EA032061B1 - Агонисты соматостатиновых рецепторов подтипа 4 (sstr4) - Google Patents

Агонисты соматостатиновых рецепторов подтипа 4 (sstr4) Download PDF

Info

Publication number
EA032061B1
EA032061B1 EA201501122A EA201501122A EA032061B1 EA 032061 B1 EA032061 B1 EA 032061B1 EA 201501122 A EA201501122 A EA 201501122A EA 201501122 A EA201501122 A EA 201501122A EA 032061 B1 EA032061 B1 EA 032061B1
Authority
EA
Eurasian Patent Office
Prior art keywords
mmol
compound
pain
group
alkyl
Prior art date
Application number
EA201501122A
Other languages
English (en)
Russian (ru)
Other versions
EA201501122A8 (ru
EA201501122A1 (ru
Inventor
Риккардо Джованнини
Юньхай Куй
Хенри Додс
Марко Феррара
Штефан Йюст
Раймунд Кюльцер
Айан Лингард
Рокко Маццаферро
Клаус Рудольф
Original Assignee
Сентрекшн Терапьютикс Корпорейшн
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 Сентрекшн Терапьютикс Корпорейшн filed Critical Сентрекшн Терапьютикс Корпорейшн
Publication of EA201501122A1 publication Critical patent/EA201501122A1/ru
Publication of EA201501122A8 publication Critical patent/EA201501122A8/ru
Publication of EA032061B1 publication Critical patent/EA032061B1/ru

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
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • A61K31/423—Oxazoles condensed with carbocyclic 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/429—Thiazoles condensed with heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—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
    • A61K31/435—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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/52—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring condensed with a ring other than six-membered
    • 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
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing 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
    • C07D413/12—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Peptides Or Proteins (AREA)
EA201501122A 2013-05-17 2014-05-15 Агонисты соматостатиновых рецепторов подтипа 4 (sstr4) EA032061B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13168224 2013-05-17
PCT/EP2014/059905 WO2014184275A1 (en) 2013-05-17 2014-05-15 New somatostatin receptor subtype 4 (sstr4) agonists

Publications (3)

Publication Number Publication Date
EA201501122A1 EA201501122A1 (ru) 2017-01-30
EA201501122A8 EA201501122A8 (ru) 2018-10-31
EA032061B1 true EA032061B1 (ru) 2019-04-30

Family

ID=48428384

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201501122A EA032061B1 (ru) 2013-05-17 2014-05-15 Агонисты соматостатиновых рецепторов подтипа 4 (sstr4)

Country Status (25)

Country Link
US (4) US9371282B2 (enExample)
EP (1) EP2997021B1 (enExample)
JP (1) JP6387086B2 (enExample)
KR (1) KR102286196B1 (enExample)
CN (1) CN105473574B (enExample)
AR (1) AR096339A1 (enExample)
AU (1) AU2014267328B2 (enExample)
BR (1) BR112015028452B1 (enExample)
CA (1) CA2912486C (enExample)
CL (1) CL2015003290A1 (enExample)
DK (1) DK2997021T3 (enExample)
EA (1) EA032061B1 (enExample)
ES (1) ES2658076T3 (enExample)
IL (1) IL242313B (enExample)
JO (1) JO3475B1 (enExample)
MX (1) MX369358B (enExample)
NO (1) NO2997021T3 (enExample)
PH (1) PH12015502524B1 (enExample)
PL (1) PL2997021T3 (enExample)
PT (1) PT2997021T (enExample)
TW (1) TWI636042B (enExample)
UA (1) UA116247C2 (enExample)
UY (1) UY35572A (enExample)
WO (1) WO2014184275A1 (enExample)
ZA (1) ZA201507958B (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA117830C2 (uk) 2013-05-17 2018-10-10 Інсайт Корпорейшн Похідні біпіразолу як інгібітори jak
US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists
JP2017526728A (ja) 2014-09-15 2017-09-14 インフラマトリー・レスポンス・リサーチ・インコーポレイテッド 炎症介在性状態の治療におけるレボセチリジン及びモンテルカスト
WO2016075239A1 (en) * 2014-11-14 2016-05-19 Boehringer Ingelheim International Gmbh Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (sstr4) agonists
EP3397631B1 (en) 2015-12-29 2021-04-07 Pfizer Inc Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
US11136312B2 (en) 2017-05-12 2021-10-05 Board of Trustees of the Southern Illinois University 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
US11912687B2 (en) 2017-05-12 2024-02-27 Board of Trustees of the Southern Illinois University 3,4,5-trisubstituted-1,2,4-triazoles and 3,4,5-trisubstituted-3-thio-1,2,4-triazoles and uses thereof
US10865163B2 (en) 2017-12-20 2020-12-15 The University Of Toledo Carbon dioxide as a directing group for C—H functionalization reactions involving Lewis basic amines, alcohols, thiols, and phosphines for the synthesis of compounds
BR122023022189A2 (pt) 2018-02-16 2024-02-20 Incyte Corporation Usos de inibidores da via de jak1 para o tratamento de distúrbios relacionados a citocinas
TWI834637B (zh) 2018-03-01 2024-03-11 日商武田藥品工業有限公司 六氫吡啶基-3-(芳氧基)丙醯胺及丙酸酯
CN112423759A (zh) 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
US11668295B2 (en) 2018-12-28 2023-06-06 Avent, Inc. Pump head for a peristaltic pump
CN112979655A (zh) 2019-12-16 2021-06-18 上海赛默罗生物科技有限公司 三唑并哒嗪类衍生物、其制备方法、药物组合物和用途
AR121682A1 (es) * 2020-03-31 2022-06-29 Takeda Pharmaceuticals Co Derivados de n-(heterociclil y heterociclilalquil)-3-bencilpiridin-2-amina como agonistas de sstr4
WO2021236518A1 (en) * 2020-05-19 2021-11-25 IRR, Inc. Levocetirizine and montelukast in the treatment of sepsis and symptoms thereof
WO2021233428A1 (zh) * 2020-05-21 2021-11-25 广州费米子科技有限责任公司 含氮饱和杂环化合物及其制备方法、药物组合物和应用
KR20230015333A (ko) * 2020-05-21 2023-01-31 광저우 페르미온 테크놀로지 씨오., 엘티디. 융합된 고리 화합물, 이의 제조 방법, 이의 약제학적 조성물 및 용도
IL298118B1 (en) 2020-06-02 2025-10-01 Incyte Corp Processes for preparing JAK1 inhibitor
WO2022012534A1 (zh) * 2020-07-13 2022-01-20 广州费米子科技有限责任公司 含氮杂环化合物、药物组合物和应用
JP2023537670A (ja) 2020-07-28 2023-09-05 シージェン インコーポレイテッド ポリペプチドを生産するための方法及びシステム
WO2022125670A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
DK4333840T3 (da) 2021-05-03 2025-11-24 Incyte Corp Jak1-vejinhibitorer til behandling af prurigo nodularis
AR127055A1 (es) * 2021-09-14 2023-12-13 Lilly Co Eli Sales agonistas de sstr4
CN120897906A (zh) 2023-03-10 2025-11-04 伊莱利利公司 制备sstr4激动剂及其盐的方法
AU2024236692A1 (en) * 2023-03-10 2025-10-16 Eli Lilly And Company Methods for the preparation and dose regimens for use of sstr4 agonists and salts thereof
CN119039274A (zh) * 2023-05-29 2024-11-29 武汉熙瑞医药科技有限公司 3-氮杂-双环[3.1.0]己烷衍生物、其制备方法及其应用
WO2025027049A1 (en) * 2023-08-02 2025-02-06 Boehringer Ingelheim International Gmbh (2s,5r)-5-(hydroxymethyl)morpholine-2-carboxamides as agonists of sstr4
WO2025096300A1 (en) 2023-10-30 2025-05-08 Eli Lilly And Company Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivatives
WO2025193591A1 (en) 2024-03-11 2025-09-18 Eli Lilly And Company Crystalline form of a tartrate salt of an sstr4 agonist
WO2025247982A1 (en) 2024-05-29 2025-12-04 Grünenthal GmbH Piperazines which act as sstr4 modulators

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010059922A1 (en) * 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
WO2012125661A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Substituted 3-azabicyclo[3.1.0]hexane derivatives useful as ccr2 antagonists

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6159941A (en) 1996-05-14 2000-12-12 Novo Nordisk A/S Use of somatostatin agonists and antagonists for treating diseases related to the eye
US6355613B1 (en) 1996-07-31 2002-03-12 Peptor Limited Conformationally constrained backbone cyclized somatostatin analogs
US6057338A (en) 1997-04-04 2000-05-02 Merck & Co., Inc. Somatostatin agonists
US6063796A (en) 1997-04-04 2000-05-16 Merck & Co., Inc. Somatostatin agonists
US20100004339A1 (en) 2003-10-06 2010-01-07 Oy Juvantia Pharma Ltd. Somatostatin Receptor 1 and/or 4 Selective Agonists and Antagonists
FI20031454A0 (fi) 2003-10-06 2003-10-06 Juvantia Pharma Ltd Oy Selektiivisiä somatostatiinireseptori 1 ja/tai 4 -agonisteja ja -antagonisteja
CA2542279C (en) * 2003-10-14 2011-08-09 Pfizer Products Inc. Bicyclic [3.1.0] derivatives as glycine transporter inhibitors
CA2672373C (en) 2006-12-19 2011-08-30 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
US8835472B2 (en) 2010-09-02 2014-09-16 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical compositions and uses thereof
CN102675290B (zh) * 2011-03-18 2014-11-12 山东亨利医药科技有限责任公司 含有并环的二氢吡唑类化合物
KR101556318B1 (ko) * 2013-05-15 2015-10-01 한국과학기술연구원 칼슘이온 채널 조절제로서 유효한 6-피라졸일아미도-3-치환된 아자바이사이클로[3.1.0]헥산 유도체
US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010059922A1 (en) * 2008-11-21 2010-05-27 Ligand Pharmaceuticals Incorporated Pyrrolidine carboxamide compounds
WO2012125661A1 (en) * 2011-03-17 2012-09-20 Merck Sharp & Dohme Corp. Substituted 3-azabicyclo[3.1.0]hexane derivatives useful as ccr2 antagonists

