MX2020003594A - Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd. - Google Patents

Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd.

Info

Publication number
MX2020003594A
MX2020003594A MX2020003594A MX2020003594A MX2020003594A MX 2020003594 A MX2020003594 A MX 2020003594A MX 2020003594 A MX2020003594 A MX 2020003594A MX 2020003594 A MX2020003594 A MX 2020003594A MX 2020003594 A MX2020003594 A MX 2020003594A
Authority
MX
Mexico
Prior art keywords
fshd
dux4
treatment
gene expression
kinase inhibitors
Prior art date
Application number
MX2020003594A
Other languages
English (en)
Inventor
Ning Shen
Angela Marie Cacace
Soto Luis Gustavo Alejandro Rojas
I I Thompson Lorin A I
Owen Brendan Wallace
Lucienne V Ronco
Alan Scott Robertson
Aaron Nakwon Chang
Original Assignee
Fulcrum Therapeutics 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 Fulcrum Therapeutics Inc filed Critical Fulcrum Therapeutics Inc
Publication of MX2020003594A publication Critical patent/MX2020003594A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N15/00—Mutation or genetic engineering; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification; Use of hosts therefor
    • C12N15/09—Recombinant DNA-technology
    • C12N15/11—DNA or RNA fragments; Modified forms thereof; Non-coding nucleic acids having a biological activity
    • C12N15/113—Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides; Antisense DNA or RNA; Triplex- forming oligonucleotides; Catalytic nucleic acids, e.g. ribozymes; Nucleic acids used in co-suppression or gene silencing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/437—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 five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/46—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates
    • C07K14/47—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals
    • C07K14/4701—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans from vertebrates from mammals not used
    • C07K14/4707—Muscular dystrophy
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6813—Hybridisation assays
    • C12Q1/6827—Hybridisation assays for detection of mutation or polymorphism
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6844—Nucleic acid amplification reactions
    • C12Q1/686—Polymerase chain reaction [PCR]
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q1/00—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions
    • C12Q1/68—Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
    • C12Q1/6876—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes
    • C12Q1/6883—Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/11—Protein-serine/threonine kinases (2.7.11)
    • C12Y207/11024—Mitogen-activated protein kinase (2.7.11.24), i.e. MAPK or MAPK2 or c-Jun N-terminal kinase
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5044—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics involving specific cell types
    • G01N33/5061—Muscle cells
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/68—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving proteins, peptides or amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/106—Pharmacogenomics, i.e. genetic variability in individual responses to drugs and drug metabolism
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Q—MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS; COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
    • C12Q2600/00—Oligonucleotides characterized by their use
    • C12Q2600/156—Polymorphic or mutational markers
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N2500/00—Screening for compounds of potential therapeutic value
    • G01N2500/10—Screening for compounds of potential therapeutic value involving cells

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Wood Science & Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Analytical Chemistry (AREA)
  • Microbiology (AREA)
  • General Engineering & Computer Science (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Cell Biology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pathology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • General Chemical & Material Sciences (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Toxicology (AREA)
  • Food Science & Technology (AREA)
  • General Physics & Mathematics (AREA)

Abstract

La presente invención se refiere a métodos y composiciones que incluyen agentes e inhibidores de la quinasa p38 que regulan la expresión de DUX4 y de los genes corriente abajo que incluyen, mas no se limitan a, ZSCAN4, LEUTX, PRAMEF2, TRIM43, MBD3L2, KHDC1L, RFPL2, CCNA1, SLC34A2, TPRX1, PRAMEF20, TRIM49, PRAMEF4, PRAME6, PRAMEF15, o ZNF280A. Se divulgan métodos útiles para tratar una enfermedad asociada con la expresión anormal de DUX4 y de los genes corriente abajo (por ejemplo, distrofia muscular facioescapulohumeral).
MX2020003594A 2017-10-05 2018-10-05 Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd. MX2020003594A (es)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762568754P 2017-10-05 2017-10-05
US201762568673P 2017-10-05 2017-10-05
US201862682563P 2018-06-08 2018-06-08
US201862682565P 2018-06-08 2018-06-08
PCT/US2018/054642 WO2019071147A1 (en) 2017-10-05 2018-10-05 INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD

Publications (1)

Publication Number Publication Date
MX2020003594A true MX2020003594A (es) 2021-04-07

Family

ID=63963605

Family Applications (2)

Application Number Title Priority Date Filing Date
MX2020003961A MX2020003961A (es) 2017-10-05 2018-10-05 Uso de inhibidores de p38 para reducir la expresion de dux4.
MX2020003594A MX2020003594A (es) 2017-10-05 2018-10-05 Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
MX2020003961A MX2020003961A (es) 2017-10-05 2018-10-05 Uso de inhibidores de p38 para reducir la expresion de dux4.

Country Status (28)

Country Link
US (5) US11479770B2 (es)
EP (3) EP3692144A1 (es)
JP (5) JP2021501130A (es)
KR (2) KR20200066655A (es)
CN (4) CN114748622B (es)
AU (2) AU2018346709A1 (es)
BR (2) BR112020006169A2 (es)
CA (4) CA3128468A1 (es)
CL (3) CL2020000911A1 (es)
CO (2) CO2020005351A2 (es)
DK (1) DK3691620T3 (es)
EC (1) ECSP20024210A (es)
ES (1) ES2927715T3 (es)
HR (1) HRP20221196T1 (es)
HU (1) HUE060024T2 (es)
IL (2) IL273589B (es)
LT (1) LT3691620T (es)
MX (2) MX2020003961A (es)
NZ (1) NZ762856A (es)
PH (2) PH12020550195A1 (es)
PL (1) PL3691620T3 (es)
PT (1) PT3691620T (es)
RS (1) RS63581B1 (es)
SG (2) SG10202110259QA (es)
TW (1) TWI793191B (es)
UY (1) UY37918A (es)
WO (2) WO2019071147A1 (es)
ZA (1) ZA202002315B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
US20210038653A1 (en) * 2018-02-02 2021-02-11 Fred Hutchinson Cancer Research Center Methods for treating facioscapulohumeral muscular dystrophy
TW202112368A (zh) 2019-06-13 2021-04-01 荷蘭商法西歐知識產權股份有限公司 用於治療有關dux4表現之疾病的抑制劑組合
WO2021105474A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. New compounds for treatment of diseases related to dux4 expression
WO2021105481A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. Novel compounds for treatment of diseases related to dux4 expression
CN111004802A (zh) * 2019-12-31 2020-04-14 深圳市疾病预防控制中心（深圳市卫生检验中心、深圳市预防医学研究所） 特异抑制p38MAPK基因表达的shRNA重组载体构建方法与应用
WO2022056266A2 (en) 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use
US20240342148A1 (en) * 2021-07-27 2024-10-17 Fulcrum Therapeutics, Inc. Methods of treating facioscapulohumeral muscular dystrophy with losmapimod
WO2024145662A1 (en) * 2022-12-30 2024-07-04 Altay Therapeutics, Inc. 2-substituted thiazole and benzothiazole compositions and methods as dux4 inhibitors

