PL3077397T3 - Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne - Google Patents

Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne

Info

Publication number
PL3077397T3
PL3077397T3 PL14815187T PL14815187T PL3077397T3 PL 3077397 T3 PL3077397 T3 PL 3077397T3 PL 14815187 T PL14815187 T PL 14815187T PL 14815187 T PL14815187 T PL 14815187T PL 3077397 T3 PL3077397 T3 PL 3077397T3
Authority
PL
Poland
Prior art keywords
fluoro
pyrazolo
pyrimidin
pyridin
amino
Prior art date
Application number
PL14815187T
Other languages
English (en)
Inventor
Jean-Damien Charrier
Christopher John Davis
Damien Fraysse
Gorka ETXEBARRIA I JARDI
Simon PEGG
Francoise Pierard
Joanne Pinder
John Studley
Carl ZWICKER
Tapan Sanghvi
Michael Waldo
Ales Medek
David Matthew Shaw
Maninder PANESAR
Yuegang Zhang
Naziha ALEM
Original Assignee
Vertex Pharmaceuticals Inc.
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 Pharmaceuticals Inc. filed Critical Vertex Pharmaceuticals Inc.
Publication of PL3077397T3 publication Critical patent/PL3077397T3/pl

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/63Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
PL14815187T 2013-12-06 2014-12-05 Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne PL3077397T3 (pl)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361912636P 2013-12-06 2013-12-06
US201462008220P 2014-06-05 2014-06-05
US201462058819P 2014-10-02 2014-10-02
EP14815187.1A EP3077397B1 (en) 2013-12-06 2014-12-05 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
PCT/US2014/068713 WO2015085132A1 (en) 2013-12-06 2014-12-05 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof

Publications (1)

Publication Number Publication Date
PL3077397T3 true PL3077397T3 (pl) 2020-04-30

Family

ID=52118034

Family Applications (1)

Application Number Title Priority Date Filing Date
PL14815187T PL3077397T3 (pl) 2013-12-06 2014-12-05 Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne

Country Status (23)

Country Link
US (3) US10160760B2 (pl)
EP (1) EP3077397B1 (pl)
JP (1) JP6543252B2 (pl)
KR (1) KR102153886B1 (pl)
CN (1) CN105934435B (pl)
AU (2) AU2014360380B2 (pl)
BR (1) BR112016012734B1 (pl)
CA (1) CA2932757C (pl)
DK (1) DK3077397T3 (pl)
ES (1) ES2768678T3 (pl)
HR (1) HRP20192183T1 (pl)
HU (1) HUE046727T2 (pl)
IL (1) IL246028B (pl)
LT (1) LT3077397T (pl)
MX (1) MX370390B (pl)
PL (1) PL3077397T3 (pl)
PT (1) PT3077397T (pl)
RS (1) RS59679B1 (pl)
RU (3) RU2720408C2 (pl)
SG (2) SG10201804791UA (pl)
SI (1) SI3077397T1 (pl)
WO (1) WO2015085132A1 (pl)
ZA (1) ZA201603893B (pl)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106496210B (zh) 2008-12-19 2020-06-09 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CA2850491C (en) 2011-09-30 2020-10-27 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors
RU2677292C2 (ru) 2011-09-30 2019-01-16 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
WO2013152298A1 (en) 2012-04-05 2013-10-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
NZ731337A (en) 2012-12-07 2019-02-22 Vertex Pharma Compounds useful as inhibitors of atr kinase
JP2016512815A (ja) 2013-03-15 2016-05-09 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キナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
PL3077397T3 (pl) 2013-12-06 2020-04-30 Vertex Pharmaceuticals Inc. Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne
SI3152212T1 (sl) 2014-06-05 2020-06-30 Vertex Pharmaceuticals Inc. Radioaktivno označeni derivati 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)-pirazolo (1,5-A)pirimidin-3- karboksamidne spojine, koristni kot inhibitor kinaze ATR, priprava navedene spojine in njene različne trdne oblike
RS59054B1 (sr) 2014-06-17 2019-08-30 Vertex Pharma Postupak za lečenje raka korišćenjem kombinacije chk1 i atr inhibitora
AU2016331955B2 (en) 2015-09-30 2022-07-21 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors
PL3533796T3 (pl) * 2016-10-28 2022-01-17 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Związek aminopirazolopirymidynowy stosowany jako inhibitor receptora o aktywności kinazy tyrozynowej czynnika neurotroficznego
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
WO2018153972A1 (en) 2017-02-24 2018-08-30 Bayer Pharma Aktiengesellschaft Combination of atr kinase inhibitors and antiandrogens
WO2018206547A1 (en) 2017-05-12 2018-11-15 Bayer Pharma Aktiengesellschaft Combination of bub1 and atr inhibitors
WO2018218197A2 (en) 2017-05-26 2018-11-29 Board Of Regents, The University Of Texas System Tetrahydropyrido[4,3-d]pyrimidine inhibitors of atr kinase
JP7159307B2 (ja) 2017-07-13 2022-10-24 ボード オブ レジェンツ,ザ ユニバーシティ オブ テキサス システム Atrキナーゼの複素環式阻害剤
US11690911B2 (en) 2017-08-04 2023-07-04 Bayer Aktiengesellschaft Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
CN111886224A (zh) 2017-08-17 2020-11-03 德州大学***董事会 Atr激酶的杂环抑制剂
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CA3084863A1 (en) 2017-12-08 2019-06-13 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
WO2019178590A1 (en) * 2018-03-16 2019-09-19 Board Of Regents, The University Of Texas System Heterocyclic inhibitors of atr kinase
WO2020064971A1 (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
US20210369705A1 (en) 2018-10-15 2021-12-02 Merck Patent Gmbh Combination therapy utilizing dna alkylating agents and atr inhibitors
US20210369724A1 (en) 2018-10-16 2021-12-02 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds
CN111117330A (zh) * 2020-01-06 2020-05-08 林才珏 一种水性油漆用发光铝颜料及其制备方法
JP2023519035A (ja) * 2020-04-05 2023-05-10 ファイザー・インク Covid-19を処置するための化合物および方法

