AR075924A1 - Compuestos de 1,1,1-trifluor-2-hidroxipropilo sustituidos por 2,3-diarilo o por heteroarilo - Google Patents

Compuestos de 1,1,1-trifluor-2-hidroxipropilo sustituidos por 2,3-diarilo o por heteroarilo

Info

Publication number
AR075924A1
AR075924A1 ARP100100926A ARP100100926A AR075924A1 AR 075924 A1 AR075924 A1 AR 075924A1 AR P100100926 A ARP100100926 A AR P100100926A AR P100100926 A ARP100100926 A AR P100100926A AR 075924 A1 AR075924 A1 AR 075924A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
halogen
carboxy
group
Prior art date
Application number
ARP100100926A
Other languages
English (en)
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 AR075924A1 publication Critical patent/AR075924A1/es

Links

Classifications

    • 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
    • C07D413/10—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 carbon chain containing aromatic rings
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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 in position 2
    • C07D235/26—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/54—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D317/46—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D317/48—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
    • C07D317/50—Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to atoms of the carbocyclic ring
    • C07D317/60—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/10—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 carbon chain containing aromatic rings
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D455/00—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine
    • C07D455/02—Heterocyclic compounds containing quinolizine ring systems, e.g. emetine alkaloids, protoberberine; Alkylenedioxy derivatives of dibenzo [a, g] quinolizines, e.g. berberine containing not further condensed quinolizine ring 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)

Abstract

Estos compuestos son antagonistas del receptor de glucocorticoides, utiles para el tratamiento y/o prevencion de enfermedades, por ejemplo la diabetes, la dislipidemia, la obesidad, la hipertension, las enfermedades cardiovasculares, el desequilibrio suprarrenal o la depresion. Reivindicacion 1: Compuestos de la formula general (1) en la que A es C-R1b o N; R1a, R1b, R1c, R1d y R1e con independencia entre sí se eligen entre el grupo formado por hidrogeno, alquilo C1-7, alquenilo C2-7, cicloalquil C3-7-alquilo C1-7, halogeno, halogeno-alquilo C1-7, halogenoalcoxi C1-7, halogeno-alquil C1-7-sulfoniloxi, hidroxi, hidroxi-alquilo C1-7, alcoxi C1-7, alcoxi C1-7-alcoxi C1-7, hidroxi-alcoxi C1-7, amino-alcoxi C1-7, ciano, carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alcoxi C1-7, alcoxi C1-7-carbonilamino-alcoxi C1-7, alquil C1-7-carboniloxi-alcoxi C1-7, aminocarbonil-alcoxi C1-7, di-alquil C1-7-amino, di-alquenil C2-7-amino, alquil C1-7-sulfonil-amino, carboxil-alquil C1-7-aminocarbonilo, fenilo, dicho fenilo está sustituido por un grupo elegido entre carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alcoxi C1-7 y aminocarbonilo, y, además, opcionalmente sustituido por uno o dos sustituyentes elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, y halogeno-alcoxi C1-7, feniloxi, cuyo anillo fenilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7; carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alcoxi C1-7 y aminocarbonilo, heteroarilo elegido entre el grupo formado por piridilo, piridazinilo, pirimidinilo y pirazinilo, dicho heteroarilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7, carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1 7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alcoxi C1-7 y aminocarbonilo; heteroariloxi, cuyo heteroarilo se elige entre el grupo formado por piridilo, piridazinilo, pirimidinilo y pirazinilo, y está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alcoxi C1-7, halogeno-alcoxi C1-7; carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7, alcoxi C1-7-carbonil-alcoxi C1-7 y aminocarbonilo, fenil-alcoxi C1-7, cuyo anillo fenilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por alquilo C1-7, halogeno, halogeno-alquilo C1-7, alquilo C1-7, hidroxi, ciano, alquil C1-7-sulfinilo, alcoxi C1-7, halogeno-alcoxi C1-7; carboxilo, carboxil-alquilo C1-7, carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7, y alcoxi C1-7-carbonil-alcoxi C1-7; y heterociclilo o heterociclilcarbonilo, cuyo heterociclilo se elige entre el grupo formado por pirrolidina, piperidina y azepina y está sustituido por carboxilo, carboxil-alquilo C1-7; carboxil-alcoxi C1-7, alcoxi C1-7-carbonilo, alcoxi C1-7-carbonil-alquilo C1-7 o alcoxi C1-7-carbonil-alcoxi C1-7; R2 se elige entre el grupo formado por alquilo C1-7, cicloalquil C3-7-alquilo C1-7, carboxil-alquilo C1-7, alcoxi C1-7-carbonil-alquilo C1-7, triazolil-alquilo C1-7 y fenilo, dicho fenilo está sin sustituir o sustituido por uno, dos o tres átomos de halogeno; R3 es hidrogeno o alquilo C1-7; o R2 y R3 junto con el átomo de carbono al que están unidos forman un anillo cicloalquilo C3-5; R4 es un anillo heteroarilo elegido entre el grupo formado por 3-oxo-3,4-dihidro-2H-benzo[1,4]oxazinilo, 3,4-dihidro-2H-benzo[1,4]oxazinilo, 2-oxo-2,3-dihidro-1H-pirido[2,3-b]-[1,4]oxazinilo, 4-oxo-4H-quinolizinilo, 2-oxo-2,3-dihidro-1H-benzoimidazoilo, 2-oxo-2,3-dihidro-benzo- oxazolilo, benzo[1,3]dioxolilo, 2-oxo-1,2-dihidro-quinolinilo y 1,3-dimetil-2,2-dioxo-2,3-dihidro-1H-2?6-benzo[1,2,5]-tiadiazolilo, dicho anillo heteroarilo está sin sustituir o sustituido por uno, dos o tres sustituyentes elegidos entre el grupo formado por alquilo C1-7, alquenilo C2-7 y halogeno, o R4 es fenilo sustituido por ciano y, además, está opcionalmente sustituido por uno o dos sustituyentes elegidos entre el grupo formado por halogeno, halogenoalquilo C1-7, alquilo C1-7, alcoxi C1-7 y halogeno-alcoxi C1-7; y R5 es hidrogeno o metilo; o sus sales farmacéuticamente aceptables.
ARP100100926A 2009-03-26 2010-03-23 Compuestos de 1,1,1-trifluor-2-hidroxipropilo sustituidos por 2,3-diarilo o por heteroarilo AR075924A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09156267 2009-03-26

