MX378277B - Metodo para tratar cancer usando una combinacion de inhibidores de chk1 y relacionado con atm y rad3 (atr). - Google Patents

Metodo para tratar cancer usando una combinacion de inhibidores de chk1 y relacionado con atm y rad3 (atr).

Info

Publication number
MX378277B
MX378277B MX2016016115A MX2016016115A MX378277B MX 378277 B MX378277 B MX 378277B MX 2016016115 A MX2016016115 A MX 2016016115A MX 2016016115 A MX2016016115 A MX 2016016115A MX 378277 B MX378277 B MX 378277B
Authority
MX
Mexico
Prior art keywords
treating cancer
administering
inhibitor
atr
protein kinase
Prior art date
Application number
MX2016016115A
Other languages
English (en)
Other versions
MX2016016115A (es
Inventor
Kumar Sanjiv
Thomas Helleday
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 MX2016016115A publication Critical patent/MX2016016115A/es
Publication of MX378277B publication Critical patent/MX378277B/es

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
    • A61K31/435—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

La presente invención se refiere a métodos para tratar cáncer en un paciente mediante la administración de un compuesto útil como inhibidor de proteína cinasa ATR en combinación con un compuesto útil como inhibidor de proteína cinasa Chk1. La combinación mencionada anteriormente muestra un efecto sinérgico sorprendente en el tratamiento del cáncer a pesar de que las proteína cinasas seleccionadas están dentro de la misma vía biológica. Además, la presente invención se refiere también a métodos para tratar el cáncer mediante la administración de un compuesto útil como inhibidor de proteína cinasa ATR; administrar un compuesto útil como inhibidor de proteína cinasa Chk1; así como la administración de un agente dañino de ADN a un paciente. Los compuestos usados en esta invención están representados por la fórmula (I) y la fórmula (II): (ver Fórmulas) en donde las variables son como se definen en la presente.
MX2016016115A 2014-06-17 2015-06-17 Metodo para tratar cancer usando una combinacion de inhibidores de chk1 y relacionado con atm y rad3 (atr). MX378277B (es)

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 (2)

Publication Number Publication Date
MX2016016115A MX2016016115A (es) 2017-03-08
MX378277B true MX378277B (es) 2025-03-10

Family

ID=53836805

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016016115A MX378277B (es) 2014-06-17 2015-06-17 Metodo para tratar cancer usando una combinacion de inhibidores de chk1 y relacionado con atm y rad3 (atr).

Country Status (23)

Country Link
US (2) US11179394B2 (es)
EP (1) EP3157566B1 (es)
JP (2) JP6936007B2 (es)
KR (1) KR20170016498A (es)
CN (1) CN107072987B (es)
AU (1) AU2015277212B2 (es)
CA (1) CA2950780C (es)
DK (1) DK3157566T3 (es)
ES (1) ES2733847T3 (es)
HR (1) HRP20191375T1 (es)
HU (1) HUE044280T2 (es)
IL (1) IL249596B (es)
LT (1) LT3157566T (es)
MX (1) MX378277B (es)
NZ (1) NZ727399A (es)
PL (1) PL3157566T3 (es)
PT (1) PT3157566T (es)
RS (1) RS59054B1 (es)
RU (1) RU2736219C2 (es)
SG (2) SG11201610500WA (es)
SI (1) SI3157566T1 (es)
WO (1) WO2015195740A1 (es)
ZA (1) ZA201608560B (es)

Families Citing this family (23)

* 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
EP3878851A1 (en) 2011-09-30 2021-09-15 Vertex Pharmaceuticals Incorporated Process for making compounds useful as inhibitors of atr kinase
RU2018108589A (ru) 2011-09-30 2019-02-25 Вертекс Фармасьютикалз Инкорпорейтед Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr
PT2833973T (pt) 2012-04-05 2017-12-21 Vertex Pharma Compostos úteis como inibidores da cinase atr e terapias de combinação dos mesmos
WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
WO2015085132A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated 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
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici
EP3355926B1 (en) 2015-09-30 2025-12-24 Vertex Pharmaceuticals Inc. Combination of dna damaging agents and atr inhibitors for use in a method for treating cancer using
IL260469B2 (en) * 2016-01-08 2025-10-01 The Institute Of Cancer Res Royal Cancer Hospital Inhibitors of ataxia telangiectasia and rad3-related protein kinase (atr) mutations for use in cancer treatment methods
ES2997263T3 (en) 2016-01-11 2025-02-14 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
EP3732301A4 (en) * 2017-12-29 2022-02-09 Vertex Pharmaceuticals Incorporated METHOD OF TREATMENT OF CANCER USING AN ATR INHIBITOR
TWI903299B (zh) 2018-03-08 2025-11-01 美商英塞特公司 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物
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
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
EP3866785A1 (en) * 2018-10-15 2021-08-25 Merck Patent GmbH Combination therapy utilizing dna alkylating agents and atr 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
EP4330376A4 (en) * 2021-04-28 2025-04-09 Shandong University METHODS TO IMPROVE EARLY EMBRYO DEVELOPMENT
KR20230055998A (ko) * 2021-10-19 2023-04-26 오가노이드사이언스 주식회사 암 치료 또는 예방용 조성물
CN119661557A (zh) * 2023-12-15 2025-03-21 上海瑛派药业有限公司 作为激酶抑制剂的二取代含氮五元杂芳基化合物及其应用

