EA201401062A1 - Бициклические пиразиноновые производные - Google Patents

Бициклические пиразиноновые производные

Info

Publication number
EA201401062A1
EA201401062A1 EA201401062A EA201401062A EA201401062A1 EA 201401062 A1 EA201401062 A1 EA 201401062A1 EA 201401062 A EA201401062 A EA 201401062A EA 201401062 A EA201401062 A EA 201401062A EA 201401062 A1 EA201401062 A1 EA 201401062A1
Authority
EA
Eurasian Patent Office
Prior art keywords
bicyclic
pirazine
derivatives
pirazine derivatives
diseases
Prior art date
Application number
EA201401062A
Other languages
English (en)
Other versions
EA027416B1 (ru
Inventor
Дитер Дорш
Ханс-Петер Бухшталлер
Жерар Муане
Ансгар Вегенер
Original Assignee
Мерк Патент Гмбх
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48013911&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201401062(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of EA201401062A1 publication Critical patent/EA201401062A1/ru
Publication of EA027416B1 publication Critical patent/EA027416B1/ru

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
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • A61P35/00Antineoplastic 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
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Соединения формулы Iв которой R, X и Y имеют значения, указанные в п.1 формулы изобретения, являются ингибиторами танкиразы и могут применяться, среди прочего, для лечения заболеваний, таких как злокачественное новообразование, сердечно-сосудистые заболевания, поражения центральной нервной системы и различные формы воспаления.
EA201401062A 2012-03-28 2013-03-19 Бициклические пиразиноновые производные EA027416B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12002215 2012-03-28
PCT/EP2013/000827 WO2013143663A1 (en) 2012-03-28 2013-03-19 Bicyclic pyrazinone derivatives

Publications (2)

Publication Number Publication Date
EA201401062A1 true EA201401062A1 (ru) 2015-04-30
EA027416B1 EA027416B1 (ru) 2017-07-31

Family

ID=48013911

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201401062A EA027416B1 (ru) 2012-03-28 2013-03-19 Бициклические пиразиноновые производные

Country Status (32)

Country Link
US (1) US9120805B2 (ru)
EP (1) EP2831077B1 (ru)
JP (1) JP6096879B2 (ru)
KR (1) KR102070567B1 (ru)
CN (1) CN104169284B (ru)
AR (1) AR090496A1 (ru)
AU (1) AU2013242492B2 (ru)
CA (1) CA2868620C (ru)
CL (1) CL2014002557A1 (ru)
CO (1) CO7111292A2 (ru)
DK (1) DK2831077T3 (ru)
EA (1) EA027416B1 (ru)
EC (1) ECSP14024526A (ru)
ES (1) ES2585044T3 (ru)
HK (1) HK1203961A1 (ru)
HR (1) HRP20160908T1 (ru)
HU (1) HUE030067T2 (ru)
IL (1) IL234713A (ru)
MX (1) MX351149B (ru)
MY (1) MY172308A (ru)
NZ (1) NZ630489A (ru)
PE (1) PE20142186A1 (ru)
PH (1) PH12014501829A1 (ru)
PL (1) PL2831077T3 (ru)
PT (1) PT2831077T (ru)
RS (1) RS54997B1 (ru)
SG (1) SG11201405750YA (ru)
SI (1) SI2831077T1 (ru)
TW (1) TWI576346B (ru)
UA (1) UA112795C2 (ru)
WO (1) WO2013143663A1 (ru)
ZA (1) ZA201407828B (ru)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104302358B (zh) 2012-03-07 2017-12-05 癌症研究协会:皇家癌症医院 3‑芳基‑5‑取代的异喹啉‑1‑酮化合物和它们的治疗用途
CN104169284B (zh) 2012-03-28 2017-03-29 默克专利股份公司 双环吡嗪酮衍生物
KR20150011838A (ko) * 2012-06-20 2015-02-02 에프. 호프만-라 로슈 아게 탄키라아제 억제제로서의 피롤로피라존
WO2015036759A1 (en) 2013-09-11 2015-03-19 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
NO3087076T3 (ru) * 2013-12-23 2018-02-24
KR101739003B1 (ko) 2014-07-11 2017-05-23 에스티팜 주식회사 신규한 트리아졸로피리미디논 또는 트리아졸로피리디논 유도체, 및 이들의 용도
WO2016006974A2 (en) * 2014-07-11 2016-01-14 St Pharm Co., Ltd. Novel triazolopyrimidinone or triazolopyridinone derivatives, and use thereof
KR20160007347A (ko) 2014-07-11 2016-01-20 에스티팜 주식회사 신규한 이미다조트리아지논 또는 이미다조피라지논 유도체, 및 이들의 용도
WO2016006975A2 (en) * 2014-07-11 2016-01-14 St Pharm Co., Ltd. Novel imidazotriazinone or imidazopyrazinone derivatives, and use thereof
PT3227297T (pt) 2014-12-05 2021-04-09 Array Biopharma Inc Pirazol[1,5-a]pirazinas, substituídas nas posições 4 e 6, como inibidores de cinases janus
CU20180019A7 (es) 2015-08-17 2018-06-05 Lupin Ltd Derivados de heteroarilo como inhibidores de parp
CN109071546B (zh) 2016-02-24 2021-03-02 辉瑞大药厂 作为jak抑制剂的吡唑并[1,5-a]吡嗪-4-基衍生物
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
WO2019034973A1 (en) 2017-08-14 2019-02-21 Pfizer Inc. PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES
EA202092779A1 (ru) 2018-05-17 2021-02-02 Байер Акциенгезельшафт Замещенные дигидропиразолопиразинкарбоксамидные производные

