PL3152212T3 - Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych - Google Patents

Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych

Info

Publication number
PL3152212T3
PL3152212T3 PL15745265T PL15745265T PL3152212T3 PL 3152212 T3 PL3152212 T3 PL 3152212T3 PL 15745265 T PL15745265 T PL 15745265T PL 15745265 T PL15745265 T PL 15745265T PL 3152212 T3 PL3152212 T3 PL 3152212T3
Authority
PL
Poland
Prior art keywords
fluoro
pyrazolo
pyrimidin
pyridin
amino
Prior art date
Application number
PL15745265T
Other languages
English (en)
Polish (pl)
Inventor
Nadia AHMAD
Jean-Damien Charrier
Chris Davis
Gorka ETXEBARRIA I JARDI
Damien Fraysse
Ronald Knegtel
Maninder PANESAR
Francoise Pierard
Joanne Pinder
Pierre-Henri Storck
John Studley
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 PL3152212T3 publication Critical patent/PL3152212T3/pl

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
PL15745265T 2014-06-05 2015-05-28 Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych PL3152212T3 (pl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462008277P 2014-06-05 2014-06-05
PCT/US2015/032879 WO2015187451A1 (en) 2014-06-05 2015-05-28 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
EP15745265.7A EP3152212B9 (en) 2014-06-05 2015-05-28 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

Publications (1)

Publication Number Publication Date
PL3152212T3 true PL3152212T3 (pl) 2020-06-15

Family

ID=53773488

Family Applications (1)

Application Number Title Priority Date Filing Date
PL15745265T PL3152212T3 (pl) 2014-06-05 2015-05-28 Radioznakowane pochodne związku 2-amino-6-fluoro-n-[5-fluoro-piridyn-3-ylo]-pirazolo[1,5-a]pirymidino-3-karboksamidu przydatne jako inhibitor kinazy atr, wytwarzanie tego związku i jego różnych postaci stałych

Country Status (22)

Country Link
US (3) US9670215B2 (2)
EP (1) EP3152212B9 (2)
JP (2) JP6568111B2 (2)
KR (1) KR102575125B1 (2)
CN (2) CN107074863B (2)
AU (2) AU2015271030B2 (2)
BR (1) BR112016028273B1 (2)
CA (1) CA2950587C (2)
DK (1) DK3152212T3 (2)
ES (1) ES2777608T3 (2)
HR (1) HRP20200186T1 (2)
IL (1) IL249361B (2)
LT (1) LT3152212T (2)
MX (2) MX373102B (2)
PL (1) PL3152212T3 (2)
PT (1) PT3152212T (2)
RS (1) RS60013B1 (2)
RU (2) RU2719583C2 (2)
SG (2) SG10201902206QA (2)
SI (1) SI3152212T1 (2)
WO (1) WO2015187451A1 (2)
ZA (1) ZA201700035B (2)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
CN108685922A (zh) 2011-09-30 2018-10-23 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CN106496173A (zh) 2011-09-30 2017-03-15 沃泰克斯药物股份有限公司 用于制备可用作atr激酶抑制剂的化合物的方法
CN108478577A (zh) 2012-04-05 2018-09-04 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
SI2941432T1 (en) 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
MX373102B (es) 2014-06-05 2020-04-17 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 útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo.
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
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
WO2017118734A1 (en) * 2016-01-08 2017-07-13 The Institute Of Cancer Research: Royal Cancer Hospital Inhibitors of ataxia-telangiectasia mutated and rad3-related protein kinase (atr) for use in methods of treating cancer
TW201840319A (zh) 2017-02-24 2018-11-16 德商拜耳廠股份有限公司 Atr激酶抑制劑與鐳-223鹽之組合
JOP20190197A1 (ar) 2017-02-24 2019-08-22 Bayer Pharma AG مثبط كيناز ايه تي آر للاستخدام في طريقة لعلاج مرض فرط التكاثر
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
WO2019014618A1 (en) 2017-07-13 2019-01-17 Board Of Regents, University Of Texas System HETEROCYCLIC INHIBITORS OF KINASE ATR
US11690911B2 (en) 2017-08-04 2023-07-04 Bayer Aktiengesellschaft Combination of ATR kinase inhibitors and PD-1/PD-L1 inhibitors
JP7290627B2 (ja) 2017-08-17 2023-06-13 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
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
EP3720973A1 (en) 2017-12-08 2020-10-14 Bayer Aktiengesellschaft Predictive markers for atr kinase inhibitors
JP7341156B2 (ja) 2018-03-16 2023-09-08 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
KR20210066837A (ko) 2018-09-26 2021-06-07 메르크 파텐트 게엠베하 암 치료를 위한 pd-1 안타고니스트, atr 억제제 및 백금화제의 조합
WO2020078905A1 (en) 2018-10-15 2020-04-23 Merck Patent Gmbh Combination therapy utilizing dna alkylating agents and atr inhibitors
WO2020078788A1 (en) 2018-10-16 2020-04-23 Bayer Aktiengesellschaft Combination of atr kinase inhibitors with 2,3-dihydroimidazo[1,2-c]quinazoline compounds

