[go: up one dir, main page]

TN2010000052A1 - Derives de pyrazole et leur utilisation comme inhibiteurs de raf - Google Patents

Derives de pyrazole et leur utilisation comme inhibiteurs de raf

Info

Publication number
TN2010000052A1
TN2010000052A1 TNP2010000052A TN2010000052A TN2010000052A1 TN 2010000052 A1 TN2010000052 A1 TN 2010000052A1 TN P2010000052 A TNP2010000052 A TN P2010000052A TN 2010000052 A TN2010000052 A TN 2010000052A TN 2010000052 A1 TN2010000052 A1 TN 2010000052A1
Authority
TN
Tunisia
Prior art keywords
raf
inhibitors
pyrazole derivatives
synthesis
compounds
Prior art date
Application number
TNP2010000052A
Other languages
English (en)
Inventor
Jingrong Jean Cui
Judith Gail Deal
Danlin Gu
Chuangxing Guo
Mary Catherine Ohnson
Robert Steven Kania
Susan Elizabeth Kephart
Maria Angelica Linton
Indrawan James Mcapline
Mason Alan Pairish
Cynthia Louise Palmer
Original Assignee
Pfizer
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40122511&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TN2010000052(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of TN2010000052A1 publication Critical patent/TN2010000052A1/fr

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne des composés de formule (I) et leurs sels pharmaceutiquement acceptables, leurs synthèse et leur utilisation comme inhibiteurs de Raf.
TNP2010000052A 2007-08-01 2010-01-29 Derives de pyrazole et leur utilisation comme inhibiteurs de raf TN2010000052A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US95323507P 2007-08-01 2007-08-01
US8005408P 2008-07-11 2008-07-11
PCT/IB2008/001952 WO2009016460A2 (fr) 2007-08-01 2008-07-21 Composés pyrazoles

Publications (1)

Publication Number Publication Date
TN2010000052A1 true TN2010000052A1 (fr) 2011-09-26

Family

ID=40122511

Family Applications (1)

Application Number Title Priority Date Filing Date
TNP2010000052A TN2010000052A1 (fr) 2007-08-01 2010-01-29 Derives de pyrazole et leur utilisation comme inhibiteurs de raf

Country Status (24)

Country Link
US (1) US7772246B2 (fr)
EP (1) EP2183243A2 (fr)
JP (1) JP4792126B2 (fr)
KR (1) KR20100038119A (fr)
CN (1) CN101815712A (fr)
AP (1) AP2010005167A0 (fr)
AR (1) AR067759A1 (fr)
AU (1) AU2008281543A1 (fr)
BR (1) BRPI0815042A2 (fr)
CA (1) CA2695114A1 (fr)
CL (1) CL2008002255A1 (fr)
CO (1) CO6251265A2 (fr)
CR (1) CR11241A (fr)
DO (1) DOP2010000047A (fr)
EA (1) EA201000113A1 (fr)
EC (1) ECSP109922A (fr)
MA (1) MA31574B1 (fr)
PA (1) PA8791801A1 (fr)
PE (1) PE20090952A1 (fr)
SV (1) SV2010003472A (fr)
TN (1) TN2010000052A1 (fr)
TW (1) TW200911243A (fr)
UY (1) UY31260A1 (fr)
WO (1) WO2009016460A2 (fr)

