AR084507A1 - Derivados de indazoliltriazol - Google Patents

Derivados de indazoliltriazol

Info

Publication number
AR084507A1
AR084507A1 ARP110104813A ARP110104813A AR084507A1 AR 084507 A1 AR084507 A1 AR 084507A1 AR P110104813 A ARP110104813 A AR P110104813A AR P110104813 A ARP110104813 A AR P110104813A AR 084507 A1 AR084507 A1 AR 084507A1
Authority
AR
Argentina
Prior art keywords
alkyl
hal
denotes
cycloalkyl
het1
Prior art date
Application number
ARP110104813A
Other languages
English (en)
Original Assignee
Merck Serono Sa
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 Serono Sa filed Critical Merck Serono Sa
Publication of AR084507A1 publication Critical patent/AR084507A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/537—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 spiro-condensed or forming part of bridged ring 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
    • A61K31/535—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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • 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
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/28—Drugs 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
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06—Antianaemics
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

Compuestos de la fórmula (1) se usan para el tratamiento de inflamación y trastornos autoinmunes. Composición farmacéutica, proceso de preparación y uso como moduladores de interleuquina-IRAK.Reivindicación 1: Un compuesto de la formula (1) en donde Q denota Ar o Het; E denota -(CH2)mCO-, -(CH2)mSO2, -(CH2)mNHCO- o un enlace simple; R1 denota H, OH, NH-alquilo C1-6, O-alquilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Cyc, Hal, Het1, O-Het1, CO-Het1, NH-Het1, CO-Ar1, O-Ar1, Ar1, NH-Ar1, -(CH2)qHet1, -CONH-(CH2)qHet1, -CONH-Het1, -(CH2)qO-Het1, -(CH2)qO-Ar1, -(CH2)qAr1, -CONH-(CH2)qAr1, -CONH-Ar1, -CONH-cicloalquilo C3-6, -(CH2)qHal, -(CH2)qCyC, CF3, -(CH2)sNH-(CH2)q-Het1, -(CH2)sNH-(CH2)q-Ar1, en donde NH-alquilo C1-6, O-alquilo C1-6, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-6 puede estar sustituido con 1 a 3 grupos seleccionados, de modo independiente, de O-alquilo C1-3, OH, CONH2, NH2; R2 denota H, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, Hal, CF3, con preferencia H; R3 denota Het1, Ar1, NRaRb, COOH, -(CH2)qHet1, -(CH2)qAr1, -(CH2)qNRaRb, -(CH2)qCOOH o alquilo C1-6, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados, de modo independiente, por OH o CF3; R4 denota H, alquilo C1-6, alquenilo C2-6, Hal; Ra denota H, alquilo C1-6 lineal, ramificado o cíclico; Rb denota H, Hetb, Arb, -CO-Hetb, -CO-Arb, un cicloalquilo C3-8 o un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por Hetb, Arb, NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal; n es 0, 1, 2, 3 ó 4; m es 0, 1, 2, 3 ó 4; q es 1, 2 ó 3; s es 0, 1, 2 ó 3; Hal denota Cl, Br, I, F, con preferencia Cl o F; Ar denota un grupo arileno monocíclico divalente o bicíclico fusionado que tiene 6 a 14 átomos de carbono, que también puede estar sustituido con 1 a 4 sustituyentes seleccionados de Hal, alquilo C1-6, -(CH2)mO-alquilo C1-6, CN, OH, NO2, CF3, -(CH2)mCOOH, -(CH2)mCOO-alquilo C1-6; Het denota un grupo heterocíclico insaturado, saturado o aromático monocíclico divalente o bicíclico fusionado que tiene 1 a 5 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo -C=O que también puede estar sustituido con 1 a 4 sustituyentes seleccionados de Hal, alquilo C1-6, -(CH2)mO-alquilo C1-6, CN, OH, NO2, CF3, -(CH2)mCOOH, -(CH2)mCOO-alquilo C1-6; Ar1 denota un anillo carbocíclico aromático monocíclico o bicíclico que tiene 6 a 14 átomos de carbono, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo, -OH, -O-alquilo C1-6, -COalquilo C1-6, -NH2, -COH, -COOH, -CONH2, un grupo Rb tales como -CH2O(alquilo C1-6), -SO2NRaRb o SO2(alquilo C1-6); Het1 denota un anillo heterocíclico saturado, insaturado o aromático monocíclico o bicíclico (fusionado, en puente o espiro) que tiene 1 a 4 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo CO, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo C3-8, -OH, -O-alquilo C1-6, -NH2, -N(alquilo C1-6)2, -COH, -COOH, -CONH2, -COalquilo C1-6, -NHCO(cicloalquilo C3-6), un grupo Rb tales como -SO2NRaRb o SO2(alquilo C1-6); Hetb denota un anillo heterocíclico saturado, insaturado o aromático monocíclico o bicíclico (fusionado o espiro) que tiene 1 a 4 heteroátomos seleccionados de modo independiente de N, O, S y/o un grupo CO, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, CN, perfluoroalquilo, -OH, -O-alquilo C1-6, -NH2, -COH, -COOH, - CONH2 o con un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal, cicloalquilo C3-8, o con un anillo heterocíclico de 4 a 8 miembros que contiene un heteroátomo seleccionado de O, S y N; Arb denota un anillo carbocíclico aromático monocíclico o bicíclico que tiene 6 a 14 átomos de carbono, que no está sustituido o que está monosustituido, disustituido o trisustituido con Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, -OH, -O-alquilo C1-6, -NH2, -COH, -COOH, -CONH2 o con un alquilo C1-6 lineal o ramificado, en donde 1 a 3 átomos de hidrógeno pueden estar reemplazados por NH2, N(alquilo C1-6)2, NH(alquilo C1-6), N(alquilo C1-6)(cicloalquilo C3-8), NH(cicloalquilo C3-8), O(alquilo C1-6), CN, OH, CF3, Hal, cicloalquilo C3-8 o con un anillo heterocíclico de 4 a 8 miembros que contiene un heteroátomo seleccionado de O, S y N; Cyc denota un anillo carbocíclico saturado o insaturado que tiene 3 a 8 átomos de carbono, con preferencia 5 ó 6 átomos de carbono, en donde 1 a 5 átomos de H están reemplazados por Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, Hal, -CF3, -OCF3, -NO2, -CN, perfluoroalquilo, alquilo C1-6 lineal o ramificado, cicloalquilo, -OH, -O-alquilo C1-6, -COalquilo C1-6, -NH2, -COH, -COOH, -CONH2, un grupo Rb tales como -CH2O(alquilo C1-6), -SO2NRaRb o SO2(alquilo C1-6); y sus derivados, solvatos, tautómeros, sales, hidratos y estereoisómeros farmacéuticamente aceptables, incluyendo sus mezclas en todas las proporciones.
ARP110104813A 2010-12-20 2011-12-20 Derivados de indazoliltriazol AR084507A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201061424890P 2010-12-20 2010-12-20
EP10195867 2010-12-20

Publications (1)

Publication Number Publication Date
AR084507A1 true AR084507A1 (es) 2013-05-22

Family

ID=43838132

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104813A AR084507A1 (es) 2010-12-20 2011-12-20 Derivados de indazoliltriazol

Country Status (24)

Country Link
US (1) US9073892B2 (es)
EP (1) EP2655357B1 (es)
JP (1) JP6007189B2 (es)
KR (1) KR101842098B1 (es)
CN (1) CN103429585B (es)
AR (1) AR084507A1 (es)
AU (1) AU2011347711B2 (es)
BR (1) BR112013015460B1 (es)
CA (1) CA2822166C (es)
EA (1) EA023544B1 (es)
ES (1) ES2592713T3 (es)
HK (1) HK1191938A1 (es)
HR (1) HRP20161127T1 (es)
HU (1) HUE029617T2 (es)
IL (1) IL226912A (es)
LT (1) LT2655357T (es)
MX (1) MX2013007149A (es)
PL (1) PL2655357T3 (es)
PT (1) PT2655357T (es)
RS (1) RS55165B1 (es)
SG (1) SG191205A1 (es)
SI (1) SI2655357T1 (es)
WO (1) WO2012084704A1 (es)
ZA (1) ZA201305483B (es)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR045563A1 (es) 2003-09-10 2005-11-02 Warner Lambert Co Anticuerpos dirigidos a m-csf
EP2654748B1 (en) * 2010-12-21 2016-07-27 Merck Sharp & Dohme Corp. Indazole derivatives useful as erk inhibitors
BR112014030812B1 (pt) 2012-06-13 2022-11-08 Incyte Holdings Corporation Compostos tricíclicos substituídos como inibidores de fgfr, seus usos, composição farmacêutica e método para inibir uma enzima fgfr
WO2014099697A1 (en) * 2012-12-20 2014-06-26 Merck Sharp & Dohme Corp. 3-ester-4-substituted orexin receptor antagonists
US9643955B2 (en) 2012-12-20 2017-05-09 Merck Sharp & Dohme Corp. 2-pyridyloxy-3-nitrile-4-substituted orexin receptor antagonists
CA2900431C (en) * 2013-02-07 2021-05-04 Merck Patent Gmbh Pyridazinone-amides derivatives
LT2953952T (lt) * 2013-02-07 2017-08-25 Merck Patent Gmbh Makrocikliniai piridazinono dariniai
SG10201708520YA (en) 2013-04-19 2017-12-28 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
TWI667233B (zh) 2013-12-19 2019-08-01 德商拜耳製藥公司 新穎吲唑羧醯胺，其製備方法、含彼等之醫藥製劑及其製造醫藥之用途
KR20160115933A (ko) * 2014-01-10 2016-10-06 오리진 디스커버리 테크놀로지스 리미티드 Irak4 억제제로서의 인다졸 화합물
CU24389B1 (es) 2014-01-13 2019-04-04 Aurigene Discovery Tech Ltd Compuestos de heterociclilo bicíclico como inhibidores de irak4
WO2016053772A1 (en) * 2014-09-30 2016-04-07 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
EP3200790B1 (en) 2014-09-30 2020-08-26 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
EP3200788B1 (en) 2014-09-30 2019-09-18 Merck Sharp & Dohme Corp. Inhibitors of irak4 activity
US9969749B2 (en) 2014-09-30 2018-05-15 Merck Sharp & Dohme Corp. Inhibitors of IRAK4 activity
JO3705B1 (ar) 2014-11-26 2021-01-31 Bayer Pharma AG إندازولات مستبدلة جديدة، عمليات لتحضيرها، مستحضرات دوائية تحتوي عليها واستخدامها في إنتاج أدوية
US10336707B2 (en) 2014-12-16 2019-07-02 Eudendron S.R.L. Heterocyclic derivatives modulating activity of certain protein kinases
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
MY189941A (en) 2015-04-22 2022-03-22 Rigel Pharmaceuticals Inc Pyrazole compounds and method for making and using the compounds
EP3195865A1 (de) 2016-01-25 2017-07-26 Bayer Pharma Aktiengesellschaft Kombinationen von irak4 inhibitoren und btk inhibitoren
US20180289685A1 (en) 2015-04-30 2018-10-11 Bayer Pharma Aktiengesellschaft Combinations of inhibitors of irak4 with inhibitors of btk
US10435396B2 (en) 2016-03-03 2019-10-08 Bayer Pharma Aktiegesellschaft 2-substituted indazoles, methods for producing same, pharmaceutical preparations that contain same, and use of same to produce drugs