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
DE59608203D1 (de) 1995-05-09 2001-12-20 Basf Ag PYRAZOLO- 1,5a]-PYRIMIDINE, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG
WO1997043267A1 (en) 1996-05-11 1997-11-20 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
US6191131B1 (en) 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company Azolo triazines and pyrimidines
US6060478A (en) 1996-07-24 2000-05-09 Dupont Pharmaceuticals Azolo triazines and pyrimidines
JPH10218881A (ja) 1997-02-03 1998-08-18 Pola Chem Ind Inc 新規なピロロピラゾロピリミジン誘導体
JP2002241379A (ja) 1997-03-21 2002-08-28 Dainippon Pharmaceut Co Ltd ３−オキサジアゾリルキノキサリン誘導体
US6235741B1 (en) 1997-05-30 2001-05-22 Merck & Co., Inc. Angiogenesis inhibitors
AU734009B2 (en) 1997-05-30 2001-05-31 Merck & Co., Inc. Novel angiogenesis inhibitors
CA2336832A1 (en) 1998-07-16 2000-01-27 Shionogi & Co., Ltd. Pyrimidine derivatives exhibiting antitumor activity
HRP20010573B1 (en) 1999-01-11 2006-04-30 Agouron Pharmaceuticals 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
CN1272328C (zh) 1999-12-17 2006-08-30 希龙公司 糖元合成酶激酶3的基于吡嗪的抑制剂
US6723332B2 (en) 2000-05-26 2004-04-20 Neurogen Corporation Oxomidazopyridine-carboxamides
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
PL211125B1 (pl) 2000-09-11 2012-04-30 Novartis Vaccines & Diagnostic Pochodne chinolinonu jako inhibitory kinazy tyrozynowej, kompozycje je zawierające i ich zastosowanie
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
EP1463742A4 (en) 2001-06-21 2006-05-10 Ariad Pharma Inc NEW PYRAZOLO AND PYRROLO PYRIMIDINES AND THEIR USES
SE0102438D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102439D0 (sv) 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
WO2003037900A2 (en) 2001-11-01 2003-05-08 Icagen, Inc. Pyrazolopyrimidines
AU2002343557A1 (en) 2001-11-21 2003-06-10 Pharmacia And Upjohn Company Substituted aryl 1,4-pyrazine derivatives
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
KR20040084896A (ko) 2002-02-06 2004-10-06 버텍스 파마슈티칼스 인코포레이티드 Ｇｓｋ-3의 억제제로서 유용한 헤테로아릴 화합물
MXPA04007775A (es) 2002-03-13 2004-10-15 Janssen Pharmaceutica Nv Derivados de sulfonilo como novedosos inhibidores de la histona desacetilasa.
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
JP4901102B2 (ja) 2002-05-03 2012-03-21 エクセリクシス， インク． プロテインキナーゼモジュレーターおよびその使用方法
US7704995B2 (en) 2002-05-03 2010-04-27 Exelixis, Inc. Protein kinase modulators and methods of use
CN1656079A (zh) 2002-05-31 2005-08-17 卫材株式会社 吡唑化合物和含有该化合物的药物组合物
AU2003240488A1 (en) 2002-06-04 2003-12-19 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
US7015227B2 (en) 2002-06-21 2006-03-21 Cgi Pharmaceuticals, Inc. Certain amino-substituted monocycles as kinase modulators
US8580782B2 (en) 2002-09-04 2013-11-12 Merck Sharp & Dohme Corp. Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
WO2004022559A1 (en) 2002-09-04 2004-03-18 Schering Corporation Pyrazolopyrimidines as cyclin dependent kinase inhibitors
TWI335919B (en) 2002-09-04 2011-01-11 Schering Corp Novel pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7563798B2 (en) 2002-09-04 2009-07-21 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
CN1701073B (zh) 2002-09-04 2011-06-22 先灵公司 作为细胞周期蛋白依赖激酶抑制剂的吡唑并[1,5-a]嘧啶
US7196092B2 (en) 2002-09-04 2007-03-27 Schering Corporation N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors
US7119200B2 (en) 2002-09-04 2006-10-10 Schering Corporation 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
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines 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
EP1537116B1 (en) 2002-09-04 2010-06-02 Schering Corporation Pyrazolopyrimidines suitable for the treatment of cancer diseases
