CN109937203A - 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 - Google Patents

一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 Download PDF

Info

Publication number
CN109937203A
CN109937203A CN201880004074.9A CN201880004074A CN109937203A CN 109937203 A CN109937203 A CN 109937203A CN 201880004074 A CN201880004074 A CN 201880004074A CN 109937203 A CN109937203 A CN 109937203A
Authority
CN
China
Prior art keywords
substituent group
alkyl
integer
independently selected
compound
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CN201880004074.9A
Other languages
English (en)
Other versions
CN109937203B (zh
Inventor
舒永志
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Meizer Pharmaceuticals Co ltd
Original Assignee
Shanghai Meizer Pharmaceuticals Co ltd
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 Shanghai Meizer Pharmaceuticals Co ltd filed Critical Shanghai Meizer Pharmaceuticals Co ltd
Publication of CN109937203A publication Critical patent/CN109937203A/zh
Application granted granted Critical
Publication of CN109937203B publication Critical patent/CN109937203B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/02Immunomodulators
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Neurology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

本发明提供了一类具有抑制并降解酪氨酸蛋白激酶JAK1或JAK2活性的化合物,具体地,本发明提供了一种如下式I所示的化合物;其中,各基团的定义如说明书中所述。本发明的化合物具有很好的JAK1或JAK2抑制及降解活性,可以用于制备治疗间JAK1或JAK2相关的疾病的药物。

Description

PCT国内申请,说明书已公开。

Claims (10)

  1. PCT国内申请,权利要求书已公开。
CN201880004074.9A 2017-09-03 2018-09-02 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物 Active CN109937203B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710783082.5A CN109422753B (zh) 2017-09-03 2017-09-03 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物
CN2017107830825 2017-09-03
PCT/CN2018/103707 WO2019042442A1 (zh) 2017-09-03 2018-09-02 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物

Publications (2)

Publication Number Publication Date
CN109937203A true CN109937203A (zh) 2019-06-25
CN109937203B CN109937203B (zh) 2021-07-23

Family

ID=65512924

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201710783082.5A Active CN109422753B (zh) 2017-09-03 2017-09-03 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物
CN201880004074.9A Active CN109937203B (zh) 2017-09-03 2018-09-02 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物

Family Applications Before (1)

Application Number Title Priority Date Filing Date
CN201710783082.5A Active CN109422753B (zh) 2017-09-03 2017-09-03 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物

Country Status (2)

Country Link
CN (2) CN109422753B (zh)
WO (1) WO2019042442A1 (zh)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20240050428A1 (en) * 2020-10-07 2024-02-15 Cullgen (Shanghai), Inc. Compounds and methods of treating cancers
CN114478532A (zh) * 2020-10-26 2022-05-13 上海美志医药科技有限公司 靶向降解Btk的化合物及其抗肿瘤用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140275031A1 (en) * 2010-03-10 2014-09-18 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP3035938A1 (en) * 2013-09-10 2016-06-29 Synta Pharmaceuticals Corp. Targeted therapeutics
CN106336413A (zh) * 2015-07-09 2017-01-18 广东东阳光药业有限公司 作为jak抑制剂的化合物及其用途
CN106432246A (zh) * 2015-08-05 2017-02-22 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2015201850B2 (en) * 2005-12-13 2017-03-02 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
US20070197590A1 (en) * 2006-01-31 2007-08-23 Demong Duane E Substituted dipiperidine ccr2 antagonists
NO2721710T3 (zh) * 2014-08-21 2018-03-31

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20140275031A1 (en) * 2010-03-10 2014-09-18 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP3035938A1 (en) * 2013-09-10 2016-06-29 Synta Pharmaceuticals Corp. Targeted therapeutics
CN106336413A (zh) * 2015-07-09 2017-01-18 广东东阳光药业有限公司 作为jak抑制剂的化合物及其用途
CN106432246A (zh) * 2015-08-05 2017-02-22 广东东阳光药业有限公司 杂芳化合物及其在药物中的应用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BING ZHOU,等: "Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression", 《J. MED. CHEM.》 *

Also Published As

Publication number Publication date
CN109422753A (zh) 2019-03-05
CN109422753B (zh) 2021-12-31
CN109937203B (zh) 2021-07-23
WO2019042442A1 (zh) 2019-03-07

Similar Documents

Publication Publication Date Title
CN109422752A (zh) 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物
CN109963844A (zh) 一类抑制并降解酪氨酸蛋白激酶alk的化合物
JP6946194B2 (ja) キナーゼを調節する化合物の固体形態
US11752154B2 (en) Pharmaceutical compositions comprising sepiapterin and uses thereof
CN109952304A (zh) 一类抑制并降解cdk的化合物
ES2929526T3 (es) Sal cristalina de L-arginina del ácido (R)-2-(7-(4-ciclopentil-3-(trifluorometil)benciloxi)-1,2,3,4-tetrahidrociclo-penta[b]indol-3-il)acético para su uso en trastornos asociados al receptor S1P1
CN110317192A (zh) 一类具有降解雄激素受体活性的化合物
BRPI0609962A2 (pt) composição farmacêutica oral, e, método para tratar um distúrbio em um mamìfero
US20220073516A1 (en) Crystalline spirocyclic compound, a dosage form containing, a method for using in treatment of disease, and a method for recrystallizing
KR20150041668A (ko) 이소티아졸로피리미디논을 사용하는 신경 발생을 자극하고 신경 변성을 억제하는 방법 및 조성물
KR102557184B1 (ko) 감각 유모 세포 사멸을 예방 또는 치료하기 위한 화합물 및 방법
JP2021513519A (ja) ムスカリン性アセチルコリン受容体m4のアンタゴニスト
JP2020530451A (ja) ムスカリン性アセチルコリン受容体m4のアンタゴニスト
US11767319B2 (en) Crystalline forms of a selective c-kit kinase inhibitor
JP2020537667A (ja) ムスカリン性アセチルコリン受容体m4のアンタゴニスト
TW202016110A (zh) Jak激酶家族之小分子抑制劑
CN109937203A (zh) 一类具有抑制并降解酪氨酸蛋白激酶jak1或jak2活性的化合物
CN109963853A (zh) 一类具有降解酪氨酸蛋白激酶jak3活性的化合物
CN109516990B (zh) 嘧啶并三氮唑类化合物、其制备方法和用途
JP2024504483A (ja) Jak阻害剤またはその塩もしくは結晶形を含有する経口製剤、並びにその製造方法及び用途
TW201831484A (zh) 巴瑞克替尼(Baricitinib)磷酸鹽晶型D及其藥物組合物
CN110407915A (zh) 一类具有抑制并降解Janus激酶(JAK1或JAK2)活性的化合物
TW202115070A (zh) 新穎的egfr抑制劑

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant