AR077820A1 - Inhibidores de las jnk - Google Patents

Inhibidores de las jnk

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Publication number
AR077820A1
AR077820A1 ARP100102908A ARP100102908A AR077820A1 AR 077820 A1 AR077820 A1 AR 077820A1 AR P100102908 A ARP100102908 A AR P100102908A AR P100102908 A ARP100102908 A AR P100102908A AR 077820 A1 AR077820 A1 AR 077820A1
Authority
AR
Argentina
Prior art keywords
hydroxy
alkyl
haloalkyl
lower alkyl
alkoxy
Prior art date
Application number
ARP100102908A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR077820A1 publication Critical patent/AR077820A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen métodos y formulaciones para inhibir las JNK y tratar los trastornos mediados por las JNK y similares, con los compuestos y procesos para obtener dichos compuestos, y las correspondientes composiciones, aquí descritas. Reivindicacion 1: Un compuesto de la formula (1) o una sal farmacéuticamente aceptable del mismo, en la que: Y, es CH o N; X es CH o N; cada X1 es con independencia halogeno, alquilo inferior, alcoxi inferior, haloalquilo inferior o hidroxi; m es el numero 0, 1 o 2; X2 es H, alquilo inferior, alcoxi inferior, amido, haloalquilo inferior o haloalcoxi inferior; X3 es alquilo inferior, alcoxi inferior o haloalquilo inferior; p es el numero 0 o 1; cada X4 es con independencia alquilo inferior, alcoxi inferior, haloalquilo inferior, hidroxi, hidroxialquilo inferior, OC(=O)Z2 o halogeno; q es el numero 0, 1 o 2; X5 es alquilo inferior; s es el numero 0, 1 o 2; r es el numero 0 o 1; Y es H, OH, C(=O)Z2, C(=O)OZ2, OZ2, OC(=O)Z2, N(Z1)C(=O)(Z2), C(Z1)2S(O)2Z2, N(Z1)S(O)2Z2, N(Z1)S(O)2N(Z1)(Z2), C(Z1)2(Z2) o (C=O)N(Z1)(Z2); Z1 es H o Z1'; Z1' es alquilo inferior, opcionalmente sustituido por uno o más Z1ö; cada Z1ö es con independencia halogeno, hidroxi, haloalquilo inferior, dialquilamino o amino; Z2 es H o Z2'; Z2' es hidroxi, alquilo inferior, alcoxi inferior, hidroxialquilo inferior, haloalquilo inferior, cicloalquilo, cicloalquil-alquilo inferior, heterocicloalquilo, heterocicloalquil-alquilo inferior, opcionalmente sustituido por uno o más Z2ö; cada Z2ö es con independencia halogeno, hidroxi, alquilo inferior, cicloalquilo, ciano, haloalquilo inferior, amino, ácido carboxílico, éster o alcoxi inferior; R1 es un enlace, C(=O), C(=O)O, C(=O)CH2OC(=O), C(=O)CH2NHC(=O)O o S(=O)2; R2 es H o R2'; R2' es hidroxi, alquilo inferior, N(R3)2, hidroxialquilo inferior o haloalquilo inferior, opcionalmente sustituido por uno o más R2ö; cada R2ö es con independencia ciano, amino, dialquilamino, hidroxi, hidroxialquilo inferior o alcoxi inferior; y cada R3 es con independencia H, alquilo inferior, cicloalquilo inferior, fenilo, heterocicloalquilo inferior o los dos R3 juntos forman un anillo heterocíclico; con la condicion de que si X es N, X2 es H, Y' es CH, R1 es C(=O), R2 es metilo, r es el numero 1, m es el numero 0, p es el numero 0, q es el numero 0, Y es N(Z1)S(O)2Z2, y Z2 es metilo, entonces Z1 no sea H ni hidroxietilo.
ARP100102908A 2009-08-10 2010-08-09 Inhibidores de las jnk AR077820A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US23252209P 2009-08-10 2009-08-10

Publications (1)

Publication Number Publication Date
AR077820A1 true AR077820A1 (es) 2011-09-28

Family

ID=42710723

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102908A AR077820A1 (es) 2009-08-10 2010-08-09 Inhibidores de las jnk

Country Status (15)

Country Link
US (1) US8536172B2 (es)
EP (1) EP2464640A1 (es)
JP (1) JP5784604B2 (es)
KR (1) KR101506318B1 (es)
CN (1) CN102471319B (es)
AR (1) AR077820A1 (es)
AU (1) AU2010283769B2 (es)
BR (1) BR112012003059A2 (es)
CA (1) CA2768749A1 (es)
IL (1) IL217756A0 (es)
IN (1) IN2012DN01231A (es)
MX (1) MX2012001449A (es)
SG (1) SG178321A1 (es)
TW (1) TW201109336A (es)
WO (1) WO2011018417A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011151357A1 (en) * 2010-06-04 2011-12-08 F. Hoffmann-La Roche Ag Inhibitors of jnk
MX2015000908A (es) * 2012-07-20 2015-09-21 Cleave Biosciences Inc Pirimidinas fusionadas como inhibidores del complejo p97.
CA2903275A1 (en) * 2013-06-26 2014-12-31 Xigen Inflammation Ltd. New use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
SG11201608242XA (en) 2014-04-04 2016-10-28 Syros Pharmaceuticals Inc Inhibitors of cyclin-dependent kinase 7 (cdk7)
WO2016100909A1 (en) 2014-12-18 2016-06-23 President And Fellows Of Harvard College METHODS FOR GENERATING STEM CELL-DERIVED β CELLS AND USES THEREOF

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101177729B1 (ko) * 2006-09-08 2012-09-07 에프. 호프만-라 로슈 아게 벤조트리아졸 키나아제 조절제
CN101547917A (zh) * 2006-12-08 2009-09-30 霍夫曼-拉罗奇有限公司 用作jnk调节剂的取代的嘧啶类化合物及它们的应用

Also Published As

Publication number Publication date
BR112012003059A2 (pt) 2016-08-02
JP5784604B2 (ja) 2015-09-24
IL217756A0 (en) 2012-03-29
US8536172B2 (en) 2013-09-17
TW201109336A (en) 2011-03-16
CN102471319A (zh) 2012-05-23
IN2012DN01231A (es) 2015-05-15
AU2010283769A1 (en) 2012-02-09
MX2012001449A (es) 2012-03-26
SG178321A1 (en) 2012-03-29
CA2768749A1 (en) 2011-02-17
CN102471319B (zh) 2014-06-18
KR20120055645A (ko) 2012-05-31
EP2464640A1 (en) 2012-06-20
JP2013501746A (ja) 2013-01-17
AU2010283769B2 (en) 2015-09-17
WO2011018417A1 (en) 2011-02-17
US20110034470A1 (en) 2011-02-10
KR101506318B1 (ko) 2015-03-26

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