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PE20160992A1 - Inhibidores de quinasa relacionada con la tropomiosina (trk) - Google Patents

Inhibidores de quinasa relacionada con la tropomiosina (trk)

Info

Publication number
PE20160992A1
PE20160992A1 PE2016000760A PE2016000760A PE20160992A1 PE 20160992 A1 PE20160992 A1 PE 20160992A1 PE 2016000760 A PE2016000760 A PE 2016000760A PE 2016000760 A PE2016000760 A PE 2016000760A PE 20160992 A1 PE20160992 A1 PE 20160992A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
tropomyosin
halo
cycloalkyl
Prior art date
Application number
PE2016000760A
Other languages
English (en)
Inventor
John L Kane Jr
Michael Kothe
Andrew Scholte
Gloria Matthews
Markus Metz
Jinyu Liu
Original Assignee
Genzyme Corp
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 Genzyme Corp filed Critical Genzyme Corp
Publication of PE20160992A1 publication Critical patent/PE20160992A1/es

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    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se refiere a compuestos de Formula (I) y sales farmaceuticamente aceptables de los mismos, donde n es 1, 2, 3, 4 o 5; m es 0, 1, 2, 3 o 4; Q1 es H, halo, arilo C6–C14, entre otros; Q2 es arilo C6–C14, cicloalquilo C3–C10, entre otros; X es CH o N, entre otros; R1 es H, halo, alquilo C1–C10, NH2, entre otros; R2 es H, halo, alquilo C1–C10, NH2, entre otros; R3 y R4 son independientemente H, alquilo C1–C10, O–alquilo C1–C10, NH2, entre otros; o –CR3R4 forman un anillo de 3 a 10 miembros, opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre alquilo C1–C10, cicloalquilo C3–C10, OH, NH2, entre otros; R5 y R6 son independientemente H, alquilo C1–C10, O–alquilo C1–C10, NH2, entre otros; o –CR5R6 forman un anillo de 3 a 10 miembros, opcionalmente sustituido con 1 a 4 sustituyentes seleccionados entre alquilo C1–C10, cicloalquilo C3–C10, OH, NH2, entre otros. Dichos compuestos son inhibidores de quinasa relacionada con la tropomiosina (inhibidores de Trk), por lo cual son utiles en el tratamiento de enfermedades inflamatorias, enfermedades autoinmunes, defectos del metabolismo oseo y cancer
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