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
Application number
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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    • A61K31/395—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
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • C—CHEMISTRY; METALLURGY
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    • C07D417/02—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
    • 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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    • A61K31/395—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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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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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    • A61K31/395—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
    • A61K31/44—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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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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    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • 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
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    • 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
    • C07D495/10—Spiro-condensed systems

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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

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

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US (2) US9850236B2 (es)
EP (2) EP3212643B1 (es)
JP (3) JP6998204B2 (es)
KR (2) KR20170127580A (es)
CN (3) CN107108599A (es)
AR (2) AR102480A1 (es)
AU (2) AU2015339087B2 (es)
BR (2) BR122017023050A2 (es)
CA (1) CA2965512C (es)
CL (3) CL2017001042A1 (es)
CO (1) CO2017005014A2 (es)
CR (2) CR20170166A (es)
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EC (1) ECSP17033054A (es)
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LT (1) LT3212643T (es)
MA (1) MA40873B1 (es)
ME (1) ME03426B (es)
MX (2) MX369567B (es)
PE (2) PE20171649A1 (es)
PH (2) PH12017500800A1 (es)
PL (1) PL3212643T3 (es)
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RS (1) RS58613B1 (es)
SG (2) SG11201703323PA (es)
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KR20210060367A (ko) 2018-03-12 2021-05-26 에스칼리에 바이오사이언시스, 비브이 스피로사이클릭 ror-감마 조절제
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JP2021527660A (ja) 2018-06-18 2021-10-14 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγｔのモジュレータとしてのフェニル及びピリジニル置換イミダゾール
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JP2021528398A (ja) 2018-06-18 2021-10-21 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγＴのモジュレーターとしての６−アミノピリジン−３−イルピラゾール
ES2925473T3 (es) 2018-06-18 2022-10-18 Janssen Pharmaceutica Nv Pirazoles de piridinilo como moduladores de RORyt
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