Family Cites Families (261)

* 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
ATE208778T1 (de) 1995-05-09 2001-11-15 Basf Ag Pyrazolo- 1,5a)-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung
EP0914318A1 (en) 1996-05-11 1999-05-12 Kings College London Pyrazines
HU229024B1 (en) 1996-07-24 2013-07-29 Bristol Myers Squibb Pharma Co Azolo-pyridimidines, pharmaceutical compositions containing the same and use thereof
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
US6191131B1 (en) 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company 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
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
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
AU748816B2 (en) 1998-07-16 2002-06-13 Shionogi & Co., Ltd. Pyrimidine derivatives exhibiting antitumor activity
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
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
JP2003516974A (ja) 1999-12-17 2003-05-20 カイロン コーポレイション グリコーゲンシンターゼキナーゼ３のピラジンベースインヒビター
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
ATE409181T1 (de) 2001-05-08 2008-10-15 Univ Yale Proteomimetische verbindungen und verfahren
WO2003000187A2 (en) 2001-06-21 2003-01-03 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
CA2465326C (en) 2001-11-01 2011-03-29 Icagen, Inc. Pyrazolopyrimidines for decreasing ion flow through a voltage-dependent sodium channel
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
BR0214309A (pt) 2001-11-21 2004-10-13 Upjohn Co Derivados aril-1,4-pirazina substituìdos
WO2003066629A2 (en) 2002-02-06 2003-08-14 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of gsk-3
CN100445276C (zh) 2002-03-13 2008-12-24 詹森药业有限公司 用作组蛋白去乙酰酶抑制剂的磺酰基衍生物
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
EP1501514B1 (en) 2002-05-03 2012-12-19 Exelixis, Inc. Protein kinase modulators and methods of use
US7429609B2 (en) 2002-05-31 2008-09-30 Eisai R & D Management Co., Ltd. Pyrazole compound and medicinal composition containing the same
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
AU2003240488A1 (en) 2002-06-04 2003-12-19 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
ES2285164T3 (es) 2002-09-04 2007-11-16 Schering Corporation Pirazolopirimidinas como inhibidores de quinasas dependientes de ciclina.
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines 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
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
MY141978A (en) 2002-09-04 2010-08-16 Schering Corp Pyrazolopyrimidines as cyclin dependent kinase inhibitors
MXPA05002571A (es) 2002-09-04 2005-09-08 Schering Corp Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina.
US8673924B2 (en) 2002-09-04 2014-03-18 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines 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
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
DE60313872T2 (de) 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
AU2003282679A1 (en) 2002-10-04 2004-05-04 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
US7550470B2 (en) 2002-12-11 2009-06-23 Merck & Co. Inc. Substituted pyrazolo[1,5-A]pyrimidines as tyrosine kinase inhibitors
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
DK1603570T5 (da) 2003-02-26 2013-12-09 Sugen Inc Aminoheteroarylforbindelser som proteinkinaseinhibitorer
US7557110B2 (en) 2003-02-28 2009-07-07 Teijin Pharma Limited Pyrazolo[1,5-A] pyrimidine derivatives
WO2004080982A1 (en) 2003-03-11 2004-09-23 Pfizer Products Inc. Pyrazine compounds as transforming growth factor (tgf) inhibitors
US7459454B2 (en) 2003-03-21 2008-12-02 Smithkline Beecham Corporation Aminopyrazine derivatives and compositions
JP2006521357A (ja) 2003-03-24 2006-09-21 メルク　エンド　カムパニー　インコーポレーテッド ナトリウムチャンネル遮断薬としてのビアリール置換６員複素環化合物
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
AU2004240586A1 (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
MXPA06002997A (es) 2003-09-18 2007-02-08 Conforma Therapeutics Corp Novedosos compuestos heterociclicos como inhibidores- hsp90.
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
CN1905873A (zh) 2003-11-19 2007-01-31 阵列生物制药公司 Mek的杂环抑制剂及其使用方法
DE10356579A1 (de) 2003-12-04 2005-07-07 Merck Patent Gmbh Aminderivate
CA2555402A1 (en) 2004-02-12 2005-09-01 Celine Bonnefous Bipyridyl amides as modulators of metabotropic glutamate receptor-5
EP1720879A2 (de) 2004-02-25 2006-11-15 Basf Aktiengesellschaft Azolopyrimidin-verbindungen und ihre verwendung zur bekämpfung von schadpilzen
WO2005117909A2 (en) 2004-04-23 2005-12-15 Exelixis, Inc. Kinase modulators and methods of use
JP2008502687A (ja) 2004-06-14 2008-01-31 タケダ サン ディエゴ インコーポレイテッド キナーゼ阻害剤
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CA2573573A1 (en) 2004-07-27 2006-02-09 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
PT1812440E (pt) 2004-11-04 2011-01-25 Vertex Pharma Pirazolo[1,5-a]pirimidinas úteis enquanto inibidores de proteínas cinases
EP1828144A2 (en) 2004-11-12 2007-09-05 OSI Pharmaceuticals, Inc. Integrin antagonists useful as anticancer agents
WO2006058120A1 (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
MX2007007797A (es) 2004-12-27 2007-08-23 Alcon Inc Analogo de aminopirazina para tratar glaucoma y otras enfermedades mediadas por rho cinasa.
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
JP4873352B2 (ja) 2005-02-16 2012-02-08 シェーリング コーポレイション Ｃｘｃｒ３アンタゴニスト活性を有する、複素環で置換されたピペラジン
DE102005007534A1 (de) 2005-02-17 2006-08-31 Bayer Cropscience Ag Pyrazolopyrimidine
WO2006114180A1 (de) 2005-04-25 2006-11-02 Merck Patent Gmbh Neuartige aza-heterozyklen als kinase-inhibitoren
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
BRPI0609802A2 (pt) 2005-05-20 2017-05-02 Alantos Pharmaceuticals Holding Inc composto, composição farmacêutica e uso de um composto
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
AR057979A1 (es) 2005-10-06 2008-01-09 Schering Corp PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
JP5052518B2 (ja) 2005-10-06 2012-10-17 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのピラゾロピリミジン
CN101321759A (zh) 2005-10-06 2008-12-10 先灵公司 作为蛋白激酶抑制剂的吡唑并嘧啶化合物
BRPI0616985B1 (pt) 2005-10-06 2021-10-26 Merck Sharp & Dohme Corp. Composto de pirazolo[1,5-a]pirimidina, e, uso de um composto
AR056876A1 (es) 2005-10-21 2007-10-31 Tanabe Seiyaku Co Compuestos de pirazolo[1-5-a]pirimidina, antagonistas de receptores canabinoides cb1, composiciones farmaceuticas que los contienen y usos en el tratamiento de enfermedades del sistema nervioso central, tales como trastornos psicoticos, neurologicos y similares
US8372851B2 (en) 2005-10-21 2013-02-12 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
EP1959951B1 (en) 2005-12-01 2009-12-23 F. Hoffmann-la Roche AG Heteroaryl substituted piperidine derivatives as l-cpt1 inhibitors
EP1970377A4 (en) 2005-12-09 2013-02-27 Meiji Seika Kaisha LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THIS AS AN ACTIVE SUBSTANCE
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
JP2009533327A (ja) 2006-03-22 2009-09-17 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 増殖性疾患を処置するためのｃ−ＭＥＴキナーゼ阻害剤
US20100273776A1 (en) 2006-03-29 2010-10-28 FOLDRx PHARMACEUTICALS, INC Inhibition of alpha-synuclein toxicity
MX2008012658A (es) 2006-03-31 2008-12-16 Schering Corp Inhibidores de cinasa.
WO2007139732A1 (en) 2006-05-22 2007-12-06 Schering Corporation Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors
US20080039450A1 (en) 2006-06-22 2008-02-14 Jensen Annika J Compounds
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
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
WO2008037477A1 (en) 2006-09-29 2008-04-03 Novartis Ag Pyrazolopyrimidines as p13k lipid kinase inhibitors
GB0619342D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
KR101107896B1 (ko) 2006-10-04 2012-01-25 에프. 호프만-라 로슈 아게 고 밀도 지단백질(ｈｄｌ)-콜레스테롤 상승제로서 3-피리딘카복스아마이드 및 2-피라진카복스아마이드 유도체
MX337906B (es) 2006-10-19 2016-03-28 Signal Pharm Llc Compuestos de heteroarilo, composiciones de los mismos, y su uso como inhibidores de proteina cinasas.
US8148361B2 (en) 2006-11-10 2012-04-03 Bristol-Myers Squibb Company Kinase inhibitors
CA2670083A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
EP2125808A2 (en) 2006-12-15 2009-12-02 Bayer Schering Pharma Aktiengesellschaft 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
GB0625659D0 (en) 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
PE20121126A1 (es) 2006-12-21 2012-08-24 Plexxikon Inc Compuestos pirrolo [2,3-b] piridinas como moduladores de quinasa
MX2009008531A (es) 2007-02-16 2009-08-26 Amgen Inc Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met.
CA2679659C (en) 2007-03-01 2016-01-19 Novartis Ag Pim kinase inhibitors and methods of their use
US8372867B2 (en) 2007-04-10 2013-02-12 Bayer Cropscience Ag Insecticidal aryl isoxazoline derivatives
PE20090288A1 (es) 2007-05-10 2009-04-03 Smithkline Beecham Corp Derivados de quinoxalina como inhibidores de la pi3 quinasa
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
EP2157090A4 (en) 2007-06-21 2011-09-07 Taisho Pharmaceutical Co Ltd PYRAZINAMIDE COMPOUND
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
HRP20151052T1 (xx) 2007-07-19 2015-11-06 H. Lundbeck A/S Peteroäślani heterocikliäśki amidi i srodne tvari
MY150032A (en) 2007-07-19 2013-11-29 Merck Sharp & Dohme Heterocyclic amide compounds as protein kinase inhibitors
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
WO2009016460A2 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
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
JP2011500778A (ja) 2007-10-25 2011-01-06 アストラゼネカ・アクチエボラーグ ピリジン及びピラジン誘導体−０８３
CN101970440A (zh) 2007-11-28 2011-02-09 先灵公司 作为蛋白激酶抑制剂的2-氟吡唑并[1，5-a]嘧啶类
WO2009075790A1 (en) 2007-12-07 2009-06-18 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors for intra-articular application
MX2010007419A (es) 2008-01-04 2010-11-12 Intellikine Inc Ciertas entidades quimicas, composiciones y metodos.
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
JP5368485B2 (ja) 2008-02-25 2013-12-18 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インヒビター
CA2712507A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
CN101945877B (zh) 2008-02-25 2013-07-03 霍夫曼-拉罗奇有限公司 吡咯并吡嗪激酶抑制剂
WO2009106444A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
CA2716856C (en) 2008-03-20 2013-02-19 Amgen Inc. Aurora kinase modulators and method of use
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
BRPI0915231A2 (pt) 2008-07-08 2018-06-12 Intellikine Inc compostos inibidores de quinase e métodos de uso
JP2011530511A (ja) 2008-08-05 2011-12-22 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
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
EP2346335B1 (en) 2008-09-24 2018-11-14 Basf Se Pyrazole compounds for controlling invertebrate pests
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
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
CA2743134A1 (en) 2008-11-10 2010-05-14 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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
EP2373653B1 (en) 2008-12-05 2014-04-02 F. Hoffmann-La Roche AG Pyrrolopyrazinyl urea kinase inhibitors
ES2921576T3 (es) 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
SG172352A1 (en) 2008-12-23 2011-07-28 Abbott Lab Anti-viral compounds
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
KR20110110286A (ko) 2009-01-30 2011-10-06 토야마 케미칼 컴퍼니 리미티드 Ｎ-아실 안트라닐산 유도체 또는 그 염
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
BRPI1008020A2 (pt) 2009-02-11 2016-03-15 Sunovion Pharmaceuticals Inc antagonistas e agonistas inversos h3 da histamina e métodos de uso dos mesmos
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
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
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
ES2483594T3 (es) 2009-07-15 2014-08-06 Abbott Laboratories Pirrolopirazinas inhibidoras de quinasas
NZ598220A (en) 2009-08-17 2014-02-28 Intellikine Llc 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
JP5802676B2 (ja) 2009-12-04 2015-10-28 センワ バイオサイエンシズ インコーポレイテッド Ｃｋ２阻害剤としてのピラゾロピリミジンおよび関連複素環化合物
CA2793086C (en) 2010-03-18 2018-08-21 Institut Pasteur Korea Substituted imidazo[1,2-a]pyridine compounds and their use in the treatment of bacterial infections
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
MX2012011549A (es) 2010-04-08 2013-01-29 Ah Usa 42 Llc Derivados de 3,5-difenil-isoxazolina sustituida como insecticidas y acaricidas.
WO2011130689A1 (en) 2010-04-15 2011-10-20 Tracon Pharmaceuticals, Inc. Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors
US9062008B2 (en) 2010-05-12 2015-06-23 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
NZ603477A (en) 2010-05-12 2014-09-26 Vertex Pharma Compounds useful as inhibitors of atr kinase
CA2798760A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated 2-aminopyridine derivatives useful as inhibitors of atr kinase
EP2568984A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9334244B2 (en) 2010-05-12 2016-05-10 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2571881A1 (en) 2010-05-20 2013-03-27 F.Hoffmann-La Roche Ag Pyrrolopyrazine derivatives as syk and jak inhibitors
MX2012013378A (es) 2010-05-20 2013-01-24 Hoffmann La Roche Derivados de pirrolo [2, 3-b] pirazina-7-carboxamida y sus uso como inhibidores de cinasa janus (jak) y cinasa tirosina del brazo (syk).
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
PT3012258T (pt) 2010-06-24 2018-12-14 Gilead Sciences Inc Composição farmacêutica compreendendo um derivado de pirazolo[1,5-a]pirimidina como agente antiviral
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
CN110003219A (zh) 2010-07-13 2019-07-12 弗·哈夫曼-拉罗切有限公司 作为irak4调节剂的吡唑并[1,5a]嘧啶和噻吩并[3,2b]嘧啶衍生物
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
US8883801B2 (en) 2010-08-23 2014-11-11 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors
RU2017127088A (ru) 2010-11-16 2019-02-04 Эррэй Биофарма Инк. Комбинация ингибиторов чекпойнт-киназы 1 и ингибиторов киназы wee 1
US8609669B2 (en) 2010-11-16 2013-12-17 Abbvie Inc. Potassium channel modulators
EP3366688B1 (en) 2010-12-08 2022-02-09 The U.S.A. as represented by the Secretary, Department of Health and Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
MX2013011450A (es) 2011-04-05 2014-02-03 Vertex Pharma Compuestos de aminopirazina utiles como inhibidores de la cinasa ataxia telangiectasia mutada y rad3 relacionados (atr).
KR102104125B1 (ko) 2011-04-21 2020-05-29 재단법인 한국파스퇴르연구소 소염 화합물
JP6005134B2 (ja) 2011-04-21 2016-10-12 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ フルオロアルキル置換ピラゾロピリジンおよびその使用
CN103502249A (zh) 2011-05-17 2014-01-08 普林斯匹亚生物制药公司 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
CA2840224C (en) 2011-06-22 2019-08-13 The General Hospital Corporation Treatment of proteinopathies
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
JP2014520863A (ja) 2011-07-13 2014-08-25 ファーマサイクリックス，インク． Ｂｒｕｔｏｎ型チロシンキナーゼの阻害剤
WO2013052263A2 (en) 2011-09-16 2013-04-11 Microbiotix, Inc. Antifungal compounds
CN108685922A (zh) 2011-09-30 2018-10-23 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
WO2013049722A1 (en) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2013049720A1 (en) 2011-09-30 2013-04-04 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
CN106496173A (zh) 2011-09-30 2017-03-15 沃泰克斯药物股份有限公司 用于制备可用作atr激酶抑制剂的化合物的方法
JP6073343B2 (ja) 2011-10-20 2017-02-01 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ サーチュイン調節因子としての置換された二環式アザ複素環およびアナログ
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2015502925A (ja) 2011-11-09 2015-01-29 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ピラジン化合物
US8846918B2 (en) 2011-11-09 2014-09-30 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
US8841337B2 (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
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
KR20160046693A (ko) 2012-04-02 2016-04-29 싸이토키네틱스, 인코포레이티드 횡격막 기능을 향상시키는 방법들
CN108478577A (zh) 2012-04-05 2018-09-04 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
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
ES2624307T3 (es) 2012-05-15 2017-07-13 Cancer Research Technology Ltd 5-[[4-[[Morfolin-2-il]metilamino]-5-(trifluorometil)-2-piridil]amino]pirazin-2-carbonitrilo y usos terapéuticos del mismo
MX2014014109A (es) 2012-05-23 2016-03-31 Savira Pharmaceuticals Gmbh Derivados de 7-oxo-4,7-dihidro-pirazolo[1,5-a]pirimidina que son utiles en el tratamiento, mejora o prevencion de una enfermedad viral.
BR112014029016A8 (pt) 2012-05-23 2018-01-09 European Molecular Biology Laboratory derivados de ácido 7-oxo-tiazolopiridina carbônico e seu uso no tratamento, melhora ou prevenção de uma doença viral
WO2014011911A2 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
JP2014022472A (ja) * 2012-07-13 2014-02-03 Sharp Corp 発光装置、照明装置および発光方法
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
EP2895475B1 (en) 2012-08-09 2016-11-09 VIIV Healthcare UK (No.5) Limited Tricyclic amidine derivatives as hiv attachment inhibitors
WO2014025854A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Piperidine amide derivatives as hiv attachment inhibitors
EP2895472B1 (en) 2012-08-09 2016-11-23 VIIV Healthcare UK (No.5) Limited Tricyclic alkene derivatives as HIV attachment inhibitors
BR112015003098A2 (pt) 2012-08-17 2017-08-22 Bayer Cropscience Ag Azaindolecarboxamidas e azaindoletiocarboxamidas como inseticidas e acaricidas.
KR20150046056A (ko) 2012-08-24 2015-04-29 에프. 호프만-라 로슈 아게 신규한 바이사이클릭피리딘 유도체
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
US9688635B2 (en) 2012-09-24 2017-06-27 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
CN108440571B (zh) 2012-10-22 2022-11-04 希望之城 Etp衍生物
BR112015003160A2 (pt) 2012-10-24 2017-07-04 Becton Dickinson Co corantes de azaindolina - cianina substituídos por hidroxamato e bioconjugados dos mesmos
SI2941432T1 (en) * 2012-12-07 2018-07-31 Vertex Pharmaceuticals Incorporated 2-AMINO-6-FLUORO-N- (5-FLUORO-4- (4- (4- (OXETHAN-3-YL) PIPERAZIN-1-CARBONYL) PIPERIDIN-1-YLIPRIDIN-3-YL) 1,5 ALFA) PYRIMIDINE-3-CARBOXAMIDE AS ATR KINAZE INHIBITOR
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
US8957078B2 (en) 2013-03-15 2015-02-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
PT3077397T (pt) 2013-12-06 2020-01-22 Vertex Pharma Composto de 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]pirazolo[1,5-a]pirimidin-3-carboxamida útil como inibidor da atr quinase, a sua preparação, diferentes formas sólidas e derivados radiomarcados do mesmo
US20150158868A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
MX373102B (es) 2014-06-05 2020-04-17 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 útil como inhibidor de ataxia telangiectasia mutada y rad3 relacionado (atr) cinasa, preparación de tal compuesto y diferentes formas sólidas del mismo.
SG11201610500WA (en) 2014-06-17 2017-01-27 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors

Also Published As

Publication number Publication date
CA2950587A1 (en) 2015-12-10
AU2015271030A1 (en) 2017-01-12
CA2950587C (en) 2022-06-28
JP2019142926A (ja) 2019-08-29
IL249361A0 (en) 2017-02-28
KR102575125B1 (ko) 2023-09-07
RU2016151208A3 (2) 2018-11-14
CN110590787A (zh) 2019-12-20
NZ727649A (en) 2020-11-27
BR112016028273B1 (pt) 2022-06-28
RS60013B1 (sr) 2020-04-30
LT3152212T (lt) 2020-05-11
MX2016015874A (es) 2017-03-27
ZA201700035B (en) 2020-05-27
US20170349596A1 (en) 2017-12-07
KR20170007858A (ko) 2017-01-20
PT3152212T (pt) 2020-03-13
RU2719583C2 (ru) 2020-04-21
US10800781B2 (en) 2020-10-13
SG10201902206QA (en) 2019-04-29
WO2015187451A1 (en) 2015-12-10
RU2020110358A (ru) 2020-04-30
US10093676B2 (en) 2018-10-09
AU2015271030B2 (en) 2019-05-16
EP3152212B1 (en) 2019-12-11
US20150353560A1 (en) 2015-12-10
SG11201610197XA (en) 2017-01-27
CN107074863B (zh) 2019-12-03
NZ764151A (en) 2023-12-22
RU2016151208A (ru) 2018-07-10
NZ764150A (en) 2023-12-22
CN107074863A (zh) 2017-08-18
EP3152212A1 (en) 2017-04-12
AU2019206032A1 (en) 2019-08-01
US9670215B2 (en) 2017-06-06
DK3152212T3 (da) 2020-03-16
WO2015187451A9 (en) 2016-05-19
ES2777608T3 (es) 2020-08-05
BR112016028273A2 (pt) 2017-08-22
MX373102B (es) 2020-04-17
MX2020003458A (es) 2020-10-07
HRP20200186T1 (hr) 2020-05-29
JP6568111B2 (ja) 2019-08-28
IL249361B (en) 2020-06-30
BR112016028273A8 (pt) 2021-03-30
US20190010163A1 (en) 2019-01-10
AU2019206032B2 (en) 2021-01-28
SI3152212T1 (sl) 2020-06-30
JP2017522276A (ja) 2017-08-10
EP3152212B9 (en) 2020-05-27

Similar Documents

Publication Publication Date Title
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
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
IL277576A (en) Mutated pyrazolo[1,5-A]pyridine compounds as RET kinase inhibitors
ZA201808431B (en) Pyrazolopyrimidine derivatives as kinase inhibitor
IL265918B (en) Converted pyrazolo[1,5–a]pyridine compounds as ret kinase inhibitors
ZA201800771B (en) Substituted pyrazolo[1,5-a]pyridine compounds as ret kinase inhibitors
ZA201704494B (en) 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors
EP3172214A4 (en) 2-amino-pyrido[2,3-d]pyrimidin-7(8h)-one derivatives as cdk inhibitors and uses thereof
EP3159342A4 (en) Pyridino[1,2-a]pyrimidone analogue used as mtor/pi3k inhibitor
EP3159341B8 (en) Pyridino[1,2-a]pyrimidone analogue used as pi3k inhibitor
ZA201903286B (en) Imidazo[1,5¿a]pyrazine derivatives as pi3kdelta inhibitors
EP3196199A4 (en) Substituted n-(pyrrolidine-3-yl)-7h-pyrrolo[2,3-d]pyrimidine-4-amine as janus kinase inhibitor
IL269144A (en) Pyrrolotriazine derivatives as kinase inhibitors
HK1262447A1 (en) Pyrrolopyrimidine compounds, use as inhibitors of the kinase lrrk2, and methods for preparation thereof
HK1238236A1 (en) 4,6-substituted-pyrazolo[1,5-a]pyrazines as janus kinase inhibitors
HUE050298T2 (hu) Pirazolo[3,4-D]pirimidin vegyületek vagy annak sói