Also Published As

Publication number Publication date
IL242313B (en) 2018-06-28
WO2014184275A1 (en) 2014-11-20
EA201501122A8 (ru) 2018-10-31
NO2997021T3 (enExample) 2018-05-19
US9371282B2 (en) 2016-06-21
JO3475B1 (ar) 2020-07-05
PT2997021T (pt) 2018-02-23
ZA201507958B (en) 2024-11-27
EP2997021B1 (en) 2017-12-20
US20180092880A1 (en) 2018-04-05
CA2912486C (en) 2023-08-22
MX2015015620A (es) 2016-03-07
HK1222850A1 (en) 2017-07-14
US20140343065A1 (en) 2014-11-20
KR20160013081A (ko) 2016-02-03
KR102286196B1 (ko) 2021-08-06
US9789082B2 (en) 2017-10-17
JP2016518430A (ja) 2016-06-23
US20170014381A1 (en) 2017-01-19
DK2997021T3 (en) 2018-02-12
MX369358B (es) 2019-11-06
TW201536741A (zh) 2015-10-01
NZ713665A (en) 2021-01-29
AR096339A1 (es) 2015-12-23
ES2658076T3 (es) 2018-03-08
PL2997021T3 (pl) 2018-05-30
CA2912486A1 (en) 2014-11-20
EP2997021A1 (en) 2016-03-23
US10166214B2 (en) 2019-01-01
BR112015028452B1 (pt) 2023-04-11
JP6387086B2 (ja) 2018-09-05
UA116247C2 (uk) 2018-02-26
US20190269650A1 (en) 2019-09-05
AU2014267328A1 (en) 2015-11-12
AU2014267328B2 (en) 2018-07-26
CN105473574A (zh) 2016-04-06
PH12015502524B1 (en) 2019-11-13
TWI636042B (zh) 2018-09-21
US10675268B2 (en) 2020-06-09
BR112015028452A2 (pt) 2017-07-25
PH12015502524A1 (en) 2016-02-29
EA201501122A1 (ru) 2017-01-30
CL2015003290A1 (es) 2016-06-17
UY35572A (es) 2014-11-28
CN105473574B (zh) 2018-02-13

Similar Documents

Publication Publication Date Title
EA032061B1 (ru) Агонисты соматостатиновых рецепторов подтипа 4 (sstr4)
AU2025204346A1 (en) Heterocyclic GLP-1 agonists
CN107406412B (zh) TGF-β抑制剂
CN106715415B (zh) 3-氨基-1,5,6,7-四氢-4h-吲哚-4-酮
JP6641367B2 (ja) ソマトスタチン受容体サブタイプ４（ｓｓｔｒ４）アゴニストとしてのモルホリンおよび１，４−オキサゼパンアミド
JP6458028B2 (ja) インドール及びピロールの新規な誘導体、その製造方法及びそれを含む医薬組成物
TW201130816A (en) New CCR2 receptor antagonists and uses thereof
JP2018527337A (ja) 二環式縮合ヘテロアリールまたはアリール化合物
EA032361B1 (ru) Трициклические соединения
WO2016044323A1 (en) Pyrrolopyrimidine derivatives as nr2b nmda receptor antagonists
JP6590927B2 (ja) ソマトスタチン受容体サブタイプ４（ｓｓｔｒ４）作動薬としてのアリール及びヘテロアリール縮合テトラヒドロ−１，４−オキサゼピンアミド
CN109689656B (zh) 7-取代的1-芳基二氮杂萘-3-羧酰胺及其用途
NZ713665B2 (en) New somatostatin receptor subtype 4 (sstr4) agonists
HK1222850B (en) New somatostatin receptor subtype 4 (sstr4) agonists
NZ717556B2 (en) Spirocyclic compounds as tryptophan hydroxylase inhibitors