CU20150119A7 - 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante - Google Patents

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

Info

Publication number
CU20150119A7
CU20150119A7 CUP2015000119A CU20150119A CU20150119A7 CU 20150119 A7 CU20150119 A7 CU 20150119A7 CU P2015000119 A CUP2015000119 A CU P2015000119A CU 20150119 A CU20150119 A CU 20150119A CU 20150119 A7 CU20150119 A7 CU 20150119A7
Authority
CU
Cuba
Prior art keywords
inhibitors
pirimidin
onas
oxazolidin
mutant
Prior art date
Application number
CUP2015000119A
Other languages
English (en)
Inventor
Thomas Raymond Caferro
Zhuoliang Chen
Young Shin Cho
Abran Q Costales
Julian Roy Levell
Gang Liu
James R Manning
Martin Sendzik
Cynthia Shafer
Michael David Shultz
James Sutton
Yaping Wang
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 CU20150119A7 publication Critical patent/CU20150119A7/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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (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)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La invención se dirige a la fórmula (I) ESPACIO PARA LA FÓRMULA o una sal farmacéuticamente aceptable del mismo, en donde R1, R2a, R2b y R3- R7 se definen en la presente. En particular, los compuestos de la invención son activos como inhibidores de proteínas IDH mutantes que tienen una actividad neomórfica, relacionadas con enfermedades o trastornos asociados a proliferación celular como el cáncer.
CUP2015000119A 2013-03-14 2015-09-14 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante CU20150119A7 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361783210P 2013-03-14 2013-03-14
US201361892131P 2013-10-17 2013-10-17
PCT/IB2014/059695 WO2014141104A1 (en) 2013-03-14 2014-03-12 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh

Publications (1)

Publication Number Publication Date
CU20150119A7 true CU20150119A7 (es) 2016-06-29

Family

ID=50382516

Family Applications (1)

Application Number Title Priority Date Filing Date
CUP2015000119A CU20150119A7 (es) 2013-03-14 2015-09-14 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante

Country Status (29)

Country Link
US (4) US9434719B2 (es)
EP (1) EP2970240B1 (es)
JP (1) JP6387360B2 (es)
KR (1) KR20150131224A (es)
CN (1) CN105263929B (es)
AP (1) AP2015008707A0 (es)
AR (1) AR095311A1 (es)
AU (1) AU2014229313B2 (es)
BR (1) BR112015023412A8 (es)
CA (1) CA2903979A1 (es)
CL (1) CL2015002472A1 (es)
CR (1) CR20150491A (es)
CU (1) CU20150119A7 (es)
DO (1) DOP2015000240A (es)
EA (1) EA028033B1 (es)
ES (1) ES2665619T3 (es)
GE (1) GEP201706699B (es)
HK (1) HK1213251A1 (es)
IL (1) IL240972A0 (es)
MX (1) MX355945B (es)
NI (1) NI201500128A (es)
PE (1) PE20151939A1 (es)
PH (1) PH12015502018A1 (es)
SG (1) SG11201507063YA (es)
TN (1) TN2015000392A1 (es)
TW (1) TW201444831A (es)
UY (1) UY35470A (es)
WO (1) WO2014141104A1 (es)
ZA (1) ZA201506452B (es)

Families Citing this family (52)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
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
KR20150131224A (ko) 2013-03-14 2015-11-24 노파르티스 아게 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
AU2014230814B2 (en) 2013-03-14 2017-12-21 Boehringer Ingelheim International Gmbh Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
CN105814028B (zh) 2013-09-06 2018-02-16 奥瑞基尼探索技术有限公司 作为免疫调节剂的1,2,4‑*二唑衍生物
CA2935423C (en) 2014-01-24 2023-11-07 Dana-Farber Cancer Institute, Inc. Antibody molecules to pd-1 and uses thereof
AU2015210750B2 (en) 2014-01-31 2020-08-20 Children's Medical Center Corporation Antibody molecules to TIM-3 and uses thereof
WO2015138920A1 (en) 2014-03-14 2015-09-17 Novartis Ag Antibody molecules to lag-3 and uses thereof
UA118610C2 (uk) 2014-09-12 2019-02-11 Бьорінгер Інгельхайм Інтернаціональ Гмбх Спіроциклічні інгібітори катепсину c
MA41044A (fr) 2014-10-08 2017-08-15 Novartis Ag Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer
WO2016061142A1 (en) 2014-10-14 2016-04-21 Novartis Ag Antibody molecules to pd-l1 and uses thereof
EP3233918A1 (en) 2014-12-19 2017-10-25 Novartis AG Combination therapies
KR102894264B1 (ko) 2015-03-10 2025-12-02 오리진 온콜로지 리미티드 면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
JO3746B1 (ar) 2015-03-10 2021-01-31 Aduro Biotech Inc تركيبات وطرق لتنشيط الإشارات المعتمدة على "منبه أو تحفيز جين انترفيرون"
JP6473270B2 (ja) 2015-07-27 2019-02-20 イーライ リリー アンド カンパニー 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−オン化合物及び変異体idh1阻害剤としてのそれらの使用
WO2017019897A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to tim-3
ES2878188T3 (es) 2015-07-29 2021-11-18 Novartis Ag Terapias de combinación que comprenden moléculas de anticuerpos contra LAG-3
EP4378957A3 (en) 2015-07-29 2024-08-07 Novartis AG Combination therapies comprising antibody molecules to pd-1
KR20250099459A (ko) 2015-11-03 2025-07-01 얀센 바이오테크 인코포레이티드 Pd-1과 특이적으로 결합하는 항체 및 그의 용도
EP3389712B1 (en) 2015-12-17 2024-04-10 Novartis AG Antibody molecules to pd-1 and uses thereof
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
EP3507367A4 (en) 2016-07-05 2020-03-25 Aduro BioTech, Inc. CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF
UY37695A (es) 2017-04-28 2018-11-30 Novartis Ag Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo
US10800760B2 (en) 2017-05-31 2020-10-13 Nantbio, Inc. Trk inhibition
WO2018237173A1 (en) 2017-06-22 2018-12-27 Novartis Ag ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES
WO2019061324A1 (en) 2017-09-29 2019-04-04 Curis Inc. CRYSTALLINE FORMS OF IMMUNOMODULATORS
US11136300B2 (en) 2017-10-11 2021-10-05 Aurigene Discovery Technologies Limited Crystalline forms of 3-substituted 1,2,4-oxadiazole
SG11202003625VA (en) 2017-11-03 2020-05-28 Aurigene Discovery Tech Ltd 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
US12398209B2 (en) 2018-01-22 2025-08-26 Janssen Biotech, Inc. Methods of treating cancers with antagonistic anti-PD-1 antibodies
CN115448923B (zh) * 2018-02-13 2024-03-22 上海青煜医药科技有限公司 嘧啶并环化合物及其制备方法和应用
CN110407855A (zh) * 2018-04-26 2019-11-05 上海嗣新生物科技有限公司 2-氨基嘧啶啶衍生物及其制备方法和用途
CN112469719B (zh) 2018-05-21 2024-01-23 内尔维亚诺医疗科学公司 杂缩合的吡啶酮化合物及其作为idh抑制剂的用途
UY38247A (es) 2018-05-30 2019-12-31 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
JP2021535198A (ja) 2018-08-17 2021-12-16 ピーティーシー セラピューティクス, インコーポレイテッド 膵臓癌を治療する方法
CN109659001B (zh) * 2018-12-18 2023-08-04 延安大学 一种防癌监管系统及方法
EP3917914A1 (en) 2019-02-01 2021-12-08 Fmc Corporation Diamino-substituted pyridines and pyrimidines as herbicides
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
AU2020240382B2 (en) 2019-03-19 2022-08-25 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
EP3962481A4 (en) * 2019-05-03 2023-03-22 Praxis Precision Medicines, Inc. KCNT1 INHIBITORS AND METHODS OF USE
JP2022548881A (ja) 2019-09-18 2022-11-22 ノバルティス アーゲー Entpd2抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法
CN114555597B (zh) * 2019-10-12 2024-06-04 浙江迈同生物医药有限公司 异柠檬酸脱氢酶(idh)抑制剂
CN111057051A (zh) * 2019-12-16 2020-04-24 武汉九州钰民医药科技有限公司 PI3K抑制剂Alpelisib的新合成方法
CN110964005A (zh) * 2019-12-16 2020-04-07 武汉九州钰民医药科技有限公司 一种Alpelisib的制备工艺
KR20230005813A (ko) 2020-02-28 2023-01-10 프락시스 프리시젼 메디신즈, 인크. Kcnt1 억제제 및 사용 방법
CN111362925B (zh) * 2020-05-26 2020-09-08 北京鑫开元医药科技有限公司 一种4-嘧啶甲酰胺类化合物、药物组合物、制备方法及应用
IL299859A (en) 2020-07-21 2023-03-01 Daiichi Sankyo Co Ltd A combination drug of temozolomide and a mutant IDH1 enzyme inhibitor
WO2022056453A1 (en) * 2020-09-14 2022-03-17 Totus Medicines Inc. Therapeutic conjugates
US20240208978A1 (en) * 2021-06-15 2024-06-27 Wigen Biomedicine Technology (shanghai) Co., Ltd. Idh mutant inhibitor and use thereof
CN117510484B (zh) * 2023-11-10 2024-11-22 中国药科大学 mIDH1/NAMPT双靶点抑制剂及其应用
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 (130)

* 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
JPS4921149B1 (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
ATE139117T1 (de) 1990-07-03 1996-06-15 Mitsui Petrochemical Ind Pyrimidin-verbindung und ihr pharmazeutisch annehmbares salz
DE69624437T2 (de) 1995-04-13 2003-08-07 Taiho Pharmaceutical Co. Ltd., Tokio/Tokyo 4,6-diarylpyrimidin-derivate und deren salze
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
CN1129597C (zh) 1997-07-24 2003-12-03 全药工业株式会社 杂环化合物和以其为有效成分的抗肿瘤剂
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
ATE236136T1 (de) 1998-01-16 2003-04-15 Hoffmann La Roche 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
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
EP1144390A2 (en) 1999-01-22 2001-10-17 Amgen Inc., Kinase inhibitors
WO2001000207A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
AU5636900A (en) 1999-06-30 2001-01-31 Merck & Co., Inc. Src kinase inhibitor compounds
JP2003503354A (ja) 1999-06-30 2003-01-28 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
EP1196411B1 (en) 1999-07-15 2003-09-17 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
HUP0301117A3 (en) * 2000-02-17 2004-01-28 Amgen Inc Thousand Oaks Imidazole derivatives kinase inhibitors, their use, process for their preparation and pharmaceutical compositions containing them
AU2001242629B2 (en) 2000-03-29 2005-08-11 Cyclacel Limited 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of 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
WO2002000647A1 (en) 2000-06-23 2002-01-03 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
JP2004514656A (ja) 2000-09-06 2004-05-20 カイロン コーポレイション グリコゲンシンターゼキナーゼ3のインヒビター
ES2266258T3 (es) 2000-09-15 2007-03-01 Vertex Pharmaceuticals Incorporated Compuestos de pirazol utiles como inhibidores de proteina cinasas.
SE0004053D0 (sv) 2000-11-06 2000-11-06 Astrazeneca Ab N-type calcium channel antagonists for the treatment of pain
EP1345925B1 (en) 2000-12-21 2006-05-17 Vertex Pharmaceuticals Incorporated Pyrazole compounds useful as protein kinase inhibitors
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
WO2002064096A2 (en) 2001-02-16 2002-08-22 Tularik Inc. Methods of using pyrimidine-based antiviral agents
EP1395561A1 (en) 2001-05-25 2004-03-10 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
EP1485380B1 (en) 2002-03-15 2010-05-19 Vertex Pharmaceuticals Incorporated Azolylaminoazines as inhibitors of protein kinases
ES2289279T3 (es) 2002-03-15 2008-02-01 Vertex Pharmaceuticals Incorporated Composiciones utiles como inhibidores de proteinquinasas.
EP1485100B1 (en) 2002-03-15 2010-05-05 Vertex Pharmaceuticals Incorporated Azinylaminoazoles as inhibitors of protein kinases
EP1485381B8 (en) 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
AU2003245669A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain aromatic monocycles as kinase modulators
EP1546115A4 (en) 2002-09-27 2010-08-04 Merck Sharp & Dohme Substituted pyrimidines
EP1562605A4 (en) 2002-10-08 2006-07-12 Massachusetts Inst Technology COMPOUNDS FOR MODULATING CHOLESTER INTRANSPORT
US7223870B2 (en) 2002-11-01 2007-05-29 Pfizer Inc. Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction
ATE527250T1 (de) 2002-11-21 2011-10-15 Novartis Ag 2,4,6-trisubstituierten pyrimidinen als phosphotidylinositol (pi) 3-kinase inhibitoren und deren verwendung zur behandlung von krebs
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles as sodium channel blockers
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
WO2004092196A2 (en) 2003-04-09 2004-10-28 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
WO2005007648A2 (en) 2003-07-16 2005-01-27 Neurogen Corporation Biaryl piperazinyl-pyridine analogues
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
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
GB0415367D0 (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
US7521457B2 (en) 2004-08-20 2009-04-21 Boehringer Ingelheim International Gmbh Pyrimidines as PLK inhibitors
US7652009B2 (en) 2004-11-30 2010-01-26 Amgem Inc. Substituted heterocycles and methods of use
US20080045525A1 (en) 2004-12-13 2008-02-21 Rajagopal Bakthavatchalam Piperazinyl-Pyridine Analogues
US20080132509A1 (en) 2004-12-13 2008-06-05 Neurogen Corporation Substituted Biaryl Analogues
BRPI0519424B8 (pt) 2004-12-28 2021-05-25 Athenex Inc compostos, composição e uso dos ditos compostos para a preparação de um medicamento para prevenção ou tratamento de um distúrbio de proliferação celular ou infecção microbiana
CA2595205A1 (en) 2005-01-19 2006-07-27 Neurogen Corporation Heteroaryl substituted piperazinyl-pyridine analogues
JP2008531537A (ja) 2005-02-25 2008-08-14 クドス ファーマシューティカルズ リミテッド 化合物
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
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
KR20080091814A (ko) 2006-01-20 2008-10-14 쉐링 코포레이션 지질혈증장애의 치료를 위한 니코틴산 수용체 효능제로서의헤테로사이클
MX2008009414A (es) 2006-01-20 2008-10-01 Schering Corp Arilsulfonas carbociclicas y heterociclicas como inhibidores de gamma secretasa.
KR101079914B1 (ko) 2006-01-27 2011-11-04 에프. 호프만-라 로슈 아게 중추신경계 장애를 위한 4-이미다졸 유도체의 용도
TW200833342A (en) 2006-12-28 2008-08-16 Basf Ag 2-substituted pyrimidines I in therapy
AU2008213808B2 (en) 2007-02-06 2011-11-10 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
BRPI0814818A2 (pt) 2007-07-09 2019-09-10 Astrazeneca Ab composto, uso de um composto, métodos para produzir um efeito anti-proliferativo e um efeito inibitório de mtor quinase em uma animal de sangue quente, método para tratar doenças, e, composição farmacêutica
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
US20110033453A1 (en) 2008-03-05 2011-02-10 Carlos Garcia-Echeverria Use of pyrimidine derivatives for the treatment of egfr dependent diseases or diseases that have acquired resistance to agents that target egfr family members
EP2474323A3 (en) 2008-03-26 2012-10-10 Novartis AG Imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
JP2011515462A (ja) 2008-03-27 2011-05-19 アウククランド ウニセルビセス リミテッド 置換されたピリミジン、及びトリアジン、並びに癌療法におけるこれらの使用
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
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
JP5747440B2 (ja) 2009-02-06 2015-07-15 住友化学株式会社 ヒドラジド化合物及びその有害生物防除用途
HRP20140265T1 (hr) 2009-02-06 2014-04-25 Nippon Shinyaku Co., Ltd. Derivat aminopirazina i odgovarajuä†i lijek
ES2740424T3 (es) 2009-03-13 2020-02-05 Agios Pharmaceuticals Inc Métodos y composiciones para trastornos relacionados con la proliferación celular
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
EP2432767B1 (en) 2009-05-19 2013-06-26 Dow AgroSciences LLC Compounds and methods for controlling fungi
US8486939B2 (en) 2009-07-07 2013-07-16 Pathway Therapeutics Inc. Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
AR077999A1 (es) 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
RU2595718C2 (ru) 2009-09-09 2016-08-27 Селджен Авиломикс Рисерч,Инк. Ингибиторы pi3-киназы и их применение
EP2502227A1 (en) 2009-11-18 2012-09-26 Nokia Corp. Data processing
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
EP2560488B1 (en) 2010-04-23 2015-10-28 Cytokinetics, Inc. Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
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
CN106167483B (zh) 2010-10-18 2019-02-15 塞伦尼斯医疗控股有限公司 可用于胆固醇动员的化合物、组合物和方法
GB201106829D0 (en) 2011-04-21 2011-06-01 Proximagen Ltd Heterocyclic compounds
MX2013009256A (es) 2011-02-11 2013-12-09 Dana Farber Cancer Inst Inc Metodo para inhibir las celulas tumorales hamartoma.
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
CA2846272A1 (en) 2011-09-01 2013-03-07 Novartis Ag Pi3k inhibitor for use in the treatment of bone cancer or for preventing metastatic dissemination primary cancer cells into the bone
AU2012313888B2 (en) 2011-09-27 2016-03-31 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
JP2014528446A (ja) 2011-10-06 2014-10-27 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. 1,3−置換アゼチジンpde10阻害剤
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
BR112014024552A2 (pt) 2012-04-02 2017-09-19 Cytokinetics Inc método para aprimorar a função do diafragma em um paciente que necessite do mesmo; método para aumentar a função, atividade, eficiência, sensibilidade ao cálcio ou tempo de fadiga do músculo esquelético no diafragma de um paciente que necessite do mesmo e método para aumentar a função, atividade, eficiência, força, sensibilidade ao cálcio ou tempo de fadiga de uma fibra muscular esquelética do diafragma.
EA032480B1 (ru) 2012-04-11 2019-06-28 Сайтокинетикс, Инк. Способы повышения устойчивости скелетных мышц к утомлению
SG11201406550QA (en) 2012-05-16 2014-11-27 Novartis Ag Dosage regimen for a pi-3 kinase inhibitor
MX2014014308A (es) 2012-05-30 2015-02-12 Hoffmann La Roche Pirrolidino heterociclos.
RU2014154009A (ru) 2012-06-06 2016-08-10 Новартис Аг Комбинация ингибитора 17-альфа-гидроксилазы (с17,20-лиазы) и специфического ингибитора pi-3k для лечения онкологического заболевания
AU2013302702A1 (en) 2012-08-16 2015-02-19 Novartis Ag Combination of Pl3K inhibitor and c-Met inhibitor
MX360703B (es) 2012-10-23 2018-11-14 Novartis Ag Proceso mejorado para la elaboración de 5-(2, 6-di-4-morfolinil-4-pirimidinil)-4-trifluoro-metil-piridin-2-amin a.
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
CN109568319A (zh) 2013-01-10 2019-04-05 普尔莫凯恩股份有限公司 非选择性激酶抑制剂
KR20150131224A (ko) 2013-03-14 2015-11-24 노파르티스 아게 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
WO2014181287A1 (en) 2013-05-09 2014-11-13 Piramal Enterprises Limited Heterocyclyl compounds and uses thereof
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
PE20151939A1 (es) 2016-01-08
EP2970240A1 (en) 2016-01-20
AP2015008707A0 (en) 2015-09-30
AR095311A1 (es) 2015-10-07
US20150152093A1 (en) 2015-06-04
MX2015012552A (es) 2016-04-18
CN105263929A (zh) 2016-01-20
HK1213251A1 (zh) 2016-06-30
US20180051015A1 (en) 2018-02-22
MX355945B (es) 2018-05-07
US9688672B2 (en) 2017-06-27
DOP2015000240A (es) 2015-12-15
EA028033B1 (ru) 2017-09-29
CL2015002472A1 (es) 2016-01-04
IL240972A0 (en) 2015-11-30
BR112015023412A2 (pt) 2017-07-18
EP2970240B1 (en) 2018-01-10
AU2014229313B2 (en) 2016-07-28
BR112015023412A8 (pt) 2018-01-23
CA2903979A1 (en) 2014-09-18
US20140275083A1 (en) 2014-09-18
SG11201507063YA (en) 2015-10-29
AU2014229313A1 (en) 2015-10-01
ES2665619T3 (es) 2018-04-26
JP2016513633A (ja) 2016-05-16
GEP201706699B (en) 2017-07-10
NI201500128A (es) 2015-11-18
CN105263929B (zh) 2018-08-28
JP6387360B2 (ja) 2018-09-05
UY35470A (es) 2014-10-31
US9434719B2 (en) 2016-09-06
TW201444831A (zh) 2014-12-01
TN2015000392A1 (en) 2017-01-03
US10112931B2 (en) 2018-10-30
CR20150491A (es) 2016-01-29
KR20150131224A (ko) 2015-11-24
EA201591745A1 (ru) 2016-01-29
WO2014141104A1 (en) 2014-09-18
PH12015502018A1 (en) 2016-01-11
ZA201506452B (en) 2016-07-27
US20160318915A1 (en) 2016-11-03