Publications (1)

Publication Number Publication Date
AR075924A1 true AR075924A1 (es) 2011-05-04

Family

ID=42238680

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100926A AR075924A1 (es) 2009-03-26 2010-03-23 Compuestos de 1,1,1-trifluor-2-hidroxipropilo sustituidos por 2,3-diarilo o por heteroarilo

Country Status (15)

Country Link
US (3) US8268820B2 (es)
EP (1) EP2411365B1 (es)
JP (1) JP5547271B2 (es)
KR (1) KR101437720B1 (es)
CN (1) CN102356068B (es)
AR (1) AR075924A1 (es)
AU (1) AU2010227606A1 (es)
BR (1) BRPI1010523A2 (es)
CA (1) CA2754176A1 (es)
ES (1) ES2458352T3 (es)
IL (1) IL214110A0 (es)
MX (1) MX2011009604A (es)
SG (1) SG174570A1 (es)
TW (1) TW201038541A (es)
WO (1) WO2010108903A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2108960A1 (en) 2008-04-07 2009-10-14 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditons modulated by PYY
US8138189B2 (en) * 2009-03-26 2012-03-20 Hoffman-La Roche Inc. Substituted benzene compounds as modulators of the glucocorticoid receptor
CA2918814C (en) * 2013-07-23 2021-10-12 Bayer Pharma Aktiengesellschaft Substituted oxopyridine derivatives and use thereof as factor xia/plasma
US10250799B2 (en) 2014-05-21 2019-04-02 Google Technology Holdings LLC Enhanced image capture
WO2017161518A1 (en) * 2016-03-23 2017-09-28 Astrazeneca Ab New physical form
CN115385765B (zh) * 2022-01-05 2023-11-10 南京工业大学 一种烷基芳基酮的合成方法

Family Cites Families (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0117485A3 (de) 1983-02-28 1985-01-23 F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft Pyridin-, Pyrazin- und Pyrimidinderivate und deren Verwendung als fungizide Wirkstoffe
DK429884A (da) 1983-10-07 1985-04-08 Hoffmann La Roche Heterocycliske forbindelser
US4699652A (en) 1985-07-22 1987-10-13 Hoffmann-La Roche Inc. Fungicidal pyridine derivatives for use in agriculture
AR023656A1 (es) 1998-09-15 2002-09-04 Syngenta Participations Ag Piridincetonas herbicidas, proceso para su preparacion, agentes herbicidas que comprenden estos compuestos y uso de estos agentes para combatir el crecimiento no deseado de plantas
JP3884232B2 (ja) 1999-03-29 2007-02-21 エフ．ホフマン−ラ ロシュ アーゲー グルコキナーゼ活性化物質
AU2003230700A1 (en) 2002-03-26 2003-10-13 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10346939A1 (de) 2003-10-06 2005-05-19 Schering Ag Heterocyclisch substituierte Pentanole, ein Verfahren zu ihrer Herstellung und ihre Verwendung als Entzündungshemmer
US20050090559A1 (en) 2003-07-01 2005-04-28 Markus Berger Heterocyclically-substituted pentanol derivatives, process for their production and their use as anti-inflammatory agents
BRPI0413234A (pt) 2003-08-01 2006-10-03 Genelabs Tech Inc derivados de imidazola bicìclica contra flaviviridae
UY28526A1 (es) 2003-09-24 2005-04-29 Boehringer Ingelheim Pharma Miméticos de glucocorticoides, métodos de preparación composiciones farmacéuticas y usos de los mismos
EP1718653A1 (en) * 2004-02-25 2006-11-08 Ligand Pharmaceuticals Inc. Glucocorticoid receptor modulator compounds and methods- utility
ES2357015T3 (es) * 2004-10-15 2011-04-15 Bayer Healthcare Llc Preparación y uso de derivados bifenil-4-ilcarbonilaminoácido para el tratamiento de la obesidad.
BRPI0611620A2 (pt) 2005-06-10 2009-01-13 Boehringer Ingelheim Int mimÉticos de glicocorticàide, mÉtodos de fazÊ-los, composiÇÕes farmacÊuticas e usos dos mesmos
CN101365722A (zh) * 2005-06-17 2009-02-11 艾兰制药国际有限公司 纯化抗Aβ抗体的方法
CA2623154A1 (en) * 2005-09-30 2007-04-12 Dainippon Sumitomo Pharma Co., Ltd. Novel fused pyrrole derivative
KR20090097908A (ko) * 2006-12-06 2009-09-16 베링거 인겔하임 인터내셔날 게엠베하 글루코코르티코이드 모사물, 이의 제조 방법, 이의 약제학적 조성물 및 용도

