RU2758686C2 - Антагонисты tlr7/8 и их применение - Google Patents

Антагонисты tlr7/8 и их применение Download PDF

Info

Publication number
RU2758686C2
RU2758686C2 RU2019105719A RU2019105719A RU2758686C2 RU 2758686 C2 RU2758686 C2 RU 2758686C2 RU 2019105719 A RU2019105719 A RU 2019105719A RU 2019105719 A RU2019105719 A RU 2019105719A RU 2758686 C2 RU2758686 C2 RU 2758686C2
Authority
RU
Russia
Prior art keywords
methyl
compound
piperidin
mmol
lcms
Prior art date
Application number
RU2019105719A
Other languages
English (en)
Russian (ru)
Other versions
RU2019105719A (ru
RU2019105719A3 (cg-RX-API-DMAC7.html
Inventor
Брайан А. ШЕРЕР
Сяолин Чэнь
Эстер КЛИРИ
Надия БРУГГЕР
Original Assignee
Мерк Патент Гмбх
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 Мерк Патент Гмбх filed Critical Мерк Патент Гмбх
Publication of RU2019105719A publication Critical patent/RU2019105719A/ru
Publication of RU2019105719A3 publication Critical patent/RU2019105719A3/ru
Application granted granted Critical
Publication of RU2758686C2 publication Critical patent/RU2758686C2/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring 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
    • A61K31/535—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
    • 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
    • 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
    • A61P17/06—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
    • 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
    • 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
    • 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/04—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to the ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D215/18—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • 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
    • C07D471/08—Bridged systems
    • 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
    • C07D471/10—Spiro-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
    • 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
    • C07D487/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Obesity (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
RU2019105719A 2016-08-08 2017-08-07 Антагонисты tlr7/8 и их применение RU2758686C2 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662371917P 2016-08-08 2016-08-08
US62/371,917 2016-08-08
PCT/US2017/045671 WO2018031434A1 (en) 2016-08-08 2017-08-07 Tlr7/8 antagonists and uses thereof

Publications (3)

Publication Number Publication Date
RU2019105719A RU2019105719A (ru) 2020-09-11
RU2019105719A3 RU2019105719A3 (cg-RX-API-DMAC7.html) 2020-10-16
RU2758686C2 true RU2758686C2 (ru) 2021-11-01

Family

ID=59656207

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2019105719A RU2758686C2 (ru) 2016-08-08 2017-08-07 Антагонисты tlr7/8 и их применение

Country Status (13)

Country Link
US (4) US10947214B2 (cg-RX-API-DMAC7.html)
EP (2) EP3497094B1 (cg-RX-API-DMAC7.html)
JP (1) JP7125385B2 (cg-RX-API-DMAC7.html)
KR (2) KR20240019867A (cg-RX-API-DMAC7.html)
CN (1) CN109563075B (cg-RX-API-DMAC7.html)
AU (1) AU2017311047B2 (cg-RX-API-DMAC7.html)
DK (1) DK3497094T3 (cg-RX-API-DMAC7.html)
ES (1) ES2944573T3 (cg-RX-API-DMAC7.html)
IL (1) IL264676B (cg-RX-API-DMAC7.html)
MX (1) MX390698B (cg-RX-API-DMAC7.html)
RU (1) RU2758686C2 (cg-RX-API-DMAC7.html)
SG (1) SG11201900947RA (cg-RX-API-DMAC7.html)
WO (1) WO2018031434A1 (cg-RX-API-DMAC7.html)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS65319B1 (sr) 2015-12-17 2024-04-30 Merck Patent Gmbh 8-cijano-5-piperidino-hinolini kao tlr7/8 antagonisti i njihova upotreba u lečenju imunoloških poremećaja
MX390698B (es) 2016-08-08 2025-03-11 Merck Patent Gmbh Antagonistas del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos.
PE20191353A1 (es) 2016-10-14 2019-10-01 Prec Biosciences Inc Meganucleasas disenadas especificamente para el reconocimiento de secuencias en el genoma del virus de la hepatitis b
WO2018089695A1 (en) * 2016-11-11 2018-05-17 Dynavax Technologies Corporation Toll-like receptor antagonist compounds and methods of use
RU2020123151A (ru) 2017-12-19 2022-01-20 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
AU2018392213B2 (en) 2017-12-20 2021-03-04 Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein
JP7098748B2 (ja) 2017-12-20 2022-07-11 インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． Ｓｔｉｎｇアダプタータンパク質を活性化するホスホン酸結合を有する２’３’環状ジヌクレオチド
JP7328977B2 (ja) 2018-02-12 2023-08-17 エフ． ホフマン－ラ ロシュ アーゲー ウイルス感染の処置および予防のための新規のスルホン化合物および誘導体
TWI818007B (zh) 2018-04-06 2023-10-11 捷克科學院有機化學與生物化學研究所 2'3'-環二核苷酸
TWI833744B (zh) 2018-04-06 2024-03-01 捷克科學院有機化學與生物化學研究所 3'3'-環二核苷酸
US11142750B2 (en) 2018-04-12 2021-10-12 Precision Biosciences, Inc. Optimized engineered meganucleases having specificity for a recognition sequence in the Hepatitis B virus genome
US12157746B2 (en) 2018-06-05 2024-12-03 Hoffmann-La Roche Inc. Tetrahydro-1H-pyrazino[2,1-a]isoindolylquinoline compounds for the treatment of autoimmune disease
EP3807270B1 (en) 2018-06-12 2023-09-13 F. Hoffmann-La Roche AG Novel heteroaryl heterocyclyl compounds for the treatment of autoimmune disease
CN112584903B (zh) * 2018-07-23 2025-12-23 豪夫迈·罗氏有限公司 用于自身免疫性疾病治疗的哌嗪化合物
CN112638908A (zh) 2018-09-04 2021-04-09 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的苯并噻唑类化合物
CN112654620B (zh) 2018-09-06 2023-08-04 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的新型吡唑并吡啶化合物
EP3847170B1 (en) 2018-09-06 2022-06-22 F. Hoffmann-La Roche AG Novel cyclic amidine compounds for the treatment of autoimmune disease
JP7530360B2 (ja) * 2018-11-30 2024-08-07 武田薬品工業株式会社 Ｔｙｋ２阻害剤およびその使用
WO2021084022A1 (en) 2019-10-31 2021-05-06 F. Hoffmann-La Roche Ag Hydropyrazino[1,2-d][1,4]diazepine compounds for the treatment of autoimmune disease
CN114667286A (zh) 2019-11-19 2022-06-24 豪夫迈·罗氏有限公司 用于治疗自身免疫性疾病的三氮杂三环类化合物
EP4061816A1 (en) 2019-11-19 2022-09-28 F. Hoffmann-La Roche AG Hydro-1h-pyrrolo[1,2-a]pyrazine compounds for the treatment of autoimmune disease
WO2021099406A1 (en) 2019-11-20 2021-05-27 F. Hoffmann-La Roche Ag Spiro(isobenzofuranazetidine) compounds for the treatment of autoimmune disease
WO2021110614A1 (en) * 2019-12-03 2021-06-10 F. Hoffmann-La Roche Ag HYDROPYRIDO[1,2-α]PYRAZINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
DK4069729T3 (da) 2019-12-06 2025-04-07 Prec Biosciences Inc Optimerede, modificerede meganukleaser med specificitet for en genkendelsessekvens i hepatitis b-virusgenomet
US20230365542A1 (en) * 2020-09-28 2023-11-16 The Regents Of The University Of California Selective Agonists of 5-HT2A Receptor and Methods of Use
WO2022221642A1 (en) 2021-04-16 2022-10-20 Gilead Sciences, Inc. Thienopyrrole compounds
US12070455B2 (en) 2021-09-10 2024-08-27 Gilead Sciences, Inc. Thienopyrrole compounds
CN115073369A (zh) * 2022-05-31 2022-09-20 汉瑞药业(荆门)有限公司 一种5-溴喹啉-8-甲醛的制备方法

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE812911C (de) * 1945-03-12 1951-09-06 Rhone Poulenc Sa Verfahren zur Herstellung von neuen substituierten Derivaten des Piperidins
CH578535A5 (en) * 1973-05-11 1976-08-13 Ciba Geigy Ag Quinoline-3-carboxylic acid derivs - with e.g. analgesic, antinociceptive, antiinflammatory and antiallergic props
WO2003076427A1 (en) * 2002-03-14 2003-09-18 Pfizer Limited Quinazoline compounds useful in therapy
WO2003105850A1 (en) * 2002-06-18 2003-12-24 Abbott Laboratories 2-aminoquinolines as melanin concentrating hormone receptor antagonists
WO2004043929A1 (en) * 2002-11-12 2004-05-27 Pfizer Products Inc. Quinoline derivatives
EP1726584A1 (en) * 2004-03-15 2006-11-29 Kyowa Hakko Kogyo Co., Ltd. 2-aminoquinazoline derivative
WO2008148468A1 (en) * 2007-06-05 2008-12-11 Sanofi-Aventis Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them
WO2015027222A2 (en) * 2013-08-23 2015-02-26 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2015057655A1 (en) * 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN104945377A (zh) * 2014-03-24 2015-09-30 南京明德新药研发股份有限公司 作为smo抑制剂的喹啉衍生物
WO2016073770A1 (en) * 2014-11-05 2016-05-12 Flexus Biosciences, Inc. Immunoregulatory agents
WO2016087593A1 (en) * 2014-12-05 2016-06-09 Syngenta Participations Ag Novel fungicidal quinolinylamidines