Family Cites Families (22)

* 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
KR19990082463A (ko) 1996-02-13 1999-11-25 돈 리사 로얄 혈관 내피 성장 인자 억제제로서의 퀴나졸린유도체
CN1116286C (zh) 1996-03-05 2003-07-30 曾尼卡有限公司 4-苯胺基喹唑啉衍生物
GB9718972D0 (en) 1996-09-25 1997-11-12 Zeneca Ltd Chemical compounds
SE9702706D0 (sv) 1997-07-11 1997-07-11 Pharmacia & Upjohn Ab Prostaglandin derivatives devoid of side-effects for the treatment of glaucoma
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
IL152682A0 (en) 2000-05-31 2003-06-24 Astrazeneca Ab Indole derivatives with vascular damaging activity
PL359181A1 (en) 2000-07-07 2004-08-23 Angiogene Pharmaceuticals Limited Colchinol derivatives as angiogenesis inhibitors
CN1255391C (zh) 2000-07-07 2006-05-10 安吉奥金尼药品有限公司 作为血管破坏剂的colchinol衍生物
CA2652167A1 (en) * 2006-05-31 2007-12-06 Philip Jones Pyrrolo[1,2-a]pyrazin-1(2h)-one and pyrrolo[1,2-d][1,2,4]triazin-1(2h)-one derivatives as inhibitors of poly(adp-ribose)polymerase (parp)
JP5496680B2 (ja) * 2006-12-28 2014-05-21 アッヴィ・インコーポレイテッド ポリ(adp−リボース)ポリメラーゼの阻害剤
WO2008107478A1 (en) 2007-03-08 2008-09-12 Janssen Pharmaceutica Nv Quinolinone derivatives as parp and tank inhibitors
DE102007032349A1 (de) 2007-07-11 2009-01-15 Bayer Healthcare Ag Imidazo-, Pyrazolopyrazine und Imidazotriazine und ihre Verwendung
WO2009130232A1 (en) 2008-04-24 2009-10-29 Glaxo Group Limited Pyrazolo [1, 5 -a] pyrazine derivatives as antagonists of v1b receptors
WO2009130231A1 (en) 2008-04-24 2009-10-29 Glaxo Group Limited Pyrrolo [1, 2-a] pyrazine derivatives as vasopressin vib receptor antagonists
US8653097B2 (en) 2008-10-17 2014-02-18 Boehringer Ingelheim International Gmbh Tetra-aza-heterocycles as phosphatidylinositol-3-kinases (P13-kinases) inhibitor
US9073927B2 (en) 2010-01-22 2015-07-07 Fundacion Centro Nacional De Investigaciones Oncologicas Carlos Iii Inhibitors of PI3 kinase
WO2011130481A1 (en) * 2010-04-16 2011-10-20 Abbott Laboratories Pyrrolopyrazinone inhibitors of kinases
CN102229611B (zh) * 2011-04-26 2012-12-12 山东大学 2,6-二芳基吡唑并[1,5-a]吡嗪-4(5H)-酮化合物及其应用
CN104169284B (zh) 2012-03-28 2017-03-29 默克专利股份公司 双环吡嗪酮衍生物
KR20150011838A (ko) * 2012-06-20 2015-02-02 에프. 호프만-라 로슈 아게 탄키라아제 억제제로서의 피롤로피라존

Also Published As

Publication number Publication date
PH12014501829B1 (en) 2014-11-10
CA2868620C (en) 2020-02-25
CN104169284B (zh) 2017-03-29
EA027416B1 (ru) 2017-07-31
HRP20160908T1 (hr) 2016-09-23
MX351149B (es) 2017-10-04
AU2013242492B2 (en) 2016-12-15
SI2831077T1 (sl) 2016-09-30
AR090496A1 (es) 2014-11-19
JP6096879B2 (ja) 2017-03-15
KR20140140099A (ko) 2014-12-08
AU2013242492A1 (en) 2014-11-13
HK1203961A1 (en) 2015-11-06
ZA201407828B (en) 2015-12-23
PE20142186A1 (es) 2014-12-29
MX2014011420A (es) 2014-11-25
CA2868620A1 (en) 2013-10-03
CL2014002557A1 (es) 2014-12-19
SG11201405750YA (en) 2014-10-30
HUE030067T2 (en) 2017-04-28
UA112795C2 (uk) 2016-10-25
EP2831077B1 (en) 2016-04-27
US9120805B2 (en) 2015-09-01
ES2585044T3 (es) 2016-10-03
CO7111292A2 (es) 2014-11-10
ECSP14024526A (es) 2015-09-30
PH12014501829A1 (en) 2014-11-10
IL234713A (en) 2016-09-29
EP2831077A1 (en) 2015-02-04
TWI576346B (zh) 2017-04-01
DK2831077T3 (en) 2016-08-15
PL2831077T3 (pl) 2016-10-31
RS54997B1 (sr) 2016-11-30
MY172308A (en) 2019-11-21
KR102070567B1 (ko) 2020-01-29
JP2015511609A (ja) 2015-04-20
TW201343650A (zh) 2013-11-01
CN104169284A (zh) 2014-11-26
PT2831077T (pt) 2016-08-12
US20150057264A1 (en) 2015-02-26
WO2013143663A1 (en) 2013-10-03
NZ630489A (en) 2016-04-29

Similar Documents

Publication Publication Date Title
EA201401062A1 (ru) Бициклические пиразиноновые производные
EA201401212A1 (ru) Производные пирролотриазинона
EA201400879A1 (ru) Производные тетрагидрохиназолинона в качестве ингибиторов tank и parp
EA201590230A1 (ru) Соединения пиразолопиримидина в качестве ингибиторов киназ
EA201400333A1 (ru) Бензонитрильные производные в качестве ингибиторов киназ
MX362939B (es) Derivados de (aza-)isoquinolinona.
EA201301302A1 (ru) Производные пиридина и пиразина
EA201301301A1 (ru) Производные тиазола
MX362855B (es) Derivados de quinazolinona como inhidores poli (adp-ribosa) polimerasa (parp).
MX362215B (es) Derivados 2-aminopirido-[4,3-d]pirimidin-5-ona y su uso como inhibidores de wee-1.
EA201500278A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
EA201491623A1 (ru) Замещенные пирролидин-2-карбоксамиды
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201290807A1 (ru) Циклобутановые и метилциклобутановые производные в качестве ингибиторов янус-киназы
EA201691032A1 (ru) Производные изохромена в качестве ингибиторов фосфоинозитид-3-киназ
EA201300610A1 (ru) Хиназолинкарбоксамидазетидины
EA201590183A1 (ru) Производные азаиндола, выступающие в качестве ингибиторов pi3k
MX2016001136A (es) Derivados de oxoquinazolinil-butanamida.
EA201491376A1 (ru) Производные 1h-пирроло[2,3-b]пиридина и их применение в качестве ингибиторов киназы
MX2016014436A (es) Derivados de heterociclil-butanamida.
EA201790603A1 (ru) Ингибиторы гистондеметилазы
EA201290744A1 (ru) Имидазо[1,2-b][1,2,4]триазины в качестве c-met ингибиторов
MX2016001134A (es) Derivados 1,3-disustituidos de ciclopentano.
MX2016008042A (es) Derivados de imidazopirazinona.

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM