PH12018501583A1 - Inhibitors of receptor-interacting protein kinase 1 - Google Patents

Inhibitors of receptor-interacting protein kinase 1

Info

Publication number
PH12018501583A1
PH12018501583A1 PH12018501583A PH12018501583A PH12018501583A1 PH 12018501583 A1 PH12018501583 A1 PH 12018501583A1 PH 12018501583 A PH12018501583 A PH 12018501583A PH 12018501583 A PH12018501583 A PH 12018501583A PH 12018501583 A1 PH12018501583 A1 PH 12018501583A1
Authority
PH
Philippines
Prior art keywords
inhibitors
receptor
protein kinase
interacting protein
necroptosis
Prior art date
Application number
PH12018501583A
Other languages
English (en)
Inventor
Anthony A Estrada
Jianwen A Feng
Brian Fox
Colin Philip Leslie
Joseph P Lyssikatos
Alfonso Pozzan
Zachary K Sweeney
Vicente Fidalgo Javier De
Original Assignee
Denali 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 Denali Therapeutics Inc filed Critical Denali Therapeutics Inc
Publication of PH12018501583A1 publication Critical patent/PH12018501583A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/12—Antidiarrhoeals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P23/00—Anaesthetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D267/02—Seven-membered rings
    • C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
    • C07D267/12—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D267/14—Seven-membered rings having the hetero atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Ophthalmology & Optometry (AREA)
PH12018501583A 2016-02-05 2018-07-25 Inhibitors of receptor-interacting protein kinase 1 PH12018501583A1 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201662292202P 2016-02-05 2016-02-05
US201662341019P 2016-05-24 2016-05-24
US201662363775P 2016-07-18 2016-07-18
US201662385217P 2016-09-08 2016-09-08
US201662417219P 2016-11-03 2016-11-03
PCT/US2017/016509 WO2017136727A2 (en) 2016-02-05 2017-02-03 Compounds, compositions and methods

Publications (1)

Publication Number Publication Date
PH12018501583A1 true PH12018501583A1 (en) 2019-04-08

Family

ID=58054535

Family Applications (1)

Application Number Title Priority Date Filing Date
PH12018501583A PH12018501583A1 (en) 2016-02-05 2018-07-25 Inhibitors of receptor-interacting protein kinase 1

Country Status (24)

Country Link
US (8) US9815850B2 (enExample)
EP (1) EP3414239A2 (enExample)
JP (2) JP6974331B2 (enExample)
KR (1) KR102808827B1 (enExample)
CN (4) CN118994191A (enExample)
AU (1) AU2017213628B2 (enExample)
CA (1) CA3012832A1 (enExample)
CL (1) CL2018002081A1 (enExample)
CO (1) CO2018008707A2 (enExample)
CR (1) CR20180413A (enExample)
DO (1) DOP2018000175A (enExample)
EA (1) EA201891620A1 (enExample)
EC (1) ECSP18066138A (enExample)
IL (2) IL287136B2 (enExample)
MA (1) MA44007A (enExample)
MX (3) MX2018009448A (enExample)
MY (1) MY196648A (enExample)
PE (1) PE20181665A1 (enExample)
PH (1) PH12018501583A1 (enExample)
SA (1) SA518392146B1 (enExample)
SG (2) SG11201806302RA (enExample)
TN (1) TN2018000276A1 (enExample)
TW (2) TWI781920B (enExample)
WO (1) WO2017136727A2 (enExample)

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI648274B (zh) 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
RU2716136C2 (ru) 2015-07-02 2020-03-06 Ф. Хоффманн-Ля Рош Аг Бициклические лактамы и способы их применения
MY197231A (en) 2015-07-22 2023-06-06 Enanta Pharm Inc Benzodiazepine derivatives as rsv inhibitors
US10961258B2 (en) 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
CN108699077B (zh) 2016-01-15 2021-03-02 英安塔制药有限公司 作为rsv抑制剂的杂环化合物
US9815850B2 (en) * 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods
TWI759301B (zh) 2016-05-24 2022-04-01 美商安美基公司 聚乙二醇化卡非佐米化合物
PT3472153T (pt) * 2016-06-16 2021-12-31 Denali Therapeutics Inc Pirimidin-2-ilamino-1h-pirazóis como inibidores de lrrk2 para uso no tratamento de distúrbios neurodegenerativos
JP7349359B2 (ja) 2016-10-17 2023-09-22 エフ． ホフマン－ラ ロシュ アーゲー 二環式ピリドンラクタム及びその使用方法。
US11071721B2 (en) 2016-12-02 2021-07-27 Genentech, Inc. Bicyclic amide compounds and methods of use thereof
US11072607B2 (en) * 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
WO2018152413A1 (en) 2017-02-16 2018-08-23 Enanta Pharmaceuticals, Inc. Processes for the preparation of benzodiazepine derivatives
EP3585782A1 (en) 2017-02-27 2020-01-01 GlaxoSmithKline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
WO2018226801A1 (en) 2017-06-07 2018-12-13 Enanta Pharmaceuticals, Inc. Aryldiazepine derivatives as rsv inhibitors
US10851115B2 (en) 2017-06-30 2020-12-01 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
WO2019006295A1 (en) 2017-06-30 2019-01-03 Enanta Pharmaceuticals, Inc. HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
CN119613408A (zh) 2017-07-14 2025-03-14 豪夫迈·罗氏有限公司 二环酮化合物及其使用方法
CN107759574B (zh) * 2017-08-29 2020-07-03 南京药石科技股份有限公司 一种5-氟-1h-吡唑-3-甲酸酯中间体及其合成方法
CN111386118B (zh) 2017-09-29 2023-05-09 英安塔制药有限公司 作为rsv抑制剂的组合药物剂
WO2019072942A1 (en) * 2017-10-11 2019-04-18 F. Hoffmann-La Roche Ag BICYCLIC COMPOUNDS FOR USE AS INHIBITORS OF KINASE RIP1
MX2020003451A (es) * 2017-10-31 2020-08-03 Hoffmann La Roche Sulfonas y sulfoxidos biciclicos y metodos de uso de los mismos.
MX394621B (es) 2017-11-13 2025-03-24 Enanta Pharm Inc Procesos para la resolucion de los derivados de la benzodiazepina-2-ona y de la benzoazepin-2-ona
WO2019094920A1 (en) * 2017-11-13 2019-05-16 Enanta Pharmaceuticals, Inc. Azepin-2-one derivatives as rsv inhibitors
CN108129288B (zh) * 2017-12-27 2021-01-22 上海毕得医药科技股份有限公司 一种反式-3-羟基环丁基甲酸的合成方法
WO2019199908A1 (en) 2018-04-11 2019-10-17 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as rsv inhibitors
EP3781571B1 (en) 2018-04-20 2024-01-17 F. Hoffmann-La Roche AG N-[4-oxo-2,3-dihydro-pyrido[3,2-b][1,4]oxazepin-3-yl]-5,6-dihydro-4h-pyrrolo[1,2-b]pyrazole-2-carboxamide derivatives and related compounds as rip1 kinase inhibitors for treating e.g. irritable bowel syndrome (ibs)
SI3788044T1 (sl) * 2018-05-03 2023-12-29 Rigel Pharmaceuticals, Inc. Spojine, ki zavirajo RIP1 in postopki za njihovo izdelavo in uporabo
PL3788045T3 (pl) * 2018-05-03 2023-10-09 Rigel Pharmaceuticals, Inc. Związki hamujące rip1 oraz sposoby ich wytwarzania i wykorzystania
WO2020001420A1 (zh) * 2018-06-26 2020-01-02 中国科学院上海有机化学研究所 一类细胞坏死抑制剂及其制备方法和用途
WO2020044206A1 (en) 2018-08-29 2020-03-05 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors for use in the treatment cancer
WO2020054657A1 (ja) * 2018-09-10 2020-03-19 科研製薬株式会社 新規ヘテロ芳香族アミド誘導体及びそれを含有する医薬
CN111138448B (zh) * 2018-11-02 2022-08-02 中国科学院上海药物研究所 抑制rip1激酶的杂环酰胺及其用途
JP7045526B2 (ja) * 2018-11-02 2022-03-31 中国科学院上海薬物研究所 Ｒｉｐ１キナーゼを阻害する複素環状アミド及びその使用
BR112021009610A2 (pt) 2018-11-20 2021-08-10 Sironax Ltd composto, composição farmacêutica, uso de um composto ou composição, e, método de inibir necrose, ferroptose, rip1 humana ou indicações relacionadas
EP3670667A1 (en) * 2018-12-19 2020-06-24 Paris Sciences et Lettres - Quartier Latin Identification of cognate pairs of ligands and receptors
CN113302193B (zh) 2019-01-11 2026-05-29 豪夫迈·罗氏有限公司 双环吡咯并三唑酮化合物及其使用方法
CA3127701C (en) * 2019-01-25 2023-08-15 Beijing Scitech-Mq Pharmaceuticals Limited Acylamino bridged heterocyclic compound, and composition and application thereof
WO2020190935A1 (en) 2019-03-18 2020-09-24 Enanta Pharmaceuticals, Inc. Benzodiazepine derivatives as rsv inhibitors
US11179400B2 (en) 2019-04-09 2021-11-23 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as RSV inhibitors
CA3142360C (en) * 2019-05-31 2023-11-14 Medshine Discovery Inc. Bicyclic compound as rip-1 kinase inhibitor and application thereof
CN110172068A (zh) * 2019-06-05 2019-08-27 河南龙湖生物技术有限公司 具有抗肿瘤活性的苯并噻唑类化合物及其制备方法和应用
US12365695B2 (en) * 2019-08-09 2025-07-22 Bisichem Co., Ltd. Fused ring heteroaryl compounds as RIPK1 inhibitors
AU2020341708B2 (en) 2019-09-06 2024-01-04 Rigel Pharmaceuticals, Inc. RIP1 inhibitory compounds and methods for making and using the same
ES3043457T3 (en) * 2019-09-06 2025-11-25 Rigel Pharmaceuticals Inc Rip1 inhibitory compounds and methods for making and using the same
US11718612B2 (en) 2019-09-06 2023-08-08 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase I for the treatment of disease
WO2021050672A1 (en) * 2019-09-11 2021-03-18 Ohio State Innovation Foundation Kinase inhibitors for the treatment of neurodegenerative diseases
IL291665B2 (en) 2019-09-27 2025-07-01 Univ Texas Inhibitors of receptor interacting protein kinase i for the treatment of disease
US11505558B1 (en) 2019-10-04 2022-11-22 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
PH12022550783A1 (en) 2019-10-04 2023-07-31 Enanta Pharm Inc Antiviral heterocyclic compounds
SMT202600151T1 (it) * 2019-11-07 2026-05-12 Rigel Pharmaceuticals Inc Composti eterociclici inibitori di rip1
AU2020391425A1 (en) * 2019-11-26 2022-06-16 Board Of Regents, The University Of Texas System Inhibitors of Receptor Interacting Protein Kinase 1 for the treatment of disease
UY39032A (es) 2020-01-24 2021-07-30 Enanta Pharm Inc Compuestos heterocíclicos como agentes antivirales
BR112022017099A2 (pt) 2020-02-28 2022-11-16 Univ Texas Composto, composição farmacêutica, método para inibição de ripk1, método para tratamento de uma doença mediada por ripk1 e método para tratamento de lesão no snc
AR121717A1 (es) 2020-04-02 2022-06-29 Rigel Pharmaceuticals Inc Inhibidores de rip1k
CA3173330A1 (en) * 2020-04-17 2021-10-21 Genzyme Corporation Eclitasertib for use in treating conditions involving systemichyperinflammatory response
TW202214617A (zh) 2020-06-02 2022-04-16 法商賽諾菲公司 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途
TWI824259B (zh) * 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
WO2022010882A1 (en) 2020-07-07 2022-01-13 Enanta Pharmaceuticals, Inc, Dihydroquinoxaline and dihydropyridopyrazine derivatives as rsv inhibitors
WO2022086840A1 (en) 2020-10-19 2022-04-28 Enanta Pharmaceuticals, Inc. Heterocyclic compounds as anti-viral agents
WO2022109360A1 (en) 2020-11-23 2022-05-27 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
CN114716427B (zh) * 2021-01-07 2024-04-26 成都贝诺科成生物科技有限公司 一种作为rip抑制剂的化合物及其制备方法和用途
WO2022171110A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Fused tricyclic compounds as rip1-kinase inhibitors and uses thereof
WO2022171111A1 (en) * 2021-02-10 2022-08-18 Zai Lab (Us) Llc Heteroaryl-fused bicyclic compound as rip1-kinase inhibitors and uses thereof
US12612412B2 (en) 2021-02-26 2026-04-28 Enanta Pharmaceuticals, Inc. Antiviral heterocyclic compounds
MX2023009961A (es) 2021-02-26 2023-09-05 Enanta Pharm Inc Compuestos heterociclicos antivirales.
TW202300490A (zh) 2021-03-11 2023-01-01 美商雷傑製藥公司 雜環rip1激酶抑制劑
JP7651929B2 (ja) 2021-04-19 2025-03-27 住友ゴム工業株式会社 ゴム組成物及びタイヤ
US11970502B2 (en) 2021-05-04 2024-04-30 Enanta Pharmaceuticals, Inc. Macrocyclic antiviral agents
CN114989156B (zh) * 2021-05-19 2024-07-05 成都贝诺科成生物科技有限公司 一种受体相互作用蛋白抑制剂及其制备方法和用途
TW202321211A (zh) 2021-08-10 2023-06-01 美商艾伯維有限公司 菸鹼醯胺ripk1抑制劑
KR20240099181A (ko) * 2021-09-17 2024-06-28 주식회사 비씨켐 Ripk1 저해제로서 융합된 이종환식 고리
CN118510775A (zh) 2021-11-11 2024-08-16 建新公司 作为ripk1抑制剂的异噁唑烷及其用途
WO2023086352A1 (en) 2021-11-12 2023-05-19 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
US11858945B2 (en) 2021-11-12 2024-01-02 Enanta Pharmaceuticals, Inc. Alkyne-containing antiviral agents
WO2023086400A1 (en) 2021-11-12 2023-05-19 Enanta Pharmaceuticals, Inc. Novel spiropyrrolidine derived antiviral agents
US11993600B2 (en) 2021-12-08 2024-05-28 Enanta Pharmaceuticals, Inc. Saturated spirocyclics as antiviral agents
KR20230100646A (ko) 2021-12-24 2023-07-05 제일약품주식회사 Ripk1 저해제로서의 신규한 화합물 및 이를 포함하는 약학적 조성물
EP4209213A1 (en) 2022-01-05 2023-07-12 Universität zu Köln Signalling-pathway inhibitor combinations for use in the treatment of cancer diseases
US12006291B2 (en) 2022-01-11 2024-06-11 Enanta Pharmaceuticals, Inc. Processes for the preparation of 4,6,7-trifluoro-1H-indole-2-carboxylic acid
EP4463229A1 (en) * 2022-01-12 2024-11-20 Denali Therapeutics Inc. Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide
CN116640156B (zh) * 2022-02-22 2025-10-24 上海齐鲁制药研究中心有限公司 Ripk1抑制剂
EP4495119A4 (en) 2022-03-16 2025-06-25 Jiangsu Hengrui Pharmaceuticals Co., Ltd. FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD AND MEDICAL USE THEREOF
US12145942B2 (en) 2022-04-05 2024-11-19 Enanta Pharmaceuticals, Inc. Spiropyrrolidine derived antiviral agents
AR129003A1 (es) 2022-04-07 2024-07-03 Enanta Pharm Inc Compuestos heterocíclicos antivirales
WO2023211997A1 (en) 2022-04-27 2023-11-02 Enanta Pharmaceuticals, Inc. Antiviral compounds
WO2024170776A1 (en) 2023-02-17 2024-08-22 Universität Zu Köln Triple kinase inhibition for the treatment of type i interferon response associated disorders
KR20260074423A (ko) * 2023-08-16 2026-05-22 주식회사 비씨켐 Rip1 키나아제 억제제로서의 피라졸-1-카르복스아미드
WO2025045253A1 (zh) * 2023-08-31 2025-03-06 杭州百诚医药科技股份有限公司 苯并氮杂䓬酮类衍生物及其用途
CN118084889B (zh) * 2024-01-16 2024-09-27 宁夏医科大学 吲哚3-芳基-5-甲酰胺类衍生物及用途
CN117849327A (zh) * 2024-03-06 2024-04-09 军科正源（北京）药物研究有限责任公司 用于检测苏金单抗抗药性抗体的方法
EP4652998A1 (en) 2024-05-21 2025-11-26 Technische Universität München Treatment of receptor-interacting protein kinase 1- mediated disease with eclitasertib
WO2026006589A1 (en) 2024-06-27 2026-01-02 Genzyme Corporation Eclitasertib for treating receptor-interacting protein kinase 1 -mediated diseases
WO2026085124A1 (en) * 2024-10-15 2026-04-23 Genzyme Corporation Process for preparing (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5- tetrahydropyrido[3,2-b][l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3- carboxamide
WO2026138869A1 (zh) * 2024-12-26 2026-07-02 津药药业股份有限公司 Ripk1抑制剂及其用途

Family Cites Families (173)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6204261B1 (en) 1995-12-20 2001-03-20 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β Converting enzyme inhibitors
US4477464A (en) 1983-02-10 1984-10-16 Ciba-Geigy Corporation Hetero-benzazepine derivatives and their pharmaceutical use
EP0187037A3 (en) 1984-12-21 1988-03-23 Takeda Chemical Industries, Ltd. Piperidine derivatives, their production and use
JPH035933Y2 (enExample) 1987-08-04 1991-02-15
EP0322779A3 (en) 1987-12-29 1991-05-08 Yoshitomi Pharmaceutical Industries, Ltd. Benzolactam compounds and pharmaceutical uses thereof
JPH0256318A (ja) 1988-08-19 1990-02-26 Fujio Asai 丸棒材の繰出しケース
JPH0295996A (ja) 1988-10-03 1990-04-06 Honda Motor Co Ltd 鞍乗型車両
JPH0334977A (ja) 1989-06-29 1991-02-14 Yoshitomi Pharmaceut Ind Ltd イミダゾリルベンゾラクタム化合物
NZ238576A (en) 1990-06-18 1994-12-22 Merck & Co Inc Pyridinone derivatives, preparation and pharmaceutical compositions thereof
EP0481614A1 (en) 1990-10-01 1992-04-22 Merck & Co. Inc. Substituted pyridopyrimidinones and related heterocycles as angiotensin II antagonists
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
US5206235A (en) 1991-03-20 1993-04-27 Merck & Co., Inc. Benzo-fused lactams that promote the release of growth hormone
CA2078758C (en) 1991-09-27 2003-12-09 Alan M. Warshawsky 2-substituted indane-2-mercaptoacetylamide derivatives useful as inhibitors of enkephalinase and ace
US5457196A (en) 1991-09-27 1995-10-10 Merrell Dow Pharmaceuticals Inc. 2-substituted indane-2-carboxyalkyl derivatives useful as inhibitors of enkephalinase and ACE
JP3358069B2 (ja) 1991-12-24 2002-12-16 武田薬品工業株式会社 三環性複素環類、その製造法及び剤
US5484917A (en) 1993-06-16 1996-01-16 Pfizer Inc. Substituted tetrahydrobenzazepinones
JP2655754B2 (ja) 1992-07-01 1997-09-24 フアイザー・インコーポレイテツド コレシストキニンレセプター拮抗剤としてのベンゾチアゼピン及びベンゾオキサゼピンの誘導体
US5420271A (en) 1992-08-24 1995-05-30 Merrell Dow Pharmaceuticals, Inc. 2-substituted indane-2-mercaptoacetylamide tricyclic derivatives useful as inhibitors of enkephalinase
JP3427937B2 (ja) 1992-08-24 2003-07-22 メレルダウファ−マス−ティカルズ インコーポレイテッド エンケファリナーゼ阻害剤として有用な新規な２‐置換インダン‐２‐メルカプトアセチルアミド三環式誘導体類
US5283241A (en) 1992-08-28 1994-02-01 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
JPH07501085A (ja) 1992-09-03 1995-02-02 ベーリンガー　インゲルハイム　コマンディトゲゼルシャフト 新規なアミノ酸誘導体、その製造方法及びこれらの化合物を含む医薬組成物
US5583130A (en) 1992-09-25 1996-12-10 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
US5317017A (en) 1992-09-30 1994-05-31 Merck & Co., Inc. N-biphenyl-3-amido substituted benzolactams stimulate growth hormone release
US5374721A (en) 1992-10-14 1994-12-20 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
EP0619751B1 (en) 1992-10-16 2003-05-07 Suprex Corporation Automated supercritical fluid extraction
GB2272439A (en) 1992-11-13 1994-05-18 Merck & Co Inc Benzo-fused lactams that inhibit the release of growth hormone
US5284841A (en) 1993-02-04 1994-02-08 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
GB9307833D0 (en) 1993-04-15 1993-06-02 Glaxo Inc Modulators of cholecystokinin and gastrin
WO1994026718A1 (fr) 1993-05-13 1994-11-24 Yoshitomi Pharmaceutical Industries, Ltd. Compose de 3-aminoazepine et son utilisation pharmaceutique
US5430144A (en) 1993-07-26 1995-07-04 Merck & Co., Inc. Benzo-fused lactams promote release of growth hormone
ES2081747B1 (es) 1993-09-07 1997-01-16 Esteve Labor Dr Amidas derivadas de tienopirroles, su preparacion y su aplicacion como medicamentos.
US5606054A (en) 1993-12-14 1997-02-25 Merck & Co., Inc. Heterocyclic-fused lactams promote release of growth hormone
SK281433B6 (sk) 1994-04-14 2001-03-12 Glaxo Wellcome Inc. 5-heterocyklo-1,5-benzodiazepínové deriváty, spôsob ich výroby, farmaceutický prostriedok s ich obsahom a ich použitie
MX9605128A (es) 1994-05-07 1997-08-30 Boehringer Ingelheim Kg Nuevos derivados de aminoacidos, procedimientos para su preparacion y composiciones farmaceuticas que contienen estos compuestos.
IL114955A (en) 1994-08-17 1999-12-22 Novo Nordisk As N-substituted naphthofused lactams and pharmaceutical compositions containing them
GB9420747D0 (en) 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
GB9420748D0 (en) 1994-10-14 1994-11-30 Glaxo Inc 1,5 benzodiazepine derivatives
GB9420763D0 (en) 1994-10-14 1994-11-30 Glaxo Inc Acetamide derivatives
JPH10509453A (ja) 1994-11-17 1998-09-14 チバ スペシャルティ ケミカルズ ホールディング インコーポレーテッド 架橋可能なモノマーおよび組成物、および架橋されたポリマー
US5587375A (en) 1995-02-17 1996-12-24 Bristol-Myers Squibb Company Azepinone compounds useful in the inhibition of ACE and NEP
ATE235472T1 (de) 1995-06-07 2003-04-15 Merck & Co Inc N-(2-oxo-2,3,4,5-tetrahydro-1h-1,5-benzodiazepi - 3-yl)-3-amide
US5700797A (en) 1995-06-07 1997-12-23 Merck & Co, Inc. N-(2,4-dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3-yl)-3-amides
US5691331A (en) 1995-06-07 1997-11-25 Merck & Co., Inc. N-(2,4-Dioxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-3yl) -3- amides
US5726171A (en) 1995-06-07 1998-03-10 Merck & Co Inc N-(1-alkyl-5-phenyl-2,3,4,5-tetrahydro-1H-benzo B! 1,4!diazepin-3yl)-acetamides
EP0761680A3 (en) 1995-09-12 1999-05-06 Ono Pharmaceutical Co., Ltd. Tetrazole compounds having Interleukin-1beta converting enzyme inhibitory activity
SI0850235T1 (en) 1995-09-15 2000-04-30 Sanofi-Synthelabo Quinolein-2(1h)-one derivatives as serotonin antagonists
WO1997024339A1 (en) 1995-12-27 1997-07-10 Ono Pharmaceutical Co., Ltd. Tetrazole derivatives and drugs containing the same as the active ingredient
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
JPH09295996A (ja) 1996-03-06 1997-11-18 Takeda Chem Ind Ltd システインプロテアーゼ阻害化合物
EP0850222B1 (en) 1996-06-29 2003-05-28 Samjin Pharmaceutical Co., Ltd. Piperazine derivatives and process for the preparation thereof
DE19638020A1 (de) 1996-09-18 1998-03-19 Solvay Pharm Gmbh Die gastrointestinale Durchblutung fördernde Arzneimittel
JP4094066B2 (ja) 1996-12-06 2008-06-04 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 インターロイキン−１β変換酵素のインヒビター
JPH10251295A (ja) 1997-03-07 1998-09-22 Ono Pharmaceut Co Ltd テトラゾール誘導体
WO1999007731A1 (en) 1997-08-11 1999-02-18 Cor Therapeutics, Inc. SELECTIVE FACTOR Xa INHIBITORS
US6211174B1 (en) 1997-10-31 2001-04-03 Merck & Co., Inc. Naphtho-fused lactams promote release of growth hormone
FR2781483A1 (fr) 1998-07-21 2000-01-28 Hoechst Marion Roussel Inc Derives de thioazepinone, procede de preparation et intermediaires de ce procede, application a titre de medicament et compositions pharmaceutiques les renfermant
DE19858253A1 (de) 1998-12-17 2000-06-21 Aventis Pharma Gmbh Verwendung von Inhibitoren des KQt1-Kanals zur Herstellung eines Medikaments zur Behandlung von Krankheiten, die durch Helminthen und Ektoparasiten hervorgerufen werden
JP2000256318A (ja) 1999-03-02 2000-09-19 Toa Eiyo Ltd 縮合複素環誘導体、その製造法およびそれを含有する医薬品
FR2803594B1 (fr) 2000-01-11 2002-07-19 Centre Nat Rech Scient Oligomeres de mimes contraints non peptidiques de dipeptides ou de tripeptides, et leurs utilisations
EP1268434A1 (en) 2000-04-03 2003-01-02 Bristol-Myers Squibb Pharma Company Cyclic lactams as inhibitors of a-beta protein production
MXPA02009755A (es) 2000-04-03 2003-03-27 Bristol Myers Squibb Pharma Co Lactamas ciclicas como inhibidores de la produccion de proteina a-beta.
WO2001079261A1 (en) 2000-04-14 2001-10-25 Corvas International, Inc. Tetrahydro-azepinone derivatives as thrombin inhibitors
ATE472539T1 (de) 2000-04-24 2010-07-15 Vertex Pharma Verfahren und zwischenprodukte zur herstellung von substituierten asparaginsäure-acetalen
GB0012671D0 (en) 2000-05-24 2000-07-19 Merck Sharp & Dohme Therapeutic agents
IL147629A0 (en) 2000-06-01 2002-08-14 Bristol Myers Squibb Pharma Co LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Aβ PROTEIN PRODUCTION
AUPQ969800A0 (en) 2000-08-28 2000-09-21 Fujisawa Pharmaceutical Co., Ltd. Pyrazolopyridine compound and pharmaceutical use thereof
WO2002020500A2 (en) 2000-09-01 2002-03-14 Icos Corporation Materials and methods to potentiate cancer treatment
GB0021831D0 (en) * 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
CA2448737C (en) 2001-07-20 2010-06-01 Boehringer Ingelheim (Canada) Ltd. Viral polymerase inhibitors
EP2335700A1 (en) 2001-07-25 2011-06-22 Boehringer Ingelheim (Canada) Ltd. Hepatitis C virus polymerase inhibitors with a heterobicylic structure
US7294457B2 (en) 2001-08-07 2007-11-13 Boehringer Ingelheim (Canada) Ltd. Direct binding assay for identifying inhibitors of HCV polymerase
WO2003031376A1 (en) 2001-10-12 2003-04-17 Aventis Pharmaceuticals Inc. Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
CA2489560A1 (en) * 2002-06-27 2004-01-08 Schering Aktiengesellschaft Substituted quinoline ccr5 receptor antagonists
US7098235B2 (en) 2002-11-14 2006-08-29 Bristol-Myers Squibb Co. Triglyceride and triglyceride-like prodrugs of glycogen phosphorylase inhibiting compounds
WO2004055008A1 (en) 2002-12-13 2004-07-01 Smithkline Beecham Corporation Compounds, compositions and methods
US7288559B2 (en) 2003-03-14 2007-10-30 Merck + Co, Inc. Carboxamide spirohydantoin CGRP receptor antagonists
ATE410161T1 (de) 2003-05-02 2008-10-15 Elan Pharm Inc 4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazol-3- carbonsäureamid-derivate und verwandte verbindungen als bradykinin b1 rezeptor antagonisten zur behandlung von entzündlichen erkrankungen
JP2005035933A (ja) 2003-07-15 2005-02-10 Takeda Chem Ind Ltd 含窒素縮合複素環化合物の製造方法
AU2004315596B2 (en) 2003-08-29 2011-11-24 President And Fellows Of Harvard College Inhibitors of cellular necrosis
NZ546663A (en) 2003-10-10 2010-01-29 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2005056577A2 (en) 2003-12-05 2005-06-23 The Regents Of The University Of California Peptide inhibitors of hiv
US20070010428A1 (en) 2004-09-03 2007-01-11 Mcmurray John S Inhibitors of signal transduction and activator of transcription 3
US7390798B2 (en) 2004-09-13 2008-06-24 Merck & Co., Inc. Carboxamide spirolactam CGRP receptor antagonists
EP1802637B1 (en) * 2004-10-13 2008-10-15 Merck & Co., Inc. Cgrp receptor antagonists
DE602005027870D1 (de) 2004-10-14 2011-06-16 Merck Sharp & Dohme Cgrp-rezeptorantagonisten
ATE424821T1 (de) 2004-12-02 2009-03-15 Prosidion Ltd Pyrrolopyridin-2-karbonsäureamide
US7875627B2 (en) 2004-12-07 2011-01-25 Abbott Laboratories Thienopyridyl compounds that inhibit vanilloid receptor subtype 1 (VR1) and uses thereof
US20060217362A1 (en) 2004-12-29 2006-09-28 Tung Jay S Novel compounds useful for bradykinin B1 receptor antagonism
WO2006079077A2 (en) 2005-01-20 2006-07-27 Acadia Pharmaceuticals Inc. Use of diltiazem or analogs thereof as modulators of ghrelin receptor
US20060281763A1 (en) 2005-03-25 2006-12-14 Axon Jonathan R Carboxamide inhibitors of TGFbeta
EA200701856A1 (ru) 2005-04-01 2008-02-28 Уорнер-Ламберт Компани Ллс Тетрагидропиридоазепин-8-оны и родственные соединения для лечения шизофрении
WO2006113432A2 (en) 2005-04-14 2006-10-26 Smithkline Beecham Corporation Compounds, compositions and methods
JO2787B1 (en) 2005-04-27 2014-03-15 امجين إنك, Alternative amide derivatives and methods of use
BRPI0616338A2 (pt) 2005-09-23 2011-06-14 Coley Pharm Group Inc mÉtodo para 1h-imidazo[4,5-c] piridinas e anÁlogos da mesma
US20090156578A1 (en) 2005-12-05 2009-06-18 PAULS Henry 3-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents
CA2633500A1 (en) 2005-12-20 2007-07-05 President And Fellows Of Harvard College Compounds, screens, and methods of treatment
GB0605689D0 (en) 2006-03-21 2006-05-03 Novartis Ag Organic compounds
WO2007126871A1 (en) 2006-03-29 2007-11-08 Array Biopharma Inc. P38 inhibitors and methods of use thereof
EP2032539A4 (en) 2006-06-09 2011-03-16 Merck Sharp & Dohme BENZAZEPINONE AS SODIUM CHANNEL BLOCKER
EP2054422B1 (en) 2006-07-20 2017-06-14 Debiopharm International SA Acrylamide derivatives as fab i inhibitors
JP5511379B2 (ja) 2006-07-21 2014-06-04 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 Ｃｇｒｐレセプターアンタゴニスト
US9987277B2 (en) 2006-10-04 2018-06-05 Janssen Sciences Ireland Uc Carboxamide 4-[(4-pyridyl)amino] pryimidines for the treatment of hepatitis C
WO2008045484A1 (en) * 2006-10-10 2008-04-17 Amgen Inc. N-aryl pyrazole compounds for use against diabetes
EP1939187A1 (en) * 2006-12-20 2008-07-02 Sanofi-Aventis Substituted heteroaryl pyridopyrimidone derivatives
US20100210649A1 (en) 2006-12-21 2010-08-19 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
US20100144715A1 (en) 2007-02-28 2010-06-10 Hoyt Scott B Substituted Benzodiazepinones, Benzoxazepinones and Benzothiazepinones as Sodium Channel Blockers
WO2008135525A2 (en) 2007-05-02 2008-11-13 Boehringer Ingelheim International Gmbh Substituted azetidines, manufacturing and use thereof as medicaments
WO2008156580A1 (en) 2007-06-13 2008-12-24 Merck & Co., Inc. Triazole derivatives for treating alzheimer's disease and related conditions
MY148484A (en) 2007-08-03 2013-04-30 Sanofi Aventis Caspase imaging probes
WO2009085256A1 (en) 2007-12-27 2009-07-09 Panacos Pharmaceuticals, Inc. Anti-hiv compounds
EP2090578A1 (en) * 2008-01-29 2009-08-19 Sanofi-Aventis Substituted arylamide diazepinopyrimidone derivatives for the treatment of neurodegenerative diseases caused by abnormal activity of GSK3-beta
EP2085399A1 (en) 2008-01-29 2009-08-05 Sanofi-Aventis substituted arylamide oxazepinopyrimidone derivatives
JP4708443B2 (ja) * 2008-01-31 2011-06-22 トヨタ自動車株式会社 作動制御マップおよび白線認識装置
JP2011512410A (ja) * 2008-02-19 2011-04-21 メルク・シャープ・エンド・ドーム・コーポレイション イミダゾベンゾアゼピンｃｇｒｐ受容体アンタゴニスト
EP2262783A2 (en) 2008-02-21 2010-12-22 Sanofi-Aventis Covalently binding imaging probes
WO2009140549A1 (en) 2008-05-14 2009-11-19 Amgen Inc. Combinations vegf(r) inhibitors and hepatocyte growth factor (c-met) inhibitors for the treatment of cancer
US7884074B2 (en) 2008-05-15 2011-02-08 Ikaria Development Subsidiary Two, LLC Compounds and methods for prevention and/or treatment of inflammation using the same
AU2009277485B2 (en) 2008-07-28 2013-05-02 Eisai R&D Management Co., Ltd. Spiroaminodihydrothiazine derivatives
UY32049A (es) 2008-08-14 2010-03-26 Takeda Pharmaceutical Inhibidores de cmet
DE102008037790A1 (de) 2008-08-14 2010-02-18 Merck Patent Gmbh Bicyclische Triazolderivate
US8088890B2 (en) 2008-09-26 2012-01-03 Fibrex Medical Research & Development Gmbh Peptides and peptidomimetic compounds, the manufacturing thereof as well as their use for preparing a therapeutically and/or preventively active pharmaceutical composition
AU2009303602B2 (en) 2008-10-14 2012-06-14 Sunshine Lake Pharma Co., Ltd. Compounds and methods of use
WO2010077752A1 (en) 2008-12-17 2010-07-08 Merck Sharp & Dohme Corp. Imidazolinone derivatives as cgrp receptor antagonists
CN102548999A (zh) 2009-01-20 2012-07-04 山东轩竹医药科技有限公司 含有取代的含氮稠杂环的头孢菌素衍生物
US8624063B2 (en) 2009-06-30 2014-01-07 Wisconsin Alumni Research Foundation Non-lactone carbocyclic and heterocyclic antagonists and agonists of bacterial quorum sensing
CN102647904A (zh) 2009-09-16 2012-08-22 赛林药物股份有限公司 新型三环蛋白激酶调节剂
WO2011059839A1 (en) 2009-10-29 2011-05-19 Sirtris Pharmaceuticals, Inc. Bicyclic pyridines and analogs as sirtuin modulators
US8481541B2 (en) 2010-03-22 2013-07-09 Hoffmann-La Roche Inc. Pyrrolopyrazine kinase inhibitors
US20130137642A1 (en) 2010-04-23 2013-05-30 Demetrios Vavvas Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells
JPWO2011142381A1 (ja) 2010-05-11 2013-08-29 藤田　岳 ベンゾ若しくはピリドイミダゾール誘導体
KR20130122531A (ko) 2010-05-24 2013-11-07 벤더르빌트 유니버시티 Ｍｇｌｕｒ５ 양성 알로스테릭 조절물로서 치환된 ６­메틸니코틴아미드
WO2012061408A2 (en) 2010-11-02 2012-05-10 Rigel Pharmaceuticals. Inc. Method for making macrocycles
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
UY34171A (es) 2011-07-01 2013-01-31 Gilead Sciences Inc Compuestos heterocíclicos fusionados como moduladores del canal iónico
US9056877B2 (en) 2011-07-19 2015-06-16 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
AR087107A1 (es) 2011-07-27 2014-02-12 Lilly Co Eli Compuesto inhibidor de la señalizacion de la trayectoria notch
WO2013013826A1 (en) 2011-07-27 2013-01-31 Friedrich-Alexander-Universität Erlangen-Nürnberg Necroptosis inhibitors for the treatment of inflammatory diseases of the gastrointestinal tract
EP2773341A2 (en) 2011-10-21 2014-09-10 Massachusetts Eye & Ear Infirmary Compositions comprising necrosis inhibitors, such as necrostatins, alone or in combination, for promoting axon regeneration and nerve function, thereby treating cns disorders
US9062075B2 (en) 2011-12-02 2015-06-23 Aurigene Discovery Technologies Limited Tetrahydropyridine derivatives as FabI inhibitors
SG11201402409UA (en) 2011-12-02 2014-10-30 Aurigene Discovery Tech Ltd Substituted pyridine derivatives as fabi inhibitors
US9217050B2 (en) 2012-04-03 2015-12-22 3M Innovative Properties Company Crosslinkable composition comprising photobase generators
WO2013189241A1 (zh) 2012-06-20 2013-12-27 上海恒瑞医药有限公司 嘧啶二胺类衍生物、其制备方法及其在医药上的应用
TWI520962B (zh) 2012-06-29 2016-02-11 貝達藥業股份有限公司 As the c-Met tyrosine kinase inhibitors novel fused pyridine derivatives
MX2015000362A (es) 2012-07-13 2015-04-14 Hoffmann La Roche Benzo(b)-azepin-2-onas antiproliferativas.
RU2015105561A (ru) 2012-08-09 2016-09-27 Ф. Хоффманн-Ля Рош Аг Замещенные гетероазепиноны
CN103664904A (zh) 2012-09-07 2014-03-26 李振 一种γ-分泌酶抑制剂及其用途
WO2014072930A2 (en) 2012-11-09 2014-05-15 Aurigene Discovery Technologies Limited Fused pyridine derivatives as antibacterial agents
TWI648274B (zh) * 2013-02-15 2019-01-21 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類 （二）
WO2014144547A2 (en) 2013-03-15 2014-09-18 The Regents Of The University Of California Amide derivatives of lactam based n-acylethanolamine acid amidase (naaa) inhibitors
FR3003860B1 (fr) 2013-03-29 2015-11-27 Oreal Composes derives d'iridoides proteges ou non, composition les comprenant, utilisation comme colorant des fibres keratiniques et dispositifs
EP2986317A4 (en) 2013-04-15 2016-10-05 Yeda Res & Dev INHIBITION OF RIP KINASES FOR THE TREATMENT OF LYSOSOMAL STORAGE DISEASES
WO2015027137A1 (en) 2013-08-23 2015-02-26 University Of Tennessee Research Foundation Improved synthesis of capuramycin and its analogues
WO2015103583A1 (en) 2014-01-06 2015-07-09 President And Fellows Of Harvard College Monobactams and methods of their synthesis and use
WO2015104677A1 (en) 2014-01-10 2015-07-16 Piramal Enterprises Limited Heterocyclic compounds as ezh2 inhibitors
EP3148543B1 (en) 2014-05-30 2020-04-08 Icahn School of Medicine at Mount Sinai Small molecule transcription modulators of bromodomains
US9616047B2 (en) 2014-06-30 2017-04-11 Regents Of University Of Minnesota Inhibitors of beta-catenin in treatment of colorectal cancer
EP3180014A1 (en) 2014-08-13 2017-06-21 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Prevention of tumour metastasis by inhibition of necroptosis
RU2017109122A (ru) 2014-08-21 2018-09-21 Глэксосмитклайн Интеллекчуал Проперти Дивелопмент Лимитед Способы лечения с использованием гетероциклических амидов в качестве ингибиторов киназы
CN107108512B (zh) 2014-10-10 2021-05-04 基因泰克公司 治疗性化合物及其用途
EP3017825A1 (en) 2014-11-06 2016-05-11 Ludwig-Maximilians-Universität München An inhibitor of the RIPK1-dependent necrosis pathway and a pharmaceutical composition comprising the same
WO2016101887A1 (en) 2014-12-24 2016-06-30 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
EP3224237B1 (en) 2014-12-24 2024-09-11 National Institute Of Biological Sciences, Beijing Necrosis inhibitors
CN107001337B (zh) 2015-01-13 2021-05-04 诺华股份有限公司 作为血管紧张素ii型拮抗剂的吡咯烷衍生物
EP3256467A1 (en) 2015-02-13 2017-12-20 GlaxoSmithKline Intellectual Property Management Limited Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2,3,4,5-tetrahydrobenzo[b][1,4]oxazepin-3-yl)-4h-1,2,4-triazole-3-carboxamide
TWI609687B (zh) 2015-04-14 2018-01-01 美國禮來大藥廠 平滑肌肉瘤之標靶性治療
RU2716136C2 (ru) * 2015-07-02 2020-03-06 Ф. Хоффманн-Ля Рош Аг Бициклические лактамы и способы их применения
WO2017022962A1 (ko) 2015-07-07 2017-02-09 가톨릭대학교 산학협력단 Ripk 억제제를 유효성분으로 포함하는 면역질환의 예방 또는 치료용 조성물
WO2017069279A1 (ja) 2015-10-23 2017-04-27 武田薬品工業株式会社 複素環化合物
US10961258B2 (en) 2015-12-21 2021-03-30 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
CN107043377A (zh) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种tlr7激动剂的三氟乙酸盐、晶型b及其制备方法、药物组合物和用途
CN107043378A (zh) 2016-02-05 2017-08-15 正大天晴药业集团股份有限公司 一种吡咯并[3,2-d]嘧啶类化合物的制备方法及其中间体
US9815850B2 (en) 2016-02-05 2017-11-14 Denali Therapeutics Inc. Compounds, compositions and methods

Also Published As

Publication number Publication date
EP3414239A2 (en) 2018-12-19
CN109071504A (zh) 2018-12-21
KR20180114910A (ko) 2018-10-19
JP2019508407A (ja) 2019-03-28
CO2018008707A2 (es) 2018-08-31
BR112018015410A2 (pt) 2018-12-18
IL287136A (en) 2021-12-01
US10604535B2 (en) 2020-03-31
MX2021013226A (es) 2022-01-06
CL2018002081A1 (es) 2018-12-14
CN118994190A (zh) 2024-11-22
PE20181665A1 (es) 2018-10-18
NZ784787A (en) 2025-02-28
TW202330479A (zh) 2023-08-01
KR102808827B1 (ko) 2025-05-19
CA3012832A1 (en) 2017-08-10
MX2018009448A (es) 2018-11-21
WO2017136727A2 (en) 2017-08-10
SG11201806302RA (en) 2018-08-30
DOP2018000175A (es) 2018-10-15
IL287136B2 (en) 2023-09-01
US20240150376A1 (en) 2024-05-09
EA201891620A1 (ru) 2019-02-28
US20200317691A1 (en) 2020-10-08
WO2017136727A3 (en) 2017-09-08
CN118994191A (zh) 2024-11-22
SG10201913587WA (en) 2020-02-27
US12358928B2 (en) 2025-07-15
IL260674B (en) 2021-10-31
US20180022759A1 (en) 2018-01-25
ECSP18066138A (es) 2018-09-30
US9896458B2 (en) 2018-02-20
IL287136B1 (en) 2023-05-01
SA518392146B1 (ar) 2023-02-12
US20250388601A1 (en) 2025-12-25
MX2021013228A (es) 2022-01-18
US9815850B2 (en) 2017-11-14
JP2022017447A (ja) 2022-01-25
US20190112318A1 (en) 2019-04-18
US20180099981A1 (en) 2018-04-12
JP6974331B2 (ja) 2021-12-01
JP7381543B2 (ja) 2023-11-15
US20230043400A1 (en) 2023-02-09
MY196648A (en) 2023-04-27
TWI781920B (zh) 2022-11-01
CN109071504B (zh) 2022-03-08
NZ745052A (en) 2025-02-28
CN114437105B (zh) 2024-10-11
TN2018000276A1 (en) 2020-01-16
TWI836679B (zh) 2024-03-21
AU2017213628A1 (en) 2018-08-23
TW201730160A (zh) 2017-09-01
CR20180413A (es) 2018-12-04
AU2017213628B2 (en) 2021-07-29
MA44007A (fr) 2018-12-19
US20170226127A1 (en) 2017-08-10
CN114437105A (zh) 2022-05-06
US10131676B2 (en) 2018-11-20

Similar Documents

Publication Publication Date Title
MX2021013228A (es) Inhibidores de proteina quinasa 1 de interaccion con receptores.
AU2015287674B2 (en) Topical antiviral compositions and methods of using the same
PH12018501151A1 (en) Tank-binding kinase inhibitor compounds
PH12019550235A1 (en) Kinase inhibitors and uses thereof
MX2016015862A (es) Compuestos inhibidores de la cinasa de union a tank.
MX2017003930A (es) Derivados de aminotriazina utiles como compuestos inhibidores de la cinasa de union a tank.
AU2019268062A1 (en) Benzoquinolone inhibitors of VMAT2
SG10201908028SA (en) Cyclopropylamines as lsd1 inhibitors
EP3735976A3 (en) Therapeutic use of mitochondria and combined mitochondrial agents
ZA201605715B (en) Cyclopropylamines as lsd1 inhibitors
MX2016012829A (es) Inhibidores de biaril cinasa.
TWD180147S (zh) 淨水器
AU2015207757A8 (en) N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of SHP2
MX2017008442A (es) Uso de picolinamidas como fungicidas.
MX2016016143A (es) Compuestos de [1,2,4]triazol sustituido.
MX2020006596A (es) Hidroxiisoxazolinas y derivados de estos.
CL2016003074A1 (es) Compuestos derivados de 2-oxi-2-fenil-n-5-pirrolidin-3-ilamino-1,3,4-tiadiazol-2-ilacetamida, inhibidores gls1 composición farmacéutica y su uso para tratar el cáncer.
MA39824A (fr) Composés azole amido-substitués
MX381489B (es) Compuesto biciclico y uso del mismo para la inhibicion de suv39h2.
PH12017500499A1 (en) Synthesis of ent-progesterone and intermediates thereof
PH12022551548A1 (en) Substituted hydroxystilbene compounds and derivatives synthesis and uses thereof
IN2014MU00495A (enExample)
TWD191501S (zh) 淨水器
TWD191502S (zh) 淨水器
JOP20180070B1 (ar) مثبطات إنزيم كيناز بروتين يتفاعل مع مستقبل 1