AR111524A1 - Compuestos bicíclicos como inhibidores de atx - Google Patents

Compuestos bicíclicos como inhibidores de atx

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Publication number
AR111524A1
AR111524A1 ARP180100600A ARP180100600A AR111524A1 AR 111524 A1 AR111524 A1 AR 111524A1 AR P180100600 A ARP180100600 A AR P180100600A AR P180100600 A ARP180100600 A AR P180100600A AR 111524 A1 AR111524 A1 AR 111524A1
Authority
AR
Argentina
Prior art keywords
alkyl
substituted
cycloalkyl
alkoxy
groups consisting
Prior art date
Application number
ARP180100600A
Other languages
English (en)
Inventor
Giorgio Patrick Di
Petra Schmitz
Markus Rudolph
Patrizio Mattei
Daniel Hunziker
Jrme Hert
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR111524A1 publication Critical patent/AR111524A1/es

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Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2009—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2095—Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/485—Inorganic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4858—Organic compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841—Filling excipients; Inactive ingredients
    • A61K9/4866—Organic macromolecular compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D405/14—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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composiciones que incluyen los compuestos y métodos de uso de los compuestos. Reivindicación 1: Compuestos de fórmula (1) y (2) en la que R¹ se selecciona entre los grupos que consisten en i) fenilo sustituido con R³, R⁴ y R⁵, ii) fenil-alquilo C₁₋₆ sustituido con R³, R⁴ y R⁵, iii) fenoxi-alquilo C₁₋₆ sustituido con R³, R⁴ y R⁵, iv) fenil-alquenilo C₂₋₆ sustituido con R³, R⁴ y R⁵, v) fenil-alquinilo C₂₋₆ sustituido con R³, R⁴ y R⁵, vi) piridinilo sustituido con R³, R⁴ y R⁵, vii) piridinil-alquilo C₁₋₆ sustituido con R³, R⁴ y R⁵, viii) piridinil-alquenilo C₂₋₆ sustituido con R³, R⁴ y R⁵, ix) piridinil-alquinilo C₂₋₆ sustituido con R³, R⁴ y R⁵, x) tiofenilo sustituido con R³, R⁴ y R⁵, xi) tiofenil-alquilo C₁₋₆ sustituido con R³, R⁴ y R⁵, xii) tiofenil-alquenilo C₂₋₆ sustituido con R³, R⁴ y R⁵, y xiii) tiofenil-alquinilo C₂₋₆ sustituido con R³, R⁴ y R⁵; Y se selecciona entre los grupos que consisten en i) -OC(O)-, y ii) -C(O)-; A se selecciona entre los grupos que consisten en i) -O-, y ii) -S-; X se selecciona entre los grupos que consisten en i) -N-, y ii) -CH-; W se selecciona entre los grupos que consisten en i) -C(O)-, y ii) -S(O)₂-; R² se selecciona entre los sistemas de anillos O, AO, AW, AX, AY y AZ del grupo de fórmulas (3); R³ se selecciona entre los grupos que consisten en i) halógeno, ii) hidroxi, iii) ciano, alquilo C₁₋₆, iv) alcoxi C₁₋₆, v) alcoxi C₁₋₆-alquilo C₁₋₆, vi) halo-alcoxi C₁₋₆, vii) halo-alquilo C₁₋₆, viii) hidroxi-alquilo C₁₋₆, ix) cicloalquilo C₃₋₈, x) cicloalquil C₃₋₈-alquilo C₁₋₆, xi) cicloalquil C₃₋₈-alcoxi C₁₋₆, xii) cicloalcoxi C₃₋₈, xiii) cicloalcoxi C₃₋₈-alquilo C₁₋₆, xiv) alquil C₁₋₆amino, xv) alquil C₁₋₆carbonilamino, xvi) cicloalquil C₃₋₈carbonilamino, xvii) alquil C₁₋₆tetrazolilo, xviii) alquil C₁₋₆tetrazolil-alquilo C₁₋₆, y xix) heterocicloalquil-alcoxi C₁₋₆; R⁴ y R⁵ se seleccionan independientemente entre los grupos que consisten en i) H, ii) halógeno, iii) hidroxi, iv) ciano, v) alquilo C₁₋₆, vi) alcoxi C₁₋₆, vii) alcoxi C₁₋₆-alquilo C₁₋₆, viii) halo-alcoxi C₁₋₆, ix) halo-alquilo C₁₋₆, x) hidroxi-alquilo C₁₋₆, xi) cicloalquilo C₃₋₈, xii) cicloalquil C₃₋₈-alquilo C₁₋₆, xiii) cicloalquil C₃₋₈-alcoxi C₁₋₆, xiv) cicloalcoxi C₃₋₈, xv) cicloalcoxi C₃₋₈-alquilo C₁₋₆, xvi) alquil C₁₋₆carbonilamino, xvii) cicloalquil C₃₋₈carbonilamino, xviii) alquil C₁₋₆tetrazolilo, xix) alquil C₁₋₆tetrazolil-alquilo C₁₋₆, y xx) heterocicloalquil-alcoxi C₁₋₆; R⁶ se selecciona entre los grupos que consisten en i) H, ii) alquilo C₁₋₆, y iii) cicloalquilo C₃₋₈; m y n se seleccionan independientemente entre 1, 2 y 3; r es 1, 2 ó 3; o sales farmacéuticamente aceptables.
ARP180100600A 2017-03-16 2018-03-15 Compuestos bicíclicos como inhibidores de atx AR111524A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP17161254 2017-03-16

Publications (1)

Publication Number Publication Date
AR111524A1 true AR111524A1 (es) 2019-07-24

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ID=58347252

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180100600A AR111524A1 (es) 2017-03-16 2018-03-15 Compuestos bicíclicos como inhibidores de atx

Country Status (7)

Country Link
US (2) US10882857B2 (es)
EP (1) EP3596060B1 (es)
JP (1) JP7090099B2 (es)
CN (1) CN110382484B (es)
AR (1) AR111524A1 (es)
TW (1) TW201840552A (es)
WO (1) WO2018167113A1 (es)

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