AR049386A1 - Mercaptoimidazoles como antagonistas del receptor ccr2 - Google Patents

Mercaptoimidazoles como antagonistas del receptor ccr2

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Publication number
AR049386A1
AR049386A1 ARP050102147A ARP050102147A AR049386A1 AR 049386 A1 AR049386 A1 AR 049386A1 AR P050102147 A ARP050102147 A AR P050102147A AR P050102147 A ARP050102147 A AR P050102147A AR 049386 A1 AR049386 A1 AR 049386A1
Authority
AR
Argentina
Prior art keywords
alkyl
amino
alkyloxy
mono
polyhalo
Prior art date
Application number
ARP050102147A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34957884&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR049386(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR049386A1 publication Critical patent/AR049386A1/es

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    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C07C211/29—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring the carbon skeleton being further substituted by halogen atoms or by nitro or nitroso groups
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Abstract

La presente se refiere a compuestos derivados de mercaptoimidazoles, un N-oxido, una sal de dicion farmacéuticamente aceptable, una amina cuaternaria, una forma polimorfica o una forma estereoquímicamente isomérica del mismo. La presente también se refiere a procesos para preparar los compuestos, su uso como antagonitas del receptor CCR2 y las composiciones farmacéuticas que los compende. Reivindicacion 1: Un compuesto de formula (1), un N-oxido, una sal de adicion farmacéuticamente aceptable, una amina cuaternaria, una forma polimorfica o una forma estereoquímicamente isomérica del mismo, en donde: R1 representa H, alquilo C1-6, cicloalquilo C3-7, alquiloxi C1-6-alquilo C1-6, di(alquil C1-6)amino-alquilo C1-6, arilo o heteroarilo; cada R2 representa independientemente halo, alquilo C1-6, alquiloxilo C1-6, alquiltio C1-6, polihalo-alquilo C1-6, polihalo-alquiloxilo C1-6, ciano, aminocarbonilo, amino, mono- o di(alquil C1-4)amino, nitro,a rilo o ariloxilo; R3 representa H, ciano, alquilo C1-6 opcionalmente sustituido con hidroxilo o alquiloxilo C1-6, C(=O)-O-R5, C(=O)-NR6aR6b, C(=S)-NR6aR6b, S(=O)2-NR6aR6b o C(=O)-R7; R4 representa H o alquilo C1-6; R5 representa H, alquilo C1-6, hidroxi-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, polihalo-alquilo C1-6, alquiloxi C1-6-alquilo C1-6, amino-alquilo C1-6, mono- o di(alquil C1-4)amino-alquilo C1-6, aminocarbonilalquilo C1-6, mono- o di(alquil C1-4)aminocarbonilalquilo C1-6 o arilo; R6a y R6b cada uno repesenta independientemente H, alquilo C1-6, amino, mono- o di(alquil C1-4)amino, ariloNH-, amino-alquilo C1-6, mono- o di(alquil C1-4)amino-alquilo C1-6, alquil C1-6carbonilamino, aminocarbonilamino, alquiloxilo C1-6, carbonilamino o hidroxi- alquilo C1-6; o R6a y R6b tomados en forma conjunta con el N al cual están ligados forman pirrolidinilo, imidazolidinilo, pirazolidinilo, piperidinilo, piperazinilo, morfolinilo, tiomorfolinilo o piperazinilo sustituido con alquilo C1-6; r7 representa H, alquilo C1-6, hidroxi-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, polihalo-alquilo C1-6, alquiloxi C1-6-alquilo C1-6, amino-alquilo C1-6, mono- o di(alquil C1-4)amino-alquilo C1-6, aminocarbonilalquilo C1-6, mono- o di(alquil C1- 4)aminocarbonilalquilo C1-6, arilo o heteroarilo; Z representa un sistema anular cíclico seleccionado entre los restos de formulas (2); cada R8 representa independientemente H, halo, alquilo C1-6, alquiloxilo C1-6, polihalo-alquilo C1-6, polihalo- alquiloxilo C1-6, ciano, aminocarbonilo, mono- o di(alquil C1-4)aminocarbonilo, amino, mono- o di(alquil C1-4)amino, hidroxi-alquil C1-6-amino, arilo, ariloxilo, piperidinilo, piperidinilamino, morfolinilo, piperazinilo o nitro; cada R9 representa independientemente H, halo o alquilo C1-6; n es 1, 2, 3, 4 o 5; arilo representa fenilo o fenilo sustituido con uno, dos, tres, cuatro o cinco sustituyentes cada uno seleccionado independientemente entre halo, alquilo C1-6, alquiloxilo C1-6, polihalo-alquilo C1-6, polihalo-alquiloxilo C1-6, ciano, aminocarbonilo, mono- o di(alquil C1-4)aminocarbonilo, amino, mono- o di(alquil C1-4)amino,feniloxilo o nitro; heteroarilo representa furanilo, tienilo, pirrolilo, oxazolilo, tiazolilo, imidazolilo, pirazolilo, isoxazolilo, isotiazolilo, oxadiazolilo, triazolilo, tiadiazolilo, piridilo, piridazinilo, pirimidinilo, pirazinilo, estando cada uno de dichos heterociclos opcionalmente sustituido con uno o dos sustituyentes cada uno seleccionado independientemente entre halo, alquilo C1-6, alquiloxilo C1-6, polihalo-alquilo C1-6, polihalo-alquiloxilo C1-6, ciano, aminocrbonilo, mono- o di(alquil C1-4)aminocarbonilo, amino, mono- o di(alquil C1-4)amino o nitro; con la condicion de que no se incluyan ni 1-(3,4-dimetoxibenzil)-4-fenil-1H-imidazol-2-tiol; ni 1-(o-clorobenzil)-5-etil-4-fenil-imidazol-2-tiol.
ARP050102147A 2004-05-26 2005-05-24 Mercaptoimidazoles como antagonistas del receptor ccr2 AR049386A1 (es)

