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)
Inventor
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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Gruenenthal GmbH
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    • 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
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/28—Drugs 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
    • 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
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/10—Drugs 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
    • 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

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  • Health & Medical Sciences (AREA)
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  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • 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 2009-03-04
EP09003075.0 2009-03-04
PCT/EP2010/001299 WO2010099938A1 (en) 2009-03-04 2010-03-03 Sulfonylated tetrahydroazolopyrazines and their use as medicinal products

Publications (1)

Publication Number Publication Date
CN102341398A true CN102341398A (zh) 2012-02-01

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CN2010800106612A Pending CN102341398A (zh) 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

Country Status (15)

Country Link
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=)

Cited By (2)

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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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WO2012028331A1 (en) * 2010-09-03 2012-03-08 Grünenthal GmbH Substituted tetrahydropyrrolopyrazine derivatives
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
ES2704744T3 (es) 2012-06-13 2019-03-19 Incyte Holdings Corp Compuestos tricíclicos sustituidos como inhibidores de FGFR
IN2014DN09346A (https=) 2012-06-13 2015-07-17 Hoffmann La Roche
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
KR102179599B1 (ko) 2012-09-25 2020-11-19 에프. 호프만-라 로슈 아게 이환형 유도체
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
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
AR098414A1 (es) 2013-11-14 2016-05-26 Bristol Myers Squibb Co PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e
CN105764905B (zh) 2013-11-26 2019-06-07 豪夫迈·罗氏有限公司 新的八氢-环丁二烯并[1，2-c；3，4-c’]二吡咯-2基
CN106103446B (zh) 2014-03-26 2019-07-30 豪夫迈·罗氏有限公司 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物
WO2015144609A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 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
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
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
KR20180054830A (ko) 2015-09-24 2018-05-24 에프. 호프만-라 로슈 아게 오토탁신(atx) 억제제로서의 이환형 화합물
RU2018112230A (ru) 2015-09-24 2019-10-30 Ф. Хоффманн-Ля Рош Аг Бициклические соединения в качестве ингибиторов atx
CR20180057A (es) 2015-09-24 2018-04-02 Hoffmann La Roche Nuevos compuestos biciclicos como inhibidores duales de atx/ca.
AU2016328365B2 (en) 2015-09-24 2020-04-23 F. Hoffmann-La Roche Ag New bicyclic compounds as dual ATX/CA inhibitors
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018167113A1 (en) 2017-03-16 2018-09-20 F. Hoffmann-La Roche Ag New bicyclic compounds as atx inhibitors
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AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
PL3759109T3 (pl) 2018-02-26 2024-03-04 Gilead Sciences, Inc. Podstawione związki pirolizyny jako inhibitory replikacji hbv
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
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WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
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WO2021067374A1 (en) 2019-10-01 2021-04-08 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
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
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
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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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BRPI1010533A2 (pt) 2016-03-15
HK1160450A1 (en) 2012-08-17
TW201035102A (en) 2010-10-01
EP2403854A1 (en) 2012-01-11
AR075539A1 (es) 2011-04-20
MX305105B (es) 2012-11-12
US20100234387A1 (en) 2010-09-16
EP2403854B1 (en) 2013-09-11
PL2403854T3 (pl) 2014-02-28
JP2012519196A (ja) 2012-08-23
US8158628B2 (en) 2012-04-17
CA2754330A1 (en) 2010-09-10
RU2011140061A (ru) 2013-04-10
AU2010220561A1 (en) 2011-10-27
IL214911A0 (en) 2011-11-30
ES2437108T3 (es) 2014-01-08
WO2010099938A1 (en) 2010-09-10
MX2011008864A (es) 2011-09-15

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Application publication date: 20120201