UA118549C2 - 2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену - Google Patents

2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену

Info

Publication number
UA118549C2
UA118549C2 UAA201507943A UAA201507943A UA118549C2 UA 118549 C2 UA118549 C2 UA 118549C2 UA A201507943 A UAA201507943 A UA A201507943A UA A201507943 A UAA201507943 A UA A201507943A UA 118549 C2 UA118549 C2 UA 118549C2
Authority
UA
Ukraine
Prior art keywords
4аlkуl
disubstituted
acyl
amino
bromodomain inhibitors
Prior art date
Application number
UAA201507943A
Other languages
English (en)
Inventor
Домінік Ейманз
Стівен Джон Еткінсон
Лі Ендрю Гаррісон
Дейвід Джонатан Герст
Роберт Пітер Ло
Меттью Ліндон
Елікзендер Престон
Джонатан Томас Сіл
Крістофер Роланд Веллавей
Original Assignee
Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50390051&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UA118549(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед filed Critical Ґлаксосмітклайн Інтеллекчуал Проперті (№ 2) Лімітед
Publication of UA118549C2 publication Critical patent/UA118549C2/uk

Links

Classifications

    • 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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4706—4-Aminoquinolines; 8-Aminoquinolines, e.g. chloroquine, primaquine
    • 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
    • A61K31/4965—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
    • A61K31/535—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
    • 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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • 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
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/44—Nitrogen atoms attached in position 4 with aryl radicals attached to said nitrogen 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
    • C07D215/38—Nitrogen atoms
    • C07D215/42—Nitrogen atoms attached in position 4
    • C07D215/46—Nitrogen atoms attached in position 4 with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen 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
    • C07D215/48—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
    • 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
    • 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
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D405/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/02—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
    • 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
    • C07D417/14—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 three or more hetero rings
    • 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
    • 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
    • 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
    • C07D498/02—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
    • C07D498/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Quinoline Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pyridine Compounds (AREA)

Abstract

Винахід стосується нових сполук, таких як (2S,3R,4R)-1-ацетил-2-циклопропіл-3-метил-4-((4-метилпіримідин-2-іл)аміно)-1,2,3,4-тетрагідрохінолін-6-карбоксамід, що має структурну формулу (І): , фармацевтичних композицій, які містять такі сполуки, та їх застосування в лікуванні гострого або хронічного аутоімунного та/або запального стану.
UAA201507943A 2013-03-14 2014-03-12 2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену UA118549C2 (uk)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361781583P 2013-03-14 2013-03-14
US201361882798P 2013-09-26 2013-09-26
PCT/EP2014/054795 WO2014140076A1 (en) 2013-03-14 2014-03-12 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors

Publications (1)

Publication Number Publication Date
UA118549C2 true UA118549C2 (uk) 2019-02-11

Family

ID=50390051

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201507943A UA118549C2 (uk) 2013-03-14 2014-03-12 2,3-дизаміщені похідні 1-ацил-4-аміно-1,2,3,4-тетрагідрохіноліну та їх застосування як інгібіторів бромодомену

Country Status (32)

Country Link
US (5) US9637456B2 (uk)
EP (2) EP2970127B1 (uk)
JP (2) JP6093046B2 (uk)
KR (1) KR101780784B1 (uk)
CN (1) CN105189461B (uk)
AU (1) AU2014230815B2 (uk)
CA (1) CA2901537C (uk)
CL (1) CL2015002658A1 (uk)
CR (1) CR20150489A (uk)
CY (1) CY1121095T1 (uk)
DK (1) DK2970127T3 (uk)
DO (1) DOP2015000239A (uk)
EA (1) EA028174B1 (uk)
ES (2) ES2704048T3 (uk)
HR (1) HRP20182179T1 (uk)
HU (1) HUE043568T2 (uk)
IL (2) IL240463B (uk)
LT (1) LT2970127T (uk)
MX (1) MX369324B (uk)
MY (1) MY187479A (uk)
NZ (1) NZ710765A (uk)
PE (1) PE20151596A1 (uk)
PH (1) PH12015502038B1 (uk)
PL (1) PL2970127T3 (uk)
PT (1) PT2970127T (uk)
RS (1) RS58264B1 (uk)
SG (1) SG11201506245QA (uk)
SI (1) SI2970127T1 (uk)
SM (1) SMT201900009T1 (uk)
UA (1) UA118549C2 (uk)
WO (1) WO2014140076A1 (uk)
ZA (1) ZA201505877B (uk)

