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PE20170682A1 - Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias - Google Patents

Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias

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Publication number
PE20170682A1
PE20170682A1 PE2017000167A PE2017000167A PE20170682A1 PE 20170682 A1 PE20170682 A1 PE 20170682A1 PE 2017000167 A PE2017000167 A PE 2017000167A PE 2017000167 A PE2017000167 A PE 2017000167A PE 20170682 A1 PE20170682 A1 PE 20170682A1
Authority
PE
Peru
Prior art keywords
halogen
metabolic
inflammatory
useful
treatment
Prior art date
Application number
PE2017000167A
Other languages
English (en)
Inventor
Glad Sanne Ormholt Schrøder
Jensen Kim Birkebaek
Nørager Niels Henrik Grøn
Ian David Sarvary
Mikkel Vestergaard
Gouliaev Alex Haahr
Lene Teuber
Luigi Piero Stasi
Original Assignee
Nuevolution As
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 Nuevolution As filed Critical Nuevolution As
Publication of PE20170682A1 publication Critical patent/PE20170682A1/es

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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—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
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

Se refiere a un derivado de pirimidina sustituido con heterociclilo opcionalmente condensado de formula (I) o las sales, hidratos, solvatos, polimorfos y estereoisomeros de los mismos, donde: Y es NR u O; R es H o alquilo C1-C4 opcionalmente sustituido; R1 es H, -OH, entre otros; R2 es H, halogeno, entre otros; R3 es hidogeno, halogeno, entre otros; R4a es H, halogeno, entre otros; R4b es H, halogeno, oxo, entre otros; R5 es (CR8R9)pOR12, entre otros; m, n y p son enteros de 0 a 4; R6a y R6b son H, halogeno, alquilo C1-C6 opcionalmente sustituido, entre otros; R8, R9 y R12 son H, alquilo C1-C6 opcionalmente sustituido, entre otros; B es un sistema de anillo tal como arilo, heteroarilo, entre otros; C es un sistema de anillo entre heteroaliciclilo C2-C9 en el que B esta unido a un atomo de carbono adyacente al N del sistema de anillo C; se exceptua el compuesto (i). Entre los compuestos preferidos tenemos los siguientes: (2R)-4,4-dimetil-2-[[6-[2-[4-(trifluorometil)fenil]pirrolidin-1-il]pirimidin-4-il]amino]pentanamida; (2R)-2-[[5-fluoro-2-(trifluorometil)-6-[2-[4-trifluorometil)fenil]pirrolidin-1-il]pirimidin-4-il]amino]-4,4-dimetil-pentanamida; entre otros. Estos compuestos modulan la actividad de un receptor huerfano relacionado con el receptor de acido retinoico (ROR). Tambien se refiere a una composicion. Dicho compuesto es util en el tratamiento de enfermedades inflamatorias, metabolicas y autoinmunes
PE2017000167A 2014-08-04 2015-07-31 Derivados de pirimidina sustituidos con heterociclilo opcionalmente condensados utiles para el tratamiento de enfermedades inflamatorias, metabolicas, oncologicas y autoinmunitarias PE20170682A1 (es)

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