JP6479476B2 - ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 - Google Patents

ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 Download PDF

Info

Publication number
JP6479476B2
JP6479476B2 JP2014558028A JP2014558028A JP6479476B2 JP 6479476 B2 JP6479476 B2 JP 6479476B2 JP 2014558028 A JP2014558028 A JP 2014558028A JP 2014558028 A JP2014558028 A JP 2014558028A JP 6479476 B2 JP6479476 B2 JP 6479476B2
Authority
JP
Japan
Prior art keywords
triazolo
pyrazin
ylamino
dihydro
dimethyl
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.)
Expired - Fee Related
Application number
JP2014558028A
Other languages
English (en)
Japanese (ja)
Other versions
JP2015508086A5 (cg-RX-API-DMAC7.html
JP2015508086A (ja
Inventor
ドイッチ，カール
クーン，ダニエル
ロス，タチアナ
ブルクドルフ，ラルス
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of JP2015508086A publication Critical patent/JP2015508086A/ja
Publication of JP2015508086A5 publication Critical patent/JP2015508086A5/ja
Application granted granted Critical
Publication of JP6479476B2 publication Critical patent/JP6479476B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
    • 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
    • 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
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P31/10—Antimycotics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Neurology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Obesity (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Transplantation (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Biotechnology (AREA)
JP2014558028A 2012-02-21 2013-01-22 ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 Expired - Fee Related JP6479476B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12001153 2012-02-21
EP12001153.1 2012-02-21
PCT/EP2013/000189 WO2013124026A1 (en) 2012-02-21 2013-01-22 8 - substituted 2 -amino - [1,2,4] triazolo [1, 5 -a] pyrazines as syk tryrosine kinase inhibitors and gcn2 serin kinase inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2017173002A Division JP2018039805A (ja) 2012-02-21 2017-09-08 ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類

Publications (3)

Publication Number Publication Date
JP2015508086A JP2015508086A (ja) 2015-03-16
JP2015508086A5 JP2015508086A5 (cg-RX-API-DMAC7.html) 2016-03-17
JP6479476B2 true JP6479476B2 (ja) 2019-03-06

Family

ID=47598786

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2014558028A Expired - Fee Related JP6479476B2 (ja) 2012-02-21 2013-01-22 ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類
JP2017173002A Withdrawn JP2018039805A (ja) 2012-02-21 2017-09-08 ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2017173002A Withdrawn JP2018039805A (ja) 2012-02-21 2017-09-08 ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類

Country Status (11)

Country Link
US (1) US9120804B2 (cg-RX-API-DMAC7.html)
EP (1) EP2817310B1 (cg-RX-API-DMAC7.html)
JP (2) JP6479476B2 (cg-RX-API-DMAC7.html)
CN (1) CN104114557B (cg-RX-API-DMAC7.html)
AR (1) AR090104A1 (cg-RX-API-DMAC7.html)
AU (1) AU2013224421B2 (cg-RX-API-DMAC7.html)
CA (1) CA2863723C (cg-RX-API-DMAC7.html)
ES (1) ES2674451T3 (cg-RX-API-DMAC7.html)
IL (1) IL233982A (cg-RX-API-DMAC7.html)
TW (1) TW201339165A (cg-RX-API-DMAC7.html)
WO (1) WO2013124026A1 (cg-RX-API-DMAC7.html)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9120804B2 (en) * 2012-02-21 2015-09-01 Merck Patent Gmbh 8-substituted 2-amino-[1,2,4] triazolo [1, 5-A] pyrazines as Syk tryrosine kinase inhibitors and GCN2 serin kinase inhibitors
NO2699580T3 (cg-RX-API-DMAC7.html) 2014-01-24 2018-02-24
US9901439B2 (en) * 2014-10-06 2018-02-27 Mark A. Anton Gore-Tex covered breast implants to minimize capsular reaction and infection while reducing palpability
EP3448522B1 (en) * 2016-04-29 2021-01-20 Iomet Pharma Ltd. Novel substituted imidazopyridine compounds as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan-2,3-dioxygenase
RS61996B1 (sr) 2016-12-22 2021-07-30 Calithera Biosciences Inc Kompozicije i postupci za inhibiranje aktivnosti arginaze
GB201709456D0 (en) * 2017-06-14 2017-07-26 Ucb Biopharma Sprl Therapeutic agents
KR20200115620A (ko) 2018-01-29 2020-10-07 메르크 파텐트 게엠베하 Gcn2 억제제 및 이의 용도
MX2020007799A (es) 2018-01-29 2020-09-18 Merck Patent Gmbh Inhibidores de cinasa no derrepresible de control de aminoacido general 2 (gcn2) y sus usos.
CA3089240A1 (en) * 2018-02-07 2019-08-15 Insmed Incorporated Certain (2s)-n-[(1s)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating anca associated vasculitides
KR102738945B1 (ko) 2018-03-01 2024-12-04 아스트라제네카 에이비이 (2s)-n-｛(1s)-1-시아노-2-[4-(3-메틸-2-옥소-2,3-디하이드로-1,3-벤족사졸-5-일)페닐]에틸｝-1,4-옥사제판-2-카복스아미드를 포함하는 약학 조성물
WO2019187942A1 (ja) * 2018-03-27 2019-10-03 本田技研工業株式会社 フッ化物イオン二次電池用正極活物質、当該活物質を用いた正極、およびフッ化物イオン二次電池、並びに当該活物質の製造方法
EP3556760A1 (en) * 2018-04-19 2019-10-23 F. Hoffmann-La Roche AG Spiro compounds
CN119751456A (zh) 2018-04-16 2025-04-04 C4医药公司 螺环化合物
EP3578561A1 (en) 2018-06-04 2019-12-11 F. Hoffmann-La Roche AG Spiro compounds
AU2019306532A1 (en) 2018-07-17 2021-03-04 Insmed Incorporated Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides for treating Lupus Nephritis
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
KR20230038697A (ko) * 2020-07-14 2023-03-21 우한 엘엘 사이언스 앤드 테크놀로지 디벨롭먼트 컴퍼니, 리미티드 Rock 억제제 및 이의 제조 방법과 용도
JP2024518530A (ja) * 2021-05-14 2024-05-01 ビーエム ファーマ コンサルティング ピーティーワイ リミテッド ウイルス感染の予防及び治療のための二環式複素環化合物
EP4359415A1 (en) * 2021-06-23 2024-05-01 Gilead Sciences, Inc. Diacylglyercol kinase modulating compounds
KR102659126B1 (ko) * 2022-03-24 2024-04-19 충남대학교산학협력단 항결핵 약학조성물
CN120584108A (zh) 2023-01-06 2025-09-02 英斯梅德股份有限公司 新型可逆dpp1抑制剂及其用途

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9624482D0 (en) 1995-12-18 1997-01-15 Zeneca Phaema S A Chemical compounds
WO1997030035A1 (en) 1996-02-13 1997-08-21 Zeneca Limited Quinazoline derivatives as vegf inhibitors
IL125954A (en) 1996-03-05 2003-06-24 Zeneca Ltd Quinazoline derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the manufacture of medicaments having an antiangiogenic and/or vascular permeability reducing effect
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
GB9714249D0 (en) 1997-07-08 1997-09-10 Angiogene Pharm Ltd Vascular damaging agents
GB9900334D0 (en) 1999-01-07 1999-02-24 Angiogene Pharm Ltd Tricylic vascular damaging agents
GB9900752D0 (en) 1999-01-15 1999-03-03 Angiogene Pharm Ltd Benzimidazole vascular damaging agents
NZ522074A (en) 2000-05-31 2004-06-25 Astrazeneca Ab Indole derivatives with vascular damaging activity
WO2002004434A1 (en) 2000-07-07 2002-01-17 Angiogene Pharmaceuticals Limited Colchinol derivatives as vascular damaging agents
EP1301498A1 (en) 2000-07-07 2003-04-16 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
US7834024B2 (en) 2007-03-26 2010-11-16 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
CN104230911A (zh) 2008-04-16 2014-12-24 波托拉医药品公司 作为syk或jak蛋白激酶抑制剂的2,6-二氨基-嘧啶-5-基甲酰胺类化合物
JP5512665B2 (ja) 2008-06-20 2014-06-04 ジェネンテック， インコーポレイテッド トリアゾロピリジンｊａｋ阻害剤化合物と方法
WO2010010184A1 (en) * 2008-07-25 2010-01-28 Galapagos Nv [1, 2, 4] triazolo [1, 5-a] pyridines as jak inhibitors
TWI453207B (zh) 2008-09-08 2014-09-21 Signal Pharm Llc 胺基三唑并吡啶，其組合物及使用其之治療方法
NZ597140A (en) * 2009-06-05 2014-01-31 Cephalon Inc Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
AU2010272578B2 (en) * 2009-07-15 2015-03-05 Cellzome Limited Substituted triazole and imidazole derivatives as gamma secretase modulators
AU2011206635B2 (en) * 2010-01-15 2015-01-22 Cellzome Limited Novel substituted triazole derivatives as gamma secretase modulators
US20110190269A1 (en) * 2010-02-01 2011-08-04 Karlheinz Baumann Gamma secretase modulators
US8486967B2 (en) * 2010-02-17 2013-07-16 Hoffmann-La Roche Inc. Heteroaryl substituted piperidines
JP4940370B2 (ja) * 2010-06-29 2012-05-30 キヤノン株式会社 電子写真感光体、プロセスカートリッジおよび電子写真装置
US9023851B2 (en) * 2010-08-27 2015-05-05 Merck Patent Gmbh Triazolopyrazine derivatives
US9120804B2 (en) * 2012-02-21 2015-09-01 Merck Patent Gmbh 8-substituted 2-amino-[1,2,4] triazolo [1, 5-A] pyrazines as Syk tryrosine kinase inhibitors and GCN2 serin kinase inhibitors

Also Published As

Publication number Publication date
US20150025058A1 (en) 2015-01-22
ES2674451T3 (es) 2018-06-29
JP2018039805A (ja) 2018-03-15
AU2013224421A1 (en) 2014-10-02
IL233982A (en) 2017-05-29
CN104114557A (zh) 2014-10-22
US9120804B2 (en) 2015-09-01
WO2013124026A8 (en) 2014-01-09
AR090104A1 (es) 2014-10-22
CA2863723A1 (en) 2013-08-29
WO2013124026A1 (en) 2013-08-29
JP2015508086A (ja) 2015-03-16
CN104114557B (zh) 2017-10-24
TW201339165A (zh) 2013-10-01
AU2013224421B2 (en) 2017-03-02
EP2817310A1 (en) 2014-12-31
CA2863723C (en) 2020-09-22
EP2817310B1 (en) 2018-03-21

Similar Documents

Publication Publication Date Title
JP6479476B2 (ja) ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類
US12162873B2 (en) Substituted nicotinimide inhibitors of BTK for treating cancer
AU2019211485B2 (en) GCN2 inhibitors and uses thereof
US9073940B2 (en) Tricyclic pyrazol amine derivatives
CN103068828B (zh) 三唑并吡嗪衍生物
TWI617560B (zh) PI3Kδ 抑制劑以及其應用和生產方法
JP6097770B2 (ja) フロピリジン誘導体
AU2013301865A1 (en) Pyridopyrimidine derivatives as protein kinase inhibitors
CA2862694C (en) Triazolo[4,5-d]pyrimidine derivatives
AU2013230286A1 (en) Triazolopyrazine derivatives
AU2014224975A1 (en) Triazolo(4,5-d)pyrimidine derivatives for the treatment of diseases such as cancer
HK1171742A (en) Tricyclic pyrazol amine derivatives

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20160121

A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20160121

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20160121

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20160818

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20160823

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20161124

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20161228

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20170508

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20170908

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20171023

A912 Re-examination (zenchi) completed and case transferred to appeal board

Free format text: JAPANESE INTERMEDIATE CODE: A912

Effective date: 20171215

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20180710

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20180809

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20181119

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20190206

R150 Certificate of patent or registration of utility model

Ref document number: 6479476

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees