AR086403A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents

Inhibidores de la tirosina-quinasa de bruton

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Publication number
AR086403A1
AR086403A1 ARP120101712A ARP120101712A AR086403A1 AR 086403 A1 AR086403 A1 AR 086403A1 AR P120101712 A ARP120101712 A AR P120101712A AR P120101712 A ARP120101712 A AR P120101712A AR 086403 A1 AR086403 A1 AR 086403A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
lower alkyl
halogen
heterocycloalkyl
Prior art date
Application number
ARP120101712A
Other languages
English (en)
Inventor
Roland J Billedeau
Rama K Kondru
Francisco Javier Lopez-Tapia
Yan Lou
Timothy D Owens
Yimin Qian
Sung So
Kshitij Chhabilbhai Sau-Thakkar
Jutta Wanner
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 AR086403A1 publication Critical patent/AR086403A1/es

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    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
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    • 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
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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    • 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
    • C07D403/02—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
    • C07D403/10—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 linked by a carbon chain containing aromatic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • 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
    • 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

Abstract

Los compuestos aquí descritos son útiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Los compuestos son útiles además para tratar enfermedades inflamatorias y autoinmunes asociadas con una proliferación aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la fórmula (1) y por lo menos un vehículo, diluyente o excipiente.Reivindicación 1: Un compuesto de la fórmula (1) en la que: - - - - - es un enlace sencillo o doble; A es un heteroarilo de 5 eslabones o es un heteroarilo bicíclico de 5 ó 6 eslabones, en el que el CONH2 está unido al heteroarilo de 5 eslabones, cada uno de ellos está opcionalmente sustituido por uno o más A’; A’ es -NHR o R4; R es H, -R1, -R1-R2-R3, -R1-R3 o -R2-R3; R1 es arilo, heteroarilo, cicloalquilo, heterocicloalquilo o heteroarilo fusionado con un heterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más R1’ o R1’’; cada R1’ es con independencia halógeno, nitro, ciano, alquilo inferior-sulfonamido, -S(O)2 u oxo; cada R1’’ es con independencia alquilo inferior, cicloalquilo, heterocicloalquilo, alcoxi inferior, amino o amido, cada uno de ellos está opcionalmente sustituido por uno o más R1’’’; cada R1’’’ es con independencia hidroxi, halógeno, amino, alquil-amino, dialquil-amino o heterocicloalquilo; R2 es -C(=O), -C(=O)O, -C(=O)NR2’, -NHC(=O)O, -C(R2’)2, -O, -C(=NH)NR2’ o -S(=O)2; cada R2’ es con independencia H o alquilo inferior; R3 es H o R4; R4 es alquilo inferior, haloalquilo inferior, alcoxi inferior, amino, (alquilo inferior)-amino, di(alquilo inferior)-amino, arilo, arilalquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-heterocicloalquilo, heterocicloalquil-alquilo, cicloalquilo bicíclico, heterocicloalquilo bicíclico, espirocicloalquilo o espiroheterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, halógeno, (alquilo inferior)-amino, di(alquilo inferior)-amino, hidroxi, hidroxi-alquilo inferior, alcoxi inferior, halógeno, nitro, amino, amido, acilo, ciano, oxo, guanidino, hidroxil-amino, carboxi, carbamoilo, carbamato, haloalcoxi inferior o haloalquilo inferior; dos grupos alquilo inferior juntos pueden formar un anillo; Q es CH o N; X es CH, N o N(X’); X’ es alquilo inferior; Y0 es H, halógeno o alquilo inferior; Y1 es Y1a, Y1b, Y1c o Y1d; Y1a es H o halógeno; Y1b es alquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; Y1c es cicloalquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, haloalquilo inferior, halógeno, hidroxi, amino, ciano y alcoxi inferior; Y1d es amino opcionalmente sustituido por uno o más alquilo inferior, alcoxi alquilo inferior o hidroxi-alquilo inferior; Y2 es H, halógeno o alquilo inferior; Y3 es H, halógeno, alquilo inferior, haloalquilo inferior, alcoxi inferior o hidroxialquilo inferior; e Y4 es H, alquilo inferior o hidroxialquilo inferior; o una sal farmacéuticamente aceptable del mismo.
ARP120101712A 2011-05-17 2012-05-15 Inhibidores de la tirosina-quinasa de bruton AR086403A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161486809P 2011-05-17 2011-05-17
US201261635470P 2012-04-19 2012-04-19

Publications (1)

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AR086403A1 true AR086403A1 (es) 2013-12-11

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Country Status (20)

Country Link
US (1) US8729078B2 (es)
EP (1) EP2709997B1 (es)
JP (1) JP5859640B2 (es)
KR (1) KR101585753B1 (es)
CN (1) CN103582637B (es)
AR (1) AR086403A1 (es)
AU (1) AU2012257802A1 (es)
BR (1) BR112013029620A2 (es)
CA (1) CA2834077A1 (es)
CO (1) CO6852067A2 (es)
EC (1) ECSP13013025A (es)
ES (1) ES2590491T3 (es)
HK (1) HK1194381A1 (es)
IL (1) IL229197A0 (es)
MA (1) MA35112B1 (es)
MX (1) MX345170B (es)
SG (1) SG194728A1 (es)
TW (1) TW201300374A (es)
WO (1) WO2012156334A1 (es)
ZA (1) ZA201308397B (es)

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JP6526189B2 (ja) 2014-07-03 2019-06-05 ベイジーン リミテッド 抗ｐｄ−ｌ１抗体並びにその治療及び診断のための使用
JP6507234B2 (ja) * 2014-10-02 2019-04-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルトンチロシンキナーゼ（ｂｔｋ）によって介入される障害の処置における使用のためのピラゾールカルボキサミド化合物
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