KR20120034613A - 키나아제 억제제로서 사용을 위한 이미다조피라진 - Google Patents

키나아제 억제제로서 사용을 위한 이미다조피라진 Download PDF

Info

Publication number
KR20120034613A
KR20120034613A KR1020117027154A KR20117027154A KR20120034613A KR 20120034613 A KR20120034613 A KR 20120034613A KR 1020117027154 A KR1020117027154 A KR 1020117027154A KR 20117027154 A KR20117027154 A KR 20117027154A KR 20120034613 A KR20120034613 A KR 20120034613A
Authority
KR
South Korea
Prior art keywords
optionally substituted
alkyl
groups
substituents 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.)
Ceased
Application number
KR1020117027154A
Other languages
English (en)
Korean (ko)
Inventor
호아킨 패스토르 페르난데즈
소니아 마르티네즈 콘잘레스
율렌 오야르자발 산타마리나
Original Assignee
센트로 내셔널 드 인베스티가시오네스 온콜로지카스 (씨엔아이오)
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 센트로 내셔널 드 인베스티가시오네스 온콜로지카스 (씨엔아이오) filed Critical 센트로 내셔널 드 인베스티가시오네스 온콜로지카스 (씨엔아이오)
Publication of KR20120034613A publication Critical patent/KR20120034613A/ko
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P41/00—Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • C07D243/16—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals
    • C07D243/18—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines substituted in position 5 by aryl radicals substituted in position 2 by nitrogen, oxygen or sulfur atoms
    • C07D243/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pulmonology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Surgery (AREA)
  • AIDS & HIV (AREA)
KR1020117027154A 2009-04-16 2010-04-16 키나아제 억제제로서 사용을 위한 이미다조피라진 Ceased KR20120034613A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP09380079 2009-04-16
EP09380079.5 2009-04-16

Related Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020177028146A Division KR101792837B1 (ko) 2009-04-16 2010-04-16 키나아제 억제제로서 사용을 위한 이미다조피라진

Publications (1)

Publication Number Publication Date
KR20120034613A true KR20120034613A (ko) 2012-04-12

Family

ID=40940522

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020117027154A Ceased KR20120034613A (ko) 2009-04-16 2010-04-16 키나아제 억제제로서 사용을 위한 이미다조피라진
KR1020177028146A Active KR101792837B1 (ko) 2009-04-16 2010-04-16 키나아제 억제제로서 사용을 위한 이미다조피라진

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020177028146A Active KR101792837B1 (ko) 2009-04-16 2010-04-16 키나아제 억제제로서 사용을 위한 이미다조피라진

Country Status (17)

Country Link
US (1) US8778935B2 (enExample)
EP (1) EP2419429B1 (enExample)
JP (1) JP5805623B2 (enExample)
KR (2) KR20120034613A (enExample)
CN (1) CN102428087B (enExample)
AU (1) AU2010238361B2 (enExample)
BR (1) BRPI1014572B8 (enExample)
CA (1) CA2756759C (enExample)
DK (1) DK2419429T3 (enExample)
EA (1) EA022629B1 (enExample)
ES (1) ES2475091T3 (enExample)
IL (1) IL215297A (enExample)
MX (1) MX2011010915A (enExample)
NZ (1) NZ596185A (enExample)
SG (1) SG175195A1 (enExample)
WO (1) WO2010119264A1 (enExample)
ZA (1) ZA201107717B (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20190005876A (ko) * 2016-04-15 2019-01-16 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
KR20190095403A (ko) * 2016-12-21 2019-08-14 아세르타 파마. 비.브이. 브루톤 티로신 키나제의 이미다조피라진 저해제

Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8563573B2 (en) 2007-11-02 2013-10-22 Vertex Pharmaceuticals Incorporated Azaindole derivatives as CFTR modulators
CA2755285C (en) 2009-03-20 2014-02-11 Yunxin Y. Bo Inhibitors of pi3 kinase
PH12012500778A1 (en) 2009-10-30 2012-11-26 Janssen Pharmaceutica Nv IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
AR080754A1 (es) 2010-03-09 2012-05-09 Janssen Pharmaceutica Nv Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10
TW201200518A (en) * 2010-03-10 2012-01-01 Kalypsys Inc Heterocyclic inhibitors of histamine receptors for the treatment of disease
US8802868B2 (en) 2010-03-25 2014-08-12 Vertex Pharmaceuticals Incorporated Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide
RU2569678C2 (ru) 2010-04-22 2015-11-27 Вертекс Фармасьютикалз Инкорпорейтед Способ получения циклоалкилкарбоксамидо-индольных соединений
US20130131057A1 (en) 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
TWI617559B (zh) 2010-12-22 2018-03-11 江蘇恆瑞醫藥股份有限公司 2-芳基咪唑并[1,2-b]嗒.2-苯基咪唑并[1,2-a]吡啶,和2-苯基咪唑并[1,2-a]吡衍生物
EP2524918A1 (en) 2011-05-19 2012-11-21 Centro Nacional de Investigaciones Oncológicas (CNIO) Imidazopyrazines derivates as kinase inhibitors
JP6115962B2 (ja) 2011-06-27 2017-04-19 ヤンセン ファーマシューティカ エヌ.ベー. 1−アリール−4−メチル−[1,2,4]トリアゾロ[4,3−a]キノキサリン誘導体
PL2841075T3 (pl) 2012-04-26 2020-09-21 The General Hospital Corporation Środki i sposoby leczenia i zapobiegania rogowaceniu łojotokowemu
CN103450204B (zh) * 2012-05-31 2016-08-17 中国科学院上海药物研究所 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途
CN102675323B (zh) * 2012-06-01 2014-04-09 南京药石药物研发有限公司 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途
WO2014001314A1 (en) 2012-06-26 2014-01-03 Janssen Pharmaceutica Nv Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl- [1,2,4] triazolo [4,3-a] quinoxaline compounds and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders
AU2013289284B2 (en) 2012-07-09 2017-03-30 Janssen Pharmaceutica Nv Inhibitors of phosphodiesterase 10 enzyme
US9145411B2 (en) 2012-08-02 2015-09-29 Asana Biosciences, Llc Substituted amino-pyrimidine derivatives
WO2014186663A2 (en) * 2013-05-17 2014-11-20 The General Hospital Corporation Methods for detecting and treating variants of seborrheic keratoses
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
LT3105218T (lt) 2014-02-13 2019-12-10 Incyte Corp Ciklopropilaminai kaip lsd1 inhibitoriai
EP3392244A1 (en) 2014-02-13 2018-10-24 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
WO2015123424A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
PL3925607T5 (pl) 2014-04-15 2026-06-01 Vertex Pharmaceuticals Incorporated Kompozycje farmaceutyczne do leczenia chorób, w których pośredniczy mukowiscydozowy przezbłonowy regulator przewodnictwa
WO2016007736A1 (en) * 2014-07-10 2016-01-14 Incyte Corporation Imidazopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
PL236355B1 (pl) * 2015-04-02 2021-01-11 Celon Pharma Spolka Akcyjna Pochodne 7-(morfolin-4-ylo)pirazolo[1,5-α]pirymidyny jako inhibitory kinazy PI3
EA201792205A1 (ru) 2015-04-03 2018-02-28 Инсайт Корпорейшн Гетероциклические соединения как ингибиторы lsd1
DK3334709T3 (da) 2015-08-12 2025-02-03 Incyte Holdings Corp Salte af en lsd1-hæmmer
US20170107216A1 (en) 2015-10-19 2017-04-20 Incyte Corporation Heterocyclic compounds as immunomodulators
MD3377488T2 (ro) 2015-11-19 2023-02-28 Incyte Corp Compuși heterociclici ca imunomodulatori
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
CA3009474A1 (en) 2015-12-22 2017-06-29 Incyte Corporation Heterocyclic compounds as immunomodulators
