AR088091A1 - Derivados de isoxazol-5-il-pirazin-2-amina como inhibidores de la quinasa atr y polimorfos de los mismos - Google Patents

Derivados de isoxazol-5-il-pirazin-2-amina como inhibidores de la quinasa atr y polimorfos de los mismos

Info

Publication number
AR088091A1
AR088091A1 ARP120103660A ARP120103660A AR088091A1 AR 088091 A1 AR088091 A1 AR 088091A1 AR P120103660 A ARP120103660 A AR P120103660A AR P120103660 A ARP120103660 A AR P120103660A AR 088091 A1 AR088091 A1 AR 088091A1
Authority
AR
Argentina
Prior art keywords
compound
formula
compounds
solid form
pharmaceutically acceptable
Prior art date
Application number
ARP120103660A
Other languages
English (en)
Spanish (es)
Inventor
Pierard Francoise
R Studley John
Charrier Jean
Damien-Littler Benjamin
Hughes Robert
Siesel David
Angell Paul
Urbina Armando
Zwicker Carl
Lconte Nicholas
Barder Timothy
Durrant Steven
Original Assignee
Vertex Pharma
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 Vertex Pharma filed Critical Vertex Pharma
Publication of AR088091A1 publication Critical patent/AR088091A1/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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • 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
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
ARP120103660A 2011-09-30 2012-10-01 Derivados de isoxazol-5-il-pirazin-2-amina como inhibidores de la quinasa atr y polimorfos de los mismos AR088091A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161541861P 2011-09-30 2011-09-30
US201161554174P 2011-11-01 2011-11-01
US201261620698P 2012-04-05 2012-04-05

Publications (1)

Publication Number Publication Date
AR088091A1 true AR088091A1 (es) 2014-05-07

Family

ID=47019162

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120103660A AR088091A1 (es) 2011-09-30 2012-10-01 Derivados de isoxazol-5-il-pirazin-2-amina como inhibidores de la quinasa atr y polimorfos de los mismos

Country Status (13)

