[go: up one dir, main page]

PE20200447A1 - Compuestos de biheteroarilo y usos de los mismos - Google Patents

Compuestos de biheteroarilo y usos de los mismos

Info

Publication number
PE20200447A1
PE20200447A1 PE2019002479A PE2019002479A PE20200447A1 PE 20200447 A1 PE20200447 A1 PE 20200447A1 PE 2019002479 A PE2019002479 A PE 2019002479A PE 2019002479 A PE2019002479 A PE 2019002479A PE 20200447 A1 PE20200447 A1 PE 20200447A1
Authority
PE
Peru
Prior art keywords
pyrimidin
biheteroaril
compounds
compound
dlk
Prior art date
Application number
PE2019002479A
Other languages
English (en)
Inventor
Anthony Estrada
Paul Gibbons
Terry Kellar
Wen Liu
Changyou Ma
Alan Olivero
Snahel Patel
Daniel Shore
Michael Siu
Kevin X Chen
Malcolm Huestis
Liting Dong
Joseph P Lyssikatos
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 PE20200447A1 publication Critical patent/PE20200447A1/es

Links

Classifications

    • 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
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53861,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K35/00Medicinal preparations containing materials or reaction products thereof with undetermined constitution
    • A61K35/12Materials from mammals; Compositions comprising non-specified tissues or cells; Compositions comprising non-embryonic stem cells; Genetically modified cells
    • A61K35/30Nerves; Brain; Eyes; Corneal cells; Cerebrospinal fluid; Neuronal stem cells; Neuronal precursor cells; Glial cells; Oligodendrocytes; Schwann cells; Astroglia; Astrocytes; Choroid plexus; Spinal cord tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • 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
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • 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
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/06Antiglaucoma agents or miotics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/02Antidotes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • C07D403/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • 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
    • C07D487/12Heterocyclic 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 three hetero rings
    • C07D487/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Virology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Psychology (AREA)
  • Developmental Biology & Embryology (AREA)
  • Cell Biology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Biotechnology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Vascular Medicine (AREA)
  • AIDS & HIV (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Anesthesiology (AREA)
  • Urology & Nephrology (AREA)

Abstract

Referido a un compuesto de formula (I-I) o sus sales, en el que R1, R2 y R3 son cada uno independientemente H, F, Cl, Br, I, alquilo C1-6 o haloalquilo C1-6; X1 es N; X2 es N o CH; y A y Cy se selecciona entre el grupo que consiste en pirrolidina, piperidina, azetidina, entre otros. Un compuesto preferido es 5-[2-(3,3-difluoro-1-piperidil)-6-[(1S,4S)-2-oxa-5-azabiciclo[2.2.1]heptan-5-il]pirimidin-4-il]pirimidin-2-amina. Estos compuestos biheteroarilos inhiben la actividad de la doble quinasa de cremallera de leucina (DLK), siendo util para el tratamiento de enfermedades neurodegenerativas.
PE2019002479A 2013-05-01 2014-04-30 Compuestos de biheteroarilo y usos de los mismos PE20200447A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361817966P 2013-05-01 2013-05-01
PCT/CN2014/076654 WO2014177060A1 (en) 2013-05-01 2014-04-30 Biheteroaryl compounds and uses thereof

Publications (1)

Publication Number Publication Date
PE20200447A1 true PE20200447A1 (es) 2020-02-28

Family

ID=51841525

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2019002479A PE20200447A1 (es) 2013-05-01 2014-04-30 Compuestos de biheteroarilo y usos de los mismos
PE2016000335A PE20161063A1 (es) 2013-05-01 2014-04-30 Compuestos de biheteroarilo y usos de los mismos

Family Applications After (1)

Application Number Title Priority Date Filing Date
PE2016000335A PE20161063A1 (es) 2013-05-01 2014-04-30 Compuestos de biheteroarilo y usos de los mismos

Country Status (22)

Country Link
US (8) US9266862B2 (es)
EP (1) EP2991978B1 (es)
JP (4) JP6229042B2 (es)
KR (2) KR101836431B1 (es)
CN (2) CN110003178B (es)
AR (1) AR096151A1 (es)
AU (2) AU2014261894C1 (es)
BR (1) BR112015027055B1 (es)
CA (1) CA2911051C (es)
CL (1) CL2015003147A1 (es)
CR (2) CR20200177A (es)
EA (3) EA029568B8 (es)
IL (2) IL296526B2 (es)
MA (3) MA48577A1 (es)
MX (1) MX2015015130A (es)
MY (1) MY182082A (es)
PE (2) PE20200447A1 (es)
PH (2) PH12015502410B1 (es)
SG (2) SG11201509027WA (es)
TW (3) TWI622587B (es)
UA (1) UA121016C2 (es)
WO (1) WO2014177060A1 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2844652B1 (en) * 2012-05-03 2019-03-13 Genentech, Inc. Pyrazole aminopyrimidine derivatives as lrrk2 modulators
CN104918934B (zh) 2013-01-18 2017-12-22 霍夫曼-拉罗奇有限公司 3‑取代的吡唑及其作为dlk抑制剂的用途
KR20160002850A (ko) * 2013-05-01 2016-01-08 에프. 호프만-라 로슈 아게 C-연결된 헤테로사이클로알킬 치환된 피리미딘 및 이의 용도
MX2015015130A (es) * 2013-05-01 2016-02-18 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos.
MX2016008110A (es) * 2013-12-20 2016-08-19 Hoffmann La Roche Derivados de pirazol como inhibidores de la cinasa de cremallera de leucina dual (dlk) y usos de los mismos.
CN104926716A (zh) * 2015-06-10 2015-09-23 哈尔滨工业大学 吡啶衍生物2,6-二[(6-甲氧基吡啶-2-基)甲基]吡啶及其合成方法
KR20190040068A (ko) * 2016-08-29 2019-04-16 보드 오브 리전츠 더 유니버시티 오브 텍사스 시스템 질환의 치료를 위한 이중 류신 지퍼 (dlk) 키나아제의 저해제
ES2895257T3 (es) 2016-12-08 2022-02-18 Univ Texas Inhibidores de biciclo[1.1.1]pentano de cremallera de leucina doble cinasa (DLK) para el tratamiento de una enfermedad
CA3067944C (en) 2017-07-14 2023-03-14 F. Hoffmann-La Roche Ag Bicyclic ketone compounds and methods of use thereof
JP7362600B2 (ja) 2017-10-11 2023-10-17 エフ. ホフマン-ラ ロシュ アーゲー Rip1キナーゼ阻害剤として使用するための二環式化合物
JP7274473B2 (ja) * 2017-10-17 2023-05-16 パラウ ファルマ,エス.エル.ユー. 4-アミノピリミジン化合物の合成
CA3078688A1 (en) 2017-10-31 2019-05-09 F. Hoffmann-La Roche Ag Bicyclic sulfones and sulfoxides and methods of use thereof
EP3781571B1 (en) 2018-04-20 2024-01-17 F. Hoffmann-La Roche AG N-[4-oxo-2,3-dihydro-pyrido[3,2-b][1,4]oxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)
US11993586B2 (en) 2018-10-22 2024-05-28 Novartis Ag Crystalline forms of potassium channel modulators
WO2020132045A1 (en) 2018-12-19 2020-06-25 Disarm Therapeutics, Inc. Inhibitors of sarm1 in combination with neuroprotective agents
AR119673A1 (es) 2019-01-11 2022-01-05 Hoffmann La Roche Compuestos bicíclicos de cetona y métodos para utilizarlos
JP2022518603A (ja) * 2019-01-31 2022-03-15 中国医▲薬▼研究▲開▼▲発▼中心有限公司 芳香環又は芳香族複素環化合物、その製造方法及び医薬使用
US11560366B2 (en) 2019-10-21 2023-01-24 Board Of Regents, The University Of Texas System Bicyclo[1.1.1]pentane inhibitors of dual leucine zipper (DLK) kinase for the treatment of disease
JP2021070684A (ja) * 2019-10-30 2021-05-06 東ソー株式会社 ハロゲン化合物の製造方法
CN115335050B (zh) * 2020-01-29 2024-05-17 卡玛瑞制药有限公司 用于治疗皮肤病症的化合物和组合物
EP4222154A1 (en) * 2020-10-02 2023-08-09 Genentech, Inc. Process for the preparation of biheteroaryl compounds and crystal forms thereof
US20250032489A1 (en) * 2021-09-01 2025-01-30 The U.S.A., As Represented By The Secretary, Department Of Health And Human Services Mixed lineage kinase inhibitors and methods of use
WO2023067550A1 (en) * 2021-10-20 2023-04-27 Yousef Najajreh Allosteric inhibitor compounds for overcoming cancer resistance
TW202435863A (zh) 2023-01-28 2024-09-16 芬蘭商奧利安公司 Cbl-b抑制劑

Family Cites Families (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
EP0652775B1 (en) 1992-07-27 2000-04-19 THE GOVERNMENT OF THE UNITED STATES OF AMERICA as represented by the SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES Targeting of liposomes to the blood-brain barrier
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
AU2001286930A1 (en) 2000-08-30 2002-03-13 The Board Of Trustees Of The Leland Stanford Junior University Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
DE60234057D1 (de) 2001-07-25 2009-11-26 Raptor Pharmaceutical Inc Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
ATE411996T1 (de) 2002-09-30 2008-11-15 Bayer Healthcare Ag Kondensierte azolpyrimidinderivate
US7220833B2 (en) 2002-12-03 2007-05-22 Thomas Nelson Artificial low-density lipoprotein carriers for transport of substances across the blood-brain barrier
JP2007505142A (ja) 2003-09-10 2007-03-08 セダーズ−シナイ メディカル センター 血液脳関門を通過する薬剤のカリウムチャネル媒介性送達
GB0508471D0 (en) 2005-04-26 2005-06-01 Celltech R&D Ltd Therapeutic agents
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
WO2008064244A2 (en) 2006-11-20 2008-05-29 The Trustees Of Columbia University In The City Of New York Phosphoinositide modulation for the treatment of neurodegenerative diseases
CA2675558A1 (en) * 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
US8293747B2 (en) 2007-07-19 2012-10-23 Merck Sharp & Dohme Corp. Heterocyclic amide compounds as protein kinase inhibitors
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
US20100056609A1 (en) 2008-08-26 2010-03-04 Washington University Methods and compositions for inhibition of axonal degeneration by modulation of the dlk/jnk pathway
MX2011004585A (es) * 2008-10-31 2011-06-01 Novartis Ag Combinacion de un inhibidor de fosfatidilinositol-3-cinasa (p13k) y un inhibidor de mtor.
GB2465405A (en) 2008-11-10 2010-05-19 Univ Basel Triazine, pyrimidine and pyridine analogues and their use in therapy
KR20120063515A (ko) 2009-09-09 2012-06-15 아빌라 테라퓨틱스, 인크. Pi3 키나제 억제제 및 이들의 용도
RU2012120783A (ru) * 2009-10-22 2013-11-27 Женентек, Инк. Модуляция дегенерации аксона
GB201004200D0 (en) 2010-03-15 2010-04-28 Univ Basel Spirocyclic compounds and their use as therapeutic agents and diagnostic probes
WO2011149950A2 (en) 2010-05-24 2011-12-01 University Of Rochester Bicyclic heteroaryl kinase inhibitors and methods of use
WO2012122383A2 (en) * 2011-03-09 2012-09-13 Avila Therapeutics, Inc. Pi3 kinase inhibitors and uses thereof
MX2015015130A (es) 2013-05-01 2016-02-18 Hoffmann La Roche Compuestos de biheteroarilo y usos de los mismos.
CN103483345B (zh) 2013-09-25 2016-07-06 中山大学 Pi3k激酶抑制剂、包含其的药物组合物及其应用
JP5920747B1 (ja) 2015-04-07 2016-05-18 エイピーエス.エスエイ アプリケーションプログラムおよびカード