US7196078B2 (en) 2002-09-04 2007-03-27 Schering Corpoartion Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors
AU2003282679A1 (en) 2002-10-04 2004-05-04 Arena Pharmaceuticals, Inc. Hydroxypyrazoles for use against metabolic-related disorders
WO2004052315A2 (en) 2002-12-11 2004-06-24 Merck & Co., Inc. Tyrosine kinase inhibitors
SE0203754D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203752D0 (sv) 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
DK1585749T3 (da) 2003-01-09 2008-09-22 Pfizer Diazepinoindol-derivater som kinaseinhibitorer
GEP20084341B (en) 2003-02-26 2008-03-25 Sugen Inc Aminoheteroaryl compounds as protein kinase inhibitors
EP1599482A4 (en) 2003-02-28 2008-10-01 Teijin Pharma Ltd PYRAZOLO1,5-A PYRIMIDINE DERIVATIVES
JP2006519833A (ja) 2003-03-11 2006-08-31 ファイザー・プロダクツ・インク トランスフォーミング成長因子（ｔｇｆ）阻害剤としてのピラジン化合物
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
US20060293339A1 (en) 2003-03-24 2006-12-28 Chakravarty Prasun K Biaryl substituted 6-membered heterocycles as sodium channel blockers
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
JP2006528980A (ja) 2003-05-15 2006-12-28 メルク　エンド　カムパニー　インコーポレーテッド Ｓ１ｐ受容体作働薬としての３−（２−アミノ−１−アザシクロ）−５−アリール−１，２，４−オキサジアゾール類
AR045595A1 (es) 2003-09-04 2005-11-02 Vertex Pharma Composiciones utiles como inhibidores de proteinas quinasas
EP2145888A1 (en) 2003-09-18 2010-01-20 Conforma Therapeutics Corporation Deazapurine derivatives as HSP90-Inhibitors
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
WO2005053662A1 (en) 2003-12-01 2005-06-16 Kudos Pharmaceuticals Limited Dna damage repair inhibitors for treatment of cancer
DE10356579A1 (de) 2003-12-04 2005-07-07 Merck Patent Gmbh Aminderivate
MXPA06007692A (es) 2004-01-05 2007-01-26 Astrazeneca Ab Heterociclos sustituidos y usos de los mismos.
JP2007524682A (ja) 2004-02-12 2007-08-30 メルク　エンド　カムパニー　インコーポレーテッド 代謝調節型グルタミン酸受容体−５の調節物質としてのビピリジルアミド
EP1720879A2 (de) 2004-02-25 2006-11-15 Basf Aktiengesellschaft Azolopyrimidin-verbindungen und ihre verwendung zur bekämpfung von schadpilzen
JP5213229B2 (ja) 2004-04-23 2013-06-19 エグゼリクシス， インコーポレイテッド キナーゼ調節因子および使用方法
WO2005123672A2 (en) 2004-06-14 2005-12-29 Takeda San Diego, Inc. Kinase inhibitors
BRPI0513899A (pt) 2004-07-27 2008-05-20 Sgx Pharmaceuticals Inc moduladores de cinase heterocìclica de anel fundido
US7626021B2 (en) 2004-07-27 2009-12-01 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
EP1812440B1 (en) 2004-11-04 2010-09-22 Vertex Pharmaceuticals, Inc. Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
US8003806B2 (en) 2004-11-12 2011-08-23 OSI Pharmaceuticals, LLC Integrin antagonists useful as anticancer agents
EP1814883A1 (en) 2004-11-22 2007-08-08 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
GB0428235D0 (en) 2004-12-23 2005-01-26 Glaxo Group Ltd Novel compounds
ATE519488T1 (de) 2004-12-27 2011-08-15 Novartis Ag Aminopyrazin-analoga zur behandlung von glaukomen und anderen durch rho-kinase verursachten krankheiten
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
WO2006088837A2 (en) 2005-02-16 2006-08-24 Schering Corporation Heterocyclic substituted piperazines with cxcr3 antagonist activity
DE102005007534A1 (de) 2005-02-17 2006-08-31 Bayer Cropscience Ag Pyrazolopyrimidine
WO2006105262A1 (en) 2005-03-29 2006-10-05 Icos Corporation HETEROARYL UREA DERIVATIVES USEFUL FOR INHIBITING CHKl
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
WO2006114180A1 (de) 2005-04-25 2006-11-02 Merck Patent Gmbh Neuartige aza-heterozyklen als kinase-inhibitoren
EA013525B1 (ru) 2005-05-20 2010-06-30 Алантос-Фармасьютикалз Холдинг, Инк. Гетеробициклические ингибиторы металлопротеазы и их применение
US20070155737A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
US20070155738A1 (en) 2005-05-20 2007-07-05 Alantos Pharmaceuticals, Inc. Heterobicyclic metalloprotease inhibitors
WO2007015632A1 (en) 2005-08-04 2007-02-08 Cgk Co., Ltd. Atm and atr inhibitor
US7776865B2 (en) 2005-10-06 2010-08-17 Schering Corporation Substituted pyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
AR057979A1 (es) 2005-10-06 2008-01-09 Schering Corp PIRAZOLPIRIMIDINAS COMO INHIBIDORAS DE PROTEíNA QUINASA. COMPOSICIONES FARMACEUTICAS.
CN101360499B (zh) 2005-10-06 2015-10-07 默沙东公司 吡唑并[1,5-a]嘧啶衍生物在制备抑制蛋白激酶的药物中的用途
WO2007044426A2 (en) 2005-10-06 2007-04-19 Schering Corporation Pyrazolopyrimidines as protein kinase inhibitors
EP1945220A1 (en) 2005-10-21 2008-07-23 Mitsubishi Tanabe Pharma Corporation Pyrazolo[1,5-a]pyrimidine compounds as cannabinoid receptor antagonists
JP5119157B2 (ja) 2005-10-21 2013-01-16 エクセリクシス， インク． カゼインキナーゼｉｉ（ｃｋ２）モジュレーターとしてのピラゾロ−ピリミジン類
TW200736260A (en) 2005-11-10 2007-10-01 Smithkline Beecham Corp Inhibitors of Akt activity
CN101321525B (zh) 2005-12-01 2013-01-30 霍夫曼-拉罗奇有限公司 作为l-cpt1抑制剂的杂芳基取代的哌啶衍生物
EP1970377A4 (en) 2005-12-09 2013-02-27 Meiji Seika Kaisha LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THIS AS AN ACTIVE SUBSTANCE
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
RU2008141761A (ru) 2006-03-22 2010-04-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) ИНГИБИТОРЫ с-МЕТ ПРОТЕИНКИНАЗЫ
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
EP2001870A2 (en) 2006-03-31 2008-12-17 Schering Corporation Kinase inhibitors
KR20090019796A (ko) 2006-05-22 2009-02-25 쉐링 코포레이션 ＣＤＫ 억제제로서의 피라졸로[1,5-ａ]피리미딘
EP2044051B1 (en) 2006-06-22 2010-01-27 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
US8198448B2 (en) 2006-07-14 2012-06-12 Amgen Inc. Fused heterocyclic derivatives and methods of use
US8217177B2 (en) 2006-07-14 2012-07-10 Amgen Inc. Fused heterocyclic derivatives and methods of use
PE20080403A1 (es) 2006-07-14 2008-04-25 Amgen Inc Derivados heterociclicos fusionados y metodos de uso
RU2009115954A (ru) 2006-09-29 2010-11-10 Новартис АГ (CH) Пиразолопиримидины в качестве ингибиторов липидной киназы р13к
GB0619342D0 (en) 2006-09-30 2006-11-08 Vernalis R&D Ltd New chemical compounds
BRPI0717845A2 (pt) 2006-10-04 2015-06-16 Hoffmann La Roche Uso de compostos, composições farmacêuticas e métodos para o tratamento e/ou profilaxia de enfermidades que podem ser tratadas com agentes de elevação de colesterol-hdl e compostos
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
NZ576278A (en) 2006-10-19 2011-12-22 Signal Pharm Llc Heteroaryl compounds, compositions thereof, and their use as protein kinase inhibitors
EP2081928B1 (en) 2006-11-10 2014-02-26 Bristol-Myers Squibb Company Pyrrolo-pyridine kinase inhibitors
CA2670083A1 (en) 2006-11-20 2008-05-29 Alantos Pharmaceuticals Holding, Inc. Heterobicyclic metalloprotease inhibitors
KR20090088962A (ko) 2006-12-15 2009-08-20 바이엘 쉐링 파마 악티엔게젤샤프트 ３-ｈ-피라졸로피리딘 및 그의 염, 이를 포함하는 제약 조성물, 이의 제조 방법 및 이의 용도
EP2125781A2 (en) 2006-12-20 2009-12-02 Amgen Inc. Substituted heterocycles and methods of use
PE20081581A1 (es) 2006-12-21 2008-11-12 Plexxikon Inc COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA
GB0625659D0 (en) 2006-12-21 2007-01-31 Cancer Rec Tech Ltd Therapeutic compounds and their use
EP2805945B1 (en) 2007-01-10 2019-04-03 MSD Italia S.r.l. Amide substituted indazoles as poly(ADP-ribose)polymerase (PARP) inhibitors
CA2676173A1 (en) 2007-02-16 2008-08-28 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
ES2431163T3 (es) 2007-03-01 2013-11-25 Novartis Ag Inhibidores de PIM quinasa y métodos para su uso
KR20090130064A (ko) 2007-04-10 2009-12-17 바이엘 크롭사이언스 아게 살충성 아릴 이속사졸린 유도체
US7592342B2 (en) 2007-05-10 2009-09-22 Smithkline Beecham Corporation Quinoxaline derivatives as PI3 kinase inhibitors