Family Cites Families (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4933447A (en) 1987-09-24 1990-06-12 Ss Pharmaceutical Co., Ltd. Quinoline derivatives
FR2798656B1 (fr) 1999-09-17 2004-12-17 Aventis Pharma Sa Derives de la quinolyl propyl piperidine, leur preparation et les compositions qui les contiennent
US20050026927A1 (en) 2001-11-14 2005-02-03 Henning Boettcher Pyrazole derivatives as psychopharmaceuticals
US7649001B2 (en) 2002-08-12 2010-01-19 Takeda Pharmaceutical Company Limited Fused benzene derivative and use
GB0227240D0 (en) 2002-11-21 2002-12-31 Glaxo Group Ltd Compounds
US20050124625A1 (en) 2003-10-21 2005-06-09 Salvati Mark E. Piperazine derivatives and their use as modulators of nuclear hormone receptor function
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
ZA200610270B (en) 2004-05-17 2008-06-25 Acadia Pharm Inc Androgen receptor modulators and method of treating disease using the same
US20070004679A1 (en) 2004-05-17 2007-01-04 Nathalie Schlienger Androgen receptor modulators and methods of treating disease using the same
WO2006009245A1 (ja) 2004-07-23 2006-01-26 Tanabe Seiyaku Co., Ltd. 含窒素縮合二環式化合物
GB0510810D0 (en) 2005-05-26 2005-06-29 Novartis Ag Organic compounds
GB0526042D0 (en) * 2005-12-21 2006-02-01 Syngenta Participations Ag Chemical compounds
US20090042857A1 (en) 2006-02-20 2009-02-12 Masuo Yamaoka Novel Pharmaceutical
EP1903038A1 (de) 2006-09-07 2008-03-26 Bayer Schering Pharma Aktiengesellschaft N-(1-Hetaryl-piperidin-4-yl)-(het)arylamide als EP2-Rezeptor Modulatoren
EP2094686A1 (en) * 2006-09-26 2009-09-02 Glaxo Group Limited 5-{2-[4-(2-methyl-5-quinolinyl)-l-piperidinyl]ethyl} quinolinone derivatives as 5ht1a receptor modulators for treating sexual dysfunction, cognition impairement, psychotic disorders, anxiety, depression, etc.
CL2008001002A1 (es) 2007-04-11 2008-10-17 Actelion Pharmaceuticals Ltd Compuestos derivados de oxazolidinona; composicion farmaceutica que comprende a dichos compuestos; y su uso para preparar un medicamento para tratar una infeccion bacteriana.
EP2285217A4 (en) 2008-05-12 2011-06-08 Amnestix Inc CONNECTIONS TO IMPROVE LEARNING AND MEMORY
EP2320895A2 (en) 2008-07-03 2011-05-18 Exelixis, Inc. Cdk modulators
CA2735779A1 (en) 2008-09-02 2010-03-11 Matthew Burger Bicyclic kinase inhibitors
AU2009321867B2 (en) 2008-12-01 2015-12-10 Merck Patent Gmbh 2,5-Diamino-substituted pyrido[4,3-d]pyrimidines as autotaxin inhibitors against cancer
EP2396328A2 (en) 2009-02-11 2011-12-21 The Regents of The University of California Toll-like receptor modulators and treatment of diseases
ES2432070T3 (es) 2009-02-24 2013-11-29 Respiratorius Ab Diazaheteroarilos broncodilatadores novedosos
US20110015219A1 (en) 2009-07-16 2011-01-20 Mallinckrodt Inc. (+)-Morphinans as Antagonists of Toll-Like Receptor 9 and Therapeutic Uses Thereof
US20120214803A1 (en) 2011-02-18 2012-08-23 Vifor (International) Ag Novel Sulfonaminoquinoline Hepcidin Antagonists
JP2013075834A (ja) * 2011-09-29 2013-04-25 Kowa Co Ｔｌｒ９阻害活性を有するピラゾロピリミジン−７−アミン誘導体
WO2013060881A1 (en) 2011-10-27 2013-05-02 Vereniging Voor Christelijk Hoger Onderwijs, Wetenschappelijk Onderzoek En Patientenzorg Pyridopyrimidines and their therapeutic use
WO2014086453A1 (en) 2012-12-07 2014-06-12 Merck Patent Gmbh Azaheterobicyclic compounds
AU2014302365B2 (en) 2013-06-26 2018-11-15 Abbvie Inc. Primary carboxamides as BTK inhibitors
EP3626717A1 (en) * 2013-10-14 2020-03-25 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN104557913B (zh) 2013-10-28 2017-02-08 上海汇伦生命科技有限公司 吡啶并嘧啶类化合物，其制备方法和用途
CA2933466A1 (en) 2013-12-13 2015-06-18 Takeda Pharmaceutical Company Limited Pyrrolo[3,2-c]pyridine derivatives as tlr inhibitors
JP6487921B2 (ja) 2013-12-17 2019-03-20 ファイザー・インク ＬＲＲＫ２阻害薬としての新規の３，４−二置換−１Ｈ−ピロロ［２，３−ｂ］ピリジンおよび４，５−二置換−７Ｈ−ピロロ［２，３−ｃ］ピリダジン
CN106536523A (zh) 2014-02-05 2017-03-22 斯特里奥肯公司 西他列汀的权宜合成
AU2015237050B2 (en) 2014-03-24 2019-05-09 Guangdong Zhongsheng Pharmaceutical Co., Ltd Quinoline derivatives as SMO inhibitors
CA2938280C (en) 2014-04-22 2022-07-12 F. Hoffmann-La Roche Ag 4-amino-imidazoquinoline compounds
GB201411236D0 (en) 2014-06-25 2014-08-06 Takeda Pharmaceutical Novel compounds
US10590086B2 (en) 2014-11-03 2020-03-17 Iomet Pharma Ltd. Pharmaceutical compound
US10584125B2 (en) * 2014-11-13 2020-03-10 Glaxosmithkline Biologicals Sa Adenine derivatives which are useful in the treatment of allergic diseases or other inflammatory conditions
MA41169A (fr) 2014-12-17 2017-10-24 Acraf Composés antibactériens à large spectre d'activité
CN108290855A (zh) 2015-07-01 2018-07-17 西北大学 被取代的喹唑啉化合物及其调节葡糖脑苷脂酶活性的用途
WO2017031427A1 (en) 2015-08-19 2017-02-23 3-V Biosciences, Inc. COMPOUNDS AND METHODS FOR INHIBITING mTOR
RS65319B1 (sr) 2015-12-17 2024-04-30 Merck Patent Gmbh 8-cijano-5-piperidino-hinolini kao tlr7/8 antagonisti i njihova upotreba u lečenju imunoloških poremećaja
WO2017147328A1 (en) * 2016-02-23 2017-08-31 Portola Pharmaceuticals, Inc. Compounds for binding proprotein convertase subtilisin/kexin type 9 (pcsk9)
MX390698B (es) 2016-08-08 2025-03-11 Merck Patent Gmbh Antagonistas del receptor 7/8 tipo toll (tlr7/8) y uso de los mismos.
ES2959782T3 (es) * 2016-12-20 2024-02-28 Fmc Corp Oxadiazoles fungicidas
US11050028B2 (en) * 2017-01-24 2021-06-29 Universal Display Corporation Organic electroluminescent materials and devices
EP3655401B1 (en) 2017-07-18 2023-09-06 Merck Patent GmbH Tlr7/8 antagonists and uses thereof
RU2020123151A (ru) 2017-12-19 2022-01-20 Мерк Патент Гмбх Антагонисты tlr7/8 и их применение
US20210300940A1 (en) 2018-07-31 2021-09-30 Merck Patent Gmbh Tlr7/8 antagonists and uses thereof

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE812911C (de) * 1945-03-12 1951-09-06 Rhone Poulenc Sa Verfahren zur Herstellung von neuen substituierten Derivaten des Piperidins
CH578535A5 (en) * 1973-05-11 1976-08-13 Ciba Geigy Ag Quinoline-3-carboxylic acid derivs - with e.g. analgesic, antinociceptive, antiinflammatory and antiallergic props
WO2003076427A1 (en) * 2002-03-14 2003-09-18 Pfizer Limited Quinazoline compounds useful in therapy
WO2003105850A1 (en) * 2002-06-18 2003-12-24 Abbott Laboratories 2-aminoquinolines as melanin concentrating hormone receptor antagonists
WO2004043929A1 (en) * 2002-11-12 2004-05-27 Pfizer Products Inc. Quinoline derivatives
EP1726584A1 (en) * 2004-03-15 2006-11-29 Kyowa Hakko Kogyo Co., Ltd. 2-aminoquinazoline derivative
WO2008148468A1 (en) * 2007-06-05 2008-12-11 Sanofi-Aventis Di(hetero)arylcyclohexane derivatives, their preparation, their use and pharmaceutical compositions comprising them
WO2015027222A2 (en) * 2013-08-23 2015-02-26 Neupharma, Inc. Certain chemical entities, compositions, and methods
WO2015057655A1 (en) * 2013-10-14 2015-04-23 Eisai R&D Management Co., Ltd. Selectively substituted quinoline compounds
CN104945377A (zh) * 2014-03-24 2015-09-30 南京明德新药研发股份有限公司 作为smo抑制剂的喹啉衍生物
WO2016073770A1 (en) * 2014-11-05 2016-05-12 Flexus Biosciences, Inc. Immunoregulatory agents
WO2016087593A1 (en) * 2014-12-05 2016-06-09 Syngenta Participations Ag Novel fungicidal quinolinylamidines

Non-Patent Citations (8)

