-2-ona y sus sales, como inhibidores de las proteinas idh mutantes; composicion farmaceutica que los comprende, utiles para el tratamiento de trastornos de la proliferacion celular tal como el cancer. CL2014000746A1 (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
CL2014000746A1 true CL2014000746A1 (es) 2014-10-03

Family

ID=47178237

Family Applications (1)

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CL2014000746A CL2014000746A1 (es) 2011-09-27 2014-03-26 Compuestos derivados de 3-pirimidin-4-il-oxazolidin-2-ona y sus sales, como inhibidores de las proteinas idh mutantes; composicion farmaceutica que los comprende, utiles para el tratamiento de trastornos de la proliferacion celular tal como el cancer.

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 (66)

* 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
EP2822944A1 (en) * 2012-03-05 2015-01-14 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
MX2015012822A (es) * 2013-03-14 2016-05-31 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante.
CA2903979A1 (en) * 2013-03-14 2014-09-18 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
WO2015003355A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
CN105593215B (zh) * 2013-07-11 2019-01-15 安吉奥斯医药品有限公司 用于治疗癌症的作为idh2突变体抑制剂的2,4-或4,6-二氨基嘧啶化合物
WO2015003360A2 (en) * 2013-07-11 2015-01-15 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
RS57508B1 (sr) 2013-09-06 2018-10-31 Aurigene Discovery Tech Ltd 1,2,4-derivati oksadiazola kao imunomodulatori
WO2015127172A1 (en) * 2014-02-20 2015-08-27 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
KR102359214B1 (ko) 2014-04-04 2022-02-07 델 마 파마슈티컬스 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체
ES2750791T3 (es) * 2014-06-17 2020-03-27 Chiesi Farm Spa Derivados de indolizina como inhibidores de fosfoinositido 3-quinasas
WO2016044787A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
WO2016044781A1 (en) * 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
HUE062424T2 (hu) 2014-09-19 2023-11-28 Forma Therapeutics Inc Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok
CA2961807A1 (en) 2014-09-19 2016-03-24 Forma Therapeutics, Inc. Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
CA2962329C (en) 2014-09-22 2023-12-19 Yu-Sheng Chao Heterocyclic compounds and use thereof
LT3202766T (lt) 2014-10-01 2020-05-11 Daiichi Sankyo Company, Limited Izoksazolo darinys, kaip mutuotos izocitrato dehidrogenazės 1 inhibitorius
JP6672288B2 (ja) 2014-10-23 2020-03-25 バイエル・ファルマ・アクティエンゲゼルシャフト 腫瘍の治療のためのmidh1阻害剤としての1−シクロヘキシル−2−フェニルアミノベンゾイミダゾール
US10086000B2 (en) 2014-12-05 2018-10-02 Merck Sharp & Dohme Corp. Tricyclic compounds as inhibitors of mutant IDH enzymes
ES2905564T3 (es) 2014-12-22 2022-04-11 Us Health Inhibidores mutantes de IDH1 útiles para tratar el cáncer
EA201791621A1 (ru) * 2015-03-10 2018-02-28 Ауриджен Дискавери Текнолоджис Лимитед 3-замещенные-1,2,4-оксадиазольные и тиадиазольные соединения в качестве иммуномодуляторов
KR102894264B1 (ko) 2015-03-10 2025-12-02 오리진 온콜로지 리미티드 면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
US9624175B2 (en) 2015-04-21 2017-04-18 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
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
WO2017019429A1 (en) * 2015-07-27 2017-02-02 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
JP6682043B2 (ja) * 2016-06-06 2020-04-15 イーライ リリー アンド カンパニー 変異体idh1阻害剤
EP3529245A4 (en) 2016-10-24 2020-12-23 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THE LATEST
JP6793836B2 (ja) * 2016-12-16 2020-12-02 イーライ リリー アンド カンパニー 変異体idh1およびidh2阻害剤としての7−フェニルエチルアミノ−4h−ピリミド[4,5−d][1,3]オキサジン−2−オン化合物
CN110291085B (zh) * 2016-12-19 2023-01-24 艾科生物科技有限公司 突变型异柠檬酸脱氢酶抑制剂、组合物及其方法
MA47212A (fr) 2017-01-06 2019-11-13 Yumanity Therapeutics Inc Méthodes de traitement de troubles neurologiques
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
AU2018346597B2 (en) 2017-10-06 2023-07-13 Forma Therapeutics, Inc. Inhibiting Ubiquitin Specific Peptidase 30
AU2018348350B2 (en) 2017-10-11 2024-05-02 Aurigene Oncology Limited Crystalline forms of 3-substituted 1,2,4-oxadiazole
WO2019084157A1 (en) 2017-10-24 2019-05-02 Yumanity Therapeutics, Inc. COMPOUNDS AND USES THEREOF
MX2020004531A (es) 2017-11-03 2020-08-03 Aurigene Discovery Tech Ltd Inhibidores dobles de tim-3 y las vias de pd-1.
EP3706798A1 (en) 2017-11-06 2020-09-16 Aurigene Discovery Technologies Limited Conjoint therapies for immunomodulation
ES3043183T3 (en) 2018-03-23 2025-11-25 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
US11013733B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1)
SMT202300073T1 (it) 2018-05-16 2023-05-12 Forma Therapeutics Inc Inibizione di idh-1 mutante
US11311527B2 (en) 2018-05-16 2022-04-26 Forma Therapeutics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
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
IL278291B2 (en) 2018-05-17 2023-10-01 Forma Therapeutics Inc Condensed bicyclic compounds are useful as ubiquitin-specific peptidase 30 inhibitors
US10980788B2 (en) 2018-06-08 2021-04-20 Agios Pharmaceuticals, Inc. Therapy for treating malignancies
AU2019296173B2 (en) * 2018-06-26 2022-01-06 Kpc Pharmaceuticals, Inc. Benzimidazole derivatives and use thereof as IDH1 inhibitors
EP4218934B1 (en) 2018-10-05 2025-06-18 Forma Therapeutics, Inc. Inhibiting ubiquitin-specific protease 30 (usp30)
MA54829A (fr) 2019-01-24 2021-12-01 Yumanity Therapeutics Inc Composés et leurs utilisations
US20230078764A1 (en) * 2019-03-22 2023-03-16 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
CN114269742B (zh) * 2019-07-10 2024-07-16 常州千红生化制药股份有限公司 作为治疗剂的4-(咪唑并[1,2-a]吡啶-3-基)-N-(吡啶基)嘧啶-2-胺的衍生物
EA202192047A1 (ru) 2019-11-13 2021-12-08 Юманити Терапьютикс, Инк. Соединения и их применение
AU2021242260B2 (en) 2020-03-23 2023-12-14 Eli Lilly And Company Combination therapy with a mutant IDH inhibitor
EP4319766A4 (en) * 2021-04-08 2025-05-28 Memorial Sloan Kettering Cancer Center NADK2 INHIBITION IN CANCER AND FIBROTIC DISEASES
EP4384273A1 (en) 2021-08-13 2024-06-19 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
WO1992000970A1 (en) 1990-07-03 1992-01-23 Mitsui Petrochemical Industries, Limited Pyrimidine compound and pharmaceutically acceptable salt 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
ES2213286T3 (es) 1997-07-24 2004-08-16 Zenyaku Kogyo Kabushiki Kaisha Compuestos heterociclicos y agente antitumoral que los contiene como ingredientes activos.
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
DK0930302T3 (da) 1998-01-16 2003-07-21 Hoffmann La Roche Benzosulfonderivater
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville Glycogen synthase kinase 3 inhibitoren
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
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
WO2001000214A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
US6329380B1 (en) 1999-06-30 2001-12-11 Merck & Co., Inc. SRC kinase inhibitor compounds
EP1206265B1 (en) 1999-06-30 2003-11-12 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
ATE250053T1 (de) 1999-07-15 2003-10-15 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
KR20030024659A (ko) * 2000-02-17 2003-03-26 암겐 인코포레이티드 키나제 억제제
GB2361236B (en) 2000-03-29 2002-04-24 Cyclacel Ltd Pyrimidines useful against proliferative disorders
AU5261001A (en) 2000-04-27 2001-11-12 Imperial Cancer Research Technology Ltd Condensed heteroaryl derivatives
KR100711042B1 (ko) 2000-04-28 2007-04-24 다나베 세이야꾸 가부시키가이샤 환상 화합물
AU2001268711A1 (en) 2000-06-23 2002-01-08 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
AU2001290912A1 (en) 2000-09-15 2002-03-26 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
BR0116493A (pt) 2000-12-21 2003-09-30 Vertex Pharma Compostos de pirazol úteis como inibidores de proteìna cinase
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
EP1363890A4 (en) 2001-02-07 2009-06-10 Ore Pharmaceuticals Inc MELANOCORTIN-4-RECEPTOR BINDING COMPOUNDS AND METHOD FOR THEIR APPLICATION
AU2002258400A1 (en) 2001-02-16 2002-08-28 Tularik Inc. Methods of using pyrimidine-based antiviral agents
MXPA03010724A (es) 2001-05-25 2004-03-02 Boehringer Ingelheim Pharma Compuestos de carbamato y oxamida como inhibidores de la produccion de citocina.
CA2450934A1 (en) 2001-06-19 2002-12-27 Marco Dodier Pyrimidine inhibitors of phosphodiesterase (pde) 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
US20040009981A1 (en) 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
US6846928B2 (en) 2002-03-15 2005-01-25 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
WO2003077921A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
AU2003245669A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
AU2003275242B2 (en) 2002-09-27 2010-03-04 Merck Sharp & Dohme Corp. Substituted pyrimidines
JP2006515274A (ja) 2002-10-08 2006-05-25 マサチューセッツ・インスティテュート・オブ・テクノロジー コレステロール輸送の調節のための化合物
US7223870B2 (en) 2002-11-01 2007-05-29 Pfizer Inc. Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction
DK2316831T3 (da) 2002-11-21 2013-06-10 Novartis Ag 2-(Morpholin-4-yl)pyrimidiner som phosphotidylinositol (PI)-3-kinaseinhibitorer samt deres anvendelse ved behandling af cancer
WO2004084824A2 (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
JP4895806B2 (ja) 2003-04-09 2012-03-14 エクセリクシス, インク. Tie−2モジュレータと使用方法
EP1651619A1 (en) 2003-07-15 2006-05-03 Neurogen Corporation Substituted pyrimidin-4-ylamin analogues as vanilloid receptor ligands
CA2531619A1 (en) 2003-07-16 2005-01-27 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
JP2007532669A (ja) 2004-04-13 2007-11-15 イカジェン インコーポレイテッド カリウムイオンチャネル調節剤としての多環式ピリミジン
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
MX2007006230A (es) 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
CA2590299A1 (en) 2004-12-13 2006-06-22 Neurogen Corporation Piperazinyl-pyridine analogues
WO2006071538A2 (en) 2004-12-13 2006-07-06 Neurogen Corporation Substituted biaryl analogues
PL1836169T3 (pl) 2004-12-28 2012-07-31 Kinex Pharmaceuticals Llc Kompozycje i sposoby leczenia zaburzeń związanych z proliferacją komórek
EP1838703A2 (en) 2005-01-19 2007-10-03 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
EP1877388A2 (en) 2005-02-25 2008-01-16 Kudos Pharmaceuticals Ltd Hydrazinomethyl, hydrazonomethyl and 5-membered heterocylic compounds which act as mtor inhibitors and their use as anti cancer agents
EP1871762A2 (en) 2005-04-18 2008-01-02 Neurogen Corporation Subtituted 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
KR20080083188A (ko) 2006-01-11 2008-09-16 아스트라제네카 아베 모르폴리노 피리미딘 유도체 및 요법에서의 그 유도체의용도
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
AR064571A1 (es) * 2006-12-28 2009-04-08 Basf Ag Pirimidinas sustituidas en posicion 2 por heterociclos nitrogenados, medicamentos y composiciones farmaceuticas que las contienen y usos de las mismas en el tratamiento del cancer.
CA2675558A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
US7957951B2 (en) 2007-03-16 2011-06-07 Robert Bosch Gmbh Address translation system for use in a simulation environment
JP2010533158A (ja) 2007-07-09 2010-10-21 アストラゼネカ アクチボラグ 化合物類−945
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
EP2474323A3 (en) 2008-03-26 2012-10-10 Novartis AG Imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
WO2009120094A2 (en) 2008-03-27 2009-10-01 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
EP2280948A1 (en) 2008-04-09 2011-02-09 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
CA2736361C (en) 2008-10-31 2017-10-10 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
WO2010068863A2 (en) 2008-12-12 2010-06-17 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
JP5263304B2 (ja) * 2009-02-06 2013-08-14 日本新薬株式会社 アミノピラジン誘導体及び医薬
CN102985557B (zh) 2009-03-13 2018-06-15 安吉奥斯医药品有限公司 用于细胞增殖相关病症的方法和组合物
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
PE20120325A1 (es) 2009-05-19 2012-04-12 Dow Agrosciences Llc Aminopirimidinas sustituidas con arilo como agentes fungicidas
CA2767008C (en) 2009-07-07 2018-01-30 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
EP2462123B1 (en) 2009-08-04 2013-10-02 Merck Sharp & Dohme Corp. 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
KR20120063515A (ko) 2009-09-09 2012-06-15 아빌라 테라퓨틱스, 인크. Pi3 키나제 억제제 및 이들의 용도
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
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
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
US20130109643A1 (en) 2010-05-10 2013-05-02 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
CN104945373A (zh) 2010-10-01 2015-09-30 诺华有限公司 制造嘧啶衍生物的方法
HRP20171587T1 (hr) 2010-10-18 2017-12-01 Cerenis Therapeutics Holding Sa Spojevi, pripravci i postupci pogodni za mobilizaciju kolesterola
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
CA2826387A1 (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
KR20140059786A (ko) 2011-09-01 2014-05-16 노파르티스 아게 골암의 치료에 사용하기 위한 또는 골 내로의 원발성 암 세포의 전이성 파종을 예방하기 위한 pi3k 억제제
US9365562B2 (en) 2011-10-06 2016-06-14 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
CN104349779A (zh) 2012-05-16 2015-02-11 诺华股份有限公司 Pi-3激酶抑制剂的剂量方案
CA2872541A1 (en) 2012-06-06 2013-12-12 Novartis Ag Combination of a 17 -alpha -hydroxylase (c17, 20 - lyase) inhibitor and a specific pi-3k inhibitor for treating a tumor disease
CA2879704A1 (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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