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
EP2014661A1 (de) 2007-06-13 2009-01-14 Bayer CropScience AG Heterocyclisch substituierte Heterocyclyl-carbonsäurederivate
UY31137A1 (es) 2007-06-14 2009-01-05 Smithkline Beecham Corp Derivados de quinazolina como inhibidores de la pi3 quinasa
WO2008156174A1 (ja) 2007-06-21 2008-12-24 Taisho Pharmaceutical Co., Ltd. ピラジンアミド化合物
CA2691003A1 (en) 2007-06-26 2008-12-31 Lexicon Pharmaceuticals, Inc. Methods of treating serotonin-mediated diseases and disorders
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
US8293747B2 (en) 2007-07-19 2012-10-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
SG187396A1 (en) 2007-07-19 2013-02-28 Lundbeck & Co As H 5-membered heterocyclic amides and related compounds
WO2009017954A1 (en) 2007-08-01 2009-02-05 Phenomix Corporation Inhibitors of jak2 kinase
CN101815712A (zh) 2007-08-01 2010-08-25 辉瑞有限公司 吡唑化合物及其作为raf抑制剂的用途
WO2009024825A1 (en) 2007-08-21 2009-02-26 Astrazeneca Ab 2-pyrazinylbenzimidazole derivatives as receptor tyrosine kinase inhibitors
US8415358B2 (en) 2007-09-17 2013-04-09 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
WO2009070567A1 (en) 2007-11-28 2009-06-04 Schering Corporation 2-fluoropyrazolo[1,5-a]pyrimidines as protein kinase inhibitors
WO2009075790A1 (en) 2007-12-07 2009-06-18 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors for intra-articular application
AU2009204483B2 (en) 2008-01-04 2014-03-13 Intellikine, Llc Certain chemical entities, compositions and methods
JP5989965B2 (ja) 2008-01-08 2016-09-07 メルク シャープ エンド ドーム リミテッド ２−｛４−［（３ｓ）−ピペリジン−３−イル］フェニル｝−２ｈ−インダゾール−７−カルボキサミドの薬学的に許容される塩
EP2085398A1 (en) 2008-02-01 2009-08-05 Merz Pharma GmbH & Co. KGaA Pyrazolopyrimidines, a process for their preparation and their use as medicine
ATE517107T1 (de) 2008-02-25 2011-08-15 Hoffmann La Roche Pyrrolopyrazinkinaseinhibitoren
PT2250172E (pt) 2008-02-25 2011-11-30 Hoffmann La Roche Inibidores de pirrolpirazina-cinase
CA2713718A1 (en) 2008-02-25 2009-09-03 F. Hoffmann-La Roche Ag Pyrrolopyrazine kinase inhibitors
MX2010008198A (es) 2008-02-25 2010-08-23 Hoffmann La Roche Inhibidores de cinasa de pirrolopirazina.
TW200940537A (en) 2008-02-26 2009-10-01 Astrazeneca Ab Heterocyclic urea derivatives and methods of use thereof
WO2009117157A1 (en) 2008-03-20 2009-09-24 Amgen Inc. Aurora kinase modulators and method of use
KR20110014613A (ko) 2008-04-28 2011-02-11 아스트라제네카 아베 치환된 복소환의 제조 방법
WO2009152087A1 (en) 2008-06-10 2009-12-17 Plexxikon, Inc. Bicyclic heteroaryl compounds and methods for kinase modulation, and indications therefor
MX2011000216A (es) 2008-07-08 2011-03-29 Intellikine Inc Inhibidores de cinasa y metodos para su uso.
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)
CN102223798A (zh) 2008-09-24 2011-10-19 巴斯夫欧洲公司 用于防治无脊椎动物害虫的吡唑化合物
MX2011004188A (es) 2008-10-21 2011-06-09 Vertex Pharma Inhibidores de la proteina cinasa c-met.
RU2539568C2 (ru) 2008-10-31 2015-01-20 Дженентек, Инк. Пиразолопиримидиновые соединения-ингибиторы jak и способы
MX2011004953A (es) 2008-11-10 2011-12-14 Vertex Pharma Compuestos utiles como inhibidores de cinasa atr.
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
JP5431495B2 (ja) 2008-12-05 2014-03-05 エフ．ホフマン−ラ ロシュ アーゲー ピロロピラジニル尿素キナーゼ阻害薬
ES2921576T3 (es) * 2008-12-19 2022-08-29 Vertex Pharma Compuestos útiles como inhibidores de la quinasa ATR
TW201028410A (en) 2008-12-22 2010-08-01 Astrazeneca Ab Chemical compounds 610
CN102264737A (zh) 2008-12-23 2011-11-30 雅培制药有限公司 抗病毒化合物
WO2010086040A1 (en) 2009-01-29 2010-08-05 Biomarin Iga, Ltd. Pyrazolo-pyrimidines for treatment of duchenne muscular dystrophy
