SG11201610500WA - Method for treating cancer using a combination of chk1 and atr inhibitors - Google Patents

Method for treating cancer using a combination of chk1 and atr inhibitors

Info

Publication number
SG11201610500WA
SG11201610500WA SG11201610500WA SG11201610500WA SG11201610500WA SG 11201610500W A SG11201610500W A SG 11201610500WA SG 11201610500W A SG11201610500W A SG 11201610500WA SG 11201610500W A SG11201610500W A SG 11201610500WA SG 11201610500W A SG11201610500W A SG 11201610500WA
Authority
SG
Singapore
Prior art keywords
chk1
combination
treating cancer
atr inhibitors
atr
Prior art date
Application number
SG11201610500WA
Other languages
English (en)
Inventor
Thomas Helleday
Kumar Sanjiv
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 SG11201610500WA publication Critical patent/SG11201610500WA/en

Links

Classifications

    • 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
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • 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
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
    • A61K31/33—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/495—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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
SG11201610500WA 2014-06-17 2015-06-17 Method for treating cancer using a combination of chk1 and atr inhibitors SG11201610500WA (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201462013136P 2014-06-17 2014-06-17
US201462043530P 2014-08-29 2014-08-29
US201462073082P 2014-10-31 2014-10-31
US201562161438P 2015-05-14 2015-05-14
PCT/US2015/036137 WO2015195740A1 (en) 2014-06-17 2015-06-17 Method for treating cancer using a combination of chk1 and atr inhibitors

Publications (1)

Publication Number Publication Date
SG11201610500WA true SG11201610500WA (en) 2017-01-27

Family

ID=53836805

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201610500WA SG11201610500WA (en) 2014-06-17 2015-06-17 Method for treating cancer using a combination of chk1 and atr inhibitors
SG10201811175WA SG10201811175WA (en) 2014-06-17 2015-06-17 Method for treating cancer using a combination of chk1 and atr inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
SG10201811175WA SG10201811175WA (en) 2014-06-17 2015-06-17 Method for treating cancer using a combination of chk1 and atr inhibitors

Country Status (23)

Country Link
US (2) US11179394B2 (ru)
EP (1) EP3157566B1 (ru)
JP (2) JP6936007B2 (ru)
KR (1) KR20170016498A (ru)
CN (1) CN107072987B (ru)
AU (1) AU2015277212B2 (ru)
CA (1) CA2950780C (ru)
DK (1) DK3157566T3 (ru)
ES (1) ES2733847T3 (ru)
HR (1) HRP20191375T1 (ru)
HU (1) HUE044280T2 (ru)
IL (1) IL249596B (ru)
LT (1) LT3157566T (ru)
MX (1) MX2016016115A (ru)
NZ (1) NZ727399A (ru)
PL (1) PL3157566T3 (ru)
PT (1) PT3157566T (ru)
RS (1) RS59054B1 (ru)
RU (1) RU2736219C2 (ru)
SG (2) SG11201610500WA (ru)
SI (1) SI3157566T1 (ru)
WO (1) WO2015195740A1 (ru)
ZA (1) ZA201608560B (ru)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3013000C (en) 2008-12-19 2022-12-13 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
PT2940017T (pt) 2011-09-30 2019-10-31 Vertex Pharma Processos para a produção de compostos úteis como inibidores de atr quinase
EP3733185B1 (en) 2011-09-30 2022-12-07 Vertex Pharmaceuticals Incorporated Treating non-small cell lung cancer with atr inhibitors
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
SI3808749T1 (sl) 2012-12-07 2023-07-31 Vertex Pharmaceuticals Incorporated Pirazolo(1,5-A)pirimidini za uporabo kot zaviralci ATR kinaze pri zdravljenju rakavih bolezni
WO2014143240A1 (en) 2013-03-15 2014-09-18 Vertex Pharmaceuticals Incorporated Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase
SI3077397T1 (sl) 2013-12-06 2020-02-28 Vertex Pharmaceuticals Inc. 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)pirazolo(1,5-A)pirimidin-3- karboksamidna spojina, koristna kot inhibitor kinaze ATR, njena priprava, različne trdne oblike in njeni radioaktivno označeni derivati
PL3152212T3 (pl) 2014-06-05 2020-06-15 Vertex Pharmaceuticals Inc. 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
WO2017059357A1 (en) 2015-09-30 2017-04-06 Vertex Pharmaceuticals Incorporated Method for treating cancer using a combination of dna damaging agents and atr inhibitors
AU2017205101B2 (en) * 2016-01-08 2023-05-04 Breast Cancer Now Inhibitors of ataxia-telangiectasia mutated and Rad3-related protein kinase (ATR) for use in methods of treating cancer
EP3936153A1 (en) 2016-01-11 2022-01-12 Celator Pharmaceuticals, Inc. Inhibiting ataxia telangiectasia and rad3-related protein (atr)
EA039513B1 (ru) * 2017-01-09 2022-02-04 Селатор Фармасьютикалз, Инк. Ингибитор атаксии-телеангиэкстазии и rad3-родственного белка (atr) и содержащие его липосомные композиции
RU2728870C2 (ru) * 2017-10-12 2020-07-31 Федеральное государственное бюджетное учреждение "Российский научный центр рентгенорадиологии" Министерства здравоохранения российской федерации (ФГБУ "РНЦРР" Минздрава России) Полипептиды для лечения онкологических заболеваний
CN111526889B (zh) * 2017-12-29 2023-06-02 沃泰克斯药物股份有限公司 使用atr抑制剂治疗癌症的方法
IL302529A (en) 2018-03-08 2023-07-01 Incyte Corp Aminopyrizine diol compounds as PI3K–y inhibitors
CN110241136B (zh) * 2018-03-09 2022-10-14 浙江大学 促进基因编辑的小分子化合物及其应用
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
CN110279704B (zh) * 2019-07-30 2022-08-26 南京师范大学 阿霉素联合用药物及其应用
CN111653322A (zh) * 2020-06-02 2020-09-11 重庆科技学院 一种快速发现Topo1抑制剂分子的筛选方法
WO2022228481A1 (en) * 2021-04-28 2022-11-03 Shandong University Methods for improving early embryo development
WO2023068820A1 (ko) * 2021-10-19 2023-04-27 오가노이드사이언스 주식회사 암 치료 또는 예방용 조성물

Family Cites Families (276)

