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.

Info

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

Links

Classifications

    • 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
    • C07D413/14Heterocyclic 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
    • 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
    • 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
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems
    • 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
    • C07D487/12Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
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)

Application Number Title Priority Date Filing Date
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 (31)

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)
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 (57)

* 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
WO2013134079A1 (en) * 2012-03-05 2013-09-12 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
ES2665619T3 (es) 2013-03-14 2018-04-26 Novartis Ag 3-Pirimidin-4-il-oxazolidin-2-onas como inhibidores de IDH mutante
AU2014229283B2 (en) * 2013-03-14 2016-07-28 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
WO2015003360A2 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
WO2015006591A1 (en) * 2013-07-11 2015-01-15 Agios Pharmaceuticals, Inc. 2,4- or 4,6-diaminopyrimidine compounds as idh2 mutants inhibitors for the treatment of cancer
US20150031627A1 (en) 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc Therapeutically active compounds and their methods of use
WO2015010297A1 (en) * 2013-07-25 2015-01-29 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
PL3041827T3 (pl) 2013-09-06 2018-09-28 Aurigene Discovery Tech Limited Pochodne 1,2,4-oksadiazolu jako immunomodulatory
WO2015127172A1 (en) * 2014-02-20 2015-08-27 Agios Pharmaceuticals, Inc. Therapeutically active compounds and their methods of use
AU2015240465B2 (en) 2014-04-04 2020-02-27 Del Mar Pharmaceuticals Use of dianhydrogalactitol and analogs or derivatives thereof 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
MX2017003626A (es) 2014-09-19 2018-01-24 Forma Therapeutics Inc Derivados de piridinil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh).
MX2017003637A (es) 2014-09-19 2018-01-24 Forma Therapeutics Inc Derivados de fenil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh).
FI3733662T3 (fi) 2014-09-19 2023-08-09 Forma Therapeutics Inc Pyridin-2(1h)-oni-kinolinonijohdannaisia mutantti-isositraattidehydrogenaasin estäjinä
NZ730195A (en) 2014-09-22 2023-12-22 National Health Res Inst Heterocyclic compounds and use thereof
AU2015325279B2 (en) * 2014-10-01 2020-02-27 Daiichi Sankyo Company, Limited Isoxazole derivative as mutant isocitrate dehydrogenase 1 inhibitor
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
EP3237385B1 (en) 2014-12-22 2021-11-24 The United States of America, as represented by The Secretary, Department of Health and Human Services Mutant idh1 inhibitors useful for treating cancer
AU2016230793B2 (en) 2015-03-10 2021-03-25 Aurigene Discovery Technologies Limited 1,2,4-oxadiazole and thiadiazole compounds as immunomodulators
SG11201706902SA (en) * 2015-03-10 2017-09-28 Aurigene Discovery Tech Ltd 3-substituted-1,2,4-oxadiazole and thiadiazole compounds as immunomodulators
WO2016171756A1 (en) 2015-04-21 2016-10-27 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
US9624175B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, 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
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
ES2764523T3 (es) * 2015-07-27 2020-06-03 Lilly Co Eli Compuestos de 7-feniletilamino-4H-pirimido[4,5-D][1,3]oxazin-2-ona y su uso como inhibidores de IDH1 mutantes
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
UA123640C2 (uk) * 2016-12-16 2021-05-05 Елі Ліллі Енд Компані Сполука 7-фенілетиламіно-4н-піримідо[4,5-d][1,3]оксазин-2-ону (варіанти) як інгібітор мутантів idh1 та idh2
WO2018118793A1 (en) * 2016-12-19 2018-06-28 Isocure Biosciences Inc. Inhibitors of mutant isocitrate dehydrogenases and compositions and methods thereof
WO2019061324A1 (en) 2017-09-29 2019-04-04 Curis Inc. CRYSTALLINE FORMS OF IMMUNOMODULATORS
ES2950757T3 (es) 2017-10-06 2023-10-13 Forma Therapeutics Inc Inhibición de la peptidasa específica de la ubiquitina 30
SG11202003081WA (en) 2017-10-11 2020-05-28 Aurigene Discovery Tech Ltd Crystalline forms of 3-substituted 1,2,4-oxadiazole
EP3700934A4 (en) 2017-10-24 2021-10-27 Yumanity Therapeutics, Inc. COMPOUNDS AND USES OF THESE COMPOUNDS
WO2019087087A1 (en) 2017-11-03 2019-05-09 Aurigene Discovery Technologies Limited Dual inhibitors of tim-3 and pd-1 pathways
CN111386128A (zh) 2017-11-06 2020-07-07 奥瑞基尼探索技术有限公司 用于免疫调节的联合疗法
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)
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
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)
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
SG11202102815SA (en) 2018-10-05 2021-04-29 Forma Therapeutics Inc Fused pyrrolines which act as ubiquitin-specific protease 30 (usp30) inhibitors
EP3941908A4 (en) * 2019-03-22 2023-05-17 Yumanity Therapeutics, Inc. CONNECTIONS 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
WO2022216903A1 (en) * 2021-04-08 2022-10-13 Memorial Sloan-Kettering Cancer Center Nadk2 inhibition in cancer and fibrotic disorders
TW202328147A (zh) 2021-08-13 2023-07-16 美商美國禮來大藥廠 7-[[(1s)-1-[4-[(1s)-2-環丙基-1-(4-丙-2-烯醯基哌𠯤-1-基)乙基]苯基]乙基]胺基]-1-乙基-4h-嘧啶并[4,5-d][1,3]㗁𠯤-2-酮之固體形式

Family Cites Families (119)

* 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
JPS4921149A (es) 1972-06-15 1974-02-25
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 (fr) 1990-07-03 1992-01-23 Mitsui Petrochemical Industries, Limited Compose de pyrimidine et sel pharmaceutiquement acceptable de ce compose
JP3145410B2 (ja) 1995-04-13 2001-03-12 大鵬薬品工業株式会社 新規な4,6−ジアリールピリミジン誘導体及びその塩
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
AU727013B2 (en) 1997-07-24 2000-11-30 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compound and antitumor agent comprising the same as effective component
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
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
DE69919707T2 (de) 1998-06-19 2005-09-01 Chiron Corp., Emeryville Glycogen synthase kinase 3 inhibitoren
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
AU768201B2 (en) 1999-01-22 2003-12-04 Amgen, Inc. Kinase inhibitors
US6498165B1 (en) 1999-06-30 2002-12-24 Merck & Co., Inc. Src kinase inhibitor compounds
CA2376951A1 (en) 1999-06-30 2001-01-04 Peter J. Sinclair Src kinase inhibitor compounds
AU6605200A (en) 1999-06-30 2001-01-31 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
WO2001005783A1 (en) 1999-07-15 2001-01-25 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
WO2001060816A1 (en) * 2000-02-17 2001-08-23 Amgen Inc. Kinase inhibitors
EP1274705A1 (en) 2000-03-29 2003-01-15 Cyclacel Limited 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders
CN100345830C (zh) 2000-04-27 2007-10-31 安斯泰来制药有限公司 稠合杂芳基衍生物
WO2001083460A1 (fr) 2000-04-28 2001-11-08 Tanabe Seiyaku Co., Ltd. Composes cycliques
WO2002000647A1 (en) 2000-06-23 2002-01-03 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
AU9502601A (en) 2000-09-06 2002-03-22 Chiron Corp Inhibitors of glycogen synthase kinase 3
AU2001292670A1 (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
BR0116411A (pt) 2000-12-21 2003-11-11 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
JP2004531571A (ja) 2001-05-25 2004-10-14 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン生産のインヒビターとしてのカルバメート及びオキサミド化合物
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
EP1485381B8 (en) 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
AU2003218215A1 (en) 2002-03-15 2003-09-29 Vertex Pharmaceuticals, Inc. Azolylaminoazines as inhibitors of protein kinases
WO2003078423A1 (en) 2002-03-15 2003-09-25 Vertex Pharmaceuticals, Inc. Compositions useful as inhibitors of protein kinases
DE60332433D1 (de) 2002-03-15 2010-06-17 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
US20040082627A1 (en) 2002-06-21 2004-04-29 Darrow James W. Certain aromatic monocycles as kinase modulators
AU2003275242B2 (en) 2002-09-27 2010-03-04 Merck Sharp & Dohme Corp. 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
AU2003295776B2 (en) 2002-11-21 2011-05-12 Novartis Vaccines And Diagnostics, Inc. 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer
EP1608622A4 (en) 2003-03-24 2009-04-01 Merck & Co Inc BIARYLSUBSTITUTED 6-LOW 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
CA2531490A1 (en) 2003-07-15 2005-02-03 Neurogen Corporation Substituted pyrimidin-4-ylamina analogues as vanilloid receptor ligands
AU2004257289A1 (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
AU2005232745A1 (en) 2004-04-13 2005-10-27 Astellas Pharma 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
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
CN101080228A (zh) 2004-12-13 2007-11-28 神经能质公司 哌嗪基-吡啶类似物
US7300931B2 (en) 2004-12-28 2007-11-27 Kinex Pharmaceuticals, Llc Compositions for treating cell proliferation disorders
AU2006206246A1 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
KR20070108916A (ko) 2005-02-25 2007-11-13 쿠도스 파마슈티칼스 리미티드 Mtor 억제제로서 작용하는 하이드라지노메틸,하이드라조노메틸 및 5-원 복소환 화합물 및 이의항암제로서의 용도
CA2606288A1 (en) 2005-04-18 2006-10-26 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
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
WO2008080937A1 (en) * 2006-12-28 2008-07-10 Basf Se 2-substituted pyrimidines i in therapy
US7977336B2 (en) 2006-12-28 2011-07-12 Banyu Pharmaceutical Co. Ltd Aminopyrimidine derivatives as PLK1 inhibitors
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
AR067478A1 (es) 2007-07-09 2009-10-14 Astrazeneca Ab Compuestos derivados de morfolina pirimidina
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
AU2009221164B2 (en) 2008-03-05 2012-07-26 Novartis Ag Use of pyrimidine derivatives for the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members
BRPI0909082A2 (pt) 2008-03-26 2019-02-26 Novartis Ag imidazoquinolinas e derivados de pirimidina como moduladores potentes de processos angiogênicos acionados por vegf
WO2009120094A2 (en) 2008-03-27 2009-10-01 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
US8575338B2 (en) 2008-04-09 2013-11-05 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
WO2010068863A2 (en) 2008-12-12 2010-06-17 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
AU2010223919B2 (en) 2009-03-13 2016-03-31 Les Laboratoires Servier Methods and compositions for cell-proliferation-related disorders
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
RU2011151603A (ru) 2009-05-19 2013-06-27 ДАУ АГРОСАЙЕНСИЗ ЭлЭсСи Соединения и способы борьбы с грибами
EP2451802A1 (en) 2009-07-07 2012-05-16 Pathway Therapeutics, Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
AR077999A1 (es) 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
CA2773848A1 (en) 2009-09-09 2011-03-17 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
US9133123B2 (en) 2010-04-23 2015-09-15 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
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
US20130109643A1 (en) 2010-05-10 2013-05-02 The Johns Hopkins University Metabolic inhibitor against tumors having an idh mutation
ES2704862T3 (es) 2010-07-16 2019-03-20 Agios Pharmaceuticals Inc Composiciones terapéuticamente activas y su método de uso
KR20130119928A (ko) 2010-10-01 2013-11-01 노파르티스 아게 피리미딘 유도체의 제조 방법
LT2629776T (lt) 2010-10-18 2017-11-10 Cerenis Therapeutics Holding Sa Junginiai, kompozicijos ir būdai, tinkami cholesterolio mobilizavimui
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
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
CN103764130A (zh) 2011-09-01 2014-04-30 诺华股份有限公司 用于治疗骨癌或者预防原发性癌细胞转移性播散入骨中的pi3k抑制剂
CA2851082A1 (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
JP6381523B2 (ja) 2012-05-16 2018-08-29 ノバルティス アーゲー Pi−3キナーゼ阻害剤の投与レジメン
CN104349771A (zh) 2012-06-06 2015-02-11 诺华股份有限公司 用于***疾病的17α-羟化酶(C17,20-裂解酶)抑制剂和特定PI-3K抑制剂的组合
CN105050623B (zh) 2012-08-16 2018-06-12 诺华股份有限公司 Pi3k抑制剂和c-met抑制剂的组合
WO2014064058A1 (en) 2012-10-23 2014-05-01 Novartis Ag Improved process for manufacturing 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine
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
UY34352A (es) 2013-04-30
SG11201400989TA (en) 2014-04-28
TW201321375A (zh) 2013-06-01
MX2014003752A (es) 2014-08-22
MA35452B1 (fr) 2014-09-01
GEP20166432B (en) 2016-02-10
WO2013046136A1 (en) 2013-04-04
CN103958506B (zh) 2017-02-22
NI201400026A (es) 2015-01-13
ZA201402144B (en) 2017-09-27
JP6026544B2 (ja) 2016-11-16
UA111503C2 (uk) 2016-05-10
JP2014528951A (ja) 2014-10-30
TWI547493B (zh) 2016-09-01
CO6920291A2 (es) 2014-04-10
ES2645968T3 (es) 2017-12-11
EA025183B1 (ru) 2016-11-30
AU2012313888A8 (en) 2014-07-24
EP2771337B1 (en) 2017-08-02
MX342326B (es) 2016-09-26
CN103958506A (zh) 2014-07-30
CU20140036A7 (es) 2014-07-30
CA2849995A1 (en) 2013-04-04
EP2771337A1 (en) 2014-09-03
CR20140143A (es) 2014-10-16
AP2014007602A0 (en) 2014-04-30
CU24269B1 (es) 2017-08-08
AR088175A1 (es) 2014-05-14
AU2012313888B2 (en) 2016-03-31
EA201490696A1 (ru) 2014-08-29
TN2014000128A1 (en) 2015-07-01
IL231786A (en) 2017-06-29
IL231786A0 (en) 2014-05-28
KR20140069235A (ko) 2014-06-09
GT201400057A (es) 2017-09-28
DOP2014000058A (es) 2014-06-01
US20140235620A1 (en) 2014-08-21
AP3907A (en) 2016-11-23
NZ624040A (en) 2016-01-29
US8957068B2 (en) 2015-02-17
PE20141581A1 (es) 2014-11-14
AU2012313888A1 (en) 2014-05-15
BR112014007310A2 (pt) 2017-04-04

Similar Documents

Publication Publication Date Title
CL2014000746A1 (es) 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.
CO2017004525A2 (es) Dihidropirrolopiridinas inhibidoras de ror-gamma
CL2014000566A1 (es) Compuestos derivados de pirrolopirimidina y purina, y sus sales farmaceuticamente aceptables; composicion farmaceutica que los comprende, util para el tratamiento del crecimiento celular anormal, tal como cancer.
CL2014001793A1 (es) Compuestos derivados de 1,3,5-triazinas sustituidas y sus sales, como inhibidores de la idh2 mutante; composicion farmaceutica que los comprende; y su uso para el tratamiento del cancer.
CO7030960A2 (es) Inhibidores de pak para el tratamiento de los trastornos de proliferación celular
DOP2015000158A (es) Inhibidores de prmt5 y sus usos
CL2014000543A1 (es) Compuestos derivados de imidazopiridazinas sustituidas con amino, inhibidores de la quinasa ,mknk2; metodo de preparacion; compuestos intermediarios y su uso; composicion farmaceutica; combinacion farmaceutica; y su uso para el tratamiento del cancer.
DOP2012000257A (es) Derivados del acido 1-amino-2-ciclopropiletilboronico
UY34545A (es) Novedosas dihidropirimidinoisoquinolinonas y composiciones farmacéuticas de las mismas para el tratamiento de trastornos inflamatorios.
CL2015002194A1 (es) Inhbidores de erk y sus usos
PE20180318A1 (es) Procedimiento para preparar isoquinolinonas y formas solidas de isoquinolinonas
UY34037A (es) Nuevo compuesto útil para el tratamiento de enfermedades degenerativas e inflamatorias.
CL2014002412A1 (es) Compuestos derivados de pirido[4,3-d]pirimidina, como inhibidores de mek; composicion farmaceutica que los comprende; y su uso para el tratamiento de enfermedades inflamatorias, infecciones, trastornos autoinmunes, enfermedades metabolicas y enfermedades malignas, entre otras.
CL2012003415A1 (es) Compuestos derivados de 2-oxo-piperidina y 1,1-dioxido-tiazina, inhibidores de mdm2; composicion farmaceutica que los comprende; y su uso para el tratamiento del cancer .
CL2016001895A1 (es) Compuestos
DOP2014000036A (es) Compuestos de piridazinona y su uso como inhibidores daao
NI201800042A (es) Nuevos derivados de pirrolo[2,3-d]pirimidina como inhibidores duales de dyrk1/clk1
CL2015000408A1 (es) Compuestos derivados de pirazolo[4,3-d]pirimidina y sus sales; composicion farmaceutica que los comprende, util para el tratamiento de enfermedades alergicas, inflamatorias, infecciosas o cancer.
CL2012002270A1 (es) Compuestos derivados de pirrolo[2,3-d]-pirimidina composición farmacéutica que los comprende; utiles en el tratamiento del cancer.
CR20140106A (es) Compuestos y composiciones como inhibidores de la quinasa c-kit
CO7160104A2 (es) Inhibidores de virus de hepatitis c
NI201300080A (es) Formas sólidas de 3 - ( 5 - amino - 2 - metil - 4 - oxo - 4h - quinazolin - 3 - il ) - piperidin - 2, 6 - diona, y sus composiciones farmacéuticas y usos
EA201400771A1 (ru) Новые производные азетидина, фармацевтические композиции и их применение
CL2016003214A1 (es) Derivados de la indolizina como inhibidores de las fosfoinositido-3 quinasas
CL2014002661A1 (es) Compuestos derivados de tienopirimidina o sus sales, como inhibidores de la alk quinasa; su proceso de preparacion; composicion farmaceutica que los comprende, util para el tratamiento del cancer.