Family Cites Families (451)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4522811A (en) 1982-07-08 1985-06-11 Syntex (U.S.A.) Inc. Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US6369068B1 (en) 1995-06-07 2002-04-09 Smithkline Beecham Corporation Amino substituted pyrimidine containing compounds
IL118544A (en) 1995-06-07 2001-08-08 Smithkline Beecham Corp History of imidazole, the process for their preparation and the pharmaceutical preparations containing them
JP2001508395A (ja) 1996-01-11 2001-06-26 スミスクライン・ビーチャム・コーポレイション 新規シクロアルキル置換イミダゾール
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
WO1997032583A1 (en) 1996-03-08 1997-09-12 Smithkline Beecham Corporation Use of csaidtm compounds as inhibitors of angiogenesis
JP2000510327A (ja) 1996-03-12 2000-08-15 スミスクライン・ビーチャム・コーポレイション 医薬的に活性な化合物の同定方法
WO1997033883A1 (en) 1996-03-13 1997-09-18 Smithkline Beecham Corporation Novel pyrimidine compounds useful in treating cytokine mediated diseases
US6235760B1 (en) 1996-03-25 2001-05-22 Smithkline Beecham Corporation Treatment for CNS injuries
US6096739A (en) 1996-03-25 2000-08-01 Smithkline Beecham Corporation Treatment for CNS injuries
WO1998007425A1 (en) 1996-08-21 1998-02-26 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US6096753A (en) 1996-12-05 2000-08-01 Amgen Inc. Substituted pyrimidinone and pyridone compounds and methods of use
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
WO1998028292A1 (en) 1996-12-23 1998-07-02 Smithkline Beecham Corporation Novel piperidine containing compounds
US5965583A (en) 1997-04-24 1999-10-12 Ortho-Mcneil Pharmaceutical, Inc. Substituted imidazoles useful in the treatment of inflammatory disease
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
AU7966198A (en) 1997-06-13 1998-12-30 Smithkline Beecham Corporation Novel pyrazole and pyrazoline substituted compounds
US6610695B1 (en) 1997-06-19 2003-08-26 Smithkline Beecham Corporation Aryloxy substituted pyrimidine imidazole compounds
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
AR016294A1 (es) 1997-07-02 2001-07-04 Smithkline Beecham Corp Compuesto de imidazol sustituido, composicion farmaceutica que la contiene, su uso en la fabricacion de un medicamento y procedimiento para supreparacion
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
CN1279682A (zh) 1997-10-20 2001-01-10 霍夫曼-拉罗奇有限公司 双环激酶抑制剂
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
EP1075467B1 (en) 1998-05-05 2005-03-30 F. Hoffmann-La Roche Ag Pyrazole derivatives as p-38 map kinase inhibitors
US6316466B1 (en) 1998-05-05 2001-11-13 Syntex (U.S.A.) Llc Pyrazole derivatives P-38 MAP kinase inhibitors
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
NZ508790A (en) 1998-05-22 2003-10-31 Scios Inc Heterocyclic compounds and methods to treat cardiac failure and other disorders
US6448257B1 (en) 1998-05-22 2002-09-10 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6589954B1 (en) 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
US6340685B1 (en) 1998-05-22 2002-01-22 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
JP2002516322A (ja) 1998-05-22 2002-06-04 スミスクライン・ビーチャム・コーポレイション 新規２−アルキル置換イミダゾール化合物
JP2002517486A (ja) 1998-06-12 2002-06-18 バーテックス ファーマシューティカルズ インコーポレイテッド ｐ３８のインヒビター
EP1112070B1 (en) 1998-08-20 2004-05-12 Smithkline Beecham Corporation Novel substituted triazole compounds
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP2002526482A (ja) 1998-09-18 2002-08-20 バーテックス ファーマシューティカルズ インコーポレイテッド ｐ３８のインヒビター
EP1119254A4 (en) 1998-10-07 2004-05-12 Smithkline Beecham Corp STROKE TREATMENT
DE69914357T2 (de) 1998-11-04 2004-11-11 Smithkline Beecham Corp. Pyridin-4-yl oder pyrimidin-4-yl substituierte pyrazine
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
AU765473B2 (en) 1999-04-23 2003-09-18 Takeda Pharmaceutical Company Limited 5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
ATE376547T1 (de) 1999-05-21 2007-11-15 Scios Inc Derivate des indol-typs als p38 kinase inhibitoren
ATE312823T1 (de) 1999-07-09 2005-12-15 Boehringer Ingelheim Pharma Verfahren zur herstellung heteroarylsubstituierter ureaverbindungen
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
KR20020032591A (ko) 1999-09-17 2002-05-03 스튜어트 알. 수터, 스티븐 베네티아너, 피터 존 기딩스 라이노바이러스 감염에서의 ｃｓａｉｄ의 용도
JP3961830B2 (ja) 1999-10-21 2007-08-22 エフ．ホフマン−ラ ロシュ アーゲー ｐ３８プロテインキナーゼのインヒビターとしてのヘテロアルキルアミノ置換二環式窒素複素環
TR200201058T2 (tr) 1999-10-21 2002-07-22 F.Hoffmann-La Roche Ag P38 protein kinaz inhibitörleri olarak, alkilaminoyla ornatılmış bisiklik, azotlu heterosikller
WO2001038312A1 (en) 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)QUINAZOLIN-2-ONE COMPOUNDS AS CSBP/p38 KINASE INHIBITORS
ES2241675T3 (es) 1999-11-23 2005-11-01 Smithkline Beecham Corporation Compuestos de 3,4-dihidro-(1h)quinazolin-2-ona como inhibidores de cspb/p38 quinasa.
JP2003517471A (ja) 1999-11-23 2003-05-27 スミスクライン・ビーチャム・コーポレイション ３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オンおよびそのＣＳＢＰ／ｐ３８キナーゼ阻害剤としての使用
AU1782301A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
AU2735201A (en) 1999-12-28 2001-07-09 Pharmacopeia, Inc. Pyrimidine and triazine kinase inhibitors
US6906067B2 (en) 1999-12-28 2005-06-14 Bristol-Myers Squibb Company N-heterocyclic inhibitors of TNF-α expression
AU2001241927A1 (en) 2000-02-28 2001-09-12 Scios Inc. Inhibitors of p38-alpha kinase
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
US6565880B2 (en) 2000-07-24 2003-05-20 Boehringer Ingelheim Pharmaceuticals, Inc. Oral dosage formulations of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
CN1275964C (zh) 2000-08-31 2006-09-20 霍夫曼-拉罗奇有限公司 作为细胞增殖抑制剂的7－氧代吡啶并嘧啶
MXPA03001733A (es) 2000-08-31 2003-05-27 Hoffmann La Roche 7-oxo-piridopirimidinas.
WO2002032862A2 (en) 2000-10-19 2002-04-25 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of smoke inhalation
AU2002248269A1 (en) 2000-10-19 2002-08-12 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
EP1333833B1 (en) 2000-10-23 2011-08-24 GlaxoSmithKline LLC Novel trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compound for the treatment of CSBP/p38 kinase mediated diseases
JP2004522713A (ja) 2000-11-17 2004-07-29 ブリストル−マイヤーズ　スクイブ　カンパニー ｐ３８キナーゼ関連疾患の処置方法およびキナーゼインヒビターとして有用なピロロトリアジン化合物
CA2429258A1 (en) 2000-11-20 2002-06-13 Scios Inc. Piperidine/piperazine-type inhibitors of p38 kinase
CA2429382A1 (en) 2000-11-20 2002-06-06 Scios Inc. Indole-type inhibitors of p38 kinase
CA2429605A1 (en) 2000-11-20 2002-05-30 Scios Inc. Indol derivative and their use as inhibitors of p38 kinase
US20020165286A1 (en) 2000-12-08 2002-11-07 Hanne Hedeman Dermal anti-inflammatory composition
WO2002058695A1 (en) 2000-12-20 2002-08-01 Merck & Co., Inc. (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents
WO2002064594A2 (en) 2001-02-12 2002-08-22 F. Hoffmann-La Roche Ag 6-substituted pyrido-pyrimidines
EP1370253B8 (en) 2001-02-28 2008-11-26 Temple University of the Commonwealth System of Higher Education Use of alpha, beta unsaturated aryl sulfones for protecting cells and tissues from ionizing radiation toxicity
ES2251582T3 (es) 2001-03-09 2006-05-01 Pfizer Products Inc. Compuestos antiinflamatorios de bencimidazol.
ATE323701T1 (de) 2001-03-09 2006-05-15 Pfizer Prod Inc Triazolopyridine als entzündungshemmende mittel
WO2002076985A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076954A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
AU2002303145A1 (en) 2001-03-23 2002-10-08 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076984A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076463A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
ATE304009T1 (de) 2001-04-04 2005-09-15 Pfizer Prod Inc Neue benzotriazole mit entzündungshemmender wirkung
US20040136949A1 (en) 2001-04-24 2004-07-15 Matthias Grell Combination therapy using anti-angiogenic agents and tnf alpha
WO2002090360A1 (en) 2001-05-10 2002-11-14 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
EP1392300A1 (en) 2001-05-11 2004-03-03 Vertex Pharmaceuticals Incorporated 2,5-disubstituted pyridine, pyrimidine, pyridazine and 1, 2, 4-triazine derivatives for use as p38 inhibitors
DE60221392T2 (de) 2001-05-24 2008-04-17 Eli Lilly And Co., Indianapolis Neue pyrrolderivate als pharmazeutische mittel
ATE415162T1 (de) 2001-06-11 2008-12-15 Vertex Pharma Isochinolin-inhibitoren von p38
US7196095B2 (en) 2001-06-25 2007-03-27 Merck & Co., Inc. (Pyrimidinyl) (phenyl) substituted fused heteroaryl p38 inhibiting and PKG kinase inhibiting compounds
JP4510442B2 (ja) 2001-06-26 2010-07-21 ブリストル−マイヤーズ スクイブ カンパニー ＴＮＦ−α発現のＮ−ヘテロ環インヒビター
DE60219793T2 (de) 2001-07-11 2008-01-24 Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield Verfahren zur Behandlung von Cytokin-Vermittelten Erkrankungen
CA2454913A1 (en) 2001-08-20 2003-02-27 Boehringer Ingelheim Pharmaceuticals, Inc. Parenteral formulations of 1-(5-tert-butyl-2-p-tolyl-2h-pryrazol-3-yl)-3-¬4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl|-urea and a cyclodextrin
AU2002331179B2 (en) 2001-08-30 2008-04-17 F. Hoffmann-La Roche Ag Aminopyrrole compounds as antiinflammatory agents
US20040235808A1 (en) 2001-09-21 2004-11-25 Jiabing Wang Androstanes as androgen receptor modulators
US7205275B2 (en) 2001-10-11 2007-04-17 Amgen Inc. Methods of treatment using specific binding agents of human angiopoietin-2
WO2003032894A2 (en) 2001-10-12 2003-04-24 Pfizer Products Inc. Method of monitoring neuroprotective treatment
GB0124928D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124938D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124936D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124932D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124933D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124939D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124931D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
GB0124941D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
JP2005511593A (ja) 2001-11-08 2005-04-28 メルク　エンド　カムパニー　インコーポレーテッド 骨粗鬆症を治療するための組成物及び方法
US20040009990A1 (en) 2001-11-09 2004-01-15 Higgins Linda S. Method to treat cystic fibrosis
US20050261836A1 (en) 2001-12-05 2005-11-24 Wuyi Meng Crystal structure of mitogen-activated protein kinase-activated protein kinase 2 and binding pockets thereof
US20030118575A1 (en) 2001-12-11 2003-06-26 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering BIRB 796 BS
AU2003206382B2 (en) 2002-01-03 2008-01-24 Smithkline Beecham Corporation Novel pharmaceutical dosage forms and method for producing same
US7605152B2 (en) 2002-01-15 2009-10-20 Merck & Co., Inc. 17-hydroxy-4-aza-androstan-3-ones as androgen receptor modulators
DE10203749A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Anticholinergika, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
DE10203753A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Xanthencarbonsäureester, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
DE10203741A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Fluorencarbonsäureester, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
US20040023961A1 (en) 2002-02-11 2004-02-05 Bayer Corporation Aryl ureas with raf kinase and angiogenisis inhibiting activity
ATE485275T1 (de) 2002-02-12 2010-11-15 Glaxosmithkline Llc Nicotinamide und deren verwendung als p38 inhibitoren
ATE410429T1 (de) 2002-03-07 2008-10-15 Hoffmann La Roche Bicyclische pyridin- und pyrimidininhibitoren von p38-kinase
AU2003218235B2 (en) 2002-03-13 2008-05-15 Merck Sharp & Dohme Corp. Fluorinated 4-azasteroid derivatives as androgen receptor modulators
WO2003079986A2 (en) 2002-03-18 2003-10-02 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
US6900208B2 (en) 2002-03-28 2005-05-31 Bristol Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
RU2310657C2 (ru) 2002-04-03 2007-11-20 Ф.Хоффманн-Ля Рош Аг Имидазоконденсированные соединения и фармацевтическая композиция, содержащая их
BR0309009A (pt) 2002-04-05 2005-03-22 Boehringer Ingelheim Pharma Método para o tratamento de hipersecreção de muco
US20030225089A1 (en) 2002-04-10 2003-12-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions based on anticholinergics and p38 kinase inhibitors
DE10216339A1 (de) 2002-04-13 2003-10-23 Boehringer Ingelheim Pharma Neue Ester hydroxy-substituierter Stickstoffheterocyclen, Verfahren zu deren Herstellung sowie deren Verwendung als Arzneimittel
WO2003087394A1 (en) 2002-04-15 2003-10-23 Glaxo Group Limited A method of identifying a modudator for a serine/theronine kinase
BR0309053A (pt) 2002-04-19 2005-02-22 Smithkline Beecham Corp Compostos
EP1503996B1 (en) 2002-04-23 2008-12-24 Bristol-Myers Squibb Company Aryl ketone pyrrolo-triazine compounds useful as kinase inhibitors
DK1497019T3 (en) 2002-04-23 2015-08-03 Bristol Myers Squibb Co PYRROLO-TRIAZINANILINE COMPOSITIONS USED AS KINase INHIBITORS
US7388009B2 (en) 2002-04-23 2008-06-17 Bristol-Myers Squibb Company Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors
US20050131005A1 (en) 2002-04-30 2005-06-16 Jiabing Wang 4-azasteroid derivatives as androgen receptor modulators
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
AU2003229305A1 (en) 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
US7008958B2 (en) 2002-05-21 2006-03-07 Bristol-Myers Squibb Company 2-substituted 5-oxazolyl indole compounds useful as IMPDH inhibitors and pharmaceutical compositions comprising same
JP4245561B2 (ja) 2002-06-11 2009-03-25 メルク エンド カムパニー インコーポレーテッド （ハロ−ベンゾカルボニル）複素２環ｐ３８キナーゼ阻害剤
DE60310730T2 (de) 2002-07-09 2007-05-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmazeutische zusammensetzungen aus anticholinergica und p38 kinase hemmern zur behandlung von erkrankungen der atemwege
EP1575506A4 (en) 2002-07-25 2008-04-23 Scios Inc METHOD FOR IMPROVING LUNG FUNCTION WITH TGF-BETA INHIBITORS
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
JP4252534B2 (ja) 2002-08-06 2009-04-08 エフ．ホフマン−ラ ロシュ アーゲー ｐ−３８ＭＡＰキナーゼインヒビターとしての６−アルコキシ−ピリド−ピリミジン類
US6872726B2 (en) 2002-08-08 2005-03-29 Boehringer Ingelheim Pharmaceuticals Inc. Fluorinated di-aryl urea compounds
AU2003256297A1 (en) 2002-08-09 2004-02-25 Eli Lilly And Company Benzimidazoles and benzothiazoles as inhibitors of map kinase
US20040110755A1 (en) 2002-08-13 2004-06-10 Boehringer Ingelheim Pharmaceuticals, Inc. Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
CA2496445A1 (en) 2002-08-14 2004-02-26 Boehringer Ingelheim Pharmaceuticals, Inc. Anticoagulant and fibrinolytic therapy using p38 map kinase inhibitors
EP1539121A4 (en) 2002-08-29 2008-08-13 Scios Inc METHOD OF REQUESTING OSTEOGENESIS
PA8579601A1 (es) 2002-08-30 2004-05-07 Pfizer Prod Inc Compuestos antiinflamatorios de di y trifloruro-triazolo-piridinas
US7005523B2 (en) 2002-08-30 2006-02-28 Pfizer Inc. Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines
US20040092547A1 (en) 2002-08-30 2004-05-13 Pfizer Inc Alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
US7037923B2 (en) 2002-08-30 2006-05-02 Pfizer, Inc. Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines
AU2003253188A1 (en) 2002-08-30 2004-03-19 Pfizer Products Inc. Novel processes and intermediates for preparing triazolo-pyridines
US7012143B2 (en) 2002-08-30 2006-03-14 Dombroski Mark A Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
AU2003268464A1 (en) 2002-09-03 2004-03-29 Scios Inc. INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
JP2006503025A (ja) 2002-09-05 2006-01-26 サイオス インク． ｐ３８ＭＡＰキナーゼの抑制による疼痛治療
US20050288503A1 (en) 2002-09-06 2005-12-29 Adams Jerry L Novel compounds
US7115644B2 (en) 2002-09-13 2006-10-03 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds
WO2004026871A1 (en) 2002-09-17 2004-04-01 Eli Lilly And Company Novel pyrazolopyridine derivatves as pharmaceutical agents
WO2004029040A1 (en) 2002-09-27 2004-04-08 Janssen Pharmaceutica N.V. 3,4-disubstituted pyrroles and their for use in treating inflammatory diseases
WO2004033632A2 (en) 2002-10-04 2004-04-22 Bristol-Myers Squibb Company Hydantoin derivatives as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace)
US20050288299A1 (en) 2002-10-09 2005-12-29 Mavunkel Babu J Azaindole derivatives as inhibitors of p38 kinase
EP1560582A4 (en) 2002-10-09 2008-03-12 Scios Inc AZAINDOL DERIVATIVES AS INHIBITORS OF THE p38 KINASE
WO2004041277A1 (en) 2002-11-01 2004-05-21 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
EP1565475B1 (en) 2002-11-18 2009-04-08 F. Hoffmann-La Roche Ag Diazinopyrimidines and their use as protein kinase inhibitors
DE10255040A1 (de) 2002-11-26 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Carbaminsäureester mit anticholinerger Wirksamkeit
AU2003299652A1 (en) 2002-12-06 2004-06-30 Scios Inc. Methods for treating diabetes
WO2004069793A2 (en) 2003-01-28 2004-08-19 Bristol-Myers Squibb Company Novel 2-substituted cyclic amines as calcium sensing receptor modulators
CN1771234A (zh) 2003-02-05 2006-05-10 布里斯托尔-迈尔斯斯奎布公司 吡咯并三嗪激酶抑制剂的制备方法
MXPA05008450A (es) 2003-02-10 2005-10-18 Vertex Pharma Procesos para la preparacion de n-heteroaril-n-aril-aminas mediante reaccion de un ester de acido n-aril-carbamico con un halo-heteroarilo y procesos analogos.
US7205322B2 (en) 2003-02-12 2007-04-17 Bristol-Myers Squibb Company Thiazolidine compounds as calcium sensing receptor modulators
DE602004001676T2 (de) 2003-02-14 2007-08-30 Pfizer Products Inc., Groton Triazolo-Pyridine als entzündungshemmende Verbindungen
MXPA05008612A (es) 2003-02-14 2005-12-05 Smithkline Beecham Corp Compuestos novedosos.
TWI325865B (en) 2003-02-27 2010-06-11 Palau Pharma Sa Pyrazolopyridine derivatives
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
MXPA05009459A (es) 2003-03-03 2006-05-17 Array Biopharma Inc Inhibidores de p38 y sus metodos de uso.
US7030112B2 (en) 2003-03-25 2006-04-18 Bristol-Myers Squibb Company Pyrrolopyridazine compounds and methods of use thereof for the treatment of proliferative disorders
GB0308186D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308201D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
GB0308185D0 (en) 2003-04-09 2003-05-14 Smithkline Beecham Corp Novel compounds
ES2279361T3 (es) 2003-04-16 2007-08-16 F. Hoffmann-La Roche Ag Derivados de (6-(fenoxi)-pirido-3,4-dipirimidin-2-il)-amina como inhibidores de p38 kinasa para el tratamiento de estados inflamatorios tal como artritis reumatoide.
MXPA05011103A (es) 2003-04-16 2005-12-12 Hoffmann La Roche Compuestos de quinazolina.
PT1618092E (pt) 2003-05-01 2010-11-22 Bristol Myers Squibb Co Compostos de pirazol-amida substituídos com arilo úteis enquanto inibidores de cinase
GB0320244D0 (en) 2003-05-06 2003-10-01 Aventis Pharma Inc Pyrazoles as inhibitors of tumour necrosis factor
WO2004100874A2 (en) 2003-05-07 2004-11-25 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
MXPA05013059A (es) 2003-06-04 2006-03-02 Pfizer Derivados de 2-amino-piridina como agonistas del adrenoceptor beta-2.
ATE517872T1 (de) 2003-06-26 2011-08-15 Novartis Ag Fünfgliedrige p38-kinaseinhibitoren auf heterocyclusbasis
CN1816370A (zh) 2003-06-30 2006-08-09 麦克公司 用作雄激素受体调节剂的17－乙酰氨基－4－氮杂甾族化合物衍生物
CA2530182A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
WO2005009367A2 (en) 2003-07-17 2005-02-03 Ambit Biosciences Corporation Treatment of diseases with kinase inhibitors
GB0317482D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
GB0317484D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as pde4 inhibitors
US20050020587A1 (en) 2003-07-25 2005-01-27 Pfizer Inc Nicotinamide derivatives useful as PDE4 inhibitors
GB0317516D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd Nicotinamide derivatives useful as PDE4 inhibitors
CA2533803A1 (en) 2003-07-29 2005-02-10 Bristol-Myers Squibb Company Biomarkers of cyclin-dependent kinase modulation
GB0318814D0 (en) 2003-08-11 2003-09-10 Smithkline Beecham Corp Novel compounds
CL2004002050A1 (es) 2003-08-13 2005-06-03 Pharmacia Corp Sa Organizada B Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros.
CN1838958A (zh) 2003-08-22 2006-09-27 贝林格尔·英格海姆药物公司 治疗慢性阻塞性肺病和肺动脉高血压的方法
US20050053600A1 (en) 2003-09-09 2005-03-10 Lane Thomas E. Methods for treating rheumatoid arthritis
EP1663228A4 (en) 2003-09-10 2010-10-06 Merck Sharp & Dohme USE OF 17-HETEROCYCLIC-4-AZASTEROIDIAN DERIVATIVES AS MODULATORS OF THE ANDROGEN RECEPTOR
SG146624A1 (en) 2003-09-11 2008-10-30 Kemia Inc Cytokine inhibitors
CA2540828A1 (en) 2003-09-30 2005-04-14 Scios Inc. Heterocyclic amides and sulfonamides
WO2005032551A1 (en) 2003-09-30 2005-04-14 Scios Inc. TREATMENT OF CARDIOVASCULAR DISEASE WITH INHIBITORS OF p38 KINASE
US7232824B2 (en) 2003-09-30 2007-06-19 Scios, Inc. Quinazoline derivatives as medicaments
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
ES2281843T3 (es) 2003-11-13 2007-10-01 F. Hoffmann-La Roche Ag Pirido-7-pirimidin-7-onas sustituidas con hidroxialquilo.
EP1538201A1 (en) 2003-12-02 2005-06-08 F.Hoffmann-La Roche Ag Method for the recombinant production and purification of protein kinases
WO2005063715A1 (en) 2003-12-18 2005-07-14 Boehringer Ingelheim Pharmaceuticals, Inc. Polymorph of birb 796, a p38map kinase inhibitor
GB0329275D0 (en) 2003-12-18 2004-01-21 Merck Sharp & Dohme Therapeutic treatment
AU2004305318A1 (en) 2003-12-18 2005-07-07 Pfizer Products Inc. Methods of treating acute inflammation in animals with p38 MAP kinase inhibitors
US20060052390A1 (en) 2003-12-24 2006-03-09 Scios, Inc. Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition
US20060058296A1 (en) 2003-12-24 2006-03-16 Scios, Inc. Treatment of osteolytic lesions associated with multiple myeloma by inhibition of p38 map kinase
US20060079461A1 (en) 2003-12-24 2006-04-13 Scios, Inc. Treatment of multiple myeloma by inhibition of p38 MAP kinase
CN1921864A (zh) 2003-12-24 2007-02-28 西奥斯公司 使用TGF－β抑制剂治疗神经胶质瘤
GB0402140D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402138D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
BRPI0507198A (pt) 2004-01-30 2007-06-26 Merck Patent Gmbh derivados de bisariluréia
TWI332003B (en) 2004-01-30 2010-10-21 Lilly Co Eli Kinase inhibitors
GB0402137D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
GB0402143D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
US7863310B2 (en) 2004-02-03 2011-01-04 Eli Lilly And Company Kinase inhibitors
US7652146B2 (en) 2004-02-06 2010-01-26 Bristol-Myers Squibb Company Process for preparing 2-aminothiazole-5-carboxamides useful as kinase inhibitors
TWI338004B (en) 2004-02-06 2011-03-01 Bristol Myers Squibb Co Process for preparing 2-aminothiazole-5-aromatic carboxamides as kinase inhibitors
CA2557398A1 (en) 2004-02-26 2005-09-09 Hans-Peter Buchstaller Benzimidazolyl derivatives as kinase inhibitors
RU2006134021A (ru) 2004-02-27 2008-04-10 Ф.Хоффманн-Ля Рош Аг (Ch) Производные гетероарил-конденсированного пиразола
KR20060114022A (ko) 2004-02-27 2006-11-03 에프. 호프만-라 로슈 아게 인다졸 유도체 및 그들을 함유하는 약학 조성물
AU2005227192A1 (en) 2004-03-11 2005-10-06 Kythera Biopharmaceuticals, Inc. Compositions and methods for preventing and treating skin and hair conditions
EP1574501A1 (en) 2004-03-11 2005-09-14 Pfizer Limited Quinolinone derivatives, pharmaceutical compositions containing them and their use
EP1577291A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylethanolamine derivatives as beta-2 agonists
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
EP1742631A4 (en) 2004-04-28 2009-11-11 Merck & Co Inc FLUORATED 4-AZASTEROIDS AS ANDROGEN RECEPTOR MODULATORS
WO2005110455A2 (en) 2004-05-13 2005-11-24 Intermune, Inc. Combination therapy for treating hepatitis virus infection
UA87854C2 (en) 2004-06-07 2009-08-25 Мерк Энд Ко., Инк. N-(2-benzyl)-2-phenylbutanamides as androgen receptor modulators
SI1761520T1 (sl) 2004-06-23 2008-10-31 Lilly Co Eli Inhibitorji kinaze
EP1609789A1 (en) 2004-06-23 2005-12-28 Eli Lilly And Company Ureido-pyrazole derivatives and their use as kinase inhibitors
US7253167B2 (en) 2004-06-30 2007-08-07 Bristol-Myers Squibb Company Tricyclic-heteroaryl compounds useful as kinase inhibitors
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
TW200618803A (en) 2004-08-12 2006-06-16 Bristol Myers Squibb Co Process for preparing pyrrolotriazine aniline compounds useful as kinase inhibitors
GEP20104973B (en) 2004-08-12 2010-04-26 Pfizer Triazolopyridinylsulfanyl derivatives as p38 map kinase inhibitors
AU2005280334A1 (en) 2004-08-25 2006-03-09 Merck Sharp & Dohme Corp. Androgen receptor modulators
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
PE20060493A1 (es) 2004-10-05 2006-09-03 Smithkline Beecham Corp Compuestos derivados de bifenil (di o tri) carboxamidas como inhibidores de serina/treonina quinasa p38
CA2584185C (en) 2004-10-13 2014-07-15 Frank Stieber Heterocyclic substituted bisarylurea derivates as kinase inhibitors
CA2583217C (en) 2004-10-18 2011-05-31 Amgen Inc. 1,3,4-thiadiazole compounds as protein kinase inhibitors
CA2585276A1 (en) 2004-10-29 2006-06-08 Merck & Co., Inc. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
WO2006055302A2 (en) 2004-11-04 2006-05-26 Scios Inc. Method of treating myelodysplastic syndromes
WO2006048266A2 (en) 2004-11-04 2006-05-11 Roche Diagnostics Gmbh Gene expression profiling of leukemias with mll gene rearrangements
GB0425057D0 (en) 2004-11-12 2004-12-15 Pfizer Ltd L-tartrate salt of N-1-adamantyl-2-{3-[(2R)-2-hydroxy-2-[4-hydroxy-3-(hydroxymethyl)phenyl]eth yl}amino)propyl]phenyl}acetamide
WO2006051373A1 (en) 2004-11-12 2006-05-18 Pfizer Limited Compounds for the treatment of diseases
WO2006055381A2 (en) 2004-11-16 2006-05-26 Merck & Co., Inc. Prodrugs of (2r)-2-propyloctanoic acid for treatment of stroke
US20080139614A1 (en) 2004-11-23 2008-06-12 Seabrook Guy R Treatment Of Stroke With Histamine H3 Inverse Agonists Or Histamine H3 Antagonists
US20060111416A1 (en) 2004-11-24 2006-05-25 Lane Charlotte A L Octahydropyrrolo[3,4-C]pyrrole derivatives
US20070224662A1 (en) 2004-12-17 2007-09-27 Jun Luo Post-translational modification of proteins in cell-free expression systems
PE20061155A1 (es) 2004-12-24 2006-12-16 Boehringer Ingelheim Int Derivados de indolinona como agentes para el tratamiento o la prevencion de enfermedades fibroticas
US20060154939A1 (en) 2004-12-24 2006-07-13 Boehringer Ingelheim International Gmbh Medicaments for the Treatment or Prevention of Fibrotic Diseases
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
ATE538118T1 (de) 2004-12-28 2012-01-15 Aska Pharm Co Ltd Pyrimidinylisoxazolderivat
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
ATE469893T1 (de) 2005-02-28 2010-06-15 Merckle Gmbh 2-sulfinyl- und 2-sulfonyl-substituierte imidazolderivate und deren verwendung als cytokininhibitoren
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
JP2008535822A (ja) 2005-03-25 2008-09-04 グラクソ グループ リミテッド 新規化合物
AR053346A1 (es) 2005-03-25 2007-05-02 Glaxo Group Ltd Compuesto derivado de 8h -pirido (2,3-d) pirimidin -7 ona 2,4,8- trisustituida composicion farmaceutica y uso para preparar una composicion para tratamiento y profilxis de una enfermedad mediada por la quinasa csbp/ rk/p38
TW200724142A (en) 2005-03-25 2007-07-01 Glaxo Group Ltd Novel compounds
US20060235020A1 (en) 2005-04-18 2006-10-19 Soojin Kim Process for preparing salts of 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide and novel stable forms produced therein
TW200716561A (en) 2005-05-11 2007-05-01 Array Biopharma Inc P38 inhibitors and methods of use thereof
WO2006127678A2 (en) 2005-05-23 2006-11-30 Smithkline Beecham Corporation Inhibition of p38 mark for treatment of obesity
GB0512429D0 (en) 2005-06-17 2005-07-27 Smithkline Beecham Corp Novel compound
US20070032506A1 (en) 2005-07-02 2007-02-08 Peter Giannousis Crystalline forms of (2r-trans)-6-chloro-5[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-n,n, 1-trimethyl-alpha-oxo-1h-indole-3-acetamide monohydrochloride
US7473784B2 (en) 2005-08-01 2009-01-06 Bristol-Myers Squibb Company Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors
US20090088458A1 (en) 2005-08-02 2009-04-02 Meissner Robert S N-(Pyridin-4-Yl)-2-Phenylbutanamides as Androgen Receptor Modulators
JP5113751B2 (ja) 2005-08-12 2013-01-09 メルク・シャープ・エンド・ドーム・コーポレイション ｐ３８キナーゼ阻害剤として有用な二環性複素環化合物
EP1928843A1 (en) 2005-08-22 2008-06-11 Amgen, Inc Bis-aryl urea compounds for the treatment of protein kinase-mediated diseaes
CN101243088B (zh) 2005-08-25 2011-06-29 霍夫曼-拉罗奇有限公司 p38 MAP激酶抑制剂及使用它的方法
EP1919877A1 (en) 2005-08-25 2008-05-14 F.Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
JP2009506006A (ja) 2005-08-25 2009-02-12 エフ．ホフマン−ラ ロシュ アーゲー ｐ３８ＭＡＰキナーゼ阻害剤およびその使用方法
CA2620104A1 (en) 2005-08-25 2007-03-01 F. Hoffman-La Roche Ag Fused pyrazole as p38 map kinase inhibitors
BRPI0615272A2 (pt) 2005-08-25 2009-08-04 Hoffmann La Roche inibidores de p38 map kinase e métodos para uso dos mesmos
EP1919919A1 (en) 2005-09-01 2008-05-14 Astellas Pharma Inc. Pyridazinone derivatives used for the treatment of pain
SI1928821T1 (sl) 2005-09-21 2009-04-30 Pfizer Ltd Derivati karboksamida kot antagonisti muskarinskih receptorjev
CA2623063A1 (en) 2005-09-26 2007-04-05 Merck & Co., Inc. N-(4-oxo-3,4-dihydroquinazolin-2-yl)butanamides as androgen receptor modulators
WO2007045989A1 (en) 2005-10-20 2007-04-26 Pfizer Limited Pyridyl derivatives useful as h3 ligands
DOP2006000233A (es) 2005-10-28 2007-06-15 Lilly Co Eli Inhibidores de cinasa
AR056582A1 (es) 2005-10-28 2007-10-10 Lilly Co Eli COMPUESTOS DE PIRAZOLIL UREA CON ACTIVIDAD INHIBITORIA DE CINASA P38 Y FORMULACIoN FARMACÉUTICA QUE LO COMPRENDE
WO2007056016A2 (en) 2005-11-02 2007-05-18 Kemia, Inc. Bisamide cytokine inhibitors
EP1945639A1 (en) 2005-11-04 2008-07-23 Pfizer Limited Tetrahydronaphthyridine derivative
AU2006313430B2 (en) 2005-11-08 2012-09-06 Ranbaxy Laboratories Limited Process for (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- [(4-hydroxy methyl phenyl amino) carbonyl]-pyrrol-1-yl]-3, 5-dihydroxy-heptanoic acid hemi calcium salt
PE20070823A1 (es) 2005-11-15 2007-08-09 Glaxo Group Ltd Sal tosilato de 8-(2,6-difluorofenil)-4-(4-fluoro-2-metilfenil)-2-{[2-hidroxi-1-(hidroximetil)etil]amino}pirido[2,3-]pirimidin-7(8h)-ona
NL2000323C2 (nl) 2005-12-20 2007-11-20 Pfizer Ltd Pyrimidine-derivaten.
WO2007075896A2 (en) 2005-12-22 2007-07-05 Kemia, Inc. Heterocyclic cytokine inhibitors
ES2389062T3 (es) 2006-01-18 2012-10-22 Amgen, Inc Compuestos de tiazol como inhibidores de proteína cinasa B (PKB)
CN101415685B (zh) 2006-01-31 2011-08-24 阿雷生物药品公司 激酶抑制剂及其使用方法
WO2007091152A1 (en) 2006-02-09 2007-08-16 Pfizer Limited Triazolopyridine compounds
EP1987022A1 (en) 2006-02-10 2008-11-05 Pfizer Products Inc. Pyridinone pyrazole urea and pyrimidinone pyrazole urea derivatives
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
KR20080100484A (ko) 2006-03-07 2008-11-18 버텍스 파마슈티칼스 인코포레이티드 류마티스관절염 치료용 ｖｘ-702의 용도
BRPI0708644A2 (pt) 2006-03-07 2011-06-07 Bristol-Myers Squibb Company compostos de pró-fármaco de anilina de pirrolotriazina úteis como inibidores de cinase
AU2007228511A1 (en) 2006-03-20 2007-09-27 Pfizer Limited Amine derivatives
EP2029581A1 (en) 2006-03-29 2009-03-04 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
JP2009533362A (ja) 2006-04-12 2009-09-17 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング キナーゼ媒介性疾患を治療するための複素環式置換ビスアリール尿素のｎ−オキシド
WO2007124181A2 (en) 2006-04-21 2007-11-01 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
AU2007257959A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
GB0612026D0 (en) 2006-06-16 2006-07-26 Smithkline Beecham Corp New use
JP2009542816A (ja) 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
US20090318424A1 (en) 2006-06-16 2009-12-24 Mauro Corsi Novel compounds
JP2009542817A (ja) 2006-06-16 2009-12-03 グラクソ グループ リミテッド 新規化合物
EP2036905B1 (en) 2006-06-28 2012-12-12 ASKA Pharmaceutical Co., Ltd. Pyridylisoxazole derivative
EP2044957A4 (en) 2006-06-28 2011-01-05 Aska Pharm Co Ltd TREATMENT AGENT FOR INFLAMMATORY BOWEL DISEASE
WO2008011032A1 (en) 2006-07-17 2008-01-24 Amgen Inc. Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors
WO2008013823A2 (en) 2006-07-26 2008-01-31 Scios Inc. Co-crystals of (2r-trans)-6-chloro-5-[[4-[(4-fluorophenyl)methyl]-2,5-dimethyl-1-piperazinyl]carbonyl]-n,n,1-trimethyl-alpha-oxo-1h-indole-3-acetamide
CA2659222C (en) 2006-07-28 2012-01-31 Onconova Therapeutics, Inc. Formulations of radioprotective .alpha., .beta. unsaturated aryl sulfones
PE20080906A1 (es) 2006-08-17 2008-07-05 Kemia Inc Derivados heteroarilo como inhibidores de citocina
WO2008024391A1 (en) 2006-08-22 2008-02-28 Scios Inc. Pharmaceutical formulations of an indole-type derivative and related methods of use
BRPI0719270A2 (pt) 2006-10-04 2014-03-11 Pfizer Ltd Derivados de sulfonamida como agonistas adrenérgicos e antagonistas muscarínicos
ES2377821T3 (es) 2006-10-11 2012-04-02 Amgen Inc. Compuestos de imidazo- y triazolo-piridina y métodos de uso de los mismos.
WO2008048540A2 (en) 2006-10-18 2008-04-24 Merck & Co., Inc. 2-hydroxy-2-phenyl/thiophenyl propionamides as androgen receptor modulators
US20100099651A1 (en) 2006-10-26 2010-04-22 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
US7943617B2 (en) 2006-11-27 2011-05-17 Bristol-Myers Squibb Company Heterobicyclic compounds useful as kinase inhibitors
WO2008071665A1 (en) 2006-12-12 2008-06-19 Smithkline Beecham Corporation A nicotinamide derivative useful as p38 kinase inhibitor
WO2008071664A1 (en) 2006-12-12 2008-06-19 Smithkline Beecham Corporation Nicotinamide derivative used as a p38 kinase inhibitor
CA2670730A1 (en) 2006-12-13 2008-06-26 Gilead Sciences, Inc. Monophosphates as mutual prodrugs of anti-inflammatory signal transduction modulators (aistm's) and beta-agonists for the treatment of pulmonary inflammation and bronchoconstriction
CA2672256C (en) 2006-12-13 2011-08-30 Pfizer Products Inc. Processes for the preparation of 3-(4-(2,4-difluorobenzyloxy)-3-bromo-6-methyl-2-oxopyridin-1(2h)-yl)-n,4-dimethylbenzamide
JP2010513370A (ja) 2006-12-19 2010-04-30 エフ．ホフマン−ラ ロシュ アーゲー ピラゾロ［３，４−ｄ］ピリミジンｐ３８ＭＡＰキナーゼインヒビター
WO2008079857A1 (en) 2006-12-20 2008-07-03 Bristol-Myers Squibb Company Crystalline forms of aryl-substituted pyrazole-amide compounds
WO2008089034A2 (en) 2007-01-11 2008-07-24 Kemia, Inc. Cytokine inhibitors
WO2008098096A1 (en) 2007-02-08 2008-08-14 Boehringer Ingelheim International Gmbh Anti-cytokine heterocyclic compounds
AU2008219165A1 (en) 2007-02-16 2008-08-28 Merck Sharp & Dohme Corp. Compositions and methods for potentiated activity of biologicaly active molecules
EP2123255B1 (en) 2007-02-16 2013-05-15 ASKA Pharmaceutical Co., Ltd. Pharmaceutical composition containing fine particle oil-based suspension
WO2008104473A2 (en) 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Pyrazolopyriidine derivatives and their use as kinase inhibitors
ES2364727T3 (es) 2007-03-16 2011-09-13 Pfizer Limited Sal clorhidrato de 5-[3-(3-hidroxifenoxi)azetidin-1-il]-5-metil-2,2-difenilhexanamida.
WO2008137176A1 (en) 2007-05-07 2008-11-13 Amgen Inc. Pyrazolo-pyridinone compounds, process for their preparation, and their pharmaceutical use
CA2685597C (en) 2007-05-07 2012-10-02 Amgen Inc. Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as p38 modulators, process for their preparation, and their pharmaceutical use
AU2008276512A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole modulators of PKB
AU2008276521B2 (en) 2007-07-17 2011-11-03 Amgen Inc. Heterocyclic modulators of PKB
US7943658B2 (en) 2007-07-23 2011-05-17 Bristol-Myers Squibb Company Indole indane amide compounds useful as CB2 agonists and method
WO2009015000A1 (en) 2007-07-25 2009-01-29 Array Biopharma Inc. Pyrazole urea derivatives used as kinase inhibitors
CA2699463A1 (en) 2007-09-14 2009-03-19 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
US8314131B2 (en) 2007-09-21 2012-11-20 Amgen Inc. Triazole fused heteroaryl compounds and methods of use thereof
CN101878221B (zh) 2007-11-30 2014-04-02 辉瑞有限公司 糖皮质激素受体激动剂
GB0724258D0 (en) 2007-12-12 2008-01-30 Glaxo Group Ltd Novel combinations
WO2009074518A1 (en) 2007-12-12 2009-06-18 Glaxo Group Limited Combinations of prolinamide p2x7 modulators with further therapeutic agents
WO2009078992A1 (en) 2007-12-17 2009-06-25 Amgen Inc. Linear tricyclic compounds as p38 kinase inhibitors
EP2235537A2 (en) 2008-01-25 2010-10-06 Bristol-Myers Squibb Pharma Company Identification of predictive markers of response to dasatinib in human colon cancer
CA2716124A1 (en) 2008-02-20 2009-08-27 Boehringer Ingelheim International Gmbh Powder inhalers
US8367671B2 (en) 2008-03-21 2013-02-05 Amgen Inc. Pyrazolo[3.4-B]pyrazine compounds as p38 modulators and methods of use as anti-inflamatory agents
JP2009263234A (ja) 2008-04-21 2009-11-12 Ranbaxy Lab Ltd ホスホジエステラーゼタイプｉｖ阻害剤の組成物
AR072008A1 (es) 2008-06-13 2010-07-28 Merck & Co Inc Compuestos heterobiciclicos como agentes de inhibicion de quinasa p38
JP2011525184A (ja) 2008-06-20 2011-09-15 ブリストル−マイヤーズ スクイブ カンパニー キナーゼ阻害剤として有用なトリアゾロピリジン化合物
US8338604B2 (en) 2008-06-20 2012-12-25 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
WO2009158450A1 (en) 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, preparation and use thereof
WO2009158446A2 (en) 2008-06-25 2009-12-30 Bristol-Myers Squibb Company Crystalline forms of ((((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbonyl)(propyl)carbamoyl)oxy)methyl (4-(phosphonooxy)phenyl)acetate, method of preparation and use thereof
US8263623B2 (en) 2008-07-11 2012-09-11 Pfizer Inc. Triazol derivatives useful for the treatment of diseases
WO2010007561A1 (en) 2008-07-15 2010-01-21 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
WO2010007552A1 (en) 2008-07-15 2010-01-21 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
WO2010025202A1 (en) 2008-08-29 2010-03-04 Amgen Inc. PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF
ES2387474T3 (es) 2008-08-29 2012-09-24 Amgen, Inc Compuestos de piridazino-piridinona para el tratamiento de enfermedades mediadas por proteína cinasa
WO2010038428A1 (ja) 2008-09-30 2010-04-08 武田薬品工業株式会社 タキサン系抗がん剤の置き換え薬
EP2206534A1 (de) 2008-10-09 2010-07-14 c-a-i-r biosciences GmbH Dibenzocycloheptanonderivate und pharmazeutische Mittel, welche diese Verbindungen enthalten
US8772481B2 (en) 2008-10-10 2014-07-08 Amgen Inc. Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
US8497269B2 (en) 2008-10-10 2013-07-30 Amgen Inc. Phthalazine compounds as p38 map kinase modulators and methods of use thereof
US20110263647A1 (en) 2009-01-15 2011-10-27 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
EP2393492A1 (en) 2009-02-09 2011-12-14 Boehringer Ingelheim International GmbH New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
JP2012518003A (ja) 2009-02-13 2012-08-09 バーテックス ファーマシューティカルズ インコーポレイテッド ２−（２，４−ジフルオロフェニル）−６−（１−（２，６−ジフルオロフェニル）ウレイド）ニコチンアミドの固体形態
EP2396302A2 (en) 2009-02-13 2011-12-21 Vertex Pharmceuticals Incorporated Processes for producing phenyl-6-(1-(phenyl)ureido)nicotinamides)
GB0902648D0 (en) 2009-02-17 2009-04-01 Argenta Discovery Ltd Pharmaceutical compounds and compositions
PE20120655A1 (es) 2009-02-17 2012-06-07 Chiesi Farma Spa Derivados de triazolopiridina como inhibidores de proteinas cinasas activadas por mitogeno p38 (map)
WO2010120963A1 (en) 2009-04-16 2010-10-21 Bristol-Myers Squibb Company Tablet formulation for p38 inhibitor and method
CN102574838B (zh) 2009-05-05 2014-07-02 默沙东公司 作为p38激酶抑制剂的吡咯并[2,3-c]吡啶衍生物
EP2470534A4 (en) 2009-08-24 2013-02-27 Merck Sharp & Dohme INHIBITION OF JAK BLOCKES TOXICITIES ASSOCIATED WITH INTERFERENCE RNA
CN104043126A (zh) 2009-10-22 2014-09-17 霍夫曼-拉罗奇有限公司 轴突变性的调节
US20110117055A1 (en) 2009-11-19 2011-05-19 Macdonald James E Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds
WO2011083387A1 (en) 2010-01-07 2011-07-14 Pfizer Limited Hydrochloride salt of biphenyl-2-yl-carbamic acid 1-{9-[(3-fluoro-4-hydroxy-benzoyl)-methyl-amino]-nonyl}-piperidin-4-yl ester
EA022360B1 (ru) 2010-03-24 2015-12-30 Онконова Терапьютикс, Инк. Композиции и способы для профилактики и лечения ран
US9060967B2 (en) 2010-03-26 2015-06-23 Onconova Therapeutics, Inc Stable aqueous formulation of (E)-4-carboxystyryl-4-chlorobenzyl sulfone
GB201009731D0 (en) 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
SG186855A1 (en) 2010-06-28 2013-02-28 Merck Patent Gmbh 2,4- diaryl - substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
JP5886842B2 (ja) 2010-07-05 2016-03-16 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ キナーゼ誘発疾患の処置に有用なビピリジル誘導体
WO2012031057A1 (en) 2010-09-01 2012-03-08 Bristol-Myers Squibb Company Bms- 582949 for the treatment of resistant rheumatic disease
RU2013129860A (ru) 2010-11-29 2015-01-10 Дженентек, Инк. Способы выявления нейродегенеративных заболеваний или нарушений
AR083868A1 (es) 2010-12-03 2013-03-27 Lilly Co Eli Compuestos de oxazol[5,4-b]piridin-5-ilo
AU2012224979B2 (en) 2011-03-09 2017-01-19 Merck Patent Gmbh Pyrido [2, 3 - b] pyrazine derivatives and their therapeutical uses
DK3081568T3 (da) 2011-05-09 2020-02-24 Eip Pharma Llc Sammensætninger og fremgangsmåder til behandling af alzheimers sygdom
CN103562198B (zh) 2011-06-10 2016-08-24 奇斯药制品公司 具有毒蕈碱受体拮抗剂和β2肾上腺素能受体激动剂活性的化合物
EP2729146B1 (en) 2011-07-08 2017-03-08 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
SG11201401795XA (en) 2011-11-11 2014-09-26 Lilly Co Eli Combination therapy for ovarian cancer
WO2013086002A1 (en) 2011-12-05 2013-06-13 Cellworks Research India Private Limited Compositions, process of preparation of said compositions and method of treating cancer
WO2013083606A1 (en) 2011-12-09 2013-06-13 Chiesi Farmaceutici S.P.A. Kinase inhibitors
ES2612259T3 (es) 2011-12-09 2017-05-16 Chiesi Farmaceutici S.P.A. Inhibidores de cinasa
US9458154B2 (en) 2011-12-09 2016-10-04 Chiesi Farmaceutici S.P.A. Kinase inhibitors
CN117736134A (zh) 2012-01-12 2024-03-22 耶鲁大学 通过e3泛素连接酶增强靶蛋白质及其他多肽降解的化合物和方法
UA113302C2 (xx) 2012-03-01 2017-01-10 Кристалічний поліморф 1-(3-трет-бутил-1-п-толіл-1h-піразол-5-іл)-3-(5-фтор-2-(1-(2-гідроксіетил)-1н-індазол-5-ілокси)бензил)сечовини гідрохлориду
ES2605942T3 (es) 2012-03-20 2017-03-17 Mereo Biopharma 1 Limited Uso de un derivado de pirazol en el tratamiento de exacerbaciones agudas de enfermedad pulmonar obstructiva crónica
JP6267193B2 (ja) 2012-05-22 2018-01-24 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 置換ジピリジルアミン類及びそれらの使用
EP2858630A4 (en) * 2012-06-07 2016-02-24 Harvard College NANOTHERAPEUTIC PRODUCTS FOR DRUG TARGETING
CA2879222A1 (en) * 2012-07-17 2014-01-23 Glaxosmithkline Llc Nicotinamide derivate in the treatment of acute coronary syndrome
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
US20150225373A1 (en) 2012-08-29 2015-08-13 Respivert Limited Kinase inhibitors
US9783556B2 (en) 2012-08-29 2017-10-10 Respivert Limited Kinase inhibitors
EP2890460B1 (en) 2012-08-29 2017-02-22 Respivert Limited Kinase inhibitors
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
US9155747B2 (en) 2012-09-13 2015-10-13 Chiesi Farmaceutici S.P.A. Isoxazolidine derivatives
US9732063B2 (en) 2012-11-16 2017-08-15 Respivert Limited Kinase inhibitors
JP6042995B2 (ja) 2012-11-30 2016-12-14 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ブルトン型チロシンキナーゼの阻害薬
US9370527B2 (en) 2012-12-28 2016-06-21 The Regents Of The University Of Michigan Amelioration of intestinal fibrosis and treatment of Crohn's disease
EP2961744B1 (en) 2013-02-27 2017-06-28 Array Biopharma, Inc. Intermediates for use in the preparation of indazole derivatives and processes for the preparation thereof
EP2970190A1 (en) 2013-03-14 2016-01-20 Respivert Limited Kinase inhibitors
GB201305714D0 (en) 2013-03-28 2013-05-15 Ucl Business Plc Method
CA2907566C (en) * 2013-04-01 2023-08-22 Pulmatrix, Inc. Tiotropium dry powders
TWI641592B (zh) 2013-04-02 2018-11-21 英商瑞斯比維特有限公司 激酶抑制劑
WO2014181213A1 (en) 2013-05-10 2014-11-13 Pfizer Inc. Crystalline form of (sa)-(-)-3-(3-bromo-4-((2,4-difluorobenzyl)oxy)-6-methyl-2-oxopyridin-1 (2h)-yl)-n,4-dimethylbenzamide
US9359354B2 (en) 2013-06-06 2016-06-07 Chiesi Farmaceutici S.P.A. Kinase inhibitors
KR20160016973A (ko) 2013-06-06 2016-02-15 키에시 파르마슈티시 엣스. 피. 에이. P38 - map 키나아제 억제제로서 [1, 2, 4] 트리아졸로 [4, 3 - a] 피리딘의 유도체
RU2015151886A (ru) 2013-06-06 2017-06-08 КЬЕЗИ ФАРМАЧЕУТИЧИ С.п.А. Ингибиторы киназ
US9707219B2 (en) 2013-07-10 2017-07-18 Glaxosmithkline Intellectual Property (No.2) Limited Losmapimod for use in treating glomerular disease
US9918989B2 (en) 2013-07-12 2018-03-20 The Regents Of The University Of California Combination therapies for malaria
US9814728B2 (en) * 2013-09-20 2017-11-14 Saint Louis University Inhibition of DUX4 expression using bromodomain and extra-terminal domain protein inhibitors (BETi)
EP3069732B1 (en) * 2013-11-14 2023-07-12 The Doshisha Drug for treating corneal endothelium by promoting cell proliferation or inhibiting cell damage
AU2014369449B2 (en) 2013-12-20 2018-07-05 Oxular Acquisitions Limited Urea derivatives useful as kinase inhibitors
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.
KR102413704B1 (ko) 2014-02-14 2022-06-24 레스피버트 리미티드 항염증성 화합물로서의 방향족 헤테로사이클릭 화합물
AU2015220873A1 (en) 2014-02-19 2016-08-11 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as BACE1 inhibitors for treatment of Alzheimer's disease
US20230190750A1 (en) 2014-06-13 2023-06-22 Genentech, Inc. Methods of treating and preventing cancer drug resistance
WO2015191996A1 (en) 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
CN114010641A (zh) 2014-07-09 2022-02-08 爱普制药有限责任公司 用于治疗神经病症的方法
MA40774A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivés de diaryle-urée en tant qu'inhibiteurs de kinase p38
EP3201189A1 (en) 2014-10-01 2017-08-09 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors
WO2016049677A1 (en) 2014-10-03 2016-04-07 The Walter And Eliza Hall Institute Of Medical Research Method of treating cancer
WO2016066687A1 (en) * 2014-10-30 2016-05-06 Glaxosmithkline Intellectual Property (No.2) Limited Losmapimod for treating copd
WO2016114655A1 (en) * 2015-01-12 2016-07-21 Ry Pharma B.V. Treating neuromuscular or neurologic disease through reducing gabaergic and/or glycinergic inhibitory neurotransmitter overstimulation
US10538763B2 (en) * 2015-01-16 2020-01-21 Ionis Pharmaceuticals, Inc. Compounds and methods for modulation of DUX4
EP3253874B1 (en) * 2015-02-06 2022-03-23 Association Institut de Myologie Treatment of facioscapulohumeral dystrophy
TWI703138B (zh) 2015-02-12 2020-09-01 義大利商吉斯藥品公司 具有蕈毒鹼受體拮抗劑及β２腎上腺素受體促效劑活性之化合物
JP6701225B2 (ja) 2015-03-09 2020-05-27 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 三環式ｄｌｋ阻害剤及びその使用
WO2016154329A2 (en) * 2015-03-24 2016-09-29 The Trustees Of The University Of Pennsylvania P38 map kinase inhibitors for treating friedreich's ataxia
JP2016193870A (ja) 2015-04-01 2016-11-17 国立大学法人広島大学 慢性骨髄性白血病治療剤
US9968604B2 (en) 2015-04-16 2018-05-15 Chiesi Farmaceutici S.P.A. Chromene derivatives as phoshoinositide 3-kinases inhibitors
CN107921106B (zh) * 2015-05-20 2023-09-08 住友制药株式会社 Wt1抗原肽和免疫调节剂的组合用途
KR20180014778A (ko) * 2015-06-03 2018-02-09 트리아스텍 인코포레이티드 제형 및 이의 용도
WO2016198698A2 (en) 2015-06-12 2016-12-15 Cnic Fundación Centro Nacional De Investigaciones Cardiovasculares Carlos Iii P38 inhibitors for the treatment and prophylaxis of liver cancer
CN108137586B (zh) 2015-09-14 2021-04-13 辉瑞大药厂 作为LRRK2抑制剂的新颖咪唑并[4,5-c]喹啉和咪唑并[4,5-c][1,5]萘啶衍生物
WO2017075013A1 (en) 2015-10-26 2017-05-04 Eip Pharma, Llc Methods and compositions for recovery from stroke
US9427439B1 (en) 2015-10-26 2016-08-30 Eip Pharma, Llc Methods and compositions for recovery from stroke
EP3383867B1 (en) 2015-12-03 2021-04-14 Chiesi Farmaceutici S.p.A. Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
EP3394058B1 (en) 2015-12-23 2020-10-14 Chiesi Farmaceutici S.p.A. N-[3-(3-{4-[[1,2,4]triazolo[4,3-a]pyridin-6-yloxy]-1,2,3,4-tetrahydro-naphthalen-1-yl} -ureido)-phenyl]-methanesulfonamide derivatives and their use as p38 mapk inhibitors
WO2017110093A1 (ja) 2015-12-24 2017-06-29 学校法人同志社 ＴＧＦ－βシグナルに起因する障害を治療または予防するための医薬およびその応用
US20190125735A1 (en) 2015-12-29 2019-05-02 Board Of Regents, The University Of Texas System Inhibition of p38 mapk for the treatment of cancer
AU2017213796A1 (en) * 2016-02-01 2018-09-20 President And Fellows Of Harvard College Small molecules for mouse satellite cell proliferation
WO2017134053A1 (en) 2016-02-04 2017-08-10 Chiesi Farmaceutici S.P.A. Pyrazole derivatives as phosphoinositide 3-kinases inhibitors
PE20190376A1 (es) 2016-06-08 2019-03-08 Support Venture Gmbh Combinaciones farmaceuticas para el tratamiento del cancer
GB201611712D0 (en) 2016-07-02 2016-08-17 Hvivo Services Ltd Methods and compounds for the treatment or prevention of severe or persistent influenza
US11123349B2 (en) 2017-02-15 2021-09-21 The University Of Melbourne Method of treatment
WO2019071147A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. INHIBITORS OF KINASE P38 REDUCING EXPRESSION OF DUX4 GENE AND DOWNSTREAM GENES FOR THE TREATMENT OF FSHD
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD
US20200297696A1 (en) 2017-11-21 2020-09-24 Saint Louis University P38 inhibitors for the treatment of fshd
US20220017908A1 (en) 2018-11-20 2022-01-20 Fulcrum Therapeutics, Inc. Compositions and methods for increasing fetal hemoglobin and treating sickle cell disease
US20220079951A1 (en) * 2018-12-20 2022-03-17 Saint Louis University Bet inhibitors for modulating dux4 expression in fshd
CN114144230B (zh) 2019-03-15 2024-04-23 弗尔康医疗公司 作为eed和prc2调节剂的大环唑并吡啶衍生物
WO2022056266A2 (en) * 2020-09-11 2022-03-17 Arrowhead Pharmaceuticals, Inc. Rnai agents for inhibiting expression of dux4, compositions thereof, and methods of use