CN105622526A (zh) * 2016-02-24 2016-06-01 湖北工业大学 一种2-氨基吡嗪衍生物的制备方法
CA3021678A1 (en) 2016-04-22 2017-10-26 Incyte Corporation Formulations of an lsd1 inhibitor
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
EP3464279B1 (en) 2016-05-26 2021-11-24 Incyte Corporation Heterocyclic compounds as immunomodulators
SG11201811414TA (en) 2016-06-20 2019-01-30 Incyte Corp Heterocyclic compounds as immunomodulators
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
US20180057486A1 (en) 2016-08-29 2018-03-01 Incyte Corporation Heterocyclic compounds as immunomodulators
MX394882B (es) * 2016-12-07 2025-03-24 Beigene Ltd Derivados de imidazo[1,5-a]pirazina como inhibidores de fosfatidilinositol-4,5-bisfosfato 3-quinasadelta (pi3kdelta)
WO2018119221A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Pyridine derivatives as immunomodulators
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
US10308644B2 (en) 2016-12-22 2019-06-04 Incyte Corporation Heterocyclic compounds as immunomodulators
WO2018119236A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Triazolo[1,5-a]pyridine derivatives as immunomodulators
EP4223369A1 (en) 2016-12-22 2023-08-09 Incyte Corporation Immunomodulator compounds and methods of use
WO2019048036A1 (en) 2017-09-06 2019-03-14 Biontech Ag SUBSTITUTED IMIDAZOQUINOLINES
NZ761680A (en) * 2017-09-08 2023-03-31 Beigene Ltd Imidazo[1,5-a]pyrazine derivatives as pi3kdelta inhibitors
KR102717072B1 (ko) 2017-10-18 2024-10-15 인사이트 코포레이션 Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체
CR20200464A (es) * 2018-03-08 2021-04-14 Incyte Corp Compuestos diólicos de aminopirazina como inhibidores de pi3k-y
SMT202300065T1 (it) 2018-03-30 2023-05-12 Incyte Corp Composti eterociclici come immunomodulatori
CN112752756B (zh) 2018-05-11 2024-06-25 因赛特公司 作为PD-L1免疫调节剂的四氢-咪唑并[4,5-c]吡啶衍生物
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
EP3623009A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Modulation of trf1 for brain cancer treatment
CA3112819A1 (en) 2018-09-13 2020-03-19 Fundacion Del Sector Publico Estatal Centro Nacional De Investigaciones Oncologicas Carlos Iii (F.S.P. Cnio) Modulation of trf1 for brain cancer treatment
EP3623370A1 (en) 2018-09-13 2020-03-18 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Novel trf1 modulators and analogues thereof
TW202115059A (zh) 2019-08-09 2021-04-16 美商英塞特公司 Pd—1/pd—l1抑制劑之鹽
JP7559059B2 (ja) 2019-09-30 2024-10-01 インサイト・コーポレイション 免疫調節剤としてのピリド[3,2-d]ピリミジン化合物
EP4058461A1 (en) 2019-11-11 2022-09-21 Incyte Corporation Salts and crystalline forms of a pd-1/pd-l1 inhibitor
US11718622B2 (en) 2020-03-16 2023-08-08 Exelixis Inc. Heterocyclic adenosine receptor antagonists
WO2022064458A1 (en) 2020-09-28 2022-03-31 1ST Biotherapeutics, Inc. Indazoles as hematopoietic progenitor kinase 1 (hpk1) inhibitors and methods of using same
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
IL302590A (en) 2020-11-06 2023-07-01 Incyte Corp Process for preparing PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
US11760756B2 (en) 2020-11-06 2023-09-19 Incyte Corporation Crystalline form of a PD-1/PD-L1 inhibitor
WO2022140647A1 (en) * 2020-12-23 2022-06-30 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
EP4049726A1 (en) 2021-02-25 2022-08-31 Fundación del Sector Público Estatal Centro Nacional de Investigaciones Oncológicas Carlos III (F.S.P. CNIO) Imidazo[1,2-a]pyrazines as inhibitors of haspin and therapeutic uses thereof
MX2023010941A (es) * 2021-03-17 2023-11-28 Janssen Sciences Ireland Unlimited Co Compuestos antibacterianos.

