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AR076066A1 - Inhibidores de la tirosina-quinasa de bruton - Google Patents

Inhibidores de la tirosina-quinasa de bruton

Info

Publication number
AR076066A1
AR076066A1 ARP100100592A ARP100100592A AR076066A1 AR 076066 A1 AR076066 A1 AR 076066A1 AR P100100592 A ARP100100592 A AR P100100592A AR P100100592 A ARP100100592 A AR P100100592A AR 076066 A1 AR076066 A1 AR 076066A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
hydroxy
halogen
lower alkyl
Prior art date
Application number
ARP100100592A
Other languages
English (en)
Inventor
Yan Lou
Keshab Sarma
Zachary Kevin Sweeney
Matthew C Lucas
Fariborz Firooznia
Daniel Fishlock
Timothy D Owens
Joshua Paul Gergely Taygerly
Steven Joseph Berthel
Jun-Bae Hong
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42097405&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR076066(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR076066A1 publication Critical patent/AR076066A1/es

Links

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • 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
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    • 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
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    • A61P35/00Antineoplastic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
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    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
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    • 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
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30Phthalazines
    • C07D237/32Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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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    • 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
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    • 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
    • C07D403/10Heterocyclic 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
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    • 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
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    • C07D413/14Heterocyclic 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
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems

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  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Pulmonology (AREA)
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  • Heart & Thoracic Surgery (AREA)
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Abstract

Los compuestos aquí descritos son utiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Estos compuestos son también utiles para tratar enfermedades inflamatorias y autoinmunes asociadas con una proliferacion aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la formula A y por lo menos un vehículo, diluyente o excipiente. Procesos de obtencion. Reivindicacion 1: Un compuesto de la formula (1): en la que: R es H, -R1, -R1-R2-R3, -R1-R3 o -R2-R3; en los que R1 es arilo, heteroarilo, cicloalquilo o heterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, hidroxi, hidroxi-alquilo inferior, alcoxi inferior, halogeno, nitro, amino, amido, ciano, oxo o halo-alquilo inferior; R2 es -C(=O), -C(=O)O, -C(=O)NR2', -NHC(=O)O, -C(R2')2, -C(=NH)NR2', -S(=O)2, -O, -C(R2')2C(=O), -C(R2')2C(=O)NR2', -C(R2')2N(R2')C(=O), -OC(R2')2, -C(R2')2NR2' o -C(=NH), cada R2' es con independencia H, alquilo inferior o haloalquilo inferior; y R3 es H o R4 es alquilo inferior, alcoxi inferior, amino, (alquilo inferior)-amino, (dialquilo inferior)-amino, arilo, aril-alquilo, alquilarilo, heteroarilo, alquil-heteroarilo, heteroaril-alquilo, cicloalquilo, alquil-cicloalquilo, cicloalquil-alquilo, heterocicloalquilo, alquil-hetero- cicloalquilo, heterocicloalquil-alquilo, cicloalquilo bicíclico, heterocicloalquilo bicíclico, espirocicloalquilo o espiroheterocicloalquilo, cada uno de ellos está opcionalmente sustituido por uno o más alquilo inferior, (alquilo inferior)-amino, (dialquilo inferior)-amino, hidroxi, hidroxi-alquilo inferior, alcoxi inferior, halogeno, nitro, amino, amido, acilo, ciano, oxo, guanidino, hidroxil-amino, carboxi, carbamoílo, carbamato, halo-alcoxi inferior o halo-alquilo inferior, en el que dos grupos alquilo inferior juntos pueden formar un anillo; X es CH o N; X' es CH o N, con la condicion de que si X es N, X' sea CH; Y1 es H, alquilo inferior o haloalquilo inferior; Y2' y cada Y2 son con independencia halogeno, oxima o alquilo inferior, dicho alquilo inferior está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por hidroxi, alcoxi inferior, haloalcoxi inferior, haloalquilo inferior, carboxi, amino y halogeno; n es el numero 0, 1 o 2; y Z* se elige entre el grupo: (2) en las que: Q es C(Y3) o N; cada Y3 es con independencia H, halogeno o alquilo inferior, dicho alquilo inferior está opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por hidroxi, alcoxi inferior, amino y halogeno; m es el numero 0 o 1; Y4 es Y4a, Y4b Y4c o Y4d; en los que Y4a es H o halogeno; Y4b es alquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por haloalquilo, halogeno, hidroxi, amino, ciano y alcoxi inferior; Y4c es cicloalquilo inferior opcionalmente sustituido por uno o más sustituyentes elegidos entre el grupo formado por alquilo inferior, haloalquilo inferior, halogeno, hidroxi, hidroxi-alquilo inferior, amino, ciano y alcoxi inferior; Y4d es amino opcionalmente sustituido por uno o más alquilo inferior, alcoxi-alquilo inferior o hidroxialquilo inferior; e Y5 es halogeno, hidroxi, alquilo inferior, alcoxi inferior, hidroxialquilo inferior, ciano o haloalquilo inferior; o una sal farmacéuticamente aceptable del mismo.
ARP100100592A 2009-03-02 2010-03-01 Inhibidores de la tirosina-quinasa de bruton AR076066A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US20902109P 2009-03-02 2009-03-02
US30006410P 2010-02-01 2010-02-01

Publications (1)

Publication Number Publication Date
AR076066A1 true AR076066A1 (es) 2011-05-18

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ID=42097405

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100592A AR076066A1 (es) 2009-03-02 2010-03-01 Inhibidores de la tirosina-quinasa de bruton

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US (1) US8299077B2 (es)
EP (1) EP2403846B1 (es)
JP (1) JP5512707B2 (es)
KR (1) KR101347978B1 (es)
CN (2) CN102341383B (es)
AR (1) AR076066A1 (es)
AU (1) AU2010220435B2 (es)
BR (1) BRPI1009112A2 (es)
CA (1) CA2753341C (es)
CL (1) CL2011002115A1 (es)
ES (1) ES2607644T3 (es)
HK (1) HK1216887A1 (es)
IL (1) IL214351A0 (es)
MX (1) MX339583B (es)
PE (2) PE20120081A1 (es)
RU (1) RU2542585C2 (es)
SG (1) SG173816A1 (es)
TW (2) TWI519529B (es)
WO (1) WO2010100070A1 (es)
ZA (1) ZA201301679B (es)

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