[go: up one dir, main page]

AR083670A1 - DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS - Google Patents

DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS

Info

Publication number
AR083670A1
AR083670A1 ARP110104042A ARP110104042A AR083670A1 AR 083670 A1 AR083670 A1 AR 083670A1 AR P110104042 A ARP110104042 A AR P110104042A AR P110104042 A ARP110104042 A AR P110104042A AR 083670 A1 AR083670 A1 AR 083670A1
Authority
AR
Argentina
Prior art keywords
het1
nhet1
atoms
hal
mono
Prior art date
Application number
ARP110104042A
Other languages
English (en)
Inventor
Dipl-Chem Dorsch Dieter Dr
Wucherer-Plietker Margarita Dra
Dr Mueller Thomas J J Prof
Merkul Eugen Dipl-Chem
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 AR083670A1 publication Critical patent/AR083670A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—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
    • 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
    • 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
    • A61P35/04—Antineoplastic agents specific for metastasis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de la fórmula (1) en donde R1 es A, -[C(R3)(R4)]nAr, -[C(R3)(R4)]nHet o -[C(R3)(R4)]nCyc; R2 es H, A, Hal, CN, -[C(R3)2]n-Ar’, -[C(R3)2]n-Het’, -[C(R3)2]n-Cyc, OR3 o N(R3)2; R3 es H o A; R4 es H, A, -[C(R3)2]nOR3, -[C(R3)2]nCOOR3, -[C(R3)2]nNR3R4 o -[C(R3)2]nHet; R3 y R4 también son juntos alquileno con 2, 3, 4 ó 5 átomos de C; A es alquilo no ramificado o ramificado con 1-6 átomos de C, en donde uno o dos grupos CH2 pueden estar reemplazados por átomos de O, N y/o S y/o por grupos -CH=CH- y/o también 1-7 átomos de H pueden estar reemplazados por F; Cyc es cicloalquilo con 3, 4, 5, 6 ó 7 átomos de C; Ar es fenilo no sustituido o mono-, di- o trisustituido con Hal, A, -[C(R3)2]nOR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2N(R3)2 y/o S(O)nA; Ar’ es fenilo no sustituido o mono-, di- o trisustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, CO-Het1, Het1, [C(R3)2]nN(R3)2, [C(R3)2]nHet1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]n-Het1, NHCONH[C(R3)2]n-N(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]nHet1, CO-Het1, CHO y/o COA; Het es un heterociclo saturado, insaturado o aromático no sustituido o mono- o disustituido con Hal, A, -[C(R3)2]nOR3, N(R3)2, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, COR3, SO2NR3 y/o S(O)nA con 1 a 4 átomos de N y/u O y/o S; Het’ es un heterociclo saturado, insaturado o aromático mono-, di- o tricíclico con 1 a 4 átomos de N, O y/o S, que no está sustituido o que puede estar mono- o disustituido con Hal, A, OR3, N(R3)2, SR3, NO2, CN, COOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, CO-Het1, Het1, [C(R3)2]nN(R3)2, [C(R3)2]nHet1, O[C(R3)2]nN(R3)2, O[C(R3)2]nHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]nN(R3)2, NHCOO[C(R3)2]nHet1, NHCONH[C(R3)2]nN(R3)2, NHCONH[C(R3)2]nHet1, OCONH[C(R3)2]nN(R3)2, OCONH[C(R3)2]n-Het1, CO-Het1, CHO, COA, =S, =NH, =NA y/u =O (oxigeno del carbonilo); Het1 es un heterociclo insaturado monocíclico con 1 a 2 átomos de N y/u O, que puede estar mono-o disustituido con A, OA, OH, Hal y/u =O (oxigeno del carbonilo); Hal es F, Cl, Br o I; n es 0, 1 ó 2; así como sus sales, tautómeros y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones. Son inhibidores de la PDK1 y la proliferación celular/vitalidad celular y se pueden emplear para el tratamiento de tumores.
ARP110104042A 2010-11-01 2011-11-01 DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS AR083670A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102010049877A DE102010049877A1 (de) 2010-11-01 2010-11-01 7-((1,2,3)Triazol-4-yl)-pyrrolo(2,3) pyrazinderivate

Publications (1)

Publication Number Publication Date
AR083670A1 true AR083670A1 (es) 2013-03-13

Family

ID=44862924

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104042A AR083670A1 (es) 2010-11-01 2011-11-01 DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS

Country Status (11)

Country Link
US (1) US8865715B2 (es)
EP (1) EP2635581B1 (es)
JP (1) JP5891233B2 (es)
CN (1) CN103168042B (es)
AR (1) AR083670A1 (es)
AU (1) AU2011325479B8 (es)
CA (1) CA2816363C (es)
DE (1) DE102010049877A1 (es)
ES (1) ES2535607T3 (es)
IL (1) IL226094A0 (es)
WO (1) WO2012059171A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102011008352A1 (de) * 2011-01-12 2012-07-12 Merck Patent Gmbh 5-([1,2,3]Triazol-4-yl)-7H-pyrrolo-[2,3-d]pyrimidinderivate
GB201114051D0 (en) 2011-08-15 2011-09-28 Domainex Ltd Compounds and their uses
CN104755478B (zh) * 2012-10-16 2017-10-10 霍夫曼-拉罗奇有限公司 丝氨酸/苏氨酸激酶抑制剂
CA2936551A1 (en) * 2014-01-24 2015-07-30 Confluence Life Sciences, Inc. Substituted pyrrolopyridines and pyrrolopyrazines for treating cancer or inflammatory diseases
TW201613916A (en) 2014-06-03 2016-04-16 Gilead Sciences Inc TANK-binding kinase inhibitor compounds
CN106715419A (zh) 2014-09-26 2017-05-24 吉利德科学公司 用作tank‑结合激酶抑制剂化合物的氨基三嗪衍生物
EP3247353A4 (en) 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
EP3394044A1 (en) 2015-12-17 2018-10-31 Gilead Sciences, Inc. Tank-binding kinase inhibitor compounds
US10138219B2 (en) 2016-02-19 2018-11-27 Pmv Pharmaceuticals Methods and compounds for restoring mutant p53 function
DE102016113714A1 (de) 2016-07-26 2018-02-01 Rosa Karl Transfektionsverfahren mit nicht-viralen Genliefersystemen
US11027260B2 (en) 2019-02-13 2021-06-08 Uchicago Argonne, Llc Low pressure nanowire membrane for catalytic reactions and methods of making and using the same
KR102838154B1 (ko) 2019-09-23 2025-07-28 피엠브이 파마슈티컬스 인코포레이티드 돌연변이체 p53 기능을 회복시키기 위한 방법 및 화합물
EP4159718A4 (en) * 2020-05-29 2023-10-04 Daegu-Gyeongbuk Medical Innovation Foundation SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF AS AN ACTIVE INGREDIENT FOR PREVENTING OR TREATING MENTAL DISEASES
CN116096704A (zh) 2020-06-24 2023-05-09 皮姆维制药公司 用于治疗癌症的组合疗法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5747469A (en) 1991-03-06 1998-05-05 Board Of Regents, The University Of Texas System Methods and compositions comprising DNA damaging agents and p53
GB9904387D0 (en) 1999-02-25 1999-04-21 Pharmacia & Upjohn Spa Antitumour synergistic composition
TWI339206B (en) * 2003-09-04 2011-03-21 Vertex Pharma Compositions useful as inhibitors of protein kinases
SI1696907T1 (sl) * 2003-10-03 2013-12-31 The Ohio State University Research Foundation Inhibitorji signaliziranja PDK-1/AKT
US7709645B2 (en) 2004-07-27 2010-05-04 Sgx Pharmaceuticals, Inc. Pyrrolo-pyridine kinase modulators
EP1778687A2 (en) 2004-07-27 2007-05-02 SGX Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
CN101052629A (zh) * 2004-08-02 2007-10-10 Osi制药公司 芳基－氨基取代的吡咯并嘧啶多激酶抑制化合物
EP1814883A1 (en) * 2004-11-22 2007-08-08 Vertex Pharmaceuticals Incorporated Bicyclic inhibitors or rho kinase
BRPI0608659A2 (pt) 2005-04-06 2010-11-30 Astrazeneca Ab composto, métodos para limitar a proliferação celular, de tratamento de um ser humano ou animal sofrendo de uma doença, e de tratamento de profilaxia do cáncer, para tratar cáncer, de tratamento de infecções associadas com cáncer, e de profilaxia de infecções associadas com cáncer, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, métodos para inibir chk1 cinase, e um pak cinase, e para limitar a tumorigênese em um ser humano ou animal, e, processo para a preparação de um composto ou um sal farmaceuticamente aceitável do mesmo
EP2038272B8 (en) 2006-06-30 2013-10-23 Sunesis Pharmaceuticals, Inc. Pyridinonyl pdk1 inhibitors
US20100216767A1 (en) 2006-12-22 2010-08-26 Mina Aikawa Quinazolines for pdk1 inhibition
EP2134346B1 (en) 2007-03-13 2011-09-21 Merck Sharp & Dohme Corp. Inhibitors of janus kinases and/or 3-phosphoinositide-dependent protein kinase-1
JP5478488B2 (ja) 2007-06-20 2014-04-23 メルク・シャープ・アンド・ドーム・コーポレーション Ｊａｎｕｓキナーゼの阻害剤
JP2011500806A (ja) 2007-10-25 2011-01-06 メルク・シャープ・エンド・ドーム・コーポレイション 治療用化合物
EP3037421A3 (en) 2008-11-25 2016-11-30 University Of Rochester Mlk inhibitors and methods of use
DE102009019962A1 (de) * 2009-05-05 2010-11-11 Merck Patent Gmbh 3-([1,2,3]Triazol-4-yl)-pyrrolo[2,3-b]pyridinderivate
EP2454262B1 (en) * 2009-07-15 2014-05-14 Abbott Laboratories Pyrrolopyrazine inhibitors of kinases
DE102009060175A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolo[2,3-d] pyrazin-7-yl-pyrimidin-Verbindungen

Also Published As

Publication number Publication date
AU2011325479B2 (en) 2015-04-09
EP2635581B1 (de) 2015-02-25
WO2012059171A1 (de) 2012-05-10
CA2816363A1 (en) 2012-05-10
CN103168042B (zh) 2015-10-21
JP2013540783A (ja) 2013-11-07
ES2535607T3 (es) 2015-05-13
US20130217951A1 (en) 2013-08-22
AU2011325479A1 (en) 2013-05-02
IL226094A0 (en) 2013-06-27
CN103168042A (zh) 2013-06-19
AU2011325479B8 (en) 2015-05-14
AU2011325479A8 (en) 2015-05-14
CA2816363C (en) 2019-03-05
US8865715B2 (en) 2014-10-21
DE102010049877A1 (de) 2012-05-03
EP2635581A1 (de) 2013-09-11
JP5891233B2 (ja) 2016-03-22

Similar Documents

Publication Publication Date Title
AR083670A1 (es) DERIVADOS DE 7-([1,2,3]TRIAZOL-4-IL)-PIRROLO[2,3-b]PIRAZINA UTILES COMO INHIBIDORES DE LA PROLIFERACION CELULAR, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y PROCEDIMIENTO PARA PREPARARLOS
AR076750A1 (es) Derivados de 3-((1,2,3) triazol -4-il)- pirrolo (2,3-b) piridina
AR072860A1 (es) Derivados de 3-(3-pirimidin-2-il-bencil)-[1,2,4]triazolo[4,3-b]piridazina
AR071208A1 (es) Derivados de piridazinona
AR066543A1 (es) Derivados de piridazinona
AR073055A1 (es) Derivados biciclicos de triazol
AR057214A1 (es) Derivados de piridazinona como inhibidores, reguladores o moduladores de quinasas.
AR067081A1 (es) Derivados de pirrolo[2,3-b]piridin-pirimidina,proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores cancerigenos y metastasis tumorales.
AR066770A1 (es) Derivados de piridazinona
AR069843A1 (es) Derivados de piridazinona, procedimiento para preparar dichos compuestos, composiciones farmaceuticas y usos de los mismos para preparar un medicamento
AR072792A1 (es) DERIVADOS DE PIRROLOPIRIDINILPIRIMIDIN-2-IL-AMINA, PROCEDIMIENTO DE PREPARACIoN Y COMPOSICIONES FARMACEUTICAS
AR076006A1 (es) Compuestos heterociclicos inhibidores de autotaxina utiles para el tratamiento de tumores, proceso para prepararlos y medicamentos que los contienen.
AR074688A1 (es) Derivados de piridazinona, procedimiento para prepararlos, medicamentos que los contienen y uso de los mismos para el tratamiento de tumores.
AR077567A1 (es) Derivados de aminopiridina
AR085110A1 (es) Derivados de 7-azaindol
AR075122A1 (es) Derivados de piridazinona
PE20121815A1 (es) Compuestos de pirrolo-pirimidina como inhibidores de cdk4/6
AR072192A1 (es) Derivados de tiazolil-piperidina
AR068872A1 (es) 5- ciano- tienopiridinas. procesos de obtencion y composiciones farmaceuticas.
AR074418A1 (es) Compuestos de benzonaftiridina, procedimiento de preparacion y su uso en el tratamiento de tumores
AR082109A1 (es) Derivados de bipiridilo
AR068659A1 (es) Derivados de imidazol inhibidores de autotaxina
AR078313A1 (es) Derivados de piridinil-imidazolona inhibidores de quinasas pi3k,composiciones farmaceuticas que los comprenden, metodo para prepararlos y uso de los mismos en el tratamiento de enfermedades autoinmunes e inflamatorias, entre otras
AR066892A1 (es) Derivados de benzoxazolona, proceso, medicamento, uso para tratar tumores y kit
AR070212A1 (es) Derivados de 4-(pirrolo[2,3-c]piridin-3-il)-pirimidinil-2-amina, proceso de preparacion, medicamentos que los contienen y usos de los mismos para el tratamiento de tumores, metastasis tumoral y/o sida.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal