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AR035838A1 - Compuestos multiciclicos que inhiben la adhesion de leucocitos mediada por vla-4 y el uso de los mismos para la preparacion de un medicamento - Google Patents

Compuestos multiciclicos que inhiben la adhesion de leucocitos mediada por vla-4 y el uso de los mismos para la preparacion de un medicamento

Info

Publication number
AR035838A1
AR035838A1 ARP000100267A ARP000100267A AR035838A1 AR 035838 A1 AR035838 A1 AR 035838A1 AR P000100267 A ARP000100267 A AR P000100267A AR P000100267 A ARP000100267 A AR P000100267A AR 035838 A1 AR035838 A1 AR 035838A1
Authority
AR
Argentina
Prior art keywords
substituted
alkyl
aryl
heteroaryl
heterocyclic
Prior art date
Application number
ARP000100267A
Other languages
English (en)
Original Assignee
Elan Pharm Inc
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 Elan Pharm Inc filed Critical Elan Pharm Inc
Publication of AR035838A1 publication Critical patent/AR035838A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/64—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings
    • C07C233/81—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 carboxyl groups
    • C07C233/82—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 carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/84—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 carboxyl groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom of a saturated carbon skeleton containing rings
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    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
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    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
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Abstract

Compuestos multicíclicos, caracterizados porque comprenden un compuesto de la fórmula (1), en la cual: el anillo A es un cicloalquilo con puente multicíclico, cicloalquenilo con puente multicíclico o grupo heterocíclico con puente multicíclico a condición de que este último no contenga una lactama y además en la cual dicho cicloalquilo con puente multicíclico, cicloalquenilo con puente multicíclico o grupo heterocíclico con puente multicíclico está opcionalmente sustituido, en cualquier anillo con capacidad de sustitución, con 1-3 sustituyentes seleccionados del grupo que consiste de alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, acilo, acilamino, tiocarbonil-amino, aciloxi, amino, amidino, alquil amidino, tioamidino, aminoacilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxi, arilo, arilo sustituido, ariloxi, ariloxi sustituido, ariloxiarilo, ariloxiarilo sustituido, ciano, halógeno, hidroxilo, nitro, carboxilo, carboxialquilo, alquil carboxilo sustituido, carboxil-cicloalquilo, cicloalquilo sustituido con carboxilo, carboxiarilo, arilo sustituido con carboxilo, carboxi heteroarilo, heteroarilo sustituido con carboxilo, carboxilheterocíclico, heterocíclico sustituido con carboxilo, cicloalquilo, cicloalquilo sustituido, guanidino, guanidinosulfona, tiol, tioalquilo, tioalquilo sustituido, tioarilo, tioarilo sustituido, tiocicloalquilo, tiocicloalquilo sustituido, tioheteroarilo, tioheteroarilo sustituido, tioheterocíclico, tioheterocíclico sustituido, heteroarilo, heteroarilo sustituido, heterocíclico sustituido, cicloalcoxi, cicloalcoxi sustituido, heteroariloxi, heteroariloxi sustituido, heterocicliloxi, heterocicliloxi sustituido, oxicarbonilamino, oxitiocarbonilamino, -OS(O)2-alquilo, -OS(O)2-alquilo sustituido, -OS(O)2-arilo, -OS(O)2-arilo sustituido, -OS(O)2-heteroarilo, -OS(O)2-heteroarilo sustituido, -OS(O)2-heterocíclico, -OS(O)2-heterocíclico sustituido, -OSO2-NRR en la cual cada R es independientemente hidrógeno o arilo, -NRS(O)2-alquilo, -NRS(O)2-alquilo sustituido, -NRS(O)2-arilo, -NRS(O)2-arilo sustituido, -NRS(O)2-heteroarilo, -NRS(O)2-heteroarilo sustituido, -NRS(O)2-heterocíclico, -NRS(O)2-heterocíclico sustituido, -NRS(O)2-NR-alquilo, -NRS(O)2-NR-alquilo sustituido, -NRS(O)2-NR-arilo, -NRS(O)2-NR-arilo sustituido, -NRS(O)2-NR-heteroarilo, -NRS(O)2-NR-heteroarilo sustituido, -NRS(O)2-NR-heterocíclico, -NRS(O)2-NR-heterocíclico sustituido en la cual R es hidrógeno o alquilo, -N[S(O)2-R']2 y -N[S(O)2-NR']2 en la cual cada R' está seleccionado independientemente del grupo que consiste de alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocíclico y heterocíclico sustituido, mono- y di- alquilamino, mono- y di-(alquil sustituido)amino, mono- y di-arilamino, mono- y arilamino di- sustituido, mono- y di-heteroarilamino, heteroarilamino mono- y di- sustituido, amino mono- y di-heterocíclico, amino heterocíclico mono- y di- sustituido, aminas di-sustituidas no simétricas que tienen diferentes sustituyentes seleccionados de alquilo, alquilo sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterocíclico y heterocíclico sustituido y grupos alquilo sustituido que tienen grupos amino bloqueados por grupos de bloqueo convencionales tales como Boc, Cbz, formilo, etc., o grupo alquilo/alquilo sustituido sustituidos con -SO2-alquilo, -SO2-alquilo sustituido, -SO2-alquenilo, -SO2-alquenilo sustituido, -SO2-cicloalquilo, -SO2-cicloalquilo sustituido, -SO2-arilo, -SO2-arilo sustituido, -SO2-heteroarilo, -SO2-heteroarilo sustituido, -SO2-heterocíclico, -SO2-heterocíclico sustituido y -SO2-NRR en la cual R es hidrógeno o alquilo; R1 está seleccionado del grupo que consiste de: (a) -CH2)x-Ar-R5 en la cual R5 está seleccionado del grupo que consiste de -O-Z-NR6R6' y -O-Z-R7 en la cual R6 y R6' están seleccionados independientemente del grupo que consiste en hidrógeno, alquilo, alquilo sustituido, cicloalquilo, cicloalquilo sustituido, heterocíclico, heterocíclico sustituido y en la cual R6 y R6' están unidos para formar un heterocíclico o un heterociclo sustituido, R7 está seleccionado del grupo que consiste de heterociclo o heterociclo sustituido, y Z está seleccionado del grupo que consiste de -C(O)- y SO2-, Ar es arilo, heteroarilo, arilo sustituido o heteroarilo sustituido; x es un entero de 1 a 4; y (b) Ar1-Ar2-C1-10 alquilo, Ar1-Ar2-C2-10 alquenilo- y Ar1-Ar2-C2-10 alquinilo, en las cuales Ar1 y Ar2 son independientemente arilo o heteroarilo, cada uno de los cuales está opcionalmente sustituido opcionalmente con 1 a 4 sustituyentes seleccionados independientemente de Rb; alquilo, alquenilo y alquinilo están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados independientemente de Ra; R2 está seleccionado del grupo que consiste de hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, aril C1-10 alquilo, heteroarilo y heteroarilo C1-10 alquilo, en los cuales alquilo, alquenilo y alquinilo están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados de Ra y arilo y heteroarilo están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados independientemente de Rb; R3 está seleccionado del grupo que consiste de hidrógeno, alquilo C1-10 opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente de Ra y Cy opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente de Rb; Ra está seleccionado del grupo que consiste de Cy, -ORd, -NO2, halógeno, -S(O)mRd, -SRd, -S(O)2ORd, -S(O)mNRdRe, -NRdRe, -O(CRfRg)nNRdRe, -C(O)Rd, -CO2Rd, -CO2(CRfRg)nCONRdRc, -OC(O)Rd, -CN, -C(O)NRdRe, -NRdC(O)Re, -OC(O)NRdRe, -NRdC(O)ORe, -NRdC(O)ORe, -NRdC(O)NRdRe, -CRd(N-ORe), CF3 y OCF3; en la cual Cy está opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente de Rc; Rb está seleccionado del grupo que consiste de R, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, aril C1-10 alquilo, heteroarilalquilo C1-10, en los cuales alquilo, alquenilo, arilo, heteroarilo están opcionalmente sustituidos con un grupo seleccionado independientemente de Rc; Rc está seleccionado del grupo que consiste de halógeno, amino, carboxi, alquilo C1-4, alcoxi C1-4, arilo, aril C1-4 alquilo, hidroxi, CF3 y ariloxi; Rd y Re están seleccionados independientemente de hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, Cy y Cy-alquilo C1-10, en los cuales alquilo, alquenilo, alquinilo y Cy están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados independientemente de Rc; o Rd y Re junto con los átomos a los cuales están unidos, forman un anillo heterocíclico con 5 a 7 miembros que contienen 0-2 átomos hetero adicionales seleccionados independientemente de oxígeno, azufre y nitrógeno; Rf y Rg están seleccionados independientemente de hidrógeno, alquilo C1-10, Cy y Cy-alquilo C1-10; o Rf y Fg junto con el átomo al cual están unidos, forman un anillo con 5 a 7 miembros que contienen 0-2 átomos hetero seleccionados independientemente de oxígeno, azufre y nitrógeno; Rh está seleccionado del grupo que consiste de hidrógeno, alquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, aril C1-10 alquilo, heteroarilo, heteroaril C1-10 alquilo, o -SO2Ri en las cuales alquilo, alquenilo y alquinilo están opcionalmente sustituidos con 1 a 4 sustituyentes seleccionados independientemente de Ra; y arilo y heteroarilo están opcionalmente sustituidos cada uno con 1 a 4 sustituyentes seleccionados independientemente de Rb; Ri está seleccionado del grupo que consiste de alquilo C1-10, alquenilo C2-10, alquinilo C2-10 y arilo, en las cuales alquilo, alquenilo, alquinilo y arilo están sustituidos opcionalmente con 1 a 4 sustituyentes seleccionados independientemente de Rc; Cy es cicloalquilo, heterociclilo, arilo o heteroarilo, X1 está seleccionado del grupo que consiste de -C(O)ORd, -P(O)(ORd)(ORe), -P(O)(Rd)(ORe), -S(O)mORd, -C(O)RdRh y 5-tetrazolilo; m es un entero de 1 a 2; n es un entero de 1 a 10; y sus sales farmacéuticamente aceptables. Algunos de estos compuestos inhiben también la adhesión de leucocitos y, en particular, la adhesión de leucocitos mediada por VLA-4. Tales compuestos son útiles en el tratamiento de enfermedades inflamatorias en un paciente mamífero, por ejemplo una persona, tal como asma, enfermedad de Alzheimer, arteriosclerosis, demencia causada por SIDA, diabetes, enfermedad de intestino inflamatorio, artritis reumatoide, transplante de tejido, metástasis tumoral e isquemia en el miocardio. Los compuestos pueden ser administrados también para el tratamiento de enfermedades inflamatorias del cerebro, tal como esclerosis múltiple.
ARP000100267A 1999-01-22 2000-01-21 Compuestos multiciclicos que inhiben la adhesion de leucocitos mediada por vla-4 y el uso de los mismos para la preparacion de un medicamento AR035838A1 (es)

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HUP0103752A3 (en) 1998-04-16 2002-11-28 Texas Biotechnology Corp Houst N,n-disubstituted amides and pharmaceutical compositions containing them that inhibit the binding of integrins to their receptors
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ATE299490T1 (de) 2005-07-15
US7115768B2 (en) 2006-10-03
WO2000043354A3 (en) 2000-11-23
CN1344247A (zh) 2002-04-10
AU3348800A (en) 2000-08-07
EP1144364A2 (en) 2001-10-17
JP2002535304A (ja) 2002-10-22
DE60021251D1 (de) 2005-08-18
US20030134874A1 (en) 2003-07-17
HK1045495A1 (zh) 2002-11-29
US6465513B1 (en) 2002-10-15
US20060074110A1 (en) 2006-04-06
EP1144364B1 (en) 2005-07-13
CA2357781A1 (en) 2000-07-27

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