Also Published As

Publication number Publication date
NZ712934A (en) 2020-10-30
US10010549B2 (en) 2018-07-03
BR112015027055A2 (pt) 2017-07-25
MY182082A (en) 2021-01-18
EP2991978B1 (en) 2025-08-20
US20140328805A1 (en) 2014-11-06
US11129832B2 (en) 2021-09-28
US20160158234A1 (en) 2016-06-09
TW201506018A (zh) 2015-02-16
PE20161063A1 (es) 2016-10-22
CA2911051C (en) 2021-08-17
NZ750661A (en) 2020-11-27
EA201991064A1 (ru) 2020-02-28
MA42164A1 (fr) 2019-01-31
EA038235B1 (ru) 2021-07-28
PH12015502410B1 (en) 2023-05-24
HK1219276A1 (zh) 2017-03-31
US9266862B2 (en) 2016-02-23
US20180117044A1 (en) 2018-05-03
TWI622587B (zh) 2018-05-01
CN105431420A (zh) 2016-03-23
EA033084B1 (ru) 2019-08-30
IL242164B (en) 2021-04-29
CA2911051A1 (en) 2014-11-06
EA201592060A1 (ru) 2016-02-29
JP2023011775A (ja) 2023-01-24
USRE47848E1 (en) 2020-02-11
IL296526B2 (en) 2025-02-01
IL296526A (en) 2022-11-01
AU2014261894A1 (en) 2015-10-29
JP6655052B2 (ja) 2020-02-26
US20200188397A1 (en) 2020-06-18
BR112015027055B1 (pt) 2023-09-26
EP2991978A1 (en) 2016-03-09
TW201841907A (zh) 2018-12-01
KR102002265B1 (ko) 2019-07-19
BR112015027055A8 (pt) 2020-01-14
TWI710558B (zh) 2020-11-21
KR101836431B1 (ko) 2018-03-09
CN110003178B (zh) 2022-02-25
EP2991978C0 (en) 2025-08-20
JP2018035187A (ja) 2018-03-08
US20200171029A1 (en) 2020-06-04
MA38624A1 (fr) 2017-02-28
SG11201509027WA (en) 2015-12-30
JP2020079264A (ja) 2020-05-28
EP2991978A4 (en) 2016-09-14
MA48577A1 (fr) 2021-03-31
US20180133219A1 (en) 2018-05-17
JP6229042B2 (ja) 2017-11-08
KR20180026806A (ko) 2018-03-13
AU2014261894B2 (en) 2018-10-18
AU2014261894C1 (en) 2019-07-11
SG10201707002VA (en) 2017-10-30
EA029568B8 (ru) 2018-08-31
AU2019200249A1 (en) 2019-01-31
CN105431420B (zh) 2019-08-13
US20160052940A1 (en) 2016-02-25
CN110003178A (zh) 2019-07-12
KR20160003241A (ko) 2016-01-08
IL296526B1 (en) 2024-10-01
US10028954B2 (en) 2018-07-24
US20170239246A9 (en) 2017-08-24
AU2019200249B2 (en) 2020-10-15
WO2014177060A1 (en) 2014-11-06
CR20150589A (es) 2015-12-07
JP2016518383A (ja) 2016-06-23
MA42164B1 (fr) 2019-12-31
MX2015015130A (es) 2016-02-18
AR096151A1 (es) 2015-12-09
PH12019502378A1 (en) 2022-05-11
PH12015502410A1 (en) 2016-02-22
CL2015003147A1 (es) 2016-06-17
CR20200177A (es) 2020-06-28
EA201792471A1 (ru) 2018-04-30
EA029568B1 (ru) 2018-04-30
TW201800403A (zh) 2018-01-01
UA121016C2 (uk) 2020-03-25

Similar Documents

Publication Publication Date Title
PE20200447A1 (es) Compuestos de biheteroarilo y usos de los mismos
PE20130184A1 (es) Compuesto heterociclico
PE20141974A1 (es) Compuestos de heterociclilo
PE20181145A1 (es) Compuestos de piridina
PE20160995A1 (es) Inhibidores de syk
AR085960A1 (es) 1,3-oxazinas como inhibidores de la bace1 y/o de la bace2
PE20171177A1 (es) Compuestos aminopirimidinilo inhibidores de jak
PE20191613A1 (es) Compuestos de pirazolo[1,5-a]piridina sustituidos como inhibidores de la quinasa ret
PE20161443A1 (es) Compuestos
PE20150230A1 (es) Nuevos diazaespirocicloalcanos y azaespirocicloalcanos
PE20190337A1 (es) NUEVOS DERIVADOS DE PIRROLO [2,3-d]PIRIMIDA, UN PROCESO PARA SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN
PE20190339A1 (es) 1h-pirazolo[4,3-b] piridinas como inhibidores de pde1
PE20161405A1 (es) Analogos de cortistatina y sintesis y usos de los mismos
PE20200700A1 (es) Compuestos macrociclicos y usos de los mismos
NZ749437A (en) Processes and intermediates for making a jak inhibitor
AR088449A1 (es) Benzilindazoles sustituidos
PE20161292A1 (es) Compuestos de nicotinamida sustituida con heteroarilo
PE20141855A1 (es) Benzotienilo-pirrolotriazinas disustituidas y sus usos
PE20180552A1 (es) Nuevos compuestos biciclicos como inhibidores duales de atx/ca
AR093184A1 (es) Compuesto de pirimidina sustituida como inhibidor de quinurenina-3-monooxigenasa y composicion farmaceutica que lo comprenden
UY40181A (es) Pesticidas de azol bicíclico sustituido con heterociclos
UY32531A (es) Nuevos compuestos para el tratamiento de trastornos del snc
UY32096A (es) Derivados de 2-carboxamida - cicloamino - urea especìficos, sus sales farmacèuticamente aceptables, composiciones contenièndolos, pro-farmacos de los mismos, procesos para su produciòn y aplicaciones
PE20141691A1 (es) Compuestos con actividad nematicida
PE20170682A1 (es) Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias