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
    • 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

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
US201762568673P 2017-10-05 2017-10-05
US201762568754P 2017-10-05 2017-10-05
US201862682565P 2018-06-08 2018-06-08
US201862682563P 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
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.
MX2020003961A MX2020003961A (es) 2017-10-05 2018-10-05 Uso de inhibidores de p38 para reducir la expresion de dux4.

Family Applications After (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) EP4159212A1 (es)
JP (5) JP2021501130A (es)
KR (2) KR20200066655A (es)
CN (4) CN114732910A (es)
AU (2) AU2018346712B2 (es)
BR (2) BR112020006677A2 (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) MX2020003594A (es)
NZ (1) NZ762856A (es)
PH (2) PH12020550195A1 (es)
PL (1) PL3691620T3 (es)
PT (1) PT3691620T (es)
RS (1) RS63581B1 (es)
SG (2) SG11202003035SA (es)
TW (1) TWI793191B (es)
UY (1) UY37918A (es)
WO (2) WO2019071144A1 (es)
ZA (1) ZA202002315B (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3128468A1 (en) * 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
EP3746082A4 (en) * 2018-02-02 2021-12-08 Fred Hutchinson Cancer Research Center METHOD OF TREATMENT OF FACIOUS CAPULOHUMERAL 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
EP4065110A1 (en) * 2019-11-29 2022-10-05 Facio Intellectual Property B.V. Novel compounds for treatment of diseases related to dux4 expression
WO2021105474A1 (en) 2019-11-29 2021-06-03 Facio Intellectual Property B.V. New 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
UY39417A (es) 2020-09-11 2022-03-31 Arrowhead Pharmaceuticals Inc Agentes de arni para inhibir la expresión de dux4, composiciones de dichos agentes, y métodos de uso
WO2023009672A1 (en) * 2021-07-27 2023-02-02 Fulcrum Therapeutics, Inc. Treatment of facioscapulohumeral muscular dystrophy with losmapimod

Family Cites Families (448)

* 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
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5658903A (en) 1995-06-07 1997-08-19 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US6369068B1 (en) 1995-06-07 2002-04-09 Smithkline Beecham Corporation Amino substituted pyrimidine containing compounds
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
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
EP1005343A1 (en) 1996-03-08 2000-06-07 Smithkline Beecham Corporation Use of csaid?tm compounds as inhibitors of angiogenesis
US6218136B1 (en) 1996-03-12 2001-04-17 Smithkline Beecham Corporation Methods of the identification of pharmaceutically active compounds
US6096748A (en) 1996-03-13 2000-08-01 Smithkline Beecham Corporation Pyrimidine compounds useful in treating cytokine mediated diseases
WO1997035855A1 (en) 1996-03-25 1997-10-02 Smithkline Beecham Corporation Novel 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
DE69816109T2 (de) 1997-04-24 2004-04-22 Ortho-Mcneil Pharmaceutical, Inc. Substituierte imidazole zur behandlung von entzündlichen krankheiten
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
EP1023066A4 (en) 1997-06-13 2001-05-23 Smithkline Beecham Corp NEW PYRAZOLE AND PYRAZOLINE SUBSTITUTED COMPOUND
CA2294137A1 (en) 1997-06-19 1998-12-23 Smithkline Beecham Corporation Novel aryloxy substituted pyrimidine imidazole compounds
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
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
GB9721437D0 (en) 1997-10-10 1997-12-10 Glaxo Group Ltd Heteroaromatic compounds and their use in medicine
JP3579350B2 (ja) 1997-10-20 2004-10-20 エフ．ホフマン−ラ ロシュ アーゲー 二環式キナーゼ阻害剤
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
JP3590586B2 (ja) 1998-05-05 2004-11-17 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ピラゾール誘導体
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
PL344330A1 (en) 1998-05-22 2001-10-22 Smithkline Beecham Corp Novel 2-alkyl substituted imidazole compounds
KR100605140B1 (ko) 1998-05-22 2006-07-28 싸이오스 인크 심장병 및 다른 질병을 치료하기 위한 헤테로 고리 화합물및 그 치료 방법
US6340685B1 (en) 1998-05-22 2002-01-22 Scios, Inc. 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
US6867209B1 (en) 1998-05-22 2005-03-15 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
US6589954B1 (en) 1998-05-22 2003-07-08 Scios, Inc. Compounds and methods to treat cardiac failure and other disorders
WO1999064400A1 (en) 1998-06-12 1999-12-16 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
WO2000010563A1 (en) 1998-08-20 2000-03-02 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
EP1114039A1 (en) 1998-09-18 2001-07-11 Vertex Pharmaceuticals Incorporated INHIBITORS OF p38
EP1119254A4 (en) 1998-10-07 2004-05-12 Smithkline Beecham Corp STROKE TREATMENT
WO2000025791A1 (en) 1998-11-04 2000-05-11 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
DE60033028T2 (de) 1999-04-23 2007-11-15 Takeda Pharmaceutical Co. Ltd. 5-pyridyl-1,3-azol-derivate, verfahren zu ihrer herstellung und ihre verwendung
ATE376547T1 (de) 1999-05-21 2007-11-15 Scios Inc Derivate des indol-typs als p38 kinase inhibitoren
MXPA02000314A (es) 1999-07-09 2004-06-22 Boehringer Ingelheim Pharma Proceso novedoso para la sintesis de compuestos de urea substituidos con heteroarilo.
US6541477B2 (en) 1999-08-27 2003-04-01 Scios, Inc. Inhibitors of p38-a kinase
HUP0204333A3 (en) 1999-09-17 2004-07-28 Smithkline Beecham Corp Use of csaids in rhinovirus infection
ES2277858T3 (es) 1999-10-21 2007-08-01 F. Hoffmann-La Roche Ag Heterociclos de nitrogeno biciclicos alquilamino sustituidos como inhibidores de proteina kinasa p38.
