EA007415B1 - Пирролопиримидины как ингибиторы протеинкиназы - Google Patents

Пирролопиримидины как ингибиторы протеинкиназы Download PDF

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Publication number
EA007415B1
EA007415B1 EA200400073A EA200400073A EA007415B1 EA 007415 B1 EA007415 B1 EA 007415B1 EA 200400073 A EA200400073 A EA 200400073A EA 200400073 A EA200400073 A EA 200400073A EA 007415 B1 EA007415 B1 EA 007415B1
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Prior art keywords
compound
compound according
effective amount
compounds
patient
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EA200400073A
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Russian (ru)
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EA200400073A1 (ru
Inventor
Пол Джозеф Кокс
Тахир Надим Маджид
Шелли Амендола
Стефани Даниель Депре
Крис Эдлин
Брайан Лесли Педгрифт
Фрэнк Халли
Майкл Эдвардз
Бернар Бодуэн
Лэйн МакФарлан Маклей
Дейвис Джон Алдос
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Авентис Фармасьютикалз Инк.
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Publication of EA200400073A1 publication Critical patent/EA200400073A1/ru
Publication of EA007415B1 publication Critical patent/EA007415B1/ru

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/14Decongestants or antiallergics
    • 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
    • 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
    • A61P37/08Antiallergic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA200400073A 2001-06-23 2002-06-21 Пирролопиримидины как ингибиторы протеинкиназы EA007415B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0115393.1A GB0115393D0 (en) 2001-06-23 2001-06-23 Chemical compounds
US30167801P 2001-06-28 2001-06-28
PCT/GB2002/002835 WO2003000695A1 (en) 2001-06-23 2002-06-21 Pyrrolopyrimidines as protein kinase inhibitors

Publications (2)

Publication Number Publication Date
EA200400073A1 EA200400073A1 (ru) 2004-08-26
EA007415B1 true EA007415B1 (ru) 2006-10-27

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Application Number Title Priority Date Filing Date
EA200400073A EA007415B1 (ru) 2001-06-23 2002-06-21 Пирролопиримидины как ингибиторы протеинкиназы

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EP (1) EP1404676A1 (et)
JP (1) JP4344607B2 (et)
CN (1) CN1294135C (et)
AU (1) AU2002314325B8 (et)
BR (1) BR0210652A (et)
CA (1) CA2451932C (et)
CZ (1) CZ20033443A3 (et)
EA (1) EA007415B1 (et)
EC (1) ECSP034922A (et)
EE (1) EE05432B1 (et)
GB (1) GB0115393D0 (et)
HU (1) HUP0400300A3 (et)
ME (1) MEP19308A (et)
NZ (1) NZ529766A (et)
OA (1) OA12632A (et)
PL (1) PL374096A1 (et)
RS (1) RS51698B (et)
SK (1) SK15882003A3 (et)
TN (1) TNSN03144A1 (et)
TR (1) TR200302242T2 (et)
UA (1) UA76760C2 (et)
WO (1) WO2003000695A1 (et)

Cited By (8)

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US8962629B2 (en) 2008-06-10 2015-02-24 Abbvie Inc. Tricyclic compounds
US9879018B2 (en) 2015-10-16 2018-01-30 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl and solid state forms thereof
USRE47221E1 (en) 2009-12-01 2019-02-05 Abbvie Inc. Tricyclic compounds
US10550126B2 (en) 2015-10-16 2020-02-04 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11365198B2 (en) 2015-10-16 2022-06-21 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11512092B2 (en) 2015-10-16 2022-11-29 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11524964B2 (en) 2015-10-16 2022-12-13 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11773106B2 (en) 2015-10-16 2023-10-03 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof

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ES2445208T3 (es) 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias
WO2005047289A1 (en) * 2003-11-17 2005-05-26 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
JP2007512316A (ja) * 2003-11-25 2007-05-17 ファイザー・プロダクツ・インク アテローム性動脈硬化症の治療方法
JP2007533753A (ja) * 2004-04-23 2007-11-22 タケダ サン ディエゴ インコーポレイテッド インドール誘導体及びキナーゼ阻害剤としてのその使用
FR2876103B1 (fr) * 2004-10-01 2008-02-22 Aventis Pharma Sa Nouveaux derives bis-azaindoles, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de kinases
WO2006044687A2 (en) 2004-10-15 2006-04-27 Takeda San Diego, Inc. Kinase inhibitors
FR2878849B1 (fr) 2004-12-06 2008-09-12 Aventis Pharma Sa Indoles substitues, compositions les contenant, procede de fabrication et utilisation
WO2006135915A2 (en) 2005-06-13 2006-12-21 Rigel Pharmaceuticals, Inc. Methods and compositions for treating degenerative bone disorders
US8119655B2 (en) 2005-10-07 2012-02-21 Takeda Pharmaceutical Company Limited Kinase inhibitors
TWI468162B (zh) 2005-12-13 2015-01-11 英塞特公司 作為傑納斯激酶(JANUS KINASE)抑制劑之經雜芳基取代之吡咯并〔2,3-b〕吡啶及吡咯并〔2,3-b〕嘧啶
BRPI0719883A2 (pt) 2006-10-09 2015-05-05 Takeda Pharmaceutical Inibidores de quinase
SG10201509887UA (en) 2007-06-13 2016-01-28 Incyte Corp Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
US8349847B2 (en) 2008-01-11 2013-01-08 Durga Prasad Konakanchi Pyrazolo [3,4-D] pyrimidine derivatives as anti-cancer agents
EA025520B1 (ru) 2009-05-22 2017-01-30 Инсайт Холдингс Корпорейшн N-(ГЕТЕРО)АРИЛПИРРОЛИДИНОВЫЕ ПРОИЗВОДНЫЕ ПИРАЗОЛ-4-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ И ПИРРОЛ-3-ИЛ-ПИРРОЛО[2,3-d]ПИРИМИДИНОВ В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-КИНАЗЫ
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
WO2011018894A1 (en) * 2009-08-10 2011-02-17 Raqualia Pharma Inc. Pyrrolopyrimidine derivatives as potassium channel modulators
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2485589A4 (en) 2009-09-04 2013-02-06 Biogen Idec Inc HETEROARYARY INHIBITORS OF BTK
MX347851B (es) 2010-03-10 2017-05-16 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
EP2574168B9 (en) 2010-05-21 2016-10-05 Incyte Holdings Corporation Topical formulation for a jak inhibitor
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
WO2012068450A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CN102093364B (zh) * 2011-01-07 2015-01-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
CN103476776B (zh) * 2011-01-07 2016-09-28 北京赛林泰医药技术有限公司 作为FAK/Pyk2抑制剂的2,4-二氨基-6,7-二氢-5H-吡咯并[2,3]嘧啶衍生物
CA2839767A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
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
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US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
PL2877467T3 (pl) 2012-07-26 2017-08-31 Glaxo Group Limited 2-(azaindolo-2-ylo)benzoimidazole jako inhibitory pad4
US10227357B2 (en) 2012-09-06 2019-03-12 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
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CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
CN105026393A (zh) 2013-03-13 2015-11-04 艾伯维公司 Cdk9激酶抑制剂
JP2016516710A (ja) 2013-03-13 2016-06-09 アッヴィ・インコーポレイテッド ピリジン系cdk9キナーゼ阻害薬
WO2014160028A1 (en) * 2013-03-14 2014-10-02 Abbvie Inc. Pyrrolopyrimindine cdk9 kinase inhibitors
TW201446763A (zh) 2013-03-14 2014-12-16 Abbvie Inc 吡咯并[2,3-b]吡啶cdk9激酶抑制劑
CA2905935A1 (en) 2013-03-14 2014-09-25 Abbvie Inc. Pyrrolo[2,3-b]pyridine cdk9 kinase inhibitors
RS60469B1 (sr) 2013-08-07 2020-07-31 Incyte Corp Dozni oblici sa produženim oslobađanjem za jak1 inhibitor
CN104804001B9 (zh) * 2014-01-24 2022-02-08 江苏柯菲平医药股份有限公司 4-取代吡咯并[2,3-d]嘧啶化合物及其用途
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Cited By (37)

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US9365579B2 (en) 2008-06-10 2016-06-14 Abbvie Inc. Tricyclic compounds
US8962629B2 (en) 2008-06-10 2015-02-24 Abbvie Inc. Tricyclic compounds
USRE47221E1 (en) 2009-12-01 2019-02-05 Abbvie Inc. Tricyclic compounds
US11186584B2 (en) 2015-10-16 2021-11-30 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-n-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10344036B2 (en) 2015-10-16 2019-07-09 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-#a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-#carboxamide and solid state forms thereof
US9963459B1 (en) 2015-10-16 2018-05-08 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-alpla]pyrrolo[2,3-e]-pyrazin-8-YL)-N-(2,2,2-Trifluoroethyl)pyrrol and solid state forms thereof
US10017517B2 (en) 2015-10-16 2018-07-10 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluorethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US11198697B1 (en) 2015-10-16 2021-12-14 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10202393B2 (en) 2015-10-16 2019-02-12 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-α]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
US10202394B2 (en) 2015-10-16 2019-02-12 Abbvie Inc. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
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US10519164B2 (en) 2015-10-16 2019-12-31 Abbvie Inc. Processes for the preparation of (3S,4R)-3,ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof
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