* Cited by examiner, † Cited by third party
Title
Amit Nayyar et al. "3D-QSAR study of ring-substituted quinoline class of anti-tuberculosis agents", Bioorganic & Medicinal Chemistry, 2006, Vol. 14, No. 3, P. 847-856. *
Andrey R. Antonchick et al. "Direct Selective Oxidative Cross-Coupling of Simple Alkanes with Heteroarenes", Angewandte Chemie International Edition, 2013, Vol.52, No. 11, P. 1-6. *
Ryoichi Kuwano et al. "Catalytic Asymmetric Hydrogenation of Quinoline Carbocycles: Unusual Chemoselectivity in the Hydrogenation of Quinolines", Royal Society of Chemistry, 2015, Vol. 51, No. 35, P. 1-4. *
Ryoichi Kuwano et al. "Catalytic Asymmetric Hydrogenation of Quinoline Carbocycles: Unusual Chemoselectivity in the Hydrogenation of Quinolines", Royal Society of Chemistry, 2015, Vol. 51, No. 35, P. 1-4. Verma Rahul et al. "Bacterial DNA Gyrase is not the target of quinolone-based anti-tuberculosis compounds", International Search Journal of Pharmacy, 2013, Vol. 4, No. 1, P. 284-292. Andrey R. Antonchick et al. "Direct Selective Oxidative Cross-Coupling of Simple Alkanes with Heteroarenes", Angewandte Chemie International Edition, 2013, Vol.52, No. 11, P. 1-6. Amit Nayyar et al. "3D-QSAR study of ring-substituted quinoline class of anti-tuberculosis agents", Bioorganic & Medicinal Chemistry, 2006, Vol. 14, No. 3, P. 847-856. Vikramdeep Monga et al. "Ring-substituted quinolines. Part 2: Synthesis and antimycobacterial activities of ring-substituted quinolinecarbohydrazide and ring-substituted quinolinecarboxamide analogues", Bioorganic & Medicinal Chemistry, 2004, Vol. 12, No. 24, P. 6 *
Verma Rahul et al. "Bacterial DNA Gyrase is not the target of quinolone-based anti-tuberculosis compounds", International Search Journal of Pharmacy, 2013, Vol. 4, No. 1, P. 284-292. *
Vikramdeep Monga et al. "Ring-substituted quinolines. Part 2: Synthesis and antimycobacterial activities of ring-substituted quinolinecarbohydrazide and ring-substituted quinolinecarboxamide analogues", Bioorganic & Medicinal Chemistry, 2004, Vol. 12, No. 24, P. 6465-6472. *
В.Г. Беликов "Фармацевтическая химия". Глава 2.6 "Связь между химической структурой, свойствами веществ и их действием на организм". - М.: МЕДпресс-информ, 2007, с. 27-29. *
Щебляков Д. В. и др. "Толл-подобные рецепторы (TLR) и их значение в опухолевой прогрессии", ACTA NATURAE, 2010, Т. 2, No. 3, C. 28-37. *

Also Published As

Publication number Publication date
CA3033240A1 (en) 2018-02-15
EP3497094A1 (en) 2019-06-19
US20240383876A1 (en) 2024-11-21
ES2944573T3 (es) 2023-06-22
US10947214B2 (en) 2021-03-16
AU2017311047A1 (en) 2019-03-21
US20180037570A1 (en) 2018-02-08
MX2019001096A (es) 2019-07-04
US20210002256A1 (en) 2021-01-07
NZ750485A (en) 2025-03-28
BR112019000696A2 (pt) 2019-04-24
WO2018031434A1 (en) 2018-02-15
IL264676B (en) 2022-04-01
AU2017311047B2 (en) 2021-07-22
SG11201900947RA (en) 2019-02-27
US20210002255A1 (en) 2021-01-07
RU2019105719A (ru) 2020-09-11
US11512069B2 (en) 2022-11-29
RU2019105719A3 (cg-RX-API-DMAC7.html) 2020-10-16
KR20240019867A (ko) 2024-02-14
DK3497094T3 (da) 2023-05-15
EP4198031A1 (en) 2023-06-21
CN109563075A (zh) 2019-04-02
JP2019527718A (ja) 2019-10-03
JP7125385B2 (ja) 2022-08-24
KR20190038616A (ko) 2019-04-08
CN109563075B (zh) 2022-09-30
KR102635885B1 (ko) 2024-02-14
MX390698B (es) 2025-03-11
EP3497094B1 (en) 2023-02-15

Similar Documents

Publication Publication Date Title
RU2758686C2 (ru) Антагонисты tlr7/8 и их применение
JP7754865B2 (ja) Ｔｌｒ７／８アンタゴニストおよびそれらの使用
AU2021218041B2 (en) Polycyclic TLR7/8 antagonists and use thereof in the treatment of immune disorders
CA3033240C (en) Tlr7/8 antagonists and uses thereof
BR112019000696B1 (pt) Antagonistas de tlr7/8, seu uso, composição farmacêutica, e kit