Also Published As

Publication number Publication date
RS63581B1 (sr) 2022-10-31
EP4159212A1 (en) 2023-04-05
NZ765534A (en) 2021-04-30
BR112020006169A2 (pt) 2020-10-20
CA3127373A1 (en) 2019-04-11
CA3128468A1 (en) 2019-04-11
AU2018346712A1 (en) 2020-04-09
EP3691620A1 (en) 2020-08-12
IL273657A (en) 2020-05-31
CA3077499A1 (en) 2019-04-11
EP3691620B1 (en) 2022-07-27
CN114748622A (zh) 2022-07-15
US11479770B2 (en) 2022-10-25
JP2024012295A (ja) 2024-01-30
TW201924676A (zh) 2019-07-01
SG10202110259QA (en) 2021-10-28
HRP20221196T1 (hr) 2022-12-09
CN111601593B (zh) 2022-04-15
PT3691620T (pt) 2022-10-06
CL2020000913A1 (es) 2020-09-25
JP2023113691A (ja) 2023-08-16
KR20200066655A (ko) 2020-06-10
JP7012152B2 (ja) 2022-02-10
IL273589B (en) 2020-11-30
US20200383963A1 (en) 2020-12-10
CA3077499C (en) 2021-09-21
ES2927715T3 (es) 2022-11-10
HUE060024T2 (hu) 2023-01-28
CO2020005351A2 (es) 2020-05-15
AU2018346712B2 (en) 2021-04-01
PH12020550195A1 (en) 2020-12-07
ECSP20024210A (es) 2020-07-31
PL3691620T3 (pl) 2022-11-21
PH12020550215A1 (en) 2021-02-15
TWI793191B (zh) 2023-02-21
CL2020000911A1 (es) 2021-02-19
NZ762856A (en) 2020-07-31
JP2020536884A (ja) 2020-12-17
IL273589A (en) 2020-05-31
UY37918A (es) 2019-04-30
US11291659B2 (en) 2022-04-05
US20230257743A1 (en) 2023-08-17
JP2021501130A (ja) 2021-01-14
CA3078232A1 (en) 2019-04-11
CN114748622B (zh) 2024-09-24
JP2022031915A (ja) 2022-02-22
US20220133704A1 (en) 2022-05-05
CN114732910B (zh) 2024-08-23
MX2020003961A (es) 2020-09-22
SG11202003035SA (en) 2020-04-29
DK3691620T3 (da) 2022-10-03
CN114732910A (zh) 2022-07-12
CN111868237A (zh) 2020-10-30
WO2019071147A1 (en) 2019-04-11
US20200332291A1 (en) 2020-10-22
ZA202002315B (en) 2021-07-28
US20220282254A1 (en) 2022-09-08
CL2020001719A1 (es) 2020-09-11
KR20200067170A (ko) 2020-06-11
EP3692144A1 (en) 2020-08-12
WO2019071144A1 (en) 2019-04-11
AU2018346709A1 (en) 2020-04-16
BR112020006677A2 (pt) 2020-10-06
LT3691620T (lt) 2022-09-26
CN111601593A (zh) 2020-08-28
CO2020005417A2 (es) 2020-07-31

Similar Documents

Publication Publication Date Title
MX2020003594A (es) Inhibidores de la quinasa p38 que reducen la expresión de dux4 y de los genes corriente abajo para el tratamiento de fshd.
CY1123561T1 (el) Ενωσεις χρησιμες ως αναστολεις κινασης
CO2019006622A2 (es) Derivados de pirazol como inhibidores de malt1
CY1121360T1 (el) Αναστολεις dna-pk
CY1120361T1 (el) Αναστολεις 2,3-διοξυγενασης ινδολαμινης (ido)
CO2018012946A2 (es) Moduladores de la vía de estrés integrada
ECSP19044183A (es) (aza)indol-, benzotiofen, y benzofuran-3-sulfonamidas
CL2018001899A1 (es) Salicilamidas de espiroheptanos y compuestos relacionados como inhibidores de cinasa rho (rock)
MX2023009561A (es) Moduladores de profarmacos de la via de estres integrada.
CL2018000198A1 (es) Composiciones de arni de transtiretina (ttr) y métodos para su uso para el tratamiento o prevencion de enfermedades asociadas con ttr
MX2020004537A (es) Moduladores de la vía integrada del estrés.
EA202091731A1 (ru) Ингибиторы аутотаксина и их применения
EA201992147A1 (ru) Ингибиторы тирозинкиназы брутона
CL2017000006A1 (es) Derivados de quinolizinona como inhibidores de pi3k
CL2021000292A1 (es) Benzimidazoles sustituidos como inhibidores de pad4.
PH12020551543A1 (en) Therapeutic modulators of the reverse mode of atp synthase
BR112017024633A2 (pt) novo amidoeteroaril aroil hidrazida etino
WO2018211324A8 (en) Prodrugs for the treatment of disease
CO2020003134A2 (es) Moduladores de la expresión de enac
GEP20227437B (en) 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
EA202090859A1 (ru) Ингибиторы киназы p38 снижают экспрессию dux4 и последующих генов для лечения fshd
EA202190844A1 (ru) Способы лечения миелопролиферативных расстройств
MX2024010153A (es) Moduladores terapeuticos del modo inverso de la atp sintasa.
PH12017501063A1 (en) Compounds for the treatment of cancer
AR100891A1 (es) Composición que comprende un inhibidor de jak-2 y un inhibidor de btk