Families Citing this family (101)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MXPA03005001A (es) * 2000-12-05 2003-09-05 Vertex Pharma Inhibidores de n- terminal c-jun cinasas (jnk) y otras proteinas cinasas.
SI2426129T1 (sl) 2005-12-13 2017-02-28 Incyte Holdings Corporation Heteroarilno substituirani pirolo(2,3-b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janusove kinaze
MX342814B (es) 2007-06-13 2016-10-13 Incyte Holdings Corp Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
EP2308877B1 (fr) 2008-08-05 2014-01-22 Daiichi Sankyo Company, Limited Dérivés d'imidazopyridin-2-one
CL2009001884A1 (es) * 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
RU2011123647A (ru) 2008-11-10 2012-12-20 Вертекс Фармасьютикалз Инкорпорейтед Соединения, полезные в качестве ингибиторов atr киназы
AU2009327357C1 (en) 2008-12-19 2017-02-02 Vertex Pharmaceuticals Incorporated Pyrazine derivatives useful as inhibitors of ATR kinase
WO2010100127A1 (fr) 2009-03-04 2010-09-10 Novartis Ag Dérivés d'imidazole disubstitués en tant que modulateurs de la protéine kinase raf
CN102458581B (zh) * 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2,3-d]嘧啶和吡咯-3-基-吡咯并[2,3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
HUE046493T2 (hu) 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
US8329724B2 (en) 2009-08-03 2012-12-11 Hoffmann-La Roche Inc. Process for the manufacture of pharmaceutically active compounds
AR077975A1 (es) * 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
WO2011028685A1 (fr) 2009-09-01 2011-03-10 Incyte Corporation Dérivés hétérocycliques de pyrazol-4-yl-pyrrolo[2,3-d] pyrimidines en tant qu'inhibiteurs de janus kinase
JP5658756B2 (ja) * 2009-09-10 2015-01-28 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Jakの阻害剤
EP2308866A1 (fr) 2009-10-09 2011-04-13 Bayer CropScience AG Phenylpyri(mi)dinylpyrazoles et leur utilisation comme fongicides
RS57219B1 (sr) 2010-03-10 2018-07-31 Incyte Holdings Corp Piperidin-4-il azetidin derivati kao inhibitori jak1
EP2569289A1 (fr) 2010-05-12 2013-03-20 Vertex Pharmaceuticals Incorporated Pyrazines utiles en tant qu'inhibiteurs de la kinase atr
WO2011143399A1 (fr) 2010-05-12 2011-11-17 Vertex Pharmaceuticals Incorporated Composés utiles en tant qu'inhibiteurs de l'atr kinase
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
KR20130066633A (ko) 2010-05-12 2013-06-20 버텍스 파마슈티칼스 인코포레이티드 Atr 키나제의 억제제로서 유용한 화합물
EP2569287B1 (fr) 2010-05-12 2014-07-09 Vertex Pharmaceuticals Inc. Composés utilisables en tant qu'inhibiteurs de la kinase atr
MX2012013082A (es) 2010-05-12 2013-05-09 Vertex Pharma Derivados de 2-aminopiridina utiles como iinhibidores de cinasa atr.
EP3087972A1 (fr) 2010-05-21 2016-11-02 Incyte Holdings Corporation Formulation topique pour un inhibiteur jak
MX2013000103A (es) 2010-06-23 2013-06-13 Vertex Pharma Derivados de pirrolo-pirazina utiles como inhibidores de cinasa art.
US8779150B2 (en) 2010-07-21 2014-07-15 Hoffmann-La Roche Inc. Processes for the manufacture of propane-1-sulfonic acid {3-[5-(4-chloro-phenyl)-1 H-pyrrolo[2,3-b]pyridine-3-carbonyl]-2,4-difluoro-phenyl}-amide
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
WO2012135631A1 (fr) 2011-03-30 2012-10-04 Arrien Pharmaeuticals Llc 5-(pyrazin-2-yl)-1h-pyrazolo[3,4-b]pyridine substituée et dérivés de pyrazolo[3,4-b]pyridine en tant qu'inhibiteurs de protéine kinase
CA2832100A1 (fr) 2011-04-05 2012-10-11 Vertex Pharmaceuticals Incorporated Composes aminopyrazines utiles en tant qu'inhibiteurs de la kinase atr
PH12013502612A1 (en) 2011-06-20 2014-04-28 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
WO2012178124A1 (fr) 2011-06-22 2012-12-27 Vertex Pharmaceuticals Incorporated Composés utiles comme inhibiteurs de la kinase atr
EP2723746A1 (fr) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Composés inhibiteurs de la kinase atr
EP2723745A1 (fr) 2011-06-22 2014-04-30 Vertex Pharmaceuticals Inc. Composés utiles comme inhibiteurs de la kinase atr
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2751088B1 (fr) 2011-09-30 2016-04-13 Vertex Pharmaceuticals Incorporated Composés utiles en tant qu'inhibiteurs de kinase atr
US8853217B2 (en) 2011-09-30 2014-10-07 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
CN103957917A (zh) 2011-09-30 2014-07-30 沃泰克斯药物股份有限公司 用atr抑制剂治疗胰腺癌和非小细胞肺癌
CA3124539A1 (fr) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Procede de fabrication d'un derive de 4-[chloro-n-hydroxycarbonimidoyl]phenyle
WO2013049722A1 (fr) 2011-09-30 2013-04-04 Vertex Pharmaceuticals Incorporated Composés utiles comme inhibiteurs de kinase atr
EP2776429A1 (fr) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Composés utiles comme inhibiteurs de kinase atr
US8841449B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776421A1 (fr) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Composés utiles comme inhibiteurs de kinase atr
US8841337B2 (en) 2011-11-09 2014-09-23 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
EP2776420A1 (fr) 2011-11-09 2014-09-17 Vertex Pharmaceuticals Incorporated Composés de pyrazine utiles comme inhibiteurs de kinase atr
CA2855243C (fr) 2011-11-11 2020-04-14 Novartis Ag Procede de traitement d'une maladie proliferative
PT2782557T (pt) 2011-11-23 2018-11-26 Array Biopharma Inc Formulações farmacêuticas
CN103159736B (zh) * 2011-12-10 2015-05-13 通化济达医药有限公司 取代的吡唑激酶抑制剂
US20140044802A1 (en) 2012-04-05 2014-02-13 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of atr kinase and combination therapies thereof
WO2013173720A1 (fr) 2012-05-18 2013-11-21 Incyte Corporation Dérivés de pyrrolopyridine et de pyrrolopyrimidine substitués par un pipéridinylcyclobutyle à titre d'inhibiteurs jak
EP2904406B1 (fr) 2012-10-04 2018-03-21 Vertex Pharmaceuticals Incorporated Procédée pour la détermination de dommage de adn augmenté par inhibition de atr
EP2909202A1 (fr) 2012-10-16 2015-08-26 Vertex Pharmaceuticals Incorporated Composés utiles en tant qu'inhibiteurs de la kinase atr
TW202228704A (zh) 2012-11-15 2022-08-01 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
RS64234B1 (sr) 2012-12-07 2023-06-30 Vertex Pharma Pirazolo[1,5-a]pirimidini korisni kao inhibitori atr kinaze za lečenje kancera
EP2945938B1 (fr) 2013-01-18 2018-03-07 F. Hoffmann-La Roche AG Pyrazoles 3 substitués et utilisation en tant qu'inhibiteurs de dlk
ES2698359T3 (es) 2013-02-20 2019-02-04 Lg Chemical Ltd Agonistas del receptor de la esfingosina-1-fosfato, métodos para preparar los mismos y composiciones farmacéuticas que los contienen como agentes activos
MX366855B (es) 2013-03-01 2019-07-26 Amgen Inc Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.
BR122021015061B1 (pt) 2013-03-06 2022-10-18 Incyte Holdings Corporation Processos e intermediários para preparar um inibidor de jak
US20140303121A1 (en) 2013-03-15 2014-10-09 Plexxikon Inc. Heterocyclic compounds and uses thereof
SG11201506687RA (en) * 2013-03-15 2015-09-29 Plexxikon Inc Heterocyclic compounds and uses thereof
US9663519B2 (en) 2013-03-15 2017-05-30 Vertex Pharmaceuticals Incorporated Compounds useful as inhibitors of ATR kinase
DK3030227T3 (da) 2013-08-07 2020-04-20 Incyte Corp Vedvarende frigivelses-doseringsformer for en jak1-inhibitor
CN114716426A (zh) 2013-08-21 2022-07-08 詹森生物制药有限公司 抗病毒化合物
CN103626767A (zh) * 2013-12-04 2014-03-12 上海药明康德新药开发有限公司 区域选择性的氮杂吲哚及其合成方法
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
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
SG11201610197XA (en) 2014-06-05 2017-01-27 Vertex Pharma Radiolabelled derivatives of a 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]- pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, the preparation of said compound and different solid forms thereof
NZ727399A (en) 2014-06-17 2022-07-29 Vertex Pharma Method for treating cancer using a combination of chk1 and atr inhibitors
EP3177618A1 (fr) 2014-08-08 2017-06-14 Amgen Inc. Composés thiazin-2-amine fusionnée à un groupement cyclopropyle utilisés en tant qu'inhibiteurs de la bêta-secrétase et leurs procédés d'utilisation
CN105777743A (zh) * 2014-12-19 2016-07-20 奥浦顿(上海)医药科技有限公司 一种吡唑并[3,4-b]吡啶类化合物中间体的制备方法和应用
HK1258570A1 (zh) 2015-09-30 2019-11-15 Vertex Pharmaceuticals Inc. 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法
CN106187899B (zh) * 2016-06-28 2019-07-16 绍兴文理学院 一种氟代氮杂芳烃的合成方法
WO2018124001A1 (fr) * 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Composé inhibiteur de signal bmp
US10787443B2 (en) * 2017-04-28 2020-09-29 Zamboni Chem Solutions Inc. RAF-degrading conjugate compounds
WO2019075243A1 (fr) 2017-10-13 2019-04-18 Plexxikon Inc. Formes solides d'un composé pour la modulation de kinases
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
CA3089832A1 (fr) 2018-01-30 2019-08-08 Incyte Corporation Procedes de preparation de (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
IL318069A (en) 2018-03-30 2025-02-01 Incyte Corp Using JAK inhibitors to treat hidradenitis suppurativa
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
CN109575019B (zh) * 2018-12-26 2020-04-14 苏州闻智生物科技有限公司 一种5-溴-7-氮杂吲哚的制备方法
WO2020168197A1 (fr) 2019-02-15 2020-08-20 Incyte Corporation Composés de pyrrolo[2,3-d]pyrimidinone en tant qu'inhibiteurs de cdk2
WO2020180959A1 (fr) 2019-03-05 2020-09-10 Incyte Corporation Composés de pyrazolyl pyrimidinylamine en tant qu'inhibiteurs de cdk2
WO2020205560A1 (fr) 2019-03-29 2020-10-08 Incyte Corporation Composés sulfonylamides utilisés comme inhibiteurs de la cdk2
WO2020223469A1 (fr) 2019-05-01 2020-11-05 Incyte Corporation Dérivés de n-(1-(méthylsulfonyl)pipéridin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine et composés apparentés utilisés en tant qu'inhibiteurs de kinase 2 dépendante des cyclines (cdk2) pour le traitement du cancer
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
CA3150681A1 (fr) 2019-08-14 2021-02-18 Incyte Corporation Composes imidazolyl-pyrimidinylamines utilises comme inhibiteurs de la cdk2
CR20220170A (es) 2019-10-11 2022-10-10 Incyte Corp Aminas bicíclicas como inhibidoras de la cdk2
WO2021120890A1 (fr) * 2019-12-20 2021-06-24 Novartis Ag Dérivés pyrazolyle utiles en tant qu'agents anticancéreux
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022040180A1 (fr) 2020-08-18 2022-02-24 Incyte Corporation Procédé et intermédiaires pour la préparation d'un inhibiteur de jak
PE20231308A1 (es) 2020-08-18 2023-08-24 Incyte Corp Proceso e intermedios para preparar un inhibidor de jak1
MX2023005078A (es) * 2020-10-30 2023-05-16 Novartis Ag Nuevas formas cristalinas de un compuesto inhibidor de kras g12c.
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
WO2023288197A1 (fr) 2021-07-12 2023-01-19 Incyte Corporation Procédé et intermédiaires pour la préparation de baricitinib
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
CN114557977A (zh) * 2022-02-16 2022-05-31 北京康立生医药技术开发有限公司 一种治疗肠癌的药物的制备方法、制剂及纯度分析方法
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
WO2025034702A1 (fr) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Rmc-6291 destiné à être utilisé dans le traitement d'une maladie ou d'un trouble lié à une protéine ras
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. Ras inhibitors
WO2025171296A1 (fr) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Inhibiteurs de ras
WO2025240847A1 (fr) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Inhibiteurs de ras

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB2306108A (en) 1995-10-13 1997-04-30 Merck & Co Inc Treatment of Raf-mediated cancers with imidazole derivatives
US6514977B1 (en) * 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
ES2239596T3 (es) * 1999-06-03 2005-10-01 Teikoku Hormone Mfg. Co., Ltd. Compuestos de pirazol sustituidos.
WO2001030154A2 (fr) 1999-10-25 2001-05-03 Basf Aktiengesellschaft Compositions agrochimiques contenant des pyrazols comme principes actifs et leur utilisation comme phytosanitaires a action fongicide
ES2237671T3 (es) * 2001-02-02 2005-08-01 Smithkline Beecham Corporation Derivados de pirazol contra la sobreexpresion de tgf.
US20040097502A1 (en) * 2001-02-02 2004-05-20 Gellibert Francoise Jeanne Pyrazoles as tgf inhibitors
CA2446864C (fr) * 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibiteurs de src et autres proteine kinases
DE60222804T2 (de) * 2001-12-21 2008-07-03 Vernalis (Cambridge) Ltd., Abington 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung
AR040442A1 (es) * 2002-06-05 2005-04-06 Pharmacia Corp Derivados de pirazol como inhibidores de la quinasa p38
GB0215844D0 (en) * 2002-07-09 2002-08-14 Novartis Ag Organic compounds
DE60330362D1 (de) * 2002-09-18 2010-01-14 Pfizer Prod Inc Neue pyrazol-verbindungen als hemmer des transformierenden wachstumsfaktors (tgf)
CL2004000234A1 (es) * 2003-02-12 2005-04-15 Biogen Idec Inc Compuestos derivados 3-(piridin-2-il)-4-heteroaril-pirazol sustituidos, antagonistas de aik5 y/o aik4; composicion farmaceutica y uso del compuesto en el tratamiento de desordenes fibroticos como esclerodermia, lupus nefritico, cicatrizacion de herid
WO2006044869A1 (fr) * 2004-10-19 2006-04-27 Arqule, Inc. Synthese d'inhibiteurs d'imidazo-oxazole et d'imidazothiazole de la map kinase p38
JP4302762B2 (ja) * 2005-01-07 2009-07-29 ファイザー・プロダクツ・インク 複素環式芳香族キノリン化合物およびpde10阻害剤としてのその使用
WO2007105058A2 (fr) 2006-03-16 2007-09-20 Pfizer Products Inc. Pyrazoles
WO2007123892A2 (fr) * 2006-04-17 2007-11-01 Arqule Inc. Inhibiteurs raf et leurs utilisations