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US20070244138A1 (en) * 2004-05-26 2007-10-18 Janssen Pharmaceutica N.V. Mercaptoimidazoles as Ccr2 Receptor Antagonists
ES2764840T3 (es) 2015-01-28 2020-06-04 Univ Bordeaux Uso de plerixafor para tratar y/o prevenir exacerbaciones agudas de la enfermedad pulmonar obstructiva crónica
US10682344B2 (en) * 2016-06-03 2020-06-16 Chemocentryx, Inc. Method of treating liver fibrosis
EP3833762A4 (en) 2018-08-09 2022-09-28 Verseau Therapeutics, Inc. OLIGONUCLEOTIDE COMPOSITIONS FOR TARGETING CCR2 AND CSF1R AND THEIR USES
WO2020207263A1 (zh) * 2019-04-08 2020-10-15 四川科伦博泰生物医药股份有限公司 苯并咪唑化合物、其制备方法及其用途

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FR1487326A (fr) 1966-01-18 1967-07-07 Clin Byla Ets Dérivés imidazoliques et leur préparation
JPS5343958B2 (es) 1972-07-29 1978-11-24
US4770689A (en) * 1986-03-10 1988-09-13 Janssen Pharmaceutica N.V. Herbicidal imidazole-5-carboxylic acid derivatives
DE10107683A1 (de) 2001-02-19 2002-08-29 Merckle Gmbh Chem Pharm Fabrik 2-Thio-substituierte Imidazolderivate und ihre Verwendung in der Pharmazie
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BRPI0511599A (pt) 2008-01-02
TW200606154A (en) 2006-02-16
CN1956980A (zh) 2007-05-02
EA200602193A1 (ru) 2007-04-27
US20070249691A1 (en) 2007-10-25
WO2005118578A1 (en) 2005-12-15
JP2008500310A (ja) 2008-01-10
PA8634401A1 (es) 2006-05-16
ZA200609846B (en) 2008-07-30
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ATE425161T1 (de) 2009-03-15
EP1753758B1 (en) 2009-03-11
MXPA06013764A (es) 2007-02-08
NO20066011L (no) 2007-02-23
CA2566187A1 (en) 2005-12-15
IL179518A0 (en) 2007-05-15

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