PE20160593A1 - Tienopirimidinas como inhibidores mknk1 y mknk2 - Google Patents

Tienopirimidinas como inhibidores mknk1 y mknk2

Info

Publication number
PE20160593A1
PE20160593A1 PE2016000657A PE2016000657A PE20160593A1 PE 20160593 A1 PE20160593 A1 PE 20160593A1 PE 2016000657 A PE2016000657 A PE 2016000657A PE 2016000657 A PE2016000657 A PE 2016000657A PE 20160593 A1 PE20160593 A1 PE 20160593A1
Authority
PE
Peru
Prior art keywords
mknk2
mknk1
pyrimidines
inhibitors
benzothieno
Prior art date
Application number
PE2016000657A
Other languages
English (en)
Inventor
Detlev Sulzle
Franziska Siegel
Kirstin Petersen
Florian Puehler
Ulrich Klar
Anja Richter
Keith Graham
Georg Kettschau
Lars Wortmann
Philip Lienau
Original Assignee
Bayer Pharma AG
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 Bayer Pharma AG filed Critical Bayer Pharma AG
Publication of PE20160593A1 publication Critical patent/PE20160593A1/es

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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

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

Abstract

Referida a derivados de tienopirimidina de formula I, donde: R1 es –C(=O)N(R3)(R4); R2a y R2b son H; R2c es H o halogeno; R2d es H, halogeno, entre otros.; R3 es C1-C6alquilo, C1-C6 alcoxi, entre otros; R4 es C1-C4alquilo, entre otros. Son compuestos preferidos: (7S)-4-(1H-indazol-5-ilamino)-N,N-dimetil-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidin-7-carboxamida; azetidin-1-il[(7S)-4-(1H-indazol-5-ilamino)-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidin-7-il]metanona, entre otros. dichos compuestos inhiben MKNK1 Y MKNK2, siendo utiles en el tratamiento de trastornos hiperproliferativos y/o angiogenesis.
PE2016000657A 2013-11-20 2014-11-17 Tienopirimidinas como inhibidores mknk1 y mknk2 PE20160593A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13193665 2013-11-20
EP14174731 2014-06-27

Publications (1)

Publication Number Publication Date
PE20160593A1 true PE20160593A1 (es) 2016-07-13

Family

ID=52000798

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2016000657A PE20160593A1 (es) 2013-11-20 2014-11-17 Tienopirimidinas como inhibidores mknk1 y mknk2

Country Status (22)

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

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
JP6888006B2 (ja) * 2015-10-29 2021-06-16 イーフェクター セラピューティクス， インコーポレイテッド Ｍｎｋ１およびｍｎｋ２を阻害するピロロ−、ピラゾロ−、イミダゾ−ピリミジンおよびピリジン化合物
JP6892444B2 (ja) * 2015-10-29 2021-06-23 イーフェクター セラピューティクス， インコーポレイテッド Ｍｎｋ１およびｍｎｋ２のイソインドリン、アザイソインドリン、ジヒドロインデノンならびにジヒドロアザインデノン阻害薬
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
EP3571206A1 (en) 2017-01-20 2019-11-27 Bayer Pharma Aktiengesellschaft Substituted imidazopyridinpyrimidines
EP3582776B1 (en) 2017-02-14 2023-11-08 Effector Therapeutics, Inc. Piperidine-substituted mnk inhibitors and methods related thereto
KR20210102211A (ko) 2018-10-24 2021-08-19 이펙터 테라퓨틱스, 인크. Mnk 억제제의 결정질 형태
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)

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Publication number Priority date Publication date Assignee Title
WO2002088138A1 (en) * 2001-04-30 2002-11-07 Bayer Corporation Novel 4-amino-5,6-substituted thiopheno[2,3-d]pyrimidines
ES2305435T3 (es) * 2002-01-10 2008-11-01 Bayer Healthcare Ag Inhibidores de la rho-quinasa.
JP4712702B2 (ja) * 2003-07-24 2011-06-29 バイエル・シエリング・フアーマ・アクチエンゲゼルシヤフト 高増殖性疾患を処置するために有用な置換されたテトラヒドロベンゾチエノピリミジンアミン化合物
JP5070053B2 (ja) * 2004-08-20 2012-11-07 バイエル・ファルマ・アクチェンゲゼルシャフト 新規な複素環
AR052019A1 (es) * 2004-10-15 2007-02-28 Bayer Pharmaceuticals Corp COMPUESTOS HETEROCICLICOS, PROCESOS DE PREPARACIoN Y MÉTODO PARA TRATAR ENFERMEDADES HIPERPROLIFERATIVAS
AU2006261082B2 (en) * 2005-06-22 2012-04-19 Boehringer Ingelheim International Gmbh Thienopyrimidines for pharmaceutical compositions
WO2007059905A2 (en) * 2005-11-25 2007-05-31 Develogen Aktiengesellschaft Thienopyrimidines treating inflammatory diseases
US8754079B2 (en) * 2010-02-26 2014-06-17 Boehringer Ingelheim International Gmbh Cycloalkyl containing thienopyrimidines for pharmaceutical compositions
CA2863259A1 (en) * 2012-01-10 2013-07-18 Nimbus Iris, Inc. Irak inhibitors and uses thereof
CA2873967A1 (en) * 2012-05-21 2013-11-28 Bayer Pharma Aktiengesellschaft Substituted benzothienopyrimidines
EP2852593A1 (en) * 2012-05-21 2015-04-01 Bayer Pharma Aktiengesellschaft Substituted pyrrolopyrimidines
CA2873975A1 (en) * 2012-05-21 2013-11-28 Bayer Pharma Aktiengesellschaft Thienopyrimidines
JP2016514087A (ja) * 2013-02-01 2016-05-19 バイエル・ファルマ・アクティエンゲゼルシャフト 置換チエノピリミジンおよびその薬学的使用
WO2015004024A1 (en) * 2013-07-08 2015-01-15 Bayer Pharma Aktiengesellschaft Substituted pyrazolo-pyridinamines

Also Published As

Publication number Publication date
IL245404A0 (en) 2016-06-30
EA201600398A1 (ru) 2016-10-31
MX2016006631A (es) 2016-08-17
TN2016000194A1 (en) 2017-10-06
WO2015074986A1 (en) 2015-05-28
AP2016009225A0 (en) 2016-05-31
CR20160235A (es) 2016-07-20
CU20160072A7 (es) 2016-10-28
PH12016500931A1 (en) 2016-06-27
BR112016011472A2 (pt) 2017-09-26
KR20160086404A (ko) 2016-07-19
EP3071577A1 (en) 2016-09-28
JP2016539113A (ja) 2016-12-15
AU2014352066A1 (en) 2016-05-26
DOP2016000118A (es) 2016-06-30
TW201605867A (zh) 2016-02-16
CL2016001218A1 (es) 2016-12-16
CN106061980A (zh) 2016-10-26
UY35848A (es) 2015-06-30
US20160297833A1 (en) 2016-10-13
CA2930873A1 (en) 2015-05-28

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