CZ20021744A3 (cs) 1999-10-21 2002-08-14 F. Hoffmann-La Roche Ag Bicyklické dusíkové heterocykly substituované heteroalkylaminoskupinou jako inhibitory P38 proteinkinázy
EP1248624A4 (en) 1999-11-23 2003-01-22 Smithkline Beecham Corp 3,4-DIHYDRO- (1H) -CHIRAZOLINE-2-ONES AND THE USE THEREOF AS CSBP / P38 KINASE INHIBITORS
ATE296809T1 (de) 1999-11-23 2005-06-15 Smithkline Beecham Corp 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
US7053099B1 (en) 1999-11-23 2006-05-30 Smithkline Beecham Corporation 3,4-dihydro-(1H)quinazolin-2-one compounds as CSBP/p38 kinase inhibitors
AU1782301A (en) 1999-11-23 2001-06-04 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p39 kinase inhibitors
EP1242385B1 (en) 1999-12-28 2009-11-25 Pharmacopeia, Inc. Cytokine, especially tnf-alpha, 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
MY141144A (en) 2000-03-02 2010-03-15 Smithkline Beecham Corp 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
MXPA02012909A (es) 2000-07-24 2004-05-05 Boehringer Ingelheim Pharma Formulaciones mejoradas de dosis oral de 1-(5-ter-butil -2-p-tiolil2h -pirazol-3 -il)-3-(4-2 (2-morfolin-4-il -etoxi) -naftalen -1-il) -urea.
PE20020506A1 (es) 2000-08-22 2002-07-09 Glaxo Group Ltd Derivados de pirazol fusionados como inhibidores de la proteina cinasa
EP1315727B1 (en) 2000-08-31 2005-06-29 F. Hoffmann-La Roche Ag 7-oxo pyridopyrimidines
BR0113628A (pt) 2000-08-31 2003-07-01 Hoffmann La Roche 7-oxo-piridopirimidinas como inibidores de uma proliferação celular
JP2004530648A (ja) 2000-10-19 2004-10-07 スミスクライン・ビーチャム・コーポレイション 炎症により促進される咳の治療のためのｐ３８阻害剤の使用
WO2002032862A2 (en) 2000-10-19 2002-04-25 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of smoke inhalation
ATE521353T1 (de) 2000-10-23 2011-09-15 Glaxosmithkline Llc Neues trisubstitutiertes 8h-pyridoä2,3- düpyrimidin-7-onderivat zur behandlung von durch csbp/p38kinase vermittelten krankheiten
AU2002232760B2 (en) 2000-11-17 2006-12-14 Bristol-Myers Squibb Company Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors
EP1339708A2 (en) 2000-11-20 2003-09-03 Scios Inc. Indole-type inhibitors of p38 kinase
WO2002046158A2 (en) 2000-11-20 2002-06-13 Scios Inc. Piperidine/piperazine-type inhibitors of p38 kinase
WO2002042292A2 (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
CA2431904A1 (en) 2000-12-20 2002-08-01 Merck & Co., Inc. (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents
ATE305303T1 (de) 2001-02-12 2005-10-15 Hoffmann La Roche 6-substituierte pyridopyrimidine
IL157541A0 (en) 2001-02-28 2004-03-28 Univ Temple METHOD FOR PROTECTING CELLS AND TISSUES FORM IONIZING RADIATION TOXICITY WITH alpha, beta UNSATURATED ARYL SULFONES
OA12552A (en) 2001-03-09 2006-06-06 Pfizer Prod Inc Triazolopyridines as anti-inflammatory agents.
CA2440211A1 (en) 2001-03-09 2002-09-19 Pfizer Products Inc. Benzimidazole anti-inflammatory compounds
WO2002076463A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
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
WO2002076984A1 (en) 2001-03-23 2002-10-03 Smithkline Beecham Corporation Compounds useful as kinase inhibitors for the treatment of hyperproliferative diseases
WO2002076396A2 (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
WO2002085405A2 (en) 2001-04-24 2002-10-31 Merck Patent Gmbh COMBINATION THERAPY USING ANTI-ANGIOGENIC AGENTS AND TNF$g(a)
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
PT1397364E (pt) 2001-05-24 2007-10-22 Lilly Co Eli Novos derivados de pirrole como agentes farmacêuticos
EP2036891A3 (en) 2001-06-11 2009-03-25 Vertex Pharmaceuticals Incorporated Isoquinoline inhibitors of P38
CA2450555A1 (en) 2001-06-25 2003-01-03 Merck & Co., Inc. (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds
WO2003002544A1 (en) 2001-06-26 2003-01-09 Bristol-Myers Squibb Company N-heterocyclic inhibitors of tnf-alpha expression
CA2453147A1 (en) 2001-07-11 2003-01-23 Boehringer Ingelheim Pharmaceuticals, Inc. Methods of treating cytokine mediated diseases
WO2003015828A1 (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
CN1281603C (zh) 2001-08-30 2006-10-25 霍夫曼-拉罗奇有限公司 作为抗炎药的氨基吡咯化合物
CA2459943A1 (en) 2001-09-21 2003-04-03 Merck & Co., Inc. 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
AU2002329570A1 (en) 2001-10-12 2003-01-30 Pfizer Products Inc. Method of monitoring neuroprotective treatment
GB0124932D0 (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
GB0124928D0 (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
GB0124936D0 (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
GB0124933D0 (en) 2001-10-17 2001-12-05 Glaxo Group Ltd Chemical compounds
WO2003039534A1 (en) 2001-11-08 2003-05-15 Merck & Co., Inc. Compositions and methods for treating osteoporosis
IL161667A0 (en) 2001-11-09 2004-09-27 Scios Inc Method and composition to treat cystic fibrosis
WO2003048340A2 (en) 2001-12-05 2003-06-12 Vertex Pharmaceuticals Incorporated Crystal structure of mitogen-activated protein kinase-activated protein kinase 2 and binding pockets thereof
WO2003049742A1 (en) 2001-12-11 2003-06-19 Boehringer Ingelheim Pharmaceuticals, Inc. Method for administering birb 796 bs
CA2471948A1 (en) 2002-01-03 2003-07-17 Smithkline Beecham Corporation Novel pharmaceutical dosage forms and method for producing same
CA2472475C (en) 2002-01-15 2010-05-18 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
DE10203741A1 (de) 2002-01-31 2003-08-14 Boehringer Ingelheim Pharma Neue Fluorencarbonsäureester, 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
WO2003068223A1 (en) 2002-02-11 2003-08-21 Bayer Corporation Aryl ureas with raf kinase and angiogenesis inhibiting activity
PT1864975E (pt) 2002-02-12 2010-12-27 Glaxosmithkline Llc Derivados de nicotinamida úteis como inibidores de p38
ES2314224T3 (es) 2002-03-07 2009-03-16 F. Hoffmann-La Roche Ag Inhibidores pirimidina y piridina biciclicos de p38 quinasa.
CN1652786A (zh) 2002-03-13 2005-08-10 麦克公司 作为雄激素受体调节剂的氟代4－氮杂甾体衍生物
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
BR0308937A (pt) 2002-04-03 2005-01-04 Hoffmann La Roche Compostos imidazo fundidos
IL163737A0 (en) 2002-04-05 2005-12-18 Boehringer Ingelheim Pharma Method of treating mucus hypersecretion
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
AU2003229689A1 (en) 2002-04-15 2003-10-27 Glaxo Group Limited A method of identifying a modudator for a serine/theronine kinase
DE60315826T2 (de) 2002-04-19 2008-05-21 Smithkline Beecham Corp. Neue verbindungen
CA2483164C (en) 2002-04-23 2011-06-07 Bristol-Myers Squibb Company Pyrrolo-triazine aniline compounds useful as kinase inhibitors
ES2318122T3 (es) 2002-04-23 2009-05-01 Bristol-Myers Squibb Company Compuestos de aril cetona pirrolo-triazina utiles como inhibidores de quinasa.
US7388009B2 (en) 2002-04-23 2008-06-17 Bristol-Myers Squibb Company Heteroaryl-substituted pyrrolo-triazine compounds useful as kinase inhibitors
GB0209891D0 (en) 2002-04-30 2002-06-05 Glaxo Group Ltd Novel compounds
JP4516839B2 (ja) 2002-04-30 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション アンドロゲン受容体修飾因子としての４−アザステロイド誘導体
WO2003097615A1 (en) 2002-05-17 2003-11-27 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-β INHIBITORS
TW200400034A (en) 2002-05-20 2004-01-01 Bristol Myers Squibb Co Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors
WO2003099206A2 (en) 2002-05-21 2003-12-04 Bristol-Myers Squibb Company Indole compounds useful as impdh inhibitors
AU2003238915B2 (en) 2002-06-11 2008-02-21 Merck & Co., Inc. (halo-benzo carbonyl)heterobicyclic p38 kinase inhibiting agents
ATE349210T1 (de) 2002-07-09 2007-01-15 Boehringer Ingelheim Pharma Pharazeutische zusammensetzungen aus anticholinergica und p38 kinase hemmern zur behandlung von erkrankungen der atemwege
CA2494367A1 (en) 2002-07-25 2004-02-05 Scios Inc. Methods for improvement of lung function using tgf-.beta. inhibitors
GB0217757D0 (en) 2002-07-31 2002-09-11 Glaxo Group Ltd Novel compounds
CN100432073C (zh) 2002-08-06 2008-11-12 霍夫曼-拉罗奇有限公司 作为p-38map激酶抑制剂的6-烷氧基-吡啶并-嘧啶
EP1549621A1 (en) 2002-08-08 2005-07-06 Boehringer Ingelheim Pharmaceuticals Inc. Fluorinated phenyl-naphthalenyl-urea compounds as inhibitors of cytokines involved in inflammatory processes
ES2274302T3 (es) 2002-08-09 2007-05-16 Eli Lilly And Company Benzimidazoles y benzotiazoles como inhibidores de la map quinasa.
US20040110755A1 (en) 2002-08-13 2004-06-10 Boehringer Ingelheim Pharmaceuticals, Inc. Combination therapy with p38 MAP kinase inhibitors and their pharmaceutical compositions
JP2006500365A (ja) 2002-08-14 2006-01-05 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド ｐ３８ＭＡＰキナーゼインヒビターを用いた抗凝固及び線維素溶解療法
WO2004019873A2 (en) 2002-08-29 2004-03-11 Scios Inc. Methods of promoting osteogenesis
US7037923B2 (en) 2002-08-30 2006-05-02 Pfizer, Inc. Alkyl-[4-(trifluorophenyl)-oxazol-5-yl]-triazolo-pyridines
PA8579601A1 (es) 2002-08-30 2004-05-07 Pfizer Prod Inc Compuestos antiinflamatorios de di y trifloruro-triazolo-piridinas
US7012143B2 (en) 2002-08-30 2006-03-14 Dombroski Mark A Cycloalkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
US7005523B2 (en) 2002-08-30 2006-02-28 Pfizer Inc. Cycloalkyl-[4-(trifluorophenyl)-oxazol-5yl]-triazolo-pyridines
BR0313961A (pt) 2002-08-30 2005-07-19 Pfizer Prod Inc Processos e intermediários para preparar triazolo-piridinas
US20040092547A1 (en) 2002-08-30 2004-05-13 Pfizer Inc Alkyl-[4-(difluorophenyl)-oxazol-5-yl]-triazolo-pyridines
US7220763B2 (en) 2002-09-03 2007-05-22 Scios, Inc. Indole-type derivatives as inhibitors of p38 kinase
CA2497951A1 (en) 2002-09-05 2004-03-18 Scios Inc. Treatment of pain by inhibition of p38 map kinase
WO2004021979A2 (en) 2002-09-06 2004-03-18 Smithkline Beecham Corporation PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS
US7115644B2 (en) 2002-09-13 2006-10-03 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds
AU2003268156A1 (en) 2002-09-17 2004-04-08 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
AU2003282920A1 (en) 2002-10-04 2004-05-04 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
WO2004032874A2 (en) 2002-10-09 2004-04-22 Scios Inc. AZAINDOLE DERIVATIVES AS INHIBITORS OF p38 KINASE
WO2004041277A1 (en) 2002-11-01 2004-05-21 Merck & Co., Inc. Carbonylamino-benzimidazole derivatives as androgen receptor modulators
RU2340618C2 (ru) 2002-11-18 2008-12-10 Ф.Хоффманн-Ля Рош Аг Диазинопиримидины и фармацевтическая композиция, содержащая их
DE10255040A1 (de) 2002-11-26 2004-06-03 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue Carbaminsäureester mit anticholinerger Wirksamkeit
WO2004053107A2 (en) 2002-12-06 2004-06-24 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
WO2004072030A2 (en) 2003-02-05 2004-08-26 Bristol-Myers Squibb Company Process for preparing pyrrolotriazine kinase inhibitors
CA2755297A1 (en) 2003-02-10 2004-08-26 Vertex Pharmaceuticals Incorporated Processes for the preparation of n-heteroaryl-n-aryl-amines by reacting an n-aryl carbamic acid ester with a halo-heteroaryl and analogous processes
US7205322B2 (en) 2003-02-12 2007-04-17 Bristol-Myers Squibb Company Thiazolidine compounds as calcium sensing receptor modulators
WO2004072072A1 (en) 2003-02-14 2004-08-26 Pfizer Products Inc. Triazolo-pyridines as anti-inflammatory compounds
WO2004073628A2 (en) 2003-02-14 2004-09-02 Smithkline Beecham Corporation Novel compounds
KR101312736B1 (ko) 2003-02-27 2013-09-27 팔라우 파르마 에스에이 피라졸로피리딘 유도체
CA2517517C (en) 2003-03-03 2012-12-18 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
US7135575B2 (en) 2003-03-03 2006-11-14 Array Biopharma, Inc. P38 inhibitors and methods of use thereof
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
GB0308185D0 (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
MXPA05010975A (es) 2003-04-16 2005-11-28 Hoffmann La Roche Derivados de (6-(fenoxi)-pirido[3,4-d]pirimidin-2-il)-amina como inhibidores de p38 cinasa para el tratamiento de condiciones inflamatorias como artritis reumatoide.
KR100812586B1 (ko) 2003-04-16 2008-03-13 에프. 호프만-라 로슈 아게 P38 키나아제 저해제로서 유용한 퀴나졸린 화합물
ATE482200T1 (de) 2003-05-01 2010-10-15 Bristol Myers Squibb Co Als kinaseinhibitoren geeignete arylsubstituierte pyrazolamidverbindungen
GB0320244D0 (en) 2003-05-06 2003-10-01 Aventis Pharma Inc Pyrazoles as inhibitors of tumour necrosis factor
CA2524409C (en) 2003-05-07 2011-12-20 Merck & Co., Inc. Androgen receptor modulators and methods of use thereof
EP1633714B1 (en) 2003-06-04 2008-01-23 Pfizer Limited 2-amino-pyridine derivatives as beta-2 adrenoreceptor agonists
ATE517872T1 (de) 2003-06-26 2011-08-15 Novartis Ag Fünfgliedrige p38-kinaseinhibitoren auf heterocyclusbasis
CA2530182A1 (en) 2003-06-30 2005-01-20 Merck & Co., Inc. 17-acetamido-4-azasteroid derivatives as androgen receptor modulators
WO2005005380A2 (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
GB0317516D0 (en) 2003-07-25 2003-08-27 Pfizer Ltd 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
US7153870B2 (en) 2003-07-25 2006-12-26 Pfizer Inc. Nicotinamide derivatives useful as PDE4 inhibitors
JP2007507204A (ja) 2003-07-29 2007-03-29 ブリストル−マイヤーズ　スクイブ　カンパニー サイクリン依存性キナーゼモデュレーションのバイオマーカー
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.
BRPI0413757A (pt) 2003-08-22 2006-10-31 Boehringer Ingelheim Pharma métodos para o tratamento de copd e da hipertensão pulmonar
US20050053600A1 (en) 2003-09-09 2005-03-10 Lane Thomas E. Methods for treating rheumatoid arthritis
WO2005025572A1 (en) 2003-09-10 2005-03-24 Merck & Co., Inc. 17-heterocyclic-4-azasteroid derivatives as androgen receptor modulators
WO2005023761A2 (en) 2003-09-11 2005-03-17 Kemia, Inc. Cytokine inhibitors
US20060019971A1 (en) 2003-09-30 2006-01-26 Higgins Linda S Treatment of cardiovascular disease with inhibitors of p38 kinase
US7232824B2 (en) 2003-09-30 2007-06-19 Scios, Inc. Quinazoline derivatives as medicaments
CA2540828A1 (en) 2003-09-30 2005-04-14 Scios Inc. Heterocyclic amides and sulfonamides
US7419978B2 (en) 2003-10-22 2008-09-02 Bristol-Myers Squibb Company Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors
KR100816321B1 (ko) 2003-11-13 2008-03-24 에프. 호프만-라 로슈 아게 히드록시알킬 치환 피리도-7-피리미딘-7-온
EP1538201A1 (en) 2003-12-02 2005-06-08 F.Hoffmann-La Roche Ag Method for the recombinant production and purification of protein kinases
GB0329275D0 (en) 2003-12-18 2004-01-21 Merck Sharp & Dohme Therapeutic treatment
RU2006121487A (ru) 2003-12-18 2007-12-27 Пфайзер Продактс Инк. (Us) СПОСОБЫ ЛЕЧЕНИЯ ОСТРОГО ВОСПАЛЕНИЯ У ЖИВОТНЫХ С ПОМОЩЬЮ ИНГИБИТОРОВ р38 МАР-киназы
EP1716121A1 (en) 2003-12-18 2006-11-02 Boehringer Ingelheim Pharmaceuticals Inc. Polymorph of birb 796, a p38map kinase inhibitor
US20060079461A1 (en) 2003-12-24 2006-04-13 Scios, Inc. Treatment of multiple myeloma by inhibition of p38 MAP kinase
US20060058296A1 (en) 2003-12-24 2006-03-16 Scios, Inc. Treatment of osteolytic lesions associated with multiple myeloma by inhibition of p38 map kinase
KR20070007055A (ko) 2003-12-24 2007-01-12 사이오스 인코퍼레이티드 Ｔｇｆ-베타 억제제를 이용한 악성 신경교종의 치료법
US20060052390A1 (en) 2003-12-24 2006-03-09 Scios, Inc. Treatment of multiple myeloma by p38 MAP kinase and proteasome inhibition
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
GB0402138D0 (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
GB0402140D0 (en) 2004-01-30 2004-03-03 Smithkline Beecham Corp Novel compounds
WO2005075425A2 (en) 2004-01-30 2005-08-18 Merck Patent Gmbh Substituted bisarylurea derivatives as kinase inhibitors
EP1720862A1 (en) 2004-02-03 2006-11-15 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
KR20060114022A (ko) 2004-02-27 2006-11-03 에프. 호프만-라 로슈 아게 인다졸 유도체 및 그들을 함유하는 약학 조성물
JP2007523936A (ja) 2004-02-27 2007-08-23 エフ．ホフマン−ラ　ロシュ　アーゲー ヘテロアリール縮合ピラゾロ誘導体
WO2005091891A2 (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
EP1577292A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylaminoethanol derivatives as beta2 receptor agonists
EP1577291A1 (en) 2004-03-17 2005-09-21 Pfizer Limited Phenylethanolamine derivatives as beta-2 agonists
EP1742631A4 (en) 2004-04-28 2009-11-11 Merck & Co Inc FLUORATED 4-AZASTEROIDS AS ANDROGEN RECEPTOR MODULATORS
CA2566677A1 (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
ES2308523T3 (es) 2004-06-23 2008-12-01 Eli Lilly And Company Inhibidores de quinasa.
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
PE20060421A1 (es) 2004-08-12 2006-06-01 Bristol Myers Squibb Co Procedimiento para preparar un compuesto de pirrolotriazina anilina como inhibidores de cinasa
SI1778686T1 (sl) 2004-08-12 2009-02-28 Pfizer Derivati triazolopiridinilsulfanila kot inhibitorji P38 MAP kinaze
CA2576988A1 (en) 2004-08-25 2006-03-09 Merck & Co., Inc. Androgen receptor modulators
US20070054916A1 (en) 2004-10-01 2007-03-08 Amgen Inc. Aryl nitrogen-containing bicyclic compounds and methods of use
AR055271A1 (es) 2004-10-05 2007-08-15 Smithkline Beecham Corp Compuesto del acido bifenil carboxilico, composicion farmaceutica que lo comprende, su uso para preparar esta ultima y proceso para prepararlo
US8003657B2 (en) 2004-10-13 2011-08-23 Merck Patent Gmbh Heterocyclic substituted bisarylurea derivatives
CN101389335A (zh) 2004-10-18 2009-03-18 安姆根有限公司 噻二唑化合物和使用方法
WO2006060108A1 (en) 2004-10-29 2006-06-08 Merck & Co., Inc. N-(pyridin-3-yl)-2-phenylbutanamides as androgen receptor modulators
US20060258582A1 (en) 2004-11-04 2006-11-16 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
CN101056842A (zh) 2004-11-16 2007-10-17 默克公司 治疗中风的(2r)－2－丙基辛酸前药
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
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
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
CN101080404B (zh) 2004-12-28 2011-06-08 Aska制药株式会社 嘧啶基异噁唑衍生物
US20060178388A1 (en) 2005-02-04 2006-08-10 Wrobleski Stephen T Phenyl-substituted pyrimidine compounds useful as kinase inhibitors
ES2351308T3 (es) 2005-02-28 2011-02-02 Merckle Gmbh Derivados de imidazol 2-sulfinil- y 2-sulfonil-sustituidos y su uso como inhibidores de citocina.
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
AR053450A1 (es) 2005-03-25 2007-05-09 Glaxo Group Ltd Derivados de 3,4-dihidro-pirimido(4,5-d)pirimidin-2-(1h)-ona 1,5,7 trisustituidos como inhibidores de la quinasa p38
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
WO2006110298A2 (en) 2005-03-25 2006-10-19 Glaxo Group Limited 8-alkyl/aryl-4-aryl-2-n- (alkylamino)-n'-substituted-n'-cyanoguanidino-8h-pyrido[2,3-d]pyrimidin-7-one compounds and use thereof
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
WO2006122230A1 (en) 2005-05-11 2006-11-16 Array Biopharma Inc. P38 inhibitors and methods of use thereof
JP2008545696A (ja) 2005-05-23 2008-12-18 スミスクライン・ビーチャム・コーポレイション 肥満の処置のためのｐ３８ｍａｒｋの阻害
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
CN101233109A (zh) 2005-08-02 2008-07-30 默克公司 用作雄激素受体调节剂的n-(吡啶-4-基)-2-苯基丁酰胺
CN102627640A (zh) 2005-08-12 2012-08-08 默沙东公司 可用作p38激酶抑制剂的杂二环化合物
US20070049592A1 (en) 2005-08-22 2007-03-01 Geuns-Meyer Stephanie D Bis-aryl urea compounds and methods of use
CA2620254A1 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 map kinase inhibitors and methods for using the same
BRPI0615442A2 (pt) 2005-08-25 2011-05-17 Hoffmann La Roche inibidores de p38 map cinase e métodos para uso dos mesmos
AU2006283945A1 (en) 2005-08-25 2007-03-01 F. Hoffmann-La Roche Ag P38 MAP kinase inhibitors and methods for using the same
KR20080031460A (ko) 2005-08-25 2008-04-08 에프. 호프만-라 로슈 아게 Ｐ38 ｍａｐ 키나아제 저해제 및 이의 사용 방법
MX2008002383A (es) 2005-08-25 2008-03-18 Hoffmann La Roche Pirazol fusionado como inhibidores de proteinas cinasas activadas por mitogenos p38.
CN101268079B (zh) 2005-09-01 2011-09-14 安斯泰来制药有限公司 用于治疗疼痛的哒嗪酮衍生物
AP1983A (en) 2005-09-21 2009-03-24 Pfizer Ltd Carboxamide derivatives as muscarinic receptor antagonists
AU2006294835B2 (en) 2005-09-26 2011-05-26 Merck Sharp & Dohme Corp. 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
DOP2006000234A (es) 2005-10-28 2007-05-31 Lilly Co Eli Inhibidores de cinasa
PE20070640A1 (es) 2005-10-28 2007-08-10 Lilly Co Eli Compuestos derivados de pirazol-isoquinolina urea como inhibidores de la cinasa p38
WO2007056016A2 (en) 2005-11-02 2007-05-18 Kemia, Inc. Bisamide cytokine inhibitors
WO2007052124A1 (en) 2005-11-04 2007-05-10 Pfizer Limited Tetrahydronaphthyridine derivative
BRPI0618379A2 (pt) 2005-11-08 2011-08-30 Ranbaxy Lab Ltd processo para preparação do hemi-sal de cálcio do ácido (3r,5r) -7-[2-(4-fluorofenil)-5-isopropil-3-fenil-4-[(4-hidroxime tilfenilamino) carbonil]-pirrol-1-il] -3, 5-diidroxi heptanóico
PE20100743A1 (es) 2005-11-15 2010-11-25 Glaxo Group Ltd Nuevos procedimientos y formulaciones
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
CA2636077C (en) 2006-01-18 2012-01-03 Amgen Inc. Thiazole compounds as protein kinase b (pkb) inhibitors
RU2442777C2 (ru) 2006-01-31 2012-02-20 Эррэй Биофарма Инк. Ингибиторы киназ и способы их применения
CA2642209A1 (en) 2006-02-09 2007-08-16 Pfizer Limited Triazolopyridine compounds
JP2009526039A (ja) 2006-02-10 2009-07-16 ファイザー・プロダクツ・インク ピリジノンピラゾール尿素およびピリミジノンピラゾール尿素誘導体
GB0603684D0 (en) 2006-02-23 2006-04-05 Novartis Ag Organic compounds
WO2007103839A2 (en) 2006-03-07 2007-09-13 Bristol-Myers Squibb Company Pyrrolotriazine aniline prodrug compounds useful as kinase inhibitors
US20070225339A1 (en) 2006-03-07 2007-09-27 Ramon Mohanlal Compositions and methods for treating rheumatoid arthritis
JP2009530364A (ja) 2006-03-20 2009-08-27 ファイザー・リミテッド アミン誘導体
US8026233B2 (en) 2006-03-29 2011-09-27 Array Biopharma Inc. P38 inhibitors and methods of use thereof
WO2007115670A1 (en) 2006-04-12 2007-10-18 Merck Patent Gmbh N-oxides of heterocyclic substituted bisarylureas for treating kinase-mediated diseases
CA2649543A1 (en) 2006-04-21 2007-11-01 Amgen Inc. Thieno-[2,3-d]pyrimidine and thieno-pyridazine compounds and methods of use
EP2035005A4 (en) 2006-06-09 2011-07-06 Kemia Inc THERAPY BASED ON CYTOKINE INHIBITORS
EP2032142A4 (en) 2006-06-16 2010-07-21 Glaxo Group Ltd NOVEL CONNECTIONS
US20100144755A1 (en) 2006-06-16 2010-06-10 Glaxo Group Limited Novel Compounds
GB0612026D0 (en) 2006-06-16 2006-07-26 Smithkline Beecham Corp New use
EP2031965A4 (en) 2006-06-16 2010-06-30 Glaxo Group Ltd NEW COMPOUNDS
KR20090031721A (ko) 2006-06-28 2009-03-27 아스카 세이야쿠 가부시키가이샤 염증성 장 질환의 처치제
ES2396251T3 (es) 2006-06-28 2013-02-20 Aska Pharmaceutical Co., Ltd. Derivado de piridilisoxazol
AU2007275696B2 (en) 2006-07-17 2011-11-10 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
WO2008105808A2 (en) 2006-07-28 2008-09-04 Onconova Therapeutics, Inc. FORMULATIONS OF RADIOPROTECTIVE α, β 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
KR20090050104A (ko) 2006-10-04 2009-05-19 화이자 리미티드 아드레날린성 효능제 및 무스카린성 길항제로서 술폰아미드 유도체
ATE542818T1 (de) 2006-10-11 2012-02-15 Amgen Inc Imidazo- und triazolopyridinverbindungen und verfahren zu deren anwendung
EP2083624A4 (en) 2006-10-18 2010-06-16 Merck Sharp & Dohme 2-HYDROXY-2-PHENYL / THIOPHENYLPROPIONAMIDE AS ANDROGEN RECEPTOR MODULATORS
CA2667543A1 (en) 2006-10-26 2008-05-02 Boehringer Ingelheim International Gmbh New pharmaceutical combinations 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
WO2008072079A2 (en) 2006-12-13 2008-06-19 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
RU2009126633A (ru) 2006-12-13 2011-01-20 Джилид Сайэнс, Инк. (US) Монофосфатные соединения, способ их получения, аэрозольный препарат (варианты) и способ профилактики и/или лечения бронхостеноза посредством указанных соединений
WO2008074676A1 (en) 2006-12-19 2008-06-26 F. Hoffmann-La Roche Ag Pyrazolo [3, 4 -d] pyrimidine p38 map kinase inhibitors
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
US8063094B2 (en) 2007-02-08 2011-11-22 Boehringer Ingelheim International Gmbh Anti-cytokine heterocyclic compounds
CN101610754A (zh) 2007-02-16 2009-12-23 Aska制药株式会社 含有微粒油性混悬液的药物组合物
US20100015218A1 (en) 2007-02-16 2010-01-21 Vasant Jadhav Compositions and methods for potentiated activity of biologically active molecules
WO2008104473A2 (en) 2007-02-28 2008-09-04 F. Hoffmann-La Roche Ag Pyrazolopyriidine derivatives and their use as kinase inhibitors
US8263583B2 (en) 2007-03-16 2012-09-11 Pfizer Limited Hydrochloride salt of 5-[3-(3-hydroxyphenoxy)azetidin-1-yl]-5-methyl-2,2-diphenylhexanamide
WO2008136948A1 (en) 2007-05-07 2008-11-13 Amgen Inc. Pyrazolo-pyridinone and pyrazolo-pyrazinone compounds as p38 modulators, process for their preparation, and their pharmaceutical use
EP2152704A1 (en) 2007-05-07 2010-02-17 Amgen, Inc Pyrazolo-pyridinone compounds, process for their preparation, and their pharmaceutical use
EP2173728A2 (en) 2007-07-17 2010-04-14 Amgen Inc. Heterocyclic modulators of pkb
AU2008276512A1 (en) 2007-07-17 2009-01-22 Amgen Inc. Thiadiazole 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
US8202899B2 (en) 2007-07-25 2012-06-19 Array Biopharma Inc. Pyrazole urea derivatives used as kinase inhibitors
WO2009034432A2 (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
BRPI0820447A2 (pt) 2007-11-30 2015-05-26 Pfizer Ltd Agonistas do receptor de glicocorticóides
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
WO2009094556A2 (en) 2008-01-25 2009-07-30 Bristol-Myers Squibb Pharma Company Identification of predictive markers of response to dasatinib in human colon cancer
JP2011512209A (ja) 2008-02-20 2011-04-21 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 粉末吸入器
WO2009117156A1 (en) 2008-03-21 2009-09-24 Amgen Inc. Pyrazolo-pyrazinone compounds and methods of use thereof
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
CN102131806A (zh) 2008-06-20 2011-07-20 百时美施贵宝公司 用作激酶抑制剂的***并吡啶化合物
WO2009155388A1 (en) 2008-06-20 2009-12-23 Bristol-Myers Squibb Company Imidazopyridine and imidazopyrazine compounds useful as kinase inhibitors
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
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
US8263623B2 (en) 2008-07-11 2012-09-11 Pfizer Inc. Triazol derivatives useful for the treatment of diseases
JP2011528346A (ja) 2008-07-15 2011-11-17 ファイザー・リミテッド ムスカリン受容体アンタゴニストとして活性のある新規化合物
WO2010007561A1 (en) 2008-07-15 2010-01-21 Pfizer Limited Novel compounds active as muscarinic receptor antagonists
US8455495B2 (en) 2008-08-29 2013-06-04 Amgen Inc. Pyridazino-pyridinone compounds and methods of use
EP2334673A1 (en) 2008-08-29 2011-06-22 Amgen Inc. PYRIDO[3,2-d]PYRIDAZINE-2(1H)-ONE COMPOUNDS AS P38 MODULATORS AND METHODS OF USE THEREOF
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
WO2010042646A1 (en) 2008-10-10 2010-04-15 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
WO2010083246A1 (en) 2009-01-15 2010-07-22 Amgen Inc. Fluoroisoquinoline substituted thiazole compounds and methods of use
US20120129820A1 (en) 2009-02-09 2012-05-24 Boehringer Ingelheim International Gmbh New pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
MX2011008499A (es) 2009-02-13 2011-09-06 Vertex Pharma Formas solidas de 2-(2,4-difluorofenil)-6-(1-(2,6-difluorofenil)ur eido)nicotinamida.
EP2396302A2 (en) 2009-02-13 2011-12-21 Vertex Pharmceuticals Incorporated Processes for producing phenyl-6-(1-(phenyl)ureido)nicotinamides)
WO2010094956A1 (en) 2009-02-17 2010-08-26 Pulmagen Therapeutics (Inflammation) Limited. Triazolopyridine derivatives as p38 map kinase inhibitors
GB0902648D0 (en) 2009-02-17 2009-04-01 Argenta Discovery Ltd Pharmaceutical compounds and compositions
WO2010120963A1 (en) 2009-04-16 2010-10-21 Bristol-Myers Squibb Company Tablet formulation for p38 inhibitor and method
AU2010245072B2 (en) 2009-05-05 2013-11-28 Merck Sharp & Dohme Corp. p38 kinase inhibiting agents
US20120157500A1 (en) 2009-08-24 2012-06-21 Weikang Tao Jak inhibition blocks rna interference associated toxicities
BR112012009257A2 (pt) 2009-10-22 2016-11-22 Genentech Inc modulação de degeneração de axônio.
WO2011063076A1 (en) 2009-11-19 2011-05-26 Itherx Pharmaceuticals, Inc. 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
US9044427B2 (en) 2010-03-24 2015-06-02 Onconova Therapeutics, Inc Compositions and methods for prevention and treatment of wounds
CA2792913C (en) 2010-03-26 2020-01-21 Onconova Therapeutics, Inc. Improved stable aqueous formulation of (e)-4-carboxystyryl-4-chlorobenzyl sulfone
GB201009731D0 (en) 2010-06-10 2010-07-21 Pulmagen Therapeutics Inflamma Kinase inhibitors
US8791113B2 (en) 2010-06-28 2014-07-29 Merck Patent Gmbh 2,4-diaryl-substituted [1,8] naphthyridines as kinase inhibitors for use against cancer
BR112012033658A2 (pt) 2010-07-05 2016-11-29 Merck Patent Gmbh derivados bipiridílicos úteis para o tratamento de doenças induzidas por quinases
WO2012031057A1 (en) 2010-09-01 2012-03-08 Bristol-Myers Squibb Company Bms- 582949 for the treatment of resistant rheumatic disease
KR20130142144A (ko) 2010-11-29 2013-12-27 제넨테크, 인크. 신경변성 질환 또는 장애의 검출 방법
AR083868A1 (es) 2010-12-03 2013-03-27 Lilly Co Eli Compuestos de oxazol[5,4-b]piridin-5-ilo
KR20140022829A (ko) 2011-03-09 2014-02-25 메르크 파텐트 게엠베하 피리도 [2, 3 - ｂ] 피라진 유도체 및 그 치료적 용도
US8697627B2 (en) 2011-05-09 2014-04-15 Eip Pharma, Llc Compositions and methods for treating alzheimer's disease
WO2012168359A1 (en) 2011-06-10 2012-12-13 Chiesi Farmaceutici S.P.A. Compounds having muscarinic receptor antagonist and beta2 adrenergic receptor agonist activity
WO2013007708A1 (en) 2011-07-08 2013-01-17 Helmholtz-Zentrum für Infektionsforschung GmbH Medicament for treatment of liver cancer
DK2780011T3 (en) 2011-11-11 2018-05-28 Lilly Co Eli COMBINATION THERAPY AGAINST OVARI 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
DK2788349T3 (en) 2011-12-09 2017-01-30 Chiesi Farm Spa kinase inhibitors
SG11201402986RA (en) 2011-12-09 2014-12-30 Chiesi Farma Spa Kinase inhibitors
KR20140103925A (ko) 2011-12-09 2014-08-27 키에시 파르마슈티시 엣스. 피. 에이. 4-히드록시-1,2,3,4-테트라히드로나프탈렌-1-일 우레아 및 호흡기 질환의 치료에서의 이들의 용도
CN104736569A (zh) 2012-01-12 2015-06-24 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
PL2819998T3 (pl) 2012-03-01 2022-06-27 Array Biopharma Inc. Krystaliczne postacie chlorowodorku 1-(3-tert-butylo-1-p-tolilo-1h-pirazol-5-ilo)-3-(5-fluoro-2-(1-(2-hydroksyetylo)-1h-indazol-5-iloksy)benzylo)mocznika
CA2866108C (en) 2012-03-20 2017-03-07 Novartis Ag Use of a pyrazole derivative in the treatment of acute exacerbations of chronic obstructive pulmonary disease
EP2852584B1 (en) 2012-05-22 2018-02-28 F. Hoffmann-La Roche AG Substituted dipyridylamines and uses thereof
KR20150036631A (ko) 2012-07-17 2015-04-07 글락소스미스클라인 엘엘씨 급성 관상동맥 증후군의 치료에서의 니코틴아미드 유도체
GB201214750D0 (en) 2012-08-17 2012-10-03 Respivert Ltd Compounds
GB201215357D0 (en) 2012-08-29 2012-10-10 Respivert Ltd Compounds
WO2014033449A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033447A2 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
WO2014033446A1 (en) 2012-08-29 2014-03-06 Respivert Limited Kinase inhibitors
US9155747B2 (en) 2012-09-13 2015-10-13 Chiesi Farmaceutici S.P.A. Isoxazolidine derivatives
WO2014076484A1 (en) 2012-11-16 2014-05-22 Respivert Limited Kinase inhibitors
CA2891634A1 (en) 2012-11-30 2014-06-05 F. Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
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
US9790206B2 (en) 2013-02-27 2017-10-17 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
MX363950B (es) 2013-04-02 2019-04-08 Topivert Pharma Ltd Derivados de urea utiles como inhibidores de quinasa.
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
BR112015029504A2 (pt) 2013-06-06 2017-07-25 Chiesi Farm Spa inibidores quinase
CN105377847A (zh) 2013-06-06 2016-03-02 奇斯药制品公司 激酶抑制剂
KR20160015221A (ko) 2013-06-06 2016-02-12 키에시 파르마슈티시 엣스. 피. 에이. 키나아제 억제제
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
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.
WO2015092423A1 (en) 2013-12-20 2015-06-25 Respivert Limited Urea derivatives useful as kinase inhibitors
CN110522731B (zh) 2014-02-14 2022-08-02 瑞斯比维特有限公司 作为抗炎化合物的芳族杂环化合物
CA2940028A1 (en) 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease
WO2015191986A1 (en) 2014-06-13 2015-12-17 Genentech, Inc. Methods of treating and preventing cancer drug resistance
JP2017517558A (ja) 2014-06-13 2017-06-29 ジェネンテック， インコーポレイテッド 癌薬剤耐性の治療方法及び防止方法
EP3166610B1 (en) 2014-07-09 2022-11-02 Eip Pharma, LLC Methods for treating neurologic disorders
WO2016051186A1 (en) 2014-10-01 2016-04-07 Respivert Limited N-phenyl-3-quinazolin-6-yl-benzamide derivatives as p38 kinase inhibitors
MA40775A (fr) 2014-10-01 2017-08-08 Respivert Ltd Dérivé d'acide 4-(4-(4-phényluréido-naphtalén -1-yl) oxy-pyridin-2-yl) amino-benzoïque utilisé en tant qu'inhibiteur de la kinase p38
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
WO2016115490A1 (en) 2015-01-16 2016-07-21 Ionis Pharmaceuticals, Inc. Compounds and methods for modulation of dux4
CA2975750C (en) * 2015-02-06 2023-06-13 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
CN107406462B (zh) 2015-03-09 2020-11-10 豪夫迈·罗氏有限公司 三环dlk抑制剂及其用途
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
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
KR102161364B1 (ko) 2015-09-14 2020-09-29 화이자 인코포레이티드 LRRK2 억제제로서 이미다조[4,5-c]퀴놀린 및 이미다조[4,5-c][1,5]나프티리딘 유도체
US9427439B1 (en) 2015-10-26 2016-08-30 Eip Pharma, Llc Methods and compositions for recovery from stroke
JP6889493B2 (ja) 2015-10-26 2021-06-18 イーアイピー ファーマ， エルエルシー 脳卒中からの回復のための方法および組成物
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
CA3008113A1 (en) 2015-12-24 2017-06-29 The Doshisha Drug for treating or preventing disorder caused by tgf-.beta. signals, and application thereof
CA3010101A1 (en) 2015-12-29 2017-07-06 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
WO2017211830A1 (en) 2016-06-08 2017-12-14 Support-Venture Gmbh Pharmaceutical combinations for treating 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
WO2018148797A1 (en) 2017-02-15 2018-08-23 The University Of Melbourne A method of treatment
CA3128468A1 (en) 2017-10-05 2019-04-11 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce dux4 and downstream gene expression 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
WO2019103926A1 (en) 2017-11-21 2019-05-31 Saint Louis University P38 inhibitors for the treatment of fshd
EP3883597A2 (en) 2018-11-20 2021-09-29 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
JP2022525199A (ja) 2019-03-15 2022-05-11 フルクラム セラピューティクス，インコーポレイテッド Ｅｅｄおよびｐｒｃ２調節物質としての大環状アゾロピリジン誘導体
UY39417A (es) * 2020-09-11 2022-03-31 Arrowhead Pharmaceuticals Inc Agentes de arni para inhibir la expresión de dux4, composiciones de dichos agentes, y métodos de uso

Also Published As

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

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
CY1120361T1 (el) Αναστολεις 2,3-διοξυγενασης ινδολαμινης (ido)
CO2018012946A2 (es) Moduladores de la vía de estrés integrada
CL2017002494A1 (es) Inhibidores de indolamina-2, 3- dioxigenasa para el tratamiento de cancer
ECSP19044183A (es) (aza)indol-, benzotiofen, y benzofuran-3-sulfonamidas
CL2018001899A1 (es) Salicilamidas de espiroheptanos y compuestos relacionados como inhibidores de cinasa rho (rock)
CL2018000198A1 (es) Composiciones de arni de transtiretina (ttr) y métodos para su uso para el tratamiento o prevencion de enfermedades asociadas con ttr
CL2017002994A1 (es) Compuestos de naftiridina como inhibidores de la quinasa jak
MX2020004537A (es) Moduladores de la vía integrada del estrés.
CR20230182A (es) MODULADORES DE PROFÁRMACOS DE LA VÍA DE ESTRÉS INTEGRADA (Divisional Expediente 2021-238)
MX2018008815A (es) Inhibidores de tirosina quinasa de bruton.
EA201992147A1 (ru) Ингибиторы тирозинкиназы брутона
UY36654A (es) Azabenzimidazoles con propiedades moduladoras del receptor ampa y composiciones farmacéuticas que los contienen
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
CO2020003134A2 (es) Moduladores de la expresión de enac
GEP20227437B (en) 1h-indazole-3-carboxamide compounds as glycogen synthase kinase 3 beta inhibitors
WO2018211324A8 (en) Prodrugs for the treatment of disease
EA202090859A1 (ru) Ингибиторы киназы p38 снижают экспрессию dux4 и последующих генов для лечения fshd
EA202190844A1 (ru) Способы лечения миелопролиферативных расстройств
MX2020000491A (es) Moduladores terapeuticos del modo inverso de la atp sintasa.