EA201600398A1 - Тиенопиримидины в качестве ингибиторов mknk1 и mknk2 - Google Patents

Тиенопиримидины в качестве ингибиторов mknk1 и mknk2

Info

Publication number
EA201600398A1
EA201600398A1 EA201600398A EA201600398A EA201600398A1 EA 201600398 A1 EA201600398 A1 EA 201600398A1 EA 201600398 A EA201600398 A EA 201600398A EA 201600398 A EA201600398 A EA 201600398A EA 201600398 A1 EA201600398 A1 EA 201600398A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
tienopyrimidines
mknk1
mknk2
inhibitors
Prior art date
Application number
EA201600398A
Other languages
English (en)
Inventor
Ульрих Клар
Ларс Вортманн
Георг Кетчау
Кейт Грэм
Аня Рихтер
Филип Лино
Флориан Пьюлер
Кирстин Петерзен
Франциска Зигель
Детлев Зюльцле
Original Assignee
Байер Фарма Акциенгезельшафт
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 Байер Фарма Акциенгезельшафт filed Critical Байер Фарма Акциенгезельшафт
Publication of EA201600398A1 publication Critical patent/EA201600398A1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—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
    • A61K31/505—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
    • A61K31/5375—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
    • A61K31/655—Azo (—N=N—), diazo (=N2), azoxy (>N—O—N< or N(=O)—N<), azido (—N3) or diazoamino (—N=N—N<) compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящее изобретение относится к замещенным тиенопиримидиновым соединениям общей формулы (I)как описано и определено в настоящей заявке, к способам получения указанных соединений, к промежуточным соединениям, полезным для получения указанных соединений, к фармацевтическим композициям и комбинациям, содержащим указанные соединения, и к применению указанных соединений для изготовления фармацевтической композиции для лечения или профилактики заболевания, в частности, гиперпролиферативного нарушения и/или нарушения ангиогенеза, в виде единственного средства или в комбинации с другими активными компонентами.
EA201600398A 2013-11-20 2014-11-17 Тиенопиримидины в качестве ингибиторов mknk1 и mknk2 EA201600398A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13193665 2013-11-20
EP14174731 2014-06-27
PCT/EP2014/074722 WO2015074986A1 (en) 2013-11-20 2014-11-17 Thienopyrimidines as mknk1 and mknk2 inhibitors

Publications (1)

Publication Number Publication Date
EA201600398A1 true EA201600398A1 (ru) 2016-10-31

Family

ID=52000798

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201600398A EA201600398A1 (ru) 2013-11-20 2014-11-17 Тиенопиримидины в качестве ингибиторов mknk1 и mknk2

Country Status (22)

Country Link
US (1) US20160297833A1 (ru)
EP (1) EP3071577A1 (ru)
JP (1) JP2016539113A (ru)
KR (1) KR20160086404A (ru)
CN (1) CN106061980A (ru)
AP (1) AP2016009225A0 (ru)
AU (1) AU2014352066A1 (ru)
BR (1) BR112016011472A2 (ru)
CA (1) CA2930873A1 (ru)
CL (1) CL2016001218A1 (ru)
CR (1) CR20160235A (ru)
CU (1) CU20160072A7 (ru)
DO (1) DOP2016000118A (ru)
EA (1) EA201600398A1 (ru)
IL (1) IL245404A0 (ru)
MX (1) MX2016006631A (ru)
PE (1) PE20160593A1 (ru)
PH (1) PH12016500931A1 (ru)
TN (1) TN2016000194A1 (ru)
TW (1) TW201605867A (ru)
UY (1) UY35848A (ru)
WO (1) WO2015074986A1 (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法
CA3002558A1 (en) * 2015-10-29 2017-05-04 Effector Therapeutics, Inc. Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit mnk1 and mnk2
WO2017075394A1 (en) * 2015-10-29 2017-05-04 Effector Therapeutics, Inc. Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2
US10000487B2 (en) 2015-11-20 2018-06-19 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
CN106727587A (zh) * 2016-11-28 2017-05-31 李娜 一种治疗心律失常的药物组合物
WO2018134335A1 (en) 2017-01-20 2018-07-26 Bayer Pharma Aktiengesellschaft Substituted imidazopyridinpyrimidines
KR20190117013A (ko) 2017-02-14 2019-10-15 이펙터 테라퓨틱스, 인크. 피페리딘-치환된 Mnk 억제제 및 그와 관련된 방법
WO2020086713A1 (en) 2018-10-24 2020-04-30 Effector Therapeutics, Inc. Crystalline forms of mnk inhibitors
CN110981903A (zh) * 2019-11-28 2020-04-10 南京正济医药研究有限公司 一种艾日布林中间体化合物提高光学纯度的精制方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6849638B2 (en) * 2001-04-30 2005-02-01 Bayer Pharmaceuticals Corporation 4-amino-5,6-substituted thiopheno [2,3-d] pyrimidines, pharmaceutical compositions containing the same, and their use in the treatment or prevention of pde7b-mediated diseases and conditions
ES2305435T3 (es) * 2002-01-10 2008-11-01 Bayer Healthcare Ag Inhibidores de la rho-quinasa.
EP1651652B1 (en) * 2003-07-24 2006-12-27 Bayer Pharmaceuticals Corporation Substituted tetrahydrobenzothienopyrimidinamine compounds useful for treating hyper-proliferative disorders
US8207172B2 (en) * 2004-08-20 2012-06-26 Bayer Intellectual Property Gmbh Pyrimidinothienoindazoles useful for the treatment of hyperproliferative disorders
UY29161A1 (es) * 2004-10-15 2006-04-28 Bayer Pharmaceuticals Corp Nuevos heterociclos
US20100143341A1 (en) * 2005-06-22 2010-06-10 Develogen Aktiengesellschaft Thienopyrimidines for pharmaceutical compositions
WO2007059905A2 (en) * 2005-11-25 2007-05-31 Develogen Aktiengesellschaft Thienopyrimidines treating inflammatory diseases
AU2011219758A1 (en) * 2010-02-26 2012-08-16 Boehringer Ingelheim International Gmbh 4 - [cycloalkyloxy (hetero) arylamino] thieno [2, 3 - d] pyrimidines having Mnkl/ Mnk2 inhibiting activity for pharmaceutical compositions
CN104582705A (zh) * 2012-01-10 2015-04-29 林伯士艾瑞斯公司 白介素-1受体相关激酶(irak)抑制剂和其用途
CN104507950B (zh) * 2012-05-21 2017-03-22 拜耳医药股份有限公司 噻吩并嘧啶
US9296757B2 (en) * 2012-05-21 2016-03-29 Bayer Pharma Aktiengesellschaft Substituted benzothienopyrimidines
US20150133426A1 (en) * 2012-05-21 2015-05-14 Bayer Pharma Aktiengesellschaft Substituted pyrrolopyrimidines
EP2951187A1 (en) * 2013-02-01 2015-12-09 Bayer Pharma Aktiengesellschaft Substituted thienopyrimidines and pharmaceutical use thereof
AU2014289415A1 (en) * 2013-07-08 2016-01-21 Bayer Pharma Aktiengesellschaft Substituted pyrazolo-pyridinamines

Also Published As

Publication number Publication date
US20160297833A1 (en) 2016-10-13
AU2014352066A1 (en) 2016-05-26
WO2015074986A1 (en) 2015-05-28
KR20160086404A (ko) 2016-07-19
CA2930873A1 (en) 2015-05-28
EP3071577A1 (en) 2016-09-28
CU20160072A7 (es) 2016-10-28
CR20160235A (es) 2016-07-20
PE20160593A1 (es) 2016-07-13
DOP2016000118A (es) 2016-06-30
AP2016009225A0 (en) 2016-05-31
MX2016006631A (es) 2016-08-17
UY35848A (es) 2015-06-30
TW201605867A (zh) 2016-02-16
BR112016011472A2 (pt) 2017-09-26
PH12016500931A1 (en) 2016-06-27
TN2016000194A1 (en) 2017-10-06
IL245404A0 (en) 2016-06-30
JP2016539113A (ja) 2016-12-15
CL2016001218A1 (es) 2016-12-16
CN106061980A (zh) 2016-10-26

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