CN102341398A - 磺酰化四氢吡咯并吡嗪及其作为药物的用途 - Google Patents

磺酰化四氢吡咯并吡嗪及其作为药物的用途 Download PDF

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Publication number
CN102341398A
CN102341398A CN2010800106612A CN201080010661A CN102341398A CN 102341398 A CN102341398 A CN 102341398A CN 2010800106612 A CN2010800106612 A CN 2010800106612A CN 201080010661 A CN201080010661 A CN 201080010661A CN 102341398 A CN102341398 A CN 102341398A
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tetrahydro
methyl
pyrrolo
phenyl
pyrazin
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Chinese (zh)
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B·默拉
S·奥伯博施
M·赖希
S·顺克
R·约斯托克
S·赫斯
M·恩格尔斯
T·格曼
E·比斯特维尔德
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Gruenenthal GmbH
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    • 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
    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61P19/00Drugs for skeletal disorders
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    • AHUMAN NECESSITIES
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    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P3/00Drugs for disorders of the metabolism
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    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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  • Health & Medical Sciences (AREA)
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  • Neurosurgery (AREA)
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  • Rheumatology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN2010800106612A 2009-03-04 2010-03-03 磺酰化四氢吡咯并吡嗪及其作为药物的用途 Pending CN102341398A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09003075.0 2009-03-04
EP09003075 2009-03-04
PCT/EP2010/001299 WO2010099938A1 (en) 2009-03-04 2010-03-03 Sulfonylated tetrahydroazolopyrazines and their use as medicinal products

Publications (1)

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CN102341398A true CN102341398A (zh) 2012-02-01

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US (1) US8158628B2 (https=)
EP (1) EP2403854B1 (https=)
JP (1) JP2012519196A (https=)
CN (1) CN102341398A (https=)
AR (1) AR075539A1 (https=)
AU (1) AU2010220561A1 (https=)
BR (1) BRPI1010533A2 (https=)
CA (1) CA2754330A1 (https=)
ES (1) ES2437108T3 (https=)
IL (1) IL214911A0 (https=)
MX (1) MX305105B (https=)
PL (1) PL2403854T3 (https=)
RU (1) RU2011140061A (https=)
TW (1) TW201035102A (https=)
WO (1) WO2010099938A1 (https=)

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CN103113324A (zh) * 2013-02-07 2013-05-22 浙江工业大学 一种n-磺酰基取代的四氢吡咯类化合物的制备方法
CN119490446A (zh) * 2024-09-23 2025-02-21 苏州艾缇克药物化学有限公司 一种左旋舒必利的重要中间体(S)-2-Boc-氨甲基吡咯烷的合成方法

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US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
DE102011082013A1 (de) * 2011-09-01 2013-03-07 Bayer Pharma AG 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
CN104364239B (zh) 2012-06-13 2017-08-25 霍夫曼-拉罗奇有限公司 二氮杂螺环烷烃和氮杂螺环烷烃
RS58514B1 (sr) 2012-06-13 2019-04-30 Incyte Holdings Corp Supstituisana triciklična jedinjenja kao inhibitori fgfr
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
MX368615B (es) 2012-09-25 2019-10-09 Hoffmann La Roche Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos.
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
PH12015502383B1 (en) 2013-04-19 2023-02-03 Incyte Holdings Corp Bicyclic heterocycles as fgfr inhibitors
TW201605859A (zh) 2013-11-14 2016-02-16 必治妥美雅史谷比公司 作為酪蛋白激酶1δ/ε抑制劑之新穎經取代之吡唑并-哌
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
EA032357B1 (ru) 2014-03-26 2019-05-31 Ф. Хоффманн-Ля Рош Аг Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
TWI712601B (zh) 2015-02-20 2020-12-11 美商英塞特公司 作為fgfr抑制劑之雙環雜環
US9580423B2 (en) 2015-02-20 2017-02-28 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41898A (fr) 2015-04-10 2018-02-13 Hoffmann La Roche Dérivés de quinazolinone bicyclique
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
BR112017026682A2 (pt) 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
AU2016328436B2 (en) 2015-09-24 2020-05-14 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft Atx阻害剤としての二環式化合物
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ.ホフマン-ラ ロシュ アーゲー Atxインヒビターとしての新規二環式化合物
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
JP7050165B2 (ja) 2018-02-26 2022-04-07 ギリアード サイエンシーズ, インコーポレイテッド Hbv複製阻害剤としての置換ピロリジン化合物
AU2019262579B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Salts of an FGFR inhibitor
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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
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3157361A1 (en) 2019-10-14 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP7832891B2 (ja) 2019-12-04 2026-03-18 インサイト・コーポレイション Fgfr阻害剤の誘導体
US12012409B2 (en) 2020-01-15 2024-06-18 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
WO2022221170A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
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CN121175287A (zh) * 2023-03-29 2025-12-19 安道麦阿甘有限公司 用于制备胺中间体的方法

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103113324A (zh) * 2013-02-07 2013-05-22 浙江工业大学 一种n-磺酰基取代的四氢吡咯类化合物的制备方法
CN103113324B (zh) * 2013-02-07 2015-08-05 浙江工业大学 一种n-磺酰基取代的四氢吡咯类化合物的制备方法
CN119490446A (zh) * 2024-09-23 2025-02-21 苏州艾缇克药物化学有限公司 一种左旋舒必利的重要中间体(S)-2-Boc-氨甲基吡咯烷的合成方法

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PL2403854T3 (pl) 2014-02-28
JP2012519196A (ja) 2012-08-23
IL214911A0 (en) 2011-11-30
RU2011140061A (ru) 2013-04-10
EP2403854B1 (en) 2013-09-11
US20100234387A1 (en) 2010-09-16
AU2010220561A1 (en) 2011-10-27
AR075539A1 (es) 2011-04-20
HK1160450A1 (en) 2012-08-17
EP2403854A1 (en) 2012-01-11
ES2437108T3 (es) 2014-01-08
MX2011008864A (es) 2011-09-15
BRPI1010533A2 (pt) 2016-03-15
MX305105B (es) 2012-11-12
TW201035102A (en) 2010-10-01
CA2754330A1 (en) 2010-09-10
US8158628B2 (en) 2012-04-17
WO2010099938A1 (en) 2010-09-10

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Application publication date: 20120201