[go: up one dir, main page]

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

Links

Classifications

    • 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
    • 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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

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

ID=47178237

Family Applications (1)

Application Number Title Priority Date Filing Date
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 (64)

* 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
PE20151939A1 (es) * 2013-03-14 2016-01-08 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
BR112015022483A2 (pt) * 2013-03-14 2017-07-18 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante
WO2015003355A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015003360A2 (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
WO2015010297A1 (en) * 2013-07-25 2015-01-29 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
HUE038169T2 (hu) 2013-09-06 2018-09-28 Aurigene Discovery Tech Ltd 1,2,4-Oxadiazol származékok mint immunomodulátorok
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
GEP20186938B (en) * 2014-06-17 2018-12-25 Chiesi Farma Spa Indolizine derivatives as phoshoinositide 3-kinases inhibitors
US9815817B2 (en) * 2014-09-19 2017-11-14 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
MX373789B (es) 2014-09-19 2020-03-23 Forma Therapeutics Inc Derivados de piridinil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh).
JP6820836B2 (ja) 2014-09-19 2021-01-27 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フェニルキノリノン誘導体
FI3733662T3 (fi) 2014-09-19 2023-08-09 Forma Therapeutics Inc Pyridin-2(1h)-oni-kinolinonijohdannaisia mutantti-isositraattidehydrogenaasin estäjinä
WO2016048861A2 (en) 2014-09-22 2016-03-31 National Health Research Institutes 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
CA2965213A1 (en) * 2014-10-23 2016-04-28 Bayer Pharma Aktiengesellschaft 1-cyclohexyl-2-phenylaminobenzimidazoles as midh1 inhibitors for the treatment of tumors
EP3226690B1 (en) * 2014-12-05 2020-05-20 Merck Sharp & Dohme Corp. Novel 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
HUE058274T2 (hu) 2015-03-10 2022-07-28 Aurigene Discovery Tech Ltd 1,2,4-oxadiazol és tiadiazol-vegyületek, mint immunmodulátorok
MX2017011612A (es) * 2015-03-10 2018-03-23 Aurigene Discovery Tech Ltd Compuestos de tiadiazol y 1,2,4-oxadiazol 3-sustituidos como inmunomoduladores.
US10407419B2 (en) 2015-04-21 2019-09-10 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
US10294206B2 (en) 2015-04-21 2019-05-21 Forma Tm2, Inc. Fused-bicyclic aryl quinolinone derivatives 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
JP6824952B2 (ja) * 2015-07-07 2021-02-03 ドイチェス クレープスフォルシュングスツェントルム シュティフトゥング デス エッフェントリッヒェン レヒツ ｍＩＤＨ１阻害剤としての２−アリール−および２−アリールアルキル−ベンズイミダゾール
US10253041B2 (en) 2015-07-27 2019-04-09 Eli Lilly And Company 7-phenylethylamino-4H-pyrimido[4,5-d][1,3]oxazin-2-one compounds and their 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
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
US11970486B2 (en) 2016-10-24 2024-04-30 Janssen Pharmaceutica Nv Compounds and uses thereof
PH12019501328B1 (en) * 2016-12-16 2023-05-12 Lilly Co Eli 7-phenylethlamino-4h-pyrimido][4,5-d][1,3] oxazin-2-one compounds as mutant 1dh1 and 1dh2 inhibitors
EP3555079A4 (en) * 2016-12-19 2020-08-19 Isocure Biosciences Inc. INHIBITORS OF MUTANT ISOCITRATEHYDROGENASES AND COMPOSITIONS AND METHODS FOR THEREOF
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
SG11202001684PA (en) 2017-10-06 2020-03-30 Forma Therapeutics Inc Inhibiting ubiquitin specific peptidase 30
CA3078872A1 (en) 2017-10-11 2019-04-18 Aurigene Discovery Technologies Limited Crystalline forms of 3-substituted 1,2,4-oxadiazole
US11873298B2 (en) 2017-10-24 2024-01-16 Janssen Pharmaceutica Nv 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
EP3706798A1 (en) 2017-11-06 2020-09-16 Aurigene Discovery Technologies Limited Conjoint therapies for immunomodulation
MX2020009942A (es) 2018-03-23 2021-01-08 Yumanity Therapeutics Inc Compuestos y usos de los mismos.
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)
US10532047B2 (en) 2018-05-16 2020-01-14 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)
WO2019222553A1 (en) 2018-05-16 2019-11-21 Forma Therapeutics, Inc. Inhibiting mutant idh-1
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
AU2019271279A1 (en) 2018-05-17 2020-11-26 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
HRP20230409T1 (hr) 2018-10-05 2023-07-07 Forma Therapeutics, Inc. Fuzionirani pirolini koji djeluju kao inhibitori ubikvitin specifične proteaze 30 (usp30)
WO2020154571A1 (en) 2019-01-24 2020-07-30 Yumanity Therapeutics, Inc. Compounds and uses thereof
MX2021011488A (es) * 2019-03-22 2021-11-17 Yumanity Therapeutics Inc Compuestos y usos de estos.
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
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

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
AT340933B (de) 1973-08-20 1978-01-10 Thomae Gmbh Dr K Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze
DE2341925A1 (de) 1973-08-20 1975-03-06 Thomae Gmbh Dr K Neue pyrimidinderivate und verfahren zu ihrer herstellung
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
JP4276376B2 (ja) 1997-07-24 2009-06-10 全薬工業株式会社 複素環式化合物及びそれを有効成分とする抗腫瘍剤
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
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
US6417185B1 (en) 1998-06-19 2002-07-09 Chiron Corporation Inhibitors of glycogen synthase kinase 3
AU768201B2 (en) 1999-01-22 2003-12-04 Amgen, Inc. Kinase inhibitors
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
US6316444B1 (en) 1999-06-30 2001-11-13 Merck & Co., Inc. SRC kinase inhibitor compounds
AU6605200A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
JP2003523942A (ja) 1999-06-30 2003-08-12 メルク エンド カムパニー インコーポレーテッド Ｓｒｃキナーゼ阻害剤化合物
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
NZ521068A (en) 2000-03-29 2005-04-29 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
ATE503743T1 (de) 2000-04-27 2011-04-15 Astellas Pharma Inc Kondensierte heteroarylderivate
CA2407231A1 (en) 2000-04-28 2002-10-23 Tanabe Seiyaku Co., Ltd. Cyclic compounds
AU2001268711A1 (en) 2000-06-23 2002-01-08 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
JP4105947B2 (ja) 2000-09-15 2008-06-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なトリアゾール化合物
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
US20030130264A1 (en) 2001-02-16 2003-07-10 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
WO2002102313A2 (en) 2001-06-19 2002-12-27 Bristol-Myers Squibb Company 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
AU2003220299A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azinylaminoazoles as inhibitors of protein kinases
US6846928B2 (en) 2002-03-15 2005-01-25 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of protein kinases
WO2003078426A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Azolylaminoazine as inhibitors of protein kinases
ATE468336T1 (de) 2002-03-15 2010-06-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
WO2004000820A2 (en) 2002-06-21 2003-12-31 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
EP1546115A4 (en) 2002-09-27 2010-08-04 Merck Sharp & Dohme 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
EA013811B1 (ru) 2002-11-21 2010-08-30 Новартис Вэксинес Энд Дайэгностикс, Инк. 2,4,6-тризамещённые пиримидины, являющиеся ингибиторами фосфотидилинозитол(pi)-3-киназы, и их применение при лечении рака
JP2006521357A (ja) 2003-03-24 2006-09-21 メルク　エンド　カムパニー　インコーポレーテッド ナトリウムチャンネル遮断薬としてのビアリール置換６員複素環化合物
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
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
DE602005024382D1 (de) 2004-04-13 2010-12-09 Astellas Pharma Inc Polycyclische pyrimidine als kaliumionenkanal-modulatoren
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
MX2007006230A (es) 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
JP2008523156A (ja) 2004-12-13 2008-07-03 ニューロジェン・コーポレーション 置換ビアリール類縁体
CA2590299A1 (en) 2004-12-13 2006-06-22 Neurogen Corporation Piperazinyl-pyridine analogues
DK1836169T5 (da) 2004-12-28 2023-10-09 Atnx Spv Llc Sammensætninger og fremgangsmåder til behandling af celleproliferationslidelser
US20080124384A1 (en) 2005-01-19 2008-05-29 Blum Charles A Heteroaryl Substituted Piperazinyl-Pyridine Analogues
AU2006217742A1 (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
AR053712A1 (es) 2005-04-18 2007-05-16 Neurogen Corp Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide)
GB2431156A (en) 2005-10-11 2007-04-18 Piramed Ltd 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase
AU2007204208A1 (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
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.
WO2008098058A1 (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
CN101801962A (zh) 2007-07-09 2010-08-11 阿斯利康(瑞典)有限公司 用于治疗增殖疾病的三取代嘧啶衍生物
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
KR20100131446A (ko) 2008-03-05 2010-12-15 노파르티스 아게 Ｅｇｆｒ 의존성 질환 또는 ｅｇｆｒ 족 구성원을 표적으로 하는 작용제에 대한 내성을 획득한 질환의 치료를 위한 피리미딘 유도체의 용도
EP2276488A1 (en) 2008-03-26 2011-01-26 Novartis AG 5imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
EP2276750A2 (en) 2008-03-27 2011-01-26 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
RU2538683C2 (ru) 2008-10-31 2015-01-10 Новартис Аг КОМБИНАЦИЯ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (Р13К) И ИНГИБИТОРА mTOR
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
EP2394999B1 (en) * 2009-02-06 2014-01-29 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
TW201041512A (en) 2009-05-19 2010-12-01 Dow Agrosciences Llc Compounds and methods for controlling fungi
AR080945A1 (es) 2009-07-07 2012-05-23 Pathway Therapeutics Inc Pirimidinil y 1,3,5-triazinil benzimidazoles y su uso en la terapia contra el cancer
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
RU2595718C2 (ru) 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
EP2509600B1 (en) * 2009-12-09 2017-08-02 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
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
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
WO2011133920A1 (en) 2010-04-23 2011-10-27 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
WO2012009678A1 (en) 2010-07-16 2012-01-19 Agios Pharmaceuticals, Inc. Therapeutically active compositions and their method of use
MY160785A (en) 2010-10-01 2017-03-15 Novartis Ag Manufacturing process for pyrimidine derivatives
RU2576402C2 (ru) 2010-10-18 2016-03-10 Серенис Терапьютикс Холдинг Са Соединения, композиции и способы, подходящие для мобилизации холестерина
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
KR20140063509A (ko) 2011-02-11 2014-05-27 다나-파버 캔서 인스티튜트 인크. 과오종 종양 세포의 억제 방법
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
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

Also Published As

Publication number Publication date
TWI547493B (zh) 2016-09-01
AU2012313888A8 (en) 2014-07-24
AR088175A1 (es) 2014-05-14
EA201490696A1 (ru) 2014-08-29
AU2012313888B2 (en) 2016-03-31
NI201400026A (es) 2015-01-13
NZ624040A (en) 2016-01-29
IL231786A (en) 2017-06-29
TN2014000128A1 (en) 2015-07-01
AU2012313888A1 (en) 2014-05-15
CU24269B1 (es) 2017-08-08
UY34352A (es) 2013-04-30
MX2014003752A (es) 2014-08-22
KR20140069235A (ko) 2014-06-09
TW201321375A (zh) 2013-06-01
BR112014007310A2 (pt) 2017-04-04
EP2771337A1 (en) 2014-09-03
SG11201400989TA (en) 2014-04-28
CO6920291A2 (es) 2014-04-10
AP2014007602A0 (en) 2014-04-30
DOP2014000058A (es) 2014-06-01
ZA201402144B (en) 2017-09-27
PE20141581A1 (es) 2014-11-14
CN103958506B (zh) 2017-02-22
AP3907A (en) 2016-11-23
ES2645968T3 (es) 2017-12-11
CL2014000746A1 (es) 2014-10-03
CR20140143A (es) 2014-10-16
PH12014500682A1 (en) 2014-05-12
CN103958506A (zh) 2014-07-30
EA025183B1 (ru) 2016-11-30
EP2771337B1 (en) 2017-08-02
UA111503C2 (uk) 2016-05-10
GEP20166432B (en) 2016-02-10
JP6026544B2 (ja) 2016-11-16
IL231786A0 (en) 2014-05-28
JP2014528951A (ja) 2014-10-30
WO2013046136A1 (en) 2013-04-04
CA2849995A1 (en) 2013-04-04
US20140235620A1 (en) 2014-08-21
US8957068B2 (en) 2015-02-17
MX342326B (es) 2016-09-26
CU20140036A7 (es) 2014-07-30
MA35452B1 (fr) 2014-09-01

Similar Documents

Publication Publication Date Title
GT201400057A (es) 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante
UY35470A (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
JOP20190194A1 (ar) مركبات نيوكليوتيدات ثنائية حلقية لعلاج السرطان
EA201101522A1 (ru) Способы лечения болезней с использованием эпиметаболического переключателя (коэнзим q10)
EA201390803A1 (ru) Ингибиторы бромодомена и их применение
EA201590005A1 (ru) Замещенные трициклические соединения как ингибиторы fgfr
PH12015502161A1 (en) Therapeutic compounds and compositions
MX337104B (es) Agentes inductores de apoptosis para el tratamiento de cancer y enfermedades inmunes y autoinmunes.
NZ719905A (en) Bicyclic heterocycle compounds and their uses in therapy
EA201270722A1 (ru) Формы рифаксимина и их применение
EA201890754A1 (ru) Соединения и способы их применения
AR082340A1 (es) Metodos y composiciones para la terapia del cancer de higado
EA201790267A1 (ru) Новые модуляторы киназ
EA201590997A1 (ru) Соединения и способы их применения
EA201270100A1 (ru) Пиримидиноны в качестве ингибиторов pi3k
EA201790273A1 (ru) Флагеллиновые композиции и их применение
EA201390682A1 (ru) Спирооксиндольные антагонисты mdm2
EA201370018A1 (ru) Составы рифаксимина и их применение
EA201290744A1 (ru) Имидазо[1,2-b][1,2,4]триазины в качестве c-met ингибиторов
CR20120508A (es) PROTEÍNA DE FUSIÓN ROBO1-Fc Y SU UTILIZACIÓN EN EL TRATAMIENTO DE TUMORES
MX379456B (es) Inhibidores de fde9 con estructura básica de imidazotriazinona y estructura básica de imidazopirazinona en el tratamiento de enfermedades periféricas.
EA201691032A1 (ru) Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ
EA201390669A1 (ru) Способы и композиции для иммунотерапии заболеваний нервной системы
ECSP14000606A (es) Agentes inductores de la apoptosis que pueden usarse para tratar el cáncer y las enfermedades inmunes y autoinmunes
EA201692313A1 (ru) Производные индолизина в качестве ингибиторов фосфоинозитид-3-киназ