AR049652A1 - Sales cuaternarias antagonistas del receptor ccr2 - Google Patents
Sales cuaternarias antagonistas del receptor ccr2Info
- Publication number
- AR049652A1 AR049652A1 ARP050102614A ARP050102614A AR049652A1 AR 049652 A1 AR049652 A1 AR 049652A1 AR P050102614 A ARP050102614 A AR P050102614A AR P050102614 A ARP050102614 A AR P050102614A AR 049652 A1 AR049652 A1 AR 049652A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- aryl
- lower alkyl
- optionally substituted
- alkoxycarbonyl
- Prior art date
Links
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- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
- C07C233/80—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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- C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
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- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
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Abstract
Formas farmacéuticamente aceptables de los mismos, que son antagonistas de CCR2 y son utiles para prevenir, tratar o mejorar los síndromes, trastornos o enfermedades en un sujeto que lo necesita. Reivindicacion 1: Un compuesto de formula (1), y formas farmacéuticamente aceptables del mismo, en la cual: A es carbonilo, tiocarbonilo o sulfonilo; X es un enlace o -CH=CH-; R1 está seleccionado de: a) arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, alcoxicarbonilo, ciano, halogeno o fenilo opcionalmente sustituido con alquilo inferior, -(CH2)n-CF3, alcoxi inferior, alcoxicarbonilo, ciano o halogeno; b) cicloalquilo C5-15 opcionalmente sustituido con uno o más de alquilo inferior, - (CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; o c) heterociclilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilalquilo inferior, arilo halogeno- sustituido, alcoxicarbonilo, ciano o halogeno; n es 0, 1, 2, 3 o 4; Y es un enlace o -CH2-; X2 es -(CH2)m- donde m es 1 o 2; R2 es -N+(R4R5)-ZR3; Z es -(CH2)p- donde p es 0, 1 o 2; R3 está seleccionado de: a) arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; b) cicloalquilo C5-15 opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; o c) heterociclilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno-sustituido, alcoxicarbonilo, ciano o halogeno; donde cuando el heterociclilo está unido a través de un miembro de anillo de átomo de carbono y un miembro de anillo heteroátomico es adyacente a dicho átomo de carbono, entonces p es 1 o 2; R4 y R5, son cada uno individualmente alquilo inferior o alquenilo inferior; alternativamente, R4 y R5 se combinan con el átomo de nitrogeno de formula (1) para formar un anillo heterociclilo de 5 a 9 átomos de anillo en total, que contienen opcionalmente un átomo del anillo, de oxígeno o azufre, donde el átomo de nitrogeno del anillo heterociclilo está sustituido con uno de alquilo inferior o alquenilo inferior para formar una sal cuaternaria, y donde -ZR3 está ausente y el anillo heterociclilo está opcionalmente sustituido con arilo opcionalmente sustituido con uno o más de alquilo inferior, -(CH2)n-CF3, alcoxi inferior, arilo, arilo halogeno sustituido, alcoxicarbonilo, ciano o halogeno.
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JP (1) | JP5137572B2 (es) |
KR (1) | KR101229416B1 (es) |
CN (1) | CN101010312B (es) |
AR (1) | AR049652A1 (es) |
AU (1) | AU2005267385B2 (es) |
BR (1) | BRPI0512623A (es) |
CA (1) | CA2571587C (es) |
EA (1) | EA012784B1 (es) |
EC (1) | ECSP067116A (es) |
ES (1) | ES2573845T3 (es) |
IL (1) | IL180197A0 (es) |
MX (1) | MX2007000036A (es) |
NI (1) | NI200600319A (es) |
NO (1) | NO20070387L (es) |
NZ (1) | NZ552173A (es) |
TW (1) | TWI407957B (es) |
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NI200600319A (es) | 2007-08-22 |
JP2008512348A (ja) | 2008-04-24 |
WO2006012135A1 (en) | 2006-02-02 |
TW200612934A (en) | 2006-05-01 |
CN101010312B (zh) | 2011-04-20 |
EA012784B1 (ru) | 2009-12-30 |
KR20070039062A (ko) | 2007-04-11 |
IL180197A0 (en) | 2007-06-03 |
ZA200700677B (en) | 2008-09-25 |
UA85597C2 (ru) | 2009-02-10 |
AU2005267385A1 (en) | 2006-02-02 |
MX2007000036A (es) | 2007-05-18 |
US7799824B2 (en) | 2010-09-21 |
ECSP067116A (es) | 2007-01-26 |
ES2573845T3 (es) | 2016-06-10 |
CN101010312A (zh) | 2007-08-01 |
BRPI0512623A (pt) | 2008-03-25 |
NO20070387L (no) | 2007-03-20 |
EP1765803B1 (en) | 2016-03-09 |
EA200700116A1 (ru) | 2007-06-29 |
US20060293379A1 (en) | 2006-12-28 |
JP5137572B2 (ja) | 2013-02-06 |
CA2571587C (en) | 2013-02-12 |
CA2571587A1 (en) | 2006-02-02 |
EP1765803A1 (en) | 2007-03-28 |
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