SG173027A1 (en) 2009-01-30 2011-08-29 Toyama Chemical Co Ltd N-acyl anthranilic acid derivative or salt thereof
US20100204265A1 (en) 2009-02-09 2010-08-12 Genelabs Technologies, Inc. Certain Nitrogen Containing Bicyclic Chemical Entities for Treating Viral Infections
WO2010093425A1 (en) 2009-02-11 2010-08-19 Sepracor Inc. Histamine h3 inverse agonists and antagonists and methods of use thereof
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
GEP201706639B (en) 2009-08-17 2017-03-27 Intellikine Llc Heterocyclic compounds and uses thereof
WO2011025706A2 (en) 2009-08-26 2011-03-03 Schering Corporation 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
KR101851130B1 (ko) 2009-12-04 2018-04-23 센화 바이오사이언시즈 인코포레이티드 Ｃｋ2 억제제로서 피라졸로피리미딘 및 관련된 헤테로사이클
ES2572387T3 (es) 2010-03-18 2016-05-31 Pasteur Institut Korea Compuestos anti-infecciosos
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
EP2558866B1 (en) 2010-04-15 2016-08-17 Tracon Pharmaceuticals, Inc. Potentiation of anti-cancer activity through combination therapy with ber pathway inhibitors
US8969356B2 (en) 2010-05-12 2015-03-03 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
NZ603478A (en) 2010-05-12 2014-09-26 Vertex Pharma 2 -aminopyridine derivatives useful as inhibitors of atr kinase
EP2569286B1 (en) 2010-05-12 2014-08-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2011143419A1 (en) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Pyrazines useful as inhibitors of atr kinase
EP2569313A1 (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
KR20130083386A (ko) 2010-05-20 2013-07-22 에프. 호프만-라 로슈 아게 피롤로[2,3-ｂ]피라진-7-카복스아마이드 유도체 및 ＪＡＫ 및 ＳＹＫ 억제제로서의 그의 용도
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
EP2585468A1 (en) 2010-06-23 2013-05-01 Vertex Pharmaceuticals Incorporated Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase
RS54761B1 (sr) 2010-06-24 2016-10-31 Gilead Sciences Pirazolo[1,5-a]pirimidini i-triazini kao antiviralni agensi
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
KR101995013B1 (ko) 2010-07-13 2019-07-02 에프. 호프만-라 로슈 아게 Irak4 조절제로서 피라졸로[1,5a]피리미딘 및 티에노[3,2b]피리미딘 유도체
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
US8609669B2 (en) 2010-11-16 2013-12-17 Abbvie Inc. Potassium channel modulators
CA2817968C (en) 2010-11-16 2019-03-12 Array Biopharma Inc. Combination of checkpoint kinase 1 inhibitors and wee 1 kinase inhibitors
EP2649075B1 (en) 2010-12-08 2018-04-25 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Substituted pyrazolopyrimidines as glucocerebrosidase activators
CA2825098C (en) 2011-01-27 2020-03-10 Universite De Montreal Pyrazolopyridine and pyrazolopyrimidine derivatives as melanocortin-4 receptor modulators
AU2012240030A1 (en) 2011-04-05 2013-10-24 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
KR102104125B1 (ko) 2011-04-21 2020-05-29 재단법인 한국파스퇴르연구소 소염 화합물
AU2012255792A1 (en) 2011-05-17 2013-11-07 Principia Biopharma Inc. Azaindole derivatives as tyrosine kinase inhibitors
EP2723747A1 (en) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
WO2012178123A1 (en) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
CN103764166B (zh) 2011-06-22 2017-10-24 通用医疗公司 蛋白质病的治疗
US9309250B2 (en) 2011-06-22 2016-04-12 Vertex Pharmaceuticals Incorporated Substituted pyrrolo[2,3-b]pyrazines as ATR kinase inhibitors
BR112014000653A2 (pt) 2011-07-13 2017-02-14 Pharmacyclics Inc inibidores de tirosina quinase de bruton
WO2013052263A2 (en) 2011-09-16 2013-04-11 Microbiotix, Inc. Antifungal compounds
RU2018108589A (ru) * 2011-09-30 2019-02-25 Вертекс Фармасьютикалз Инкорпорейтед Лечение рака поджелудочной железы и немелкоклеточного рака легкого ингибиторами atr