* 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
HUP9801135A2 (hu) 1995-05-09 1998-08-28 Basf Aktiengesellschaft Pirazolo[1,5-a]pirimidinek, eljárás előállításukra és alkalmazásuk
CA2253910A1 (en) 1996-05-11 1997-11-20 King's College London Pyrazines
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
ATE375344T1 (de) 1996-07-24 2007-10-15 Bristol Myers Squibb Pharma Co Azolotriazine und pyrimidine
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
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
CA2291709A1 (en) 1997-05-30 1998-12-03 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2336832A1 (en) 1998-07-16 2000-01-27 Shionogi & Co., Ltd. Pyrimidine derivatives exhibiting antitumor activity
EP1140936B1 (en) 1999-01-11 2004-03-17 Agouron Pharmaceuticals, Inc. Tricyclic inhibitors of poly(adp-ribose) polymerases
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
WO2001044206A1 (en) 1999-12-17 2001-06-21 Chiron Corporation Pyrazine based inhibitors of glycogen synthase kinase 3
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
US20030028018A1 (en) 2000-09-11 2003-02-06 Chiron Coporation Quinolinone derivatives
CA2421120C (en) 2000-09-11 2008-07-15 Chiron Corporation Quinolinone derivatives as tyrosine kinase inhibitors
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
WO2002089738A2 (en) 2001-05-08 2002-11-14 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
AU2003215087B2 (en) 2002-02-06 2009-07-16 Vertex Pharmaceuticals Incorporated Heteroaryl compounds useful as inhibitors of GSK-3
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
CA2484209C (en) 2002-05-03 2013-06-11 Exelixis, Inc. Protein kinase modulators and methods of use
KR20050004214A (ko) 2002-05-31 2005-01-12 에자이 가부시키가이샤 피라졸 화합물 및 이것을 포함하여 이루어지는 의약 조성물
WO2003101993A1 (en) 2002-06-04 2003-12-11 Neogenesis Pharmaceuticals, Inc. Pyrazolo` 1,5a! pyrimidine compounds as antiviral agents
US7449488B2 (en) 2002-06-04 2008-11-11 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl 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
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
EP1537116B1 (en) 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
EP1534709B1 (en) 2002-09-04 2007-06-13 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines 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
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
AR041136A1 (es) 2002-09-04 2005-05-04 Pharmacopeia Drug Discovery Pirazolopirimidinas como inhibidores de cinasas dependientes de clclinas
WO2004026229A2 (en) 2002-09-04 2004-04-01 Schering Corporation Pyrazolo[1,5-a]pyrimidines compounds as cyclin dependent kinase inhibitors
AU2003282679A1 (en) 2002-10-04 2004-05-04 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
AU2003299651A1 (en) 2002-12-11 2004-06-30 Merck And Co., Inc. 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
PL378372A1 (pl) 2003-01-09 2006-04-03 Pfizer Inc. Tricykliczne związki jako inhibitory kinaz białkowych do wzmacniania skuteczności środków przeciwnowotworowych i radioterapii
PT1603570E (pt) 2003-02-26 2013-03-26 Sugen Inc Compostos de aminoheteroarilo como inibidores da proteína quinase
EP1599482A4 (en) 2003-02-28 2008-10-01 Teijin Pharma Ltd PYRAZOLO1,5-A PYRIMIDINE DERIVATIVES
WO2004080982A1 (en) 2003-03-11 2004-09-23 Pfizer Products Inc. Pyrazine compounds as transforming growth factor (tgf) inhibitors
US7449464B2 (en) 2003-03-12 2008-11-11 Kudos Pharmaceuticals Limited Phthalazinone derivatives
JP2006520794A (ja) 2003-03-21 2006-09-14 スミスクライン ビーチャム コーポレーション 化合物
AU2004224392A1 (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
EP1625123A4 (en) 2003-05-15 2007-08-29 Merck & Co Inc 3- (2-AMINO-1-AZACYCLYL) -5-ARYL-1,2,4-OXADIAZOLE AS S1P RECEPTOR AGONISTS
TWI339206B (en) 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