Also Published As

Publication number Publication date
JP4792126B2 (ja) 2011-10-12
MA31574B1 (fr) 2010-08-02
EA201000113A1 (ru) 2010-08-30
SV2010003472A (es) 2011-03-23
CL2008002255A1 (es) 2009-04-17
KR20100038119A (ko) 2010-04-12
PA8791801A1 (es) 2009-03-31
CN101815712A (zh) 2010-08-25
UY31260A1 (es) 2009-03-02
PE20090952A1 (es) 2009-07-19
AU2008281543A1 (en) 2009-02-05
JP2010535189A (ja) 2010-11-18
EP2183243A2 (fr) 2010-05-12
ECSP109922A (es) 2010-03-31
AR067759A1 (es) 2009-10-21
CR11241A (es) 2010-04-27
WO2009016460A2 (fr) 2009-02-05
US20090221608A1 (en) 2009-09-03
AP2010005167A0 (en) 2010-02-28
CO6251265A2 (es) 2011-02-21
WO2009016460A8 (fr) 2009-10-15
US7772246B2 (en) 2010-08-10
CA2695114A1 (fr) 2009-02-05
DOP2010000047A (es) 2010-04-15
WO2009016460A3 (fr) 2009-03-26
TW200911243A (en) 2009-03-16
BRPI0815042A2 (pt) 2015-02-10

Similar Documents

Publication Publication Date Title
TN2010000052A1 (fr) Derives de pyrazole et leur utilisation comme inhibiteurs de raf
TN2009000085A1 (fr) Derives de pyrido (2,3-d) pyrimidinone et leur utilisation comme inhibiteurs de pi3
TW200626610A (en) Analogs of 17-hydroxywortmannin as PI3K inhibitors
WO2007105058A3 (fr) Pyrazoles
ATE542813T1 (de) 6-substituierte 2- heterocyclylaminopyrazinverbindungen als chk-1- inhibitoren
MA34644B1 (fr) Dérivés de pyrazole aminopyrimidine en tant que modulateurs du lrrk2
EA201071339A1 (ru) Фосфорсодержащие производные в качестве ингибиторов киназы
NI201000059A (es) Inhibidores de la cinasa c-fms.
MA33492B1 (fr) Inhibiteurs de bace
UA97821C2 (en) Cyclized derivatives as eg-5 inhibitors
EA201100503A1 (ru) Глюкозидные производные и их применения
MA32351B1 (fr) Derives d'aminodihydrothiazine a titre d'inhibiteurs de bace pour le traitement de la maladie d'alzheimer
EA201291217A1 (ru) ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ 1-(β-D-ГЛЮКОПИРАНОЗИЛ)-2-ТИЕНИЛМЕТИЛБЕНЗОЛА КАК ИНГИБИТОРЫ НЗПГ
TN2009000329A1 (fr) DERIVES DE 2-AMINO-5,7-DIHYDRO-6H-PYRROLO[3,4-d]-PYRIMIDINE SERVANT D'INHBITEURS DE HSP-90 POUR LE TRAITEMENT DU CANCER
TW200833675A (en) Nicotinamide derivatives
MX2010009416A (es) Compuestos heterociclicos como inhibidores de cxcr2.
MX2009007302A (es) Derivados de purina.
MA33384B1 (fr) Sulfonamides hétérocycliques, leurs utilisations et compositions pharmaceutiques les contenant
TW200612958A (en) Substituted imidazole derivatives
UA107784C2 (en) Inhibitor of melanin production
EA200900631A1 (ru) Замещённые пиразолы и триазолы, как ингибиторы кбв (кинезин-белок веретена)
EA200801608A1 (ru) Производные бензимидазолонкарбоновой кислоты
EA201100696A1 (ru) 1-(арилсульфонил)-4-(пиперазин-1-ил)-1h-бензимидазолы в качестве лигандов 5-гидрокситриптамина-6
NO20081207L (no) Isoquinolines as IGF-1R inhibitors
EA201001348A1 (ru) Пирролопиримидинкарбоксамиды