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2607813B1 (fr) 1986-12-05 1989-03-31 Montpellier I Universite Alkylamino-8 imidazo (1,2-a) pyrazines et derives, leur preparation et leur application en therapeutique
HUP0202648A3 (en) 1998-06-12 2003-02-28 Sod Conseils Rech Applic Imidazolyl derivatives, pharmaceutical compositions containing them and their use
US7566734B2 (en) 2000-08-01 2009-07-28 Societe De Conseils De Recherches Et D'applications Scientifiques, S.A.S. Imidazolyl derivatives
WO2002060492A1 (en) * 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
TWI312347B (en) 2001-02-08 2009-07-21 Eisai R&D Man Co Ltd Bicyclic nitrogen-containing condensed ring compounds
BR0309398A (pt) * 2002-04-19 2005-02-01 Cellular Genomics Inc Composto ou um seu sal, hidrato, solvato, forma cristalina, diastereÈmero, prodroga farmaceuticamente aceitável, ou misturas deles, composição farmacêutica, e, métodos para tratar uma condição envolvida com a cinase em um mamìfero, para tratar câncer, e para identificar uma cinase
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003270489A1 (en) 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
JP4799864B2 (ja) * 2002-09-23 2011-10-26 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン
US7189723B2 (en) * 2003-02-10 2007-03-13 Cgi Pharmaceuticals, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
GB0423653D0 (en) 2004-10-25 2004-11-24 Piramed Ltd Pharmaceutical compounds
EP1928237A4 (en) 2005-09-02 2011-03-09 Abbott Lab NEW HETEROCYCLES BASED ON IMIDAZO
CA2621983A1 (en) * 2005-09-09 2007-03-22 Schering Corporation Azafused cyclin dependent kinase inhibitors
WO2007096764A2 (en) 2006-02-27 2007-08-30 Glenmark Pharmaceuticals S.A. Bicyclic heteroaryl derivatives as cannabinoid receptor modulators
PL2041139T3 (pl) 2006-04-26 2012-05-31 Hoffmann La Roche Związki farmaceutyczne
JP2009539840A (ja) * 2006-06-06 2009-11-19 シェーリング コーポレイション プロテインキナーゼ阻害剤としてのイミダゾピラジン
WO2008059373A1 (en) 2006-11-17 2008-05-22 Raqualia Pharma Inc. Imidazo [1, 2-a] pyrazine derivatives and their use as acid pump antagonists
PE20090365A1 (es) 2007-06-14 2009-04-04 Schering Corp Imidazopirazinas como inhibidores de proteina quinasa
DE102007032349A1 (de) * 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20190005876A (ko) * 2016-04-15 2019-01-16 블루프린트 메디신즈 코포레이션 액티빈 수용체 유사 키나아제의 저해제
KR20190095403A (ko) * 2016-12-21 2019-08-14 아세르타 파마. 비.브이. 브루톤 티로신 키나제의 이미다조피라진 저해제