KR20060070572A (ko) 2003-09-18 2006-06-23 콘포마 세러퓨틱스 코포레이션 Ｈｓｐ90-저해제로서의 신규 헤테로시클릭 화합물
WO2005034952A2 (en) 2003-10-07 2005-04-21 The Feinstein Institute For Medical Research Isoxazole and isothiazole compounds useful in the treatment of inflammation
PL1689387T3 (pl) 2003-11-19 2012-02-29 Array Biopharma Inc Bicykliczne inhibitory MEK i sposoby ich otrzymywania
DK1684736T3 (da) 2003-12-01 2011-11-21 Kudos Pharm Ltd Inhibitorer af DNA-skadereparation til behandling af cancer
DE10356579A1 (de) 2003-12-04 2005-07-07 Merck Patent Gmbh Aminderivate
AU2004312193B2 (en) 2004-01-05 2008-09-25 Astrazeneca Ab Thiophene derivatives as CHK 1 inihibitors
EP1715867A4 (en) 2004-02-12 2009-04-15 Merck & Co Inc BIPYRIDYL AMIDES AS MODULATORS OF GLUTAMATE METABOTROPIC REPEATER-5
EP1720879A2 (de) 2004-02-25 2006-11-15 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
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
SG156685A1 (en) 2004-07-27 2009-11-26 Sgx Pharmaceuticals Inc Fused ring heterocycle kinase modulators
KR20070090172A (ko) 2004-11-04 2007-09-05 버텍스 파마슈티칼스 인코포레이티드 단백질 키나아제의 억제제로서 유용한피라졸로[1,5-ａ]피리미딘
WO2006053342A2 (en) 2004-11-12 2006-05-18 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
US20080269249A2 (en) 2004-12-27 2008-10-30 Alcon, Inc. Aminopyrazine analogs for treating glaucoma and other 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
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
US8093244B2 (en) 2005-03-29 2012-01-10 Icos Corporation Heteroaryl urea derivatives useful for inhibiting CHK1
TWI375673B (en) 2005-04-11 2012-11-01 Abbott Lab 1h-benzimidazole-4-carboxamides substituted with a quaternary carbon at the 2-position are potent parp inhibitors
EP1874769B1 (de) 2005-04-25 2011-09-14 Merck Patent GmbH Neuartige aza-heterozyklen als kinase-inhibitoren
US20060293345A1 (en) 2005-05-20 2006-12-28 Christoph Steeneck 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
EP1931675B1 (en) 2005-10-06 2015-01-14 Merck Sharp & Dohme Corp. Pyrazolo(1, 5a) pyrimidines as protein kinase inhibitors
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
EP1931676B1 (en) 2005-10-06 2011-11-16 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
TWI421078B (zh) 2005-10-06 2014-01-01 Merck Sharp & Dohme 關卡激酶抑制劑及其用途
EP1945220A1 (en) 2005-10-21 2008-07-23 Mitsubishi Tanabe Pharma Corporation Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists
WO2007048065A2 (en) 2005-10-21 2007-04-26 Exelixis, Inc. Pyrimidinones as casein kinase ii (ck2) modulators
TW200736260A (en) 2005-11-10 2007-10-01 Smithkline Beecham Corp Inhibitors of Akt activity
JP4855478B2 (ja) 2005-12-01 2012-01-18 エフ．ホフマン−ラ ロシュ アーゲー Ｌ−ｃｐｔ１阻害剤としてのヘテロアリール置換されたピペリジン誘導体
JP5064237B2 (ja) 2005-12-09 2012-10-31 Ｍｅｉｊｉ Ｓｅｉｋａファルマ株式会社 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
BRPI0620463A2 (pt) 2005-12-22 2011-11-16 Alcon Res Ltd composição farmacêutica oftálmica, compostos, e seus usos
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
US7872031B2 (en) 2006-03-22 2011-01-18 Vertex Pharmaceuticals Incorporated c-MET protein kinase inhibitors
JP2009531443A (ja) 2006-03-29 2009-09-03 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド α−シヌクレイン毒性の抑制
US7700601B2 (en) 2006-03-31 2010-04-20 Schering Corporation Substituted indazoles of formula 1.0 that are kinase inhibitors
WO2007139732A1 (en) 2006-05-22 2007-12-06 Schering Corporation Pyrazolo [1, 5-a] pyrimidines as cdk inhibitors
AU2007263017A1 (en) 2006-06-22 2007-12-27 Biovitrum Ab (Publ) Pyridine and pyrazine derivatives as MNK kinase inhibitors
JP2009541323A (ja) 2006-06-22 2009-11-26 マリンクロット インコーポレイテッド 拡張された共役を有するピラジン誘導体およびその使用
AR061793A1 (es) 2006-07-05 2008-09-24 Mitsubishi Tanabe Pharma Corp Compuesto de pirazolo[1,5-a] pirimidina y composicion farmaceutica
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20121506A1 (es) 2006-07-14 2012-11-26 Amgen Inc Compuestos triazolopiridinas como inhibidores de c-met
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
EP2081933B1 (en) 2006-09-29 2011-03-23 Novartis AG Pyrazolopyrimidines as pi3k 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
UY30639A1 (es) 2006-10-17 2008-05-31 Kudos Pharm Ltd Derivados sustituidos de 2h-ftalazin-1-ona, sus formas cristalinas, proceso de preparacion y aplicaciones
BRPI0717767A2 (pt) 2006-10-19 2013-11-12 Signal Pharm Llc Composto, composição farmacêutica, e, métodos para tratar ou prevenir câncer, uma condição inflamatória, uma condição imunológica ou uma condição metabólica, e para inibir uma quinase em uma célula de expressa a dita quinase
WO2008060907A2 (en) 2006-11-10 2008-05-22 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
AU2007321924A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
CA2672367A1 (en) 2006-12-15 2008-06-19 Bayer Schering Pharma Aktiengesellschaft 3-h-pyrazolopyridines and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
WO2008079291A2 (en) 2006-12-20 2008-07-03 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
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
WO2008084261A1 (en) 2007-01-10 2008-07-17 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Amide substituted indazoles as poly(adp-ribose)polymerase (parp) inhibitors
EP2114898A2 (en) 2007-02-16 2009-11-11 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
BRPI0808523A2 (pt) 2007-03-01 2014-08-19 Novartis Vaccines & Diagnostic Inibidores de pim cinase e métodos de seu uso
JP5548119B2 (ja) 2007-04-10 2014-07-16 バイエル・クロップサイエンス・アーゲー 殺虫性アリールイソオキサゾリン誘導体
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
US20100190980A1 (en) 2007-06-21 2010-07-29 Taisho Pharmaceutical Co., Ltd Pyrazinamide compound
KR20100037047A (ko) 2007-06-26 2010-04-08 렉시컨 파마슈티컬스 인코퍼레이티드 세로토닌-매개 질환 및 장애의 치료 방법
US20090012103A1 (en) 2007-07-05 2009-01-08 Matthew Abelman Substituted heterocyclic compounds
WO2009006580A1 (en) 2007-07-05 2009-01-08 Cv Therapeutics, Inc. Optionally condensed dihydropyridine, dihydropyrimidine and dihydropyrane derivatives acting as late sodium channel blockers
GB0713259D0 (en) 2007-07-09 2007-08-15 Astrazeneca Ab Pyrazine derivatives 954
UA105758C2 (ru) 2007-07-19 2014-06-25 Х. Луннбек А/С 5-членные гетероциклические амиды и родственные соединения
CN101801958B (zh) 2007-07-19 2014-01-29 默沙东公司 作为蛋白质激酶抑制剂的杂环酰胺化合物
WO2009016460A2 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
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
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.
US8436185B2 (en) 2008-01-08 2013-05-07 Merck Sharp & Dohme Corp. Pharmaceutically acceptable salts of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
EP2247592B1 (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
PL2250172T3 (pl) 2008-02-25 2012-01-31 Hoffmann La Roche Pirolopirazynowe inhibitory kinazy
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
BRPI0911808A2 (pt) 2008-04-28 2016-10-18 Astrazeneca Ab método para preparar um composto, e, composição
WO2009152087A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor
CN102124009B (zh) 2008-07-08 2014-07-23 因特利凯公司 激酶抑制剂及其使用方法
WO2010017047A1 (en) 2008-08-05 2010-02-11 Merck & Co., Inc. Therapeutic compounds
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
EP2767537B1 (en) 2008-08-06 2017-04-12 Medivation Technologies, Inc. Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
ES2710701T3 (es) 2008-09-24 2019-04-26 Basf Se Compuestos de pirazol para el control de plagas de invertebrados
WO2010048131A1 (en) 2008-10-21 2010-04-29 Vertex Pharmaceuticals Incorporated C-met protein kinase inhibitors
CA2740792C (en) 2008-10-31 2016-06-21 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
CN102264743B (zh) 2008-11-25 2015-02-11 罗彻斯特大学 Mlk抑制剂及其使用方法