Family Cites Families (268)

* 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
US6221335B1 (en) * 1994-03-25 2001-04-24 Isotechnika, Inc. Method of using deuterated calcium channel blockers
EP0824533B1 (de) 1995-05-09 2001-11-14 Basf Aktiengesellschaft PYRAZOLO- 1,5a]-PYRIMIDINE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG
EP0914318A1 (en) 1996-05-11 1999-05-12 Kings College London Pyrazines
US6191131B1 (en) 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company Azolo triazines and pyrimidines
PT915880E (pt) 1996-07-24 2007-12-31 Bristol Myers Squibb Pharma Co Azol triazinas e pirimidinas
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
JPH10218881A (ja) 1997-02-03 1998-08-18 Pola Chem Ind Inc 新規なピロロピラゾロピリミジン誘導体
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
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
JP2002501532A (ja) 1997-05-30 2002-01-15 メルク エンド カンパニー インコーポレーテッド 新規血管形成阻害薬
AU748816B2 (en) 1998-07-16 2002-06-13 Shionogi & Co., Ltd. Pyrimidine derivatives exhibiting antitumor activity
US6440710B1 (en) * 1998-12-10 2002-08-27 The Scripps Research Institute Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds
US6245759B1 (en) 1999-03-11 2001-06-12 Merck & Co., Inc. Tyrosine kinase inhibitors
US6660753B2 (en) 1999-08-19 2003-12-09 Nps Pharmaceuticals, Inc. Heteropolycyclic compounds and their use as metabotropic glutamate receptor antagonists
JP2001302666A (ja) 1999-09-21 2001-10-31 Nissan Chem Ind Ltd アゾール縮合ヘテロ環アニライド化合物及び除草剤
ATE234299T1 (de) * 1999-12-03 2003-03-15 Pfizer Prod Inc Sulfamoylheteroarylpyrazolverbindungen zur verwendung als analgetisches/entzündungshemmendes mittel
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
KR100688308B1 (ko) 1999-12-17 2007-02-28 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 글리코겐 신타아제 키나제3의 피라진 기제 저해제
AU2001264932A1 (en) 2000-05-26 2001-12-11 Neurogen Corporation Oxo-imidazopyrimidine-carboxamides and their use as gaba brain receptor ligands
US20020041880A1 (en) 2000-07-05 2002-04-11 Defeo-Jones Deborah Method of treating cancer
US6849660B1 (en) 2000-08-01 2005-02-01 Isis Pharmaceuticals, Inc. Antimicrobial biaryl compounds
US7067520B2 (en) 2000-11-17 2006-06-27 Ishihara Sangyo Kaisha, Ltd. Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts
EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
GB0103926D0 (en) 2001-02-17 2001-04-04 Astrazeneca Ab Chemical compounds
AU2002305450A1 (en) 2001-05-08 2002-11-18 Yale University Proteomimetic compounds and methods
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
EP1506196B1 (en) 2001-11-01 2012-01-18 Icagen, Inc. Pyrazolopyrimidines as sodium channel inhibitors
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
CA2467870A1 (en) 2001-11-21 2003-06-05 Pharmacia & Upjohn Company Substituted aryl 1,4-pyrazine derivatives
MXPA04007697A (es) 2002-02-06 2004-11-10 Vertex Pharma Compuestos de heteroarilo utiles como inhibidores de gsk-3.
AU2003218738B2 (en) 2002-03-13 2009-01-08 Janssen Pharmaceutica N.V. Sulfonyl-derivatives as novel inhibitors of histone deacetylase
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
WO2003093297A2 (en) 2002-05-03 2003-11-13 Exelixis, Inc. Protein kinase modulators and methods of use
CA2482838A1 (en) 2002-05-31 2003-12-11 Eisai Co., Ltd. Pyrazole compounds and pharmaceutical compositions containing the compound
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
WO2003101993A1 (en) 2002-06-04 2003-12-11 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
WO2004000318A2 (en) 2002-06-21 2003-12-31 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
CN1701074A (zh) 2002-09-04 2005-11-23 先灵公司 用作依赖细胞周期蛋白激酶抑制剂的吡唑并嘧啶
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
CA2497444C (en) 2002-09-04 2010-11-30 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
US7601724B2 (en) 2002-09-04 2009-10-13 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
AR041133A1 (es) 2002-09-04 2005-05-04 Pharmacopeia Drug Discovery Pirazolopirimidinas como inhibidores de la quinasa dependientes de la ciclina
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
NZ539165A (en) 2002-09-04 2008-03-28 Schering Corp Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
WO2004033431A2 (en) 2002-10-04 2004-04-22 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
TW200413273A (en) * 2002-11-15 2004-08-01 Wako Pure Chem Ind Ltd Heavy hydrogenation method of heterocyclic rings
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
PL216368B1 (pl) 2003-02-26 2014-03-31 Sugen Związki aminoheteroarylowe oraz ich zastosowanie
US7557110B2 (en) 2003-02-28 2009-07-07 Teijin Pharma Limited Pyrazolo[1,5-A] pyrimidine derivatives
EP1606267B1 (en) 2003-03-11 2008-07-30 Pfizer Products Inc. Pyrazine compounds as transforming growth factor (tgf) inhibitors
WO2004084813A2 (en) 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles 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
CN1788008A (zh) 2003-05-15 2006-06-14 麦克公司 作为s1p受体激动剂的3-(2-氨基-1-氮杂环基)-5-芳基-1,2,4-噁二唑
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
US7138401B2 (en) 2003-09-18 2006-11-21 Conforma Therapeutics Corporation 2-aminopurine analogs having HSP90-inhibiting activity
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
WO2005051301A2 (en) 2003-11-19 2005-06-09 Array Biopharma Inc. Heterocyclic inhibitors of mek and methods of use thereof
DE10356579A1 (de) 2003-12-04 2005-07-07 Merck Patent Gmbh Aminderivate
JP2007524682A (ja) 2004-02-12 2007-08-30 メルク エンド カムパニー インコーポレーテッド 代謝調節型グルタミン酸受容体−5の調節物質としてのビピリジルアミド
WO2005080396A2 (de) 2004-02-25 2005-09-01 Basf Aktiengesellschaft Azolopyrimidin-verbindungen und ihre verwendung zur bekämpfung von schadpilzen
EP1750727A2 (en) 2004-04-23 2007-02-14 Exelixis, Inc. Kinase modulators and methods of use
US20080153869A1 (en) 2004-06-14 2008-06-26 Bressi Jerome C Kinase Inhibitors
KR20070053236A (ko) 2004-07-27 2007-05-23 에스지엑스 파마슈티컬스, 인코포레이티드 융합 고리 헤테로사이클 키나제 조절제
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP1809621A1 (en) * 2004-11-02 2007-07-25 Pfizer, Inc. Methods of preparing indazole compounds
NZ555236A (en) 2004-11-04 2010-10-29 Vertex Pharma Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
EP1828144A2 (en) 2004-11-12 2007-09-05 OSI Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
NZ555566A (en) 2004-11-22 2009-12-24 Vertex Pharma Pyrrolopyrazines and pyrazolopyrazines useful as inhibitors of protein kinases
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
WO2007076360A1 (en) 2005-12-22 2007-07-05 Alcon Research, Ltd. (indazol-5-yl)-pyrazines and (1,3-dihydro-indol-2-one)- pyrazines for treating rho kinase-mediated diseases and conditions
US7635699B2 (en) 2004-12-29 2009-12-22 Bristol-Myers Squibb Company Azolopyrimidine-based inhibitors of dipeptidyl peptidase IV and methods
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
US20060156482A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
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
AU2006214477A1 (en) 2005-02-16 2006-08-24 Pharmacopeia, Inc. Heterocyclic substituted piperazines with CXCR3 antagonist activity
DE102005007534A1 (de) 2005-02-17 2006-08-31 Bayer Cropscience Ag Pyrazolopyrimidine
EP1874769B1 (de) 2005-04-25 2011-09-14 Merck Patent GmbH Neuartige aza-heterozyklen als kinase-inhibitoren
CA2608890C (en) 2005-05-20 2011-08-02 Alantos-Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155737A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
US7776865B2 (en) 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
AU2006299424A1 (en) * 2005-10-06 2007-04-12 Auspex Pharmaceuticals, Inc. Deuterated inhibitors of gastric H+, K+-ATPase with enhanced therapeutic properties
EP1942900B1 (en) 2005-10-06 2015-06-03 Merck Sharp & Dohme Corp. Use of pyrazolo [1,5-a] pyrimidine derivatives for inhibiting kinases methods for inhibiting protein kinases
CA2624500A1 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
AR055206A1 (es) 2005-10-06 2007-08-08 Schering Corp Pirazolo[1, 5 - a]pirimidinas como inhibidoras de proteina quinasa, composiciones farmaceuticas y combinaciones con agentes citostaticos que las comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer.
EP1945220A1 (en) 2005-10-21 2008-07-23 Mitsubishi Tanabe Pharma Corporation Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists
CA2626742A1 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrazolo-pyrimidines as casein kinase ii (ck2) modulators
AR056786A1 (es) 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
BRPI0619086A2 (pt) 2005-12-01 2011-09-20 Hoffmann La Roche compostos, processo para a sua manufatura, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são moduladas por inibidores de l-cpt1, e seu uso
WO2007066805A1 (ja) 2005-12-09 2007-06-14 Meiji Seika Kaisha, Ltd. リンコマイシン誘導体およびこれを有効成分とする抗菌剤
US7750168B2 (en) * 2006-02-10 2010-07-06 Sigma-Aldrich Co. Stabilized deuteroborane-tetrahydrofuran complex
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
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
CN101454314A (zh) 2006-03-31 2009-06-10 先灵公司 激酶抑制剂
AU2007268083A1 (en) 2006-05-22 2007-12-06 Schering Corporation Pyrazolo [1, 5-A] pyrimidines as CDK inhibitors
ES2340093T3 (es) 2006-06-22 2010-05-28 Biovitrum Ab (Publ) Derivados pirazina y piridina como inhibidores de cinasa mnk.
EP2038261A2 (en) 2006-06-22 2009-03-25 Mallinckrodt Inc. Pyrazine derivatives with extended conjugation and uses thereof
AR061793A1 (es) 2006-07-05 2008-09-24 Mitsubishi Tanabe Pharma Corp Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
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
EP2457913B1 (en) 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
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
US20080176870A1 (en) 2006-11-20 2008-07-24 Bert Nolte Heterobicyclic metalloprotease inhibitors
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
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
MX2009010071A (es) 2007-04-10 2009-10-16 Bayer Cropscience Ag Derivados de aril isoxazolina insecticidas.
WO2008141065A1 (en) 2007-05-10 2008-11-20 Smithkline Beecham Corporation Quinoxaline derivatives as p13 kinase inhibitors
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
EP2014661A1 (de) 2007-06-13 2009-01-14 Bayer CropScience AG Heterocyclisch substituierte Heterocyclyl-carbonsäurederivate
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
EP2170306A1 (en) 2007-06-26 2010-04-07 Lexicon Pharmaceuticals, Inc. Methods of treating serotonin-mediated diseases and disorders
WO2009006580A1 (en) 2007-07-05 2009-01-08 Cv Therapeutics, Inc. Optionally condensed dihydropyridine, dihydropyrimidine and dihydropyrane derivatives acting as late sodium channel blockers
US20090012103A1 (en) 2007-07-05 2009-01-08 Matthew Abelman Substituted heterocyclic compounds
GB0713259D0 (en) 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
EA017250B1 (ru) 2007-07-19 2012-11-30 Х. Лундбекк А/С 5-членные гетероциклические амиды и их применение для модуляции рецептора p2x
US8293747B2 (en) 2007-07-19 2012-10-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
CN101815712A (zh) 2007-08-01 2010-08-25 辉瑞有限公司 吡唑化合物及其作为raf抑制剂的用途
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
WO2009037247A1 (en) 2007-09-17 2009-03-26 Neurosearch A/S Pyrazine derivatives and their use as potassium channel modulators
AU2008315746A1 (en) 2007-10-25 2009-04-30 Astrazeneca Ab Pyridine and pyrazine derivatives useful in the treatment of cell proliferative disorders
JP2011504931A (ja) 2007-11-28 2011-02-17 シェーリング コーポレイション プロテインキナーゼ阻害剤としての2−フルオロピラゾロ[1,5−a]ピリミジン
WO2009075790A1 (en) 2007-12-07 2009-06-18 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors for intra-articular application
MX2010006748A (es) * 2007-12-19 2010-08-18 Vertex Pharma Pirazolo[1,5-a]pirimidinas utiles como inhibidores de jak2.
SG187425A1 (en) 2008-01-04 2013-02-28 Intellikine Llc Certain chemical entities, compositions and methods
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
BRPI0908494A2 (pt) 2008-02-25 2015-08-11 Hoffmann La Roche Inibidores de pirrolopirazina quinase
EP2250172B1 (en) 2008-02-25 2011-08-31 F. Hoffmann-La Roche AG Pyrrolopyrazine kinase inhibitors
JP5485178B2 (ja) 2008-02-25 2014-05-07 エフ.ホフマン−ラ ロシュ アーゲー ピロロピラジンキナーゼ阻害剤
KR20100114095A (ko) 2008-02-25 2010-10-22 에프. 호프만-라 로슈 아게 피롤로피라진 키나아제 저해제
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
JP2011515401A (ja) 2008-03-20 2011-05-19 アムジエン・インコーポレーテツド オーロラキナーゼモジュレーターおよび使用方法
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
CA2730106A1 (en) 2008-07-08 2010-01-14 Intellikine, Inc. Kinase inhibitors and methods of use
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
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
WO2010034738A2 (en) 2008-09-24 2010-04-01 Basf Se Pyrazole compounds for controlling invertebrate pests
CA2740583A1 (en) 2008-10-21 2010-04-29 Vertex Pharmaceuticals Incorporated C-met protein kinase inhibitors
AU2009308675A1 (en) 2008-10-31 2010-05-06 Genentech, Inc. Pyrazolopyrimidine JAK inhibitor compounds and methods
RU2011123647A (ru) 2008-11-10 2012-12-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, полезные в качестве ингибиторов atr киназы
WO2010059836A1 (en) 2008-11-20 2010-05-27 Decode Genetics Ehf Substituted aza-bridged bicyclics for cardiovascular and cns disease
WO2010068483A2 (en) 2008-11-25 2010-06-17 University Of Rochester Mlk inhibitors and methods of use
JP5431495B2 (ja) 2008-12-05 2014-03-05 エフ.ホフマン−ラ ロシュ アーゲー ピロロピラジニル尿素キナーゼ阻害薬
CN106496210B (zh) 2008-12-19 2020-06-09 沃泰克斯药物股份有限公司 用作atr激酶抑制剂的化合物
ES2567047T3 (es) 2008-12-23 2016-04-19 Abbvie Inc. Derivados de pirimidina anti-virales
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
CA2750452A1 (en) 2009-01-30 2010-08-05 Toyama Chemical Co., Ltd. N-acyl anthranilic acid derivative or salt thereof
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
JP2012517471A (ja) 2009-02-11 2012-08-02 スノビオン プハルマセウトイカルス インコーポレイテッド ヒスタミンh3インバースアゴニスト及びアンタゴニスト、並びにその使用方法
CN101537007A (zh) 2009-03-18 2009-09-23 中国医学科学院血液病医院(血液学研究所) N-(噻吩-2)吡唑并[1,5-a]嘧啶-3-甲酰胺类化合物在制备抗恶性肿瘤药物方面的应用
WO2010111653A2 (en) 2009-03-27 2010-09-30 The Uab Research Foundation Modulating ires-mediated translation
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
EP2454262B1 (en) 2009-07-15 2014-05-14 Abbott Laboratories Pyrrolopyrazine inhibitors of kinases
WO2011022439A1 (en) 2009-08-17 2011-02-24 Intellikine, Inc. Heterocyclic compounds and uses thereof
US8669259B2 (en) 2009-08-26 2014-03-11 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
CN101671336B (zh) 2009-09-23 2013-11-13 辽宁利锋科技开发有限公司 芳杂环并嘧啶衍生物和类似物及其制备方法和用途
US8575177B2 (en) 2009-12-04 2013-11-05 Senhwa Biosciences, Inc. Pyrazolopyrimidines and related heterocycles as CK2 inhibitors
BR112012023576B1 (pt) 2010-03-18 2022-08-23 Institut Pasteur Korea Compostos anti-infecciosos e composições compreendendo os mesmos
US8518945B2 (en) 2010-03-22 2013-08-27 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
WO2011121096A1 (en) 2010-03-31 2011-10-06 Dkfz Deutsches Krebsforschungszentrum PYRAZOL[1,5-a]PYRIMIDINE DERIVATIVES AS WNT PATHWAY ANTAGONISTS
CA2794428A1 (en) 2010-04-08 2011-10-13 Pfizer Inc. Substituted 3,5-diphenyl-isoxazoline derivatives as insecticides and acaricides
ES2602475T3 (es) 2010-04-15 2017-02-21 Tracon Pharmaceuticals, Inc. Potenciación de la actividad anticáncer por terapia de combinación con inhibidores de la vía BER
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
AU2011253025A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2011143425A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2011143422A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of atr kinase
CA2799904A1 (en) 2010-05-20 2011-11-24 F. Hoffmann-La Roche Ag Pyrrolo [2, 3 - b] pyrazine - 7 - carboxamide derivatives and their use as jak and syk inhibitors
KR20130083387A (ko) 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 Syk 및 jak 억제제로서 피롤로피라진 유도체
US8623869B2 (en) 2010-06-23 2014-01-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
DK2585467T3 (en) 2010-06-24 2016-06-13 Gilead Sciences Inc PYRAZOLO [1,5-A] PYRIMIDINES AND TRIAZINES AS ANTIVIRAL AGENTS
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
JP5985473B2 (ja) 2010-07-13 2016-09-06 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft IRAK4モジュレーターとしてのピラゾロ[1,5a]ピリミジン及びチエノ[3,2b]ピリミジン誘導体
EP2407478A1 (en) 2010-07-14 2012-01-18 GENETADI Biotech, S.L. New cyclotetrapeptides with pro-angiogenic properties
WO2012022045A1 (en) 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
EP2608669B1 (en) 2010-08-23 2016-06-22 Merck Sharp & Dohme Corp. NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
US8609669B2 (en) 2010-11-16 2013-12-17 Abbvie Inc. Potassium channel modulators
JP6091422B2 (ja) 2010-11-16 2017-03-08 アレイ バイオファーマ、インコーポレイテッド チェックポイントキナーゼ1阻害剤とwee1キナーゼ阻害剤の組み合わせ
PT2649075T (pt) 2010-12-08 2018-07-30 Us Health Pirazolopirimidinas substituídas como ativadores de glucocerebrosidase
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
KR20140027974A (ko) 2011-04-05 2014-03-07 버텍스 파마슈티칼스 인코포레이티드 Tra 키나제의 억제제로서 유용한 아미노피라진 화합물
WO2012143796A2 (en) 2011-04-21 2012-10-26 Institut Pasteur Korea Anti-inflammation compounds
ES2583086T3 (es) 2011-04-21 2016-09-19 Bayer Intellectual Property Gmbh Pirazolopiridinas sustituidas con fluoroalquilo y su uso
US9187487B2 (en) 2011-05-17 2015-11-17 Principia Biopharma, Inc. Azaindole derivatives as tyrosine kinase inhibitors
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
WO2012178125A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9845327B2 (en) 2011-06-22 2017-12-19 The General Hospital Corporation Treatment of proteinopathies
US9096602B2 (en) 2011-06-22 2015-08-04 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-B]pyrazines as ATR kinase inhibitors
BR112014000653A2 (pt) 2011-07-13 2017-02-14 Pharmacyclics Inc inibidores de tirosina quinase de bruton
WO2013052263A2 (en) 2011-09-16 2013-04-11 Microbiotix, Inc. Antifungal compounds
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
RU2677292C2 (ru) 2011-09-30 2019-01-16 Вертекс Фармасьютикалз Инкорпорейтед Способы получения соединений, которые можно использовать в качестве ингибиторов киназы atr
MX2014003796A (es) 2011-09-30 2015-01-16 Vertex Pharma Compuestos utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
CA2850491C (en) 2011-09-30 2020-10-27 Vertex Pharmaceuticals Incorporated Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2768509B1 (en) 2011-10-20 2017-03-22 Glaxosmithkline LLC Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013071093A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Pyrazine compounds useful as inhibitors of atr kinase
WO2013071088A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776422A1 (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
WO2013138436A1 (en) 2012-03-14 2013-09-19 Bristol-Myers Squibb Company Cyclolic hydrazine derivatives as hiv attachment inhibitors
MX354965B (es) 2012-04-02 2018-03-27 Cytokinetics Inc Metodo para mejorar la funcion del diafragma.
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2013152198A1 (en) * 2012-04-04 2013-10-10 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
WO2013152298A1 (en) 2012-04-05 2013-10-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN103373996A (zh) 2012-04-20 2013-10-30 山东亨利医药科技有限责任公司 作为crth2受体拮抗剂的二并环衍生物
MX358819B (es) 2012-05-15 2018-09-05 Cancer Research Tech Ltd 5-[[4-[[morfolin-2-il]metilamino]-5-(trifluorometil)-2-piridil]am ino]pirazina-2-carbonitrilo y usos terapeuticos del mismo.
KR20150009553A (ko) 2012-05-23 2015-01-26 사피라 파르마슈티칼즈 게엠베하 7-옥소-티아졸로피리딘 탄산 유도체 및 바이러스성 질환의 치료, 개선 또는 예방에서의 이의 용도
WO2013174931A1 (en) 2012-05-23 2013-11-28 Savira Pharmaceuticals Gmbh 7-oxo-4,7 -dihydro- pyrazolo [1, 5 -a] pyrimidine derivatives which are useful in the treatment, amelioration or prevention of a viral disease
US20140018361A1 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
KR20150039832A (ko) 2012-08-06 2015-04-13 사피라 파르마슈티칼즈 게엠베하 디하이드록시피리미딘 탄산 유도체 및 바이러스성 질환의 치료, 개선 또는 예방에서의 이의 용도
US9655888B2 (en) 2012-08-09 2017-05-23 VIIV Healthcare UK (No.5) Limited Tricyclic alkene derivatives as HIV attachment inhibitors
ES2614034T3 (es) 2012-08-09 2017-05-29 VIIV Healthcare UK (No.5) Limited Derivados de amidina tricíclica como inhibidores de la unión del VIH
EP2895471B1 (en) 2012-08-09 2016-11-23 VIIV Healthcare UK (No.5) Limited Piperidine amide derivatives as hiv attachment inhibitors
RU2015109064A (ru) 2012-08-17 2016-10-10 Байер Кропсайенс Аг Амиды азаиндолкарбоновых и азаиндолтиокарбоновых кислот в качестве инсектицитов и акарицидов
BR112015002950A2 (pt) 2012-08-24 2017-08-08 Hoffmann La Roche novos derivados de bicíclico-piridina
WO2014035140A2 (en) 2012-08-30 2014-03-06 Kainos Medicine, Inc. Compounds and compositions for modulating histone methyltransferase activity
US9475816B2 (en) 2012-09-07 2016-10-25 Takeda Pharmaceutical Company Limited Substituted-1,4-dihydropyrazolo[4,3-b]indoles
WO2014042433A2 (en) 2012-09-14 2014-03-20 Kainos Medicine, Inc. Compounds and compositions for modulating adenosine a3 receptor activity
TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
EP2897618B1 (en) 2012-09-24 2021-11-17 Neupharma, Inc. Certain chemical entities, compositions, and methods
DK2904406T3 (en) 2012-10-04 2018-06-18 Vertex Pharma METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE
CA2900335C (en) 2012-10-22 2021-10-26 City Of Hope Synthetic analogs of epipolythiodioxopiperazines and uses thereof
EP2912464B1 (en) 2012-10-24 2017-04-26 Becton Dickinson and Company Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same
NZ731337A (en) 2012-12-07 2019-02-22 Vertex Pharma Compounds useful as inhibitors of atr kinase
JP2016512239A (ja) 2013-03-15 2016-04-25 バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated Atrキナーゼの阻害剤として有用な化合物
WO2014143242A1 (en) * 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2016512815A (ja) 2013-03-15 2016-05-09 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キナーゼの阻害剤として有用な縮合ピラゾロピリミジン誘導体
PL3077397T3 (pl) 2013-12-06 2020-04-30 Vertex Pharmaceuticals Inc. Związek 2-amino-6-fluoro-n-[5-fluoro-pirydyn-3-ylo]pyrazolo [1,5-a]pirymidino-3-karboksamidu przydatny jako inhibitor kinazy atr, jego wytwarzanie, różne postacie stałe i ich radioznakowane pochodne
US20150158868A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
SI3152212T1 (sl) 2014-06-05 2020-06-30 Vertex Pharmaceuticals Inc. Radioaktivno označeni derivati 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)-pirazolo (1,5-A)pirimidin-3- karboksamidne spojine, koristni kot inhibitor kinaze ATR, priprava navedene spojine in njene različne trdne oblike
RS59054B1 (sr) 2014-06-17 2019-08-30 Vertex Pharma Postupak za lečenje raka korišćenjem kombinacije chk1 i atr inhibitora

Also Published As

Publication number Publication date
LT3077397T (lt) 2020-01-27
AU2014360380B2 (en) 2019-03-21
SG11201604519PA (en) 2016-07-28
CN105934435A (zh) 2016-09-07
BR112016012734B1 (pt) 2022-09-13
HRP20192183T1 (hr) 2020-02-21
RU2019113160A (ru) 2019-06-17
RU2016126919A (ru) 2018-12-06
RU2720408C2 (ru) 2020-04-29
IL246028B (en) 2020-01-30
RU2750148C1 (ru) 2021-06-22
US20150158872A1 (en) 2015-06-11
BR112016012734A2 (pl) 2017-08-08
US20190256516A1 (en) 2019-08-22
JP2016539155A (ja) 2016-12-15
BR112016012734A8 (pt) 2020-05-19
JP6543252B2 (ja) 2019-07-10
EP3077397A1 (en) 2016-10-12
ZA201603893B (en) 2019-11-27
WO2015085132A1 (en) 2015-06-11
AU2019200723B2 (en) 2021-08-26
RU2019113160A3 (pl) 2019-11-19
US11485739B2 (en) 2022-11-01
US10160760B2 (en) 2018-12-25
KR102153886B1 (ko) 2020-09-09
CA2932757A1 (en) 2015-06-11
DK3077397T3 (da) 2019-12-16
SG10201804791UA (en) 2018-07-30
CA2932757C (en) 2023-10-31
SI3077397T1 (sl) 2020-02-28
IL246028A0 (en) 2016-08-02
MX370390B (es) 2019-12-11
RU2687276C2 (ru) 2019-05-13
ES2768678T3 (es) 2020-06-23
US10815239B2 (en) 2020-10-27
US20210032255A1 (en) 2021-02-04
EP3077397B1 (en) 2019-09-18
PT3077397T (pt) 2020-01-22
HUE046727T2 (hu) 2020-03-30
AU2019200723A1 (en) 2019-02-21
AU2014360380A1 (en) 2016-06-30
KR20160093720A (ko) 2016-08-08
NZ720909A (en) 2020-10-30
CN105934435B (zh) 2019-02-22
MX2016007371A (es) 2016-09-08
RU2016126919A3 (pl) 2018-12-06
RS59679B1 (sr) 2020-01-31

Similar Documents

Publication Publication Date Title
ZA201603893B (en) 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof
ZA201700035B (en) Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
HK1222659A1 (zh) 吡咯並 嘧啶衍生物,它們的製備方法和它們作爲激酶抑制劑的用途
HRP20171724T1 (hr) Imidazo[1,2-b]piridazin derivati kao inhibitori kinaze
HRP20190152T1 (hr) Kombinacija pirolo[2,3-d]pirimidinskih derivata s jednim ili više dodatnih sredstava kao inhibitori kinaza srodnih janus kinazi (jak)
IL228968A0 (en) Kinase-inhibiting pyrazolo[4,3-d]pyrimidine compounds, preparations containing them and their uses
PT3486245T (pt) 2-amino-n-(piperidin-1-il-piridin-3- il)pirazolo[1,5alfa]pirimidina-3-carboxamida como inibidor da quinase atr
HK1255467A1 (zh) 作為雙重dyrk1/clk1抑制劑的新的吡咯並[2,3-d]嘧啶衍生物
EP2788000A4 (en) PYRROLOPYRIMIDINES AS INHIBITORS OF KINASE JANUS
IL240877A0 (en) History of triazolo [5,4-d] pyrimidine, their preparation and pharmaceutical preparations containing them
IL266305B (en) History of [4,2,1]triazolo[5,1-a]pyrimidine as pde2 inhibitors
HK1219101A1 (zh) 作為 激酶抑制劑的 ***並 吡啶的衍生物
EP3196199A4 (en) Substituted n-(pyrrolidine-3-yl)-7h-pyrrolo[2,3-d]pyrimidine-4-amine as janus kinase inhibitor