CN102574857B - 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物 - Google Patents

作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物 Download PDF

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Publication number
CN102574857B
CN102574857B CN201080039685.0A CN201080039685A CN102574857B CN 102574857 B CN102574857 B CN 102574857B CN 201080039685 A CN201080039685 A CN 201080039685A CN 102574857 B CN102574857 B CN 102574857B
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pyrrolo
pyrimidin
diaza
octane
spiro
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CN102574857A (zh
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S·F·尼尔森
D·R·格雷夫
C·里特斯嘉德
G·格鲁-索伦森
E·R·奥特森
T·D·波尔森
S·C·舒
A·穆雷
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Leo Pharma AS
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    • C07—ORGANIC CHEMISTRY
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    • 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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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
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    • 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
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    • 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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  • Chemical Kinetics & Catalysis (AREA)
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  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
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  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Emergency Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
CN201080039685.0A 2009-07-08 2010-07-08 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物 Expired - Fee Related CN102574857B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US22394309P 2009-07-08 2009-07-08
US61/223,943 2009-07-08
PCT/DK2010/000105 WO2011003418A1 (en) 2009-07-08 2010-07-08 Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors

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CN102574857A CN102574857A (zh) 2012-07-11
CN102574857B true CN102574857B (zh) 2015-06-10

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US (1) US9346809B2 (cg-RX-API-DMAC7.html)
EP (1) EP2451813B1 (cg-RX-API-DMAC7.html)
JP (1) JP5690823B2 (cg-RX-API-DMAC7.html)
CN (1) CN102574857B (cg-RX-API-DMAC7.html)
AR (1) AR077465A1 (cg-RX-API-DMAC7.html)
BR (1) BR112012000422A2 (cg-RX-API-DMAC7.html)
CA (1) CA2767079A1 (cg-RX-API-DMAC7.html)
TW (1) TW201105674A (cg-RX-API-DMAC7.html)
WO (1) WO2011003418A1 (cg-RX-API-DMAC7.html)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp 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 HETEROARYL-BTK INHIBITORS
CN102984941B (zh) 2009-09-04 2016-08-17 密执安大学评议会 用于治疗白血病的组合物和方法
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
ES2617339T3 (es) 2010-12-16 2017-06-16 Calchan Limited Derivados de pirrolopirimidina inhibidores de ASK1
US9233964B2 (en) * 2011-01-07 2016-01-12 Leo Pharma A/S Sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use therof
CN103547580B (zh) 2011-03-22 2016-12-07 阿迪维纳斯疗法有限公司 取代的稠合三环化合物、其组合物及医药用途
CN103502249A (zh) 2011-05-17 2014-01-08 普林斯匹亚生物制药公司 作为酪氨酸激酶抑制剂的氮杂吲哚衍生物
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
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
EP2788000B1 (en) * 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
EA201590053A1 (ru) * 2012-06-20 2015-08-31 Новартис Аг Модуляторы пути системы комплемента и их применение
EP2892534B8 (en) * 2012-09-06 2021-09-15 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
US9593115B2 (en) 2012-09-21 2017-03-14 Advinus Therapeutics Ltd. Substituted fused tricyclic compounds, compositions, and medicinal applications thereof
TWI646099B (zh) * 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
JP6305510B2 (ja) * 2013-03-19 2018-04-04 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． ヤヌスキナーゼ阻害剤としての非環式シアノエチルピラゾロピリドン
