[go: up one dir, main page]

AR077267A1 - Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes. - Google Patents

Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes.

Info

Publication number
AR077267A1
AR077267A1 ARP100102285A ARP100102285A AR077267A1 AR 077267 A1 AR077267 A1 AR 077267A1 AR P100102285 A ARP100102285 A AR P100102285A AR P100102285 A ARP100102285 A AR P100102285A AR 077267 A1 AR077267 A1 AR 077267A1
Authority
AR
Argentina
Prior art keywords
nrara
alqc1
ora
halo
substituted
Prior art date
Application number
ARP100102285A
Other languages
English (en)
Inventor
Minna Bui
Yi Chen
Timothy David Cushing
Jason A Duquette
Benjamin Fisher
Lopez De Turiso Felix Gonzalez
Xiaolin Hao
Xiao He
Michael G Johnson
Brian Lucas
Original Assignee
Amgen Inc
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 Amgen Inc filed Critical Amgen Inc
Publication of AR077267A1 publication Critical patent/AR077267A1/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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • 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
    • 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
    • A61P19/02—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/02—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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Reivindicacion 1: Un compuesto caracterizado porque tiene la estructura de formula (1) o cualquier sal farmacéuticamente aceptable del mismo, en donde: X1 es C(R10) o N; X2 es C o N; X3 es C o N; X4 es C o N; X5 es C o N; en donde al menos dos de X2, X3, X4 y X5 son C; X6 es C(R6) o N; X7 es C(R7) o N; X8 es C(R10) o N; Y es N(R8), O, o S; n es 0, 1, 2 o 3; R1 es un anillo bicíclico de 8, 9, 10 u 11 miembros o monocíclico de 5, 6 o 7 miembros de enlace directo, ligado a alqC1-4, ligado a OalqC1-2, ligado a alqC1-2O, ligado a N(Ra) o ligado a O saturado, saturado parcialmente o no saturado que contiene 0, 1, 2, 3 o 4 átomos seleccionados de N, O y S, pero que contiene no más de un átomo O, o S, sustituido por 0, 1, 2 o 3 sustituyentes independientemente seleccionados de halo, alqC1-6, haloalqC1-4, ciano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, - NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaalqC2-6NRaRa y -NRaalqC2-6ORa, en donde los átomos de carbono disponibles del anillo están adicionalmente sustituidos por 0, 1 o 2 grupos oxo o tioxo, y en donde el anillo está adicionalmente sustituido por 0 o 1 grupo directamente enlazado, ligado a SO2, ligado a C(=O) o ligado a CH2 seleccionado de fenilo, piridilo, pirimidilo, morfolino, piperazinilo, piperadinilo, ciclopentilo, ciclohexilo todos de los cuales sustituidos además por 0, 1, 2 o 3 grupos Rb independientes; R2 se selecciona de H, halo, alqC1-6, haloalqC1-4, ciano, nitro, ORa, NRaRa, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -S(=O) Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa y -S(=O)2N(Ra)C(=O)NRaRa; R3 se selecciona de H, halo, nitro, ciano, alqC1-4, OalqC1-4, OhaloalqC1-4, NHalqC1-4, N(alqC1-4)alqC1-4 y haloalqC1-4; R4 es, independientemente, en cada caso, halo, nitro, ciano, alqC1-4, OalqC1-4, OhaloalqC1-4, NHalqC1-4, N(alqC1-4)alqC1-4, haloalqC1-4 o un anillo monocíclico de 5, 6 o 7 miembros no saturado que contiene 0, 1, 2, 3 o 4 átomos seleccionados de N, O y S, pero que contiene no más de un O, o S, el anillo está sustituido por 0, 1, 2 o 3 sustituyentes seleccionados de halo, alqC1-4, haloalqC1-3, -OalqC1-4, -NH2, -NHalqC1-4, -N(alqC1-4)alqC1-4; R5 es, independientemente, en cada caso, H, halo, alqC1-6, haloalqC1-4, o alqC1-6 sustituido por 1, 2 o 3 sustituyentes seleccionados de halo, ciano, OH, OalqC1-4, alqC1-4, haloalqC1-3, OalqC1-4, NH2, NHalqC1-4 y N(alqC1-4)alqC1-4; o ambos grupos R5 juntos forman un espiroalqC3-6 sustituido por 0, 1, 2 o 3 sustituyentes seleccionados de halo, ciano, OH, OalqC1-4, alqC1-4, haloalqC1-3, OalqC1-4, NH2, NHalqC1-4 y N(alqC1-4)alqC1-4; R6 es H, halo, NHR9 u OH, ciano, Oalq C1-4, alq C1-4, haloalq C1-3, Oalq C1-4, -C(=O)ORa, -C(=O)N(Ra)Ra o -N(Ra)C(=O)Rb; R7 se selecciona de H, halo, haloalq C1-4, ciano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaalqC2-6NRaRa, -NRaalqC2-6ORa y alqC1-6, en donde el alqC1-6 está sustituido por 0, 1, 2 o 3 sustituyentes seleccionados de halo, haloalq C1-4, ciano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaalqC2-6NRaRa, y -NRaalqC2-6ORa, y el alqC1-6 está adicionalmente sustituido por 0 o 1 anillos monocíclicos de 5, 6 o 7 miembros saturado, saturado parcialmente o no saturado que contienen 0, 1, 2, 3 o 4 átomos seleccionados de N, O y S, pero que contienen no más de un O, o S, en donde los átomos de carbono disponibles del anillo están sustituidos por 0, 1 o 2 grupos oxo o tioxo, en donde el anillo está sustituido por 0, 1, 2 o 3 sustituyentes independientemente seleccionados de halo, nitro, ciano, alq C1-4, Oalq C1-4, Ohaloalq C1-4, NHalq C1-4, N(alqC1-4)alqC1-4 y haloalq C1-4; o R7 y R8 juntos forman un puente -C=N- en donde el átomo de carbono está sustituido por H, halo, ciano, o un anillo monocíclico de 5, 6 o 7 miembros saturado, saturado parcialmente o no saturado que contiene 0, 1, 2, 3 o 4 átomos seleccionados de N, O y S, pero que contiene no más de un O, o S, en donde los átomos de carbono disponibles del anillo están sustituidos por 0, 1 o 2 grupos oxo o tioxo, en donde el anillo está sustituido por 0, 1, 2, 3 o 4 sustituyentes seleccionados de halo, alq C1-6, haloalq C1-4, ciano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, -OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, -S(=O)Ra, -S(=O)2Ra, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaalqC2-6NRaRa y NRaalqC2-6ORa; o R7 y R9 juntos forman un puente -N=C- en donde el átomo de carbono está sustituido por H, halo, alq C1-6, haloalq C1-4, ciano, nitro, ORa, NRaRa, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -S(=O)Ra, -S(=O)2Ra o -S(=O)2NRaRa; R8 es H, alq C1-6, C(=O)N(Ra)Ra, C(=O)Rb o haloalq C1-4; R9 es H, alqC1-6 o haloalq C1-4; R10 es cada que se presenta H, halo, alq C1-3, haloalq C1-3 o ciano; R11 se selecciona de H, halo, alq C1-6, haloalq C1-4, ciano, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Ra, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Ra, OalqC2-6NRaRa, -OalqC2-6ORa, -SRa, -S(=O)Ra, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Ra, -S(=O)2N(Ra)C(=O)ORa, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Ra, -N(Ra)C(=O)ORa, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Ra, -N(Ra)S(=O)2NRaRa, -NRaalqC2-6NRaRa, -NRaalqC2-6ORa, -NRaalqCO2Ra, -NRaalqC2-6SO2Rb, -CH2C(=O)Ra, -CH2C(=O)ORa, -CH2C(=O)NRaRa, -CH2C(=NRa)NRaRa, -CH2ORa, -CH2OC(=O)Ra, -CH2OC(=O)NRaRa, -CH2OC(=O)N(Ra)S(=O)2Ra, -CH2OalqC2-6NRaRa, -CH2OalqC2-6ORa, -CH2SRa, -CH2S(=O)Ra, -CH2S(=O)2Rb, -CH2S(=O)2NRaRa, -CH2S(=O)2N(Ra)C(=O)Ra, -CH2S(=O)2N(Ra)C(=O)ORa, -CH2S(=O)2N(Ra)C(=O)NRaRa, -CH2NRaRa, -CH2N(Ra)C(=O)Ra, -CH2N(Ra)C(=O)ORa, -CH2N(Ra)C(=O)NRaRa, -CH2N(Ra)C(=NRa)NRaRa, -CH2N(Ra)S(=O)2Ra, -CH2N(Ra)S(=O)2NRaRa, -CH2NRaalqC2-6NRaRa, -CH2NRaalqC2-6ORa, -CH2NRaalqC2-6CO2Ra, -CH2NRaalqC2-6SO2Rb, -CH2Rc, -C(=O)Rc y -C(=O)N(Ra)Rc; Ra es independientemente, cada que se presenta, H o Rb; Rb es independientemente, cada que se presenta, fenilo, bencilo o alq C1-6, el fenilo, bencilo y alqC1-6 están sustituidos por 0, 1, 2 o 3 sustituyentes seleccionados de halo, alq C1-4, haloalq C1-3, -OH, -Oalq C1-4, -NH2, -NHalqC1-4 y -N(alqC1-4)alqC1-4; y Rc es un anillo de 4, 5 o 6 miembros saturado o parcialmente saturado que contiene 1, 2 o 3 heteroátomos seleccionados de N, O y S, el anillo está sustituido por 0, 1, 2 o 3 sustituyentes seleccionados de halo, alq C1-4, haloalq C1-3, -Oalq C1-4, -NH2, -NHalqC1-4 y -N(alqC1-4)alqC1-4.
ARP100102285A 2009-06-25 2010-06-25 Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes. AR077267A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US22048809P 2009-06-25 2009-06-25

Publications (1)

Publication Number Publication Date
AR077267A1 true AR077267A1 (es) 2011-08-17

Family

ID=43066540

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100102285A AR077267A1 (es) 2009-06-25 2010-06-25 Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes.

Country Status (17)

Country Link
US (2) US20100331306A1 (es)
EP (1) EP2445900B1 (es)
JP (1) JP2013527123A (es)
KR (1) KR20140068742A (es)
AR (1) AR077267A1 (es)
AU (1) AU2010265974B2 (es)
BR (1) BRPI1016150A2 (es)
CA (1) CA2781865A1 (es)
CL (1) CL2011003296A1 (es)
EA (1) EA201270013A1 (es)
IL (1) IL216885A0 (es)
MX (1) MX2011013510A (es)
SG (1) SG176986A1 (es)
TW (1) TW201111362A (es)
UY (1) UY32743A (es)
WO (1) WO2010151740A2 (es)
ZA (1) ZA201200611B (es)

Families Citing this family (82)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2137186T1 (sl) * 2007-03-23 2016-04-29 Amgen Inc. Heterociklične spojine in njihove uporabe
CA2680853C (en) 2007-03-23 2012-07-17 Amgen Inc. 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
WO2009155121A2 (en) * 2008-05-30 2009-12-23 Amgen Inc. Inhibitors of pi3 kinase
MX2011013901A (es) 2009-06-25 2012-05-08 Amgen Inc Derivados de 4h-pirido [1,2-a] pirimidin-4-ona como inhibidores de pi3k.
WO2010151740A2 (en) 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
PT2448938E (pt) 2009-06-29 2014-07-31 Incyte Corp Pirimidinonas como inibidoras de pi3k
EP2513109A1 (en) 2009-12-18 2012-10-24 Amgen Inc. Heterocyclic compounds and their uses
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
UY33304A (es) 2010-04-02 2011-10-31 Amgen Inc Compuestos heterocíclicos y sus usos
WO2011130342A1 (en) 2010-04-14 2011-10-20 Incyte Corporation FUSED DERIVATIVES AS ΡI3Κδ INHIBITORS
US8604032B2 (en) 2010-05-21 2013-12-10 Infinity Pharmaceuticals, Inc. Chemical compounds, compositions and methods for kinase modulation
JO2998B1 (ar) 2010-06-04 2016-09-05 Amgen Inc مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
MX2012015143A (es) * 2010-06-30 2013-07-03 Amgen Inc Compuestos heterociclicos que contienen nitrogeno como inhibidores de pi3k delta.
AU2011272853A1 (en) * 2010-07-01 2013-01-10 Amgen Inc. Heterocyclic compounds and their use as inhibitors of PI3K activity
AU2011329806A1 (en) * 2010-11-17 2013-05-30 Amgen Inc. Quinoline derivatives as PIK3 inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Ｐｉ３ｋ阻害剤としてのｎ−（１−（置換フェニル）エチル）−９ｈ−プリン−６−アミン
WO2012087784A1 (en) * 2010-12-23 2012-06-28 Amgen Inc. Heterocyclic compounds and their uses
CN102070520A (zh) * 2011-01-14 2011-05-25 华东师范大学 以3-氧代-2,3-二芳基丙醛制备3-芳基取代喹啉的方法
WO2012100732A1 (en) * 2011-01-24 2012-08-02 Glaxo Group Limited Retinoid-related orphan receptor gamma modulators, composition containing them and uses thereof
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
CA2831582C (en) 2011-03-28 2019-01-08 Mei Pharma, Inc. (alpha-substituted aralkylamino and heteroarylalkylamino) pyrimidinyl and 1,3,5-triazinyl benzimidazoles, pharmaceutical compositions thereof, and their use in treating proliferative diseases
RS58326B1 (sr) * 2011-05-04 2019-03-29 Rhizen Pharmaceuticals S A Nova jedinjenja kao modulatori proteinskih kinaza
CN103998442B (zh) 2011-08-29 2016-09-14 无限药品股份有限公司 杂环化合物及其用途
EP3196202B1 (en) 2011-09-02 2019-02-27 Incyte Holdings Corporation Heterocyclylamines as pi3k inhibitors
WO2013038427A1 (en) * 2011-09-12 2013-03-21 Council Of Scientific & Industrial Research ARYLATED β-DICARBOIMYL COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF
MX352672B (es) 2011-09-27 2017-12-04 Amgen Inc Compuestos heterocíclicos como inhibidores de mdm2 para el tratamiento del cáncer.
ES2661510T3 (es) 2011-12-15 2018-04-02 Novartis Ag Uso de inhibidores de la actividad o función de PI3K
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
DK2834231T3 (en) * 2012-04-04 2016-04-18 Amgen Inc HETEROCYCLIC COMPOUNDS AND THEIR USES
UY34893A (es) 2012-07-10 2014-02-28 Takeda Pharmaceutical Derivados de azaindol
BR112015008515A2 (pt) 2012-10-16 2017-07-04 Janssen Pharmaceutica Nv moduladores de ror t de quinolinila ligada à heteroarila
CA2888485C (en) 2012-10-16 2021-01-26 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of ror.gamma.t
AU2013331496B2 (en) 2012-10-16 2017-07-27 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of ROR-gamma-t
EA035391B1 (ru) 2012-11-08 2020-06-05 Ризен Фармасьютикалз Са Фармацевтические композиции, содержащие ингибитор pde4 и ингибитор pi3-дельта или двойной ингибитор pi3-дельта-гамма киназы
US9029384B2 (en) 2012-12-21 2015-05-12 Gilead Calistoga, LLC. Phosphatidylinositol 3-kinase inhibitors
JP6125663B2 (ja) 2012-12-21 2017-05-10 ギリアード カリストガ エルエルシー ホスファチジルイノシトール３−キナーゼ阻害剤としての置換ピリミジンアミノアルキル−キナゾロン
EP2958902B1 (en) 2013-02-19 2017-11-15 Amgen Inc. Cis-morpholinone and other compounds as mdm2 inhibitors for the treatment of cancer
MX374513B (es) 2013-03-14 2025-03-06 Amgen Inc Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer.
US9481667B2 (en) 2013-03-15 2016-11-01 Infinity Pharmaceuticals, Inc. Salts and solid forms of isoquinolinones and composition comprising and methods of using the same
JOP20200296A1 (ar) 2013-06-10 2017-06-16 Amgen Inc عمليات صنع وأشكال بلورية من mdm2 مثبط
HK1223911A1 (zh) 2013-06-14 2017-08-11 Gilead Sciences, Inc. 磷脂醯肌醇3-激酶抑制剂
EP3057422B1 (en) 2013-10-15 2019-05-15 Janssen Pharmaceutica NV Quinolinyl modulators of ror(gamma)t
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
ES2739621T3 (es) 2013-10-15 2020-02-03 Janssen Pharmaceutica Nv Moduladores de alcohol secundario de ROR Gamma T de tipo quinolinilo
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
JP6423423B2 (ja) 2013-10-15 2018-11-14 ヤンセン ファーマシューティカ エヌ．ベー． Ｒｏｒγｔのアルキル結合キノリニルモジュレーター
EP4039256A1 (en) 2013-11-11 2022-08-10 Amgen Inc. Combination therapy including an mdm2 inhibitor and dasatinib or nilotinib for the treatment of chronic myeloid leukemia
UY35945A (es) 2014-01-09 2015-08-31 Takeda Pharmaceutical Derivados de azaindol
WO2015106014A1 (en) 2014-01-09 2015-07-16 Takeda Pharmaceutical Company Limited Azaindole derivatives
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
CU24428B1 (es) 2014-07-04 2019-06-04 Lupin Ltd Derivados de quinolizinona como inhibidores de pi3k
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
PL3262046T3 (pl) 2015-02-27 2021-05-04 Incyte Corporation Sole inhibitora pi3k i sposoby ich wytwarzania
CN106008479B (zh) * 2015-03-06 2020-01-10 南京圣和药业股份有限公司 作为磷脂酰肌醇3-激酶δ抑制剂的取代嘧啶类化合物及其应用
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
KR101845931B1 (ko) 2015-06-18 2018-04-05 한국화학연구원 헤테로아릴 유도체 또는 이의 약학적으로 허용가능한 염, 이의 제조방법 및 이를 유효성분으로 포함하는 pi3 키나아제 관련 질환의 예방 또는 치료용 약학적 조성물
CA3124815A1 (en) 2016-03-05 2017-09-14 Hangzhou Zhengxiang Pharmaceuticals Co., Ltd. Quinoline analogs as phosphatidylinositol 3-kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2018016416A (es) * 2016-07-04 2019-05-09 Bayer Cropscience Ag Benzosultamas y sus analogos y sus usos como fungicidas.
TW201815787A (zh) 2016-09-23 2018-05-01 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201813963A (zh) 2016-09-23 2018-04-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
TW201825465A (zh) 2016-09-23 2018-07-16 美商基利科學股份有限公司 磷脂醯肌醇3-激酶抑制劑
JOP20190272A1 (ar) 2017-05-22 2019-11-21 Amgen Inc مثبطات kras g12c وطرق لاستخدامها
AU2018271862B2 (en) 2017-05-23 2022-12-15 Mei Pharma, Inc. Combination therapy
US11351176B2 (en) 2017-08-14 2022-06-07 Mei Pharma, Inc. Combination therapy
AU2018329920B2 (en) 2017-09-08 2022-12-01 Amgen Inc. Inhibitors of KRAS G12C and methods of using the same
MA52501A (fr) 2018-05-04 2021-03-10 Amgen Inc Inhibiteurs de kras g12c et leurs procédés d'utilisation
KR102884803B1 (ko) 2018-06-01 2025-11-12 인사이트 코포레이션 Pi3k 관련 장애의 치료를 위한 투여 요법
US11285156B2 (en) 2018-06-12 2022-03-29 Amgen Inc. Substituted piperazines as KRAS G12C inhibitors
KR20250171404A (ko) 2018-08-31 2025-12-08 암젠 인크 Mdm2 억제제의 제조 방법
JP7377679B2 (ja) 2018-11-19 2023-11-10 アムジエン・インコーポレーテツド がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法
EP3738593A1 (en) 2019-05-14 2020-11-18 Amgen, Inc Dosing of kras inhibitor for treatment of cancers
CA3140392A1 (en) 2019-05-21 2020-11-26 Amgen Inc. Solid state forms
EP4045047A1 (en) 2019-10-15 2022-08-24 Amgen Inc. Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers
WO2021126816A1 (en) 2019-12-16 2021-06-24 Amgen Inc. Dosing regimen of a kras g12c inhibitor
TW202334089A (zh) 2021-11-02 2023-09-01 美商夫雷爾醫療公司 Ｐｐａｒｇ反向激動劑及其用途

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT72878B (en) 1980-04-24 1983-03-29 Merck & Co Inc Process for preparing mannich-base hydroxamic acid pro-drugs for the improved delivery of non-steroidal anti-inflammatory agents
DE3020458C2 (de) 1980-05-29 1986-07-31 Herzog, Thomas, Prof. Dr., 3500 Kassel Vorgehängte Fassaden-, Bau- oder Dekorationsplatte
TW232013B (es) 1992-04-24 1994-10-11 Takeda Pharm Industry Co Ltd
KR100224135B1 (ko) 1993-01-28 1999-10-15 다께다 구니오 퀴놀린 또는 퀴나졸린 유도체, 그 제조 및 용도
WO1995024394A1 (en) 1994-03-08 1995-09-14 Takeda Chemical Industries, Ltd. Quinoline or quinazoline derivatives as anti-inflammatory agents, in particular for treating arthritis
US6043062A (en) 1995-02-17 2000-03-28 The Regents Of The University Of California Constitutively active phosphatidylinositol 3-kinase and uses thereof
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5822910A (en) 1997-10-02 1998-10-20 Shewmake; I. W. Fishing line tensioning device
WO1999047485A1 (en) * 1998-03-18 1999-09-23 Humanetics Corporation Process for effecting allylic oxidation using dicarboxylic acid imides and chromium reagents
US6355636B1 (en) * 1999-04-21 2002-03-12 American Cyanamid Company Substituted 3-cyano-[1.7],[1.5], and [1.8] naphthyridine inhibitors of tyrosine kinases
SI2137186T1 (sl) * 2007-03-23 2016-04-29 Amgen Inc. Heterociklične spojine in njihove uporabe
CA2680853C (en) * 2007-03-23 2012-07-17 Amgen Inc. 3- substituted quinoline or quinoxaline derivatives and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
CA2700088A1 (en) 2007-09-26 2009-04-02 Astellas Pharma Inc. Quinolone derivative
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン， エルエルシー 複素環キナーゼ阻害剤
WO2010056865A1 (en) 2008-11-14 2010-05-20 Gilead Palo Alto, Inc. Quinoline derivatives as ion channel modulators
GB0821693D0 (en) * 2008-11-27 2008-12-31 Ucb Pharma Sa Therapeutic agents
US8513284B2 (en) 2009-02-13 2013-08-20 Ucb Pharma, S.A. Fused pyridine and pyrazine derivatives as kinase inhibitors
WO2010151740A2 (en) 2009-06-25 2010-12-29 Amgen Inc. Heterocyclic compounds and their uses
EP2499126B1 (en) 2009-11-12 2015-01-07 UCB Pharma, S.A. Fused bicyclic pyridine and pyrazine derivatives as kinase inhibitors
EP2513109A1 (en) * 2009-12-18 2012-10-24 Amgen Inc. Heterocyclic compounds and their uses
AU2011272853A1 (en) * 2010-07-01 2013-01-10 Amgen Inc. Heterocyclic compounds and their use as inhibitors of PI3K activity

