[go: up one dir, main page]

MX355945B - 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. - Google Patents

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

Info

Publication number
MX355945B
MX355945B MX2015012552A MX2015012552A MX355945B MX 355945 B MX355945 B MX 355945B MX 2015012552 A MX2015012552 A MX 2015012552A MX 2015012552 A MX2015012552 A MX 2015012552A MX 355945 B MX355945 B MX 355945B
Authority
MX
Mexico
Prior art keywords
mutant idh
oxazolidin
pyrimidin
inhibitors
ones
Prior art date
Application number
MX2015012552A
Other languages
English (en)
Other versions
MX2015012552A (es
Inventor
Sutton James
David Shultz Michael
Liu Gang
Q Costales Abran
Shafer Cynthia
Raymond Caferro Thomas
Chen Zhuoliang
Shin Cho Young
Roy Levell Julian
R Manning James
Sendzik Martin
Wang Yaping
Zhao Qian
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 MX2015012552A publication Critical patent/MX2015012552A/es
Publication of MX355945B publication Critical patent/MX355945B/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)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

La invención se refiere a la fórmula (I): (ver Fórmula) o a una sal farmacéuticamente aceptable de la misma, en donde R1, R2a, R2b y R3-R7 se describen en la presente. La invención también se refiere a un composición que contiene un compuesto de la fórmula (I), y al uso de estos compuestos en la inhibición de las proteínas de IDH mutante que tienen una actividad neomórfica. La invención se refiere además al uso de un compuesto de la fórmula (I) en el tratamiento de las enfermedades o los trastornos asociados con dichas proteínas de IDH mutante, incluyendo, pero no limitándose a, trastornos de proliferación celular, tales como cáncer.
MX2015012552A 2013-03-14 2014-03-12 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. MX355945B (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 (2)

Publication Number Publication Date
MX2015012552A MX2015012552A (es) 2016-04-18
MX355945B true MX355945B (es) 2018-05-07

Family

ID=50382516

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015012552A MX355945B (es) 2013-03-14 2014-03-12 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras 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 (51)

* 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
PL2970283T3 (pl) 2013-03-14 2021-05-31 Boehringer Ingelheim International Gmbh Podstawione (benzylocyjanometylo)amidy kwasu 2-aza-bicyklo[2.2.1]heptano-3-karboksylowego będące inhibitorami katepsyny c
MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
SG11201601682RA (en) 2013-09-06 2016-04-28 Aurigene Discovery Tech Ltd 1,2,4-oxadiazole derivatives as immunomodulators
JOP20200094A1 (ar) 2014-01-24 2017-06-16 Dana Farber Cancer Inst Inc جزيئات جسم مضاد لـ pd-1 واستخداماتها
JOP20200096A1 (ar) 2014-01-31 2017-06-16 Children’S Medical Center Corp جزيئات جسم مضاد لـ tim-3 واستخداماتها
PH12016501545B1 (en) 2014-03-14 2023-12-06 Immutep Sas Antibody molecules to lag-3 and uses thereof
JP2017526716A (ja) 2014-09-12 2017-09-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング カテプシンｃのスピロ環状阻害剤
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
CA2964367C (en) 2014-10-14 2024-01-30 Novartis Ag Antibody molecules to pd-l1 and uses thereof
WO2016100882A1 (en) 2014-12-19 2016-06-23 Novartis Ag Combination therapies
HK1248603A1 (zh) 2015-03-10 2018-10-19 Aduro Biotech, Inc. 用於活化"干扰素基因的刺激剂"依懒性信号传导的组合物和方法
RS62960B1 (sr) 2015-03-10 2022-03-31 Aurigene Discovery Tech Ltd Jedinjenja 1,2,4-oksadiazola i tiadiazola kao imunomodulatori
WO2017019429A1 (en) 2015-07-27 2017-02-02 Eli Lilly And Company 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds and theit use as mutant idh1 inhibitors
EP4378957A3 (en) 2015-07-29 2024-08-07 Novartis AG Combination therapies comprising antibody molecules to pd-1
WO2017019897A1 (en) 2015-07-29 2017-02-02 Novartis Ag Combination therapies comprising antibody molecules to tim-3
DK3317301T3 (da) 2015-07-29 2021-06-28 Immutep Sas Kombinationsterapier omfattende antistofmolekyler mod lag-3
JP2019500893A (ja) 2015-11-03 2019-01-17 ヤンセン バイオテツク，インコーポレーテツド Ｐｄ−１及びｔｉｍ−３に特異的に結合する抗体及びそれらの使用
KR102833068B1 (ko) 2015-12-17 2025-07-14 노파르티스 아게 Pd-1에 대한 항체 분자 및 그의 용도
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 to cd73 and uses thereof
WO2019061324A1 (en) 2017-09-29 2019-04-04 Curis Inc. CRYSTALLINE FORMS OF IMMUNOMODULATORS
SG11202003081WA (en) 2017-10-11 2020-05-28 Aurigene Discovery Tech Ltd Crystalline forms of 3-substituted 1,2,4-oxadiazole
EP3703683A1 (en) 2017-11-03 2020-09-09 Aurigene Discovery Technologies Limited Dual inhibitors of tim-3 and pd-1 pathways
WO2019087092A1 (en) 2017-11-06 2019-05-09 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
EP3797107B1 (en) 2018-05-21 2022-08-10 Nerviano Medical Sciences S.r.l. Heterocondensed pyridone compounds and their use as idh inhibitors
AR126019A1 (es) 2018-05-30 2023-09-06 Novartis Ag Anticuerpos frente a entpd2, terapias de combinación y métodos de uso de los anticuerpos y las terapias de combinación
CA3109386A1 (en) 2018-08-17 2020-03-19 Ptc Therapeutics, Inc. Use of 5-fluoro-2-(6-fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine in the treatment of pancreatic cancer
CN109659001B (zh) * 2018-12-18 2023-08-04 延安大学 一种防癌监管系统及方法
MX2021009163A (es) 2019-02-01 2021-09-10 Fmc Corp Piridinas y pirimidinas sustituidas con diamino como herbicidas.
US12157730B2 (en) 2019-03-19 2024-12-03 Voronoi Inc. Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component
HUE073283T2 (hu) 2019-03-19 2026-01-28 Voronoi Inc Heteroaril-származék, eljárás annak elõállítására és azt hatóanyagként tartalmazó gyógyászati készítmény
CA3139063A1 (en) * 2019-05-03 2020-11-12 Praxis Precision Medicines, Inc. Kcnt1 inhibitors and methods of use
CN114502590A (zh) 2019-09-18 2022-05-13 诺华股份有限公司 Entpd2抗体、组合疗法、以及使用这些抗体和组合疗法的方法
WO2021068698A1 (en) * 2019-10-12 2021-04-15 Shanghai Meton Pharmaceutical Co., Ltd Iso-citrate dehydrogenase (idh) inhibitor
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
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
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
KR20230042065A (ko) 2020-07-21 2023-03-27 다이이찌 산쿄 가부시키가이샤 테모졸로마이드와 돌연변이 idh1 효소 억제제의 조합 의약
TW202227138A (zh) * 2020-09-14 2022-07-16 美商托特斯藥品公司 治療性共軛體
EP4356914A4 (en) * 2021-06-15 2025-01-08 Wigen Biomedicine Technology (Shanghai) Co., Ltd. IDH MUTANT INHIBITOR AND ITS USE
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
DE69120221T2 (de) 1990-07-03 1996-11-21 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
EP1020462B1 (en) 1997-07-24 2004-02-11 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compounds and antitumor agent containing the same as active ingredient
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
PT930302E (pt) 1998-01-16 2003-07-31 Hoffmann La Roche Derivados de benzo-sulfona
US7045519B2 (en) 1998-06-19 2006-05-16 Chiron Corporation Inhibitors of glycogen synthase kinase 3