CN105189508B (zh) * 2013-03-19 2018-11-23 默沙东公司 作为janus激酶抑制剂的环烷基腈吡唑并吡啶酮
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
WO2014146492A1 (en) 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
US9233953B2 (en) * 2013-10-16 2016-01-12 Boehringer Ingelheim International Gmbh Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
SI3077395T1 (en) * 2013-12-05 2018-03-30 Pfizer Inc. Pyrrolo(2,3-d)pyrimidinyl, pyrrolo(2,3-b)pyrazinyl and pyrrolo(2,3-d)pyridinyl acrylamides
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
NO2721710T3 (cg-RX-API-DMAC7.html) 2014-08-21 2018-03-31
USRE49687E1 (en) 2014-09-09 2023-10-10 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
TWI703150B (zh) 2015-06-04 2020-09-01 美商庫拉腫瘤技術股份有限公司 用於抑制ｍｅｎｉｎ及ｍｌｌ蛋白之交互作用的方法及組合物
HK1246593A1 (zh) 2015-06-04 2018-09-14 Kura Oncology, Inc. 用於抑制menin蛋白与mll蛋白的相互作用的方法及组合物
PH12018501955B1 (en) 2016-03-16 2024-01-24 Kura Oncology Inc Bridged bicyclic inhibitors of menin-mll and methods of use
PL3429591T3 (pl) 2016-03-16 2023-07-17 Kura Oncology, Inc. Podstawione pochodne tieno[2,3-d]pirymidyny jako inhibitory meniny-mll i metody ich zastosowania
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
WO2018134352A1 (en) * 2017-01-20 2018-07-26 Leo Pharma A/S Bicyclic amines as novel jak kinase inhibitors
RU2761626C2 (ru) * 2017-02-03 2021-12-13 Лео Фарма А/С ПРОИЗВОДНЫЕ 5-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-5-АЗАСПИРО[2.5]ОКТАН-8-КАРБОНОВОЙ КИСЛОТЫ В КАЧЕСТВЕ НОВЫХ ИНГИБИТОРОВ JAK-КИНАЗЫ
WO2018175746A1 (en) 2017-03-24 2018-09-27 Kura Oncology, Inc. Methods for treating hematological malignancies and ewing's sarcoma
EP3609903A1 (en) * 2017-05-23 2020-02-19 Theravance Biopharma R&D IP, LLC Thiocarbamate prodrugs of tofacitinib
WO2018226976A1 (en) 2017-06-08 2018-12-13 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
EP3684361A4 (en) 2017-09-20 2021-09-08 Kura Oncology, Inc. SUBSTITUTED INHIBITORS OF MENIN-MLL AND METHOD OF USING
EP3697786B1 (en) 2017-10-18 2022-08-31 Blueprint Medicines Corporation Substituted pyrrolopyridines as inhibitors of activin receptor-like kinase
KR20190043437A (ko) * 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
ES2935615T3 (es) 2017-12-15 2023-03-08 Union Therapeutics As Azetidina dihidrotienopiridinas sustituidas y su uso como inhibidores de la fosfodiesterasa
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
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
CN108456212A (zh) * 2018-05-30 2018-08-28 杨文思 一种化合物或其溶剂合物，或前体，或它们的药学上可接受的盐、药物及其用途
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CN120040470A (zh) 2018-11-20 2025-05-27 乔治敦大学 用于治疗神经退行性、肌退行性和溶酶体贮积病症的组合物和方法
KR102112336B1 (ko) * 2019-08-12 2020-05-18 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
MX2022002646A (es) 2019-09-05 2022-04-26 Incyte Corp Formulacion de ruxolitinib para la reduccion de comezon en dermatitis atopica.
CN115397815B (zh) * 2020-03-17 2024-06-14 江苏恒瑞医药股份有限公司 稠合二环类衍生物、其制备方法及其在医药上的应用
CN113698403B (zh) * 2020-05-21 2022-06-28 南京亘泰医药技术有限公司 (1r,4r,7r)-7-氨基-2-氮杂双环[2,2,1]庚烷衍生物及制备方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN114681461A (zh) * 2020-12-28 2022-07-01 杭州邦顺制药有限公司 用于红斑狼疮治疗的化合物
CN114681460A (zh) * 2020-12-28 2022-07-01 杭州邦顺制药有限公司 用于脓毒症治疗的化合物
US20240360157A1 (en) * 2021-01-07 2024-10-31 Biogen Ma Inc. Tyk2 inhibitors
CN117157293A (zh) * 2021-03-16 2023-12-01 怡诺安有限公司 作为蛋白激酶抑制剂的杂环化合物的新型盐及其用途
AU2022239128B2 (en) * 2021-03-16 2024-09-05 Hk Inno.N Corporation Novel salts of heterocyclic compound as protein kinase inhibitor and uses thereof
CN116514844A (zh) * 2022-01-20 2023-08-01 思路迪生物医药(上海)有限公司 一类噻吩并嘧啶类衍生物及其作为泛kras突变抑制剂的用途
WO2024211696A1 (en) * 2023-04-07 2024-10-10 Biogen Ma Inc. 1h-pyrrolo[2,3-b]pyridin-4-yl]-2-oxopyrrolidine-3-carbonitrile derivatives as tyrosine kinase 2 (tyk2) inhibitors for the treatment of inflammatory diseases
CN121532192A (zh) * 2023-06-02 2026-02-13 爱默发现股份有限公司 犬Janus激酶抑制剂及其用途

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999065908A1 (en) * 1998-06-19 1999-12-23 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS
WO1999065909A1 (en) * 1998-06-19 1999-12-23 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS
WO2009021169A2 (en) * 2007-08-08 2009-02-12 Lexicon Pharmaceuticals, Inc. (7h-pyrr0l0 [2, 3-d] pyrimidin-4-yl) -piperazines as kinase inhibitors for the treatment of cancer and inflammation

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60037345T2 (de) 1999-12-10 2008-11-13 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-Verbindungen
WO2003022214A2 (en) 2001-09-06 2003-03-20 Millennium Pharmaceuticals, Inc. Piperazine and homopiperazine compounds
JP4768265B2 (ja) 2002-10-15 2011-09-07 シンタ ファーマシューティカルズ コーポレーション 新規化合物
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
NZ590160A (en) 2003-11-21 2012-07-27 Array Biopharma Inc AKT protein kinase inhibitors
EP1689407A1 (en) 2003-11-25 2006-08-16 Pfizer Products Inc. Method of treatment of atherosclerosis
SG133602A1 (en) 2003-12-17 2007-07-30 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
TWI380816B (zh) 2004-04-13 2013-01-01 Synta Pharmaceuticals Corp 抑制介白素-１２（ｉｌ-１２）生成之二鹽抑制劑
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
JP4652826B2 (ja) 2005-01-14 2011-03-16 タッチパネル・システムズ株式会社 情報入力装置
KR20070104641A (ko) 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
WO2006091450A1 (en) 2005-02-18 2006-08-31 Lexicon Genetics Incorporated 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds
EP2354140A1 (en) 2005-05-20 2011-08-10 Vertex Pharmaceuticals Incorporated Pyrrolopyridines useful as inhibitors of protein kinase
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
EA200801968A1 (ru) 2006-03-11 2009-02-27 Вернэлис (Р&Д) Лтд. Пирролопиримидиновые производные, используемые в качестве ингибиторов hsp90
SG170828A1 (en) 2006-04-05 2011-05-30 Vertex Pharmaceuticals Inc Us Deazapurines useful as inhibitors of janus kinases
WO2008005368A2 (en) * 2006-06-30 2008-01-10 Abbott Laboratories Piperazines as p2x7 antagonists
EP2139869A2 (en) 2007-04-13 2010-01-06 SuperGen, Inc. Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders
CA2711614A1 (en) * 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999065908A1 (en) * 1998-06-19 1999-12-23 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS
WO1999065909A1 (en) * 1998-06-19 1999-12-23 Pfizer Products Inc. PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS
CN1305480A (zh) * 1998-06-19 2001-07-25 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物
CN1305479A (zh) * 1998-06-19 2001-07-25 辉瑞产品公司 吡咯并[2,3－d]嘧啶化合物
WO2009021169A2 (en) * 2007-08-08 2009-02-12 Lexicon Pharmaceuticals, Inc. (7h-pyrr0l0 [2, 3-d] pyrimidin-4-yl) -piperazines as kinase inhibitors for the treatment of cancer and inflammation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Jak inhibitor induces S phase cell-cycle arrest and augments TRAIL-induced apoptosis in human hepatocellular carcinoma cells;Hiroyuki Fuke，等;《Biochemical and Biophysical Research Communications》;20070921;第363卷(第3期);第738–744页 *

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