NI201200066A - Métodos de síntesis y purificación de compuestos heteroarilos - Google Patents

Métodos de síntesis y purificación de compuestos heteroarilos

Info

Publication number
NI201200066A
NI201200066A NI201200066A NI201200066A NI201200066A NI 201200066 A NI201200066 A NI 201200066A NI 201200066 A NI201200066 A NI 201200066A NI 201200066 A NI201200066 A NI 201200066A NI 201200066 A NI201200066 A NI 201200066A
Authority
NI
Nicaragua
Prior art keywords
heteroaryl compounds
methods
purification
synthesis
conditions
Prior art date
Application number
NI201200066A
Other languages
English (en)
Inventor
L Harris Roy
Sapienza John
Shevlin Graziella
Papa Patrick
Packard Garrick
Zhao Jingjing
Mortensen Deborah
Riggs Jennifer
Perrin-Ninkovic Sophie
Elsner Jan
Choudhury Anusuya
Gingsee Lee Branden
Anthony Jokiel Patrick
Antonio Gamboa Juan
Georges Beauchamps Marie
Michael Kreilein Matthew
Atul Kothare Mohit
Pye Philip
Wei-Hwa Leong William
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 NI201200066A publication Critical patent/NI201200066A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J23/00—Catalysts comprising metals or metal oxides or hydroxides, not provided for in group B01J21/00
    • B01J23/16—Catalysts 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic 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
    • C07D241/14—Heterocyclic 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Hematology (AREA)
  • Materials Engineering (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Endocrinology (AREA)
  • Cardiology (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

Se proporcionan en el presente documento métodos para preparar Compuestos Heteroarilos que tienen la siguiente estructura: Fórmula (I) o Fórmula (II): en donde R1 - R4 son como se define en este documento. Los compuestos Heteroarilos son útiles para tratar o prevenir el cáncer, afecciones inflamatorias, afecciones inmunológicas, enfermedades neurodegenerativas, diabetes, obesidad, trastornos neurológicos, enfermedades relacionadas con la edad, o afecciones cardiovasculares.
NI201200066A 2009-10-26 2012-04-25 Métodos de síntesis y purificación de compuestos heteroarilos NI201200066A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US25491709P 2009-10-26 2009-10-26
US32848010P 2010-04-27 2010-04-27

Publications (1)

Publication Number Publication Date
NI201200066A true NI201200066A (es) 2012-08-13

Family

ID=43922466

Family Applications (1)

Application Number Title Priority Date Filing Date
NI201200066A NI201200066A (es) 2009-10-26 2012-04-25 Métodos de síntesis y purificación de compuestos heteroarilos

Country Status (23)

Country Link
US (3) US8569494B2 (es)
EP (2) EP3091021B1 (es)
JP (2) JP2013508456A (es)
KR (2) KR20120091240A (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) NZ618135A (es)
PH (2) PH12012500825A1 (es)
RU (1) RU2557242C2 (es)
SG (1) SG10201500511TA (es)
WO (1) WO2011053518A1 (es)
ZA (1) ZA201202959B (es)

Families Citing this family (61)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2300013B2 (en) 2008-05-21 2024-11-13 Takeda Pharmaceutical Company Limited Phosphorous derivatives as kinase inhibitors
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus 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
CA2743449C (en) 2008-11-12 2016-10-18 Ariad Pharmaceuticals, Inc. Pyrazinopyrazines and derivatives as kinase inhibitors
EP2704572B1 (en) 2011-05-04 2015-12-30 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
KR101978537B1 (ko) * 2011-10-19 2019-05-14 시그날 파마소티칼 엘엘씨 Tor 키나제 억제제를 사용한 암의 치료
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
US9403829B2 (en) * 2011-12-02 2016-08-02 Signal Pharmaceuticals, 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
JP6114317B2 (ja) 2012-02-24 2017-04-12 シグナル ファーマシューティカルズ，エルエルシー Ｔｏｒキナーゼ阻害剤の組合せ療法を用いて、非小細胞肺がんを処置する方法
WO2013138557A1 (en) 2012-03-15 2013-09-19 Signal Pharmaceuticals, Llc Treatment of cancer with tor kinase inhibitors
AU2013202993B2 (en) 2012-03-15 2015-09-03 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
MY198666A (en) 2012-03-15 2023-09-14 Signal Pharm Llc Treatment of cancer with tor kinase inhibitors
CN107137402A (zh) 2012-03-15 2017-09-08 西格诺药品有限公司 用tor激酶抑制剂治疗癌症
JP6469567B2 (ja) 2012-05-05 2019-02-13 アリアド・ファーマシューティカルズ・インコーポレイテッド Ｅｇｆｒ発動性がんの細胞増殖阻害用化合物
LT3495367T (lt) 2012-06-13 2021-02-25 Incyte Holdings Corporation Pakeistieji tricikliniai junginiai, kaip fgfr inhibitoriai
AU2015213397B2 (en) * 2012-10-18 2017-07-27 Signal Pharmaceuticals, Llc Treatment of cancer with TOR kinase inhibitors
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
MX2015009209A (es) 2013-01-16 2016-03-17 Signal Pharm Llc Compuestos sustituidos de pirrolopirimidina, composiciones de los mismos, y metodos de tratamiento con los mismos.
JP2016516671A (ja) * 2013-02-28 2016-06-09 シグナル ファーマシューティカルズ，エルエルシー Ｔｏｒキナーゼ阻害剤を用いたがんの治療
WO2014158650A1 (en) * 2013-03-13 2014-10-02 Dow Agrosciences Llc Preparation of 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
EP2986318A1 (en) * 2013-04-17 2016-02-24 Signal Pharmaceuticals, LLC Combination therapy comprising a tor kinase inhibitor and an imid compound for treating cancer
MX368286B (es) * 2013-04-17 2019-09-27 Signal Pharm Llc Terapia de combinacion que comprende un inhibidor de tor cinasa y un compuesto de quinazolinona 5-sustituida para tratar cancer.
CA2908353C (en) * 2013-04-17 2021-11-02 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
TW201526894A (zh) * 2013-04-17 2015-07-16 Signal Pharm Llc 藉二氫吡并吡治療癌症
CA2908957C (en) * 2013-04-17 2021-05-18 Signal Pharmaceuticals, Llc Combination therapy comprising a dihydropyrazino-pyrazine compound and an androgen receptor antagonist for treating prostate cancer
HK1221168A1 (zh) 2013-04-17 2017-05-26 西格诺药品有限公司 用於治疗癌症的包括tor激酶抑制剂和n-(3-(5-氟-2-(4-(2-甲氧基乙氧基)苯基氨基)嘧啶-4-基氨基)苯基)丙烯醯胺的组合疗法
EA030726B1 (ru) * 2013-04-17 2018-09-28 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи ФАРМАЦЕВТИЧЕСКИЕ СОСТАВЫ, СПОСОБЫ, ТВЕРДЫЕ ФОРМЫ И СПОСОБЫ ПРИМЕНЕНИЯ, ОТНОСЯЩИЕСЯ К 1-ЭТИЛ-7-(2-МЕТИЛ-6-(1H-1,2,4-ТРИАЗОЛ-3-ИЛ)ПИРИДИН-3-ИЛ)-3,4-ДИГИДРОПИРАЗИНО[2,3-b]ПИРАЗИН-2(1H)-ОНУ
US9505764B2 (en) * 2013-04-17 2016-11-29 Signal Pharmaceuticals, Llc Treatment of cancer with dihydropyrazino-pyrazines
AU2014254059B2 (en) * 2013-04-17 2019-06-06 Signal Pharmaceuticals, Llc Combination therapy comprising a TOR kinase inhibitor and a cytidine analog for treating cancer
LT2986610T (lt) 2013-04-19 2018-04-10 Incyte Holdings Corporation Bicikliniai heterociklai, kaip fgfr inhibitoriai
HK1223286A1 (zh) 2013-05-29 2017-07-28 西格诺药品有限公司 7-(6-(2-羟基丙-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)-酮的药物组合物、其固体形式及它们的使用方法
JP2016540726A (ja) 2013-10-04 2016-12-28 シグナル ファーマシューティカルズ，エルエルシー 遺伝子突然変異を特徴とする癌の予防又は治療におけるｔｏｒキナーゼ阻害剤
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
US9718824B2 (en) 2014-04-16 2017-08-01 Signal Pharmaceuticals, Llc Solid forms comprising 7-(6-(2-hydroxypropan-2-yl)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
EP3131552B1 (en) 2014-04-16 2020-07-15 Signal Pharmaceuticals, LLC Methods for treating cancer using tor kinase inhibitor combination therapy
JP2017511367A (ja) * 2014-04-16 2017-04-20 シグナル ファーマシューティカルズ，エルエルシー １−エチル−７−（２−メチル−６−（１Ｈ−１，２，４−トリアゾール−３−イル）ピリジン−３−イル）−３，４−ジヒドロピラジノ［２，３−ｂ］ピラジン−２（１Ｈ）−オン及び共形成物を含む固体形態、その組成物及び使用方法
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
EA201790189A1 (ru) 2014-07-14 2017-11-30 СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи Способы лечения злокачественного новообразования с использованием замещенных пирролопиримидиновых соединений, композиции на их основе
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
ES2959860T3 (es) 2017-06-22 2024-02-28 Celgene Corp Tratamiento del carcinoma hepatocelular caracterizado por la infección por el virus de la hepatitis B
MX2020011718A (es) 2018-05-04 2021-02-15 Incyte Corp Formas solidas de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr) y procesos para prepararlas.
ES3061844T3 (en) 2018-05-04 2026-04-07 Incyte Corp Salts of an fgfr inhibitor
US11628162B2 (en) 2019-03-08 2023-04-18 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
TWI891666B (zh) 2019-10-14 2025-08-01 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
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021113462A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Derivatives of an fgfr inhibitor
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
TW202200563A (zh) * 2020-04-29 2022-01-01 中國商北京泰德製藥股份有限公司 喹喔啉酮衍生物作為kras g12c突變蛋白的不可逆抑制劑
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
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
JP2024522189A (ja) 2021-06-09 2024-06-11 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての三環式ヘテロ環
EP4352060A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors

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
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
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
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
BR9610486A (pt) * 1995-09-22 1999-05-11 Sumitomo Chemical Co Derivados de pirazin-2-ona seu uso e intermediários para a sua produção
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
CA2305370C (en) 1997-09-26 2006-11-28 Zentaris Gmbh Azabenzimidazole-based compounds for modulating serine/threonine protein kinase function
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
EP1347982B1 (en) * 2000-12-12 2005-11-16 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
EA007062B1 (ru) 2001-09-04 2006-06-30 Бёрингер Ингельхайм Фарма Гмбх Унд Ко. Кг Новые дигидроптеридиноны, способы их получения и их применение в качестве лекарственных средств
JP2005506350A (ja) 2001-10-18 2005-03-03 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド サイトカイン阻害薬としての１，４−二置換ベンゾ−縮合尿素化合物
US7247621B2 (en) * 2002-04-30 2007-07-24 Valeant Research & Development Antiviral phosphonate compounds and methods therefor
KR20050006221A (ko) * 2002-05-06 2005-01-15 제네랩스 테크놀로지스, 인코포레이티드 Ｃ형 간염 바이러스 감염 치료용의 뉴클레오시드 유도체
WO2004042002A2 (en) 2002-08-05 2004-05-21 University Of Massachusetts Compounds for modulating rna interference
AU2003270701B2 (en) * 2002-10-31 2009-11-12 Amgen Inc. Antiinflammation 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
MXPA05007503A (es) 2003-01-17 2005-09-21 Warner Lambert Co Heterociclicos 2-aminopiridina sustituidos como inhibidores de proliferacion celular.
CA2517020C (en) 2003-02-26 2012-06-26 Boehringer Ingelheim Pharma Gmbh & Co. Kg Dihydropteridinones, method for the production and use thereof in the form of drugs
GB2400101A (en) 2003-03-28 2004-10-06 Biofocus Discovery Ltd Compounds capable of binding to the active site of protein kinases
BRPI0419345B8 (pt) 2003-05-30 2021-05-25 Gilead Pharmasset Llc uso do (2’r)-2’-desoxi-2’-flúor-2’-c-metil nucleosídeo e de uma composição farmacêutica que o compreende
WO2005013894A2 (en) * 2003-06-26 2005-02-17 Merck & Co., Inc. Benzodiazepine cgrp receptor antagonists
WO2005120511A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
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
US7855205B2 (en) 2004-10-29 2010-12-21 Janssen Pharmaceutica Nv Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders
US8153640B2 (en) 2004-10-29 2012-04-10 Tibotec Pharmaceuticals Ltd. HIV inhibiting bicyclic pyrimdine derivatives
SE0403006D0 (sv) * 2004-12-09 2004-12-09 Biovitrum Ab New compounds
EP1828186A1 (en) 2004-12-13 2007-09-05 Sunesis Pharmaceuticals, Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors
PT1853588E (pt) 2005-02-16 2008-08-25 Astrazeneca Ab Compostos químicos
WO2006091737A1 (en) 2005-02-24 2006-08-31 Kemia, Inc. Modulators of gsk-3 activity
PT1869049E (pt) * 2005-03-21 2009-05-26 Lilly Co Eli Compostos de imidazopiridazina
WO2006108103A1 (en) 2005-04-05 2006-10-12 Pharmacopeia, Inc. Purine and imidazopyridine derivatives for immunosuppression
GB0519245D0 (en) * 2005-09-20 2005-10-26 Vernalis R&D Ltd Purine compounds
JP2009523701A (ja) * 2005-12-28 2009-06-25 武田薬品工業株式会社 縮合複素環化合物およびその用途
WO2007079186A2 (en) * 2005-12-30 2007-07-12 Merck & Co., Inc. 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
NZ571540A (en) * 2006-04-21 2010-10-29 Pfizer Prod Inc Pyridine[3,4-b]pyrazinones for inhibiting PDE-5
DK2069352T5 (en) 2006-08-02 2017-04-03 Cytokinetics Inc SPECIFIC CHEMICAL UNITS, COMPOSITIONS AND PROCEDURES
EP2471529A3 (en) * 2006-09-05 2012-10-10 Emory University Kinase Inhibitors for Preventing or Treating Pathogen Infection and Method of Use Thereof
US20100144738A1 (en) * 2006-09-05 2010-06-10 William Bornmann Inhibitors of c-met and uses thereof
CL2007002866A1 (es) * 2006-10-04 2008-07-04 Pharmacopeia Inc Compuestos derivados de 6-sustituidos-2-(bencimidazolil) purina y purinona; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento de enfermedades autoinmunes, enfermedad inflamatoria, enfermedad mediada por m
US7902187B2 (en) * 2006-10-04 2011-03-08 Wyeth Llc 6-substituted 2-(benzimidazolyl)purine and purinone derivatives for immunosuppression
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
US7981893B2 (en) * 2006-10-19 2011-07-19 Signal Pharmaceuticals, Llc Heteroaryl compounds, compositions thereof, and methods of treatment therewith
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
TW200904817A (en) * 2007-06-19 2009-02-01 Astrazeneca Ab Compounds and uses thereof
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
US8642660B2 (en) * 2007-12-21 2014-02-04 The University Of Rochester Method for altering the lifespan 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
AU2009324894B2 (en) 2008-11-25 2015-04-09 University Of Rochester MLK inhibitors and methods of use

