TW201105674A - Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof - Google Patents

Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof Download PDF

Info

Publication number
TW201105674A
TW201105674A TW099122542A TW99122542A TW201105674A TW 201105674 A TW201105674 A TW 201105674A TW 099122542 A TW099122542 A TW 099122542A TW 99122542 A TW99122542 A TW 99122542A TW 201105674 A TW201105674 A TW 201105674A
Authority
TW
Taiwan
Prior art keywords
diaza
pyrrolo
pyrimidin
spiro
oct
Prior art date
Application number
TW099122542A
Other languages
English (en)
Chinese (zh)
Inventor
Simon Feldbaek Nielsen
Daniel Rodriguez Greve
Carsten Ryttersgaard
Gunnar Grue-Sorensen
Erik Rytter Ottosen
Tina Dahlerup Poulsen
Soren Christian Schou
Anthony Murray
Original Assignee
Leo Pharma As
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 Leo Pharma As filed Critical Leo Pharma As
Publication of TW201105674A publication Critical patent/TW201105674A/zh

Links

Classifications

    • 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P11/06Antiasthmatics
    • 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
    • A61P17/04Antipruritics
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/08Antiseborrheics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/14Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/14Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
TW099122542A 2009-07-08 2010-07-08 Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof TW201105674A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22394309P 2009-07-08 2009-07-08

Publications (1)

Publication Number Publication Date
TW201105674A true TW201105674A (en) 2011-02-16

Family

ID=42542759

Family Applications (1)

Application Number Title Priority Date Filing Date
TW099122542A TW201105674A (en) 2009-07-08 2010-07-08 Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof

Country Status (9)

Country Link
US (1) US9346809B2 (enExample)
EP (1) EP2451813B1 (enExample)
JP (1) JP5690823B2 (enExample)
CN (1) CN102574857B (enExample)
AR (1) AR077465A1 (enExample)
BR (1) BR112012000422A2 (enExample)
CA (1) CA2767079A1 (enExample)
TW (1) TW201105674A (enExample)
WO (1) WO2011003418A1 (enExample)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
EP2432472B1 (en) 2009-05-22 2019-10-02 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
MY156727A (en) 2009-05-22 2016-03-15 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
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
US8993552B2 (en) 2009-09-04 2015-03-31 The Regents Of The University Of Michigan Compositions and methods for treatment of leukemia
WO2011029043A1 (en) 2009-09-04 2011-03-10 Biogen Idec Ma Inc. Heteroaryl btk inhibitors
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
JP5927201B2 (ja) 2010-12-16 2016-06-01 カルチャン リミテッド Ask1阻害ピロロピリミジン誘導体
KR20140058402A (ko) * 2011-01-07 2014-05-14 레오 파마 에이/에스 단백질 티로신 키나제 억제제로서의 신규한 설파미드 피페라진 유도체 및 이의 약제학적 용도
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
MX2013013331A (es) 2011-05-17 2014-10-17 Principia Biopharma Inc Derivados de azaindol como inhibidores de tirosina-cinasas.
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp 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
WO2013085802A1 (en) * 2011-12-06 2013-06-13 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
AU2013277154A1 (en) * 2012-06-20 2014-12-18 Jonathan E. Grob Complement pathway modulators and uses thereof
CN104981247A (zh) * 2012-09-06 2015-10-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
IN2015DN02008A (enExample) 2012-09-21 2015-08-14 Advinus Therapeutics Ltd
JP6359546B2 (ja) 2012-11-01 2018-07-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害薬としての三環式縮合チオフェン誘導体
TWI761825B (zh) 2012-11-15 2022-04-21 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
MX384910B (es) 2013-03-06 2025-03-14 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak.
WO2014146493A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Acyclic cyanoethylpyrazolo pyridones as janus kinase inhibitors
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
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
EP2976338B1 (en) 2013-03-19 2018-01-03 Merck Sharp & Dohme Corp. N-(2-cyano heterocyclyl)pyrazolo pyridones as janus kinase inhibitors
SG11201600815WA (en) 2013-08-07 2016-03-30 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
US9233953B2 (en) * 2013-10-16 2016-01-12 Boehringer Ingelheim International Gmbh Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
ES2654051T3 (es) * 2013-12-05 2018-02-12 Pfizer Inc. Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinil acrilamidas
BR112016025427A2 (pt) 2014-04-30 2017-08-15 Incyte Corp processos de preparação de um inibidor de jak1 e formas do mesmo
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
NO2721710T3 (enExample) * 2014-08-21 2018-03-31
WO2016040330A1 (en) 2014-09-09 2016-03-17 The Regents Of The University Of Michigan Thienopyrimidine and thienopyridine compounds and methods of use thereof
AR104020A1 (es) 2015-06-04 2017-06-21 Kura Oncology Inc Métodos y composiciones para inhibir la interacción de menina con proteínas mill
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
MX387806B (es) 2016-03-16 2025-03-19 Kura Oncology Inc Inhibidores biciclicos con puente sustituidos de menina-mll y metodos de uso
EP3429591B1 (en) 2016-03-16 2023-03-15 Kura Oncology, Inc. Substituted thieno[2,3-d]pyrimidine derivatives as inhibitors of menin-mll and methods of use
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
CN110291090A (zh) * 2017-01-20 2019-09-27 利奥制药有限公司 作为新型jak激酶抑制剂的双环胺
JP7101176B2 (ja) * 2017-02-03 2022-07-14 レオ ファーマ アクティーゼルスカブ 新規JAKキナーゼ阻害剤としての5-(7H-ピロロ[2,3-d]ピリミジン-4-イル)-5-アザスピロ[2.5]オクタン-8-カルボン酸誘導体
EP3601249A4 (en) 2017-03-24 2020-12-16 Kura Oncology, Inc. METHODS OF TREATMENT OF MALIGNANT HEMOPATHIES AND EWING'S SARCOMA
EP3609903A1 (en) * 2017-05-23 2020-02-19 Theravance Biopharma R&D IP, LLC Thiocarbamate prodrugs of tofacitinib
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
TW201920170A (zh) 2017-09-20 2019-06-01 美商庫拉腫瘤技術股份有限公司 經取代之menin-mll 抑制劑及使用方法
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
DK3724196T3 (da) * 2017-12-15 2023-01-16 Union Therapeutics As Substituerede azetidindihydrothienopyridiner og anvendelse deraf som phosphodiesterasehæmmere
KR102526964B1 (ko) 2018-02-26 2023-04-28 길리애드 사이언시즈, 인코포레이티드 Hbv 복제 억제제로서의 치환된 피롤리진 화합물
CN113768934A (zh) 2018-03-30 2021-12-10 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
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
CN113272308B (zh) 2018-11-20 2025-03-18 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
US11510923B2 (en) 2019-09-05 2022-11-29 Incyte Corporation Ruxolitinib formulation for reduction of itch in atopic dermatitis
CN118530260A (zh) * 2020-03-17 2024-08-23 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
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
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
JP7813290B2 (ja) * 2021-01-07 2026-02-12 バイオジェン・エムエイ・インコーポレイテッド Tyk2阻害剤
KR20220129494A (ko) * 2021-03-16 2022-09-23 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물의 신규 염 및 이들의 용도
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
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
JP2026513962A (ja) * 2023-04-07 2026-05-01 バイオジェン・エムエイ・インコーポレイテッド 炎症性疾患の処置のためのチロシンキナーゼ2(TYK2)阻害剤としての1H-ピロロ[2,3-b]ピリジン-4-イル]-2-オキソピロリジン-3-カルボニトリル誘導体
AU2024279063A1 (en) * 2023-06-02 2025-12-18 Animol Discovery, Inc. Inhibitors of canine janus kinase and uses thereof

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
PL198640B1 (pl) * 1998-06-19 2008-07-31 Pfizer Prod Inc Związki pirolo[2,3-d]pirymidynowe, środek farmaceutyczny i zastosowanie tych związków
EA006227B1 (ru) 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
US7115741B2 (en) 2001-09-06 2006-10-03 Levy Daniel E 4-thieno[2,3-D]pyrimidin-4-YL piperazine compounds
CA2502356A1 (en) 2002-10-15 2004-04-29 Synta Pharmaceuticals Corp. Aromatic bicyclic heterocyles to modulate 1l - 12 production
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050130954A1 (en) 2003-11-21 2005-06-16 Mitchell Ian S. AKT protein kinase inhibitors
CA2545192A1 (en) 2003-11-25 2005-06-09 Pfizer Products Inc. Method of treatment of atherosclerosis
CA2549485A1 (en) 2003-12-17 2005-07-07 Pfizer Products Inc. Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
US7745436B2 (en) 2004-04-13 2010-06-29 Synta Pharmaceuticals Corporation Disalt inhibitors of IL-12 production
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
EP1844050B1 (en) 2005-02-03 2009-01-14 Vertex Pharmaceuticals, Inc. Pyrrolopyrimidines useful as inhibitors of protein kinase
WO2006091450A1 (en) 2005-02-18 2006-08-31 Lexicon Genetics Incorporated 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds
KR20080016659A (ko) 2005-05-20 2008-02-21 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로서 유용한 피롤로피리딘
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
JP2009533323A (ja) 2006-03-11 2009-09-17 ヴァーナリス アールアンドディー リミテッド Hsp90阻害剤として用いられるピロロピリミジン誘導体
CA2648250A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
US20080076924A1 (en) * 2006-06-30 2008-03-27 Patrick Betschmann Piperazines as P2X7 antagonists
CA2682733A1 (en) 2007-04-13 2008-10-23 Supergen, Inc. Axl kinase inhibitors
PT2188289E (pt) * 2007-08-08 2015-12-21 Lexicon Pharmaceuticals Inc (7h-pirrolo[2,3-d]pirimidin-4-il)piperazinas como inibidores de quinases para o tratamento de cancro e de inflamação
CN101959887B (zh) * 2008-01-08 2013-07-31 阵列生物制药公司 作为激酶抑制剂的吡咯并吡啶

Also Published As

Publication number Publication date
EP2451813A1 (en) 2012-05-16
CN102574857B (zh) 2015-06-10
BR112012000422A2 (pt) 2017-05-09
JP5690823B2 (ja) 2015-03-25
EP2451813B1 (en) 2014-10-01
AR077465A1 (es) 2011-08-31
CA2767079A1 (en) 2011-01-13
US20120178740A1 (en) 2012-07-12
CN102574857A (zh) 2012-07-11
WO2011003418A1 (en) 2011-01-13
US9346809B2 (en) 2016-05-24
JP2012532152A (ja) 2012-12-13

Similar Documents

Publication Publication Date Title
CN102574857B (zh) 作为jak受体和蛋白酪氨酸激酶抑制剂的杂环化合物
TWI334353B (en) 4-methylpyridopyrimidinone compounds
US8394820B2 (en) N-azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof
CN101678014B (zh) 杂环激酶调节剂
CA1049515A (en) Derivatives of 1,7-dihydro-2h-pyrazolo (4',3':5,6) -pyrido(4,3-d) pyrimidine-2,4-(3h)-diones
TWI397530B (zh) 經取代的三唑并吡啶及其類似物
CN101379041B (zh) 含有苯并咪唑结构单元的三环n-杂芳基-甲酰胺衍生物,它们的制备与它们的治疗应用
US10669286B2 (en) Fused pentacyclic imidazole derivatives as modulators of TNF activity
CN102459242B (zh) 苯氧基甲基杂环化合物
TW200808325A (en) Novel compounds
AU2006350748A2 (en) 7-substituted purine derivatives for immunosuppression
TW200940542A (en) Pyrimidyl cyclopentanes as AKT protein kinase inhibitors
AU2009257712A1 (en) Pyrrolo [2, 3-c] pyridine derivatives as p38 kinase inhibiting agents
US10654861B2 (en) Fused pentacyclic imidazole derivatives as modulators of TNF activity
AU2002211827B2 (en) Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
CN105814044A (zh) 作为tnf活性调节剂的四氢咪唑并吡啶衍生物
TW201026701A (en) Pyrazolopyrimidine derivatives as histamine H4 receptor antagonists
CN110256420A (zh) 四氢吡啶并嘧啶衍生物及其制备方法和用途
KR20250174938A (ko) 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제로서의 티아졸로피리딘 유도체
CN101203516A (zh) 用于免疫抑制的嘌呤及咪唑并吡啶衍生物
CN116063305A (zh) 具有btk和/或ret活性的大环化合物及其在医药上的用途
HK1170734A (en) Heterocyclic compounds as jak receptor and protein tyrosine kinase inhibitors