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PE20171104A1 - Pirazolpiridinaminas como inhibidores de mknk1 y mknk2 - Google Patents

Pirazolpiridinaminas como inhibidores de mknk1 y mknk2

Info

Publication number
PE20171104A1
PE20171104A1 PE2017001100A PE2017001100A PE20171104A1 PE 20171104 A1 PE20171104 A1 PE 20171104A1 PE 2017001100 A PE2017001100 A PE 2017001100A PE 2017001100 A PE2017001100 A PE 2017001100A PE 20171104 A1 PE20171104 A1 PE 20171104A1
Authority
PE
Peru
Prior art keywords
mknk1
mknk2
inhibitors
hydrogen
pyridinamines
Prior art date
Application number
PE2017001100A
Other languages
English (en)
Inventor
Anja Giese
Ulrich Klar
Keith Graham
Georg Kettschau
Detlev Sulzle
Philip Lienau
Kirstin Petersen
Julien Lefranc
Nicole Schmidt
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 PE20171104A1 publication Critical patent/PE20171104A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • 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

Landscapes

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

Abstract

Se refiere a un compuesto de formula general I, donde: R1 es hidrogeno, halogeno, entre otros; R2 es hidrogeno, C1-C6 alquilo, entre otros; R3 es hidrogeno, C1-C6 alquilo, C3-C6 cicloalquilo, entre otros. Son compuestos preferidos: (RS) N,N-dimetil-4-(pirazolo[1,5-a]piridin-5-ilamino)-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidina-7-carboxamida; Acido (7S)-4-(pirazolo[1,5-a]piridin-5-ilamino)-5,6,7,8-tetrahidro[1]benzotieno[2,3-d]pirimidina-7-carboxilico; entre otros. Tambien se refiere a un metodo de preparacion y a una composicion farmaceutica. Dichos compuestos son derivados de pirazolpiridinamina inhibidores de las quinasas MKNK1 y MKNK2, siendo utiles en el tratamiento de trastornos hiperproliferativos, enfermedad inflamatoria, entre otros.
PE2017001100A 2014-12-19 2015-12-14 Pirazolpiridinaminas como inhibidores de mknk1 y mknk2 PE20171104A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14199096 2014-12-19
EP15187501 2015-09-29

Publications (1)

Publication Number Publication Date
PE20171104A1 true PE20171104A1 (es) 2017-08-07

Family

ID=54884024

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017001100A PE20171104A1 (es) 2014-12-19 2015-12-14 Pirazolpiridinaminas como inhibidores de mknk1 y mknk2

Country Status (27)

Country Link
US (1) US10487092B2 (es)
EP (1) EP3233866B1 (es)
JP (1) JP2018501250A (es)
KR (1) KR20170095985A (es)
CN (1) CN107250138A (es)
AU (1) AU2015366417A1 (es)
BR (1) BR112017013148A2 (es)
CA (1) CA2971242A1 (es)
CL (1) CL2017001615A1 (es)
CO (1) CO2017005968A2 (es)
CR (1) CR20170264A (es)
CU (1) CU20170086A7 (es)
DO (1) DOP2017000146A (es)
EA (1) EA201791363A1 (es)
EC (1) ECSP17038893A (es)
GT (1) GT201700138A (es)
IL (1) IL252686A0 (es)
MX (1) MX2017008161A (es)
NI (1) NI201700078A (es)
PE (1) PE20171104A1 (es)
PH (1) PH12017501133A1 (es)
SG (1) SG11201704916TA (es)
SV (1) SV2017005466A (es)
TN (1) TN2017000258A1 (es)
TW (1) TW201625648A (es)
UY (1) UY36460A (es)
WO (1) WO2016096721A1 (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
WO2017081003A1 (en) * 2015-11-12 2017-05-18 Bayer Pharma Aktiengesellschaft Substituted pyrazolopyridinamines
DK3582776T3 (da) 2017-02-14 2024-01-08 Effector Therapeutics Inc Piperidinsubstituerede mnk-hæmmere og dertil relaterede fremgangsmåder
CN113286592A (zh) 2018-10-24 2021-08-20 效应治疗股份有限公司 Mnk抑制剂的结晶形式
CN111803476A (zh) * 2020-08-14 2020-10-23 华中科技大学协和深圳医院 芬戈莫德用于抑制革兰阳性细菌活性的用途
IL301285A (en) 2020-09-10 2023-05-01 Precirix N V Antibody fragment against fap
US20230000986A1 (en) * 2021-07-01 2023-01-05 Board Of Regents, The University Of Texas System Mnk inhibitors and eif4e phosphorylation modulation to treat inflammatory pain in the aged
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
EP4518911A1 (en) 2022-05-02 2025-03-12 Precirix N.V. Pre-targeting

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5011472A (en) 1988-09-06 1991-04-30 Brown University Research Foundation Implantable delivery system for biological factors
CA2530281C (en) 2003-07-24 2013-02-12 Bayer Pharmaceuticals Corporation Substituted tetrahydrobenzothienopyrimidinamine compounds useful for treating hyper-proliferative disorders
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
EP3239154A1 (en) * 2011-01-10 2017-11-01 Nimbus Iris, Inc. Irak inhibitors and uses thereof
ES2592404T3 (es) * 2012-05-21 2016-11-30 Bayer Pharma Aktiengesellschaft Benzotienopirimidinas sustituidas
HK1206723A1 (en) * 2012-05-21 2016-01-15 Bayer Pharma Aktiengesellschaft Thienopyrimidines
CN104781251B (zh) * 2012-11-08 2016-12-14 百时美施贵宝公司 可作为激酶调节剂的经双环杂环取代的吡啶基化合物
CA2899665A1 (en) 2013-02-01 2014-08-07 Bayer Pharma Aktiengesellschaft Substituted thienopyrimidines and pharmaceutical use thereof

Also Published As

Publication number Publication date
EP3233866B1 (en) 2021-04-21
UY36460A (es) 2016-07-29
SG11201704916TA (en) 2017-07-28
GT201700138A (es) 2018-12-06
DOP2017000146A (es) 2017-07-31
ECSP17038893A (es) 2017-07-31
TN2017000258A1 (en) 2018-10-19
CU20170086A7 (es) 2017-11-07
SV2017005466A (es) 2018-10-02
CL2017001615A1 (es) 2018-03-16
WO2016096721A1 (en) 2016-06-23
JP2018501250A (ja) 2018-01-18
EA201791363A1 (ru) 2018-01-31
CN107250138A (zh) 2017-10-13
CR20170264A (es) 2017-07-21
PH12017501133A1 (en) 2017-11-27
US10487092B2 (en) 2019-11-26
BR112017013148A2 (pt) 2019-11-19
IL252686A0 (en) 2017-08-31
MX2017008161A (es) 2017-09-18
AU2015366417A1 (en) 2017-06-29
US20180162877A1 (en) 2018-06-14
EP3233866A1 (en) 2017-10-25
CA2971242A1 (en) 2016-06-23
NI201700078A (es) 2017-09-22
CO2017005968A2 (es) 2017-10-20
KR20170095985A (ko) 2017-08-23
TW201625648A (zh) 2016-07-16

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