EP3219329A1 (en) 2016-03-17 2017-09-20 Bayer Pharma Aktiengesellschaft Combinations of copanlisib
HUE049331T2 (hu) 2016-04-29 2020-09-28 Bayer Pharma AG Indazolok szintézise
SI3448848T1 (sl) 2016-04-29 2024-01-31 Bayer Pharma Aktiengesellschaft Polimorfna oblika N-(6-(2-hidroksipropan-2-il)-2-(2-(metilsulfonil)etil)-2H-indazol-5-il) -6-(trifluormetil)piridin-2-karboksamida
AU2017272505B9 (en) 2016-06-01 2021-10-28 Bayer Animal Health Gmbh Substituted indazoles useful for treatment and prevention of allergic and/or inflammatory diseases in animals
JOP20180011A1 (ar) 2017-02-16 2019-01-30 Gilead Sciences Inc مشتقات بيرولو [1، 2-b]بيريدازين
WO2018178947A2 (en) 2017-03-31 2018-10-04 Aurigene Discovery Technologies Limited Compounds and compositions for treating hematological disorders
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019060693A1 (en) 2017-09-22 2019-03-28 Kymera Therapeutics, Inc. CRBN LIGANDS AND USES THEREOF
JP7366031B2 (ja) 2017-09-22 2023-10-20 カイメラ セラピューティクス， インコーポレイテッド タンパク質分解剤およびそれらの使用
JP2020537678A (ja) 2017-10-19 2020-12-24 バイエル・アニマル・ヘルス・ゲーエムベーハー 動物における疾患の治療および予防のための縮合ヘテロ芳香族ピロリドンの使用
IL308364A (en) 2017-10-31 2024-01-01 Curis Inc Compounds and preparations for the treatment of hematological disorders
WO2019111218A1 (en) 2017-12-08 2019-06-13 Cadila Healthcare Limited Novel heterocyclic compounds as irak4 inhibitors
BR112020012997A2 (pt) 2017-12-26 2020-12-01 Kymera Therapeutics, Inc. degradadores de irak e usos dos mesmos
WO2019140387A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Crbn ligands and uses thereof
US11485743B2 (en) 2018-01-12 2022-11-01 Kymera Therapeutics, Inc. Protein degraders and uses thereof
GB201801226D0 (en) 2018-01-25 2018-03-14 Redx Pharma Plc Modulators of Rho-associated protein kinase
SG11202010882XA (en) 2018-05-04 2020-11-27 Incyte Corp Salts of an fgfr inhibitor
KR20210018265A (ko) 2018-05-04 2021-02-17 인사이트 코포레이션 Fgfr 억제제의 고체 형태 및 이의 제조 방법
WO2020010177A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Tricyclic crbn ligands and uses thereof
TWI721483B (zh) 2018-07-13 2021-03-11 美商基利科學股份有限公司 吡咯并[1,2-b]嗒𠯤衍生物
WO2020113233A1 (en) 2018-11-30 2020-06-04 Kymera Therapeutics, Inc. Irak degraders and uses thereof
EP3924340A1 (en) * 2019-02-11 2021-12-22 Merck Patent GmbH Indazolyl-isoxazole derivatives for the treatment of diseases such as cancer
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
JP2022545542A (ja) 2019-08-30 2022-10-27 ライジェル ファーマシューティカルズ， インコーポレイテッド ピラゾール化合物、その製剤並びに化合物及び／又は製剤を使用する方法
MX2022003830A (es) 2019-10-02 2022-05-12 Kainos Medicine Inc Compuesto de n-(1h-imidazol-2-il)benzamida y composicion farmaceutica que comprende el mismo como ingrediente activo.
JP2022552324A (ja) 2019-10-14 2022-12-15 インサイト・コーポレイション Ｆｇｆｒ阻害剤としての二環式複素環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US20230034723A1 (en) * 2019-10-31 2023-02-02 Hoffmann-La Roche Inc. Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
JP2023509366A (ja) 2019-12-17 2023-03-08 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US11866405B2 (en) 2020-12-10 2024-01-09 Astrazeneca Ab Substituted indazoles as IRAK4 inhibitors
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
KR102607237B1 (ko) * 2023-06-07 2023-11-30 주식회사 젠센 신규한 트리아졸이 치환된 인다졸 유도체 및 이의 용도

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040087642A1 (en) * 2002-10-24 2004-05-06 Zeldis Jerome B. Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain
ZA200503242B (en) * 2002-10-24 2006-10-25 Celgene Corp Treatment of pain with JNK inhibitors
US20050090529A1 (en) * 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
US6984652B2 (en) * 2003-09-05 2006-01-10 Warner-Lambert Company Llc Gyrase inhibitors
JP2008540345A (ja) * 2005-04-29 2008-11-20 セルジーン・コーポレーション １−（５−（１ｈ−１，２，４−トリアゾール−５−イル）（１ｈ−インダゾール−３−イル））−３−（２−ピペリジルエトキシ）ベンゼンの固体形態
SG182187A1 (en) 2007-06-08 2012-07-30 Abbott Gmbh & Co Kg 5-heteroaryl substituted indazoles as kinase inhibitors

Also Published As

Publication number Publication date
JP2014500286A (ja) 2014-01-09
PL2655357T3 (pl) 2016-12-30
ES2592713T3 (es) 2016-12-01
KR20130133252A (ko) 2013-12-06
LT2655357T (lt) 2016-10-10
CA2822166C (en) 2019-10-29
HRP20161127T1 (hr) 2016-11-18
CN103429585B (zh) 2015-07-08
WO2012084704A1 (en) 2012-06-28
EA201300730A1 (ru) 2013-12-30
AU2011347711A1 (en) 2013-08-01
US20130274241A1 (en) 2013-10-17
PT2655357T (pt) 2016-09-28
CA2822166A1 (en) 2012-06-28
EP2655357B1 (en) 2016-06-22
EA023544B1 (ru) 2016-06-30
HK1191938A1 (en) 2014-08-08
BR112013015460A2 (pt) 2016-09-20
SI2655357T1 (sl) 2016-10-28
JP6007189B2 (ja) 2016-10-12
BR112013015460B1 (pt) 2022-01-25
HUE029617T2 (en) 2017-03-28
US9073892B2 (en) 2015-07-07
IL226912A (en) 2017-01-31
KR101842098B1 (ko) 2018-03-26
CN103429585A (zh) 2013-12-04
AU2011347711B2 (en) 2017-02-02
MX2013007149A (es) 2013-10-30
SG191205A1 (en) 2013-07-31
ZA201305483B (en) 2014-06-25
RS55165B1 (sr) 2017-01-31
EP2655357A1 (en) 2013-10-30

Similar Documents

Publication Publication Date Title
AR084507A1 (es) Derivados de indazoliltriazol
AR080328A1 (es) Tienopirimidinas que contienen un grupo alquilo sustituido inhibidoras de quinasas mnk1 y/o mnk2, composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de trastornos metabolicos tales como diabetes y obesidad, y trastornos hiperproliferativos, entre otros
EA201490453A1 (ru) Замещенные аналоги (e)-n-(1-фенилэтилиден)бензогидразида в качестве ингибиторов деметилазы гистонов
AR087591A1 (es) Derivados de ciclohexil azetidina como inhibidores de jak
AR084011A1 (es) Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen
CU20130116A7 (es) Derivados de heteroarilo como moduladores de nachr alfa 7
AR088226A1 (es) Derivados piperidinicos heterociclicos, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de enfermedades neurodegenerativas
AR064010A1 (es) Inhibidores de la actividad de la akt
PE20110805A1 (es) Compuestos con anillos espiro-triciclicos como moduladores de beta-secretasas y metodos de uso
AR086983A1 (es) Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
AR076435A1 (es) Compuestos de indazoles sustituidos, composiciones farmaceuticas que los contienen y procesos de obtencion de los mismos
AR067413A1 (es) Compuestos heterociclicos que contienen ciclopenta[d]pirimidina inhibidores de proteinquinasas akt, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de las mismas para el tratamiento de enfermedades hiperproliferativas, tales como cancer
AR073480A1 (es) Benzamidas, su preparacion y su uso como medicamentos
CO6321248A2 (es) Derivados de triazol utiles para el tratamiento de enfermedades
CL2012000999A1 (es) Compuestos derivados de pirazoloespirocetona sustituida, inhibidores de acetil-coa carboxilasa; composicion farmaceutica que los comprende; uso para tratar o retrasar la progresion o el inicio de diabetes tipo 2, higado graso no alcoholico (hgna) o la resistencia hepatica a la insulina.
AR084457A1 (es) Derivados de biciclo[3,2,1]octilamida
AR070136A1 (es) Pirimidil ciclopentanos como inhibidores de la akt proteina quinasa
AR093725A1 (es) Quinazolincarboxamida azetidinas
AR078278A1 (es) Antagonistas de la tiazol y oxazol hepcidina, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento de anemias y enfermedades asociadas a deficiencias de hierro.
AR076008A1 (es) Derivados de hidroximetil-isoxazol moduladores de receptores gaba a, composiciones farmaceuticas que los contienen, metodo para prepararlos y uso de los mismos para el tratamiento del alzheimer y otros trastornos cognitivos.
AR100806A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
AR072819A1 (es) Derivados de triazolo[4,3-a]piridina,procedimiento de preparacion,intermediarios de dicho proceso,composiciones farmaceuticas que los comprenden y uso de los mismos, como inhibidores de la proteinquinasa met,para el tratamiento de canceres,psoriasis,enfermedades del sistema nervioso central y otras
AR100810A1 (es) Inhibidores de fosfatidilinositol 3-quinasa
ES2606839T3 (es) Tetraaza-ciclopenta[a]indenilo y su uso como moduladores alostéricos positivos
CU20090048A7 (es) Nuevos derivados de diosmetina, su procedimiento de preparación y las composiciones farmacéuticas que los contienen

Legal Events

Date Code Title Description
FG Grant, registration