Also Published As

Publication number Publication date
CN102428087A (zh) 2012-04-25
JP2012524053A (ja) 2012-10-11
CA2756759C (en) 2017-11-07
HK1167142A1 (en) 2012-11-23
CN102428087B (zh) 2015-06-17
KR20170116250A (ko) 2017-10-18
US20120083492A1 (en) 2012-04-05
IL215297A0 (en) 2011-12-29
JP5805623B2 (ja) 2015-11-04
BRPI1014572B1 (pt) 2021-07-13
WO2010119264A1 (en) 2010-10-21
US8778935B2 (en) 2014-07-15
ES2475091T3 (es) 2014-07-10
EP2419429B1 (en) 2014-03-26
MX2011010915A (es) 2012-01-27
BRPI1014572A2 (pt) 2016-04-26
EA022629B1 (ru) 2016-02-29
AU2010238361B2 (en) 2015-08-06
SG175195A1 (en) 2011-11-28
ZA201107717B (en) 2015-08-26
IL215297A (en) 2016-08-31
AU2010238361A1 (en) 2011-11-10
NZ596185A (en) 2013-01-25
KR101792837B1 (ko) 2017-11-02
BRPI1014572B8 (pt) 2022-07-19
EP2419429A1 (en) 2012-02-22
DK2419429T3 (da) 2014-06-23
EA201101497A1 (ru) 2012-04-30
CA2756759A1 (en) 2010-10-21

Similar Documents

Publication Publication Date Title
KR101792837B1 (ko) 키나아제 억제제로서 사용을 위한 이미다조피라진
JP5752232B2 (ja) プロテインキナーゼ阻害剤としての置換ピロロトリアジン化合物
AU2009302360B2 (en) Imidazopyridazinecarbonitriles useful as kinase inhibitors
US20130131057A1 (en) New bicyclic compounds as pi3-k and mtor inhibitors
CN102388055B (zh) 咪唑并[2,1-b][1,3,4]噻二唑衍生物
TW202417455A (zh) 新穎三雜環化合物及藥學組成物
CN105916859A (zh) 杂环化合物
KR20160086930A (ko) 피롤로피롤론 유도체 및 bet 억제제로서의 그의 용도
CN111936144B (zh) Jak抑制剂
US11034696B2 (en) Compounds for inhibiting LRRK2 kinase activity
TW202023550A (zh) 作為vanin抑制劑之雜芳族化合物
EP2480549B1 (en) Fused imidazo[3,2-d]pyrazines as PI3 kinase inhibitors
US20240374606A1 (en) Substituted pyrazine-2-carboxamides as hpk1 inhibitors for the treatment of cancer
AU2015274285B2 (en) Pyrimidine compounds and methods using the same
TW202510855A (zh) 作為mrgprx2拮抗劑之雙環雜環化合物
HK1167142B (en) Imidazopyrazines as inhibitors of protein kinases
WO2024061118A1 (zh) 大环含氮冠醚化合物及其作为蛋白激酶抑制剂的应用
WO2012020227A1 (en) Tricyclic compounds for use as kinase inhibitors

Legal Events

Date Code Title Description
PA0105 International application

Patent event date: 20111115

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
A201 Request for examination
PA0201 Request for examination

Patent event code: PA02012R01D

Patent event date: 20150323

Comment text: Request for Examination of Application

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

Comment text: Notification of reason for refusal

Patent event date: 20160719

Patent event code: PE09021S01D

E601 Decision to refuse application
PE0601 Decision on rejection of patent

Patent event date: 20170228

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20160719

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I

E601 Decision to refuse application
E801 Decision on dismissal of amendment
PE0601 Decision on rejection of patent

Patent event date: 20170705

Comment text: Decision to Refuse Application

Patent event code: PE06012S01D

Patent event date: 20160719

Comment text: Notification of reason for refusal

Patent event code: PE06011S01I

PE0801 Dismissal of amendment

Patent event code: PE08012E01D

Comment text: Decision on Dismissal of Amendment

Patent event date: 20170705

Patent event code: PE08011R01I

Comment text: Amendment to Specification, etc.

Patent event date: 20170530

Patent event code: PE08011R01I

Comment text: Amendment to Specification, etc.

Patent event date: 20161019

Patent event code: PE08011R01I

Comment text: Amendment to Specification, etc.

Patent event date: 20150323

A107 Divisional application of patent
PA0104 Divisional application for international application

Comment text: Divisional Application for International Patent

Patent event code: PA01041R01D

Patent event date: 20170929