Also Published As

Publication number Publication date
CN102356068B (zh) 2014-04-23
EP2411365B1 (en) 2014-03-19
ES2458352T3 (es) 2014-05-05
SG174570A1 (en) 2011-10-28
CA2754176A1 (en) 2010-09-30
KR101437720B1 (ko) 2014-09-03
US20100249124A1 (en) 2010-09-30
EP2411365A1 (en) 2012-02-01
JP5547271B2 (ja) 2014-07-09
BRPI1010523A2 (pt) 2016-03-15
TW201038541A (en) 2010-11-01
KR20110118827A (ko) 2011-11-01
US20130172335A1 (en) 2013-07-04
CN102356068A (zh) 2012-02-15
US8450313B2 (en) 2013-05-28
IL214110A0 (en) 2011-08-31
MX2011009604A (es) 2011-09-28
JP2012521388A (ja) 2012-09-13
US20120232071A1 (en) 2012-09-13
US8268820B2 (en) 2012-09-18
AU2010227606A1 (en) 2011-08-11
WO2010108903A1 (en) 2010-09-30

Similar Documents

Publication Publication Date Title
AR075924A1 (es) Compuestos de 1,1,1-trifluor-2-hidroxipropilo sustituidos por 2,3-diarilo o por heteroarilo
AR079334A1 (es) Derivados de oxazin amino
AR061486A1 (es) Derivados de 2-pirazinacarboxamida
AR054024A1 (es) Derivados de piridina -3- carboxamida como agonistas inversos de cb1
PE20080841A1 (es) Derivados de quinazolinona e isoquinolinona y su uso para el tratamiento o prevencion de trastornos relacionados con el estres o la depresion
AR076170A1 (es) Derivados heterociclicos imidazolicos y/o oxazolicos utiles como agentes antivirales para hepatitis c y composiciones farmaceuticas que los comprenden.
CO6150164A2 (es) Derivados de 2-metilmorfolina pirido-,pirazo-ypirimido-pirimidina como inhibidores de mtor
AR057989A1 (es) Derivados de indol-2-il-amida 1,5-sustituida. procesos de obtencion y composiciones farmaceuticas
AR079224A1 (es) Compuestos insecticidas basados en derivados de isoxazolina
AR058984A1 (es) Derivados de ciclohexil piperazinil metanona
AR076002A1 (es) Derivados imidazolicos heterociclicos utiles como agentes antivirales para hepatitis c y composiciones farmaceuticas que los comprenden.
ES2422299T3 (es) Indoles (4,5-dihidro) indoles tricíclicos
PE20150621A1 (es) Derivados de 2,4-diamino-pirimidina n2, n4-disustituidos como inhibidores de jak3
PE20120764A1 (es) Derivados de isotiazolo-pirimidindiona como moduladores de trpa1
AR049696A1 (es) Derivados de indol
PE20120031A1 (es) Compuestos aril metil benzoquinazolinona como moduladores alostericos positivos del receptor m1
PE20110028A1 (es) Derivados de isoxazol y su uso como potenciadores de los receptores metabotropicos de glutamato
CO6220878A2 (es) Composicion herbicida que comprende un derivado de isoxazolina o una sal del mismo
CU24375B1 (es) Derivados de pirazol fusionados activos como moduladores del receptor de farnesoide x
PE20121158A1 (es) Derivados de feniletinilo como moduladores alostericos positivos (map)
AR075597A1 (es) Derivados de indol como antagonistas de receptores crth2, composiciones farmaceuticas que los contienen y uso de los mismos para el tratamiento del asma y otras enfermedades alergicas .
PE20211240A1 (es) Inhibidores de endonucleasa cap-dependientes
AR072166A1 (es) Derivado de piperidina y su uso como inhibidor de renina superior
AR049331A1 (es) Derivados de imidazopiridinas, imidazoquinolinas e iimidazonaftiridinas sustituidas con amidas como moduladores de biosintesis de citoquinas. composiciones farmaceuticas.
AR049652A1 (es) Sales cuaternarias antagonistas del receptor ccr2

Legal Events

Date Code Title Description
FB Suspension of granting procedure