AR063945A1 - Acidos carboxilicos inhibidores de la metalproteinasa matriz. - Google Patents

Acidos carboxilicos inhibidores de la metalproteinasa matriz.

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Publication number
AR063945A1
AR063945A1 ARP070103738A ARP070103738A AR063945A1 AR 063945 A1 AR063945 A1 AR 063945A1 AR P070103738 A ARP070103738 A AR P070103738A AR P070103738 A ARP070103738 A AR P070103738A AR 063945 A1 AR063945 A1 AR 063945A1
Authority
AR
Argentina
Prior art keywords
nhc
nr4r5
aralkyl
heteroaryl
cycloalkyl
Prior art date
Application number
ARP070103738A
Other languages
English (en)
Inventor
Venkata P Palle
Ranadheer Rddy
Manoj Kumar Khera
Manoj Kumar Tiwari
Viswajanani J Sattigeri
Sunanda G Dastidar
Punit Kumar Srivastava
Original Assignee
Ranbaxy Lab Ltd
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 Ranbaxy Lab Ltd filed Critical Ranbaxy Lab Ltd
Publication of AR063945A1 publication Critical patent/AR063945A1/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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Abstract

La presente se relaciona con ácidos carboxílicos sustituidos mediante beta-hidroxi y amino, que actuan como inhibidores de la metaloproteasa matriz, ácidos carboxílicos beta-hidroxi diastereoméricamente puros, procesos correspondientes para la síntesis de composiciones farmacéuticas que contienen los compuestos de la presente. Los compuestos de la presente son utiles en el tratamiento de diversas enfermedades inflamatorias, de autoinmunidad y alérgicas, como ser los métodos para tratar el asma, la artritis reumatoidea, COPD, rinitis, osteoartritis, artritis soriásica, psoriasis, fibrosis pulmonar, desordenes en la cura de heridas, inflamacion pulmonar, síndrome de perturbacion respiratoria agudo, periodontitis, esclerosis multiple, gingivitis, ateroesclerosis, proliferacion neoíntima, que lleva a la restenosis y a la insuficiencia cardiaca isquémica, ataque apopléjico, enfermedades renales, metástasis tumoral y otros desordenes inflamatorios caracterizados por la hiper- expresion e hiper-activacion de una rnetaloproteinasa matriz utilizando los compuestos. Reivindicacion 1: Un compuesto de la formula 1, en donde: * representa un centro asimétrico estereogénico de configuracion definida seleccionada de (R, R), (S, S), (R, S) y (S, R); n es un entero de 1 a 5; R1 es hidrogeno, alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, heteroarilo, aralquilo, alcoxi, ariloxi, alqueniloxi o alquiniloxi opcionalmente sustituido; R2 es heterociclilo, heteroarilo, NR4R5, -NHC(=Y)R4, -NHC(=Y)NR5Rx, -NHC(=O)OR4 , -NHSO2R4, C(=Y)NR4R5, C(=O)OR6, en donde; Y es oxígeno o azufre, OR5,-OC(=O)NR4R5, O-acilo, S(O)mR4, -SO2N(R4)2, ciano, amidino o guanidino; Rx es R4 o -SO2N(R4)2; R6 es hidrogeno, alquilo, cicloalquilo, aralquilo, heteroarilalquilo, heterociclilalquilo o cicloalquilalquilo en donde R4 es alquilo, alquenilo, alquinilo, cicloalquilo, arilo, heterociclilo, heteroarilo, aralquilo, heteroarilalquilo, heterociclilalquilo o cicloalquilalquilo; y m es un entero 0-2; R5 es H o R4; R3 es H, F, alquilo, cicloalquilalquilo o aralquilo; A es OH, OR4, -OC(=O)NR4R5, O-acilo, NH2, NR4R5, -NHC(=Y)R4, -NHC(=Y)NR5Rx, -NHC(=O)OR4, -NHSO2R4; Q es arilo o heteroarilo opcionalmente sustituido.
ARP070103738A 2006-08-22 2007-08-22 Acidos carboxilicos inhibidores de la metalproteinasa matriz. AR063945A1 (es)

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