Families Citing this family (53)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9073878B2 (en) 2012-11-21 2015-07-07 Zenith Epigenetics Corp. Cyclic amines as bromodomain inhibitors
WO2014080291A2 (en) 2012-11-21 2014-05-30 Rvx Therapeutics Inc. Biaryl derivatives as bromodomain inhibitors
US9271978B2 (en) 2012-12-21 2016-03-01 Zenith Epigenetics Corp. Heterocyclic compounds as bromodomain inhibitors
EP2970271B1 (en) 2013-03-14 2017-11-08 Janssen Pharmaceutica NV P2x7 modulators
ES2704048T3 (es) * 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio
TWI627174B (zh) 2013-03-14 2018-06-21 比利時商健生藥品公司 P2x7調控劑
US9040534B2 (en) 2013-03-14 2015-05-26 Janssen Pharmaceutica Nv [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
TWI599567B (zh) 2013-03-14 2017-09-21 健生藥品公司 P2x7調節劑
US9227985B2 (en) 2013-03-15 2016-01-05 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
SG11201510409QA (en) 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
EP3019502B1 (en) 2013-07-08 2017-05-17 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors
AU2014298051B2 (en) 2013-07-31 2018-11-15 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
US9399640B2 (en) 2013-11-26 2016-07-26 Incyte Corporation Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors
WO2015081189A1 (en) 2013-11-26 2015-06-04 Incyte Corporation Bicyclic heterocycles as bet protein inhibitors
US9309246B2 (en) 2013-12-19 2016-04-12 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
MY180775A (en) 2014-04-23 2020-12-09 Incyte Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
WO2016039977A1 (en) 2014-09-12 2016-03-17 Janssen Pharmaceutica Nv P2x7 modulators
JP6625616B2 (ja) 2014-09-12 2019-12-25 ヤンセン ファーマシューティカ エヌ.ベー. P2x7調節n−アシル−トリアゾロピラジン
TR201820050T4 (tr) * 2014-09-12 2019-01-21 Glaxosmithkline Ip No 2 Ltd Bromodomain inhibitörleri olarak tetrahidrokinolin türevleri.
US9527864B2 (en) 2014-09-15 2016-12-27 Incyte Corporation Tricyclic heterocycles as BET protein inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
WO2016087942A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridines as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
GB201504694D0 (en) 2015-03-19 2015-05-06 Glaxosmithkline Ip Dev Ltd Covalent conjugates
WO2017040963A1 (en) 2015-09-03 2017-03-09 Forma Therapeutics, Inc. [6,6] fused bicyclic hdac8 inhibitors
CA2998545A1 (en) 2015-09-22 2017-03-30 Glaxosmithkline Intellectual Property (No.2) Limited Pyridinone dicarboxamide for use as bromodomain inhibitors
WO2017075377A1 (en) 2015-10-29 2017-05-04 Incyte Corporation Amorphous solid form of a bet protein inhibitor
US10654818B2 (en) 2015-12-03 2020-05-19 Bayer Pharma Aktiengesellschaft Furane derivatives as inhibitors of ATAD2
WO2017205536A2 (en) * 2016-05-24 2017-11-30 Genentech, Inc. Therapeutic compounds and uses thereof
KR102643344B1 (ko) 2016-06-20 2024-03-07 인사이트 코포레이션 Bet 저해제의 결정질 고체 형태
US20190247302A1 (en) * 2016-10-21 2019-08-15 University Of Miami Materials and methods for treating ophthalmic inflammation
TW201910336A (zh) * 2017-08-08 2019-03-16 大陸商江蘇恆瑞醫藥股份有限公司 一種咪唑并異吲哚類衍生物的製備方法
CN110041253B (zh) * 2018-01-17 2022-03-29 上海翰森生物医药科技有限公司 吡啶类n-氧化衍生物及其制备方法和应用
TWI825085B (zh) * 2018-03-30 2023-12-11 日商協和麒麟股份有限公司 具有抗癌活性之化合物
MY205440A (en) 2018-09-28 2024-10-21 Janssen Pharmaceutica Nv Monoacylglycerol lipase modulators
TW202035409A (zh) 2018-09-28 2020-10-01 比利時商健生藥品公司 單醯基甘油脂肪酶調節劑
AU2019372121A1 (en) 2018-10-30 2021-05-27 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
CN109836385B (zh) * 2019-04-04 2021-12-17 上海翰森生物医药科技有限公司 四氢喹啉类n-氧化衍生物及其制备方法和应用
GB201905721D0 (en) 2019-04-24 2019-06-05 Univ Dundee Compounds
AU2020299592A1 (en) 2019-07-02 2022-02-17 Nuvation Bio Inc. Heterocyclic compounds as BET inhibitors
AU2020358948A1 (en) 2019-09-30 2022-05-26 Janssen Pharmaceutica Nv Radiolabelled MGL PET ligands
TW202126638A (zh) 2019-09-30 2021-07-16 日商協和麒麟股份有限公司 Bet分解劑
BR112022019077A2 (pt) 2020-03-26 2022-12-27 Janssen Pharmaceutica Nv Moduladores da monoacilglicerol lipase
TWI783480B (zh) * 2020-05-27 2022-11-11 美商美國禮來大藥廠 用於抑制cdk7之化合物
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4095128A1 (en) 2021-05-25 2022-11-30 Centre national de la recherche scientifique Tetrahydroquinoline (thq) coumpounds
US12527741B2 (en) 2021-06-17 2026-01-20 Wisconsin Alumni Research Foundation Modular dendron micelles for treatment of pulmonary diseases related to fibrosis and viral infection including COVID-19
WO2023274418A1 (zh) * 2021-07-02 2023-01-05 南京明德新药研发有限公司 蛋白降解靶向嵌合体类化合物
WO2023196512A1 (en) * 2022-04-08 2023-10-12 Plexium, Inc. Propargyl compounds and pharmaceutical compositions that modulate brd4
WO2024073072A1 (en) 2022-09-30 2024-04-04 Bp Asset Iii, Inc. Topical pharmaceutical formulations for bd2-preferential bromodomain and extra terminal inhibitor
WO2025034745A1 (en) * 2023-08-07 2025-02-13 University Of Pittsburgh - Of The Commonwealth System Of Higher Education 4-aminopiperidines as selective modulators of potassium channels

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9004781D0 (en) 1990-03-02 1990-04-25 Glaxo Group Ltd Device
SE0101161D0 (sv) 2001-03-30 2001-03-30 Astrazeneca Ab New compounds
US20050228016A1 (en) 2002-06-13 2005-10-13 Enrique Michelotti Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex
PL376156A1 (en) * 2002-10-04 2005-12-27 Millennium Pharmaceuticals, Inc. Pgd2 receptor antagonists for the treatment of inflammatory diseases
WO2004052863A1 (ja) * 2002-12-06 2004-06-24 Kyowa Hakko Kogyo Co., Ltd. 抗炎症剤
WO2004072042A2 (en) 2003-02-12 2004-08-26 Carex S.A. Quinoline derivative and their use for modulation of lxr activity
WO2005007094A2 (en) 2003-07-09 2005-01-27 Tularik Inc. Asthma and allergic inflammation modulators
CN1901958B (zh) 2003-11-03 2011-03-09 葛兰素集团有限公司 流体分配装置
WO2010110380A1 (ja) * 2009-03-27 2010-09-30 興和株式会社 縮合ピペリジン化合物及びこれを含有する医薬
EP2415764A4 (en) * 2009-03-31 2012-08-08 Kowa Co PROPHYLACTIC AND / OR THERAPEUTIC AGENT AGAINST ANEMIA WITH A TETRAHYDROCHINOLINE COMPOUND AS AN ACTIVE SUBSTANCE
GB0919431D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919434D0 (en) * 2009-11-05 2009-12-23 Glaxosmithkline Llc Novel compounds
GB0919432D0 (en) 2009-11-05 2009-12-23 Glaxosmithkline Llc Use
GB201106743D0 (en) * 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201106750D0 (en) 2011-04-21 2011-06-01 Glaxosmithkline Llc Novel compounds
GB201107325D0 (en) 2011-05-04 2011-06-15 Glaxosmithkline Llc Novel compounds
WO2013027168A1 (en) 2011-08-22 2013-02-28 Pfizer Inc. Novel heterocyclic compounds as bromodomain inhibitors
ES2704048T3 (es) * 2013-03-14 2019-03-14 Glaxosmithkline Ip No 2 Ltd Derivados de 1-acil-4-amino-1,2,3,4-tetrahidroquinolina-2,3-disustituida y su uso como inhibidores de bromodominio

Also Published As

Publication number Publication date
DOP2015000239A (es) 2015-12-15
US20210046073A1 (en) 2021-02-18
PT2970127T (pt) 2019-01-16
BR112015022426A2 (pt) 2017-07-18
SI2970127T1 (sl) 2019-02-28
EP2970127A1 (en) 2016-01-20
US9637456B2 (en) 2017-05-02
CR20150489A (es) 2015-11-20
MY187479A (en) 2021-09-23
MX2015012815A (es) 2016-02-03
EP3511323A1 (en) 2019-07-17
HRP20182179T1 (hr) 2019-02-22
NZ710765A (en) 2020-05-29
JP6530773B2 (ja) 2019-06-12
ES2915658T3 (es) 2022-06-24
ES2704048T3 (es) 2019-03-14
CA2901537A1 (en) 2014-09-18
MX369324B (es) 2019-11-05
SG11201506245QA (en) 2015-09-29
LT2970127T (lt) 2019-02-11
US11478478B2 (en) 2022-10-25
PE20151596A1 (es) 2015-11-24
US10034881B2 (en) 2018-07-31
JP6093046B2 (ja) 2017-03-08
WO2014140076A1 (en) 2014-09-18
ZA201505877B (en) 2021-09-29
US10583139B2 (en) 2020-03-10
KR101780784B1 (ko) 2017-09-21
JP2016510782A (ja) 2016-04-11
IL263354B (en) 2021-09-30
CA2901537C (en) 2021-09-07
IL240463A0 (en) 2015-09-24
US20180303831A1 (en) 2018-10-25
DK2970127T3 (en) 2019-01-28
US20170189401A1 (en) 2017-07-06
PH12015502038A1 (en) 2016-01-18
CL2015002658A1 (es) 2016-08-19
AU2014230815B2 (en) 2016-12-08
IL240463B (en) 2018-12-31
IL263354A (en) 2018-12-31
KR20150132455A (ko) 2015-11-25
CN105189461B (zh) 2018-05-15
RS58264B1 (sr) 2019-03-29
US20230040299A1 (en) 2023-02-09
EP3511323B1 (en) 2022-03-02
EP2970127B1 (en) 2018-10-24
PL2970127T3 (pl) 2019-05-31
SMT201900009T1 (it) 2019-02-28
JP2017125025A (ja) 2017-07-20
EA028174B1 (ru) 2017-10-31
HK1219954A1 (en) 2017-04-21
CY1121095T1 (el) 2019-12-11
HUE043568T2 (hu) 2019-08-28
PH12015502038B1 (en) 2021-06-23
AU2014230815A1 (en) 2015-10-01
CN105189461A (zh) 2015-12-23
US20160016908A1 (en) 2016-01-21
EA201591429A1 (ru) 2016-03-31

Similar Documents

Publication Publication Date Title
PH12015502038B1 (en) 2,3-disubstituted 1 -acyl-4-amino-1,2,3,4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors
CY1125610T1 (el) Παραγωγο κινολινης υψηλης καθαροτητας και μεθοδος για την παρασκευη του
BR112015021983A8 (pt) compostos heterocíclicos, composições e usos dos mesmos
JO3807B1 (ar) مشتقات حمض هيدروكسي جديدة، عملية لتحضيرها وتركيبات صيدلية تحتوي عليها
PH12015502047A1 (en) Novel pyrimidine and pyridine compounds and their usage
PH12014501719A1 (en) Pyridone derivatives
AU2015207757A8 (en) N-azaspirocycloalkane substituted n-heteroaryl compounds and compositions for inhibiting the activity of SHP2
MD20160095A2 (ro) Derivaţi de pirimidiniloxi-benzen utilizaţi ca erbicide
PH12015501933B1 (en) Novel pyridine derivatives
JO3509B1 (ar) معدلات p2x7
PH12018500446A1 (en) Pyridinone dicarboxamide for use as bromodomain inhibitors
GEP20207108B (en) Substituted 2,4 diamino-quinoline as new anticancer agents
MX2016005993A (es) Anfifilos biscationicos y triscationicos como agentes antimicrobianos.
EA201690072A1 (ru) Состав, содержащий гиполипидемическое средство
AU2017269673A1 (en) Pyridine dicarboxamide derivatives as bromodomain inhibitors
PL401473A1 (pl) Nowe, silnie fluorescencyjne substancje heterocykliczne i sposób ich otrzymywania
MX2017003238A (es) Metodo para preparar 2'-o-fucosil-lactosa.
MX2020004842A (es) Compuestos heterociclicos antiinfecciosos y sus usos.
MX2015007309A (es) Derivado de hidantoina.
MX2018016339A (es) Compuestos heterociclicos antiinfecciosos y sus usos.
MX2015010790A (es) Derivados de anilina sustituidos con n-heteroarilo como antivirales de vhc.
PL410423A1 (pl) 4-chloro-2-metylofenoksyoctany alkoksymetylobis(2-hydroksyetylo)metyloamoniowe,  sposób otrzymywania i zastosowanie jako środków  ochrony roślin
MX362994B (es) Preparacion farmaceutica que comprende un derivado de aminopirazol.
EA201591697A1 (ru) Гидрохлоридные соли антибиотического соединения
TH174504A (th) อนุพันธ์ของ 2,3-ไดซับสทิทิวเทด 1-แอซิล-4-อะมิโน-1,2,3,4-เททราไฮโดรควิโนน และการใช้ของมันเป็นตัวยับยั้งโบรโมโดเมน