PE20171649A1 - ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T - Google Patents

ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T

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Publication number
PE20171649A1
PE20171649A1 PE2017000795A PE2017000795A PE20171649A1 PE 20171649 A1 PE20171649 A1 PE 20171649A1 PE 2017000795 A PE2017000795 A PE 2017000795A PE 2017000795 A PE2017000795 A PE 2017000795A PE 20171649 A1 PE20171649 A1 PE 20171649A1
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PE
Peru
Prior art keywords
gamma
alkyl
compounds
formula
ror
Prior art date
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PE2017000795A
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English (en)
Inventor
Hariharan Venkatesan
Virginia Tanis
Olaf Kinzel
Christian Gege
Christoph Steeneck
Gerald Kleymann
Thomas Hoffmann
Steven Goldberg
Anne M Fourie
Xiaohua Xue
Original Assignee
Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20171649A1 publication Critical patent/PE20171649A1/es

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    • 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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
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    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • A61K31/425—Thiazoles
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    • 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
    • A61K31/44—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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    • A61K31/435—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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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    • 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
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • C07D495/10—Spiro-condensed systems

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  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
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Abstract

Referida a un compuesto de formula I, donde: X es CH, CR1 o N; A1 es alquilo C1-C2; A2 es ciclobutilo o alquilo C1-C4 opcionalmente sustituido o A1 y A2 juntos con el nitrogeno al que estan unidos forman un anillo azetidinilo, piperidinilo, entre otros; R1 es Cl, C(CH3)3, entre otros; R2 es H, F o Cl, o R1 y R2 juntos con el fenilo al que estan unidos forman un grupo naftalenilo o quinolinilo; R3 es CF3 o CH2CH3; A3 es H; A4 es H, alquilo C1-C5, entre otros. Son compuestos preferidos los compuestos de formula i), ii), iii), entre otros. Tambien se refiere a una composicion farmaceutica y a un procedimiento de obtencion. Dichos compuestos son moduladores del receptor nuclear ROR(gamma)t, siendo utiles en el tratamiento de enfermedades inflamatorias, artritis reumatoide, soriasis, entre otros.
PE2017000795A 2014-10-30 2015-10-30 ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T PE20171649A1 (es)

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US201462072563P 2014-10-30 2014-10-30

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PE20171649A1 true PE20171649A1 (es) 2017-11-13

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PE2017002473A PE20180250A1 (es) 2014-10-30 2015-10-30 ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE RORyT
PE2017000795A PE20171649A1 (es) 2014-10-30 2015-10-30 ALCOHOLES TRIFLUOROMETILICOS COMO MODULADORES DE ROR(gamma)T

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US (2) US9850236B2 (es)
EP (2) EP3354651B1 (es)
JP (3) JP6998204B2 (es)
KR (2) KR20170078750A (es)
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CN112292373A (zh) 2018-06-18 2021-01-29 詹森药业有限公司 作为RORγt的调节剂的吡啶基吡唑类
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