Country Link
US (1) US8846686B2 (enExample)
EP (1) EP2751099B1 (enExample)
JP (1) JP2014528419A (enExample)
KR (1) KR20140084112A (enExample)
CN (1) CN103958507A (enExample)
AR (1) AR088091A1 (enExample)
AU (1) AU2012315611A1 (enExample)
CA (1) CA2850564A1 (enExample)
IL (1) IL231814A0 (enExample)
IN (1) IN2014KN00943A (enExample)
MX (1) MX2014003796A (enExample)
TW (1) TW201332999A (enExample)
WO (1) WO2013049722A1 (enExample)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP5836367B2 (ja) 2010-05-12 2015-12-24 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼ阻害剤として有用な化合物
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
US9096584B2 (en) 2010-05-12 2015-08-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2013529643A (ja) 2010-06-23 2013-07-22 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用なピロロピラジン誘導体
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) 2011-06-22 2014-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
RU2018147217A (ru) 2011-09-30 2019-01-18 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
US8853217B2 (en) * 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
AU2012315384B2 (en) 2011-09-30 2017-08-10 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with ATR inhibitors
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
IN2014KN00943A (enExample) 2011-09-30 2015-08-21 Vertex Pharma
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN104582795B (zh) * 2012-04-05 2018-04-20 沃泰克斯药物股份有限公司 可用作atr激酶抑制剂的化合物及其组合疗法
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
US8912198B2 (en) * 2012-10-16 2014-12-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
LT3418281T (lt) 2012-12-07 2021-01-11 Vertex Pharmaceuticals Inc. Pirazolo[1,5-a]pirimidinai, naudotini kaip atr kinazės inhibitoriai, skirti vėžinių ligų gydymui
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
HUE046727T2 (hu) 2013-12-06 2020-03-30 Vertex Pharma Az ATR-kináz inhibitoraként használható vegyület, 2-amino-6-fluoro-N-[5-fluoro-piridin-3-IL]-pirazolo-[1,5-A]-pirimidin-3-karboxamid, ennek elõállítása, különbözõ szilárd formái és ezek radioaktív nyomjelzett származékai
ES2777608T3 (es) 2014-06-05 2020-08-05 Vertex Pharma Derivados radiomarcados de un compuesto de 2-amino-6-fluoro-N-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-carboxamida útiles como inhibidores de ATR cinasa, la preparación de dicho compuesto y diferentes formas sólidas del mismo
US11179394B2 (en) 2014-06-17 2021-11-23 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of Chk1 and ATR inhibitors
TWI656121B (zh) 2014-08-04 2019-04-11 德商拜耳製藥公司 2-(嗎啉-4-基)-1,7-萘啶
CN105471583B (zh) * 2014-09-11 2019-01-29 比亚迪股份有限公司 车载电器的电子认证方法和电子认证系统
US11464774B2 (en) 2015-09-30 2022-10-11 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
EP3936153B1 (en) * 2016-01-11 2024-08-21 Celator Pharmaceuticals, Inc. Inhibiting ataxia telangiectasia and rad3-related protein (atr)
FR3058062A1 (fr) * 2016-10-27 2018-05-04 Selexel Nouvelle utilisation d'un oligonucleotide double brin
WO2018153972A1 (en) 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and antiandrogens
JOP20190197A1 (ar) 2017-02-24 2019-08-22 Bayer Pharma AG مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر
WO2018153969A1 (en) 2017-02-24 2018-08-30 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with radium-223 salt
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
EP3661560B1 (en) 2017-08-04 2025-02-26 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and pd-1/pd-l1 inhibitors
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
WO2019110586A1 (en) 2017-12-08 2019-06-13 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
CN109507429A (zh) * 2018-02-14 2019-03-22 复旦大学 基于CRISPR/cas9和过氧化物酶APEX2系统识别分析特异性位点相互作用蛋白的方法
CA3114024A1 (en) 2018-09-26 2020-04-02 Merck Patent Gmbh Combination of a pd-1 antagonist, an atr inhibitor and a platinating agent for the treatment of cancer
JP2022505041A (ja) 2018-10-15 2022-01-14 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング Dnaアルキル化剤及びatr阻害剤を使用する併用療法
EP3866805A1 (en) 2018-10-16 2021-08-25 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
CN112899321B (zh) * 2019-11-19 2024-12-24 上海天慈国际药业有限公司 一种劳拉替尼关键中间体制备方法
CN112694497A (zh) * 2020-12-25 2021-04-23 蚌埠中实化学技术有限公司 一种4-异丙基磺酰基苯硼酸的制备方法
EP4332103A4 (en) 2021-05-12 2025-09-03 Chia Tai Tianqing Pharmaceutical Group Co Ltd ATR INHIBITOR COMPOUND CONTAINING A SULFOXIMINE
US20250026742A1 (en) * 2021-08-13 2025-01-23 Suzhou Ark Biopharmaceutical Co., Ltd. Compound as atr kinase inhibitor
CN116444496B (zh) * 2023-06-16 2023-11-24 药康众拓(北京)医药科技有限公司 一种嘧啶联氘代吡唑类化合物及其应用

Family Cites Families (128)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4309430A (en) 1980-06-27 1982-01-05 Merck & Co., Inc. Pyrazinyl-1,2,4-oxadiazole-5-ones, for treatment of edema, and processes for preparing same
US5329012A (en) 1987-10-29 1994-07-12 The Research Foundation Of State University Of New York Bis(acyloxmethyl)imidazole compounds
JP2597917B2 (ja) 1990-04-26 1997-04-09 富士写真フイルム株式会社 新規な色素形成カプラー及びそれを用いたハロゲン化銀カラー写真感光材料
CA2253910A1 (en) 1996-05-11 1997-11-20 King's College London Pyrazines
JP2002241379A (ja) 1997-03-21 2002-08-28 Dainippon Pharmaceut Co Ltd 3−オキサジアゾリルキノキサリン誘導体
AU748816B2 (en) 1998-07-16 2002-06-13 Shionogi & Co., Ltd. Pyrimidine derivatives exhibiting antitumor activity
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
CN1272328C (zh) 1999-12-17 2006-08-30 希龙公司 糖元合成酶激酶3的基于吡嗪的抑制剂
US6849660B1 (en) 2000-08-01 2005-02-01 Isis Pharmaceuticals, Inc. Antimicrobial biaryl compounds
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
CA2446380A1 (en) 2001-05-08 2002-11-14 Yale University Proteomimetic compounds and methods
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
DE60234269D1 (de) 2001-11-21 2009-12-17 Pharmacia & Upjohn Co Llc Substituierte aryl 1,4-pyrazin derivate
KR20040084896A (ko) 2002-02-06 2004-10-06 버텍스 파마슈티칼스 인코포레이티드 Gsk-3의 억제제로서 유용한 헤테로아릴 화합물
ES2306859T3 (es) 2002-03-13 2008-11-16 Janssen Pharmaceutica Nv Derivados de sulfonil como nuevos inhibidores de histona deacetilasa.
GB0206860D0 (en) 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
GB0209715D0 (en) 2002-04-27 2002-06-05 Astrazeneca Ab Chemical compounds
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
AU2003234464B2 (en) 2002-05-03 2009-06-04 Exelixis, Inc. Protein kinase modulators and methods of use
CN1656079A (zh) 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
DE602004015429D1 (de) 2003-03-11 2008-09-11 Pfizer Prod Inc Pyrazinverbindungen als inhibitoren des transforming growth factor (tgf)
WO2004084813A2 (en) 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
WO2004084824A2 (en) 2003-03-24 2004-10-07 Merck & Co., Inc. Biaryl substituted 6-membered heterocyles as sodium channel blockers
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
CA2524867A1 (en) 2003-05-15 2004-12-02 Merck & Co., Inc. 3-(2-amino-1-azacyclyl)-5-aryl-1,2,4-oxadiazoles as s1p receptor agonists
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYLAMIDE AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTOR-5
WO2005123672A2 (en) 2004-06-14 2005-12-29 Takeda San Diego, Inc. Kinase inhibitors
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
US7452993B2 (en) 2004-07-27 2008-11-18 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
WO2006053342A2 (en) 2004-11-12 2006-05-18 Osi Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
AU2005309566A1 (en) 2004-11-22 2006-06-01 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or Rho kinase
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
EP1830853B1 (en) 2004-12-27 2011-08-10 Novartis AG Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
US7622583B2 (en) 2005-01-14 2009-11-24 Chemocentryx, Inc. Heteroaryl sulfonamides and CCR2
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
CN101163692B (zh) 2005-02-16 2012-01-18 先灵公司 具有cxcr3拮抗活性的杂环取代的哌嗪
EP1874769B1 (de) 2005-04-25 2011-09-14 Merck Patent GmbH Neuartige aza-heterozyklen als kinase-inhibitoren
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
TW200736260A (en) 2005-11-10 2007-10-01 Smithkline Beecham Corp Inhibitors of Akt activity
DE602006011363D1 (de) 2005-12-01 2010-02-04 Hoffmann La Roche Heteroaryl-substituierte piperidin-derivate als l-cpt1-hemmer
US7871982B2 (en) 2005-12-09 2011-01-18 Meiji Seika Kaisha, Ltd. Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient
MX2008008328A (es) 2005-12-22 2008-09-15 Alcon Res Ltd (indazol-5-il)-pirazinas y (1,3-dihidro-indol-2-ona)-pirazinas para tratar enfermedades y condiciones mediadas con rho cinasa.
ITMI20060311A1 (it) 2006-02-21 2007-08-22 Btsr Int Spa Dispositivo perfezionato di alimentazione di filo o filatio ad una macchina tessile e metodo per attuare tale alimentazione
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
TW200800203A (en) 2006-03-08 2008-01-01 Astrazeneca Ab New use
KR20090007347A (ko) 2006-03-22 2009-01-16 버텍스 파마슈티칼스 인코포레이티드 증식성 장애의 치료를 위한 c-MET 단백질 키나제 억제제
WO2007126964A2 (en) 2006-03-31 2007-11-08 Schering Corporation Kinase inhibitors
DE602007004618D1 (de) 2006-06-22 2010-03-18 Biovitrum Ab Publ Pyridin- und pyrazinderivate als mnk-kinaseinhibitoren
US9216963B2 (en) 2006-06-22 2015-12-22 Medibeacon Inc. Pyrazine derivatives with extended conjugation and methods of using the same in optical applications
JP2010504933A (ja) 2006-09-29 2010-02-18 ノバルティス アーゲー Pi3k脂質キナーゼ阻害剤としてのピラゾロピリミジン
GB0619342D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
EP2074096B1 (en) 2006-10-04 2012-06-27 F. Hoffmann-La Roche AG 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as hdl-cholesterol raising agents
JP5244118B2 (ja) 2006-11-10 2013-07-24 ブリストル−マイヤーズ スクイブ カンパニー 新規キナーゼ阻害剤
US20090062273A1 (en) 2006-12-15 2009-03-05 Ingo Hartung 3-H-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same.
AU2007338792B2 (en) 2006-12-20 2012-05-31 Amgen Inc. Substituted heterocycles and methods of use
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
GB0625659D0 (en) 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
CA2676173A1 (en) 2007-02-16 2008-08-28 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
CN101679266B (zh) 2007-03-01 2015-05-06 诺华股份有限公司 Pim激酶抑制剂及其应用方法
NZ580241A (en) 2007-04-10 2011-02-25 Bayer Cropscience Ag Insecticidal aryl isoxazoline derivatives
TW200902008A (en) 2007-05-10 2009-01-16 Smithkline Beecham Corp Quinoxaline derivatives as PI3 kinase inhibitors
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
WO2008156174A1 (ja) 2007-06-21 2008-12-24 Taisho Pharmaceutical Co., Ltd. ピラジンアミド化合物
CA2691003A1 (en) 2007-06-26 2008-12-31 Lexicon Pharmaceuticals, Inc. Methods of treating serotonin-mediated diseases and disorders
GB0713259D0 (en) 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
CN101711245B (zh) 2007-07-19 2015-03-25 H.隆德贝克有限公司 5元杂环酰胺及相关的化合物
BRPI0814441A2 (pt) 2007-07-19 2015-07-14 Schering Corp Compostos de amida heterocíclica como inibidores de proteína cinase
BRPI0815042A2 (pt) 2007-08-01 2015-02-10 Pfizer Compostos de pirazol
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
EP2203436A1 (en) 2007-09-17 2010-07-07 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
EP2215085B1 (en) 2007-10-25 2011-09-07 AstraZeneca AB Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
ATE519763T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazin-kinasehemmer
ATE517107T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
ATE522536T1 (de) 2008-02-25 2011-09-15 Hoffmann La Roche Pyrrolopyrazin-kinasehemmer
RU2503676C2 (ru) 2008-02-25 2014-01-10 Ф.Хоффманн-Ля Рош Аг Пирролопиразиновые ингибиторы киназы
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
US8110576B2 (en) 2008-06-10 2012-02-07 Plexxikon Inc. Substituted pyrrolo[2,3b]pyrazines and methods for treatment of raf protein kinase-mediated indications
GB0814364D0 (en) 2008-08-05 2008-09-10 Eisai London Res Lab Ltd Diazaindole derivatives and their use in the inhibition of c-Jun N-terminal kinase
JP2012506381A (ja) 2008-10-21 2012-03-15 バーテックス ファーマシューティカルズ インコーポレイテッド c−METタンパク質キナーゼ阻害剤
KR101712576B1 (ko) 2008-11-10 2017-03-06 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
CN102264743B (zh) 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
ES2464458T3 (es) 2008-12-05 2014-06-02 F. Hoffmann-La Roche Ag Pirrolopirazinil-ureas como inhibidores de quinasas
PL3354650T3 (pl) 2008-12-19 2022-06-13 Vertex Pharmaceuticals Incorporated Związki przydatne jako inhibitory kinazy atr
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
AU2010214101A1 (en) 2009-02-11 2011-09-01 Sunovion Pharmaceuticals Inc. Histamine H3 inverse agonists and antagonists and methods of use thereof
JP2012522013A (ja) 2009-03-27 2012-09-20 ザ ユーエービー リサーチ ファウンデーション 調節ires媒介翻訳
CN102471345A (zh) 2009-07-15 2012-05-23 雅培制药有限公司 激酶的吡咯并吡嗪抑制剂
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
WO2011124998A1 (en) 2010-04-08 2011-10-13 Pfizer Inc. Substituted 3,5- di phenyl - isoxazoline derivatives as insecticides and acaricides
WO2011130689A1 (en) 2010-04-15 2011-10-20 Tracon Pharmaceuticals, Inc. Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors
JP2013526540A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
WO2011143423A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8962631B2 (en) 2010-05-12 2015-02-24 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526538A (ja) 2010-05-12 2013-06-24 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
US9096584B2 (en) 2010-05-12 2015-08-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP5836367B2 (ja) 2010-05-12 2015-12-24 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼ阻害剤として有用な化合物
EP2571880A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolo [2, 3 - b]pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
MX2012013194A (es) 2010-05-20 2013-01-22 Hoffmann La Roche Derivados pirrolopirazinas como inhibidores de cinasas tirocina-cinasa del baso (syk) y cinasa de janus (jak).
JP2013529643A (ja) 2010-06-23 2013-07-22 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用なピロロピラジン誘導体
CN102311396B (zh) 2010-07-05 2015-01-07 暨南大学 一种吡嗪类衍生物和其制备方法及在制药中的应用
EP2407478A1 (en) 2010-07-14 2012-01-18 GENETADI Biotech, S.L. New cyclotetrapeptides with pro-angiogenic properties
CA2832100A1 (en) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
MX2013013331A (es) 2011-05-17 2014-10-17 Principia Biopharma Inc Derivados de azaindol como inhibidores de tirosina-cinasas.
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2014522818A (ja) 2011-06-22 2014-09-08 バーテックス ファーマシューティカルズ インコーポレイテッド Atrキナーゼ阻害剤として有用な化合物
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
IN2014KN00943A (enExample) 2011-09-30 2015-08-21 Vertex Pharma
RU2018147217A (ru) 2011-09-30 2019-01-18 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
AU2012315384B2 (en) 2011-09-30 2017-08-10 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with ATR inhibitors
US8841450B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013071090A1 (en) * 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776429A1 (en) * 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776421A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase

Also Published As

Publication number Publication date
EP2751099B1 (en) 2017-06-14
TW201332999A (zh) 2013-08-16
KR20140084112A (ko) 2014-07-04
US8846686B2 (en) 2014-09-30
CN103958507A (zh) 2014-07-30
IL231814A0 (en) 2014-05-28
MX2014003796A (es) 2015-01-16
US20130089625A1 (en) 2013-04-11
WO2013049722A1 (en) 2013-04-04
AU2012315611A1 (en) 2014-04-17
IN2014KN00943A (enExample) 2015-08-21
AU2012315611A8 (en) 2014-05-08
CA2850564A1 (en) 2013-04-04
JP2014528419A (ja) 2014-10-27
EP2751099A1 (en) 2014-07-09

Similar Documents

Publication Publication Date Title
ES2644828T3 (es) Inhibidores de histona desmetilasa
IN2014KN00943A (enExample)
WO2014143242A8 (en) Compounds useful as inhibitors of atr kinase
EP4534538A3 (en) Compounds useful as inhibitors of atr kinase
ES2553610T3 (es) Inhibidores de la caseína cinasa 1 delta (CK1delta)
MX2011004953A (es) Compuestos utiles como inhibidores de cinasa atr.
NZ720511A (en) Compounds useful as inhibitors of atr kinase and combination therapies thereof
MX2012013081A (es) Compuestos utiles como inhibidores de cinasa atr.
HK1223096A1 (zh) 用作par-2信號通路抑制劑的咪唑並噠嗪
BR112020020768A2 (pt) Derivados de pirazol-triazina e/ou pirazol-pirimidina como inibidor seletivo de cinase dependente de ciclina
MX2011006503A (es) Derivados de pirazina utiles como inhibidores de la cinasa de atr.
WO2011143423A3 (en) Compounds useful as inhibitors of atr kinase
CL2013002228A1 (es) Compuestos derivados de pirrolo[2,3-b]piridina, modulador de quinasa b-raf; composiciones farmaceuticas; procedimientos de preparacion; utiles en el tratamiento de la isquemia, alzheimer, parkinson, demencia, tumores, leucemia, artritis reumatoide, miastenia gravis, enfermedad renal, entre otras.
AR094313A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR077462A1 (es) 3-oxo-2,3-dihidro-1h-isoindol-4-carboxamidas
MX2014000536A (es) Compuestos de 4-piperidinilo para usarse como inhibidores de tanquirasa.
MX363715B (es) Formas solidas de un inhbidor de cdk4/6 selectivo.
BR112013011593A2 (pt) cristal de derivado de morfinan 7-carbamoíla-6,7-insaturada e método para produzir o mesmo
CU20130116A7 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
EA201171415A1 (ru) Ингибиторы белков семейства iap
AR057714A1 (es) Nueva forma cristalina iv de la agomelatina, un procedimiento para su preparacion, y las composiciones farmaceuticas que la contienen
WO2012124907A3 (ko) L-α-글리세릴 포스포릴 콜린의 I형 및 II형 결정과 그 제조방법
WO2015011120A3 (en) Salts of dasatinib in crystalline form
Thapa et al. 2, 4-Diaryl benzofuro [3, 2-b] pyridine derivatives: Design, synthesis, and evaluation of topoisomerase inhibitory activity and cytotoxicity
ES2650604T3 (es) Nueva forma cristalina VII de agomelatina, método de preparación y utilización de la misma, así como composición farmacéutica que la contiene

Legal Events

Date Code Title Description
FB Suspension of granting procedure