Similar Documents

Publication Publication Date Title
UY35470A (es) 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante
EA202090291A3 (ru) Производные бипиразола в качестве ингибиторов jak
UY34657A (es) ?derivados macrocíclicos para el tratamiento de enfermedades?.
GT201500051A (es) Inhibidores de glucosilceramida sintasa
GT201400057A (es) 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante
CL2017000290A1 (es) Inhibidores de la proteína kinasa c y métodos de su uso.
GT201300215A (es) Inhibidores de glucosilceramida sintasa
CR20160035A (es) Inhibidores de bromodominios
UY34750A (es) ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
MX389256B (es) Compuestos heterociclicos y usos de los mismos.
MX2019010735A (es) Sistemas y metodos para la produccion dirigida de una proteina terapeutica dentro de una celula objetivo.
CU24335B1 (es) Piridopirimidinas sustituidas como inhibidores de la quinasa mek y útiles para el tratamiento del cáncer
MX385716B (es) Métodos para mejorar el rendimiento del animal.
MX2015012822A (es) 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante.
MX383590B (es) Inhibidores de kdm1a para el tratamiento de enfermedades.
MX374452B (es) Inhibidores de glucosilceramida sintasa para el tratamiento de enfermedades.
PE20151023A1 (es) Triazolopirazinas
MX379456B (es) Inhibidores de fde9 con estructura básica de imidazotriazinona y estructura básica de imidazopirazinona en el tratamiento de enfermedades periféricas.
MX372754B (es) Metodos y composiciones relacionadas con p62 para el tratamiento y profilaxis del cancer.
GEAP201813996A (en) Tamoxifen derivatives for treatment of neoplastic diseases, especially with high her2 protein level
MX2018005987A (es) Compuestos heterociclicos para el tratamiento de enfermedades.
MX2020009966A (es) Formas de dosificacion y usos terapeuticos de la l-4-cloro quinurenina.
MX2018007361A (es) Moléculas pequeñas para inhibir la actividad de quimiocinas, la actividad de una cinasa y/o el crecimiento de células cancerosas.
AR085105A1 (es) Dosificacion para tratamiento con anticuerpos anti-dominio 7 de tipo de factor de crecimiento epidermico (anti-egfl7)
NI201500172A (es) Composiciones farmacéuticas