Also Published As

Publication number Publication date
BRPI1016150A2 (pt) 2016-04-19
TW201111362A (en) 2011-04-01
WO2010151740A2 (en) 2010-12-29
MX2011013510A (es) 2012-03-07
UY32743A (es) 2010-12-31
IL216885A0 (en) 2012-03-01
SG176986A1 (en) 2012-02-28
EA201270013A1 (ru) 2012-06-29
AU2010265974B2 (en) 2014-09-11
US20100331306A1 (en) 2010-12-30
EP2445900A2 (en) 2012-05-02
WO2010151740A4 (en) 2011-05-19
CA2781865A1 (en) 2010-12-29
CL2011003296A1 (es) 2012-06-08
EP2445900B1 (en) 2016-03-02
KR20140068742A (ko) 2014-06-09
AU2010265974A1 (en) 2012-01-19
WO2010151740A3 (en) 2011-03-31
US9873704B2 (en) 2018-01-23
US20160333017A1 (en) 2016-11-17
ZA201200611B (en) 2012-10-31
JP2013527123A (ja) 2013-06-27

Similar Documents

Publication Publication Date Title
AR077267A1 (es) Derivados nitrogenados heterociclicos inhibidores selectivos de pi3k, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de enfermedades inflamatorias y/o autoinmunes.
AR074358A1 (es) Derivados de pirazina como inhibidores de la fosfodiesterasa 10
ES2525763T3 (es) Derivados del ácido fenilalcanoico sustituido y sus usos para el tratamiento de enfermedades respiratorias
AR043700A1 (es) Derivados de 3-substituida-4-pirimidona
AR046297A1 (es) Inhibidores de la dpp - iv metodos para prepararlos y composiciones farmaceuticas que los contienen como agente activo
AR078045A1 (es) Derivados de pirimidina, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de un medicamento para el tratamiento del cancer
AR054560A1 (es) Espiropiperidina como inhibidores de beta-secretasa para el tratamiento de la enfermedad de alzheimer
AR100442A1 (es) Derivados de pirido[1,2-a]pirimidin-4-ona para tratar atrofia muscular espinal
AR100691A1 (es) Esteroides neuroactivos, composiciones, y usos de los mismos
AR083169A1 (es) Compuestos para tratar enfermedades neurodegenerativas
PE20181093A1 (es) Compuestos heterociclicos y usos de los mismos
PE20181298A1 (es) Inhibidores de bromodominio bivalentes y usos de los mismos
PE20181045A1 (es) Compuestos utiles como inmunomoduladores
AR078152A1 (es) Compuestos heterociclicos, utiles para el tratamiento de hcv y composiciones farmaceuticas que los comprenden
AR076486A1 (es) Inhibidores de fosfoinositida 3 kinasa y composiciones farmaceuticas que los contienen.
UY30804A1 (es) Derivados de nicotinamida, sus sales y solvatos, composiciones farmacéuticas conteniendolas y aplicaciones
AR043111A1 (es) Derivados monoacilados de o-fenilendiaminas
AR082886A1 (es) Compuestos y composiciones farmaceuticas que los contienen
AR062677A1 (es) Derivados de biaril-sulfonamida, procesos de produccion y composiciones farmaceuticas que los comprenden
AR083367A1 (es) Compuestos de tipo quinazolinona como antagonistas de crth
AR096979A1 (es) Derivados de pirrol, su procedimiento de preparación y las composiciones farmacéuticas que los contienen
AR083849A1 (es) Antagonistas de mdm2 de espiro-oxindol
AR063602A1 (es) Derivados de espiroindolinona, formulaciones farmaceuticas que los contienen y su uso en la obtencion de un medicamento para el tratamiento de trastornos oncologicos.
AR044402A1 (es) Compuestos heterociclicos y su uso como inmunodepresores. composiciones farmaceuticas que los contienen.
AR070221A1 (es) Derivados de ftalazinona inhibidores de polimerasas, composiciones farmaceuticas que los contienen y usos de los mismos para prevenir y/o tratar tumores cancerigenos,lesiones isquemicas y otras enfermedades asociadas.

Legal Events

Date Code Title Description
FA Abandonment or withdrawal