ATE274510T1 (de) 1998-06-19 2004-09-15 Chiron Corp Glycogen synthase kinase 3 inhibitoren
US6495558B1 (en) 1999-01-22 2002-12-17 Amgen Inc. Kinase inhibitors
WO2000043373A2 (en) 1999-01-22 2000-07-27 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
EP1194152A4 (en) 1999-06-30 2002-11-06 Merck & Co Inc Links to SRC kinase inhibition
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
AU2001237041B9 (en) * 2000-02-17 2005-07-28 Amgen Inc. Kinase inhibitors
HUP0300382A3 (en) 2000-03-29 2006-11-28 Cyclacel Ltd 2-substituted 4-heteroaryl-pyrimidines and their use in the treatmetn of proliferative disorders and pharmaceutical compositions containing the compounds
CN1186324C (zh) 2000-04-27 2005-01-26 山之内制药株式会社 稠合杂芳基衍生物
CN1440393A (zh) 2000-04-28 2003-09-03 田边制药株式会社 环状化合物
JP2004501913A (ja) 2000-06-23 2004-01-22 ブリストル−マイヤーズ　スクイブ　ファーマ　カンパニー ヘテロアリール−フェニル置換Ｘａ因子阻害剤
AU9502601A (en) 2000-09-06 2002-03-22 Chiron Corp Inhibitors of glycogen synthase kinase 3
CA2422367C (en) 2000-09-15 2010-05-18 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
WO2002059111A2 (en) 2000-12-21 2002-08-01 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
EP1363890A4 (en) 2001-02-07 2009-06-10 Ore Pharmaceuticals Inc MELANOCORTIN-4-RECEPTOR BINDING COMPOUNDS AND METHOD FOR THEIR APPLICATION
US20030130264A1 (en) 2001-02-16 2003-07-10 Tularik Inc. Methods of using pyrimidine-based antiviral agents
MXPA03010724A (es) 2001-05-25 2004-03-02 Boehringer Ingelheim Pharma Compuestos de carbamato y oxamida como inhibidores de la produccion de citocina.
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
ATE466580T1 (de) 2002-03-15 2010-05-15 Vertex Pharma Azolylaminoazine als proteinkinasehemmer
AU2003220300A1 (en) 2002-03-15 2003-09-29 Binch, Hayley Compositions useful as inhibitors of protein kinases
US20040009981A1 (en) 2002-03-15 2004-01-15 David Bebbington Compositions useful as inhibitors of protein kinases
EP1485381B8 (en) 2002-03-15 2010-05-12 Vertex Pharmaceuticals Incorporated Azolylaminoazine as inhibitors of protein kinases
US20040082627A1 (en) 2002-06-21 2004-04-29 Darrow James W. Certain aromatic monocycles as kinase modulators
WO2004029204A2 (en) 2002-09-27 2004-04-08 Merck & Co., Inc. Substituted pyrimidines
US20040171073A1 (en) 2002-10-08 2004-09-02 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
US7423148B2 (en) 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
CA2519677A1 (en) 2003-03-24 2004-10-07 Merck & Co., Inc. Biaryl substituted 6-membered heterocycles as sodium channel blockers
US20050014753A1 (en) 2003-04-04 2005-01-20 Irm Llc Novel compounds and compositions as protein kinase inhibitors
EP1610774A4 (en) 2003-04-09 2008-07-16 Exelixis Inc TIE-2 MODULATORS AND METHODS OF USE
WO2005009977A1 (en) 2003-07-15 2005-02-03 Neurogen Corporation Substituted pyrimidin-4-ylamina analogues as vanilloid receptor ligands
WO2005007648A2 (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
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
GB0415367D0 (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
MX2007006230A (es) 2004-11-30 2007-07-25 Amgen Inc Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer.
WO2006071538A2 (en) 2004-12-13 2006-07-06 Neurogen Corporation Substituted biaryl analogues
US20080045525A1 (en) 2004-12-13 2008-02-21 Rajagopal Bakthavatchalam Piperazinyl-Pyridine 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
CN101107245A (zh) 2005-01-19 2008-01-16 神经能质公司 经杂芳基取代的哌嗪-吡啶类似物
US20100130473A1 (en) 2005-02-25 2010-05-27 Marc Geoffrey Hummersone Compounds
AU2006236387A1 (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
BRPI0706395A2 (pt) 2006-01-11 2011-03-22 Astrazeneca Ab composto, uso do mesmo, métodos para produzir um efeito anti-proliferativo em um animal de sangue quente e para tratar doença, composição farmacêutica, e, processo para preparar um composto
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
CA2637717A1 (en) 2006-01-20 2007-08-02 Schering Corporation Heterocycles as nicotinic acid receptor agonists for the treatment of dyyslipidemia
AU2007207481B2 (en) 2006-01-20 2012-08-23 Merck Sharp & Dohme Corp. Carbocyclic and heterocyclic arylsulfones as gamma secretase inhibitors
WO2007085556A2 (en) 2006-01-27 2007-08-02 F. Hoffmann-La Roche Ag Use of 4-imidazole derivatives for cns disorders
WO2008080937A1 (en) 2006-12-28 2008-07-10 Basf Se 2-substituted pyrimidines i in therapy
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
WO2009007748A2 (en) 2007-07-09 2009-01-15 Astrazeneca Ab Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases
WO2009066084A1 (en) 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
RU2496500C2 (ru) 2008-03-05 2013-10-27 Новартис Аг Применение производных пиримидина для лечения egfr-зависимых заболеваний или заболеваний с приобретенной резистентностью к агентам, направленным против членов семейства egfr
CA2717948C (en) 2008-03-26 2016-09-06 Novartis Ag 5imidazoquinolines and pyrimidine derivatives as potent modulators of vegf-driven angiogenic processes
US20110053907A1 (en) 2008-03-27 2011-03-03 Auckland Uniservices Limited Substituted pyrimidines and triazines and their use in cancer therapy
TW200948362A (en) 2008-04-09 2009-12-01 Mitsubishi Tanabe Pharma Corp New compounds and their uses
GB0815369D0 (en) 2008-08-22 2008-10-01 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
US20110195966A1 (en) 2008-10-31 2011-08-11 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
ES2453474T3 (es) 2009-02-06 2014-04-07 Nippon Shinyaku Co., Ltd. Derivados de aminopirazina y medicamento correspondiente
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
US20120121515A1 (en) 2009-03-13 2012-05-17 Lenny Dang 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
CA2760911A1 (en) 2009-05-19 2010-11-25 George E. Davis Compounds and methods for controlling fungi
ES2706185T3 (es) 2009-07-07 2019-03-27 Mei Pharma Inc Pirimidinil y 1,3,5-triazinil bencimidazoles y sus usos en la terapia contra el cáncer
TWI393716B (zh) 2009-08-04 2013-04-21 Merck Sharp & Dohme 作為ｉｘａ因子抑制劑之雜環化合物
AR077999A1 (es) 2009-09-02 2011-10-05 Vifor Int Ag Antagonistas de pirimidin y triazin-hepcidina
TWI499592B (zh) 2009-09-09 2015-09-11 Avila Therapeutics Inc Ｐｉ３激酶抑制劑及其用途
WO2011060816A1 (en) 2009-11-18 2011-05-26 Nokia Corporation Data processing
WO2011072174A1 (en) * 2009-12-09 2011-06-16 Agios Pharmaceuticals, Inc. Therapeutically active compounds for use in the treatment of cancer characterized as having an idh mutation
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
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
WO2011143160A2 (en) * 2010-05-10 2011-11-17 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
CN103140479B (zh) 2010-10-01 2015-04-08 诺华有限公司 制造嘧啶衍生物的方法
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
BR112013020159A2 (pt) 2011-02-11 2016-11-08 Dana Farber Cancer Inst Inc método para inibir células tumorais de 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
AU2012300835A1 (en) 2011-09-01 2014-03-13 Novartis Ag PI3K inhibitor for use in the treatment of bone cancer or for preventing metastatic dissemination primary cancer cells into the bone
JP6026544B2 (ja) 2011-09-27 2016-11-16 ノバルティス アーゲー 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類
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
CN108553467A (zh) 2012-04-02 2018-09-21 赛特凯恩蒂克公司 改善膈肌功能的方法
CA2869675C (en) 2012-04-11 2022-06-14 Cytokinetics, Inc. Methods for improving resistance to skeletal muscle fatigue
CN104349779A (zh) 2012-05-16 2015-02-11 诺华股份有限公司 Pi-3激酶抑制剂的剂量方案
WO2013178569A1 (en) 2012-05-30 2013-12-05 F. Hoffmann-La Roche Ag Pyrrolidino heterocycles
AU2013271871A1 (en) 2012-06-06 2014-11-20 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
BR112015007243B1 (pt) 2012-10-23 2022-02-08 Novartis Ag Processo aperfeiçoado para fabricação de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4- trifluorometilpiridin-2-amina
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
DK3007689T3 (en) 2013-01-10 2018-06-14 Pulmokine Inc NON-SELECTIVE KINASE INHIBITORS
MX355945B (es) 2013-03-14 2018-05-07 Novartis Ag 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.
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
TW201444831A (zh) 2014-12-01
AR095311A1 (es) 2015-10-07
GEP201706699B (en) 2017-07-10
ES2665619T3 (es) 2018-04-26
US9434719B2 (en) 2016-09-06
JP6387360B2 (ja) 2018-09-05
US20160318915A1 (en) 2016-11-03
BR112015023412A8 (pt) 2018-01-23
CN105263929B (zh) 2018-08-28
ZA201506452B (en) 2016-07-27
NI201500128A (es) 2015-11-18
US20180051015A1 (en) 2018-02-22
HK1213251A1 (zh) 2016-06-30
AU2014229313B2 (en) 2016-07-28
JP2016513633A (ja) 2016-05-16
US20140275083A1 (en) 2014-09-18
UY35470A (es) 2014-10-31
AU2014229313A1 (en) 2015-10-01
EP2970240B1 (en) 2018-01-10
MX2015012552A (es) 2016-04-18
BR112015023412A2 (pt) 2017-07-18
IL240972A0 (en) 2015-11-30
US10112931B2 (en) 2018-10-30
US20150152093A1 (en) 2015-06-04
CU20150119A7 (es) 2016-06-29
EP2970240A1 (en) 2016-01-20
PH12015502018A1 (en) 2016-01-11
SG11201507063YA (en) 2015-10-29
TN2015000392A1 (en) 2017-01-03
DOP2015000240A (es) 2015-12-15
CL2015002472A1 (es) 2016-01-04
CA2903979A1 (en) 2014-09-18
KR20150131224A (ko) 2015-11-24
CR20150491A (es) 2016-01-29
EA201591745A1 (ru) 2016-01-29
AP2015008707A0 (en) 2015-09-30
US9688672B2 (en) 2017-06-27
WO2014141104A1 (en) 2014-09-18
CN105263929A (zh) 2016-01-20
EA028033B1 (ru) 2017-09-29

Similar Documents

Publication Publication Date Title
PH12015502018A1 (en) 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
MX2015012822A (es) 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante.
TN2014000128A1 (en) 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
PH12018502125A1 (en) Bipyrazole derivatives as jak inhibitors
PH12018500041A1 (en) Substituted aza compoounds as irak-4 inhibitors
MX359032B (es) Inhibidores de pirrolopirazina cinasa.
MX362550B (es) Inhibidores ciclicos de glutaminasa.
PH12016502382A1 (en) Substituted indazole compounds as irak4 inhibitors
PH12017502407A1 (en) Fused pyrimidine compound or salt thereof
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
MX355088B (es) Inhibidores de tienopirimidina de proteina cinasa c atipica.
EA201590661A1 (ru) Азахиназолиновые ингибиторы атипичной протеинкиназы c
MX352928B (es) Compuestos de piridazina-amida.
PH12016500225B1 (en) Novel quinoline-substituted compound
GEP20166474B (en) Pyrazolospiroketone derivatives for use as acetyl-coa carboxylase inhibitors
MX372964B (es) Derivados de fenil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh)
CA2929436C (en) Compounds, pharmaceutical composition and methods for use in treating inflammatory diseases
PH12016501461A1 (en) 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors
MX2014013758A (es) Derivados de tiazolcarboxamida para usarse como inhibidores de nampt.

Legal Events

Date Code Title Description
FG Grant or registration