US8765751B2 (en) 2011-09-30 2014-07-01 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP3878851A1 (en) 2011-09-30 2021-09-15 Vertex Pharmaceuticals Incorporated Process for making compounds useful as inhibitors of atr kinase
CA2850564A1 (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
EP2768509B1 (en) 2011-10-20 2017-03-22 Glaxosmithkline LLC Substituted bicyclic aza-heterocycles and analogues as sirtuin modulators
WO2013071090A1 (en) 2011-11-09 2013-05-16 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2776429A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
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
EP2776420A1 (en) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Pyrazine 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
EP2793882A4 (en) 2011-12-22 2015-04-29 Threshold Pharmaceuticals Inc ADMINISTRATION OF HYPOXIA-ACTIVATED PRODRUGS IN COMBINATION WITH CHK1 INHIBITORS FOR THE TREATMENT OF CANCER
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
AU2013243671B2 (en) 2012-04-02 2017-09-21 Cytokinetics, Inc. Methods for improving diaphragm function
PT2833973T (pt) 2012-04-05 2017-12-21 Vertex Pharma Compostos úteis como inibidores da cinase atr e terapias de combinação dos mesmos
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
KR20210156333A (ko) * 2012-05-15 2021-12-24 캔써 리서치 테크놀로지 리미티드 5-[[4-[[모르폴린-2-일]메틸아미노]-5-(트리플루오로메틸)-2-피리딜]아미노]피라진-2-카보니트릴 및 그의 치료적 용도
CN104334563B (zh) 2012-05-23 2017-03-08 萨维拉制药有限公司 7‑氧代‑噻唑并吡啶碳酸衍生物和它们在治疗、改善或预防病毒疾病中的用途
HK1204987A1 (en) 2012-05-23 2015-12-11 Savira Pharmaceuticals Gmbh 7-oxo-4,7 -dihydro- pyrazolo [1, 5 -a]pyrimidine derivatives which are useful in the treatment, amelioration or prevention of a viral disease
US20140018361A1 (en) 2012-07-11 2014-01-16 Nimbus Iris, Inc. Irak inhibitors and uses thereof
WO2014015523A1 (en) 2012-07-27 2014-01-30 Hutchison Medipharma Limited Novel heteroaryl and heterocycle compounds, compositions and methods
CA2879245A1 (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
US9505752B2 (en) 2012-08-09 2016-11-29 Viiv Healthcare Uk (No. 5) Limited 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
WO2014025850A1 (en) 2012-08-09 2014-02-13 Bristol-Myers Squibb Company Tricyclic amidine derivatives as hiv attachment inhibitors
KR20150044895A (ko) 2012-08-17 2015-04-27 바이엘 크롭사이언스 아게 살곤충제 및 살응애제로서의 아자인돌 카르복실산 아미드 및 아자인돌 티오카르복실산 아미드
MX2015001099A (es) 2012-08-24 2015-04-08 Hoffmann La Roche Nuevos derivados biciclicos de piridina.
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
CN104812389B (zh) 2012-09-24 2020-07-17 润新生物公司 某些化学实体、组合物及方法
WO2014055756A1 (en) 2012-10-04 2014-04-10 Vertex Pharmaceuticals Incorporated Method for measuring atr inhibition mediated increases in dna damage
CA2900335C (en) 2012-10-22 2021-10-26 City Of Hope Synthetic analogs of epipolythiodioxopiperazines and uses thereof
US9012643B2 (en) 2012-10-24 2015-04-21 Becton, Dickinson And Company Hydroxamate substituted azaindoline-cyanine dyes and bioconjugates of the same
WO2014089379A1 (en) 2012-12-07 2014-06-12 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
EP2970288A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2970289A1 (en) 2013-03-15 2016-01-20 Vertex Pharmaceuticals Inc. Compounds useful as inhibitors of atr kinase
US20150158868A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase
WO2015085132A1 (en) 2013-12-06 2015-06-11 Vertex Pharmaceuticals Incorporated 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
HRP20200186T1 (hr) 2014-06-05 2020-05-29 Vertex Pharmaceuticals Inc. Radioaktivno obilježeni derivati 2-amino-6-fluoro-n-[5-fluoro-piridin-3-il]-pirazolo[1,5-a]pirimidin-3-karboksamid spojeva koji se koriste kao inhibitori atr kinaze, priprava navedenih spojeva i njihovi različiti čvrsti oblici

Also Published As

Publication number Publication date
AU2015277212A1 (en) 2017-01-12
CN107072987A (zh) 2017-08-18
WO2015195740A1 (en) 2015-12-23
SI3157566T1 (sl) 2019-08-30
HUE044280T2 (hu) 2019-10-28
BR112016029523A8 (pt) 2021-07-20
JP2017524673A (ja) 2017-08-31
RU2017101189A3 (es) 2019-02-06
LT3157566T (lt) 2019-08-12
EP3157566A1 (en) 2017-04-26
CA2950780C (en) 2023-05-16
NZ727399A (en) 2022-07-29
ZA201608560B (en) 2020-05-27
PT3157566T (pt) 2019-07-11
US11179394B2 (en) 2021-11-23
RU2017101189A (ru) 2018-07-25
US20150359797A1 (en) 2015-12-17
MX2016016115A (es) 2017-03-08
RU2736219C2 (ru) 2020-11-12
PL3157566T3 (pl) 2019-10-31
AU2015277212B2 (en) 2020-07-02
SG10201811175WA (en) 2019-01-30
CN107072987B (zh) 2020-02-07
HRP20191375T1 (hr) 2019-11-01
ES2733847T3 (es) 2019-12-03
SG11201610500WA (en) 2017-01-27
IL249596A0 (en) 2017-02-28
KR20170016498A (ko) 2017-02-13
BR112016029523A2 (pt) 2017-08-22
RS59054B1 (sr) 2019-08-30
US20220249489A1 (en) 2022-08-11
EP3157566B1 (en) 2019-05-01
IL249596B (en) 2021-05-31
JP2020019815A (ja) 2020-02-06
JP6936007B2 (ja) 2021-09-15
DK3157566T3 (da) 2019-07-22
CA2950780A1 (en) 2015-12-23

Similar Documents

Publication Publication Date Title
MX378277B (es) Metodo para tratar cancer usando una combinacion de inhibidores de chk1 y relacionado con atm y rad3 (atr).
MX374452B (es) Inhibidores de glucosilceramida sintasa para el tratamiento de enfermedades.
MX2017004618A (es) Inhibidores de la biosintesis de sulfato de heparano para el tratamiento de enfermedades.
EA201791018A1 (ru) Производные 6-амино-7-бицикло-7-деазапурина в качестве ингибиторов протеинкиназы
MX2017009571A (es) Inhibidores heterociclicos de itk para el tratamiento de la inflamacion y cancer.
MX2016017288A (es) Metodos para tratar el cancer con inhibidores de tigit y agentes contra el cancer.
EA201690406A1 (ru) Селективные ингибиторы grp94 и способы их применения
MX380092B (es) Tratamiento de la osteoartritis.
CU24389B1 (es) Compuestos de heterociclilo bicíclico como inhibidores de irak4
EA201890768A2 (ru) Лечение злокачественной опухоли ингибиторами tor-киназы
TN2017000125A1 (en) Compositions and methods for inhibition of hao1 (hydroxyacid oxidase 1 (glycolate oxidase)) gene expression
EA201391390A1 (ru) Циклопропиламины в качестве ингибиторов lsd
PH12017501019A1 (en) Isoxazole hydromaxamic acid compounds as lpxc inhibitors
MX2014013752A (es) Inhibidores de nampt.
EA201890567A1 (ru) Способ лечения рака
PH12014502513A1 (en) Nampt inhibitors
EA201591543A1 (ru) Комбинированные терапии для лечения рака с применением микрорнк и ингибиторов egfr-tki
MX370270B (es) Inhibidores de glucosilceramida sintasa para el tratamiento de enfermedades.
IN2015DN01151A (es)
MX348311B (es) Inhibidores nampt.
GEP20166489B (en) 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
MY183490A (en) Compositions and methods for inhibiting expression of the alas1 gene
MX394452B (es) Inhibicion de la actividad de olig2.
MX379585B (es) Composición para usarse en el tratamiento de cáncer que presenta pérdida hemicigota de tp53.
EA201590744A1 (ru) Лечение рака tor киназными ингибиторами