AR085637A1 - Derivados de pirido[2,3-b]pirazina - Google Patents

Derivados de pirido[2,3-b]pirazina

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Publication number
AR085637A1
AR085637A1 ARP120100764A ARP120100764A AR085637A1 AR 085637 A1 AR085637 A1 AR 085637A1 AR P120100764 A ARP120100764 A AR P120100764A AR P120100764 A ARP120100764 A AR P120100764A AR 085637 A1 AR085637 A1 AR 085637A1
Authority
AR
Argentina
Prior art keywords
cyy
nyy
denotes
het3
het2
Prior art date
Application number
ARP120100764A
Other languages
English (en)
Inventor
Dipl-Chem Dorsch Dieter Dr
Jonczyk Alfred Dr
Hoelzemann Guenter Dr
Amendt Christiane Dra
Zenke Frank Dr
Original Assignee
Merck Patent Gmbh
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 Merck Patent Gmbh filed Critical Merck Patent Gmbh
Publication of AR085637A1 publication Critical patent/AR085637A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)

Abstract

Uso de tales compuestos, en donde la inhibición, regulación y/o modulación de la transducción de señales por proteínas que consumen ATP como quinasas desempeña un papel importante, en particular a inhibidores de las quinasas TGF-b receptoras y uso de tales compuestos para el tratamiento de enfermedades inducidas por quinasas, en particular para el tratamiento de tumores.Reivindicación 1: Compuestos de la fórmula (1), en donde: X denota ausencia, NR4 o CR5R6; R1 denota arilo monocíclico C3-8 o un heteroarilo monocíclico C1-8 y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, cada uno de los cuales puede estar sustituido, de modo independiente ente sí, con al menos un sustituyente seleccionado del grupo que consiste en Y, Hal, CN, CF3, OY; R2 denota H, A, -OY, -NH2 o -NAA; R3 denota H, A, -OY o -NYY; R4, R5, R6 denotan, de modo independiente entre sí, ausencia, H, A; R7 denota Hal, A, -(CYY)n-OY, -(CYY)n-NYY, (CYY)n-Het2, (CYY)n-O-Het2, SY, NO2, CN, COOY, -CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -CO-Het2, -O(CYY)n-NYY, -O(CYY)n-Het2, -NH-COOA, -NH-CO-NYY, -NH-COO-(CYY)n-NYY, -NH-COO-(CYY)nHet2, -NH-CO-NH-(CYY)n-NYY, -NH-CO-NH(CYY)n-Het2, -OCO-NH-(CYY)n-NYY, -OCO-NH-(CYY)n-Het2, CHO, COA, =S, =NY, =O; Y denota H o A; A denota alquilo no ramificado o ramificado C1-10, en donde 1, 2, 3, 4, 5, 6 ó 7 átomos de H se pueden reemplazar, de modo independiente entre sí, por Hal y/o en donde uno o dos grupos CH2 pueden estar reemplazados, de modo independiente entre sí, por un O, S, SO, SO2, un grupo -CY=CY- y/o un grupo -CºC- o denota alquilo cíclico C3-7; Het denota un heterociclo mono-, bi- o tricíclico saturado o insaturado C3-20 y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente R7; Het2 denota un heterociclo mono-, bi- o tricíclico saturado o insaturado C3-20 y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo de Hal, A, -(CYY)n-OY, -(CYY)n-NYY, (CYY)n-Het3, (CYY)n-O-Het3, SY, NO2, CN, COOY, -CO-NYY, -NY-COA, -NY-SO2A, SO2-NYY, S(O)mA, -CO-Het3, -O(CYY)n-NYY, -O(CYY)n-Het3, -NH-COOA, -NH-CO-NYY, -NH-COO-(CYY)n-NYY, -NH-COO-(CYY)n-Het3, -NH-CO-NH-(CYY)n-NYY, -NH-CO-NH(CYY)-Het3, -OCO-NH-(CYY)n-NYY, -OCO-NH-(CYY)n-Het3, CHO, COA, =S, =NY, =O; Het3 denota un heterociclo mono-, bi- o tricíclico saturado o insaturado C3-20 y 1, 2, 3, 4 ó 5 átomos de N, O y/o S, que puede estar sustituido, de modo independiente entre sí, con al menos un sustituyente seleccionado del grupo de Hal, A, -(CYY)n-OY, -(CYY)n-NYY, SY, NO2, CN, COOY,-CO-NYY, -NY-COA, -NY-SO2A, -SO2-NYY, S(O)mA, -NH-COOA, -NH-CO-NYY, CHO, COA, =S, =NY, =O; Hal denota F, Cl, Br o I; m denota 0, 1 ó 2; n denota 0, 1, 2, 3 ó 4; y sus sales, solvatos, tautómeros y estereoisómeros fisiológicamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP120100764A 2011-03-09 2012-03-09 Derivados de pirido[2,3-b]pirazina AR085637A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP11001944 2011-03-09

Publications (1)

Publication Number Publication Date
AR085637A1 true AR085637A1 (es) 2013-10-16

Family

ID=45607719

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP120100764A AR085637A1 (es) 2011-03-09 2012-03-09 Derivados de pirido[2,3-b]pirazina

Country Status (16)

Country Link
US (1) US9051318B2 (es)
EP (1) EP2683715B1 (es)
JP (1) JP6104824B2 (es)
KR (1) KR20140022829A (es)
CN (1) CN103391938B (es)
AR (1) AR085637A1 (es)
AU (1) AU2012224979B2 (es)
BR (1) BR112013022948A2 (es)
CA (1) CA2829287C (es)
EA (1) EA201300997A1 (es)
ES (1) ES2542647T3 (es)
IL (1) IL228265A (es)
MX (1) MX2013010163A (es)
SG (1) SG193301A1 (es)
WO (1) WO2012119690A1 (es)
ZA (1) ZA201307511B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012119690A1 (en) * 2011-03-09 2012-09-13 Merck Patent Gmbh Pyrido [2, 3 - b] pyrazine derivatives and their therapeutical uses
CA2935392C (en) 2014-01-01 2022-07-26 Medivation Technologies, Inc. Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity
US10233170B2 (en) * 2014-04-08 2019-03-19 Rigel Pharmaceuticals, Inc. 2,3-disubstituted pyridine compounds as TGF-beta inhibitors and methods of use
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
PT3691620T (pt) 2017-10-05 2022-10-06 Fulcrum Therapeutics Inc Os inibidores da quinase p38 reduzem a expressão de dux4 e genes a jusante para o tratamento de fshd
CN109053598B (zh) * 2018-06-14 2021-04-13 温州大学 一种芳基取代喹唑啉化合物及其合成方法
EP4087657A1 (en) 2020-01-08 2022-11-16 Synthis Therapeutics, Inc. Alk5 inhibitor conjugates and uses thereof

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EP1511738A4 (en) 2002-05-17 2007-05-09 Scios Inc TREATMENT OF FIBROPROLIFERATIVE DISEASES USING TGF BETA INHIBITORS
CA2494367A1 (en) 2002-07-25 2004-02-05 Scios Inc. Methods for improvement of lung function using tgf-.beta. inhibitors
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CA2540342A1 (en) 2003-10-31 2005-05-12 Neurogen Corporation 4-amino (aza) quinoline derivatives as capsaicin receptor agonists
CN1921864A (zh) * 2003-12-24 2007-02-28 西奥斯公司 使用TGF－β抑制剂治疗神经胶质瘤
TW200621251A (en) 2004-10-12 2006-07-01 Neurogen Corp Substituted biaryl quinolin-4-ylamine analogues
CA2593482A1 (en) 2005-01-14 2006-07-20 Neurogen Corporation Heteroaryl substituted quinolin-4-ylamine analogues
BRPI0619424B1 (pt) 2005-12-05 2022-02-08 Pfizer Products Inc Uso de inibidores c-met/hgfrs para a fabricação de medicamentos
EP1990342A1 (en) 2007-05-10 2008-11-12 AEterna Zentaris GmbH Pyridopyrazine Derivatives, Process of Manufacturing and Uses thereof
JP4751856B2 (ja) 2007-07-03 2011-08-17 本田技研工業株式会社 車体側部構造
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Also Published As

Publication number Publication date
ES2542647T3 (es) 2015-08-07
CN103391938B (zh) 2016-02-24
MX2013010163A (es) 2013-10-30
IL228265A (en) 2016-12-29
IL228265A0 (en) 2013-11-25
CN103391938A (zh) 2013-11-13
WO2012119690A1 (en) 2012-09-13
EP2683715A1 (en) 2014-01-15
JP6104824B2 (ja) 2017-03-29
KR20140022829A (ko) 2014-02-25
AU2012224979A1 (en) 2013-10-24
AU2012224979B2 (en) 2017-01-19
BR112013022948A2 (pt) 2016-12-06
SG193301A1 (en) 2013-10-30
US20130345227A1 (en) 2013-12-26
EP2683715B1 (en) 2015-04-15
US9051318B2 (en) 2015-06-09
JP2014511390A (ja) 2014-05-15
EA201300997A1 (ru) 2014-02-28
ZA201307511B (en) 2016-08-31
CA2829287A1 (en) 2012-09-13
CA2829287C (en) 2019-12-17

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