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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Emergency Medicine (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)
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
PT1966202E (pt) 2005-12-13 2012-01-03 Incyte Corp Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase
TW201100429A (en) 2009-05-22 2011-01-01 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
PL2432472T3 (pl) 2009-05-22 2020-03-31 Incyte Holdings Corporation 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK
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
WO2011029054A1 (en) 2009-09-04 2011-03-10 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
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2651417B1 (en) 2010-12-16 2016-11-30 Calchan Limited Ask1 inhibiting pyrrolopyrimidine derivatives
WO2012093169A1 (en) * 2011-01-07 2012-07-12 Leo Pharma A/S Novel sulfamide piperazine derivatives as protein tyrosine kinase inhibitors and pharmaceutical use thereof
WO2012127506A1 (en) 2011-03-22 2012-09-27 Advinus Therapeutics Limited Substituted fused tricyclic compounds, compositions and medicinal applications thereof
WO2012158785A1 (en) 2011-05-17 2012-11-22 Principia Biopharma Inc. Azaindole derivatives as tyrosine kinase inhibitors
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
US8993756B2 (en) * 2011-12-06 2015-03-31 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
CN104662015B (zh) * 2012-06-20 2017-03-29 诺华股份有限公司 补体途径调节剂及其用途
WO2014039714A2 (en) * 2012-09-06 2014-03-13 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP2015529242A (ja) 2012-09-21 2015-10-05 アドヴィヌス セラピューティクス リミテッドAdvinus Therapeutics Limited 置換された縮合三環式化合物、組成物およびその医薬用途
BR112015009942A2 (pt) * 2012-11-01 2017-07-11 Incyte Corp derivados de tiofeno fundidos tricíclicos como inibidores de jak
NZ708157A (en) 2012-11-15 2019-07-26 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備jak抑制劑之方法及中間物
WO2014146246A1 (en) * 2013-03-19 2014-09-25 Merck Sharp & Dohme Corp. Cycloalkyl nitrile pyrazolo pyridones as janus kinase inhibitors
BR112015023878A2 (pt) 2013-03-19 2017-07-18 Merck Sharp & Dohme composto, composição farmacêutica, e, uso de um composto
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
RU2015144385A (ru) * 2013-03-19 2017-04-26 Мерк Шарп И Доум Корп. Ациклические цианоэтилпиразолопиридоны в качестве ингибиторов янус-киназы
MX394928B (es) 2013-08-07 2025-03-24 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
US9233953B2 (en) * 2013-10-16 2016-01-12 Boehringer Ingelheim International Gmbh Derivatives of 4-(piperazinylcarbonyl)thiane-1, 1-dione which inhibit GlyT1
NZ720092A (en) * 2013-12-05 2019-05-31 Pfizer Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
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 (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
WO2016197027A1 (en) 2015-06-04 2016-12-08 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with mll proteins
CN114539284A (zh) 2016-03-16 2022-05-27 库拉肿瘤学公司 经取代的menin-mll抑制剂及使用方法
BR112018068702A2 (pt) 2016-03-16 2019-01-15 Kura Oncology Inc inibidores bicíclicos em ponte de menin-mll e métodos de uso
JOP20190024A1 (ar) 2016-08-26 2019-02-19 Gilead Sciences Inc مركبات بيروليزين بها استبدال واستخداماتها
RU2764980C2 (ru) * 2017-01-20 2022-01-24 Лео Фарма А/С Бициклические амины в качестве новых ингибиторов jak-киназы
US10799507B2 (en) 2017-02-03 2020-10-13 Leo Pharma A/S 5-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-5-azaspiro[2.5]octane-8-carboxylic acid derivatives as novel JAK kinase inhibitors
US11944627B2 (en) 2017-03-24 2024-04-02 Kura Oncology, Inc. Methods for treating hematological malignancies and Ewing's sarcoma
CN110662755A (zh) * 2017-05-23 2020-01-07 施万生物制药研发Ip有限责任公司 托法替尼的硫代氨基甲酸酯前药
US11542248B2 (en) 2017-06-08 2023-01-03 Kura Oncology, Inc. Methods and compositions for inhibiting the interaction of menin with MLL proteins
WO2019060365A1 (en) 2017-09-20 2019-03-28 Kura Oncology, Inc. SUBSTITUTED MÉNINE-MLL INHIBITORS AND METHODS OF USE
CN111566102B (zh) 2017-10-18 2023-09-08 缆图药品公司 作为激活素受体样激酶抑制剂的取代的吡咯并吡啶
JOP20180094A1 (ar) * 2017-10-18 2019-04-18 Hk Inno N Corp مركب حلقي غير متجانس كمثبط بروتين كيناز
PT3724196T (pt) 2017-12-15 2023-01-13 Union Therapeutics As Azetidina di-hidrotienopiridinas substituídas e a sua utilização como inibidores de fosfodiesterase
WO2019165374A1 (en) 2018-02-26 2019-08-29 Gilead Sciences, Inc. Substituted pyrrolizine compounds as hbv replication inhibitors
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
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
JP7629200B2 (ja) 2018-11-20 2025-02-13 ジョージタウン ユニバーシティ 神経変性、筋変性及びリソソーム蓄積障害を治療するための組成物及び方法
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.
CA3167999A1 (en) * 2020-03-17 2021-09-23 Xin Li Fused bicyclic derivative, preparation method therefor, and pharmaceutical use thereof
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
WO2022150446A1 (en) * 2021-01-07 2022-07-14 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
CA3212256A1 (en) * 2021-03-16 2022-09-22 Juhyun Lee 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
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
EP1087970B1 (en) 1998-06-19 2004-04-28 Pfizer Products Inc. PYRROLO 2,3-d]PYRIMIDINE COMPOUNDS
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CN1195755C (zh) 1999-12-10 2005-04-06 辉瑞产品公司 吡咯并[2,3-d]嘧啶化合物
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
NZ547327A (en) 2003-11-21 2009-08-28 Array Biopharma Inc AKT protein kinase inhibitors
MXPA06005882A (es) 2003-11-25 2006-06-27 Pfizer Prod Inc Metodo de tratamiento de la aterosclerosis.
CN1893952A (zh) 2003-12-17 2007-01-10 辉瑞产品公司 用于治疗移植排斥的吡咯并[2,3-d]嘧啶化合物
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
NZ564065A (en) 2005-05-20 2011-03-31 Vertex Pharma 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
ATE531718T1 (de) 2006-03-11 2011-11-15 Vernalis R&D Ltd Als hsp90-inhibitoren verwendete pyrrolopyrimidinderivate
CA2648250A1 (en) 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
WO2008005368A2 (en) * 2006-06-30 2008-01-10 Abbott Laboratories Piperazines as p2x7 antagonists
WO2008128072A2 (en) 2007-04-13 2008-10-23 Supergen, Inc. Axl kinase inhibitors useful for the treatment of cancer or hyperproliferative disorders
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
WO2009089352A1 (en) * 2008-01-08 2009-07-16 Array Biopharma Inc. Pyrrolopyridines as kinase inhibitors

Also Published As

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

Similar Documents

Publication Publication Date Title
TW201105674A (en) Novel JAK receptor and protein tyrosine kinase inhibitors and pharmaceutical use thereof
TWI334353B (en) 4-methylpyridopyrimidinone compounds
US8394820B2 (en) N-azabicyclic carboxamide derivatives, preparation thereof and therapeutic use thereof
CA1049515A (en) Derivatives of 1,7-dihydro-2h-pyrazolo (4',3':5,6) -pyrido(4,3-d) pyrimidine-2,4-(3h)-diones
AU2008254588B2 (en) Heterocyclic kinase modulators
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
CA2932008A1 (en) Fused tricyclic benzimidazoles derivatives as modulators of tnf activity
MX2007012393A (es) Derivados de purina e imidazopiridina para la inmunosupresion.
CA2727315A1 (en) Pyrrolo [2, 3-c] pyridine derivatives as p38 kinase inhibiting agents
AU2002211827B2 (en) Amino-substituted tetracyclic compounds useful as anti-inflammatory agents and pharmaceutical compositions comprising same
US20190100525A1 (en) Fused Pentacyclic Imidazole Derivatives as Modulators of TNF Activity
CN105814044A (zh) 作为tnf活性调节剂的四氢咪唑并吡啶衍生物
CN113747894B (zh) 成纤维细胞生长因子受体2(fgfr2)的降解剂
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
KR20250172652A (ko) 신경학적 및 정신의학적 장애의 치료에 유용한 무스카린성 아세틸콜린 수용체 m4의 양성 알로스테릭 조절제로서의 1,6-나프티리딘 유도체