SG171956A1 (en) 2008-12-05 2011-07-28 Hoffmann La Roche Pyrrolopyrazinyl urea kinase inhibitors
CA3013000C (en) 2008-12-19 2022-12-13 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of atr kinase
TW201028410A (en) 2008-12-22 2010-08-01 Astrazeneca Ab Chemical compounds 610
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
MX2011008059A (es) 2009-01-30 2011-10-11 Toyama Chemical Co Ltd Derivado del acido n-acil antranilico o sal del mismo.
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
KR20110132564A (ko) 2009-02-11 2011-12-08 선오비온 파마슈티컬스 인코포레이티드 히스타민 ｈ3 역 작용제 및 길항제, 및 이의 사용 방법
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
AR077468A1 (es) 2009-07-09 2011-08-31 Array Biopharma Inc Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa
WO2011008830A1 (en) 2009-07-15 2011-01-20 Abbott Laboratories Pyrrolopyrazine inhibitors of kinases
AU2010284254B2 (en) 2009-08-17 2015-09-17 Intellikine, Llc Heterocyclic compounds and uses thereof
EP2470183B1 (en) 2009-08-26 2015-09-16 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
AU2010326268B2 (en) 2009-12-04 2016-11-03 Senhwa Biosciences, Inc. Pyrazolopyrimidines and related heterocycles as CK2 inhibitors
KR101732212B1 (ko) 2010-03-18 2017-05-02 재단법인 한국파스퇴르연구소 항감염성 화합물
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
JP2013529200A (ja) 2010-05-12 2013-07-18 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
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
JP2013526539A (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ピラジン
AU2011253021A1 (en) 2010-05-12 2012-11-29 Vertex Pharmaceuticals Incorporated 2 -aminopyridine derivatives useful as inhibitors of ATR kinase
WO2011143425A2 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2569313A1 (en) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
JP2013529204A (ja) 2010-05-20 2013-07-18 エフ．ホフマン−ラ ロシュ アーゲー ピロロ［２，３−ｂ］ピラジン−７−カルボキサミド誘導体とＪＡＫ及びＳＹＫ及び阻害剤としてのそれらの使用
KR20130083387A (ko) 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 Syk 및 jak 억제제로서 피롤로피라진 유도체
SA111320519B1 (ar) 2010-06-11 2014-07-02 Astrazeneca Ab مركبات بيريميدينيل للاستخدام كمثبطات atr
CA2803802A1 (en) 2010-06-23 2011-12-29 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
AU2011270798B2 (en) 2010-06-24 2015-03-19 Gilead Sciences, Inc. Pyrazolo [1, 5 -a] pyrimidines 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
WO2012007375A1 (en) 2010-07-13 2012-01-19 F. Hoffmann-La Roche Ag Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators
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
EP2640386B1 (en) * 2010-11-16 2017-01-18 Array Biopharma Inc. Combination of checkpoint kinase 1 inhibitors and wee 1 kinase inhibitors
RS63320B1 (sr) 2010-12-08 2022-07-29 The U S A As Represented By The Secretary Department Of Health And Human Services Supstituisani pirazolopirimidini kao aktivatori glukocerebrozidaze
WO2012100342A1 (en) 2011-01-27 2012-08-02 Université de Montréal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
EP2694498B1 (en) 2011-04-05 2016-03-30 Vertex Pharmaceuticals Incorporated Aminopyrazine compounds useful as inhibitors of tra kinase
ES2583086T3 (es) 2011-04-21 2016-09-19 Bayer Intellectual Property Gmbh Pirazolopiridinas sustituidas con fluoroalquilo y su uso
KR20140093610A (ko) 2011-04-21 2014-07-28 재단법인 한국파스퇴르연구소 소염 화합물
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
CN103764166B (zh) 2011-06-22 2017-10-24 通用医疗公司 蛋白质病的治疗
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US8822469B2 (en) 2011-06-22 2014-09-02 Vertex Pharmaceuticals Incorporated Pyrrolo[2,3-B]pyrazines useful as inhibitors of ATR kinase
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
US9138436B2 (en) 2011-07-13 2015-09-22 Pharmacyclics Llc Inhibitors of Bruton's tyrosine kinase
WO2013052263A2 (en) 2011-09-16 2013-04-11 Microbiotix, Inc. Antifungal compounds
EP2751088B1 (en) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2751099B1 (en) 2011-09-30 2017-06-14 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
EP3733185B1 (en) 2011-09-30 2022-12-07 Vertex Pharmaceuticals Incorporated Treating non-small cell lung cancer with atr inhibitors
PT2940017T (pt) 2011-09-30 2019-10-31 Vertex Pharma Processos para a produção de compostos úteis como inibidores de atr quinase
BR112014009531A8 (pt) 2011-10-20 2018-01-16 Glaxosmithkline Llc aza-heterociclos bicíclicos substituídos e análogos como moduladores de sirtuína
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine 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
WO2013071094A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US8846917B2 (en) 2011-11-09 2014-09-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2013096687A1 (en) * 2011-12-22 2013-06-27 Threshold Pharmaceuticals, Inc. Administration of hypoxia activated prodrugs in combination with chk1 inhibitors for treating cancer
US9193725B2 (en) 2012-03-14 2015-11-24 Bristol-Meyers Squibb Company Cyclic hydrazine derivatives as HIV attachment inhibitors
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
CA2868507A1 (en) 2012-04-02 2013-10-10 Cytokinetics, Inc. Methods for improving diaphragm function
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
CN106279142B (zh) 2012-05-15 2019-05-03 癌症研究技术有限公司 5-[[4-[[吗啉-2-基]甲基氨基]-5-(三氟甲基)-2-吡啶基]氨基]吡嗪-2-腈及其治疗应用
US9434745B2 (en) 2012-05-23 2016-09-06 Savira Pharmaceuticals Gmbh 7-oxo-thiazolopyridine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
BR112014029006A2 (pt) 2012-05-23 2017-06-27 European Molecular Biology Laboratory derivados de 7-oxo-4,7-di-hidro-pirazolo[1,5-a]pirimidina que são úteis no tratamento, melhora ou prevenção de uma doença viral
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
WO2014023691A1 (en) 2012-08-06 2014-02-13 Savira Pharmaceuticals Gmbh Dihydroxypyrimidine carbonic acid derivatives and their use in the treatment, amelioration or prevention of a viral disease
WO2014025854A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Piperidine amide derivatives as hiv attachment inhibitors
WO2014025852A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Tricyclic alkene derivatives as hiv attachment inhibitors
EP2895475B1 (en) 2012-08-09 2016-11-09 VIIV Healthcare UK (No.5) Limited Tricyclic amidine derivatives as hiv attachment inhibitors
CN104718206B (zh) 2012-08-17 2017-03-08 拜尔农作物科学股份公司 作为杀虫剂和杀螨剂的氮杂吲哚甲酰胺和氮杂吲哚硫代甲酰胺
CN104583197B (zh) 2012-08-24 2017-05-17 霍夫曼-拉罗奇有限公司 新型双环吡啶衍生物
WO2014035140A2 (en) 2012-08-30 2014-03-06 Kainos Medicine, Inc. Compounds and compositions for modulating histone methyltransferase activity
WO2014039831A1 (en) 2012-09-07 2014-03-13 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
JP6465803B2 (ja) 2012-10-22 2019-02-06 シティ・オブ・ホープＣｉｔｙ ｏｆ Ｈｏｐｅ Ｅｔｐ誘導体
EP2912464B1 (en) 2012-10-24 2017-04-26 Becton Dickinson and Company Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same
SI3808749T1 (sl) 2012-12-07 2023-07-31 Vertex Pharmaceuticals Incorporated Pirazolo(1,5-A)pirimidini za uporabo kot zaviralci ATR kinaze pri zdravljenju rakavih bolezni
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. 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
US8969360B2 (en) 2013-03-15 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
SI3077397T1 (sl) 2013-12-06 2020-02-28 Vertex Pharmaceuticals Inc. 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)pirazolo(1,5-A)pirimidin-3- karboksamidna spojina, koristna kot inhibitor kinaze ATR, njena priprava, različne trdne oblike in njeni radioaktivno označeni derivati
US20150158868A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
PL3152212T3 (pl) 2014-06-05 2020-06-15 Vertex Pharmaceuticals Inc. 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

Also Published As

Publication number Publication date
RU2017101189A (ru) 2018-07-25
EP3157566B1 (en) 2019-05-01
CA2950780A1 (en) 2015-12-23
US20150359797A1 (en) 2015-12-17
RS59054B1 (sr) 2019-08-30
AU2015277212B2 (en) 2020-07-02
NZ727399A (en) 2022-07-29
BR112016029523A2 (pt) 2017-08-22
PT3157566T (pt) 2019-07-11
CN107072987A (zh) 2017-08-18
EP3157566A1 (en) 2017-04-26
WO2015195740A1 (en) 2015-12-23
US11179394B2 (en) 2021-11-23
MX2016016115A (es) 2017-03-08
ZA201608560B (en) 2020-05-27
SG10201811175WA (en) 2019-01-30
LT3157566T (lt) 2019-08-12
US20220249489A1 (en) 2022-08-11
AU2015277212A1 (en) 2017-01-12
HUE044280T2 (hu) 2019-10-28
ES2733847T3 (es) 2019-12-03
CN107072987B (zh) 2020-02-07
RU2736219C2 (ru) 2020-11-12
PL3157566T3 (pl) 2019-10-31
JP2017524673A (ja) 2017-08-31
SI3157566T1 (sl) 2019-08-30
DK3157566T3 (da) 2019-07-22
CA2950780C (en) 2023-05-16
IL249596B (en) 2021-05-31
JP6936007B2 (ja) 2021-09-15
BR112016029523A8 (pt) 2021-07-20
HRP20191375T1 (hr) 2019-11-01
JP2020019815A (ja) 2020-02-06
IL249596A0 (en) 2017-02-28
KR20170016498A (ko) 2017-02-13
RU2017101189A3 (ru) 2019-02-06

Similar Documents

Publication Publication Date Title
ZA201608560B (en) Method for treating cancer using a combination of chk1 and atr inhibitors
IL249658A0 (en) Methods of treating cancer using tigit inhibitors and anticancer agents
HK1232153A1 (zh) 用於治療癌症的 拮抗劑和 抑制劑的組合
HK1258570A1 (zh) 使用dna損傷劑及atr抑制劑的組合治療癌症的方法
IL304252A (en) Cancer treatment methods
IL246760A0 (en) Combination of pd-1 antagonist and vegfr inhibitor for cancer treatment
IL289947A (en) A method for treating cancer
HK1249469A1 (zh) 用RORγ抑制劑治療癌症的方法
SG11201607130RA (en) Combination method for treatment of cancer
IL266182A (en) Farensyltransferase inhibitors for use in cancer treatment methods
HK1243407A1 (zh) Ripk2抑制劑及用其治療癌症的方法
IL268722A (en) Methods of treating cancer with farnesyl-transferase inhibitors
IL272473A (en) Methods of treating cancer with farnesyltransferase inhibitors
GB201510197D0 (en) Method of treating ovarian cancer
GB201418640D0 (en) Agents and methods for treatment of cancer