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MX341704B - Métodos de síntesis y purificación de compuestos de heteroarilo. - Google Patents

Métodos de síntesis y purificación de compuestos de heteroarilo.

Info

Publication number
MX341704B
MX341704B MX2012004887A MX2012004887A MX341704B MX 341704 B MX341704 B MX 341704B MX 2012004887 A MX2012004887 A MX 2012004887A MX 2012004887 A MX2012004887 A MX 2012004887A MX 341704 B MX341704 B MX 341704B
Authority
MX
Mexico
Prior art keywords
heteroaryl compounds
methods
purification
synthesis
conditions
Prior art date
Application number
MX2012004887A
Other languages
English (en)
Other versions
MX2012004887A (es
Inventor
Packard Garrick
Sapienza John
Atul Kothare Mohit
Perrin-Ninkovic Sophie
Elsner Jan
Papa Patrick
Riggs Jennifer
L Harris Roy
Mortensen Deborah
Shevlin Graziella
Zhao Jingjing
Gingsee Lee Branden
Anthony Jokiel Patrick
Antonio Gamboa Juan
Georges Beauchamps Marie
Michael Kreilein Matthew
Pye Philip
Wei-Hwa Leong William
Choudhury Anusuya
Original Assignee
Signal Pharm Llc
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 Signal Pharm Llc filed Critical Signal Pharm Llc
Publication of MX2012004887A publication Critical patent/MX2012004887A/es
Publication of MX341704B publication Critical patent/MX341704B/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/16Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00 of arsenic, antimony, bismuth, vanadium, niobium, tantalum, polonium, chromium, molybdenum, tungsten, manganese, technetium or rhenium
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/20Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Materials Engineering (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

En la presente se proveen métodos para preparar compuestos de heteroarilo teniendo la siguiente estructura: fórmula (I) o fórmula (II): en donde R1-R4 son como se define en la presente. Los compuestos de heteroarilo son útiles para tratar o prevenir cáncer, condiciones inflamatorias, condiciones inmunológicas, enfermedades neurodegenerativas, diabetes, obesidad, trastornos neurológicos, enfermedades relacionadas con la edad o condiciones cardiovasculares.
MX2012004887A 2009-10-26 2010-10-22 Métodos de síntesis y purificación de compuestos de heteroarilo. MX341704B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25491709P 2009-10-26 2009-10-26
US32848010P 2010-04-27 2010-04-27
PCT/US2010/053678 WO2011053518A1 (en) 2009-10-26 2010-10-22 Methods of synthesis and purification of heteroaryl compounds

Publications (2)

Publication Number Publication Date
MX2012004887A MX2012004887A (es) 2012-06-08
MX341704B true MX341704B (es) 2016-08-31

Family

ID=43922466

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012004887A MX341704B (es) 2009-10-26 2010-10-22 Métodos de síntesis y purificación de compuestos de heteroarilo.

Country Status (23)

Country Link
US (3) US8569494B2 (es)
EP (2) EP2493472B1 (es)
JP (2) JP2013508456A (es)
KR (2) KR101903925B1 (es)
CN (2) CN106117213B (es)
AR (1) AR078788A1 (es)
AU (1) AU2010313585B2 (es)
BR (1) BR112012009751A2 (es)
CA (1) CA2778615C (es)
CO (1) CO6541598A2 (es)
CR (1) CR20120211A (es)
EC (1) ECSP12011831A (es)
ES (2) ES2613664T3 (es)
IL (1) IL219368A (es)
MX (1) MX341704B (es)
MY (1) MY177695A (es)
NI (1) NI201200066A (es)
NZ (2) NZ599549A (es)
PH (1) PH12014500392B1 (es)
RU (1) RU2557242C2 (es)
SG (1) SG10201500511TA (es)
WO (1) WO2011053518A1 (es)
ZA (1) ZA201202959B (es)

Families Citing this family (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EP2300013B2 (en) 2008-05-21 2024-11-13 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
WO2010056311A1 (en) 2008-11-12 2010-05-20 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
WO2012151561A1 (en) 2011-05-04 2012-11-08 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
EA030664B1 (ru) * 2011-10-19 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Лечение злокачественной опухоли ингибиторами tor-киназы
CN104093398B (zh) * 2011-12-02 2017-03-15 西格诺药品有限公司 7‑(6‑(2‑羟基丙烷‑2‑基)吡啶‑3‑基)‑1‑((反式)‑4‑甲氧基环己基)‑3,4‑二氢吡嗪并[2,3‑b]吡嗪‑2(1h)‑酮、其固体形式的药物组合物及其使用方法
AU2015201807B2 (en) * 2011-12-02 2016-12-08 Signal Pharmaceuticals, Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methocyclohexyl)-3,4-dihydropyrazino[2,3-b] pyrazin-2(1H)-one, a solid form thereof and methods of their use
MY174308A (en) 2012-02-24 2020-04-06 Signal Pharm Llc Methods for treating non-small cell lung using tor kinase inhibitor combination therapy
TWI664968B (zh) 2012-03-15 2019-07-11 標誌製藥公司 使用tor激酶抑制劑之癌症治療
BR112014022707A2 (pt) 2012-03-15 2020-10-27 Signal Pharmaceuticals, Llc uso de uma quantidade eficaz de um inibidor de quinase tor, método para melhorar os critérios de avaliação, método para a inibição da fosforilação, método para a inibição da atividade de proteína, método para a medição da inibição da fosforilação, kit
SG11201405686PA (en) 2012-03-15 2014-10-30 Signal Pharm Llc Treatment of cancer with tor kinase inhibitors
CN104519885A (zh) 2012-03-15 2015-04-15 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
AU2013204563B2 (en) 2012-05-05 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
PT3176170T (pt) 2012-06-13 2019-02-05 Incyte Holdings Corp Compostos tricíclicos substituídos como inibidores de fgfr
AU2013202768B2 (en) * 2012-10-18 2015-11-05 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
AU2013203714B2 (en) 2012-10-18 2015-12-03 Signal Pharmaceuticals, Llc Inhibition of phosphorylation of PRAS40, GSK3-beta or P70S6K1 as a marker for TOR kinase inhibitory activity
AU2015213397B2 (en) * 2012-10-18 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
WO2014113429A2 (en) 2013-01-16 2014-07-24 Signal Pharmaceuticals, Llc Substituted pyrrolopyrimidine compounds, compositions thereof, and methods of treatment therewith
CA2902858A1 (en) * 2013-02-28 2014-09-04 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
US20140275502A1 (en) * 2013-03-13 2014-09-18 Dow Agrosciences Llc Process for the preparation of certain triaryl rhamnose carbamates
US9273399B2 (en) 2013-03-15 2016-03-01 Ppg Industries Ohio, Inc. Pretreatment compositions and methods for coating a battery electrode
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
KR102242505B1 (ko) * 2013-04-17 2021-04-20 시그날 파마소티칼 엘엘씨 암 치료용 tor 키나제 억제제 및 시티딘 유사체를 포함하는 병용 요법
EP2986298A1 (en) 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Treatment of cancer with dihydropyrazino-pyrazines
JP6382949B2 (ja) * 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー 癌を治療するためのtorキナーゼ阻害剤及び5−置換キナゾリノン化合物を含む組合せ療法
JP6382945B2 (ja) * 2013-04-17 2018-08-29 シグナル ファーマシューティカルズ,エルエルシー ジヒドロピラジノ−ピラジンによる癌治療
TW201526894A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
NZ629469A (en) * 2013-04-17 2017-05-26 Signal Pharm Llc Methods for treating cancer using dihydropyrazino-pyrazine compound combination therapy
MX2015014455A (es) * 2013-04-17 2016-07-21 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y n-(3-(5-fluoro-2-(4-(2-metoxietoxi)fenilamino)pirimidin-4-ilamino )fenil)acrilamida para tratar cancer.
TW201527300A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 關於1-乙基-7-(2-甲基-6-(1H-1,2,4-三唑-3-基)吡啶-3-基)-3,4-二氫吡并[2,3-b]吡-2(1H)-酮之醫藥調配物、方法、固態型式及使用方法
KR102382576B1 (ko) * 2013-04-17 2022-04-08 시그날 파마소티칼 엘엘씨 암 치료를 위한 TOR 키나제 억제제 및 IMiD 화합물을 포함하는 조합요법
KR102469849B1 (ko) 2013-04-19 2022-11-23 인사이트 홀딩스 코포레이션 Fgfr 저해제로서 이환식 헤테로사이클
NZ629486A (en) 2013-05-29 2017-11-24 Signal Pharm Llc Pharmaceutical compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino [2,3-b]pyrazin-2(1h)-one, a solid form thereof and methods of their use
WO2015051251A1 (en) 2013-10-04 2015-04-09 Signal Pharmaceuticals, Llc A tor kinase inhibitor in the prevention or treatment of cancer characterized by gene mutations
US9512129B2 (en) 2014-04-16 2016-12-06 Signal Pharmaceuticals, Llc Solid forms comprising 1-ethyl-7-(2-methyl-6-(1H-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one and a coformer
NZ714742A (en) * 2014-04-16 2017-04-28 Signal Pharm Llc Solid forms of 1-ethyl-7-(2-methyl-6-(1h-1,2,4-triazol-3-yl)pyridin-3-yl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1h)-one, compositions thereof and methods of their use
US9737535B2 (en) 2014-04-16 2017-08-22 Signal Pharmaceuticals, Llc Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines
WO2015160882A1 (en) 2014-04-16 2015-10-22 Signal Pharmaceuticals, Llc SOLID FORMS COMPRISING 7-(6-(2-HYDROXYPROPAN-2YL) PYRIDIN-3-YL)-1-(TRANS)-4-METHOXYCYCLOHEXYL)-3, 4-DIHYDROPYRAZINO[2,3-b] PYRAZIN-2(1H)-ONE, AND A COFORMER, COMPOSITIONS AND METHODS OF USE THEREOF
NZ629796A (en) 2014-07-14 2015-12-24 Signal Pharm Llc Amorphous form of 4-((4-(cyclopentyloxy)-5-(2-methylbenzo[d]oxazol-6-yl)-7h-pyrrolo[2,3-d]pyrimidin-2-yl)amino)-3-methoxy-n-methylbenzamide, compositions thereof and methods of their use
AU2015289929A1 (en) 2014-07-14 2017-03-02 Signal Pharmaceuticals, Llc Methods of treating a cancer using substituted pyrrolopyrimidine compounds, compositions thereof
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
SG11201706287PA (en) 2015-02-20 2017-09-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
EA202090103A1 (ru) 2017-06-22 2020-04-24 Селджин Корпорейшн Лечение гепатоцеллюлярной карциномы, которая характеризуется вирусной инфекцией гепатита b
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
PE20210920A1 (es) 2018-05-04 2021-05-19 Incyte Corp Formas solidas de un inhibidor de fgfr y procesos para prepararlas
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202128685A (zh) 2019-10-14 2021-08-01 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
MX2022006691A (es) 2019-12-04 2022-09-19 Incyte Corp Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr).
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115151532B (zh) * 2020-04-29 2023-06-06 北京泰德制药股份有限公司 喹喔啉二酮衍生物作为kras g12c突变蛋白的不可逆抑制剂
WO2022166866A1 (zh) * 2021-02-08 2022-08-11 南京明德新药研发有限公司 二氢吡嗪并吡嗪类大环化合物
JP2024513575A (ja) 2021-04-12 2024-03-26 インサイト・コーポレイション Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法
TW202313611A (zh) 2021-06-09 2023-04-01 美商英塞特公司 作為fgfr抑制劑之三環雜環

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3507866A (en) 1967-08-08 1970-04-21 Merck & Co Inc 1h - imidazo(4,5-b)pyrazin - 2 - one and processes for their preparation
US3567725A (en) 1968-11-20 1971-03-02 Merck & Co Inc Process for preparation of 1h-imidazo-(4,5-b)pyrazin-2-ones
US4317909A (en) 1980-03-24 1982-03-02 Sterling Drug Inc. Preparation of 1,3-dihydro-5-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones
US4294836A (en) 1980-03-24 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]-pyridine-2-thiones and their cardiotonic use
US4294837A (en) 1980-03-28 1981-10-13 Sterling Drug Inc. 1,3-Dihydro-6-(pyridinyl)-2H-imidazo[4,5-b]pyridin-2-ones and -imidazo[4,5-b]pyridine-2-thiones and their cardiotonic use
US4309537A (en) 1980-03-28 1982-01-05 Sterling Drug Inc. Production of imidazo[4,5-b]pyridin-2-ones or thiones
GB8709448D0 (en) 1987-04-21 1987-05-28 Pfizer Ltd Heterobicyclic quinoline derivatives
JPS63275582A (ja) 1987-05-02 1988-11-14 Naade Kenkyusho:Kk 2−アミノイミダゾ〔4,5−b〕ピリジン誘導体の製造方法
DD262026A1 (de) 1987-07-10 1988-11-16 Akad Wissenschaften Ddr Verfahren zur herstellung von 4-substituierten 6-(pyrid-4-yl)-2,4-dihydro-1h-imidazo[4,5-b]pyrid-2-onen
FR2643903A1 (fr) 1989-03-03 1990-09-07 Union Pharma Scient Appl Nouveaux derives de benzimidazole, leurs procedes de preparation, intermediaires de synthese, compositions pharmaceutiques les contenant, utiles notamment pour le traitement des maladies cardiovasculaires, et des ulceres duodenaux
US4963561A (en) 1990-02-28 1990-10-16 Sterling Drug Inc. Imidazopyridines, their preparation and use
TW274550B (es) 1992-09-26 1996-04-21 Hoechst Ag
HUP0400257A2 (hu) * 1995-09-22 2004-05-28 Sumitomo Chemical Co., Ltd. Herbicid hatású pirazin-2-on-származékok, ezek alkalmazása és előállításuk során alkalmazható intermedierek
DE19601627A1 (de) 1996-01-18 1997-07-24 Bayer Ag Heteroatomhaltige Cyclopentanopyridyl-Oxazolidinone
US6031105A (en) * 1996-04-09 2000-02-29 Pfizer Inc Substituted pyridines
TR200001546T2 (tr) 1997-09-26 2000-10-23 Asta Medica Aktiengesellschaft Serin/treonin protein kinaz fonksiyonunu modüle etmek için azabenzimidazol esaslı bileşikler.
ZA9810490B (en) 1997-12-03 1999-05-20 Dainippon Pharmaceutical Co 2-Aryl-8-oxodihydropurine derivative process for the preparation thereof pharmaceutical composition containing the same and intermediate therefor
JP2003146987A (ja) 1999-05-31 2003-05-21 Dainippon Pharmaceut Co Ltd 2−アリールプリン−9−アセトアミド誘導体
JP3814125B2 (ja) 1999-06-02 2006-08-23 大日本住友製薬株式会社 2−アリール−8−オキソジヒドロプリン誘導体からなる医薬
JP2002100363A (ja) 2000-09-25 2002-04-05 Mitsubishi Chemicals Corp リチウム二次電池用正極材料、リチウム二次電池用正極及びリチウム二次電池
JP2002167387A (ja) 2000-11-29 2002-06-11 Dainippon Pharmaceut Co Ltd 2−(7,8−ジヒドロ−8−オキソ−9h−プリン−9−イル)酢酸誘導体
WO2002048152A2 (en) 2000-12-12 2002-06-20 Neurogen Corporation Spiro[isobenzofuran-1,4'-piperidin]-3-ones and 3h-spiroisobenzofuran-1,4'-piperidines
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
AU2002337047B2 (en) 2001-09-04 2008-01-10 Boehringer Ingelheim Pharma Gmbh & Co. Kg Novel dihydropteridinones, method for producing the same and the use thereof as medicaments
EP1438048A1 (en) 2001-10-18 2004-07-21 Boehringer Ingelheim Pharmaceuticals Inc. 1,4-disubstituted benzo-fused urea compounds as cytokine inhibitors
US7247621B2 (en) 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
CN1653077A (zh) 2002-05-06 2005-08-10 健亚生物科技公司 治疗c型肝炎病毒感染的核苷衍生物
US20040204420A1 (en) 2002-08-05 2004-10-14 Rana Tariq M. Compounds for modulating RNA interference
EP1556053A4 (en) 2002-10-31 2006-04-19 Amgen Inc ANTI-INFLAMMATORY AGENTS
RU2005118401A (ru) * 2002-11-12 2006-01-10 Байер Фармасьютикалс Корпорейшн (US) Производные индолилпиразинона, применимые для лечения гиперпролиферативных нарушений и заболеваний, связанных с ангиогенезом
WO2004065378A1 (en) 2003-01-17 2004-08-05 Warner-Lambert Company Llc 2-aminopyridine substituted heterocycles as inhibitors of cellular proliferation
DK1599478T3 (da) 2003-02-26 2007-09-17 Boehringer Ingelheim Pharma Dihydropteridinoner, fremgangsmåde til fremstilling af disse og anvendelse af disse som lægemiddel
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
EP2345657A1 (en) 2003-05-30 2011-07-20 Pharmasset, Inc. Modified fluorinated nucleoside analogues
ATE461196T1 (de) 2003-06-26 2010-04-15 Merck Sharp & Dohme Benzodiazepin-cgrp-rezeptor-antagonisten
CN101123968A (zh) 2004-06-04 2008-02-13 艾科斯有限公司 肥大细胞病的治疗方法
DE102004029784A1 (de) 2004-06-21 2006-01-05 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue 2-Benzylaminodihydropteridinone, Verfahren zur deren Herstellung und deren Verwendung als Arzneimittel
WO2006001266A1 (ja) 2004-06-23 2006-01-05 Banyu Pharmaceutical Co., Ltd. 2-アリールプリン誘導体の製造方法
GB0420719D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006036883A2 (en) 2004-09-24 2006-04-06 Janssen Pharmaceutica, N.V. Imidazo{4,5-b}pyrazinone inhibitors of protein kinases
JP5118972B2 (ja) 2004-10-29 2013-01-16 テイボテク・フアーマシユーチカルズ Hiv阻害性二環式ピリミジン誘導体
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
SE0403006D0 (sv) * 2004-12-09 2004-12-09 Biovitrum Ab New compounds
WO2006065703A1 (en) 2004-12-13 2006-06-22 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
DK1853588T3 (da) 2005-02-16 2008-09-15 Astrazeneca Ab Kemiske forbindelser
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
PL1869049T3 (pl) * 2005-03-21 2009-07-31 Lilly Co Eli Związki imidazopirydazyny
JP2008534689A (ja) 2005-04-05 2008-08-28 ファーマコペイア, インコーポレイテッド 免疫抑制のためのプリン及びイミダゾピリジン誘導体
GB0519245D0 (en) * 2005-09-20 2005-10-26 Vernalis R&D Ltd Purine compounds
TW200732331A (en) * 2005-12-28 2007-09-01 Takeda Pharmaceuticals Co Fused heterocyclic compound and use thereof
US7915271B2 (en) * 2005-12-30 2011-03-29 Merck Sharp & Dohme Corp. 1,3-oxazolidin-2-one derivatives useful as CETP inhibitors
US20090281075A1 (en) 2006-02-17 2009-11-12 Pharmacopeia, Inc. Isomeric purinones and 1h-imidazopyridinones as pkc-theta inhibitors
CN101454320B (zh) * 2006-04-21 2012-12-19 辉瑞产品公司 吡啶并[3,4-b]吡嗪酮
WO2008016669A2 (en) 2006-08-02 2008-02-07 Cytokinetics, Incorporated Certain chemical entities, compositions and methods
US20100144738A1 (en) 2006-09-05 2010-06-10 William Bornmann Inhibitors of c-met and uses thereof
JP5600004B2 (ja) 2006-09-05 2014-10-01 エモリー ユニバーシティー 感染の予防または治療のためのチロシンキナーゼ阻害剤
US7902187B2 (en) 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
AR063142A1 (es) 2006-10-04 2008-12-30 Pharmacopeia Inc Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen.
EP2457913B1 (en) * 2006-10-19 2017-04-19 Signal Pharmaceuticals, LLC Heteroaryl compounds, compositions thereof, and methods of treatment therewith
ES2383370T3 (es) 2006-10-19 2012-06-20 Signal Pharmaceuticals Llc Compuestos de heteroarilo, sus composiciones y uso de los mismos como inhibidores de proteína quinasa
SA08290245B1 (ar) * 2007-04-23 2012-02-12 استرازينيكا ايه بي مشتقات كربو كساميد جديدة من -n (8-اريل رباعي هيدرو نفثالين غير متجانس- 2- يل) أو -n (5-اريل كرومان غير متجانس -3-يل) لعلاج الألم
AR067027A1 (es) * 2007-06-19 2009-09-30 Astrazeneca Ab Derivados de 2, 3-dihidro-1h-pirrol[3, 4b]quinolin-1-ona, una composicion farmaceutica que los comprende y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la modulacion de la actividad del receptor gaba a.
JP2009046435A (ja) * 2007-08-21 2009-03-05 Mitsubishi Tanabe Pharma Corp グルココルチコイド受容体モジュレーター
US8067459B2 (en) * 2007-10-16 2011-11-29 Arqule, Inc. Lapachone compounds and methods of use thereof
EP2219646A4 (en) 2007-12-21 2010-12-22 Univ Rochester METHOD FOR MODIFYING THE LIFETIME OF EUKARYOTIC ORGANISMS
US8110578B2 (en) 2008-10-27 2012-02-07 Signal Pharmaceuticals, Llc Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway
EP2379561B1 (en) 2008-11-25 2015-11-04 University Of Rochester Mlk inhibitors and methods of use

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