Also Published As

Publication number Publication date
ES2751705T3 (es) 2020-04-01
RU2012121806A (ru) 2013-12-10
KR101903925B1 (ko) 2018-10-02
MX2012004887A (es) 2012-06-08
ECSP12011831A (es) 2012-06-29
EP2493472B1 (en) 2016-12-07
US20130245254A1 (en) 2013-09-19
US8569494B2 (en) 2013-10-29
IL219368A (en) 2016-10-31
NZ599549A (en) 2013-11-29
US20140155593A1 (en) 2014-06-05
WO2011053518A1 (en) 2011-05-05
BR112012009751A2 (pt) 2020-09-24
IL219368A0 (en) 2012-06-28
JP2013508456A (ja) 2013-03-07
PH12014500392B1 (en) 2015-06-01
EP3091021B1 (en) 2019-08-28
KR20120091240A (ko) 2012-08-17
ZA201202959B (en) 2013-06-26
AU2010313585A1 (en) 2012-05-17
CN102686225A (zh) 2012-09-19
CN106117213A (zh) 2016-11-16
PH12012500825A1 (en) 2015-03-13
US20110137028A1 (en) 2011-06-09
MX341704B (es) 2016-08-31
EP3091021A1 (en) 2016-11-09
SG10201500511TA (en) 2015-03-30
US9079900B2 (en) 2015-07-14
AR078788A1 (es) 2011-11-30
CA2778615A1 (en) 2011-05-05
KR20170120196A (ko) 2017-10-30
AU2010313585B2 (en) 2015-11-26
MY177695A (en) 2020-09-23
CR20120211A (es) 2012-07-30
RU2557242C2 (ru) 2015-07-20
CO6541598A2 (es) 2012-10-16
US8686135B2 (en) 2014-04-01
CA2778615C (en) 2019-04-23
JP6338622B2 (ja) 2018-06-06
NZ618135A (en) 2015-05-29
JP2017014240A (ja) 2017-01-19
PH12014500392A1 (en) 2015-06-01
EP2493472A4 (en) 2013-03-13
EP2493472A1 (en) 2012-09-05
CN106117213B (zh) 2022-03-18
ES2613664T3 (es) 2017-05-25

Similar Documents

Publication Publication Date Title
CO6541598A2 (es) Métodos de síntesis y purificación de compuestos de heteroarilo
BR112012010253A2 (pt) compostos de pirimidina como moduladores do receptor delta opioide
CO6511283A2 (es) Primidinas sustituidas útiles en el tratamiento de enfermedades tales como cancer
CR20140071A (es) Nuevos compuestos de 4-piperidinilo para uso como inhibidores de la tankirasa
EA201290305A1 (ru) Производные трициклического пиразоламина
CU20120099A7 (es) Derivados de pirazina y su uso en el tratamiento de trastornos neurológicos
ECSP11011084A (es) INHIBIDORES DE mTOR CINASA PARA INDICADORES DE ONCOLOGÍA Y ENFERMEDADES ASOCIADAS CON LA TRAYECTORIA mTOR / PI3K / AKT
CU20110142A6 (es) Procedimiento para tratar enfermedades inflamatorias o alérgicas
MA32505B1 (fr) 5-alcynyl-pyrimidines
CO6480975A2 (es) Mimetico de smac
NI201100049A (es) Compuestos orgánicos.
CR11818A (es) Derivados de triazol utiles para el tratamiento de enfermedades
CL2012001461A1 (es) Compuestos derivados de difenil-pirazolopiridinas, moduladores del receptor nuclear nurr-1; compuestos intermediarios; composición farmacéutica; y su uso para el tratamiento y prevención de enfermedades neurodegenerativas, traumatismos cerebrales, enfermedades inflamatorias, osteoporosis, cáncer, entre otras.
MX2011009780A (es) Pirimidinas sustituidas para el tratamiento del cancer.
CO7310531A2 (es) 4-metil-2,3,8,9,9b-pentaaza-ciclopenta [a] naftalenos
IN2014DN05772A (es)
CR9347A (es) Derivados de pirimidina para el tratamiento de trastornos hiperproliferativos
MX2012001413A (es) Compuestos azaheterociclicos novedosos.
MX2016007128A (es) Compuestos del receptor 6 de quimiocina (ccr6).
EA201101675A1 (ru) Спироэпоксиды как промежуточные продукты синтеза
ECSP11010867A (es) Compuestos novedosos de fenilamino-isonicotinamida
UA107455C2 (uk) Похідні індолу як протиракові агенти
CY1117706T1 (el) Παραγωγα οξαζολινης και ισοξαζολινης ως ρυθμιστες crac
MX2012007835A (es) Derivados de oxazolopirimidina sustituida en 2, 5,7.
IN2012DN03846A (es)